ANDROGENS (Systemic)

Some commonly used brand names are:

In the U.S.?

• Androderm ³
• AndroGel ³
• Android ²
• Android-F ¹
• Andro L.A. 200 ³
• Andronate 100 ³
• Andronate 200 ³
• Andropository 200 ³
• Andryl 200 ³
• Delatest ³
• Delatestryl ³
• Depotest ³
• Depo-Testosterone ³
• Everone 200 ³
• Halotestin ¹
• ORETON Methyl ²
• T-Cypionate ³
• Testamone 100 ³
• Testaqua ³
• Testex ³
• Testoderm ³
• Testoderm with Adhesives ³
• Testoderm TTS ³
• Testopel Pellets ³
• Testred ²
• Testred Cypionate 200 ³
• Testrin-P.A. ³
• Virilon ²
• Virilon IM ³

In Canada?

• Andriol ³
• Delatestryl ³
• Depo-Testosterone Cypionate ³
• Halotestin ¹
• Malogen in Oil ³
• Metandren ²
• Scheinpharm Testone-Cyp ³

Category

• Androgen?Fluoxymesterone; Methyltestosterone; Testosterone
• Antianemic?Fluoxymesterone; Testosterone
• Antineoplastic?Fluoxymesterone; Methyltestosterone; Testosterone

Description

Androgens (AN-droe-jens) are male hormones. Someandrogens are naturally produced in the body and are necessary for the normalsexual development of males.

Androgens are used for several reasons, such as:

• to replace the hormone when the body is unable to produce enoughon its own.
• to stimulate the beginning of puberty in certain boys who are latestarting puberty naturally.
• to treat certain types of breast cancer in females.

In addition, some of these medicines may be used for other conditions asdetermined by your doctor.

Androgens are available only with your doctor's prescription, in the followingdosage forms:

Oral
• Fluoxymesterone
  • Tablets (U.S. and Canada)
• Methyltestosterone
  • Capsules (U.S.)
  • Tablets (U.S. and Canada)
• Testosterone
  • Capsules (Canada)

Parenteral
• Testosterone
  • Injection (U.S. and Canada)

Subcutaneous
• Testosterone
  • Implants (Pellets) (U.S.)

Topical
• Testosterone
  • Gel
  • Ointment
  • Transdermal systems (skin patches) (U.S.)

Before Using This Medicine

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

Allergies?Tell your doctor if you have ever had any unusual orallergic reaction to androgens. Also tell your health care professional ifyou are allergic to any other substances, such as foods, preservatives, ordyes.

Pregnancy?Androgens are not recommended during pregnancy. Whengiven to pregnant women, the medicine has caused male features to developin female babies.

Breast-feeding?Use is not recommended in nursing mothers, sinceandrogens may pass into the breast milk and may cause unwanted effects inthe nursing baby, such as premature (too early) sexual development in malesand development of male features in female babies.

Children?Androgens may cause children to stop growing. Inaddition, androgens may make male children develop too fast sexually and maycause male-like changes in female children.

Older adults?When older male patients are treated with androgens,they may have an increased risk of enlarged prostate (a male gland) or theirexisting prostate cancer may get worse. For these reasons, a prostate examinationand a blood test to check for prostate cancer is often done before androgensare prescribed for men over 50 years of age. These examinations may be repeatedduring treatment.

Other medicines?Although certain medicines should not be usedtogether at all, in other cases two different medicines may be used togethereven if an interaction might occur. In these cases, your doctor may want tochange the dose, or other precautions may be necessary. When you are takingandrogens, it is especially important that your health care professional knowif you are taking any of the following:

