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Primary information
ThPP IDTh1127
Therapeutic Peptide/Protein NameBuserelin
SequencepGlu-His-Trp-Ser-Tyr-D-Ser(tBu)-Leu-Arg-Pro-NHEt view full sequnce in fasta
Functional ClassificationIIIc
Molecular WeightN.A.
Chemical FormulaC62H90N16O15
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)N.A.
Half Life50-80 minutes by IV dose, 80 mins. By SC dose, 1-2 hrs by Intranasal dose
DescriptionBuserelin is a luteinizing hormone-releasing hormone (LHRH) agonist. It is a synthetic hormone which stimulates the pituitary gland's gonadotrophin-releasing hormone receptor (GnRHR) and is used in prostate cancer treatment.
Indication/DiseaseBuserelin may be used in the treatment of hormone-responsive cancers such as prostate cancer or breast cancer, estrogen-dependent conditions (such as endometriosis or uterine fibroids), and in assisted reproduction.
PharmacodynamicsN.A.
Mechanism of ActionBuserelin 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.
ToxicityN.A.
MetabolismN.A.
AbsorptionN.A.
Volume of DistributionN.A.
ClearanceN.A.
CategoriesN.A.
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionN.A.
TargetLutropin-choriogonadotropic hormone receptor,Gonadotropin-releasing hormone receptor
Information of corresponding available drug in the market
Brand NameSuprecur (Nasal Spray Solution)
CompanySanofi-Aventis
Brand DiscriptionIt contains a medicine called buserelin acetate. This belongs to a group of medicines called gonadotropin releasing hormone analogues. This is a synthetic version of a hormone that occurs naturally in the body. It works by lowering the production of sex hormones.
Prescribed forTreatment of endometriosis – an illness where some of the tissues that line the womb are found elsewhere in the body. As part of a treatment for infertility – it works by stopping the natural production of hormones that control ovulation. Synthetic hormones are then used to artificially stimulate ovulation. Your doctor should give you more information about how your treatment works
Chemical NameN.A.
FormulationEach spray dose contains 150 micrograms of the active substance, buserelin as buserelin acetate. The other ingredients are citric acid, sodium citrate, sodium chloride and benzalkonium chloride in aqueous solution
Physcial Appearnce150 micrograms Nasal Spray Solution
Route of AdministrationNasal spray
Recommended DosageTreatment of endometriosis: The usual dose is one spray in each nostril three times each day. This is to make a total daily dose of 900 micrograms; Use the spray in the morning, at mid-day and in the evening; Treatment will be for a maximum of 6 months;Treatment should be started on the first or second day of your menstrual period.This is to lower the chances you may be pregnant. Your doctor may perform a pregnancy test if there is any doubt; You may get a menstrual period after the first few weeks of using this medicine. You may also carry on getting breakthrough bleeding or spotting As part of treatment for infertility.
ContraindicationDo not use this medicine and tell your doctor if: You are allergic (hypersensitive) to buserelin or goserelin, benzalkonium chloride or other ingredients of Suprecur Nasal Spray. Signs of an allergic reaction include: a rash, swallowing or breathing problems, swelling of your lips, face, throat or tongue; You have abnormal menstrual bleeding where the cause is not endometriosis; You have a tumour that is not affected by hormones; You are pregnant or breast-feeding.This medicine is for use in women only. If you are not sure, talk to your doctor or pharmacist before using Suprecur Nasal Spray.
Side Effects Allergic reaction, diarrhoea, pain, swelling or a feeling of tension in stomach, weight gain, difficulty in breathing, decreased urination. These could be signs of a serious side effect called ’Ovarian Hyperstimulation Syndrome’. This is more likely if you are taking other hormones as well as Suprecur Nasal Spray (buserelin) as part of a treatment for infertility.
Useful Linkhttp://www.drugs.com/uk/pdf/leaflet/468555.pdf
PubMed ID25496312, 25293536, 25276180, 24690459, 24657556
3-D StructureN.A.