Histrelin
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Histrelin
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| Systematic (IUPAC) name | |
| ? | |
| Identifiers | |
| CAS number | |
| ATC code | H01 |
| PubChem | ? |
| Chemical data | |
| Formula | C66H86N18O12 |
| Mol. mass | 1323.5 g/mol |
| Pharmacokinetic data | |
| Bioavailability | 92% |
| Protein binding | 70% |
| Metabolism | Hepatic |
| Half life | 4 hours |
| Excretion | Undetermined |
| Therapeutic considerations | |
| Pregnancy cat. |
X(US) |
| Legal status | |
| Routes | Subcutaneous implant |
Histrelin acetate is a nonapeptide analog of gonadotropin-releasing hormone (GnRH) with added potency. When present in the bloodstream, it acts on particular cells of the pituitary gland called gonadotropes. Histrelin stimulates these cells to release luteinizing hormone and follicle-stimulating hormone. Thus it is considered a gonadotropin-releasing hormone agonist or GnRH agonist.
[edit] Pharmacology
In a process known as downregulation, daily stimulation of pituitary gonadotropes causes them to become desensitized to the effects of histrelin. As a consequence, levels of LH and FSH fall after a short period of time. From that point forward, as long as histrelin is administered, the levels of LH and FSH in the blood remain low.
This prolonged lowering of LH and FSH levels is the rationale for therapy using GnRH agonists. Since LH and FSH stimulate the gonads to produce estrogens and androgens in females and males respectively, histrelin can effectively be used to decrease the sex steroids in the blood of patients.
Histrelin is marketed by Valera Pharmaceuticals under the brand name Supprelin.
[edit] Indications
Histrelin is used to treat hormone-sensitive cancers of the prostate in men and uterine fibroids in women. In addition, histrelin is used to treat central precocious puberty.
It is available as a daily intramuscular injection. A 12-month depot injection (Supprelin-LA) is currently undergoing the approval process with the U.S. Food and Drug Administration.
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