indication

For treatment of prostate cancer, endometriosis, uterine fibroids and premature puberty

pharmacology

Used in the palliative treatment of advanced prostate cancer. Leuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis.

mechanism of action

Leuprolide binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretion.

toxicity

In rats subcutaneous administration of 250 to 500 times the recommended human dose, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is a clinical counterpart of this phenomenon. In early clinical trials with leuprolide acetate doses as high as 20 mg/day for up to two years caused no adverse effects differing from those observed with the 1 mg/day dose.

biotransformation

Primarily degraded by peptidase and not by cytochrome P450 enzymes.

absorption

Bioavailability by subcutaneous administration is comparable to that by intravenous administration.

half life

~3 hours

route of elimination

Excretion in urine