英文药名: Medrol(methyl prednisolone tablets) 中文药名: 美卓乐(甲基泼尼松片) 品牌药生产厂家: Pfizer 药品名称 美卓乐 Medrol 甲基泼尼松片 生产厂家 Pfizer 辉瑞 药理作用 甲泼尼龙属合成的糖皮质激素。糖皮质激素透过细胞膜，并与胞浆内特异的受体结合。此结合物随后进入细胞核内与DNA（染色体）结合，启动mRNA的转录，继而合成各种酶蛋白，据认为全身给药的糖皮质激素最终通过这些酶发挥多种作用。皮质类固醇的最大药理作用出现在血药峰浓度之后，表明其大部分作用是通过改变酶活性引发的，而不是药物的直接作用。糖皮质激素不仅对炎症和免疫过程有重要影响，而且影响碳水化合物、蛋白质和脂肪代谢，并且对心血管系统、骨骼和肌肉系统及中枢神经系统也有作用。 作用于炎症和免疫过程：糖皮质激素的大部分治疗作用都与它的抗炎、免疫抑制和抗过敏特性有关，这些特性会导致下列结果：减少炎症病灶周围的免疫活性细胞；减少血管扩张；稳定溶酶体膜；抑制吞噬作用；减少前列腺素和相关物质的产生。4 mg甲波尼龙的糖皮质激素样作用（抗炎作用）与20 mg氢化可的松相同。甲波尼龙仅有很低的盐皮质激素样作用（200 mg甲波尼龙等价于1 mg脱氧皮质酮）。 对碳水化合物及蛋白质代谢的作用：糖皮质激素具有分解蛋白质的作用，释出的氨基酸经糖异生过程在肝脏转化为葡萄糖和糖原。由于外周组织对葡萄糖的吸收减少，导致血糖增高和葡萄糖尿，有糖尿病倾向的患者尤其明显。 对脂肪代谢的作用：糖皮质激素具有分解脂肪的作用，该作用主要影响四肢，另外糖皮质激素又具有脂肪合成的作用，该作用在胸部、颈部和头部尤为明显。所有这些导致了脂肪的重新分布。 药代动力学 人体内小肠灌注实验证明，类固醇主要在小肠近端被吸收，远端吸收率约为近端的50%。甲泼尼龙在体内与蛋白和皮质素转运蛋白形成弱的、可解离的结合。结合型甲泼尼龙约为40-90%。甲泼尼龙与可的松同样经肝脏代谢，主要的代谢产物为20-β羟基甲泼尼和20-β-羟基-6α-甲泼尼龙，这些代谢产物以葡萄糖醛酸盐、硫酸盐和非结合型化合物的形式随尿液排出。结合反应主要在肝脏进行，少量在肾脏进行。 适应症 风湿性疾病 作为辅助疗法短期使用（帮助患者度过急性期或危重期）用于：银屑病性关节炎；类风湿性关节炎，包括青少年类风湿性关节炎（个别患者可能需要低剂量维持治疗）；强直性脊柱炎；急性或亚急性滑囊炎；急性非特异性腱鞘炎；急性痛风性关节炎；创伤后骨关节炎；骨关节炎引发的滑膜炎；上踝炎。 用于疾病危重期或作为下列疾病的维持治疗：系统性红斑狼疮；全身性皮肌炎（多肌炎）；急性风湿性心肌炎；风湿性多肌痛；巨细胞关节。 过敏状态 用于控制如下以常规疗法难以处理的严重或损伤机能的过敏性疾病：季节性或全年性过敏性鼻炎；血清病；支气管哮喘；药物过敏反应；接触性皮炎。 眼部疾病 累及眼部及其附属器的严重的急慢性过敏和炎症反应，例如：过敏性角膜边缘溃疡；眼部带状疱疹；眼前段感染；弥漫性后部葡萄膜炎和脉络膜炎；交感性眼炎；角膜炎；脉络膜视网膜炎；视神经炎；虹膜炎、虹膜睫状体炎。 呼吸道疾病 症状性肉瘤病；其它方法不能控制的吕弗勒氏综合征；铍中毒；与适当的抗结核化疗法合用于暴发性或扩散性肺结核；吸入性肺炎。 水肿状态 用于无尿毒症的自发性或狼疮性肾病综合征的利尿及缓解蛋白尿。 胃肠道疾病 帮助患者度过以下疾病的危重期：溃疡性结肠炎和局限性回肠炎。 神经系统 多发性硬化症急性危重期；控制脑部肿瘤引起的水肿。 其它 与适当的抗结核化疗法合用，用于伴有蛛网膜下腔阻塞或趋于阻塞的结核性脑膜炎；累及神经或心肌的旋毛虫病。器官移植。 