Leuprorelin Acetate Introduction
Leuprorelin Acetate is a synthetic gonadotropin-releasing hormone (GnRH) agonist used in men with prostate cancer, in women with endometriosis, and in boys with central precocious puberty (CPP). Leuprorelin Acetate works by affecting the hormones that control sexual maturation in both adults and children.
Uses For Leuprorelin Acetate
Leuprorelin Acetate is mainly used to treat advanced prostate cancer, as well as pre-cocious puberty and endometriosis in women.
| Brand Name | Leuprorelin Acetate |
|---|---|
| Type | |
| Weight | |
| Generic | Leuprorelin Acetate |
| Manufacturer | |
| Available in | English বাংলা |
Mechanism of Action
Leuprorelin Acetate acts a synthetic agonist of GnRH, which decreases the production of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). It works by reducing the levels of testosterone and estrogen which can help to treat cancer.
How Long Does It Take to Work?
Leuprorelin Acetate usually starts to work within a few weeks, with the effects becoming more noticeable over the course of months. In prostate cancer patients, lower testosterone levels can be seen in as little as one month.
Absorption
Leuprorelin Acetate is easily absorbed into the body and is rapidly converted into its active form. It has a bioavailability of approximately 70%.
Route of Elimination
Leuprorelin Acetate is metabolized and excreted in the urine and feces as metabolites.
Dosage
Adult: Palliative treatment of advanced prostate cancer: 1 mg as single daily dose by SC inj. Depot preparations may be given by IM or SC route, dosage and route may differ between different brands and countries. In the UK: As depot preparations: 3.75 mg every mth as single IM/SC inj; or 11.25 mg every 3 mth via SC inj. In the US: As depot preparations: 7.5 mg every mth, or 22.5 mg every 3 mth, or 30 mg every 4 mth via IM/SC inj depending on the preparations; or 45 mg every 6 mth via SC inj.Endometriosis: As depot preparations: 3.75 mg every mth given as a single IM/SC inj or 11.25 mg every 3 mth as IM depot Inj. Initiate treatment during the 1st 5 days of menstrual cycle up to 6 mth. May be used with norethindrone acetate 5 mg daily for initial management of endometriosis and for management of recurrence symptoms. Duration of retreatment: Should not exceed one additional 6 mth course.
Uterine fibroids: As depot preparations: In combination with iron therapy for women with anaemia due to uterine fibroids, 3.75 mg every mth given as a single IM/SC inj or 11.25 mg every 3 mth as IM Inj. Treatment duration: Usually up to 3 mth.
Preparation for intrauterine surgery: Endometrial preparation prior to intrauterine surgery: As depot preparations: 3.75 mg as a single inj via IM/SC given 5-6 wk before the procedure; therapy should be initiated during days 3-5 of the menstrual cycle.
Child: Precocious puberty: As aqueous soln inj: Initial: 50 mcg/kg daily by SC inj, may be titrated upwards by 10 mcg/kg/day if total down-regulation is not achieved. As depot preparations: Initial: 0.3 mg/kg/dose (minimum dose: 7.5 mg) given every 4 wk via IM inj; which equates to children ≤25 kg: 7.5 mg; >25-37.5 kg: 11.25 mg and >37.5 kg: 15 mg given every 4 wk. Maintenance: May titrate dose upwards in steps of 3.75 mg every 4 wk if down-regulation is not achieved. Consider discontinuing therapy before age 11 (females) and age 12 (males).
Leuprorelin Acetate is administered as an intramuscular or subcutaneous injection. The recommended dosage for prostate cancer is 3.75 mg once every 4 weeks, and for endometriosis and CPP, the recommended dosage is 11.25 mg once a month.
Administration
Leuprorelin Acetate is administered as an intramuscular or subcutaneous injection. Injections should be made deep into the gluteal muscle or deep subcutaneous tissue of the abdomen.
Side Effects
Common side effects of Leuprorelin Acetate include hot flashes, nausea, fatigue, headache, abdominal pain, dizziness, breast swelling and tenderness, and insomnia.
Toxicity
Leuprorelin Acetate is generally well tolerated and does not have any known serious side effects. However, it is important to note that it can cause serious allergic reactions, and it is also possible to develop an infection with repeated use.
Precautions
Before taking Leuprorelin Acetate , tell your doctor if you have any allergies, if you have had any eye problems, if you are pregnant or planning to become pregnant, or if you are breastfeeding.
Interactions
Leuprorelin Acetate may interact with other medications, including hormonal contraceptives, steroidal drugs and antifungal drugs. It is important to tell your doctor about all medications that you are taking before starting treatment.
Disease Interactions
Leuprorelin Acetate may interact with certain diseases, such as diabetes mellitus, hypertension, and hepatic impairment. It is important to tell your doctor about all diseases that you have before starting treatment.
Drug Interactions
Leuprorelin Acetate may interact with other medications, such as hormones, sedatives, steroids, anti-diabetics, and antifungal medications. It is important to tell your doctor about all medications that you are taking before starting treatment.
Food Interactions
Leuprorelin Acetate may interact with certain foods, such as grapefruit juice and licorice root. It is important to tell your doctor about any foods or supplements that you are taking before starting treatment.
Pregnancy Use
Leuprorelin Acetate should not be used during pregnancy as it is an agonist of gonadotropin-releasing hormone, which may have negative effects on a developing fetus.
Lactation Use
Leuprorelin Acetate should not be used during lactation as it is an agonist of gonadotropin-releasing hormone, which may have negative effects on a developing baby.
Acute Overdose
An acute overdose of leuprorelin acetate is unlikely, but if it should occur, seek immediate medical attention. Symptoms of an overdose include nausea, vomiting, headache, dizziness, and abdominal pain.
Contraindications
Leuprorelin Acetate should not be used by those who are pregnant or breastfeeding, those with active estrogen-dependent tumors, and those with hypersensitivity to leuprorelin acetate or its components.
Use Direction
Leuprorelin Acetate should be administered deep into the gluteal muscle or deep subcutaneous tissue of the abdomen as per your doctor’s instructions. It should not be administed in any other area.
Storage Condition
Leuprorelin Acetate should be stored at room temperature in a tightly closed container, away from heat and direct light.
Volume of Distribution
Leuprorelin Acetate has a volume of distribution of approximately 22 L/kg.
Half Life
Leuprorelin Acetate has a terminal elimination half-life of approximately 8 hours.
Clearance
Leuprorelin Acetate has an average clearance rate of 8.7 L/h.
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