Alti-Pindolol

Generic Name: pindolol (Oral route)

PIN-doe-lol

Commonly used brand name(s)

In the U.S.

• Visken

In Canada

• Alti-Pindolol

Available Dosage Forms:

• Tablet

Therapeutic Class: Cardiovascular Agent

Pharmacologic Class: Beta-Adrenergic Blocker, Nonselective

Uses For Alti-Pindolol

Pindolol is used alone or together with other medicines (such as hydrochlorothiazide) to treat high blood pressure (hypertension). High blood pressure adds to the workload of the heart and arteries. If it continues for a long time, the heart and arteries may not function properly. This can damage the blood vessels of the brain, heart, and kidneys, resulting in a stroke, heart failure, or kidney failure. High blood pressure may also increase the risk of heart attacks. These problems may be less likely to occur if blood pressure is controlled .

This medicine is a beta-blocker. It works by affecting the response to nerve impulses in certain parts of the body, like the heart. As a result, the heart beats slower and decreases the blood pressure. When the blood pressure is lowered, the amount of blood and oxygen is increased to the heart .

This medicine is available only with your doctor's prescription .

Before Using Alti-Pindolol

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies have not been performed on the relationship of age to the effects of pindolol in the pediatric population. Safety and efficacy have not been established .

Geriatric

No information is available on the relationship of age to the effects of pindolol in geriatric patients .

Pregnancy

	Pregnancy Category	Explanation
All Trimesters	B	Animal studies have revealed no evidence of harm to the fetus, however, there are no adequate studies in pregnant women OR animal studies have shown an adverse effect, but adequate studies in pregnant women have failed to demonstrate a risk to the fetus.

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

• Thioridazine

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Albuterol


• Amiodarone


• Arformoterol


• Bambuterol


• Bitolterol


• Broxaterol


• Clenbuterol


• Clonidine


• Colterol


• Diltiazem


• Dronedarone


• Epinephrine


• Fenoldopam


• Fenoterol


• Formoterol


• Hexoprenaline


• Indacaterol


• Isoetharine


• Levalbuterol


• Metaproterenol


• Pirbuterol


• Procaterol


• Reproterol


• Rimiterol


• Ritodrine


• Salmeterol


• Terbutaline


• Tretoquinol


• Tulobuterol


• Verapamil

Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Acarbose


• Aceclofenac


• Acemetacin


• Acetohexamide


• Alclofenac


• Alfuzosin


• Amlodipine


• Apazone


• Arbutamine


• Benfluorex


• Benoxaprofen


• Bromfenac


• Bufexamac


• Bunazosin


• Carprofen


• Chlorpropamide


• Clometacin


• Clonixin


• Dexketoprofen


• Diclofenac


• Diflunisal


• Digoxin


• Dipyrone


• Doxazosin


• Droxicam


• Etodolac


• Etofenamate


• Felbinac


• Felodipine


• Fenbufen


• Fenoprofen


• Fentiazac


• Floctafenine


• Flufenamic Acid


• Flurbiprofen


• Gliclazide


• Glimepiride


• Glipizide


• Gliquidone


• Glyburide


• Guar Gum


• Ibuprofen


• Indomethacin


• Indoprofen


• Insulin


• Insulin Aspart, Recombinant


• Insulin Glulisine


• Insulin Lispro, Recombinant


• Isoxicam


• Ketoprofen


• Ketorolac


• Lacidipine


• Lercanidipine


• Lornoxicam


• Manidipine


• Meclofenamate


• Mefenamic Acid


• Meloxicam


• Metformin


• Mibefradil


• Miglitol


• Moxisylyte


• Nabumetone


• Naproxen


• Nicardipine


• Nifedipine


• Niflumic Acid


• Nilvadipine


• Nimesulide


• Nimodipine


• Nisoldipine


• Nitrendipine


• Oxaprozin


• Oxyphenbutazone


• Phenoxybenzamine


• Phentolamine


• Phenylbutazone


• Pirazolac


• Piroxicam


• Pirprofen


• Pranidipine


• Prazosin


• Propyphenazone


• Proquazone


• Repaglinide


• St John's Wort


• Sulindac


• Suprofen


• Tamsulosin


• Tenidap


• Tenoxicam


• Terazosin


• Tiaprofenic Acid


• Tolazamide


• Tolbutamide


• Tolmetin


• Trimazosin


• Troglitazone


• Urapidil


• Zomepirac

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Angina (severe chest pain)—May provoke chest pain if stopped too quickly .

• Asthma or


• Bradycardia (slow heartbeat) or


• Heart block or


• Heart failure—Should not use in patients with these conditions .

• Diabetes or


• Hyperthyroidism (overactive thyroid) or


• Hypoglycemia (low blood sugar)—May cover up some of the signs and symptoms of these diseases, such as a fast heartbeat .

• Kidney disease or


• Liver disease—Use with caution. The effects may be increased because of slower removal from the body .

• Lung disease (e.g., bronchitis, emphysema)—May cause difficulty with breathing in patients with this condition .

Proper Use of pindolol

This section provides information on the proper use of a number of products that contain pindolol. It may not be specific to Alti-Pindolol. Please read with care.

In addition to the use of this medicine, treatment for your high blood pressure may include weight control and changes in the types of foods you eat, especially foods high in sodium. Your doctor will tell you which of these are most important for you. You should check with your doctor before changing your diet .

Many patients who have high blood pressure will not notice any signs of the problem. In fact, many may feel normal. It is very important that you take your medicine exactly as directed and that you keep your appointments with your doctor even if you feel well .

Remember that this medicine will not cure your high blood pressure, but it does help control it. You must continue to take it as directed if you expect to lower your blood pressure and keep it down. You may have to take high blood pressure medicine for the rest of your life. If high blood pressure is not treated, it can cause serious problems such as heart failure, blood vessel disease, stroke, or kidney disease .

Do not interrupt or stop taking this medicine without first checking with your doctor. Your doctor may want you to gradually reduce the amount you are taking before stopping it completely. Some conditions may become worse when the medicine is stopped suddenly, which can be dangerous .

Dosing

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For oral dosage form (tablets):
  
  • For high blood pressure:
    
    • Adults—At first, 5 milligrams (mg) two times a day. Your doctor may adjust your dose as needed.
    
    
    • Children—Use and dose must be determined by your doctor .
    
    
  
  

Missed Dose

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Precautions While Using Alti-Pindolol

It is very important that your doctor check your progress at regular visits to make sure this medicine is working properly and to check for unwanted effects .

Pindolol may cause heart failure in some patients. Check with your doctor right away if you are having chest pain or discomfort; dilated neck veins; extreme fatigue; irregular breathing; an irregular heartbeat; shortness of breath; swelling of the face, fingers, feet, or lower legs; weight gain; or wheezing .

This medicine may cause changes in your blood sugar levels. Also, this medicine may cover up signs of low blood sugar, such as a rapid pulse rate. Check with your doctor if you have these problems or if you notice a change in the results of your blood or urine sugar tests .

Make sure any doctor or dentist who treats you knows that you are using this medicine. You may need to stop using this medicine several days before having surgery .

Alti-Pindolol Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

More common

• Swelling of the face, fingers, feet, or lower legs

Less common

• Burning, crawling, itching, numbness, prickling, "pins and needles", or tingling feelings


• chest pain


• difficult or labored breathing


• shortness of breath


• tightness in chest


• wheezing

Rare

• Decreased urine output


• dilated neck veins


• extreme fatigue


• fast, irregular, pounding, or racing heartbeat or pulse


• irregular breathing


• seeing, hearing, or feeling things that are not there


• troubled breathing


• weight gain

Get emergency help immediately if any of the following symptoms of overdose occur:

Symptoms of overdose

• Blurred vision


• dizziness


• headache


• nervousness


• pounding in the ears


• slow heartbeat

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

• Joint pain


• muscle pain


• sleeplessness


• trouble sleeping


• unable to sleep


• unusual tiredness or weakness

Less common

• Itching skin


• muscle cramps


• nausea


• stomach soreness or discomfort


• unusual dreams


• weakness

Rare

• Rash

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

See also: Alti-Pindolol side effects (in more detail)

The information contained in the Thomson Reuters Micromedex products as delivered by Drugs.com is intended as an educational aid only. It is not intended as medical advice for individual conditions or treatment. It is not a substitute for a medical exam, nor does it replace the need for services provided by medical professionals. Talk to your doctor, nurse or pharmacist before taking any prescription or over the counter drugs (including any herbal medicines or supplements) or following any treatment or regimen. Only your doctor, nurse, or pharmacist can provide you with advice on what is safe and effective for you.

The use of the Thomson Reuters Healthcare products is at your sole risk. These products are provided "AS IS" and "as available" for use, without warranties of any kind, either express or implied. Thomson Reuters Healthcare and Drugs.com make no representation or warranty as to the accuracy, reliability, timeliness, usefulness or completeness of any of the information contained in the products. Additionally, THOMSON REUTERS HEALTHCARE MAKES NO REPRESENTATION OR WARRANTIES AS TO THE OPINIONS OR OTHER SERVICE OR DATA YOU MAY ACCESS, DOWNLOAD OR USE AS A RESULT OF USE OF THE THOMSON REUTERS HEALTHCARE PRODUCTS. ALL IMPLIED WARRANTIES OF MERCHANTABILITY AND FITNESS FOR A PARTICULAR PURPOSE OR USE ARE HEREBY EXCLUDED. Thomson Reuters Healthcare does not assume any responsibility or risk for your use of the Thomson Reuters Healthcare products.

More Alti-Pindolol resources

• Alti-Pindolol Side Effects (in more detail)
• Alti-Pindolol Use in Pregnancy & Breastfeeding
• Drug Images
• Alti-Pindolol Drug Interactions
• Alti-Pindolol Support Group
• 0 Reviews for Alti-Pindolol - Add your own review/rating

Compare Alti-Pindolol with other medications

• High Blood Pressure

Acticin Topical

Generic Name: permethrin (Topical route)

per-METH-rin

Commonly used brand name(s)

In the U.S.

