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methyltestosterone (Android, Testred, Metandren, Oretan, Virilon)
Tradenames: Android, Testred, Metandren, Oretan, Virilon. DEA-controlled substance: class 3
Indications:
- androgen insufficiency
- replacement therapy in hypogonadism & delayed puberty (male)
- cryptorchidism
- anorchia
- Klinfelter's syndrome [5]
- impotence (male)
- inoperable breast cancer
- LHRH deficiency [5]
- scrotal pain/mass [5]
- orchitis [5]
Contraindications: Caution:
1) liver or kidney disease
2) heart disease
3) prepubertal patients: may accelerate bone maturation without compensatory gain in linear growth
4) REF 4 DOES NOT RECOMMEND USE; USE TESTOSTERONE INSTEAD
Dosage:
1) hypogonadism: 10-40 mg PO QD
2) postpubertal cryptorchism: 30 mg QD
3) inoperabable breast cancer: 50-200 mg/day
4) buccal tablet should not be chewed or swallowed
Tabs: 10 & 25 mg
Monitor:
- radiographic exam of wrist & hand every 6 months to assess bone maturation & epiphyseal centers in prepubertal patients
Adverse effects:
1) common (> 10%)
- edema, acne
- Males: virilism, priapism
- Females: virilism, amenorrhea, breast tenderness
2) less common (1-10%)
- GI irritation, nausea/vomiting, hepatic dysfunction
- Males: prostatic hypertrophy, prostate cancer, impotence
- Females: hirsutism
3) uncommon (< 1%)
- gynecomastia, amenorrhea, hypercalcemia, leukopenia, polycythemia, hepatic necrosis, cholestatic hepatitis, hypersensitivity
4) males
- gynecomastia
- excessive frequency & duration of penile erections
- male pattern baldness
- retention of water & electrolytes
- suppression of clotting factors
5) females
- amenorrhea
- deepening of voice
- clitoral enlargement
Drug interactions:
1) may increase anticoagulant effect of warfarin
2) imipramine in combination may result in paranoid response
Mechanism of action: androgen
Interactions
drug adverse effects of androgens
General
androgen or anabolic steroid
androstenol
ketosteroid
Properties
SIZE: MW = 300 G/M
MISC-INFO: elimination route LIVER
pregnancy-category X
safety in lactation ?
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998 - not on National VA formulary
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Prescriber's Letter 10(8):46 2003
- Deprecated Reference
Substructures
testosterone (Delatestryl Testopel, Striant, Intrinsa, Xyosted)
Component-of
conjugated estrogens (Premarin)/methyltestosterone Estratest
estrogen/methyltestosterone