Buserelin
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Contents |
Indications
- palliative treatment of prostate cancer, usually in combination with other agents
- management of endometriosis
Dosage
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- depot injections of 6.6 & 10 mg under investigation
- used in combination with androgen antagonist bicalutamide ( Casodex)
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Pharmacokinetics
- bioavailability of intranasal form is 3%
- peak serum levels within 11 hours of intranasal or SQ administration
- protein binding is 15%
- metabolized primarily to buserelin 5-9 which is inactive
- 1/3 eliminated in urine, 2/3 as intact buserelin
- 1/2life 75 minutes, prolonged with renal insufficiency
Adverse-effects
- local discomfort at the injection site
- hot flashes
- decreased libido
- headache
- vaginal dryness
- depression
- emotional lability
- nausea
- weight gain
- breast pain
- premenstrual syndrome
- fatigue
- dizziness
- loss of bone mineral density
- tumor flare (mostly in 1st 2 weeks due to initial stimulation of hormone production)
- pulmonary fibrosis (rare)
- drug adverse effects of GnRH agonists
Mechanism-of-action
- GnRH analog (nonapeptide, i.e. 9 residues)
- affects LH & FSH release from the pituitary
- decline in testosterone & estradiol production
- causes chemical castration
- retards growth of hormone-sensitive tissue
More General Terms
- synthetic peptide
- gonadotropin-releasing hormone agonist (GnRH analog)
- antineoplastic agent (chemotherapeutic agent)
Additional Terms
Internet Database
References
DrugDex Drug Evaluation, vol 105, 2000