• Acticin


• Elimite


• Nix Creme Rinse

In Canada

• Nix


• Nix Dermal Cream

Available Dosage Forms:

• Lotion


• Spray


• Cream


• Liquid

Therapeutic Class: Pediculicide

Chemical Class: Pyrethroid

Uses For Acticin

Permethrin 1% lotion is used to treat head lice infections. It acts by destroying both the lice and their eggs. The 5% cream is used to treat scabies infections by destroying the mites which cause scabies.

Before Using Acticin

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Studies on this medicine have been done only in adult patients, and there is no specific information comparing use of topical permethrin in children with use in other age groups.

Geriatric

Many medicines have not been studied specifically in older people. Therefore, it may not be known whether they work exactly the same way they do in younger adults or if they cause different side effects or problems in older people. There is no specific information comparing use of topical permethrin in the elderly with use in other age groups.

Pregnancy

	Pregnancy Category	Explanation
All Trimesters	B	Animal studies have revealed no evidence of harm to the fetus, however, there are no adequate studies in pregnant women OR animal studies have shown an adverse effect, but adequate studies in pregnant women have failed to demonstrate a risk to the fetus.

Breast Feeding

Studies in women suggest that this medication poses minimal risk to the infant when used during breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. Tell your healthcare professional if you are taking any other prescription or nonprescription (over-the-counter [OTC]) medicine.

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

The presence of other medical problems may affect the use of topical permethrin. Make sure you tell your doctor if you have other medical problems, especially:

• Severe inflammation of the scalp—Use of permethrin may make the condition worse

Proper Use of permethrin

This section provides information on the proper use of a number of products that contain permethrin. It may not be specific to Acticin. Please read with care.

Keep this medicine away from the eyes. If you accidentally get some in your eyes, flush them thoroughly with water at once.

Permethrin lotion which is used to treat lice, comes in a container that holds only one treatment. Use as much of the medicine as you need and discard any remaining lotion properly.

For the treatment of head lice (1% lotion):

• Shampoo the hair and scalp using regular shampoo.


• Thoroughly rinse and towel dry the hair and scalp.


• Allow hair to air dry for a few minutes.


• Shake the permethrin lotion well before applying.


• Thoroughly wet the hair and scalp with the permethrin lotion. Be sure to cover the areas behind the ears and on the back of the neck also. Allow the lotion to remain in place for 10 minutes.


• Then, rinse the hair and scalp thoroughly and dry with a clean towel.


• When the hair is dry, you may want to comb the hair with a fine-toothed comb to remove any remaining nits (eggs) or nit shells.

Head lice can be easily transferred from one person to another by direct contact with clothing, hats, scarves, bedding, towels, washcloths, hairbrushes and combs, or hairs from infected persons. Therefore, all members of your household should be examined for head lice and should receive treatment if they are found to be infected. If you have any questions about this, check with your doctor.

For the treatment of scabies (5% cream):

• Read package directions carefully before using.


• Thoroughly wash and dry skin.


• Massage the cream into the skin from the head to the soles of the feet, paying special attention to creases in the skin, hands, feet, between fingers and toes, underarms, and groin.


• Scabies rarely infests the scalp of adults, although the hairline, neck, side of the head, and forehead may be infested in older people and in infants. Infants should be treated on the scalp, side of the head, and forehead.


• Leave the permethrin cream on the skin for 8 to 14 hours.


• Wash off by taking a shower or bath.


• Change into clean clothes.


• After treatment, itching may continue for up to 4 weeks.

Dosing

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For topical dosage forms (cream and lotion):
  
  • For head lice:
    
    • Adults and children 2 years of age and older—Apply to the hair and scalp one time.
    
    
    • Children up to 2 years of age—Use and dose must be determined by your doctor.
    
    
  
  
  • For scabies:
    
    • Adults and children 2 months of age and older—Apply to the skin one time.
    
    
    • Children up to 2 months of age—Use and dose must be determined by your doctor.
    
    
  
  

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Precautions While Using Acticin

To prevent reinfection or spreading of the infection to other people, good health habits are required. These include the following:

• Machine wash all clothing (including hats, scarves, and coats), bedding, towels, and washcloths in very hot water and dry them by using the hot cycle of a dryer for at least 20 minutes. Clothing or bedding that cannot be washed should be dry cleaned or sealed in an airtight plastic bag for 2 weeks.


• Shampoo all wigs and hairpieces.


• Wash all hairbrushes and combs in very hot soapy water (above 130 °F) for 5 to 10 minutes and do not share them with other people.


• Clean the house or room by thoroughly vacuuming upholstered furniture, rugs, and floors.


• Wash all toys in very hot soapy water (above 130 °F) for 5 to 10 minutes or seal in an airtight plastic bag for 2 weeks. This is especially important for stuffed toys used on the bed.

Acticin Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

Less common or rare

• Burning, itching, numbness, rash, redness, stinging, swelling, or tingling of the scalp

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

See also: Acticin Topical side effects (in more detail)

The information contained in the Thomson Reuters Micromedex products as delivered by Drugs.com is intended as an educational aid only. It is not intended as medical advice for individual conditions or treatment. It is not a substitute for a medical exam, nor does it replace the need for services provided by medical professionals. Talk to your doctor, nurse or pharmacist before taking any prescription or over the counter drugs (including any herbal medicines or supplements) or following any treatment or regimen. Only your doctor, nurse, or pharmacist can provide you with advice on what is safe and effective for you.

The use of the Thomson Reuters Healthcare products is at your sole risk. These products are provided "AS IS" and "as available" for use, without warranties of any kind, either express or implied. Thomson Reuters Healthcare and Drugs.com make no representation or warranty as to the accuracy, reliability, timeliness, usefulness or completeness of any of the information contained in the products. Additionally, THOMSON REUTERS HEALTHCARE MAKES NO REPRESENTATION OR WARRANTIES AS TO THE OPINIONS OR OTHER SERVICE OR DATA YOU MAY ACCESS, DOWNLOAD OR USE AS A RESULT OF USE OF THE THOMSON REUTERS HEALTHCARE PRODUCTS. ALL IMPLIED WARRANTIES OF MERCHANTABILITY AND FITNESS FOR A PARTICULAR PURPOSE OR USE ARE HEREBY EXCLUDED. Thomson Reuters Healthcare does not assume any responsibility or risk for your use of the Thomson Reuters Healthcare products.

More Acticin Topical resources

• Acticin Topical Side Effects (in more detail)
• Acticin Topical Use in Pregnancy & Breastfeeding
• Acticin Topical Support Group
• 0 Reviews for Acticin Topical - Add your own review/rating

Compare Acticin Topical with other medications

• Head Lice
• Lice
• Scabies

Avodart

Generic Name: Dutasteride
Class: 5-alpha-Reductase Inhibitors
VA Class: HS900
Chemical Name: 5α,17β)-N-[2,5-bis(trifluoromethyl)phenyl]-3-oxo-4-azaandrost-1-ene-17-carboxamide
Molecular Formula: C₂₇H₃₀F₆N₂O₂
CAS Number: 164656-23-9

Special Alerts:

[Posted 06/09/2011] ISSUE: FDA notified healthcare professionals that the Warnings and Precautions section of the labels for the 5-alpha reductase inhibitor (5-ARI) class of drugs has been revised to include new safety information about the increased risk of being diagnosed with a more serious form of prostate cancer (high-grade prostate cancer).

BACKGROUND: The new safety information is based on FDA’s review of two large, randomized controlled trials––the Prostate Cancer Prevention Trial (PCPT) and the Reduction by Dutasteride of Prostate Cancer Events (REDUCE) trial. Finasteride (Proscar), dutasteride (Avodart), and dutasteride in combination with tamsulosin (marketed combination product as Jalyn) are approved to improve symptoms of an enlarged prostate gland (benign prostatic hyperplasia or BPH). Proscar and Avodart are also approved to reduce the risk of urinary retention or surgery related to an enlarged prostate. Finasteride (Propecia) is approved to treat male pattern hair loss.

RECOMMENDATION: Prior to initiating therapy with 5-ARIs, perform appropriate evaluation to rule out other urological conditions, including prostate cancer, that might mimic benign prostatic hyperplasia (BPH). See Drug Safety Communication for a Data Summary and additional information. For more information visit the FDA website at: and .

Introduction

Selective inhibitor of steroid 5α-reductase isoenzymes, which are necessary for conversion of testosterone to 5α-dihydrotestosterone (DHT).^{1 4 9}

Uses for Avodart

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Benign Prostatic Hyperplasia (BPH)

Treatment of symptomatic BPH¹ to improve symptoms and reduce the risk of acute urinary retention and the need for surgery.^{1 3} Ineffective in patients who do not have evidence of prostatic enlargement.¹¹

Although drug therapy usually is not as effective as surgical therapy, it may provide adequate symptomatic relief with fewer and less serious adverse effects compared with surgery.¹¹

Steroid 5α-reductase inhibitors may be a useful alternative to surgery in patients with obstructive manifestations who are unwilling to undergo surgical correction of BPH;⁸ may aid those who may be at increased risk from, but not necessarily candidates for, prostate surgery.^{4 8 10} Also may be considered in patients who have symptomatic prostatic enlargement but whose symptoms are not bothersome (i.e., do not interfere with activities of daily living) in order to prevent progression of the disease.¹¹

May consider combined therapy with an α₁-adrenergic blocker and 5α-reductase inhibitor for men with bothersome moderate to severe BPH and demonstrable prostatic enlargement.¹¹ Has been more effective than therapy with either drug alone in preventing long-term BPH symptom progression.¹¹ Men at risk for BPH progression are most likely to benefit from combination therapy.¹¹

Avodart Dosage and Administration

Administration

Oral Administration

Administer orally without regard to meals.¹

The capsules should be swallowed whole.¹

Dosage

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Adults

Benign Prostatic Hyperplasia

Oral

Initially and for maintenance therapy, 0.5 mg once daily.¹

While early symptomatic improvement (e.g., within 3 months) may occur, ≥6 months of therapy may be necessary to determine clinical benefit.² Generally, therapy is continued for life.⁹

Special Populations

Hepatic Impairment

No specific dosage recommendations for hepatic impairment.¹ (See Hepatic Impairment under Cautions.)

Renal Impairment

Dosage adjustment not required.¹

Geriatric Patients

Dosage adjustment not required.¹

Cautions for Avodart

Contraindications

• 
  

  Known or suspected pregnancy.¹ (See Fetal/Neonatal Morbidity and also Pregnancy under Cautions.)

  
  


• 
  

  Use in women or children.¹

  
  


• 
  

  Known hypersensitivity to dutasteride, other 5α-reductase inhibitors, or any ingredient in the formulation.¹

  
  

Warnings/Precautions

Warnings

Fetal/Neonatal Morbidity

May cause fetal harm; teratogenicity demonstrated in animals.¹ Animal studies indicate adverse effects on embryofetal development of male fetuses exposed to the drug during pregnancy (e.g., abnormalities of the external genitalia, decreased prostatic and seminal vesicular weights, distended preputial glands, nipple development).¹

Because of the potential for absorption through the skin and the subsequent potential risk to a male fetus, pregnant women or women who may become pregnant should not handle the capsules.^{1 2}

If contact is made with leaking capsules, wash the affected area immediately with soap and water.^{1 2}

To prevent potential fetal exposure, men receiving the drug should not donate blood during dutasteride therapy and for at least 6 months following discontinuance of the drug.¹

Seminal drug concentrations not sufficient to warrant the use of condoms to prevent exposure to dutasteride.¹⁰

General Precautions

Patient Assessment

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Evaluate candidates for dutasteride therapy for other urologic conditions that might mimic BPH, such as infection,⁴ prostate ^{1 4} or bladder cancer,⁴ stricture disease,⁴ uncontrolled diabetes mellitus,⁴ neurogenic bladder,⁴ or CHF.^{4 7}

Perform digital rectal examinations, as well as other screening tests for prostate cancer, before initiating therapy and periodically thereafter.^{1 7 8}

Monitor patients with a large residual urinary volume and/or severely diminished urinary flow carefully for obstructive uropathy.^{4 7} Such patients may not be candidates for dutasteride therapy,¹ and may require surgery.^{4 7}

Prostate-specific Antigen (PSA)

Decreases PSA concentrations; may interfere with interpretation of serum PSA determinations.¹ (See Specific Drugs and Laboratory Tests under Interactions.)

Specific Populations

Pregnancy

Category X.¹ (See Fetal/Neonatal Morbidity and also Contraindications under Cautions.)

Lactation

Not known whether dutasteride is distributed into milk, but use of the drug is contraindicated in women.^{1 10}

Pediatric Use

Safety and efficacy not established, but the drug is not indicated for use in children.¹

Geriatric Use

No substantial differences in safety and efficacy relative to younger men.¹

Hepatic Impairment

Not studied in patients with hepatic impairment.¹ Increased exposure to the drug is probable.¹ Use with caution.¹

Common Adverse Effects

Impotence, decreased libido, ejaculation disorder, gynecomastia (breast tenderness, enlargement).¹

Interactions for Avodart

Metabolized by CYP isoenzymes 3A4 and 3A5 to active metabolites; not metabolized by CYP isoenzymes 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, or 2E1.¹

Drugs Affecting Hepatic Microsomal Enzymes

Potential pharmacokinetic interaction with inhibitors of CYP3A4 (decreased clearance and increased serum concentrations of dutasteride).¹

Specific Drugs and Laboratory Tests

Drug or Test	Interaction	Comments
Amlodipine	Pharmacokinetic interaction unlikely1
Cholestyramine	Pharmacokinetic or pharmacodynamic interaction unlikely1
Cimetidine	Decreased clearance and increased serum concentrations of dutasteride1	Use concomitantly with care
Ciprofloxacin	Decreased clearance and increased serum concentrations of dutasteride1	Use concomitantly with care1
Digoxin	Pharmacokinetic or pharmacodynamic interaction unlikely1
Diltiazem	Decreased clearance and increased serum concentrations of dutasteride1	Not considered clinically important1
Ketoconazole	Decreased clearance and increased serum concentrations of dutasteride1	Use concomitantly with care1
Ritonavir	Decreased clearance and increased serum concentrations of dutasteride1
Tamsulosin	Pharmacokinetic or pharmacodynamic interaction unlikely1
Terazosin	Pharmacokinetic or pharmacodynamic interaction unlikely1
Test for PSA	50% decrease in serum PSA concentration after ≥6 months of treatment1 3 6 9 10 No substantial change in ratio of free to total PSA (percentage of free PSA)1	Establish a new baseline PSA 3–6 months after initiation of treatment1 For clinical interpretation of isolated PSA values in men receiving dutasteride for ≥6 months, double the reported value for PSA for comparison with normal values in men not receiving the drug1 3 No adjustment of reported value of ratio appears to be necessary1
Troleandomycin	Decreased clearance and increased serum concentrations of dutasteride1
Verapamil	Decreased clearance and increased serum concentrations of dutasteride1	Not considered clinically important1
Warfarin	Pharmacokinetic or pharmacodynamic interaction unlikely1

Avodart Pharmacokinetics

Absorption

Bioavailability

Absolute bioavailability is approximately 60%.¹

Onset

Reduces serum and prostatic 5α-dihydroxytestosterone (DHT) concentrations maximally within 1–2 weeks of initiation of therapy.¹

Duration

Serum drug concentrations are detectable for up to 4–6 months following discontinuance of therapy.¹

Food

Decreases peak serum concentrations.¹ Not considered clinically important.¹

Distribution

Extent

Widely distributed; volume of distribution is 300–500 L.¹

Distributes into semen.¹

Plasma Protein Binding

Highly bound to albumin (99%) and α-1 acid glycoprotein (96.6%).¹

Elimination

Metabolism

Metabolized by CYP3A4 and CYP3A5 to active metabolites.¹

Elimination Route

Excreted in the feces (45%) and urine (<1%) mainly as metabolites; approximately 55% remained unaccounted.¹

Half-life

Terminal half-life is approximately 5 weeks at steady state.¹

Special Populations

In patients with hepatic impairment, pharmacokinetics not studied.¹ Metabolized extensively in the liver, and increased exposure to the drug is probable in hepatic impairment.¹

In adolescents (<18 years of age), pharmacokinetics not studied.¹

In patients with renal impairment, pharmacokinetics not studied; however, <0.1% of a dose is excreted in urine in healthy individuals.¹

In women, pharmacokinetics not studied; use contraindicated.¹

Effects of race on pharmacokinetics not studied.¹

Stability

Storage

Oral

Capsules

25°C (may be exposed to 15–30°C).¹

ActionsActions

• 
  

  Competitive inhibitor of both the type 1 and type 2 isoenzymes of steroid 5α-reductase.^{1 9} These enzymes convert testosterone to DHT.^{1 9}

  
  


• 
  

  Reduces serum and prostatic DHT concentrations substantially.¹ DHT appears to be the principal androgen responsible for initial development and subsequent enlargement of the prostate gland.^{1 9}

  
  


• 
  

  Increases serum testosterone (generally remaining within the normal range) and prostatic testosterone concentrations.^{1 3 9}

  
  

Advice to Patients

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

• 
  

  Importance of obtaining and reading patient information on dutasteride before initiation of therapy and with each new prescription refill.¹

  
  


• 
  

  Importance of advising pregnant women or women who may become pregnant to avoid handling the drug.¹ (See Pregnancy under Cautions.)

  
  


• 
  

  Advise patients that a decrease in the volume of ejaculate may occur but that this does not appear to interfere with normal sexual function.¹

  
  


• 
  

  Advise patients of the small possibility of impotence and decreased libido.^{1 10}

  
  


• 
  

  Advise patients of possibility of developing enlarged or tender breasts.¹

  
  


• 
  

  Advise patients of possibility of allergic reactions (e.g., rash, pruritus, urticaria, swelling of lips or face).¹

  
  


• 
  

  Advise patients that ≥6 months of therapy may be required before improvement in BPH symptoms occurs.²

  
  


• 
  

  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.¹

  
  


• 
  

  Importance of advising patients of other important precautionary information.¹ (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Dutasteride

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Capsules, liquid-filled	0.5 mg	Avodart	GlaxoSmithKline

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 07/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Avodart 0.5MG Capsules (GLAXO SMITH KLINE): 30/$129.98 or 90/$354.97

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions June 09, 2011. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. GlaxoSmithKline. Avodart (dutasteride) soft gelatin capsules prescribing information. Research Triangle Park, NC; 2005 May.

2. GlaxoSmithKline. Avodart (dutasteride) soft gelatin capsules patient information. Research Triangle Park, NC; Undated. Available at: . Accessed 2006 Aug 15.

3. Roehrborn CG, Boyle P, Nickel JC et al. Efficacy and safety of a dual inhibitor of 5-alpha-reductase types 1 and 2 (dutasteride) in men with benign prostatic hyperplasia. Urology. 2002 60:434-41.

4. Dull P, Reagan RW, Bahnson RR. Managing benign prostatic hyperplasia. Am Fam Physician. 2002; 66:77-84, 87-8. [IDIS 483339] [PubMed 12126034]

5. Roehrborn CG, McConnell JD, Lieber M et al. Serum prostate-specific antigen concentration is a powerful predictor of acute urinary retenion and need for surgery in men with clinical benign prostatic hyperplasia. PLESS study group. Urology. 1999; 53:473-80. [PubMed 10096369]

6. Potts JM. Prospective identification of National Institutes of Health category IV prostatitis in men with elevated prostate specific antigen. J Urol. 2000; 164:1550-3. [IDIS 455479] [PubMed 11025702]

7. de la Rossette JJ, Alivizatos G, Madersbacher S et al. EAU guidelines on benign prostatic hyperplasia (BPH). Eur Urol. 2001; 40:256-63. [PubMed 11684840]

8. Agency for Health Care Policy and Research. Benign prostatic hyperplasia: diagnosis and treatment. J Am Geriatric Soc. 1998; 46:1163-5.

