Leuprorelin Acetate

Drugs affecting Gonadotrophin · GnRH analogue

Indications

Advanced prostatic cancer. Endometriosis. Preparation of endometrium prior to intrauterine surgical procedures. Preoperative management of uterine fibroids to reduce their size and associated bleeding. 11.25 mg Inj: Management of endometriosis, including pain relief and reduction of endometriotic lesions.

Dosage

Adults: Advanced prostatic cancer: 3.75 mg as single SC or IM inj every mth. Endometriosis: 3.75 mg as single SC or IM inj every mth for a max 6 mth. Start during first 5 days of cycle. Co-administer HRT to reduce bone loss and vasomotor symptoms. Surgery: 3.75 mg as single SC or IM inj given during days 3-5 of cycle 5-6 wk before surgery. Uterine fibroids: 3.75 mg as single SC or IM inj every mth for 3-4 mth, max of 6 mth. Management of endometriosis, including pain relief and reduction of endometriotic lesions: 11.25 mg as single IM inj at 3 mth intervals for a period of 6 mth only. Initiate treatment during first 5 days of menstrual cycle. Children: Not applicable.

Administration

Adults: Single-use kit: For a single IM injection. Prefilled dual-chamber syringe: Remove the needle guard and advance the plunger to expel air from the syringe. Inject the entire contents of the syringe IM (Lupron) or SC (Eligard) as for a normal injection. Injection: Vary the injection site periodically. Use the syringes provided in the kit, if alternate syringes are needed, use insulin syringes. Depot-Ped: Must be administered under physician supervision as a single IM injection. Injection: May be administered by a patient/parent or healthcare provider as a single SC injection. Stability: Injection: Store below room temperature (25°C). Avoid freezing. Protect from light. Store vial in carton until use. Depot: Store at 25°C, excursions are permitted to 15°C-30°C. The product does not contain a preservative, therefore discard if not used immediately.

Adverse Effects

Transient increase in bone pain and urinary obstruction, impotence, decreased libido, peripheral oedema, hypertension, palpitations, muscle weakness, GI upset, anorexia, arthralgia, myalgia, headache, dizziness, fever, fatigue, insomnia, paraesthesia, visual disturbances, weight changes, increases in liver function test values, irritation at inj site, pulmonary embolism. Rarely, thrombocytopenia, leucopenia. Hypersensitivity reactions, spinal fracture, paralysis, hypotension, worsening of depression. Hot flushes, emotional liability, vaginal dryness, breast tenderness, acne, vaginal discharge or bleeding in first month.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: Use barrier contraceptive. Undiagnosed vaginal bleeding. Uterine fibroid patients at risk from osteoporosis with bone density below normal range. Precautions: To reduce risk of flare on initial therapy, an anti-androgen may be administered 3 days before therapy and continued for 2-3 weeks. Patients at risk of ureteric obstruction and spinal cord compression; monitor in first few weeks and consider anti-androgens. Diabetes. Patients at risk from osteoporosis. In treatment of uterine fibroids, confirm diagnosis and exclude an ovarian mass before starting therapy. Warn patients of possibility of abnormal bleeding or pain due to acute degeneration of submucous fibroids. Exclude pregnancy before starting therapy. Progressive brain tumours. Risk factors for metabolic or cardiovascular…

Interactions

Drugs that prolong QT interval or cause torsade de pointes.

Advice to Patient

Administer as directed by prescriber. For self-administration, use syringe provided by manufacturer. If manufacturer’s syringe is unavailable, use only a 0.5 mL disposable, low-dose, U-100 insulin syringe to ensure accurate dosage. Substitution of syringes is not recommended for leuprolide acetate for injectable suspension. Contact prescriber if there is fast or irregular heartbeat, chest pain, palpitations, difficulty in urination, changes in urinary pattern, irregularity in menstruation, memory problems, depression, unrelieved nausea or vomiting, numbness of extremities, breast pain or swelling, difficulty in breathing, redness/pain/swelling at injection site. Wear cool clothes and stay in cool environment to prevent hot flashes. Female patients of childbearing age should use non-hormonal form of contraception during leuprolide therapy. Discontinue medication and inform prescriber if…

Pharmacokinetics

Onset of action: Following transient increase, testosterone suppression occurs in approx. 2-4 wks of continued therapy. Onset of therapeutic suppression for precocious puberty: Leuprolide: 2-4 wks; Leuprolide depot: 1 month. Metabolism: Major metabolite, pentapeptide (M-1). Bioavailability: SC: 94%. Half-life elimination: Approx. 3 hrs. Excretion: Urine (<5%).

Compiled by Healify Pharmacy from published drug references. How we compile it →

Always consult a pharmacist or doctor.