Lorelin Depot Inj. 11.25mg
LHRH ANALOGUE DEPOT INJECTION
ONCE EVERY 3 MONTHS!
A depot preparation of Leuprorelin Acetate with Microencapsulated formulation which• Demonstrates continuous release of drug.
• Offers effective suppression of Testosterone after a SC or IM injection.
Lorelin depot is recommended for• Prostate Cancer
• Endometriosis
• Uterine Leiomyomata
• Central Precocious Puberty
Leuprorelin is 80 times more potent than natural LHRH.Sustained occupation of pituitary GnRH receptors by Leuprorelin results in desensitization and/or downregulation of receptors in the anterior pituitary, thereby suppressing gonadotrophin release and reducing testosterone release by the human testes to castrate levels.
It act directly on cell growth in human prostatic cancer cells, behaving like a negative growth factor. [12]
It offers maximum androgen blockade in combination with Nonsteroidal Anti Androgen (NSAA) as compared to NSAA Monotherapy having the highest estimated quality adjusted survival. [13]
BRIEF PRESCRIBING INFORMATION:
Drug Description: Leuprolide acetate is a synthetic nonapeptide analog of naturally occurring gonadotropin –releasing hormone (GnRH or LH-RH). The analog possesses greater potency than the natural hormone. When and How to give: Advanced Prostate Cancer: for effective hormone control – Lorelin 11.25mg once in 3 months along with antiandrogen to control testosterone flares.Endometriosis: for management of endometriosis, including pain relief and reduction of endometriotic lesions. Prescribed with Norethindrone acetate 5mg daily. Helps in preventing recurrence symptoms. Duration of initial treatment or retreatment should be limited to 6 months.Uterine Leiomyomata (Fibroids): Lorelin 11.25mg, 3 monthly concomitantly with iron therapy is indicated for preoperative hematologic improvement of patients with anemia caused by fibroids. Description: Lorelin Depot injection is a fine powder containing 11.25mg of Leuprorelin acetate, a synthetic analogue of LHRH in a vial. Indications: Prostatic Cancer, Endometriosis, Uterine Leiomyomata, Premenopausal Breast Cancer & Central Precocious Puberty. Mode of administration: Given IM/SC. Absorption: Mean plasma concentration 36.3ng/ml at 4 hours. Released at a constant rate following the onset of steady state levels during third week after dosing & these levels decline to near the lower limit of detection by 12 weeks. Distribution: Mean steady state volume of distribution was 27L. In vitro binding to human plasma proteins = 43-49%. Metabolism: One mg bolus of leuprolide acetate IV – mean systemic clearance 7.6l/h. Terminal elimination half-life of approx. 3 hours. Less than 5% of the dose was recovered as parent metabolite in the urine. Precautions: Mutagenesis, Impairment of fertility, Pregnancy Category X, Teratogenic, Nursing mothers, Geriatric use. Side Effects: Hot flushes, Sweating, Amenorrhea, Withdrawal bleeding, Reduced libido, Vaginal dryness, Breast tenderness, Arthralgia, Myalgia, Peripheral edema, Dizziness, Headache, Nausea, Vomiting, Constipation, Injection site reaction, Thrombophlebitis, Decreased bone mass. Storage: Store at room temperature. M.R.P: 21,000/- PKR