9. Anon. Dutasteride (avodart) for benign prostatic hyperplasia. Med Lett Drugs Ther. 2002; 44:109-10. [PubMed 12500154]

10. GlaxoSmithKline. Research Triangle Park, NC: Personal communication.

11. American Urological Association. Guideline on the management of benign prostatic hyperplasia (BPH)(2003/updated 2006). Available at: . Accessed 2006 Aug 10.

More Avodart resources

• Avodart Side Effects (in more detail)
• Avodart Use in Pregnancy & Breastfeeding
• Drug Images
• Avodart Drug Interactions
• Avodart Support Group
• 14 Reviews for Avodart - Add your own review/rating

• Avodart Prescribing Information (FDA)


• Avodart Consumer Overview


• Avodart Advanced Consumer (Micromedex) - Includes Dosage Information


• Avodart MedFacts Consumer Leaflet (Wolters Kluwer)


• Dutasteride Professional Patient Advice (Wolters Kluwer)

Compare Avodart with other medications

• Benign Prostatic Hyperplasia

Androxy

fluoxymesterone

Dosage Form: Tablets

CIII

REV. 5-04

15021-09

Androxy™ (Fluoxymesterone Tablets, USP)

Rx only

Androxy Description

Androxy™ (Fluoxymesterone Tablets, USP) contains fluoxymesterone, a synthetic androgen. The androgens are steroids that develop and maintain primary and secondary male sex characteristics. Androgens are derivatives of cyclopentano-perhydrophenanthrene. Endogenous androgens are C-19 steroids with a side chain at C-17, and with two angular methyl groups. Testosterone is the primary endogenous androgen. Fluoxymesterone is a synthetic derivative of testosterone.

In their active form, all drugs in the class have a 17-beta-hydroxy group. 17-alpha-alkylation and halogenation at position 9 (fluoxymesterone) increase the pharmacologic activity per unit weight compared to testosterone when given orally. Fluoxymesterone is a white or practically white odorless, crystalline powder, melting at about 240°C with some decomposition. It is practically insoluble in water, sparingly soluble in alcohol and slightly soluble in chloroform. Chemically fluoxymesterone is designated 9-fluoro-11β, 17β-dihydroxy-17-methylandrost-4-en-3-one. Structurally it may be represented as follows:

Androxy™ (Fluoxymesteron Tablets, USP) for oral administration contains 10 mg of fluoxymesterone USP.

Inactive Ingredients: croscarmellose sodium, D&C Yellow #10 Aluminum Lake, FD&C Blue #1 Aluminum Lake, FD&C Yellow #6 Aluminum Lake, anhydrous lactose, magnesium stearate, microcrystalline cellulose, pregelatinized starch (corn), and sodium lauryl sulfate.

Androxy - Clinical Pharmacology

Endogenous androgens are responsible for the normal growth and development of the male sex organs and for maintenance of secondary sex characteristics. These effects include growth and maturation of prostate, seminal vesicles, penis, and scrotum; development of male hair distribution, such as beard, pubic, chest, and axillary hair; laryngeal enlargement; vocal cord thickening; alterations in body musculature; and fat distribution.

Androgens also cause retention of nitrogen, sodium, potassium, and phosphorus, and decreased urinary excretion of calcium. Androgens have been reported to increase protein anabolism and decrease protein catabolism. Nitrogen balance is improved only when there is sufficient intake of calories and protein.

Androgens are responsible for the growth spurt of adolescence and for the eventual termination of linear growth which is brought about by fusion of the epiphyseal growth centers. In children, exogenous androgens accelerate linear growth rates but may cause a disproportionate advancement in bone maturation. Use over long periods may result in fusion of the epiphyseal growth centers and termination of growth process. Androgens have been reported to stimulate the production of red blood cells by enhancing the production of erythropoietic stimulating factor.

During exogenous administration of androgens, endogenous testosterone release is inhibited through feedback inhibition of pituitary luteinizing hormone (LH). At large doses of exogenous androgens, spermatogenesis may also be suppressed through feedback inhibition of pituitary follicle stimulating hormone (FSH).

There is a lack of substantial evidence that androgens are effective in fractures, surgery, convalescence, and functional uterine bleeding.

Pharmacokinetics

Testosterone given orally is metabolized by the gut, and 44 percent is cleared by the liver in the first pass. Oral doses as high as 400 mg per day are needed to achieve clinically effective blood levels for full replacement therapy. The 17-alpha-alkylated derivatives (fluoxymesterone and methyltestosterone) are less extensively metabolized by the liver and have longer half lives. They are more suitable for oral administration than testosterone.

Testosterone in plasma is 98 percent bound to a specific testosterone-estradiol binding globulin, and about two percent is free. Generally, the amount of this sex-hormone binding globulin in the plasma will determine the distribution of testosterone between free and bound forms, and the free testosterone concentration will determine its half-life.

About 90 percent of a dose of testosterone is excreted in the urine as glucuronic and sulfuric acid conjugates of testosterone and its metabolites; about six percent of a dose is excreted in the feces, mostly in the unconjugated form. Inactivation of testosterone occurs primarily in the liver. Testosterone is metabolized to various 17-keto steroids through two different pathways. There are considerable variations of the half-life of testosterone as reported in the literature, ranging from 10 to 100 minutes. The half-life of fluoxymesterone is reported to be 10 hours.

In responsive tissues the activity of testosterone appears to depend on reduction to dihydrotestosterone, which binds to cytosol receptor proteins. The steroid-receptor complex is transported to the nucleus where it initiates transcription events and cellular changes related to androgen action.

Indications and Usage for Androxy

Males

Androxy™ Tablets are indicated for replacement therapy in conditions associated with a deficiency or absence of endogenous testosterone.

Primary hypogonadism (congenital or acquired)—Testicular failure due to cryptorchidism, bilateral torsion, orchitis, vanishing testis syndrome, or orchidectomy.

Hypogonadotropic hypogonadism (congenital or acquired)—Idiopathic gonadotropin or luteinizing hormone-releasing hormone (LHRH) deficiency, or pituitary-hypothalamic injury from tumors, trauma, or radiation. (Appropriate adrenal cortical and thyroid hormone replacement therapy are still necessary, however, and are actually of primary importance.)

If the above conditions occur prior to puberty, androgen replacement therapy will be needed during the adolescent years for development of secondary sexual characteristics. Prolonged androgen treatment will be required to maintain sexual characteristics in these and other males who develop testosterone deficiency after puberty.

Delayed puberty—Androxy™ (Fluoxymesterone Tablets, USP) may be used to stimulate puberty in carefully selected males with clearly delayed puberty. These patients usually have a familial pattern of delayed puberty that is not secondary to a pathological disorder; puberty is expected to occur spontaneously at a relatively late date. Brief treatment with conservative doses may occasionally be justified in these patients if they do not respond to psychological support. The potential adverse effect on bone maturation should be discussed with the patient and parents prior to androgen administration. An X-ray of the hand and wrist to determine bone age should be obtained every six months to assess the effect of treatment on the epiphyseal centers (see WARNINGS).

Females

Metastatic mammary cancer—Androxy™ (Fluoxymesterone Tablets, USP) may be used secondarily in women with advancing inoperable metastatic (skeletal) mammary cancer who are one to five years postmenopausal. Primary goals of therapy in these women include ablation of the ovaries. Other methods of counteracting estrogen activity are adrenalectomy, hypophysectomy, and/or antiestrogen therapy. This treatment has been used in premenopausal women with breast cancer who have benefited from oophorectomy and are considered to have a hormone-responsive tumor. Judgment concerning androgen therapy should be made by an oncologist with expertise in this field.

Contraindications

Androgens are contraindicated in men with carcinomas of the breast or with known or suspected carcinomas of the prostate and in women who are or may become pregnant. When administered to pregnant women, androgens cause virilization of the external genitalia of the female fetus. This virilization includes clitoromegaly, abnormal vaginal development, and fusion of genital folds to form a scrotal-like structure. The degree of masculinization is related to the amount of drug given and the age of the fetus and is most likely to occur in the female fetus when the drugs are given in the first trimester. If the patient becomes pregnant while taking androgens, she should be apprised of the potential hazard to the fetus.

Warnings

This drug has not been shown to be safe and effective for the enhancement of athletic performance. Because of the potential risk of serious adverse health effects, this drug should not be used for such purpose.

In patients with breast cancer and in immobilized patients, androgen therapy may cause hypercalcemia by stimulating osteolysis. In patients with cancer, hypercalcemia may indicate progression of bony metastasis. If hypercalcemia occurs, the drug should be discontinued and appropriate measures instituted.

Prolonged use of high doses of androgens has been associated with the development of peliosis hepatis and hepatic neoplasms including hepatocellular carcinoma (see PRECAUTIONS, Carcinogenesis). Peliosis hepatis can be a life-threatening or fatal complication.

Cholestatic hepatitis and jaundice occur with 17-alpha-alkylated androgens at a relatively low dose. If cholestatic hepatitis with jaundice appears or if liver function tests become abnormal, the androgen should be discontinued and the etiology should be determined. Drug-induced jaundice is reversible when the medication is discontinued.

Geriatric patients treated with androgens may be at an increased risk for the development of prostatic hypertrophy and prostatic carcinoma.

Due to sodium and water retention, edema with or without congestive heart failure may be a serious complication in patients with preexisting cardiac, renal, or hepatic disease. In addition to discontinuation of the drug, diuretic therapy may be required. If the administration of fluoxymesterone is restarted, a lower dosage should be used.

Gynecomastia frequently develops and occasionally persists in patients being treated for hypogonadism.

Androgen therapy should be used cautiously in healthy males with delayed puberty. The effect on bone maturation should be monitored by assessing bone age of the wrist and hand every six months. In children, androgen treatment may accelerate bone maturation without producing compensatory gain in linear growth. This adverse effect may result in compromised adult stature. The younger the child the greater the risk of compromising final mature height.

