Description

Simple

A medication used during a medical procedure called controlled ovarian hyperstimulation in women, which is used to increase the success of pregnancy.

Clinical

A GnRH antagonist used in assisted reproduction in women undergoing controlled ovarian hyperstimulation to control ovulation by inhibiting the premature LH surges.

Overview

Ganirelix is an injectable competitive gonadotropin-releasing hormone antagonist (GnRH antagonist). It is utilized frequently in assisted reproduction therapy to control the occurrence of ovulation. The drug exerts its effects by inhibiting the action of GnRH in the pituitary gland, leading to fast suppression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). Ganirelix is used in fertility treatment to prevent premature ovulation that could result in the harvesting of eggs that are too immature to be used in procedures such as in vitro fertilization. Ganirelix is marketed by Merck & Co., Inc. as Orgalutran®.

Pharmacology

Indication

For the inhibition of premature LH surges in women undergoing controlled ovarian hyperstimulation.

Pharmacodynamic

Information currently not available.

Mechanism of action

Ganirelix acts by competitively blocking the GnRH receptors on the pituitary gonadotroph and subsequent transduction pathway. It induces a rapid, reversible suppression of gonadotropin secretion. The suppression of pituitary LH secretion by ganirelix is more pronounced than that of FSH. An initial r... Read more

Absorption

Ganirelix is rapidly absorbed following subcutaneous injection with maximum serum concentrations reached approximately one hour after dosing.

Protein binding

81.9%.

Volume of distribution

The mean (SD) volume of distribution of Ganirelix in healthy females following intravenous administration of a single 250 mg dose is 43.7 (11.4) L.

Clearance

Single dose: 2.4L/hourMultiple dose: 3.3L/hour

Half life

16.2 hours.

Route of elimination

On average, 97.2% of the total radiolabeled ganirelix dose is recovered in the feces and urine (75.1% and 22.1%, respectively) over 288 h following intravenous single dose administration of 1 mg [14 75 C]-ganirelix acetate. Urinary excretion is virtually complete in 24 h, whereas fecal excretion sta... Read more

Toxicity

Information currently not available.

Adverse Effects

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: Suspected pregnancy
      • Drugbank Id: DBCOND0107509
  • Hypersensitivity:
    • Gonadotropin-Releasing Hormone
    • Gonadotropin-Releasing Hormone analogue
  • Regions: US
  • Regions: US
  • Patient Conditions:
      • Name: Pregnancy
      • Drugbank Id: DBCOND0018394

Food Interactions

    Information currently not available.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
2 References
  1. 1 . Oberye J, Mannaerts B, Huisman J, Timmer C: Local tolerance, pharmacokinetics, and dynamics of ganirelix (Orgalutran) administration by Medi-Jector compared to conventional needle injections. Hum Reprod. 2000 Feb;15(2):245-9.PubMed: 10655292
  2. 2 . Royster GD, Retzloff MG, Robinson RD, King JA, Propst AM: Effect of length of controlled ovarian hyperstimulation using a gonadotropin-releasing hormone antagonist on in vitro fertilization pregnancy rates. J Reprod Med. 2012 Sep-Oct;57(9-10):415-20.PubMed: 23091989