【中文品名】布舍瑞林 【药效类别】抗肿瘤药 【通用药名】BUSERELIN 【别　　名】Hoe-766, Profact, Receptal, S-746766, Suprecor, Suprecur, Suprefact, Suprefakt 【化学名称】 1-9-Luteinizing hormone-releasing factor (swine), 6-[O-(1,1-dimethylethyl)-D-serine]-9-(N-ethyl-L-prolinamide)- 【CA登记号】[57982-77-1] 【结 构 式】 【分 子 式】CHNOPS· 【分 子 量】 【收录药典】 【开发单位】HMR 【首次上市】1984年，德国 【性　　状】 【用　　途】 一种合成的戈那瑞林类似物。用于治疗晚期前列腺癌、子宫内膜异位和子宫肌瘤。对绝经期妇女乳腺癌患者，本品和卵巢切除术效果相同. 布舍瑞林 Buserelin〔Ⅰ〕 （Suprefact） 　　 【制剂】注射液：1mg(1ml)喷鼻液：1mg(1ml)，喷1次100μg 　　 【药理及应用】GnRH类似物。使用初期可促使LH、FSH和性激素分泌增加，经1～2周开始产生相反作用，性激素分泌可降低到去势水平。临床主要用于前列腺癌、乳腺癌等。开始时皮下注射〔男性配合使用氟他胺(Flutamide)〕，维持治疗则采用鼻腔喷入 　　 【用法】皮下注射：每次500μg，1日3次，连续7天。鼻腔：每次100～200μg，1日3次 　　 【注意】可有面部发热、恶心、呕吐、头痛、皮疹、无力、骨痛、性欲减低、排尿困难等。过敏者，应停药。孕妇、哺乳期、对苯甲醇过敏者忌用 features Buserelin Generic name: buserelin nasal spray Brand name: Suprefact Active ingredient: buserelin Package: Nasal Spray17.5ml N1 Manufacturer: Flumed-Farm SRL What is it used for? Endometriosis (nasal spray only). Fertility treatment (nasal spray or injection). This medicine is used to prepare the pituitary gland before starting treatment with gonadotrophins (FSH and LH) to artificially stimulate ovulation. Advanced prostate cancer in men. Suprefact nasal spray both contain the active ingredient buserelin, which is a type of medicine known as a gonadorelin (LHRH) analogue. It acts on the pituitary gland in the brain. The pituitary gland produces and stores various hormones, including the sex hormones, luteinizing hormone (LH) and follicle-stimulating hormone (FSH). In women, FSH and LH cause the production of estrogen by the ovaries and help control the menstrual cycle. The amount of LH and FSH released from the pituitary gland is controlled by another hormone, called gonadorelin (LHRH). Gonadorelin acts on LHRH receptors in the pituitary gland, causing the release of LH and FSH and hence the subsequent production of estrogen in women. Buserelin is a synthetic form of gonadorelin. It acts on the LHRH receptors in the pituitary gland in the same way as natural gonadorelin. Initially, buserelin causes an increase in the amount of FSH and LH released from the pituitary gland, with resulting increase in estrogen production. However, chronic administration of buserelin desensitizes the pituitary gland. This means that it produces less and less FSH and LH, which in turn stops the production of estrogen in women. This reduction in the level of estrogen is used to treat endometriosis. Endometriosis is a condition where tissue resembling the womb or uterus lining (endometrial) grows in other sites in the body. The growth of this tissue is stimulated by estrogen, so decreasing estrogen levels with buserelin will stop the growth of this tissue, thereby relieving symptoms. Buserelin is given by nasal spray to treat endometriosis. A six month course of treatment is recommended and this should not be exceeded or repeated. Buserelin is also used in fertility treatment. In women who are infertile due to problems with their natural ovulation, it is used desensitize the pituitary gland and stop the natural production of FSH and LH. Synthetic FSH, LH and hCG (gonadotrophins) are then administered to artificially stimulate ovulation. Buserelin can be given by injection under the skin (subcutaneously) or by nasal spray for infertility treatment. The buserelin in Suprefact nasal spray is absorbed into the bloodstream through the rich supply of blood vessels found in the lining of the nose. The medicine is absorbed even if you have a cold, however if this is the case, you should blow your nose thoroughly before using the spray. The growth of some prostate cancers is stimulated by testosterone. Reducing the body's levels of testosterone therefore deprives the tumour of testosterone and causes it to shrink. Treatment is started with buserelin injection, which is administered under the skin (subcutaneously) every eight hours for seven days. After this, the treatment is continued with buserelin nasal spray, used six times a day in each nostril. The medicine is absorbed into the bloodstream through the rich supply of blood vessels found in the lining of the nose. The medicine is absorbed even if you have a cold. As the buserelin may at first increase testosterone levels, it may cause an initial temporary tumour 'flare' with symptoms such as urinary obstruction and bone pain, before the cancer begins to shrink. Some men may be particularly prone to these symptoms. If this applies to you, your doctor will also treat you with another type of anti-cancer medicine, known as an anti-androgen (eg cyproterone acetate or flutamide) to prevent this. The anti-androgen will be started three days before the buserelin and continued for the first two to three weeks of treatment. What are the Contraindications? Children. Women who have passed the menopause. Pregnancy. Breastfeeding. Vaginal bleeding of unknown cause. Hormone dependent cancer. This medicine should not be used if you are allergic to one or any of its ingredients. Please inform your doctor or pharmacist if you have previously experienced such an allergy. If you feel you have experienced an allergic reaction, stop using this medicine and inform your doctor or pharmacist immediately. What are the Side reactions? Medicines and their possible side effects can affect individual people in different ways. The following are some of the side effects that are known to be associated with this medicine. Just because a side effect is stated here does not mean that all people using this medicine will experience that or any side effect. Nasal irritation, nose bleeds, hoarseness and taste or smell disturbances (only applicable to the nasal spray). Hot flushes. Increased sweating. Dry vagina. Decreased sex drive. Decrease in bone density. Change in breast size. Breast tenderness. Splitting nails. Dry skin or eyes. Fluid retention, causing swelling (edema) of the face, arms or legs. Disturbances of the gut such as diarrhea, constipation, nausea, vomiting or abdominal pain. Production of breast milk. Dizziness. Awareness of your heartbeat (palpitations). Anxiety or nervousness. Headache. Sleep disturbances. Blurred vision. Tiredness. Appetite and weight changes. Increase or decrease in scalp or body hair. Blood disorders. The side effects listed above may not include all of the side effects reported by the medicine's manufacturer. For more information about any other possible risks associated with this medicine, please read the information provided with the medicine or consult your doctor or pharmacist.