【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.

【药理作用】
本品为GnRH的类似物。用药初期可促使LH、FSH和性激素分泌增加，经1～2周后产生相反作用，性激素分泌可降低到去势水平。

【临床应用】
主要用于前列腺癌、绝经期前后的乳腺癌及子宫内膜异位症。男性配合使用氟他胺(Flutamide)。

【用药监护】

(1)对GnRH类似物和苯甲醇过敏者、孕妇、哺乳期妇女禁用。有发展为尿道阻塞、脊髓压迫倾向的男性患者慎用，在治疗的第1个月应密切监护。

(2)药物不良反应：男性患者可见潮红、性欲下降、排尿困难，偶见乳房肿胀、触痛；前列腺癌患者在给药初期有骨骼疼痛暂时加重；女性患者有潮红、多汗、性欲下降、头痛、抑郁、阴道干燥、乳房大小的变化，乳腺癌患者在给药初期会有症状的加剧，子宫内膜异位患者可发生停经；女性可能发生骨密度降低，对骨代谢异常的女性应注意。

【用法与用量】

皮下：每日3次，每次0.5mg，连续7日；维持治疗采用鼻腔喷入：每次0.1～

0.2mg，每日3次。

【制剂】

注射剂：1mg；鼻喷剂：1mg(1喷0.1mg)。

【贮法】

避光，密闭，阴凉干燥处保存。

【管理分类】

处方药。

Suprefact Nasal Spray

Product Description

Suprefact Nasal Spray 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. It is used to treat prostate cancer by lowering the amount of the hormone ‘testosterone’. 2. Before you use Suprefact Nasal Spray Do not use this medicine and tell your doctor if: You are allergic (hypersensitive) to: Buserelin Other similar medicines such as goserelin Any of the other ingredients of Suprefact Nasal Spray (listed in Section 6 below) Signs of an allergic reaction include: a rash, swallowing or breathing problems, swelling of your lips, face, throat or tongue You have a tumour that is not affected by changes in hormone levels You have had an operation to remove your testicles Do not use if any of the above apply to you. If you are not sure, talk to your doctor or pharmacist before using Suprefact Nasal Spray. Take special care with Suprefact Nasal Spray Check with your doctor or pharmacist before using your medicine if: T You have depression T You have high blood pressure. Your blood pressure must be checked regularly T You have diabetes. You should check your blood glucose levels regularly T You have metabolic bone disease or have additional risk factors for osteoporosis such as chronic alcohol abuse, smoking, a family history of osteoporosis or are on long term therapy with anticonvulsants or corticosteroids If you are not sure if any of the above apply to you, talk to your doctor or pharmacist before using Suprefact Nasal Spray. Taking other medicines Please tell your doctor or pharmacist if you are taking or have recently taken any other medicines. This includes medicines you buy without a prescription, including herbal medicines. This is because Suprefact Nasal Spray can affect the way some other medicines work. Also some medicines can affect the way Suprefact Nasal Spray works. In particular, tell your doctor or pharmacist if you are taking the following: Medicines for diabetes Pregnancy and breast-feeding This medicine is intended for use in men. However, there is another type of this medicine which can be used in women. Women should not use either type of this medicine if they are pregnant or breast feeding. Driving and using machines You may feel dizzy, drowsy or have blurred eyesight while using this medicine. If this happens, do not drive or use any tools or machines. Important information about some of the ingredients of Suprefact Nasal Spray Suprefact Nasal Spray contains benzalkonium chloride. This may cause difficulty breathing, wheezing or tightness in the chest (bronchospasm). 3. How to use Suprefact Nasal Spray Always use Suprefact Nasal Spray exactly as your doctor has told you. You should check with your doctor or pharmacist if you are not sure. Using this medicine Your doctor will normally give you Suprefact injection for seven days. The doctor will then start you on the nasal spray on the 8th day of your treatment. It is very important you use this medicine regularly and space the doses out evenly through the day This medicine can be used if you have a cold. If you have a cold, blow your nose thoroughly before using the spray. If you are using a nasal decongestant wait at least 30 minutes after using Suprefact Nasal Spray before using the decongestant Your doctor will monitor your hormone levels by taking regular blood samples If you feel the effect of your medicine is too weak or too strong, do not change the dose yourself, but ask your doctor How to use Suprefact Nasal Spray: 1. Preparing the spray Remove the screw cap from bottle Remove the metered-dose nebulizer from transparent plastic container and take off both protective caps Screw the nebulizer on to the bottle 2. If you are using the spray for the first time Hold the bottle upright Pump 5 to 8 times until an even spray is produced. This initial pumping is for the purpose of filling the system and testing the spray. It should not be repeated after the first use in order to avoid wasting the medicine 3. Using the spray Keep the bottle upright Bend your head slightly over the bottle Spray the solution into the nose 4. After using the spray After use leave the nebulizer on the bottle After replacing the protective cap on the nebulizer, the spray bottle is best stored in its transparent container in an upright position How much Suprefact Nasal Spray to use: Treatment of Prostate Cancer: The usual dose is one spray in each nostril six times each day. Use the spray: In the morning – before and after breakfast At midday – before and after lunch In the evening – before and after dinner Your doctor will tell you how long to continue using this medicine If you use more Suprefact Nasal Spray than you should If you use more Suprefact Nasal Spray than you should, tell a doctor or go to a hospital casualty department straight away. Take