甲羟孕酮(DEPO-PROVERA仿制药)MEDROXYPROGESTERONE

药店国别： 产地国家：美国 处方药：是 所属类别： 150毫克/毫升/注射器/盒 包装规格： 150毫克/毫升/注射器/盒 计价单位：盒 生产厂家中文参考译名： 生产厂家英文名： 原产地英文商品名：MEDROXYPROGESTERONE(DEPO-PROVERA GENERIC) 150MG/ML/SYRINGE/BOX 原产地英文药品名：MEDROXYPROGESTERONE ACETATE 中文参考商品译名：甲羟孕酮(DEPO-PROVERA仿制药) 150毫克/毫升/注射器/盒 中文参考药品译名：醋酸甲羟孕酮

简介

部分中文甲羟孕酮处方资料(仅供参考) 分类名称 一级分类：妇产科用药 二级分类：避孕药 三级分类：长效避孕药 药品英文名：Medroxyprogesterone 药品别名：安宫黄体酮、得普乐、狄波-普维拉、甲孕酮、麦普安、法禄达、羟甲孕酮、Farlutal、Provera、Deporone、MDPA、Depo-Provera 药物剂型 1.片剂：2mg，4mg，10mg， 2.注射剂：150mg; 3.长效注射剂(粉)：150mg; 4.环甲孕酮油注射剂：含本品25mg与环戊雌醇5mg; 5.甲羟孕酮硅橡胶阴道环：含本品100～200mg。 药理作用 本品为作用较强的孕激素，无雌激素活性。口服或注射后在体内适量内源性雌激素基础上，可将增生期子宫内膜转变为分泌期内膜，为受精卵植入做准备。其孕激素活性于皮下注射时为黄体酮的20～30倍，口服时为炔孕酮的10～15倍。主要作用为促进子宫内膜增殖分泌，完成受孕准备，保护胎儿安全生长;也具有改变月经周期、增强宫颈黏液稠度和抑制排卵等作用。 大剂量的本品具有抗肿瘤作用，也具有显著的增进患者食欲、缓解疼痛。本药有对抗雌激素的作用，但不对抗雌激素对脂蛋白的良性作用，亦无明显雄激素效应，最接近天然的孕酮。主要能增加宫颈黏液黏稠度，大剂量可抑制垂体促性腺激素而抑制排卵，有长效抗生育作用。本品作为抗肿瘤激素使用时，通过多年的实验和临床研究证明本类制剂可有双重作用，并与剂量相关。 1.通过负反馈作用抑制垂体前叶，使促黄体激素(LH)、促肾上腺皮质激素(ACTH)及其他生长因子的产生受到抑制。 2.大剂量照射对敏感细胞具有直接细胞毒作用。本品主要通过使细胞内的雌激素受体(ER)不能更新，抵消雌激素的促进肿瘤细胞生长的效应，而对耐药的细胞则无此作用。对子宫内膜癌病理检查可看到染色体的损伤。本品还可通过增强E2-脱氧酶的活性从而降低细胞内雌激素的水平，诱导肝5α-还原酶使雄激素不能转变为雌激素等。 药动学 口服吸收率平均为5.7%，腹腔注射生物利用度优于口服及肌内注射，而且耐受性好。血浆半衰期为4～5h，肌内注射后储存在局部组织中缓慢释放，产生长效作用，可维持2～4周以上，剂量较大时可达3个月之久。口服经肝代谢，1～2天内以硫酸盐和葡萄糖醛酸盐形式主要从尿中排泄。在母乳中有分泌。药物代谢个体差异性较大。 适应证 1.大剂量可用作长效避孕。临床常用于痛经、功能性闭经、功能失调性子宫出血、先兆流产或习惯性流产、子宫内膜异位等。 2.大剂量也可用于治疗肾细胞癌、乳腺癌、子宫内膜癌、前列腺癌及增强晚期癌症患者的食欲，改善一般状况和增加体重。 禁忌证 血栓性静脉炎、血栓栓塞、脑卒中、严重肝肾功能不全、已知或怀疑乳房或生殖器恶性肿瘤、高钙血症、过期流产、子宫出血、妊娠、凝血功能障碍或对本品过敏的患者禁用。 注意事项 1.有精神抑郁者慎用。 2.治疗前应全面体检(特别是乳腺与盆腔检查)。长期用药需注意检查肝功能，特别注意乳房检查。 3.孕激素可引起一定程度体液潴留，癫痫、偏头痛、哮喘等情况应严密观察。 4.在应用过程中有血栓形成的征象，如突发视力障碍、复视、偏头痛，应立即检查。如有视盘水肿或视网膜血管病变，应立即停药。 5.长期给本品应按28天周期计算本品的用药日期。 