Histrelin
- Atc Codes:H01CA03
- CAS Codes:76712-82-8
- PHARMGKB ID:76712-82-8
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Denmark: Vantas; Germany: Vantas; Ireland: Vantas; UK: Vantas.
North America
USA: Supprelin LA, Vantas; Canada: Vantas.
Latin America
Argentina: Vantas.
Drug combinations
Chemistry
Histrelin: C~66~H~86~N~18~O~12~. Mw: 1323.50. (1) Luteinizing hormone-releasing factor (pig), 6-[1-(phenylmethyl)-D-histidine]-9-(N-ethyl-L-prolinamide)-10-deglycinamide-; (2) 5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-Nt-benzyl-D-histidyl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide. CAS-76712-82-8 (1985).
Pharmacologic Category
Antineoplastic Agents; Endocrine Therapy; Gonadotropin Releasing Hormone Agonist. (ATC-Code: H01CA03).
Mechanism of action
Gonadotropin secretion inhibitor. Continuous administration results in suppression of luteinizing hormone (LH), follicle-stimulating hormone (FSH), and subsequent decrease in testosterone (females and males) and estrogen (premenopausal females).
Therapeutic use
Palliative treatment of advanced prostate cancer. Treatment of children with central precocious puberty (CPP).
Pregnancy and lactiation implications
Fetal harm and increase in fetal mortalities noted in animal studies. Histrelin is contraindicated for use during pregnancy or in women who may become pregnant. Excretion in breast milk unknown.
Unlabeled use
Contraindications
Hypersensitivity to histrelin acetate, GnRH, GnRH-agonist analogs, or any component of the formulation.
Warnings and precautions
Transient increases in estradiol serum levels (female) or testosterone levels (female and male) might occur during the first week of treatment. Spinal cord compression, and ureteral obstruction reported (both may contribute to paralysis when used for prostate cancer). Possible worsening of symptoms.