Androcap

Approved Indications:

• Male Hypogonadism (Testosterone Replacement Therapy):
  For adult males with primary (testicular failure) or secondary (hypothalamic or pituitary) hypogonadism confirmed by clinical features and laboratory tests.
• Delayed Puberty in Males (selected cases):
  In adolescent males with delayed puberty due to confirmed hypogonadism and after exclusion of other causes.
• Transgender Hormone Therapy (Off-label but widely accepted):
  Used as part of masculinizing hormone therapy in transgender men (female-to-male individuals).
• Andropause Symptoms (Off-label use):
  Used in older men presenting with clinical symptoms of testosterone deficiency, though such use requires thorough risk-benefit evaluation.

Intramuscular (IM) Injection (Long-acting depot):

• Adults (Hypogonadism):
  1000 mg IM every 10–14 weeks (initial loading dose followed by maintenance dosing).
  The second dose is administered after 6 weeks of the first injection, followed by maintenance every 10–14 weeks.
• Adolescents (Delayed Puberty):
  Dosing is individualized, typically 50–100 mg IM every 2–4 weeks for a limited duration (e.g., 6 months), under specialist supervision.

Oral Capsule (Testosterone Undecanoate form):

• Typical adult dose:
  120–160 mg/day in divided doses with meals initially; maintenance dose ranges from 40–120 mg/day depending on response.

Transgender Men (Off-label):
Same as adult male hypogonadism dosing, with dose titrated to maintain testosterone within the typical adult male range.

Renal/Hepatic Impairment:
Use with caution. Not recommended in severe hepatic impairment. Monitor LFTs periodically.

Administration Advice:

• IM Form: Deep gluteal injection by a trained healthcare provider.
• Oral Form: Take with meals containing fat for optimal absorption.

Testosterone Undecanoate is a synthetic ester of testosterone. After administration, it is gradually hydrolyzed to testosterone, the primary endogenous male sex hormone. Testosterone binds to intracellular androgen receptors in target tissues, forming a hormone-receptor complex that translocates into the nucleus and modulates gene transcription. This promotes development and maintenance of secondary sexual characteristics, anabolic effects on muscle and bone, erythropoiesis, and libido. In the hypothalamus-pituitary-gonadal axis, it provides negative feedback to suppress luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion.

• Absorption:
  Oral testosterone undecanoate is absorbed via the lymphatic system (bypassing first-pass metabolism). IM form provides slow release from the depot.
• Bioavailability:
  Oral: Variable (~3–7%); enhanced with high-fat meals.
  IM: Nearly complete.
• Distribution:
  Widely distributed; 98% protein-bound (to SHBG and albumin).
• Metabolism:
  Primarily hepatic via CYP3A4 and other pathways to active androgens (e.g., dihydrotestosterone) and estrogens (via aromatase).
• Half-life:
  IM: ~21 days (range 18–30 days);
  Oral: ~2–5 hours per dose.
• Excretion:
  Metabolites excreted mainly in urine (~90%) and feces (~6%).

• Pregnancy:
  Category X. Contraindicated in pregnancy. Testosterone exposure may cause virilization of the female fetus.
• Lactation:
  Not indicated in females. Testosterone is likely excreted in breast milk, and exposure can adversely affect the infant. Contraindicated in breastfeeding.

• Primary Class: Androgen; Anabolic Steroid
• Subclass: Long-acting Testosterone Ester

• Known hypersensitivity to testosterone undecanoate or excipients
• Male breast cancer
• Prostate cancer (known or suspected)
• Pregnant or breastfeeding women
• Severe hepatic impairment
• History of thromboembolic disorders
• Polycythemia (hematocrit >54%)
• Untreated obstructive sleep apnea

• Cardiovascular Risk: May increase risk of myocardial infarction, stroke, and hypertension; monitor closely in patients with cardiac disease.
• Polycythemia: Can raise hematocrit; monitor hematocrit and hemoglobin regularly.
• Prostate Monitoring: Evaluate PSA and perform prostate exam before and during treatment, especially in older men.
• Liver Function: Periodically monitor LFTs; avoid use in severe hepatic impairment.
• Edema Risk: Caution in patients with heart failure or renal dysfunction.
• Sleep Apnea Worsening: Particularly in obese or elderly males.
• Secondary Exposure Risk (for topical/oral): Unintended exposure to women or children must be avoided.

Common (Systemic):

• Skin: Acne, oily skin
• Reproductive: Increased libido, testicular atrophy, reduced sperm count
• Musculoskeletal: Muscle cramps, joint pain
• Psychological: Mood swings, irritability

Serious:

• Cardiovascular: Hypertension, thromboembolism, myocardial infarction
• Hepatic: Hepatic dysfunction, cholestasis (oral forms)
• Hematologic: Polycythemia (dose-dependent)
• Urologic: Prostate hypertrophy, possible acceleration of prostate cancer
• Respiratory (IM Form): Pulmonary oil microembolism (POME) — rare but life-threatening, causes cough, chest pain, dyspnea

Rare:

• Gynecomastia
• Allergic reactions
• Depression or anxiety

• Anticoagulants (e.g., Warfarin): Increased anticoagulant effect; monitor INR closely.
• Corticosteroids: May increase risk of edema and fluid retention.
• Insulin/Antidiabetics: May enhance hypoglycemic effects; monitor blood glucose.
• CYP3A4 inducers (e.g., Rifampin, Phenytoin): May reduce testosterone levels.
• CYP3A4 inhibitors (e.g., Ketoconazole): May increase testosterone effects/toxicity.
• Alcohol: Increased risk of liver toxicity (with oral forms); potential exacerbation of aggression/mood swings.

• FDA (2023 Update):
  Emphasized cardiovascular risk warning; recommends individualized risk assessment before initiation.
• Endocrine Society Guidelines (Updated 2024):
  Reaffirm testosterone undecanoate as a preferred long-acting injectable formulation in male hypogonadism.
  Endorses its use in transgender men under close monitoring.
• EMA Guidance (2022):
  Warns against off-label use in age-related testosterone decline without confirmed hypogonadism due to potential cardiovascular and prostate risks.

• Injection (Vial):
  Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C–30°C.
  Protect from light. Do not refrigerate or freeze.
  Keep in upright position.
• Oral Capsules:
  Store below 25°C.
  Protect from moisture and direct sunlight.
  Keep in original container; tightly closed.
• Handling Precautions:
  For IM injections, trained personnel should administer under sterile conditions.
  Shake vial before use if instructed. Discard unused portions appropriately.