Leuprorelina Gp-Pharm Depot Trimestral (Leuprorelin Acetate)

• Leuprorelin acetate acts on the gonadotropin‑releasing hormone pathway and is indicated for several hormone‑dependent conditions.
• Advanced prostate cancer: reduces testosterone production to slow tumor progression.
• Endometriosis: suppresses estrogen to alleviate pelvic pain and lesion growth.
• Uterine fibroids: lowers estrogen levels, leading to reduction in fibroid size and menstrual bleeding.
• Precocious puberty: delays early sexual development by inhibiting gonadotropin release.

• Leuprorelin acetate is a synthetic analogue of GnRH that binds with high affinity to pituitary GnRH receptors. Initial binding causes a transient surge in luteinizing hormone (LH) and follicle‑stimulating hormone (FSH) release, followed by receptor desensitization and down‑regulation, resulting in markedly reduced LH and FSH secretion and consequently decreased production of sex steroids such as testosterone and estrogen.

Leuprorelin acetate may cause a range of adverse reactions, which are categorized by frequency and severity.

Common Side Effects

• Hot flashes: sudden feeling of warmth often with sweating.
• Injection site reactions: pain, redness, or swelling at the intramuscular site.
• Headache: mild to moderate intensity.
• Decreased libido: reduced sexual desire.
• Mood changes: irritability or depressive symptoms.
• Menstrual irregularities: spotting or amenorrhea in women.

Serious or Rare Side Effects

• Severe allergic reaction (anaphylaxis): difficulty breathing, swelling of face or throat.
• Bone loss/osteoporosis: increased risk of fractures with long‑term use.
• Cardiovascular events: hypertension, thromboembolic complications.
• Adrenal insufficiency: fatigue, hypotension, electrolyte imbalance.
• Pituitary apoplexy (rare): sudden severe headache and visual disturbances.

Before initiating leuprorelin acetate therapy, several precautions should be observed to ensure patient safety.

• Monitor hormone levels: regular assessment of testosterone or estradiol to confirm suppression.
• Assess bone health: consider calcium and vitamin D supplementation and periodic bone density scans.
• Screen cardiovascular risk: evaluate blood pressure, lipid profile, and history of thromboembolic disease.
• Contraindicated in pregnancy: avoid use in women who are or may become pregnant.
• Use caution in hepatic or renal impairment: adjust monitoring as needed.
• Store at 2-8°C: keep refrigerated, protect from light, do not freeze or shake.

Leuprorelin acetate can interact with other medicines, affecting its efficacy or safety.

Major Interactions (Avoid)

• Strong estrogen‑containing hormonal contraceptives: may counteract GnRH‑mediated suppression.
• CYP3A4 inducers (e.g., rifampin, carbamazepine): may reduce plasma levels and effectiveness.
• Concurrent androgen therapy: can oppose testosterone suppression in prostate cancer.
• Use with other GnRH antagonists: may lead to antagonistic pharmacodynamic effects.

Moderate Interactions (Monitor Closely)

• Bisphosphonates: monitor bone density and calcium levels.
• Antidepressants (SSRIs, SNRIs): watch for amplified mood changes.
• Antihypertensive agents: blood pressure may fluctuate due to hormonal changes.