Ganirelix is a synthetic decapeptide and a competitive gonadotropin-releasing hormone (GnRH) antagonist. It is primarily used in assisted reproductive technologies (ART) to control ovulation. Here's an overview of its pharmacology:
Mechanism of Action:
GnRH Receptor Antagonist: Ganirelix competitively blocks GnRH receptors on the pituitary gonadotroph, quickly resulting in the suppression of gonadotropin secretion. This prevents the premature luteinizing hormone (LH) surge, allowing for better control over ovulation timing.
Pharmacokinetics:
Absorption: Ganirelix is administered via subcutaneous injection and is rapidly absorbed.
Distribution: It has a large volume of distribution.
Metabolism: Ganirelix is metabolized by peptidases.
Excretion: The drug and its metabolites are excreted primarily via the urine (75%) and feces (22%).
Elimination Half-Life: The elimination half-life is approximately 16.2 hours.
Clinical Use:
Controlled Ovarian Hyperstimulation: Used in ART to prevent premature ovulation, ensuring that eggs are harvested at the optimal time for procedures such as in vitro fertilization (IVF).
Side Effects:
Common Side Effects: Abdominal pain, headache, injection-site reactions, nausea, ovarian hyperstimulation syndrome (OHSS), vaginal bleeding, pelvic pain, and anaphylactoid reactions.
Serious Side Effects: Potential for severe allergic reactions, including angioedema and urticaria
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