Precautions

General

Women should be observed for signs of virilization (deepening of the voice, hirsutism, acne, clitoromegaly, and menstrual irregularities). Discontinuation of drug therapy at the time of evidence of mild virilism is necessary to prevent irreversible virilization. Such virilization is usual following androgen use at high doses and is not prevented by concomitant use of estrogens. A decision may be made by the patient and the physician that some virilization will be tolerated during treatment for breast carcinoma.

Because androgens may alter serum cholesterol concentration, caution should be used when administering these drugs to patients with a history of myocardial infarction or coronary artery disease. Serial determinations of serum cholesterol should be made and therapy adjusted accordingly. A causal relationship between myocardial infarction and hypercholesterolemia has not been established.

Information for Patients

Male adolescent patients receiving androgens for delayed puberty should have bone development checked every six months.

The physician should instruct patients to report any of the following side effects of androgens:

Adult or adolescent males—too frequent or persistent erections of the penis.

Women—hoarseness, acne, changes in menstrual periods, or more facial hair.

All patients—Any nausea, vomiting, changes in skin color, or ankle swelling.

Laboratory Tests

Women with disseminated breast carcinoma should have frequent determination of urine and serum calcium levels during the course of androgen therapy (see WARNINGS).

Because of the hepatotoxicity associated with the use of 17-alpha-alkylated androgens, liver function tests should be obtained periodically.

Periodic (every six months) X-ray examinations of bone age should be made during treatment of prepubertal males to determine the rate of bone maturation and the effects of androgen therapy on the epiphyseal centers.

Hemoglobin and hematocrit should be checked periodically for polycythemia in patients who are receiving high doses of androgens.

Drug Interactions

When administered concurrently, the following drugs may interact with androgens:

Anticoagulants, oral—C-17 substituted derivatives of testosterone, such as methandrostenolone, have been reported to decrease the anticoagulant requirement. Patients receiving oral anticoagulant therapy require close monitoring especially when androgens are started or stopped.

Antidiabetic drugs and insulin—In diabetic patients, the metabolic effects of androgens may decrease blood glucose and insulin requirements.

ACTH and corticosteroids—Enhanced tendency toward edema. Use caution when giving these drugs together, especially in patients with hepatic or cardiac disease.

Oxyphenbutazone—May result in elevated serum levels of oxyphenbutazone.

Drug/Laboratory Test Interactions

Androgens may decrease levels of thyroxine-binding globulin, resulting in decreased total T4 serum levels and increased resin uptake of T3 and T4. Free thyroid hormone levels remain unchanged, however, and there is no clinical evidence of thyroid dysfunction.

Carcinogenesis

Testosterone has been tested by subcutaneous injection and implantation in mice and rats. The implant induced cervical-uterine tumors in mice, which metastasized in some cases. There is suggestive evidence that injection of testosterone into some strains of female mice increases their susceptibility to hepatoma. Testosterone is also known to increase the number of tumors and decrease the degree of differentiation of chemically-induced carcinomas of the liver in rats.

There are rare reports of hepatocellular carcinoma in patients receiving long-term therapy with androgens in high doses. Withdrawal of the drugs did not lead to regression of the tumors in all cases.

Geriatric patients treated with androgens may be at an increased risk for the development of prostatic hypertrophy and prostatic carcinoma.

Pregnancy—Teratogenic Effects

Category X (see CONTRAINDICATIONS)

Nursing Mothers

It is not known whether androgens are excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from androgens, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Pediatric Use

Androgen therapy should be used very cautiously in children and only by specialists who are aware of the adverse effects on bone maturation. Skeletal maturation must be monitored every six months by an X-ray of the hand and wrist (see INDICATIONS AND USAGE, and WARNINGS).

Adverse Reactions

Endocrine and Urogenital, Female—The most common side effects of androgen therapy are amenorrhea and other menstrual irregularities, inhibition of gonadotropin secretion, and virilization, including deepening of the voice and clitoral enlargement. The latter usually is not reversible after androgens are discontinued. When administered to a pregnant woman, androgens cause virilization of external genitalia of the female fetus.

Male—Gynecomastia, and excessive frequency and duration of penile erections. Oligospermia may occur at high dosages (see CLINICAL PHARMACOLOGY).

Skin and Appendages—Hirsutism, male pattern baldness, and acne.

Fluid and Electrolyte Disturbances—Retention of sodium, chloride, water, potassium, calcium (see WARNINGS), and inorganic phosphates.

Gastrointestinal—Nausea, cholestatic jaundice, alterations in liver function tests; rarely, hepatocellular neoplasms, peliosis hepatis, hepatic coma, and death. (See WARNINGS.)

Hematologic—Suppression of clotting factors II, V, VII, and X; bleeding in patients on concomitant anticoagulant therapy; and polycythemia.

Nervous System—Increased or decreased libido, headache, anxiety, depression, and generalized paresthesia.

Metabolic—Increased serum cholesterol.

Miscellaneous—Hypersensitivity; rarely, anaphylactoid reactions.

Drug Abuse and Dependence

Androxy™ Tablets are classified as a Schedule III controlled substance under the Anabolic Steroids Control Act of 1990.

Overdosage

There have been no reports of acute overdosage with androgens.

Androxy Dosage and Administration

Androxy™ (Fluoxymesterone Tablets, USP), for oral administration, may be given as a single daily dose or in divided doses. Dosage and duration of therapy will depend on age, sex, diagnosis, patient's response to treatment, and appearance of adverse effects. The following recommendations will serve as a guide to therapy with Androxy™ Tablets.

In males with delayed puberty: Various dosage regimens have been used; some call for lower dosages initially with gradual increases as puberty progresses, with or without a decrease to maintenance levels. Other regimens call for higher dosage to induce pubertal changes and lower dosage for maintenance after puberty. The chronological and skeletal ages must be taken into consideration, both in determining the initial dose and in adjusting the dose. Dosage is within the range of 2.5 to 20 mg daily, although generally in the lower range of 2.5 to 10 mg daily, and for a limited duration, for example 4 to 6 months. X-rays should be taken at appropriate intervals to determine the amount of bone maturation and skeletal development (see INDICATIONS AND USAGE, and WARNINGS).

Male hypoganadism: As replacement therapy, i.e., for eunuchism, a daily dose of 5 to 20 mg is suggested. It is usually preferable to start therapy at a higher level within the range (e.g., 10 mg), with subsequent adjustment as required.

Palliation of inoperable mammary cancer in women: A daily dose of 10 to 40 mg, given in divided doses, is recommended. To determine if there will be an objective response, treatment should be continued for three months or more. Patients must be followed closely because androgen therapy occasionally appears to accelerate the disease. Thus, many experts prefer to use a shorter acting androgen preparation, such as Androxy™ Tablets, rather than those with prolonged activity, particularly during the early stages of androgen therapy.

In palliation of advanced mammary carcinoma: Hormone therapy is adjunctive to and not a replacement for conventional therapy. Duration of therapy will depend on the response of the condition and the appearance of adverse reactions.

How is Androxy Supplied

Androxy™ (Fluoxymesterone Tablets, USP) 10 mg are round, green, scored compressed tablets debossed with 832 and 86 and are available in bottles of 100.

Dispense in a tight, light-resistant container as defined in the USP.

Store at controlled room temperature 15 - 30°C (59 - 86°F).

Keep out of reach of children.

REV. 05-04

15021-09

Manufactured by:

UPSHER-SMITH LABORATORIES, INC.

Minneapolis, MN 55447

Androxy  fluoxymesterone  tablet

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 0832-0086 Route of Administration ORAL DEA Schedule CIII

INGREDIENTS Name (Active Moiety) Type Strength fluoxymesterone (fluoxymesterone) Active 10 MILLIGRAM  In 1 TABLET croscarmellose sodium Inactive   D&C Yellow #10 Aluminum Lake Inactive   FD&C Blue #1 Aluminum Lake Inactive   FD&C Yellow #6 Aluminum Lake Inactive   anhydrous lactose Inactive   magnesium stearate Inactive   microcrystalline cellulose Inactive   pregelatinized corn starch Inactive   sodium lauryl sulfate Inactive

Product Characteristics Color GREEN (GREEN) Score 2 pieces Shape ROUND (ROUND) Size 7mm Flavor Imprint Code 832;86 Contains          Coating false Symbol false

Packaging # NDC Package Description Multilevel Packaging 1 0832-0086-00 100 TABLET In 1 BOTTLE None

Revised: 12/2006UPSHER-SMITH LABORATORIES, INC.

More Androxy resources

• Androxy Side Effects (in more detail)
• Androxy Dosage
• Androxy Use in Pregnancy & Breastfeeding
• Androxy Drug Interactions
• Androxy Support Group
• 0 Reviews for Androxy - Add your own review/rating

• Androxy Concise Consumer Information (Cerner Multum)


• Androxy MedFacts Consumer Leaflet (Wolters Kluwer)


• Fluoxymesterone Professional Patient Advice (Wolters Kluwer)


• Fluoxymesterone Monograph (AHFS DI)

Compare Androxy with other medications

• Breast Cancer
• Breast Cancer, Palliative
• Delayed Puberty, Male
• Hypogonadism, Male
• Postmenopausal Symptoms

Alkeran

Generic Name: Melphalan
Class: Antineoplastic Agents
VA Class: AN100
CAS Number: 148-82-3

• Experience of Supervising Clinician


• 
  

  For administration only by individuals experienced in the administration of chemotherapeutic agents.^{b c}

  
  
  • Hematologic Toxicity
  
  
  • 
    

    Risk of severe bone marrow suppression (e.g., thrombocytopenia, leukopenia), resulting in bleeding and infection.^{b c} (See Hematologic Effects under Cautions.)

    
    
  
  
  • Mutagenicity and Carcinogenicity
  
  
  • 
    

    Known carcinogen.^{b c} (See Mutagenicity and Carcinogenicity under Cautions.)

    
    
  
  
  • 
    

    Produces chromosomal aberrations in vitro and in vivo; considered potentially mutagenic in humans.^{b c} (See Mutagenicity and Carcinogenicity under Cautions.)

