Leuprolide
- Atc Codes:L02AE02
- CAS Codes:74381-53-6
- PHARMGKB ID:74381-53-6
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Enantone; Belgium: Eligard, Lucrin; Bulgaria: Eligard, Lucrin; Cyprus: Daronda, Eligard; Czech Republic: Eligard, Lucrin; Denmark: Eligard, Procren; Estonia: Eligard; Finland: Eligard, Enanton, Procren; France: Eligard, Enantone; Germany: Eligard, Enanton, Enantone, Klebrocid, Leupro, Leuprone, Leuprorelin, Sixantone, Trenantone; Greece: Daronda, Elityran, Leuprol; Ireland: Eligard, Leuprorelin, Prostap; Italy: Eligard, Enantone; Latvia: Eligard; Lithuania: Eligard, Lucrin; Netherlands: Eligard, Leuproreline, Lucrin; Poland: Eligard, Lucrin; Portugal: Eligard, Lucrin; Romania: Eligard, Lucrin; Slovakia: Eligard, Leuprorelin, Lucrin; Slovenia: Eligard; Spain: Eligard, Ginecrin, Procrin; Sweden: Eligard, Enanton, Procren; UK: Prostap.
North America
Canada: Eligard, Lupron; USA: Eligard, Leuprolide, Lupron.
Latin America
Argentina: Eligard, Lectrum, Leprid, Lupron; Brazil: Eligard, Lectrum, Lorelin, Reliser; Mexico: Lectrum, Lorelin, Lucrin, Prelar.
Drug combinations
Leuprolide and Bicalutamide
Leuprolide and Flutamide
Chemistry
Leuprolide Acetate: C~59~H~84~N~16~O~12~.(C~2~H~4~O~2~)~n~ (n=1 or 2). Mw: 1209.41 (as free base). (1) Luteinizing hormone-releasing factor, 6-D-leucine-9-(N-ethyl-L-prolinamide)-10-deglycinamide acetate; (2) 5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tryosyl-D-leucyl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide acetate. CAS-74381-53-6 (1981).
Pharmacologic Category
Antineoplastic Agents; Endocrine Therapy; Gonadotropin-Releasing Hormone Agonist. (ATC-Code: L02AE02).
Mechanism of action
Agonist of luteinizing hormone-releasing hormone (LHRH). Potent inhibitor of gonadotropin secretion. Suppression of ovarian and testicular steroidogenesis with continuous administration, with subsequent decrease in testosterone (male) and estrogen (female) levels. May also have direct inhibitory effect on the testes.
Therapeutic use
Palliative treatment of advanced prostate cancer. Management of endometriosis. Treatment of anemia caused by uterine leiomyomata (fibroids). Central precocious puberty.
Pregnancy and lactiation implications
Fetal abnormalities and increased fetal mortality noted in animal studies. Contraindicated during pregnancy.
Unlabeled use
Treatment of breast, ovarian, and endometrial cancer. Infertility. Prostatic hyperplasia.
Contraindications
Hypersensitivity to leuprolide, GnRH, GnRH-agonist analogs, or any component of the formulation. Undiagnosed abnormal vaginal bleeding. Pregnancy. Breast-feeding. Some preparations not indicated for use in women and/or children.
Warnings and precautions
Hazardous agent. Possible abnormal menses in females treated for precocious puberty. Decreased bone density (when used for ≥6 months). Exacerbation of endometriosis or uterine leiomyomata might occur initially. Rare cases of pituitary apoplexy (frequently secondary to pituitary adenoma) observed. Spinal cord compression reported when used for prostate cancer. Transient increases in testosterone can lead to tumor flare, bone pain, hematuria, bladder outlet obstruction and neuropathy in prostate cancer patients during the first few weeks of therapy. Urinary tract obstruction reported when used for prostate cancer. Use with caution in history of psychiatric illness. Rarely associated with retinal artery occlusion in abnormal arteriovenous anastomosis (e.g. patent foramen ovale).