Ganirelix acetate -@- Gonadotropin Hormone Antagonists - Sex Hormones
Drug Name:
Ganirelix acetate -@- Gonadotropin Hormone Antagonists - Sex Hormones
List Of Brands:
Indication Type Description:
Pharmacology/ Pharmacokinetics
Drug Interaction:
Gonodrotropins - because ganirelix can suppress the secretion of pitutiary gonodotropin , dose
adjustments of exogenous gonodrotropins may be necessary when used during the controlled
ovarian stimulation
Adverse Reaction:
Adverse reactions-
Abdominal pain gynaecological 4% death fetal 3% Headache 3%
Ovarian hyperstimulation syndrome 2%
Vaginal bleeding 1% Injection site reaction 1% Abdominal pain 1%
Contra-Indications:
Hypersensitivity to any of its components
Special Precautions-
Latex allergy- the packing of this product contains natural rubber latex which may cause
allergic reaction
Hypersensitivity reactions- caution is advised in patients with hypersensitivity to GnRH
Carefully monitor these patients after the first injection
Anaphylactic reactions of ganirelix have not been reported
Pregnancy- safe use of ganerelix during pregnancy has not been established
Lactation- not known whether this drug is excreted in breast milk .
Ganerelix should not be used by breast-feeding women.
Dosages/ Overdosage Etc:
Indication-
Infertility
Dosage-
After initiating follicle stimulating hormone FSH therapy, on day 2 or 3 of the cycle ganirelix 250mcg
may be adminstered subcutaneously once daily during the early -to-mild follicular phase
Patient Information:
1. Prior to therapy with ganerelix, inform patients of the duration of the treatment and monitoring
procedures that will be required.
2. Discuss the risk of possible adverse reactions.
3. Do not prescribe ganerelix if the patient is pregnant
Pharmacology/ Pharmacokinetics:
Ref- Drug Facts And comparisons(2010)
Pharmacology-
Ganirelix is a synthetic decapeptide with high degree antagonistic activity against
occuring gonadotropin -releasing (GnRH) . Genirelix is derived from native GnRH
with substitution of amino acids at positions 1.2,3,6,8,and 10
Pharmacokinnetics-
The pharmcokinetics parameters of single and multiple dose injections of Ganirelix
in healthy adults females are summarised in the following table.
Steady-state serum concentrations are reached after 3 days of treatment-
The pharmacokinetic of ganerelix are dose-proportional in the dose range
125mg to 500mcg.
Mean Pharmacokinetic Parameters of Ganirelix
Absorption
Mean absolute bioavailability 91/1%
Cmax 14.8ng/ml, 11.2 ng/ml
Tmax 1.1
Distribution
Vd 43.7L, 76.5L
Protein binding 81.9%
Metabolism
Metabolites 1 to 4 peptide and 1 to 6 peptide
Excretion
Site feces (75.1%) urine (22.1%)
Elimination t 1/2 12.8, 16.2h
clearance 2.4 L/h, 3.3
Pregnancy and lactation:
Pregnancy-
Safe use of ganerelix during pregnancy has not been established
Lactation-
Not known whether this drug is excreted in breast milk .
Ganerelix should not be used by breast-feeding women.