    
    
  
  
  • Hypersensitivity Reactions
  
  
  • 
    

    Hypersensitivity reactions, including anaphylaxis, reported.^c

    
    
  
  

Introduction

Antineoplastic agent; nitrogen mustard derivative; alkylating agent.^{a b c}

Uses for Alkeran

Multiple Myeloma

Used alone and as a component of various chemotherapeutic regimens in the palliative treatment of multiple myeloma.^{a b c}

As effective as cyclophosphamide; combination of either agent with prednisone is considered treatment of choice.^{a d}

Ovarian Cancer

Palliative treatment of nonresectable epithelial ovarian cancer.^{113 122 b}

Has been administered intraperitoneally† for treatment of advanced ovarian cancer confined to the peritoneal cavity and/or associated with malignant ascites.¹⁰¹

Breast Cancer

Has been used alone or as a component of various chemotherapeutic regimens as an adjunct to surgery in the treatment of breast cancer†.^{134 135 136 138 139 a}

Melanoma

Has been used alone and in combination regimens in isolated limb perfusion† for palliative treatment of locally recurrent or unresectable in-transit metastatic melanoma† of the extremities.^{144 145 146 148}

Amyloidosis

Has been used with prednisone in the treatment of amyloidosis†.¹⁴¹

Alkeran Dosage and Administration

General

• 
  

  Adjust dosage carefully according to clinical and hematologic response, based on weekly blood counts, and tolerance of the patient to obtain optimum therapeutic results with minimum adverse effects.^{a b}

  
  


• 
  

  Consult specialized references for procedures for proper handling and disposal of antineoplastics.^{106 b c}

  
  

Administration

Administer orally or by IV infusion.^{b c}

Has been administered by regional isolation perfusion† (e.g., for melanoma†)^{144 145 146 148 149} and intraperitoneally† (e.g., for advanced ovarian cancer).¹⁰¹

Usually administered orally;^{113 123 124 125 126 127 b} however, can also be administered IV in the palliative treatment of multiple myeloma^{106 114 115 116 117 118 120} in patients in whom oral therapy is not feasible.^{106 118 120 c}

Oral Administration

Administer orally on an empty stomach.¹⁰⁸

Administer continuously (as single daily doses) or intermittently (e.g., daily for 7 days every 4–6 weeks).^{a b}

IV Administration

For drug compatibility information, see Compatibility under Stability.

Administer IV only by individuals experienced in the administration of the drug.^{a c}

Administer diluted solution slowly into a freely running IV infusion via an injection port or into a central venous line.^c

Avoid extravasation; do not administer by direct injection into a peripheral vein.^c (See Local Effects under Cautions.)

Handle cautiously (e.g., use protective gloves);^c avoid exposure during handling and preparation of IV solution.^c If skin or mucosal contact occurs, immediately wash skin or mucosa with soap and water and flush with water.^c

Reconstitution

Reconstitute vial containing 50 mg of melphalan by rapidly adding 10 mL of the diluent provided by the manufacturer with a 20-gauge or larger needle to provide a solution containing 5 mg/mL.^{106 118 119 c}

Shake vigorously until a clear solution is obtained.^{106 118 119 c} Must be diluted (immediately after reconstitution) prior to IV infusion.^a

Dilution

Immediately dilute reconstituted solution with 0.9% sodium chloride injection to a concentration not >0.45 mg/mL.^{106 118 119 c}

Rate of Administration

Administer by IV infusion over >15 minutes.^{106 119 120 c} Administration should be completed within 60 minutes of reconstitution.^{106 119 c}

Dosage

Available as melphalan and melphalan hydrochloride; dosage expressed in terms of melphalan.^{106 b c}

Consult published protocols for the dosage of melphalan and other chemotherapeutic agents and the method and sequence of administration.^a

Consider dosage adjustments based on the blood cell nadir and blood counts taken on the day of therapy.^{106 113 119} Generally, maintain leukocyte count between 3000–3500/mm³.^b

Therapeutic response may occur gradually over several months.^b 3–12 months of repeated courses or continuous therapy may be required to evaluate drug response and obtain maximum benefit from the drug.^{a b}

Adults

Multiple Myeloma

Oral

Usual initial and maintenance dosage regimen: 6 mg daily for 2–3 weeks.^{a b} Withhold therapy until leukocyte and platelet counts increase (i.e., up to 4 weeks) and then initiate maintenance therapy of 2 mg daily.^{a b} Adjust dosage, as required, to maintain a degree of bone marrow depression.^{a b}

Alternatively, 10 mg daily for 7–10 days.¹¹³ Withhold therapy until platelet and leukocyte counts exceed 100,000/mm³ and 4000/mm³, respectively, and then initiate maintenance therapy of 2 mg daily.¹¹³ Adjust dosage, as required, to between 1–3 mg daily, depending on hematologic response.¹¹³

Alternatively, 0.15 mg/kg daily for 7 days.^{a b} Withhold therapy until platelet and leukocyte counts increase (i.e., 2–6 weeks), and then initiate maintenance therapy of ≤0.05 mg/kg daily.^b Adjust dosage, as required, depending on hematologic response.^b

Alternatively, 0.25 mg/kg daily for 4 days or 0.2 mg/kg daily for 5 days, with prednisone; administer at 4–6 week-intervals, if granulocyte and platelet counts are normal.^b

IV

Usual dosage: 16 mg/m² at 2-week intervals for 4 doses.^{106 118 119 120} After satisfactory recovery from toxicity, initiate maintenance therapy of 16 mg/m² at 4-week intervals.^{106 118 119 120}

Ovarian Cancer

Oral

Usual dosage: 0.2 mg/kg daily for 5 successive days; administer at intervals of 4–5 weeks.^{113 b}

Special Populations

Hepatic Impairment

No specific dosage recommendations at this time.^{b c}

Renal Impairment

Oral

In patients with moderate to severe renal impairment, consider reducing initial dosage; however, no specific dosage recommendations at this time.^b

IV

In patients with renal impairment (BUN ≥30 mg/dL), reduce dosage by 50%. ^{106 118 120 c}

Geriatric Patients

Select dosage with caution because of age-related decreases in hepatic, renal, and/or cardiac function and potential for concomitant disease and drug therapy.^{b c}

Cautions for Alkeran

Contraindications

• 
  

  Prior resistance to melphalan therapy.^{a b c}

  
  


• 
  

  Known hypersensitivity to melphalan or any ingredient in the formulation.^{a b c}

  
  

Warnings/Precautions

Warnings

Adequate Patient Evaluation and Monitoring

Administer only under constant supervision by clinicians experienced in therapy with cytotoxic agents.^{a b c}

Hematologic Effects

Risk of dose-limiting myelosuppression, manifested principally by leukopenia and thrombocytopenia; anemia also may occur.^{a b c d}

Severe myelosuppression more common with IV melphalan than with oral melphalan.^c

Leukocyte and platelet nadirs generally occur 2–3 weeks after treatment; recovery usually occurs 4–5 weeks after treatment.^{a c} Irreversible bone marrow depression has been reported.^{106 113 119 c}

Careful hematologic monitoring required.^a Perform CBCs (leukocyte count with differential, platelet count, hemoglobin) prior to and at periodic intervals during therapy (i.e., prior to each subsequent course of oral melphalan and prior to each subsequent dose of IV melphalan).^{106 b c} Withhold therapy until leukocyte count is >3000/mm³ and platelet count is >100,000/mm³.^b

Monitor closely for symptoms of bone marrow suppression (e.g., severe infections, bleeding, symptomatic anemia).^{b c}

Use with caution in patients with compromised bone marrow reserve (i.e., prior radiation therapy or prior therapy with other cytotoxic agents).^{b c}

Positive direct Coombs’ test results and concurrent hemolytic anemia have been reported.^a

Mutagenicity and Carcinogenicity

Possible leukemia or secondary malignancies; assess risk/benefits of therapy.^{106 113 b c d}

Causes chromatid or chromosome damage in humans.^{106 113 b c}

Fetal/Neonatal Morbidity and Mortality

May cause fetal harm; teratogenicity and embryolethality demonstrated in animals.^{106 113 b c} Avoid pregnancy during therapy.^{b c} If used during pregnancy or patient becomes pregnant, apprise of potential fetal hazard.^{106 113 b c}

Fertility

Reversible and irreversible testicular suppression reported.^{b c d}

Ovarian suppression and amenorrhea reported in premenopausal females.^{106 113 b c d}

Local Effects

Extravasation may produce severe local tissue necrosis.^c

Administration by regional isolation perfusion may cause erythema and/or edema of perfused area, thrombophlebitis, necrotizing fasciitis, and varying degrees of vesiculation and tissue necrosis; amputation sometimes has been necessary.^{147 148}

Sensitivity Reactions

Hypersensitivity Reactions

Hypersensitivity reactions, including anaphylaxis, urticaria, pruritus, edema, rashes, tachycardia, bronchospasm, dyspnea, and hypotension reported in 2% of patients receiving IV melphalan and rarely in patients receiving oral melphalan.^{a b c}

If hypersensitivity reaction occurs, discontinue immediately and initiate appropriate therapy as indicated (e.g., plasma volume expanders, vasopressors, corticosteroids, antihistamines).^{106 b c}

Cross-Sensitivity

Potential for cross-sensitivity (rash) between melphalan and other alkylating agents.^a

General Precautions

Immunization.

Avoid administration of live vaccines to immunocompromised patients.^{b c}

Pulmonary Toxicity

Pulmonary embolism, sometimes fatal,¹⁴⁸ and fibrosis have been reported.^{106 113 148 d}

Specific Populations

Pregnancy

Category D.^{b c} (See Fetal/Neonatal Morbidity and Mortality and also Fertility, under Cautions.)

