Methitest

Dosage Forms & Strengths

tablet: Schedule III

• 10mg

capsule: Schedule III

• 10mg

Androgen Deficiency (Male)

Oral: 10-50 mg/day

Buccal: 5-25 mg/day

Hypogonadism, Climacteric & Impotence (Male)

Oral: 10-40 mg/day

Postpubertal Cryptorchidism (Male)

Oral: 30 mg/day

Inoperable Breast Carcinoma (Female)

Oral: 50-200 mg/day

Buccal: 25-100 mg/day

Postpartum Breast Pain & Engorgement (Female)

Oral: 80 mg/day x 3-5 days post-parturition

Buccal: 40 mg/day x 3-5 days

Other Information

Buccal absorption produces twice androgenic activity as oral tablets

Monitor: Virilization in females; priapism & excessive sexual arousal in males

Other Indications & Uses

Females: Inoperable metastatic breast cancer 1-5 years postmenopausal; post-partum breast pain & engorgement

Males: Delayed puberty

Off-label: Male climacteric impotence

Dosage Forms & Strengths

tablet: Schedule III

• 10mg

capsule: Schedule III

• 10mg

To Induce Pubertal Changes in Hypogonadal Males

10 mg PO qDay

Methitest is part of the drug classes:

• 3 oxoandrosten 4 derivatives

• Androgens and female sex hormones in combination with other drugs

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.

Methitest™ Tablets contain methyltestosterone, USP, a synthetic androgen. Androgens are steroids that develop and maintain primary and secondary male sex characteristics. Methyltestosterone Tablets are to be taken orally.

Androgens are derivatives of cyclopentanoperhydrophenanthrena. 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. In their active form, all drugs in the class have a 17-beta-hydroxy group. 17-alpha alkylation (methyltestosterone) increases the pharmacologic activity per unit weight compared to testosterone when given orally.

Methyltestosterone is the 17α-methyl derivative of testosterone, the true testicular hormone. Chemically, methyltestosterone is 17β-hydroxy-17-methylandrost-4-en-3-one, with the empirical formula C20H30O2, a molecular weight of 302.5, and the following structural formula:

C20H30O2 m.w. 302.46 (CAS-58-18-4)
17β-Hydroxy-17-methylandrost-4-en-3-one

Methyltestosterone is a white to creamy-white, odorless, slightly hydroscopic powder. It is practically insoluble in water, and is soluble in alcohol and other organic solvents. Methyltestosterone Tablets contain methyltestosterone, USP and acacia, lactose monohydrate, confectioner's sugar, corn starch, powdered cellulose, sodium lauryl sulfate, magnesium stearate, pregelatinized starch, and guar gum.

Methyltestosterone Tablets 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 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.

Overdose of medication may be reflected in the occurrence of the signs and symptoms associated with testosterone-anabolic drugs. Nausea and appearance of the early manifestations of edema should be looked for. However, there has been no report of acute overdosage with androgens.

Prior to initiating methyltestosterone, confirm the diagnosis of hypogonadism by ensuring that serum testosterone concentrations have been measured in the morning on at least two separate days and that these serum testosterone concentrations are below the normal range.

Dosage must be strictly individualized. The suggested dosage for androgens varies depending on the age, sex, and diagnosis of the individual patient. Adjustments and duration of dosage will depend upon the patient's response and the appearance of adverse reactions.

Males

In the androgen-deficient male the guideline for replacement therapy indicates the usual initial dosage of 10-50 mg daily.

Various dosage regimens have been used to induce pubertal changes in hypogonadel males: some experts have advocated lower dosages initially, gradually increasing the dose as puberty progresses, with or without a decrease to maintenance levels. Other experts emphasize that higher dosages are needed to induce pubertal changes and lower dosages can be used 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.

Dosages used in delayed puberty generally are in the lower ranges of those given above, and are for limited duration, for example, 4 to 6 months.

Females

Women with metastatic breast carcinoma must be followed closely because androgen therapy occasionally appears to accelerate the disease. Thus, many experts prefer to use the shorter acting androgen preparations rather than those with prolonged activity for treating breast carcinoma particularly during the early stages of androgen therapy.

Guideline dosages of androgens for use in the palliative treatment of women with metastatic breast cancer are 50-200 mg daily.

Each compressed, single-scored, round, white tablet contains 10 mg of methyltestosterone for oral use. Each tablet is debossed with "7037" on one side, and scored on the other side.

Protect from Light, Moisture and Heat. Store at controlled room temperature, 15°-30°C (59°-86°F).

This package is not for household dispensing. Dispense in a tight, light-resistant container as defined in the USP, with a child-resistant closure, as required.

Rx Only

Dist. by:
Impax Generics
Hayward, CA 94544

120-11
Rev. 11/2016

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 Methitest) 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 Methitest) 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 Methitest) at signs of mild virilization may prevent irreversible virilization.[Ref]

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