Buserelin


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : SC Advanced prostate carcinoma Initial: 500 mcg 8 hrly for 7 days. Maintenance: 200 mcg once daily. Depot 6.3 mg implant 8 wkly or 9.45 mg 12 wkly. Pituitary desensitisation before ovulation induction w/ gonadotrophins 200-500 mcg/day until pituitary downregulation occurs, usually for 1-3 wk. Nasal Endometriosis 150 mcg into each nostril 3 times/day for about 6 mth. Pituitary desensitisation before ovulation induction w/ gonadotrophins 150 mcg 4 times/day beginning on day 1 or day 21 of the menstrual cycle until pituitary downregulation occurs, usually for 1-3 wk.
Dosage Details
Nasal
Pituitary desensitisation before ovulation induction with gonadotrophins
Adult: 150 mcg 4 times daily intranasally, beginning either on day 1 or day 21 of the menstrual cycle. Therapy should be continued until pituitary downregulation occurs, which normally takes 1-3 wk; if necessary, 300 mcg 4 times daily may be given.

Nasal
Endometriosis
Adult: 150 mcg sprayed into each nostril tid. Usual treatment duration: About 6 mth.

Subcutaneous
Advanced prostatic carcinoma
Adult: Initially, 500 mcg injected every 8 hr for 7 days. Maintenance: 200 mcg once daily. Alternatively maintenance may also be given intranasally: 200 mcg into each nostril tid. For depot preparations: 6.3 mg implant every 8 wk or 9.45 mg every 12 wk; to be injected into lateral abdominal wall. An anti-androgen treatment such as cyproterone acetate may be given for at least 3 days before starting therapy and continued for at least 3 wk to prevent disease flare.

Subcutaneous
Pituitary desensitisation before ovulation induction with gonadotrophins
Adult: 200-500 mcg daily. Therapy should be continued until pituitary downregulation occurs, which normally takes 1-3 wk; if necessary, 500 mcg bid may be given.
Contraindications
Hormone-dependent tumors. Pituitary adenoma, weight-related amenorrhoea.
Special Precautions
Hypertension, diabetes, depression, polycystic ovarian disease. Avoid use of nasal decongestants before and at least 30 min after treatment. Men at risk from tumor flare. Pregnancy and lactation.
Adverse Reactions
GI disturbances, headache/lightheadedness, increase in menstrual bleeding, mood changes, nervousness, palpitations, acne, dry skin, decreased glucose tolerance, changes in scalp and body hair, ovarian hyperstimulation, reactions or pain at site of injection, thrombophloebitis, swelling, pruritus, hypersensitivity reactions, tumor flare (may manifest as increase in bone pain), spinal cord compression, worsening of urinary tract symptoms with hematuria and urinary obstruction, vag dryness, hot flushes, loss of libido, osteoporosis. In men, hot flushes, breast swelling, tenderness and sexual dysfunction.
Drug Interactions
Drugs affecting pituitary secretion of gonadotrophins, hormonal therapy and corticosteroids may alter the response. Spironolactone and levodopa can stimulate secretion of gonadotrophins. Phenothiazines, dopamine antagonists, digoxin and sex hormones can inhibit gonadotrophin secretion.
Lab Interference
Alterations in liver function tests and blood lipids.
Action
Description: Buserelin is an analogue of gonadorelin. It stimulates the synthesis and release of follicle-stimulating hormone and luteinising hormone in the anterior lobe of the pituitary. A single dose has the effect of increasing circulating sex hormones; continued admin leads to down regulation of gonadotropin synthesis in the pituitary and results in paradoxical reduction in sex hormone secretion.
Pharmacokinetics:
Absorption: Completely absorbed after SC inj. Plasma concentrations peak about 1 hr after admin.
Metabolism: Metabolised by tissue peptidases.
Excretion: Excreted in urine and bile as unchanged drug and metabolites. Half-life: 80 minutes.
Disclaimer: This information is independently developed by MIMS based on Buserelin from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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