Lactation

Not known whether melphalan is distributed into milk;^{106 113 b c} discontinue nursing or the drug.^{106 113 b c}

Pediatric Use

Safety and efficacy not established.^{106 113}

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults.^{b c}

Renal Impairment

Increased bone marrow suppression and risk of severe leukopenia in patients with renal impairment receiving IV melphalan; dosage reduction should be considered.^c Closely monitor patients with azotemia receiving oral melphalan; oral dosage reductions may be required.^{106 118 b} (See Renal Impairment under Dosage and Administration.)

Common Adverse Effects

Bone marrow suppression, mild nausea.^b

Interactions for Alkeran

Specific Drugs

Drug	Interaction	Comments
Carmustine	Possible reduced threshold for carmustine-induced pulmonary toxicity with IV melphalan106 119 c
Cimetidine	Possible reduced serum melphalan concentrations secondary to cimetidine-induced inhibition of GI absorption of melphalan 109	Monitor for decreased melphalan activity109
Cisplatin	Possible decreased clearance of melphalan secondary to cisplatin-induced renal impairment106 119 c
Cyclosporine	Possible increased risk of cyclosporine-induced nephrotoxicity107 112 c	Monitor renal function107 112 c Consider reducing cyclosporine dosage in patients receiving high-dose melphalan112
Interferon alfa	Interferon alfa-induced fever may increase plasma elimination of melphalan110 111
Nalidixic acid	Possible increased incidence of severe hemorrhagic necrotic enterocolitis in pediatric patients106 119 c

Alkeran Pharmacokinetics

Absorption

Bioavailability

Absorption from the GI tract is incomplete and extremely variable.^{a b}

Food

Food decreases bioavailability by about 35%.¹⁰⁸

Distribution

Extent

Rapidly distributed throughout total body water;^a distributes into CSF in low concentrations.^{106 113 119 b c}

Not known whether melphalan crosses the placenta or is distributed into milk.^{a b c}

Plasma Protein Binding

About 60–90% (30% irreversibly); mainly albumin and to a lesser extent α₁-acid glycoprotein.^{106 113 119 b c}

Elimination

Metabolism

Undergoes spontaneous hydrolysis in plasma to monohydroxymelphalan and dihydroxymelphalan.^{a b c}

Elimination Route

20–35% of oral dose excreted in urine within 24 hours; 20–50% excreted in feces within 6 days.^a

Not removed by hemodialysis.^{106 113}

Half-life

Following oral administration, terminal half-life of unchanged drug is 1.5 hours;^a terminal half-lives of monohydroxymelphalan and dihydroxymelphalan are 2–3 times longer.^a

Following IV administration, terminal half-life is about 75 minutes.^{106 c}

Stability

Storage

Oral

Tablets

2–8°C.^b

Parenteral

Powder for Injection

15–30°C; protect unopened vials from light.^c

Reconstituted and diluted solutions are unstable; following reconstitution, 1% of label strength hydrolyzed every 10 minutes.^c Use within 60 minutes of reconstitution.^c

Following reconstitution, do not refrigerate; refrigeration of reconstituted solution may cause precipitation.^c

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

Parenteral

Solution Compatibility^HID

¹ Incompatible by standard definition; recommended for dilution with use in shorter periods of time.

Incompatible

Dextrose 5% in water

Ringer’s injection, lactated

Sodium chloride 0.9%1

Drug Compatibility

Y-Site CompatibilityHID

Compatible

Acyclovir sodium

Amikacin sulfate

Aminophylline

Ampicillin sodium

Aztreonam

Bleomycin sulfate

Bumetanide

Buprenorphine HCl

Butorphanol tartrate

Calcium gluconate

Carboplatin

Carmustine

Cefazolin sodium

Cefepime HCl

Cefotaxime sodium

Cefotetan disodium

Ceftazidime

Ceftizoxime sodium

Ceftriaxone sodium

Cefuroxime sodium

Cimetidine HCl

Cisplatin

Clindamycin phosphate

Co-trimoxazole

Cyclophosphamide

Cytarabine

Dacarbazine

Dactinomycin

Daunorubicin HCl

Dexamethasone sodium phosphate

Diphenhydramine HCl

Doxorubicin HCl

Doxycycline hyclate

Droperidol

Enalaprilat

Etoposide

Famotidine

Filgrastim

Floxuridine

Fluconazole

Fludarabine phosphate

Fluorouracil

Furosemide

Gallium nitrate

Ganciclovir sodium

Gentamicin sulfate

Granisetron HCl

Haloperidol lactate

Heparin sodium

Hydrocortisone sodium phosphate

Hydrocortisone sodium succinate

Hydromorphone HCl

Hydroxyzine HCl

Idarubicin HCl

Ifosfamide

Imipenem–cilastatin sodium

Lorazepam

Mannitol

Mechlorethamine HCl

Meperidine HCl

Mesna

Methotrexate sodium

Methylprednisolone sodium succinate

Metoclopramide HCl

Metronidazole

Mitomycin

Mitoxantrone HCl

Morphine sulfate

Nalbuphine HCl

Ondansetron HCl

Pentostatin

Potassium chloride

Prochlorperazine edisylate

Promethazine HCl

Ranitidine HCl

Sodium bicarbonate

Streptozocin

Teniposide

Thiotepa

Ticarcillin disodium–clavulanate potassium

Tobramycin sulfate

Vancomycin HCl

Vinblastine sulfate

Vincristine sulfate

Vinorelbine tartrate

Zidovudine

Incompatible

Amphotericin B

Chlorpromazine HCl

ActionsActions

• 
  

  Interferes with DNA replication and transcription of RNA, and ultimately results in the disruption of nucleic acid function.^a

  
  


• 
  

  Active against both resting and rapidly dividing tumor cells.^{b c}

  
  


• 
  

  Possesses some immunosuppressive activity.^a

  
  

Advice to Patients

• 
  

  Risk of bone marrow suppression, hypersensitivity reactions, infertility, pulmonary toxicities, and secondary malignancies.^{106 113 b c d}

  
  


• 
  

  Advise patients that oral melphalan should be taken on an empty stomach.¹⁰⁸

  
  


• 
  

  Importance of close medical supervision of patients receiving melphalan.^{a b c}

  
  


• 
  

  Importance of informing clinicians if rash, bleeding, fever, persistent cough, nausea, vomiting, amenorrhea, weight loss, or unusual lumps or masses occur.^{b c}

  
  


• 
  

  Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed; necessity for clinicians to advise women to avoid pregnancy.^{b c}

  
  


• 
  

  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as concomitant illnesses.^{b c}

  
  


• 
  

  Importance of informing patients of other important precautionary information.^b (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Melphalan

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Tablets	2 mg	Alkeran (with povidone; scored)	Celgene

Melphalan Hydrochloride

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Parenteral	For injection	50 mg (of melphalan)	Alkeran (with povidone and with diluent containing alcohol 0.52 mL, propylene glycol, and sodium citrate)	Celgene

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 03/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Alkeran 2MG Tablets (CELGENE CORP): 50/$245.98 or 150/$719.94

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions February 2008. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

Only references cited for selected revisions after 1984 are available electronically.

84. Einhorn N. Acute leukemia after chemotherapy (melphalan). Cancer. 1978; 41:444-7. [IDIS 101911] [PubMed 272946]

100. McElwain TJ, Powles RL. High-dose intravenous melphalan for plasma-cell leukaemia and myeloma. Lancet. 1983; 2:822-4. [IDIS 176847] [PubMed 6137651]

101. Howell SB, Pfeifle CE, Olshen RA. Intraperitoneal chemotherapy with melphalan. Ann Intern Med. 1984; 101:14-8. [IDIS 188162] [PubMed 6732077]

102. Greene MH, Harris EL, Gershenson DM et al. Melphalan may be a more potent leukemogen than cyclophosphamide. Ann Intern Med. 1986; 105:360-7. [IDIS 220340] [PubMed 3740675]

103. Fisher B, Rockette H, Fisher ER et al. Leukemia in breast cancer patients following adjuvant chemotherapy or postoperative radiation: the NSABP experience. J Clin Oncol. 1985; 3:1640-58. [PubMed 3906049]

104. Ovarian epithelial cancer. From: PDQ. Physician data query (database). Bethesda, MD: National Cancer Institute; 2000 Oct.

105. Wadler S, Yeap B, Vogl S et al. Randomized trial of initial therapy with melphalan versus cisplatin-based combination chemotherapy in patients with advanced ovarian carcinoma: initial and long term results—Eastern Cooperative Oncology Group Study E2878. Cancer. 1996; 77:733-42. [IDIS 363630] [PubMed 8616766]

106. Glaxo Wellcome. Alkeran (melphalan hydrochloride) for injection prescribing information. Research Triangle Park, NC; 1998 Aug.

107. Melphalan (Alkeran) interactions: cyclosporine (Sandimmune). In: Hansten PD, Horn JR. Drug interactions and updates. Vancouver, WA: Applied Therapeutics, Inc; 1993:411.

108. Melphalan (Alkeran) interactions: food. In: Hansten PD, Horn JR. Drug interactions and updates. Vancouver, WA: Applied Therapeutics, Inc; 1993:411.

109. Melphalan (Alkeran) interactions: H₂ receptor antagonists. In: Hansten PD, Horn JR. Drug interactions and updates. Vancouver, WA: Applied Therapeutics, Inc; 1993:410.

110. Antineoplastic drug interactions: melphalan (Alkeran). In: Hansten PD, Horn JR. Drug interactions and updates. Vancouver, WA: Applied Therapeutics, Inc; 1993:410.

111. Ehrsson H, Eksborg S, Wallin I et al. Oral melphalan pharmacokinetics: influence of interferon-induced fever. Clin Pharmacol Ther. 1990; 47:86-90. [IDIS 262868] [PubMed 2295223]

112. Cyclosporine/melphalan. In: Tatro DS, Olin BR, Hebel SK eds. Drug interaction facts. St. Louis: JB Lippincott Co; 1993(January):237.

113. Glaxo Wellcome. Alkeran (melphalan) 2-mg scored tablets prescribing information. Research Triangle Park, NC; 1999 Aug.

