Gonarelix
Gonarelix Uses, Dosage, Side Effects, Food Interaction and all others data.
Gonarelix 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). Gonarelix 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. Gonarelix is marketed by Merck & Co., Inc. as Orgalutran®.
| Trade Name | Gonarelix |
| Availability | Prescription only |
| Generic | Ganirelix |
| Ganirelix Other Names | Ganirelix |
| Related Drugs | Sprintec, Estarylla, ethinyl estradiol / norethindrone, Ortho Tri-Cyclen, Tri-Sprintec |
| Weight | 0.25mg |
| Type | Injection |
| Formula | C80H113ClN18O13 |
| Weight | Average: 1570.35 Monoisotopic: 1568.8423035 |
| Protein binding | 81.9%. |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | Ranbaxy Laboratories (sun Pharma) |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Gonarelix 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.
Gonarelix is also used to associated treatment for these conditions: Controlled ovarian hyperstimulation therapy
How Gonarelix works
Gonarelix 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.Gonarelix Drug Interaction
Gonarelix Disease Interaction
Volume of Distribution
The mean (SD) volume of distribution of Gonarelix in healthy females following intravenous administration of a single 250 mg dose is 43.7 (11.4) L.
Elimination Route
Gonarelix 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.
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