|
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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|