114. Cooper MR, McIntyre OR, Propert KJ et al. Single, sequential, and multiple alkylating agent therapy for multiple myeloma: a CALGB study. J Clin Oncol. 1986; 4:1331-9. [PubMed 3528403]

115. Cornwell GG III, Pajak TF, Kochwa S et al. Vincristine and prednisone prolong the survival of patients receiving intravenous or oral melphalan for multiple myeloma: Cancer and Leukemia Group B experience. J Clin Oncol. 1988; 6:1481-90. [PubMed 3047338]

116. Harley JB, Pajak TF, McIntyre OR et al. Improved survival of increased-risk myeloma patients on combined triple-alkylating-agent therapy: a study of the CALGB. Blood. 1979; 54:13-22.

117. Osterborg A, Ahre A, Björkholm M et al. Oral versus intravenous melphalan and prednisone treatment in multiple myeloma stage II: a randomized study from the Myeloma Group of Central Sweden. Acta Oncol. 1990; 29:727-31. [PubMed 2223143]

118. Burroughs Wellcome. General questions and answers on Alkeran (melphalan HCl) for injection (ALK1-2). Research Triangle Park, NC: 1993 Apr 16.

119. Burroughs Wellcome. Formulary information: new Alkeran for injection (melphalan hydrochloride) 50 mg vial. Research Triangle Park, NC: 1993 Feb.

120. Burroughs Wellcome. Use of Alkeran (melphalan HCl) for injection in the treatment of multiple myeloma (ALK4-2). Research Triangle Park, NC: 1993 Apr 15.

121. Burroughs Wellcome, Research Triangle Park, NC: Personal communication.

122. Anon. Drugs of choice for cancer chemotherapy. Med Lett Drugs Ther. 2000; 42:83-92. [PubMed 10994034]

123. Dunbar CE, Nienhuis AW. Multiple myeloma: new approaches to therapy. JAMA. 1993; 269:2412-6. [IDIS 313813] [PubMed 7683062]

124. Österborg A, Björkholm M, Björeman M et al. Natural interferon-α in combination with melphalan/prednisone versus melphalan/prednisone in the treatment of multiple myeloma stages II and III: a randomized study from the myeloma group of central Sweden. Blood. 1993; 81:1428-34. [IDIS 312028] [PubMed 8453092]

125. MacLennan ICM, Chapman C, Dunn J et al. Combined chemotherapy with ABCM versus melphalan for treatment of myelomatosis. Lancet. 1992; 339:200-5. [IDIS 290524] [PubMed 1346171]

126. Gregory WM, Richards MA, Malpas JS. Combined chemotherapy versus melphalan and prednisolone for treatment of myelomatosis. Lancet. 1992; 339:1353-4. [PubMed 1350010]

127. Clarke M, Gray R, Dunn J et al. Combination chemotherapy for myelomatosis. Lancet. 1992; 340:433. [IDIS 300719] [PubMed 1353589]

128. Breast cancer. From: PDQ. Physician data query (database). Bethesda, MD: National Cancer Institute; 1995 Dec 12.

129. Early Breast Cancer Trialists’ Collaborative Group. Systemic treatment of early breast cancer by hormonal, cytotoxic, or immune therapy: 133 randomized trials involving 31,000 recurrences and 24,000 deaths among 75,000 women. Lancet. 1992; 339:1-15,71-85. [IDIS 290641] [PubMed 1345950]

130. Bonadonna G, Brusamolino E, Valagussa P et al. Combination chemotherapy as an adjuvant treatment in operable breast cancer. N Engl J Med. 1976; 294:405-10. [PubMed 1246307]

131. Bonadonna G, Valagussa P, Moliterni A et al. Adjuvant cyclophosphamide, methotrexate, and fluorouracil in node-positive breast cancer: the results of 20 years of follow-up. N Engl J Med. 1995; 332:901-6. [IDIS 344958] [PubMed 7877646]

132. Wood WC, Budman DR, Korzun AH et al. Dose and dose intensity of adjuvant chemotherapy for stage II, node-positive breast carcinoma. N Engl J Med. 1994; 330:1253-9. [IDIS 329429] [PubMed 8080512]

133. Bonadonna G, Zambetti M, Valagussa P. Sequential or alternating doxorubicin and CMF regimens in breast cancer with more than three positive nodes: ten-year results. JAMA. 1995; 273:542-7. [IDIS 342272] [PubMed 7837388]

134. Fisher B, Redmond C, Wickerman DL et al. Doxorubicin-containing regimens for the treatment of stage II breast cancer: the National Surgical Adjuvant Breast and Bowel Project experience. J Clin Oncol. 1989; 7:572-82. [PubMed 2651576]

135. Fisher B, Glass A, Redmond C et al. l-Phenylalanine mustard (l-PAM) in the management of breast cancer: an update of earlier findings and a comparison with those utilizing l-PAM plus fluorouracil (5-FU). Cancer. 1977; 39(Suppl):2883-903. [PubMed 194679]

136. Fisher ER, Redmond C, Fisher B. Pathologic findings from the National Surgical Adjuvant Breast Cancer Project. VIII. Relationship of chemotherapeutic responsiveness to tumor differentiation. Cancer. 1983; 51:181-91. [IDIS 165062] [PubMed 6821810]

137. Fisher B, Redmond C, Brown A et al. Adjuvant chemotherapy with and without tamoxifen in the treatment of primary breast cancer: 5-year results from the National Surgical Adjuvant Breast and Bowel Project Trial. J Clin Oncol. 1986; 4:459-71. [PubMed 2856857]

138. Rivkin SE, Green S, Metch B et al. Adjuvant CMFVP versus melphalan for operable breast cancer with positive axillary nodes: 10-year results of a Southwest Oncology Group Study. J Clin Oncol. 1989; 7:1229-38. [PubMed 2671283]

139. Fisher B, Redmond C, Brown A et al. Influence of tumor estrogen and progesterone receptor levels on the response to tamoxifen and chemotherapy in primary breast disease. J Clin Oncol. 1983; 1:227-41. [PubMed 6366135]

140. Food and Drug Administration. Orphan designations pursuant to Section 526 of the Federal Food and Cosmetic Act as amended by the Orphan Drug Act (P.L. 97-414), to June 28, 1996. Rockville, MD; 1996 Jul.

141. Kyle RA, Gertz MA, Greipp PR et al. A trial of three regimens for primary amyloidosis: colchicine alone, melphalan and prednisone, and melphalan, prednisone, and colchicine. N Engl J Med. 1997; 336:1202-7. [IDIS 383378] [PubMed 9110907]

142. Falk RH, Comenzo RL, Skinner M. The systemic amyloidoses. N Engl J Med. 1997; 337:898-909. [IDIS 391785] [PubMed 9302305]

143. Skinner M, Anderson JJ, Simms R et al. Treatment of 100 patients with primary amyloidosis: a randomized trial of melphalan, prednisone, and colchicine versus colchicine only. Am J Med. 1996; 100:290-8. [IDIS 362735] [PubMed 8629674]

144. Melanoma. From: PDQ. Physician data query (database). Bethesda, MD: National Cancer Institute; 2000 Aug.

145. Duran Garcia E, Santolaya R, Requena T. Treatment of malignant melanoma. Ann Pharmacother. 1999; 33:730-8. [IDIS 428254] [PubMed 10410188]

146. Houghton A, Coit D, Bloomer W et al. NCCN melanoma practice guidelines. National Comprehensive Cancer Network. Oncology (Huntingt). 1998; 12:153-77.

147. Koops HS, Vaglini M, Suciu S et al. Prophylactic isolated limb perfusion for localized, high-risk limb melanoma: results of a multicenter randomized phase III trial. European Organization for Research and Treatment of Cancer Malignant Melanoma Cooperative Group Protocol 18832, the World Health Organization Melanoma Program Trial 15, and the North American Perfusion Group Southwest Oncology Group-8593. J Clin Oncol. 1998; 16:2906-12. [IDIS 414236] [PubMed 9738557]

148. Hafstrom L, Rudenstam CM, Blomquist E et al. Regional hyperthermic perfusion with melphalan after surgery for recurrent malignant melanoma of the extremities. Swedish Melanoma Study Group. J Clin Oncol. 1991; 9:2091-4. [PubMed 1960549]

149. Fraker DL, Alexander HR, Andrich M et al. Treatment of patients with melanoma of the extremity using hyperthermic isolated limb perfusion with melphalan, tumor necrosis factor, and interferon gamma: results of a tumor necrosis factor dose-escalation study. J Clin Oncol. 1996; 14:479-89. [IDIS 362040] [PubMed 8636761]

a. AHFS drug information 2007. McEvoy GK, ed. Melphalan. Bethesda, MD: American Society of Health-System Pharmacists; 2007:1125-8.

b. Glaxo Wellcome. Alkeran (melphalan hydrochloride) tablets prescribing information. Research Triangle Park, NC; 2004 Nov.

c. Glaxo Wellcome. Alkeran (melphalan hydrochloride) for injection prescribing information. Research Triangle Park, NC; 2007 Mar.

d. Treatment Guidelines from the Medical Letter Drugs of Choice for Cancer. Abramowicz M, ed. New Rochelle, NY: The Medical Letter, Inc.; 2003 Mar: 94.

HID. Trissel LA. Handbook on injectable drugs. 14th ed. Bethesda, MD: American Society of Health-System Pharmacists; 2007:1046-53.

More Alkeran resources

• Alkeran Side Effects (in more detail)
• Alkeran Use in Pregnancy & Breastfeeding
• Drug Images
• Alkeran Drug Interactions
• Alkeran Support Group
• 0 Reviews for Alkeran - Add your own review/rating

• Alkeran Prescribing Information (FDA)


• Alkeran MedFacts Consumer Leaflet (Wolters Kluwer)


• Alkeran Concise Consumer Information (Cerner Multum)


• Alkeran Advanced Consumer (Micromedex) - Includes Dosage Information


• Melphalan Prescribing Information (FDA)


• Melphalan Professional Patient Advice (Wolters Kluwer)

Compare Alkeran with other medications

• Multiple Myeloma
• Ovarian Cancer