6.长期使用本品的妇女不宜吸烟。 7.大剂量(500mg以上)服用时，应取坐位或立位，饮足量水。必要时，可将片剂分为两半服用。 8.注射剂不得与其他药品混合使用，用前摇匀。 9.绝经后应用雌激素替代疗法者，加用孕激素7天以上可降低内膜增生发生率。用孕激素12～14天可提供最佳的内膜成熟并消除增生变化。 10.室温下保存。 11.肌内注射应用长的粗针头做深部注射，如此可以减少局部无菌性脓肿或炎性浸润。用于肿瘤患者时，必须在有经验的肿瘤化疗医师的指导下使用，当发生血栓栓塞、偏头痛或眼疾病时停止使用。大剂量长期用药会产生肾上腺皮质激素反应，尤其要注意糖尿病和高血压患者。本品可能引起阴道出血，但要注意排除更严重的诱因。早期妊娠使用本品会使胎儿产生先天性心脏发育不全。动物(小猎犬)长期用药导致了乳房结节的产生，这些小结节是恶性的，但人体上尚未有相同的报道。 不良反应 1.可发生突破出血、点滴出血、经量改变、闭经、水肿、体重变化(增加或减少)、胆汁淤积性黄疸、过敏反应、皮疹、精神抑郁、失眠、恶心。如发生突破出血，应详细检查排除器质性疾病，可根据出血量加服炔雌醇0.05～0.1mg，连服3天，即可止血。 2.大剂量用于肿瘤可引起孕酮类反应如乳房疼痛、溢乳、阴道出血、闭经、月经不调、宫颈分泌异常、子宫糜烂等;长期应用也有肾上腺皮质功能亢进的表现如满月脸、库欣综合征、体重增加等。亦可产生类似皮质激素的影响，如可引起体重增加、腹痛、头痛、情绪改变、手颤、出汗、夜间小腿痉挛等肾上腺素类似的反应。也有引起阻塞性黄疸的报道。 3.本品可引起凝血功能异常。用法用量1.避孕：长效甲羟孕酮粉针剂配成水混悬液注射，每3个月肌内注射150mg，于月经2～7天给药。环甲孕酮油注射剂为每月注射1针。产妇于分娩4周后再开始使用。甲羟孕酮阴道环为本品缓释系统，行经时取出，可连续使用3～6个月。2.先兆流产：口服每次4～8mg，每天2～3次。3.习惯性流产：开始3个月，每天服10mg，第4～4.5个月每天20mg，最后减量停药。 4.痛经：月经周期第6天开始，每天2～4mg，连服20天;或于月经第1天开始，每天3次，连服3天。 5.功能性闭经：每天4～8mg，连用5～10天。 6.子宫内膜异位症：可从每天6～8mg开始，逐渐增加至每天总量20～30mg，连用6～8周。 7.用于肿瘤：口服每天500～1000mg。1次或分2次服用，连用10天。以后视病情改为每天250～500mg，可长期服用。肌内注射开始每次500mg，每天1次.最多4周，以后改为每周3次。 8.用于子宫内膜癌和前列腺癌：每天0.2～0.5g; 9.用于肾腺癌：每天0.2～0.5g。10.肌内注射：(1)用于乳腺癌：每天0.5～1.0g，连续4周，然后每2周肌内注射0.5g，维持治疗或口服每天1.0～1.5g;(2)用于子宫内膜癌和前列腺癌：肌内注射每次0.5g，每周2次，然后改为维持剂量每周肌内注射0.5g或口服每天0.2～0.5g。 药物相应作用 与氨鲁米特同用，可降低氨鲁米特的生物利用度。专家点评本品为作用较强的孕激素，无雌激素活性，口服和注射均有效。其孕激素活性于皮下注射时为黄体酮的20～30倍。口服时为炔孕酮的10～15倍。国内报道，对60例各种肿瘤患者分为3组：A组(20例)第1周期为化疗加用甲羟孕酮，第2、3周期单用化疗;B组(20例)第1周期单用化疗，第2周期为化疗加用甲羟孕酮，第3周期单用化疗;C组(20例)第3个周期均用化疗加用甲羟孕酮。甲羟孕酮用量为每次500mg，每天2次，连续3～9周。结果3组患者大多数人进食增加，分别占75.0%、80%、90.0%;3组中体重增加的患者分别为85.0%、80.0%、95.0%。按WHO骨髓受抑的毒性标准，达Ⅲ度以上者，单化疗组为52.8%;化疗甲羟孕酮组19.0%甲羟孕酮可明显改善化疗药的上述毒副作用，有增强化疗患者食欲及体重、保护骨髓功能的作用，不失为一种有益的化疗保护药。

