Testosterone is the primary endogenous androgen, a steroid hormone synthesized from cholesterol in the Leydig cells of the testes (95%), and to a lesser extent in the adrenal cortex and ovaries. In the Indian market, it is available in various exogenous formulations for replacement therapy in androgen-deficient males. It is essential for the development and maintenance of male sexual characteristics, muscle mass, bone density, red blood cell production, and overall sense of well-being.
Adult: Dose is HIGHLY formulation-specific and individualized based on serum levels and response. General ranges: 1. Injectable Testosterone Enanthate/Cypionate: 50-400 mg intramuscularly every 2-4 weeks. 2. Testosterone Undecanoate (long-acting): 1000 mg IM at initiation, at 6 weeks, then every 10-14 weeks. 3. Transdermal Gel (1% or 1.62%): 5-10 g (delivering 50-100 mg testosterone) applied once daily to clean, dry skin. 4. Buccal Tablet: 30 mg applied to gum twice daily.
Note: IM Injections: Use deep gluteal or thigh muscle, rotate sites. Transdermal Gel: Apply to shoulders, upper arms, or abdomen; wash hands thoroughly; avoid skin-to-skin contact with others, especially women and children. Buccal Tablet: Apply to gum above incisor tooth; do not chew/swallow; rotate sites; avoid eating/drinking for 1 hour.
Testosterone and its active metabolite, DHT, bind to and activate intracellular androgen receptors (ARs) in target tissues (e.g., prostate, seminal vesicles, skin, hair follicles, muscle, bone, brain). The hormone-receptor complex translocates to the nucleus, binds to specific DNA sequences (Androgen Response Elements), and modulates the transcription of target genes, leading to anabolic and androgenic effects.
Pregnancy: CATEGORY X. Contraindicated. Can cause virilization of the external genitalia of the female fetus (clitoral enlargement, labial fusion). Potential risk of spontaneous abortion.
Driving: Usually no effect. However, patients should be cautioned about potential dizziness, headaches, or mood changes that could impair ability.
| Warfarin and other Anticoagulants | Testosterone may potentiate anticoagulant effect by reducing clotting factor synthesis and increasing fibrinolysis; increased risk of bleeding. | Major |
| Corticosteroids (e.g., Prednisolone) | Increased risk of severe fluid retention and edema. | Moderate |
| Insulin and Oral Hypoglycemics | Testosterone may alter insulin sensitivity; blood glucose monitoring required; dose adjustment may be needed. | Moderate |
| Cyclosporine, Tacrolimus | Testosterone may inhibit CYP3A4, potentially increasing levels of these immunosuppressants and risk of toxicity. | Moderate |
| Prostate cancer drugs (GnRH agonists, Antiandrogens e.g., Bicalutamide) | Pharmacological antagonism; concurrent use is contraindicated. | Major |
| ACTH or Corticotropin | Enhanced risk of edema. | Moderate |
Same composition (Testosterone (NA)), different brands: