Buserelin

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Suprecur; Belgium: Suprefact; Bulgaria: Suprefact Depot; Denmark: Suprecur, Suprefact; Finland: Suprecur, Suprefact Depot; France: Bigonist, Suprefact; Germany: Metrelef, Profact, Suprefact Depot; Greece: Suprecur Depot, Suprefact; Hungary: Suprefact; Ireland: Suprecur, Suprefact; Italy: Suprefact; Luxembourg: Suprefact; Netherlands: Suprefact; Portugal: Suprefact; Spain: Suprecur, Suprefact; Sweden: Suprecur, Suprefact; UK: Suprecur, Suprefact.

North America

Canada: Suprefact.

Latin America

Argentina: Suprefact; Brazil: Suprefact Depot; Mexico: Suprefact Depot.

Asia

Japan: Buserecur, Fuset, Itorelin, Suprecur.

Drug combinations

Chemistry

Buserelin Acetate: C~60~H~86~N~16~O~13~ C~2~H~4~O~2~. Mw: 1299.48. (1) Luteinizing hormone-releasing factor (pig), 6-[O-(1,1-dimethylethyl)-D-serine]-9-(N-ethyl-L-prolinamide)-10-deglycinamide-, monoacetate (salt); (2) 5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-O-tert-butyl-D-seryl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide monoacetate. CAS-68630-75-1; CAS-57982-77-1 (buserelin)(1979).

Pharmacologic Category

Gonadotropin Releasing Hormone Agonists. (ATC-Code: L02AE01).

Mechanism of action

Following an initial rise in the pituitary gonadotropin luteinizing hormone (LH) and follicle-stimulating hormone (FSH), chronic administration of buserelin results in a sustained suppression of LH and FSH and an interference with the production of ovarian and testicular steroids. Eventually, a decline in gonadal steroids to castration levels is observed.

Therapeutic use

Palliative treatment in hormone-dependent advanced prostate cancer (stage D). Treatment of endometriosis in women who do not require surgical intervention as first-line therapy.

Pregnancy and lactiation implications

Buserelin is contraindicated in pregnant women. Not recommended during lactation.

Unlabeled use

Diagnostic test for hypogonadotropic hypogonadism in males with delayed puberty.

Contraindications

Hypersensitivity to buserelin or any component of the formulation. Patients with nonhormone-dependent prostate cancer. Patients who have undergone orchiectomy. Patients with undiagnosed abnormal vaginal bleeding. Pregnancy.

Warnings and precautions

Reactions including allergic asthma with dyspnea as well as rare anaphylactic/anaphylactoid shock observed. A transient (usual duration <10 days) exacerbation of the signs and symptoms of the disease process may be observed with the initiation of therapy. The development of pituitary adenomas may rarely be seen with long-term therapy. Use caution in history of depression. Reduced glucose tolerance noted in rare cases. A transient exacerbation of the signs/symptoms of endometriosis may occur. Oral contraceptives should be discontinued prior to starting therapy. Increases in blood pressure (including hypertensive crisis) may occur in patients being treated for hypertension. Treatment inducing a hypoestrogenic state may lead to changes in bone density. Use of buserelin for >6 months or in association with other risk factors may contribute to additional bone loss. Initiation of therapy without a concomitant antiandrogen agent may lead to a transient worsening of symptoms including bone pain, weakness of leg muscles, impaired micturition, hydronephrosis, lymphostasis, or thrombosis with pulmonary embolus. In prostatic disease, a transient increase in symptoms may occur early in therapy.

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