Ganirelix Acetate

Ganirelix Acetate Uses, Dosage, Side Effects, Food Interaction and all others data.

Ganirelix Acetate 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 Acetate 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 Acetate is marketed by Merck & Co., Inc. as Orgalutran®.

Trade Name Ganirelix Acetate
Availability Prescription only
Generic Ganirelix
Ganirelix Other Names Ganirelix
Related Drugs Sprintec, Estarylla, ethinyl estradiol / norethindrone, Ortho Tri-Cyclen, Tri-Sprintec
Weight 250mcg/0.5ml,
Type Subcutaneous solution
Formula C80H113ClN18O13
Weight Average: 1570.35
Monoisotopic: 1568.8423035
Protein binding

81.9%.

Groups Approved
Therapeutic Class
Manufacturer
Available Country United States
Last Updated: September 19, 2023 at 7:00 am
Ganirelix Acetate
Ganirelix Acetate

Uses

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

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

Ganirelix Acetate is also used to associated treatment for these conditions: Controlled ovarian hyperstimulation therapy

How Ganirelix Acetate works

Ganirelix Acetate 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 release of endogenous gonadotropins has not been detected with ganirelix, which is consistent with an antagonist effect. Upon discontinuation of ganirelix, pituitary LH and FSH levels are fully recovered within 48 hours.

Food Interaction

No interactions found.

Ganirelix Acetate Drug Interaction

Moderate: hcg

Ganirelix Acetate Disease Interaction

Major: severe allergiesModerate: renal/hepatic impairment

Volume of Distribution

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

Elimination Route

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

Half Life

16.2 hours.

Clearance

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

Elimination Route

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 starts to plateau 192 h after dosing.

Innovators Monograph

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