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Ganirelix

U.S. Brand Names: Antagon�(r)



Synonyms: Ganirelix Acetate



Generic Available: No



Canadian Brand Names: Antagon�(r); Orgalutran�(r)



Use: Inhibits premature luteinizing hormone (LH) surges in women undergoing controlled ovarian hyperstimulation in fertility clinics.



Pregnancy Risk Factor: X



Pregnancy Implications: Fetal resorption occurred in pregnant rats and rabbits. These effects are results of hormonal alterations and could result in fetal loss in humans. The drug should not be used in pregnant women.



Lactation: Excretion in breast milk unknown/not recommended



Contraindications: Hypersensitivity to ganirelix or any component of the formulation; hypersensitivity to gonadotropin-releasing hormone or any other analog; known or suspected pregnancy



Warnings/Precautions: Should only be prescribed by fertility specialists. The packaging contains natural rubber latex (may cause allergic reactions). Pregnancy must be excluded before starting medication.



Adverse Reactions:

1% to 10%:

Central nervous system: Headache (3%)

Endocrine & metabolic: Ovarian hyperstimulation syndrome (2%)

Gastrointestinal: Abdominal pain (5%), nausea (1%), and abdominal pain (1%)

Genitourinary: Vaginal bleeding (2%)

Local: Injection site reaction (1%)

<1%: Congenital abnormalities



Drug Interactions: No formal studies have been performed



Stability: Store at controlled room temperature of 15°C to 30°C (59°F to 86°F)



Mechanism of Action: Competitively blocks the gonadotropin-release hormone receptors on the pituitary gonadotroph and transduction pathway. This suppresses gonadotropin secretion and luteinizing hormone secretion preventing ovulation until the follicles are of adequate size.



Pharmacodynamics/Kinetics:

Absorption: SubQ: Rapid

Distribution: Mean Vd: 43.7 L

Protein binding: 81.9%

Metabolism: Hepatic to two primary metabolites (1-4 and 1-6 peptide)

Bioavailability: 91.1%

Half-life elimination: 16.2 hours

Time to peak: 1.1 hours

Excretion: Feces (75%) within 288 hours; urine (22%) within 24 hours



Dosage: Adult: SubQ: 250 mcg/day during the mid-to-late phase after initiating follicle-stimulating hormone on day 2 or 3 of cycle. Treatment should be continued daily until the day of chorionic gonadotropin administration.



Monitoring Parameters: Ultrasound to assess the follicle's size



Patient Education: This drug can only be given by injection as demonstrated. Use this and any other medications as directed by prescriber; do not skip any doses. You must keep all scheduled ultrasound appointments. You may experience headache (use of mild analgesic may help); or nausea (small, frequent meals, good mouth care, chewing gum, or sucking hard candy may help). Report immediately any sudden or acute abdominal pain; vaginal bleeding; or pain, itching, or signs of infection at injection site. Note: Packaging contains natural rubber latex; if you have a known latex allergy advise prescriber. Pregnancy/breast-feeding precautions: Do not get pregnant while taking this drug. Breast-feeding is not recommended.



Nursing Implications: Teach patient/spouse to give SubQ injections. Discuss ultrasound schedule and timing of other medications used.



Dental Health: Effects on Dental Treatment: No significant effects or complications reported



Dental Health: Vasoconstrictor/Local Anesthetic Precautions: No information available to require special precautions



Mental Health: Effects on Mental Status: None reported



Mental Health: Effects on Psychiatric Treatment: None reported



Dosage Forms: Injection, solution, as acetate: 250 mcg/0.5 mL [prefilled glass syringe with 27-gauge x 1/2 inch needle]



International Brand Names: Antagon�(r) (CA); Orgalutran�(r) (AT, CA, CH, CY, CZ, DE, DK, EG, ES, FR, GB, IL, IT, JO, KW, LB, NL, NO, NZ, PL, RO, SE, SY, TH, YU)




Review Date:
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