BLACK BOX WARNING
- testosterone has been associated with serious cardiovascular adverse events; potential risk of pulmonary oil microembolism with some injectable forms
testosterone
Brand: Androgel, Testim, Axiron, Depo-Testosterone
⚠ BBW Prototype Drug
Drug Class: androgen
Drug Family: hormone
Subclass: natural androgen / anabolic steroid
Organ Systems: endocrinereproductive
Mechanism of Action
Binds androgen receptors in target tissues (reproductive tract, skeletal muscle, bone, CNS, prostate). AR-testosterone complex acts as a transcription factor activating androgen response elements, mediating anabolic (muscle, bone mass) and androgenic (virilization) effects. Partially converted to DHT (dihydrotestosterone) by 5-alpha reductase and to estradiol by aromatase.
androgen receptor (AR)
Indications
- male hypogonadism (primary or secondary)
- delayed puberty in males
- hormone replacement in transgender men
- female-to-male transition
Contraindications
- prostate cancer
- male breast cancer
- women (relative; specific circumstances with monitoring)
- serious cardiac, hepatic, or renal disease
Adverse Effects
Common
- erythrocytosis (elevated hematocrit)
- acne
- oily skin
- sleep apnea exacerbation
- testicular atrophy
- infertility
Serious
- cardiovascular events (polycythemia, thrombosis)
- prostate cancer stimulation
- hepatotoxicity (oral 17-alpha-alkylated forms)
- secondary exposure to topicals (children, women)
- gynecomastia (from aromatization to estradiol)
Pharmacokinetics (ADME)
| Absorption | topical (gel): ~10% absorbed; IM depot (cypionate, enanthate): slow absorption from oil depot |
| Distribution | 98% protein bound (SHBG 44%, albumin 54%) |
| Metabolism | hepatic; converts to DHT (5-alpha reductase) and estradiol (aromatase) |
| Excretion | renal (90%) and fecal (6%) |
| Half-life | 10–100 min (endogenous); 8 days (cypionate ester depot) |
| Onset | weeks (clinical effects) |
| Peak | varies by formulation |
| Duration | 1–4 weeks (IM); daily (topical) |
| Protein Binding | 98% |
| Vd | moderate |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| warfarin | testosterone potentiates anticoagulant effect; increased bleeding risk | major |
| insulin | testosterone improves insulin sensitivity; hypoglycemia risk in diabetics | moderate |
Nursing Considerations
- Monitor hematocrit at baseline, 3 months, and annually; hold if hematocrit >54% due to thrombosis risk.
- Topical gels: educate patient about secondary exposure risk; apply to shoulders/upper arms; wash hands after application; cover with clothing; avoid skin-to-skin contact with women or children.
- Monitor PSA (prostate-specific antigen) and DRE annually in men over 40; do not initiate if suspected prostate cancer.
- Check LFTs and lipid panel at baseline and periodically; some testosterone formulations cause adverse lipid changes.
Clinical Pearls
- Testosterone therapy in male hypogonadism causes azoospermia/oligospermia by suppressing intratesticular testosterone production via the HPG axis; men wishing to preserve fertility should use human chorionic gonadotropin (hCG) instead.
- Oral 17-alpha-alkylated testosterone (methyltestosterone) should be avoided due to significant hepatotoxicity; transdermal, injectable, and buccal forms are preferred.
Safety Profile
Pregnancy contraindicated
Lactation contraindicated
Renal Adjustment Not required
Hepatic Adjustment Required
TDM Not required
Concordance Terms
Cross-referenced clinical concepts — click any term to see all content where it appears.