Android

Android is part of the drug classes:

• 3 oxoandrosten 4 derivatives

• Androgens and female sex hormones in combination with other drugs

Follow your doctor's instructions about any restrictions on food, beverages, or activity.

• Tell all of your health care providers that you take Android. This includes your doctors, nurses, pharmacists, and dentists.
• This medicine does not help you to be better at sports.
• If you stop taking this medicine all of a sudden, you may have signs of withdrawal. Tell your doctor if you have any bad effects.
• If you have high blood sugar (diabetes), you will need to watch your blood sugar closely.
• Check blood pressure and heart rate as the doctor has told you. Talk with the doctor.
• Have blood work checked as you have been told by the doctor. Talk with the doctor.
• This medicine may raise the chance of blood clots, a stroke, or a heart attack. Talk with the doctor.
• This medicine may affect certain lab tests. Tell all of your health care providers and lab workers that you take Android.
• This medicine is an anabolic steroid. Anabolic steroid drugs have been abused and misused before. Anabolic steroid abuse can lead to dependence and very bad health problems. These health problems include heart or blood vessel problems, stroke, liver problems, and mental or mood problems. Talk with the doctor.
• If you are 65 or older, use this medicine with care. You could have more side effects.
• Use with care in children. Talk with the doctor.
• This medicine may affect growth in children and teens in some cases. They may need regular growth checks. Talk with the doctor.
• This medicine may affect sperm in men. This may affect being able to father a child. Talk with the doctor.
• This medicine may cause harm to the unborn baby if you take it while you are pregnant. If you are pregnant or you get pregnant while taking Android, call your doctor right away.

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

• Store at room temperature.
• Protect from light.
• Protect from heat.
• Store in a dry place. Do not store in a bathroom.
• Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
• Check with your pharmacist about how to throw out unused drugs.

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 the growth and maturation of prostate, seminal vesicles, penis, and scrotum; the 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. Drugs in this class also cause retention of nitrogen, sodium, potassium, 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 synthetic androgen, methylTESTOSTERone, is less extensively metabolized by the liver and has a longer half-life. It is more suitable than testosterone for oral administration.

Testosterone in plasma is 98 percent bound to a specific testosterone-estradiol binding globulin, and about 2 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; and 6 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-ketosteroids 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.

In many 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.

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 these drugs, she should be apprised of the potential hazard to the fetus.

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. A decision may be made by the patient and the physician that some virilization will be tolerated during treatment for breast carcinoma.

Information for the Patient

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.
		Any male adolescent patient receiving androgens for delayed puberty should have bone development checked every six months.
Women:		Hoarseness, acne, changes in menstrual periods or more hair on the face.
All Patients:		Any nausea, vomiting, changes in skin color or ankle swelling.

Laboratory Tests

1. Women with disseminated breast carcinoma should have frequent determination of urine and serum calcium levels during the course of androgen therapy (see WARNINGS). 2. Because of the hepatotoxicity associated with the use of 17-alpha-alkylated androgens, liver function tests should be obtained periodically. 3. Periodic (every 6 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. 4. Hemoglobin and hematocrit should be checked periodically for polycythemia in patients who are receiving high doses of androgens.

Drug Interactions

1. Anticoagulants: C-17 substituted derivatives of testosterone, such as methandrostenolone, have been reported to decrease the anticoagulant requirements of patients receiving oral anticoagulants. Patients receiving oral anticoagulant therapy require close monitoring, especially when androgens are started or stopped. 2. Oxyphenbutazone: Concurrent administration of oxyphenbutazone and androgens may result in elevated serum levels of oxyphenbutazone. 3. Insulin: In diabetic patients the metabolic effects of androgens may decrease blood glucose and insulin requirements.

Drug/Laboratory Test Interferences

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

Animal Data

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.

Human Data

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

Pregnancy 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 hand and wrist (see INDICATIONS AND USAGE and WARNINGS).

MethylTESTOSTERone capsules USP 10 mg are red capsules imprinted "VRX 0901" on both sections. They are available in bottles of 100.

NDC 0187-0902-01

Store at 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature].