• Acetaminophen (e.g., Tylenol) (with long-term, high-dose use) or
• Amiodarone (e.g., Cordarone) or
• Anabolic steroids (nandrolone [e.g., Anabolin], oxandrolone [e.g.,Anavar], oxymetholone [e.g., Anadrol], stanozolol [e.g., Winstrol]) or
• Anti-infectives by mouth or by injection (medicines for infection)or
• Antithyroid agents (medicines for overactive thyroid) or
• Carbamazepine (e.g., Tegretol) or
• Carmustine (e.g., BiCNU) or
• Chloroquine (e.g., Aralen) or
• Dantrolene (e.g., Dantrium) or
• Daunorubicin (e.g., Cerubidine) or
• Disulfiram (e.g., Antabuse) or
• Divalproex (e.g., Depakote) or
• Estrogens (female hormones) or
• Etretinate (e.g., Tegison) or
• Gold salts (medicines for arthritis) or
• Hydroxychloroquine (e.g., Plaquenil) or
• Mercaptopurine (e.g., Purinethol) or
• Methotrexate (e.g., Mexate) or
• Methyldopa (e.g., Aldomet) or
• Naltrexone (e.g., Trexan) (with long-term, high-dose use) or
• Oral contraceptives (birth control pills) containing estrogen or
• Phenothiazines (acetophenazine [e.g., Tindal], chlorpromazine [e.g.,Thorazine], fluphenazine [e.g., Prolixin], mesoridazine [e.g., Serentil],perphenazine [e.g., Trilafon], prochlorperazine [e.g., Compazine], promazine[e.g., Sparine], promethazine [e.g., Phenergan], thioridazine [e.g., Mellaril],trifluoperazine [e.g., Stelazine], triflupromazine [e.g., Vesprin], trimeprazine[e.g., Temaril]) or
• Phenytoin (e.g., Dilantin) or
• Plicamycin (e.g., Mithracin) or
• Valproic acid (e.g., Depakene)?Use of these medicines withandrogens may increase the chance of liver problems. Your doctor may wantyou to have extra blood tests that check your liver while you are taking anyof these medicines with an androgen

• Anticoagulants (blood thinners)?Androgens can increase theeffect of these medicines and possibly cause excessive bleeding

Other medical problems?The presence of other medicalproblems may affect the use of androgens. Make sure you tell your doctor ifyou have any other medical problems, especially:

• Breast cancer (in males) or
• Prostate cancer?Androgens can cause growth of these tumors

• Breast cancer (in females)?Androgens may cause high calciumlevels in the blood to become worse

• Diabetes mellitus (sugar diabetes)?Androgens can increase ordecrease blood sugar levels. Careful monitoring of blood glucose should bedone

• Edema (swelling of face, hands, feet, or lower legs) or
• Kidney disease or
• Liver disease?These conditions can be worsened by the fluidretention (keeping too much water in the body) that can be caused by androgens.Also, liver disease can prevent the body from removing the medicine from thebloodstream as fast as it normally would. This could increase the chance ofside effects occurring

• Enlarged prostate?Androgens can cause further enlargement ofthe prostate

• Heart or blood vessel disease?Androgens can make these conditionsworse because androgens may increase blood cholesterol levels. Also, androgenscan cause fluid retention (keeping too much water in the body), which alsocan worsen heart or blood vessel disease

Proper Use of This Medicine

Take this medicine only as directed.Do not take more of it and do not take it more often than your doctor ordered. Doing so may increase the chance of side effects.

There are two types of testosterone skin patches. The matrix-type is appliedto skin of the scrotum. The reservoir-type is never applied to the skin ofthe scrotum. It is applied to other parts of the body. Be sure you know whichtype you are using so that you will apply it properly. These skin patchescome with patient directions. Read them carefully before using the patch.

For patients taking fluoxymesterone or methyltestosterone:

• Take this medicine with food to lessen possible stomach upset, unlessotherwise directed by your doctor.

For patients using the matrix-type skin patch of testosterone (Testoderm or Testoderm with Adhesives):

• You must apply the patch to the scrotum because the medicine easilypasses into your body at this area. Other areas of your skin are too thickfor the medicine to work properly.
• Wash and dry your hands thoroughly before and after handling thepatch.
  • Before applying the patch:
    • Clean and dry your scrotum.
    • You should also dry-shave this area once a week by using a shaveronly (no soap or water). To dry-shave, stretch the skin of your scrotum withyour fingers. Use short gentle strokes with no pressure on the razor to removethe hair. Do not use shaving cream or hair-removing creams (e.g., Nair).
    • You may sit with your legs apart or stand while applying the patch.
  • To apply the patch:
    • Open the wrapper containing the patch at the point shown on the package.
    • Carefully remove the patch from its protective plastic liner by peelingthe patch from the liner starting at the corner.
    • Warm your scrotum for a few seconds before applying the patch toachieve the best results. Stretch the skin of your scrotum gently to removethe folds by pulling the penis up and to the side. Another way is to pullyour scrotum down. Use your first and middle fingers to stretch the skin ofyour scrotum.
    • Place the shiny side of the patch onto the warm stretched skin ofyour scrotum.
    • Press the shiny side of the patch firmly in place with the palm ofyour hand for about 10 seconds. Make sure there is good contact, especiallyaround the edges. The patch should stick to your scrotum and show the naturalwrinkles of your scrotum.
    • Put on comfortable, close-fitting briefs (underwear) after applyingthe patch.
    • If a patch becomes loose or falls off, you may reapply it or discardit and apply a new patch.
  • To remove the skin patch:
    • Gently peel the patch from the skin.
    • You may reuse the patch after removing it for swimming, bathing,showering, or sexual activity. First, remove the patch and place the shiny(sticky) side up on a counter. Before you reapply the patch, be sure the skinon your scrotum is dry. Then, follow the directions to reapply the patch.
    • When the wearing period is over, fold the patch in half with thesticky sides together. Place the folded, used patch in its protective pouchor in aluminum foil. Be sure to throw it away out of the reach of childrenand pets.

