MethylTESTOSTERone

Pronunciation

(meth il tes TOS te rone)

U.S. Brand Names

Android®; Methitest™; Testred®; Virilon®

Generic Available

No

Use

Male: Hypogonadism; delayed puberty; impotence and climacteric symptoms

Female: Palliative treatment of metastatic breast cancer

Restrictions

C-III

Pregnancy Risk Factor

X

Lactation

Excretion in breast milk unknown/contraindicated

Contraindications

Hypersensitivity to methyltestosterone or any component of the formulation; in males, known or suspected carcinoma of the breast or the prostate; pregnancy

Warnings/Precautions

Use with extreme caution in patients with liver or kidney disease or serious heart disease; may accelerate bone maturation without producing compensatory gain in linear growth

Adverse Reactions

Frequency not defined.

Male: Virilism, priapism, prostatic hyperplasia, prostatic carcinoma, impotence, testicular atrophy, gynecomastia

Female: Virilism, menstrual problems (amenorrhea), breast soreness, hirsutism (increase in pubic hair growth), atrophy

Cardiovascular: Edema

Central nervous system: Headache, anxiety, depression

Dermatologic: Acne, "male pattern" baldness, seborrhea

Endocrine & metabolic: Hypercalcemia, hypercholesterolemia

Gastrointestinal: GI irritation, nausea, vomiting

Hematologic: Leukopenia, polycythemia

Hepatic: Hepatic dysfunction, hepatic necrosis, cholestatic hepatitis

Miscellaneous: Hypersensitivity reactions

Overdosage/Toxicology

Abnormal liver function tests

Drug Interactions

Anticoagulants, oral: May have increased effect; monitor INR

Cyclosporine: Toxicity may occur; avoid concurrent use

Hypoglycemics, oral: May have increased effect; monitor blood glucose

Mechanism of Action

Stimulates receptors in organs and tissues to promote growth and development of male sex organs and maintains secondary sex characteristics in androgen-deficient males

Pharmacodynamics/Kinetics

Metabolism: Hepatic

Excretion: Urine

Dosage

Adults (buccal absorption produces twice the androgenic activity of oral tablets):

Male:

Hypogonadism, male climacteric and impotence: Oral: 10-40 mg/day

Androgen deficiency:

Oral: 10-50 mg/day

Buccal: 5-25 mg/day

Postpubertal cryptorchidism: Oral: 30 mg/day

Female:

Breast pain/engorgement:

Oral: 80 mg/day for 3-5 days

Buccal: 40 mg/day for 3-5 days

Breast cancer:

Oral: 50-200 mg/day

Buccal: 25-100 mg/day

Monitoring Parameters

In prepubertal children, perform radiographic examination of the hand and wrist every 6 months to determine the rate of bone maturation and to assess the effect of treatment on the epiphyseal centers.

Patient Education

Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Do not take any new medication during therapy unless approved by prescriber. Take as directed; do not discontinue without consulting prescriber. If you have diabetes, monitor serum glucose closely and notify prescriber of changes; this medication can alter hypoglycemic requirements. May cause acne, growth of body hair, loss of libido, impotence, or menstrual irregularity (usually reversible); or nausea or vomiting (small, frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help). Report changes in menstrual pattern; deepening of voice or unusual growth of body hair; fluid retention (swelling of ankles, feet, or hands, respiratory difficulty, or sudden weight gain); change in color of urine or stool; yellowing of eyes or skin; unusual bruising or bleeding; or other adverse reactions. Pregnancy/breast-feeding precautions: Inform prescriber if you are pregnant. Do not get pregnant or cause a pregnancy (males) during or for 1 month following therapy. Consult prescriber for instruction on appropriate barrier contraceptive measures. This drug may cause severe fetal defects. Do not breast-feed.

Dental Health: Effects on Dental Treatment

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Mental Health: Effects on Mental Status

None reported

Mental Health: Effects on Psychiatric Treatment

May cause leukopenia; use caution with clozapine and carbamazepine

Dosage Forms

Capsule (Android®, Testred®, Virilon®): 10 mg

Tablet (Methitest™): 10 mg

International Brand Names

Afro® (TR); Gynosterone® (IL); Methyltestosterone March® (TH); Metiltestosteron® (RO); Testotonic B® (IL)