Antineoplastic Agent, Gonadotropin-Releasing Hormone Agonist
Leuprorelin acetate is a synthetic nonapeptide agonist of naturally occurring gonadotropin releasing hormone (GnRH) that, when given continuously, inhibits pituitary gonadotropin secretion and suppresses testicular steroidogenesis inmales.
藥動學
Onset of action:
1. Following transient increase, testosterone suppression occurs in ~2 to 4 weeks of continued therapy.
2. Onset of therapeutic suppression for precocious puberty: (Leuprolide) 2 to 4 weeks; (Leuprolide depot) 1 month Distribution:
1. Vd: 27 L
2. Protein binding: 43% to 49% Metabolism:
1. Metabolized to smaller inactive peptides, then may be further catabolized; Major metabolite, pentapeptide (M-1)
2. Half-life elimination: ~3 hours Excretion:
1. Urine (<5% as parent and major metabolite)
2. Clearance: 8.34 L/hour
禁忌症
1. Hypersensitivity to leuprolide, GnRH, GnRH-agonist analogs, or any component of the formulation
2. Pregnancy
3. Undiagnosed abnormal vaginal bleeding
懷孕分類
X; Use is contraindicated during pregnancy
哺乳分類
Use is contraindicated in nursing women
副作用
Hot flashes, malaise, nausea and fatigue, transient local irritation at the site of injection
劑量和給藥方法
ELIGARD 22.5 mg is administered as a single subcutaneous injection every 3 months.
小兒調整劑量
腎功能調整劑量
There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
肝功能調整劑量
There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).