Busarlin 0.5
(Buserelin acetate 0.5mg/0.5ml)

Drug Effects

Synonyms(It is also Known As)


  • Buserelin (OS: BAN)
  • Buserelina (OS: DCIT)
  • Buséréline (OS: DCF)
  • Hoe 766 (IS)
  • S 746766 (IS)
  • Buserelin (PH: BP 2011, Ph. Eur. 7)
  • Buséréline (PH: Ph. Eur. 7)
  • Buserelinum (PH: Ph. Eur. 7)
  • Buserelin Acetate (OS: JAN, USAN, BANM).

Chemical Structure


Chemical Formula


C62H90N16O15 .

Usage


  • Buserelin is used to treat cancer of the prostate gland.
  • It is similar to a hormone normally released from the hypothalamus gland. When given regularly, buserelin decreases testosterone levels. Reducing the amount of testosterone in the body is one way of treating cancer of the prostate.

Adverse Effect


  • Bone pain
  • numbness or tingling of the hands or feet
  • trouble with urinating
  • weakness in the legs
  • Mechanism Action


    Buserelin stimulates the pituitary gland's gonadotrophin-releasing hormone receptor (GnRHR). Buserelin desensitizes the GnRH receptor, reducing the amount of LH and testosterone. However, there is a concomitant surge in LH and testosterone levels with the decrease in androgens, so antiandrogens must administered

    Drug Interaction


    • If you are taking more than one medicine they may interact with each other. At times your prescriber may decide to use medicines that interact, in other cases this may not be appropriate.
    • The decision to use medicines that interact depends on your specific circumstances. Your prescriber may decide to use medicines that interact, if it is believed that the benefits of taking the medicines together outweigh the risks. In such cases, it may be necessary to alter your dose or monitor you more closely.
    • Tell your prescriber the names of all the medicines that you are taking so that they can consider all possible interactions. This includes all the medicines which have been prescribed by your GP, hospital doctor, dentist, nurse, health visitor, midwife or pharmacist. You must also tell your prescriber about medicines which you have bought over the counter without prescriptions.
    • The following types of medicine may interact with Buserelin acetate:

    • anticonvulsants
    • antidiabetics
    • corticosteroids
    • gonadotrophins
    • sex hormones
    • If you are taking Buserelin acetate and one of the above types of medicines, make sure your prescriber knows about it.

     

    Pregnancy Category


    Pregnancy Category X- Studies in animals or humans have demonstrated fetal abnormalities and/or there is positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience, and the risks involved in use of the drug in pregnant women clearly outweigh potential benefits.

    Absorption


    Oral Absorption low, due to proteolysis in the GI tract4.

    Distribution


    high concentrations in liver; low concentrations in kidney, pituitary, thyroid .

    Metabolism


    liver, kidney, hypothalamus, pituitary gland6: enzymatic degradation by pyroglutamate aminopeptidase, endopeptidase, and post-proline-cleaving enzymes.

    Elemination


    urine 13-30%: 67% as buserelin, 32% as buserelin-(5-9)-pentapeptide feces7 bile: unchanged drug and metabolites terminal half life 72-80 min Excretion clearance no information found 

    References


    1. http://products.sanofi.ca/en/suprefact.pdf

    2. http://www.abbiolabs.com/Products/CEK010007Buserelin.pdf

    3. http://www.nhs.uk/ipgmedia/national/macmillan%20cancer%20support/assets/buserelin(suprefact)(cb).pdf.