For patients using the reservoir-type skin patch oftestosterone (Androderm or Testoderm TTS):

• Apply the patch called Androderm to theabdomen, back, thighs, or arms. Apply the patch called Testoderm TTS to the back, arms, or upper buttocks. Do not apply these patches to the scrotum.
• Do not apply the patch to areas of the body that seem bony, suchas the top of the shoulders or near the elbows, or to areas that may haveto support your body while sleeping or sitting, such as the hips or shoulderblades. Apply each new patch to a different place. Do not reapply a patchto the same area of skin for 7 days.
• Wash and dry your hands thoroughly before and after handling thepatch.
  • Before applying the patch, clean and dry the application site.
  • To apply the patch:
    • Open the wrapper containing the patch at the point shown on the package.
    • Carefully remove the patch from its protective plastic liner by peelingthe patch from the liner, starting at the corner.
    • Place the shiny side of the patch onto the skin.
    • Press the shiny side of the patch firmly in place with the palm ofyour hand for about 10 seconds. Be sure there is good contact, especiallyaround the edges.
    • If a patch becomes loose or falls off, you may reapply it or discardit and apply a new patch.
  • To remove the skin patch:
    • Gently peel the patch from the skin.
    • You do not need to remove this patch for swimming, bathing, showering,or sexual activity.
    • When the wearing period is over, fold the patch in half with thesticky sides together. Place the folded, used patch in its protective pouchor in aluminum foil. Be sure to throw it away out of the reach of childrenand pets.

Dosing?The dose ofthese medicines will be different for different patients. Follow your doctor's orders or the directions on the label. The followinginformation includes only the average doses of these medicines. If your dose is different, do not change it unless your doctor tellsyou to do so.

The number of capsules or tablets that you take depends on the strengthof the medicine. Also, the number of doses you take eachday, the time between doses, and the length of time you take the medicinedepend on the medical problem for which you are taking the androgen.

For fluoxymesterone
• For oral dosage form (tablets):
  • For androgen hormone replacement in men:
    • Adults?5 milligrams (mg) one to four times a day.
  • For treatment of breast cancer in women:
    • Adults?10 to 40 mg a day in divided doses.
  • For treatment of delayed sexual development in boys:
    • Children?2.5 to 10 mg a day for four to six months.

For methyltestosterone
• For oral dosage forms (capsules or tablets):
  • For androgen hormone replacement in men:
    • Adults?10 to 50 milligrams (mg) a day.
  • For treatment of breast cancer in women:
    • Adults?50 mg one to four times a day. Your doctor may decreaseyour dose to 50 mg two times a day after two to four weeks.
  • For treatment of delayed sexual development in boys:
    • Children?5 to 25 mg a day for four to six months.

