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methyltestosterone (Android, Methitest, Testred)

 

Classes: Androgens; Antineoplastics, Hormones

Dosing and uses of Android, Methitest (methyltestosterone)

 

Adult dosage forms and 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

 

Pediatric dosage forms and strengths

tablet: Schedule III

  • 10mg

capsule: Schedule III

  • 10mg

 

To Induce Pubertal Changes in Hypogonadal Males

10 mg PO qDay

 

Android, Methitest (methyltestosterone) adverse (side) effects

>10%

Edema

Acne

Breast soreness

Priapism

Menstrual irregularities

Virilization

 

Frequency not defined

Edema wiith or without congestive heart failure

Gynecomastia

Suppression of clotting factors II, V, VII & X, Erythrocytosis

Cholestatic jaundice syndrome

Neoplasm of liver

Anaphylaxis

 

Warnings

Contraindications

Known or suspected prostate CA, males w/ breast cancer

Pregnancy

 

Cautions

Cardiac dz, hepatic dz, renal dz, elderly

Hypercalcemia may occur in breast CA pts

Risk of jaundice, cholestatic hepatitis, abnl LFTs & potentially fatal hepatic peliosis - discontinue if any of these occur

Pts. easily sexually aroused

 

Pregnancy and lactation

Pregnancy category: X

Lactation: excreted into breast milk, avoid

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Android, Methitest (methyltestosterone)

Half-Life: 10-100 min

Peak Plasma Time: 1-2 hr

Bioavailability: absorbed from GI tract & oral mucosa

Protein Bound: 98%

Metabolism: less extensively undergoes first-pass hepatic metabolism than testosterone, suitable for PO admin

 

Excretion

Urine: 90%

Feces: 6%

 

Mechanism of action

Synthetic testosterone derivatives with anabolic & androgenic activity; promoting growth & development of male sex organs & maintaining secondary sex characteristics in androgen-deficient males