| Primary information |
|---|
| ThPP ID | Th1127 |
| Therapeutic Peptide/Protein Name | Buserelin |
| Sequence | pGlu-His-Trp-Ser-Tyr-D-Ser(tBu)-Leu-Arg-Pro-NHEt view full sequnce in fasta |
| Functional Classification | IIIc |
| Molecular Weight | N.A. |
| Chemical Formula | C62H90N16O15 |
| Isoelectric Point | N.A. |
| Hydrophobicity | N.A. |
| Melting Point (℃) | N.A. |
| Half Life | 50-80 minutes by IV dose, 80 mins. By SC dose, 1-2 hrs by Intranasal dose |
| Description | Buserelin 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/Disease | Buserelin 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. |
| Pharmacodynamics | N.A. |
| Mechanism of 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. |
| Toxicity | N.A. |
| Metabolism | N.A. |
| Absorption | N.A. |
| Volume of Distribution | N.A. |
| Clearance | N.A. |
| Categories | N.A. |
| Patents Number | N.A. |
| Date of Issue | N.A. |
| Date of Expiry | N.A. |
| Drug Interaction | N.A. |
| Target | Lutropin-choriogonadotropic hormone receptor,Gonadotropin-releasing hormone receptor |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Suprecur (Nasal Spray Solution) |
| Company | Sanofi-Aventis |
| Brand Discription | It 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 for | Treatment 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 Name | N.A. |
| Formulation | Each 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 Appearnce | 150 micrograms Nasal Spray Solution |
| Route of Administration | Nasal spray |
| Recommended Dosage | Treatment 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. |
| Contraindication | Do 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 Link | http://www.drugs.com/uk/pdf/leaflet/468555.pdf |
| PubMed ID | 25496312, 25293536, 25276180, 24690459, 24657556 |
| 3-D Structure | N.A. |