For testosterone
• For injection dosage form:
  • For androgen hormone replacement in men:
    • Adults?25 to 50 milligrams (mg) injected into a muscle twoor three times a week.
  • For treatment of breast cancer in women:
    • Adults?50 to 100 mg injected into a muscle three times a week.
  • For treatment of delayed sexual development in boys:
    • Children?Up to 100 mg injected into a muscle once a month forfour to six months.
• For subcutaneous dosage form (implants):
  • For androgen hormone replacement in men:
    • Adults?150 to 450 milligram (mg) (two to six implants) insertedinto the skin every three to six months.
  • For treatment of delayed sexual development in boys:
    • Children?Use and dose must be determined by your doctor.
• For topical dosage forms :
  • For androgen hormone replacement in men:
    When using the brand name AndroGel 1% testosterone gel
    • Adults?The recommended starting dose is 5 gramsapplied once daily (preferably in the morning) to clean, dry , intact skinof the shoulders and upper arms and/or abdomen. Allow the application sitesto dry prior to dressing and wash hands with soap and water after application.
    • Children?Use and dose must be determined by your doctor.
    When using the brand name Testoderm or Testoderm with Adhesives patches(matrix-type)
    • Adults?4 or 6 mg (one patch) applied to your scrotum once aday at about 8 a.m. The patch should be worn at least twenty-two of the twenty-fourhours in a day.
    • Children?Use and dose must be determined by your doctor.
    When using the brand name Androderm patches (reservoir-type)
    • Adults and teenagers 15 years of age and older?2.5 to 7.5 mg(one to three patches) applied to the abdomen, back, thighs, or upper armsonce a day at about 10 p.m. The patch(es) should be worn for twenty-four hoursa day.
    • Children up to 15 years of age?Use and dose must be determinedby your doctor.
    When using the brand name Testoderm TTS patches (reservoir-type)
    • Adults?5 mg (one patch) applied to the back, arms, or upperbuttocks once a day at about 8 a.m. Your doctor may increase your dose ifnecessary. The patch should be worn at least twenty-two of the twenty-fourhours in a day.
    • Children up to 18 years of age?Use and dose must be determinedby your doctor.

For testosterone cypionate or testosterone enanthate
• For injection dosage form:
  • For androgen hormone replacement in men:
    • Adults?50 to 400 milligrams (mg) injected into a muscle everytwo to four weeks.
  • For treatment of breast cancer in women:
    • Adults?200 to 400 mg injected into a muscle every two to fourweeks.
  • For treatment of delayed sexual development in boys:
    • Children?Up to 100 mg injected into a muscle once a month forfour to six months.

For testosterone propionate
• For injection dosage form:
  • For androgen hormone replacement in men:
    • Adults?25 to 50 milligrams (mg) injected into a muscle twoor three times a week.
  • For treatment of breast cancer in women:
    • Adults?50 to 100 mg injected into a muscle three times a week.
  • For treatment of delayed sexual development in boys:
    • Children?Up to 100 milligrams injected into a muscle once amonth for four to six months.

For testosterone undecanoate
• For oral dosage form (capsules):
  • For androgen hormone replacement in men:
    • Adults?120 to 160 milligrams (mg) divided into two doses aday taken with meals for two to three weeks. Then dose is reduced to 40 to120 mg a day, taken with meals, and divided into 2 doses a day when possible.

Missed dose?For oral dosage forms: If you miss a dose of thismedicine and your dosing schedule is:

• One dose a day?Take, use, or apply the missed dose as soonas possible. However, if you do not remember it until the next day, skip themissed dose and go back to your regular dosing schedule. Do not double doses.
• More than one dose a day?Take or use the missed dose as soonas possible. However, if it is almost time for your next dose, skip the misseddose and go back to your regular dosing schedule. Do not double doses.

For topical dosage forms (patches): If you miss a dose of this medicineor your patch falls off within 12 hours after applying it and cannot be reapplied,skip the rest of the dose and go back to your regular dosing schedule. Donot double doses.

If you have any questions about this, check with your doctor.

Storage?To store this medicine:

• Keep out of the reach of children.
• Store away from heat and direct light.
• Do not store in the bathroom, near the kitchen sink, or in otherdamp places. Heat or moisture may cause the medicine to break down.
• Keep the injection form of this medicine from freezing.
• Do not keep outdated medicine or medicine no longer needed. Be surethat any discarded medicine is out of the reach of children.

Precautions While Using This Medicine

Your doctor should check your progress at regularvisits to make sure this medicine does not cause unwanted effects.

For patients with diabetes mellitus (sugar diabetes):

• This medicine may affect blood sugar levels. If you notice a changein the results of your blood or urine sugar tests or if you have any questions,check with your doctor.

For patients using the brand name Testoderm patches(matrix-type):

• In some cases, this medicine can pass from you to your sexual partner.Tell your doctor if your female sex partner has a great increase in acne.Also, tell your doctor if her hair begins to grow in odd places like her upperlip, chest, or back. This will not occur if you are using the reservoir-typeskin patch because it is not applied to the scrotum and because it has a protectiveliner.

For patients using the brand name Androgel

• Wait 5 or 6 hours after applying the gel before showering or swimming.
• Gel contains alcohol which is flammable- avoid fire, flame or smokinguntil the gel is dried.