the medicine pack with you. This is so the doctor knows what you have used. The following effects may occur: feeling weak, headache, feeling nervous, hot flushes, feeling dizzy, feeling sick, stomach pain, swelling of the legs and breast pain. If you forget to use Suprefact Nasal Spray If you forget a dose, take it as soon as you remember it. However, if it is nearly time for the next dose, skip the missed dose. Do not take a double dose to make up for a forgotten dose. If you stop using Suprefact Nasal Spray. Keep using Suprefact Nasal Spray until your doctor tells you to stop. If you stop, your prostate cancer may get worse. Blood Tests Using Suprefact Nasal Spray may affect the results of some blood tests. In particular, Suprefact Nasal Spray can change the level of liver enzymes and fats in the blood (lipids) shown up in blood tests. If you are going to have a blood test, it is important to tell your doctor you are using Suprefact Nasal Spray. If you have any further questions on the use of this product, ask your doctor or pharmacist. 4. Possible side effects Like all medicines, Suprefact can cause side effects, although not everybody gets them. Stop using Suprefact and see a doctor or go to a hospital straight away if; You have an allergic reaction. The signs may include: a rash, swallowing or breathing problems, swelling of your lips, face, throat or tongue You have leg pain, difficulty breathing or being short of breath and chest pain. This could be because of blood clots in your body and lungs Tell your doctor straight away if you notice any of the following serious side effects: You bruise more easily than usual. This could be because of a blood problem called ‘thrombocytopenia’ You get a lot of infections. Signs include fever, sore throat or mouth ulcers. These could be signs of a blood problem called leucopenia You have nose bleeds and a hoarse voice Changes in your sense of taste or smell You have severe headaches and eyesight problems. This is very rare but if it happens it could be due to tumours on the pituitary gland. This gland is found at the base of the brain Your blood pressure becomes higher. This is very rare but if it happens you may get symptoms such as crushing chest pain, confusion, problems with your eyesight, tiredness and an uneven heartbeat You have problems passing water (urine) You have sharp pain or aching in your side in the area between the ribs and the hips. These could be signs of a swollen kidney You feel tired and your body is swollen. These could be signs of fluid build up in the tissues called lymphostasis Tell your doctor or pharmacist if any of the following side effects get serious or lasts longer than a few days: Loss of sex drive (libido) Atrophy (shrinking) of the testes Bone or muscle discomfort such as shoulder pain or stiffness or muscle weakness. If Suprefact Nasal Spray is used for a long period of time, it may increase the risk of you getting a condition called ‘osteoporosis’. This is when your bones are more likely to break Lowered tolerance to glucose which may lead to worsening of existing diabetes Changes in body weight, changes in appetite and increased thirst Mood changes such as feeling depressed or worsening of depression and feeling anxious Feeling nervous, dizzy, tired or drowsy Headache and disturbed sleep Problems with memory and concentration Unusual skin sensations such as numbness, tingling, pricking, burning or creeping on the skin. This can feel like ‘pins and needles’ (usually in the arms and legs) and is called paraesthesia Dry eyes (possibly leading to eye irritation in people who wear contact lenses), blurred eyesight, feeling of pressure behind the eyes Hearing problems such as ringing in the ears (tinnitus) Very fast, uneven or forceful heartbeat (palpitations) Facial swelling (puffiness) due to water retention which may also cause swollen arms or legs Feeling or being sick, stomach ache, pain in the lower abdomen, diarrhoea or constipation  Dry skin or acne or hot flushes Hair grows more than normal (including body and facial hair) Hair loss (including body or facial hair) Splitting of nails Increase in breast size or breast tenderness Changes in the level of liver enzymes, fats (lipids) and a substance called ‘bilirubin’ in the blood shown up in blood tests Talk to your doctor or pharmacist if any of the side effects gets serious or lasts longer than a few days, or if you notice any side effects not listed in this leaflet. 5. How to store Suprefact Nasal Spray Keep this medicine in a safe place where children cannot see or reach it. Do not use Suprefact Nasal Spray after the expiry date which is stated on the bottle. The expiry date refers to the last day of that month. Store below 25 °C. Do not freeze. Once opened the product should be used within 1 week. Any remaining spray should be disposed of after this time. Medicines should not be disposed of via wastewater or household waste. Ask your pharmacist how to dispose of medicines no longer required. These measures will help to protect the environment. 6. Further Information What Suprefact Nasal Spray contains Each spray dose contains 100 micrograms of the active substance, buserelin as buserelin acetate The other ingredients are citric acid monohydrate, sodium citrate dihydrate, sodium chloride, benzalkonium chloride and water for injections.