Manufactured for:

Valeant Pharmaceuticals North America LLC
Bridgewater, NJ 08807 USA

By:
Valeant Canada LP

1956 Bourdon Street

Montreal, Quebec, H4M 1V1

[Part #]
Revised: September 2016

Applies to methyltestosterone: compounding powder, oral capsule, oral tablet

Cardiovascular

Cardiovascular effects have included edema (with and without congestive heart failure).[Ref]

Endocrine

Endocrine side effects have included gynecomastia. Cautious use is recommended in patients with existing gynecomastia.

During exogenous administration of androgens, endogenous testosterone release is inhibited through feedback inhibition of pituitary luteinizing hormone (LH). Large doses of exogenous androgens may suppress spermatogenesis through inhibition of pituitary follicle stimulating hormone (FSH).

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 and there is no clinical evidence of thyroid dysfunction.[Ref]

Renal

Renal side effects have included retention of nitrogen, sodium, potassium, chloride, water, and phosphorus and decreased urinary excretion of calcium. Patients should be instructed to report edema.[Ref]

Hepatic

Hepatic side effects have included life-threatening peliosis hepatitis and hepatic abnormalities including hepatic neoplasms and hepatocellular carcinomas following prolonged therapy with high doses of androgen. Tumor regression did not occur in all cases following medication withdrawal.

Cholestatic hepatitis, jaundice, and abnormal liver function tests have occurred during androgen therapy. Drug-induced jaundice is reversible following drug discontinuation.[Ref]

Genitourinary

Genitourinary side effects have included oligospermia and decreased ejaculatory volume following chronic administration and/or large dosages of androgens. Elderly male patients may experience prostatic enlargement resulting in urinary obstruction. Priapism and excessive stimulation may develop. Methyltestosterone should be discontinued if any of these effects occur. If continued therapy is necessary, resume methyltestosterone (the active ingredient contained in Android) at a lower dosage.

In female patients the use of androgens has resulted in virilization, including deepening voice, hirsutism, acne, clitomegaly (not reversible), and menstrual abnormalities. Discontinuation of methyltestosterone at signs of mild virilization may prevent irreversible virilization.[Ref]

Metabolic

Metabolic side effects have included osteolytic-induced hypercalcemia in immobilized patients or those with metastatic breast disease.

Androgens affect electrolyte balance, nitrogen retention, and urinary calcium excretion. Edema, with and without congestive heart failure has occurred during testosterone therapy.

Androgens have precipitated acute intermittent porphyria.

Increased cholesterol levels have occurred during androgen therapy.[Ref]

Dermatologic

Dermatologic side effects have included hirsutism, acne, male-patterned baldness and seborrhea.[Ref]

Gastrointestinal

Gastrointestinal side effects have included nausea and vomiting.[Ref]

Musculoskeletal

Testosterone is involved in termination of linear bone growth by closure of the epiphyseal growth centers. Monitoring of bone age is recommended during methyltestosterone (the active ingredient contained in Android) treatment in healthy males with delayed puberty.

Myalgia and pain have been reported.[Ref]

Hematologic

Hematologic side effects have included alteration in clotting factors II, V, VII and X and polycythemia due to increased red cell production.[Ref]

Hypersensitivity

Hypersensitivity side effects have included rare reports of rash and anaphylactoid reactions.[Ref]

Local

Local side effects have included inflammation and pain at injection or dermal application site.[Ref]

Nervous system

Nervous system side effects have included altered libido (increased/decreased), headache, anxiety, depression, generalized paresthesia, or sleep apnea syndrome.[Ref]

Oncologic

Oncologic side effects have included hepatic neoplasms and hepatocellular carcinomas following prolonged therapy with large doses of androgens.[Ref]

Respiratory

Respiratory side effects have included potentiation of sleep apnea, particularly in obese patients or those with chronic lung disease. Androgen therapy for hypogonadal conditions has been reported to[Ref]

Other

Other side effects have included virilization including deepening voice, hirsutism, acne, clitomegaly (not reversible), and menstrual abnormalities in female patients. Discontinuation of methyltestosterone (the active ingredient contained in Android) at signs of mild virilization may prevent irreversible virilization.[Ref]

Some side effects of Android may not be reported. Always consult your doctor or healthcare specialist for medical advice. You may also report side effects to the FDA.