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Ganirelix
U.S. Brand Names
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Pregnancy/Breast-Feeding Implications
Contraindications
Warnings/Precautions
Adverse Reactions
Drug Interactions
Stability
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Monitoring Parameters
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms

U.S. Brand Names
Antagon™

Synonyms
Ganirelix acetate

Pharmacological Index

Antigonadotropic Agent


Use

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


Pregnancy Risk Factor

X


Pregnancy/Breast-Feeding 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. Breast-feeding is not recommended.


Contraindications

Known hypersensitivity of ganirelix or to any of its components, known 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 (2.4%)

Gastrointestinal: Abdominal pain (4.8%), nausea (1.1%), and abdominal pain (1%)

Genitourinary: Vaginal bleeding (1.8%)

Local: Injection site reaction (1.1%)

<1%: Congenital abnormalities


Drug Interactions

No formal studies have been performed


Stability

Store at controlled room temperature (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: S.C.: Rapidly absorbed

Time to maximum concentration: 1.1 hours

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: 16.2 hours

Elimination: In feces (75%) and urine (22%). Urinary excretion is complete at 24 hours, whereas fecal excretion is complete at 288 hours after dosing.


Usual Dosage

Adult: S.C.: 250 mcg/day during the early to midfollicular phase after initiating follicle-stimulating hormone. Treatment should be continued daily until the day of chorionic gonadotropin administration.


Monitoring Parameters

Ultrasound to assess the follicle's size


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

No effects or complications reported


Patient Information

Nurse to teach how to administer S.C. injections. Give at a similar time daily as instructed by fertility clinic. Do not skip doses. Keep all ultrasound appointments. Report any sudden weight gain, abdominal discomfort, or shortness of breath to clinic. Do not take if pregnant.


Nursing Implications

Teach patient/spouse to give S.C. injections. Discuss ultrasound schedule and timing of other medications used.


Dosage Forms

Prefilled glass syringe: 250 mcg/0.5 mL with 27-gauge x 1/2 inch needle


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