英文版说明书

Pharmacological action:The active substance (INN) Medroxyprogesterone .(Medroxyprogesterone)The use of Provera: Contraception, particularly in women of late reproductive age inoperable, recurrent and metastatic carcinoma of the endometrium and kidney (additional palliative therapy), hormone-dependent forms of recurrent breast cancer in postmenopausal period of women.Inside – secondary amenorrhea, dysfunctional uterine bleeding, premenstrual syndrome, vasomotor symptoms of menopause, endometriosis, the diagnosis of primary and secondary amenorrhea, prevention and treatment of osteoporosis in postmenopauznom period (in combination with estrogen and calcium supplementation), prevention of endometrial changes in replacement therapy estrogen in postmenopausal women.Contra-Provera: hypersensitivity, thrombophlebitis, thromboembolic syndrome or a history of stroke, liver disease, vaginal bleeding of unspecified etiology, pregnancy, breastfeeding (stop).Side effects: Menstrual irregularities, thromboembolism, insomnia, irritability, drowsiness, fatigue, weakness, depression, dizziness, headache, edema, nausea, abdominal pain and abdominal discomfort, breast tenderness, galactorrhea, cervical erosion, hirsutism, alopecia , fever, weight change, moon face, osteoporosis, urticaria, pruritus, acne, anaphylaxis and anaphylactoid reactions.Interaction: aminoglutethimide reduces plasma concentrations and reduces efficiency.Dosage and administration: V / m, as a contraceptive and for the removal of vasomotor symptoms of menopause – 150 mg 1 time in 3 months, with endometriosis, 50 mg 1 time per week or 100 mg of 1 every 2 weeks course of at least 6 months.B / B with endometrial cancer or kidney disease – 400-1000 mg weekly, while achieving clinical improvement – 400 mg 1 time per month.Inside, in endometrial cancer or kidney disease – 200-600 mg / day for breast cancer – 400-1200 mg / day. For the prevention and treatment of osteoporosis in postmenopausal women – from 12-15 to 25 day of the month at 5-10 mg 1 time a day.Precautions: The first method should be used only on the 5th day of normal menstrual period (guarantee of the absence of pregnancy). You must use an additional contraceptive method for 2 weeks after the first injection. Every three months we recommend an injection of the drug (increased reliability of contraception), when the cycle changes during the reception of required medical consultation. With dysfunctional uterine bleeding necessarily rule out uterine cancer, and other organic lesions. Suspicion for the development of thrombophilic states (thrombophlebitis, cerebrovascular disorders, pulmonary artery branches thromboembolism, renal thrombosis) require immediate repeal. Care must be taken for epilepsy, migraine, asthma, cardiac and renal failure, given the possible delay of the liquid. With care prescribe for patients with diabetes, depression.Special instructions: The intake of medroxyprogesterone may change the results of laboratory tests (including sulfabromoftaleinovogo and other liver function tests) – reduction of steroids in plasma and urine (progesterone, estradiol, pregnandiol, testosterone, cortisol), gonadotropins, globulin, sex hormone binding, the level of T3, elevated levels of prothrombin, factors VII, VIII, IX, X.The advantages of injectable contraceptive Provera: * High contraceptive efficacy; * As a result of contraception there is absolutely no need to worry; * Easy to use: Provera is suitable for those women who for one reason or another can not take a daily hormone pills; * Provera helps to significantly reduce the risk of inflammatory diseases of the genital organs and ectopic pregnancy; * Decrease the frequency of metabolic changes, as the drug does not pass through the liver; * Provera provides a therapeutic effect of endometriosis, premenstrual syndrome and menopausal syndrome, some of the menstrual cycle; * Provera reduces the intensity of menstruation and menstrual pain; * Provera may make breast-feeding women and women with high blood pressure, headaches; * Ease of use and privacy: invisible injection, and the fact of birth may be kept secret, that is for some women is extremely important.First injection of a woman can be done in 3 – 5 days of the menstrual cycle. For those who want to use Provera after birth, the injection should be carried out within five days after delivery for breastfeeding mothers – only 6 weeks. During the first 2 weeks after the first injection of the drug should be used in addition to any non-hormonal contraceptive.There can be subsequent injections made about once every three months exacted, then every 12 weeks and 5 days. Such regimes are due to the peculiarities of the drug and provide it with maximum efficiency. If for any reason, the injection was not made on time, every time, you must first make sure that the woman is not pregnant, and then "catch up". The next 14 days after the "check" our experts recommend the use of additional methods of contraception, with the exception of other hormones (best fit condom or spermicide).Women who use Provera, you need to know what injection can be done only in a medical facility by a qualified doctor or nurse. The spot can not be massaged or rubbed, it is better after a couple of hours to spend in a relaxed atmosphere. During the life of the injectable contraceptive, you must strictly adhere to the deadlines, which gynecologists recommend our center to conduct a special calendar, which record the date made and the date of the next injection. There is also a need to make information about the menstrual cycle (duration, amount of bleeding, mood) and show them to your gynecologist.