Side Effects of This Medicine

Discuss these possible effects with your doctor:

• Tumors of the liver, liver cancer, or peliosis hepatis (a form ofliver disease) have occurred during long-term, high-dose therapy with androgens.Although these effects are rare, they can be very serious and may cause death.
• Androgens can stimulate existing prostate cancer in men who alreadyhave it but have not yet been diagnosed. Also, the prostate (a male gland)may become enlarged. Enlargement of the prostate does not mean that cancerwill develop. If enlargement occurs and you have difficulty in urinating,it is a good idea to be checked by your doctor.
• When androgens are used in women, especially in high doses, male-likechanges may occur, such as hoarseness or deepening of the voice, unnaturalhair growth, or unusual hair loss. Most of these changes will go away if themedicine is stopped as soon as the changes are noticed. However, some changes,such as voice changes or enlarged clitoris, may not go away.
• When androgens are used in high doses in males, they interfere withthe production of sperm. This effect is usually temporary and only happensduring the time you are taking the medicine. However, discuss this possibleeffect with your doctor if you are planning on having children.

Alongwith its needed effects, a medicine may cause some unwanted effects. Althoughnot all of these side effects appear very often, when they do occur they mayrequire medical attention. Check with your doctor as soon as possible if anyof the following side effects occur:

More common

For females only

Acne or oily skin; decreased breastsize; irregular menstrual cycles; hoarseness or deepening of voice; increase in sizeof female genitals; increase in unnatural hair growthor male pattern baldness

Note:

These symptoms may occur in females whose male sexual partner usesa scrotal patch.

For males only

Blistering of skin under patch (especially when the nonscrotalpatch is applied to bony areas of the skin); breastsoreness or enlargement; frequent or continuing erectionof penis lasting up to 4 hours or painful penile erections lasting longerthan 4 hours; frequent urge to urinate; itching or redness of skin under patch (less likely with nonscrotalpatch) or at site of implants, mild to severe

For prepubertal boys only

Acne; early growth of pubic hair; enlargement of penis; frequent or continuingerections

Less common

For males or females

Dizziness; frequent or continuing headache; lack or loss of strength; nausea; overall body flushing, redness, or itchingof skin; rapid weight gain; rapidly changing moods, such as depersonalization, dysphoria, euphoria, depression,paranoia, and quick to react or overreact emotionally; swelling of feet or lower legs; unusual bleeding; unusual tiredness; vomiting; yellow skin or eyes (occurring with fluoxymesteroneor methyltestosterone more often than with testosterone)

For females with breast cancer or bedridden males or females?inaddition to the side effects listed above

Confusion or mental depression; constipation; increased thirst; increasedurge to urinate or increased amount of urine

For males only

Black, tarry stools; burning sensationor hardening or thickening of skin under patch; chills; continuing pain at site of implants; difficulty in urinating; itching, skinredness, or rash under patch, severe (less likely with nonscrotal patch); pain in scrotum or groin; vomiting ofblood or material that looks like coffee grounds

Rare

For males or females?more likely with oral androgens or long-termor high doses of androgens

Abdominal or stomach pain, continuing; bad breath odor, continuing; black, tarry or light-coloredstools or dark urine; fever; hives; loss of appetite, continuing; mood or mental changes; purple or redspots on body or inside the mouth or nose; sore throat; swelling, pain, or tenderness of abdomen; vomiting of blood

Other sideeffects may occur that usually do not need medical attention. These side effectsmay go away during treatment as your body adjusts to the medicine. However,check with your doctor if any of the following side effects continue or arebothersome:

Less common

For males and females

Acne, mild; diarrhea; hair loss or thinning of hair; increase in pubichair growth; infection, pain, redness, or other irritationat site of injection; decrease or increase in sexualdesire or drive; nervousness; stomach pain; trouble in sleeping

For males only

Decrease in testicle size; infection,pain, redness, swelling, sores, or other skin irritation underneath patch

Otherside effects not listed above may also occur in some patients. If you noticeany other effects, check with your doctor.

Additional Information

Once a medicine has been approvedfor marketing for a certain use, experience may show that it is also usefulfor other medical problems. Although these uses are not included in productlabeling, androgens are used in certain patients with the following medicalconditions:

• Anemias (blood problems)
• Delayed growth spurt
• Development of male features in transsexuals
• Microphallus (underdevelopment of the penis)
• Lichen sclerosus (a skin problem of the vulva)

Other than the above information, there is no additional information relatingto proper use, precautions, or side effects for these uses.