用法用量 根据不同疾病的治疗需要，初始剂量可在每天4-48 mg之间调整。症状较轻者，通常给予较低剂量即可，某些患者则可能需要较高的初始剂量。临床上需要用较高剂量治疗的疾病包括多发性硬化症（200 mg/天）、脑水肿（200-1000 mg/天）和器官移植（可达7 mg/kg/天）。 若经过一段时间的充分治疗后未见令人满意的临床效果，应停用本药而改用其它合适的治疗方法。若经过长期治疗后需停药时，建议逐渐递减，而不能突然撤药。当临床症状出现好转，应在适当的时段内逐渐递减初始剂量，直至能维持已有的临床效果的最低剂量，此剂量即为最佳维持剂量。还应注意对药物剂量作维持的监测。当出现下列情况时可能需要调整剂量： 病情减轻或加重导致临床表现改变，患者对药物反应的个体差异，以及患者遇到与正在治疗的疾病无关的紧急状况。 在最后一种情况下，可能需要根据患者的情况在一段时间内加大剂量。这里必须强调的是，剂量需求不是一成不变的，必须根据治疗的疾病和患者的反应作个体化调整。 隔日疗法 隔日疗法是一种服用皮质类固醇的方法，即指在隔日早晨一次性给予两天的皮质类固醇总量。采用这种治疗方法旨在为需要长期服药的患者提供皮质激素的治疗作用，同时减少某些不良反应，例如在垂体-肾上腺皮质轴的抑制、类柯兴氏综合征、皮质激素撤药症状和对儿童生长的抑制。 任何疑问，请遵医嘱！ 不良反应 体液及电解质紊乱：钠潴留，某些敏感患者出现充血性心力衰竭、高血压、体液潴留、钾离子流失及低钾性碱中毒。 肌肉骨骼系统：类固醇性肌病，肌无力，骨质疏松，病理性骨折，脊椎压缩性骨折及无菌性坏死。 胃肠道：可能穿孔或出血的消化道溃疡、消化道出血、胰腺炎、食道炎及肠穿孔。 皮肤病：妨碍伤口愈合，瘀点和瘀斑及皮肤脆薄。 代谢：体内蛋白质分解造成的负氮平衡。 神经病：颅内压升高，假性脑肿瘤、精神错乱及癫痫发作。 内分泌：月经失调，引发柯兴氏症、抑制脑垂体-肾上腺皮质轴、糖耐量降低、引发潜在的糖尿病，增加糖尿病患者对胰岛素和口服降糖药的需求及抑制儿童生长。 眼：后房囊下白内障，眼内压增高及眼球突出。 免疫系统：掩盖感染，潜在感染发作，机会性感染，过敏反应及可能抑制皮试反应。 禁忌症 全身性霉菌感染，对甲泼尼龙过敏者。 注意事项 服用皮质类固醇治疗发生异常紧急状况的患者，在紧急状况发生前、发生时和发生后须加大速效皮质类固醇的剂量。皮质类固醇可能会掩盖感染的若干症状，使用期间亦可能发生新的感染。使用皮质类固醇可能会减弱抵抗力而无法使感染局限。 长期服用皮质类固醇可能引发累及视神经的后房囊下白内障、青光眼，而且可能增加眼部继发真菌和病毒感染的可能性。可能发生过敏反应（例如血管神经性水肿）。中剂量和大剂量氢化可的松或可的松能引起血压升高，水钠潴留和失钾过多。除非大剂量服用，合成的衍生物较少出现上述作用，限钠、补钾的饮食可能是必要的。所有皮质类固醇均会增加钙离子的流失。服用皮质类固醇的患者不可接种牛痘，也不可接受其它免疫措施，特别是大剂量服用的患者，因为有出现神经系统并发症和缺乏抗体反应的可能性。 本药用于结核活动期患者时，应仅限于暴发性或扩散性结核病，这时皮质激素可与适当的抗结核病药物联用以控制病情。如皮质类固醇用于结核病潜伏期或结核菌素试验阳性的患者时，必须密切观察以防疾病复发。此类患者长期服用皮质类固醇期间应接受化学预防治疗。关于皮质类固醇治疗是否会导致消化道溃疡尚未达成共识，但服用糖皮质激素会掩盖溃疡的症状，使穿孔或出血在未感到明显疼痛时就出现。长期大剂量服用糖皮质激素往往伴随着骨质疏松，但不易被发现。长期每天分剂量用糖皮质激素会抑制儿童的生长，这种治疗方法只可用于非常危重的情况。通常隔日疗法可避免或减少这种不良反应。大剂量糖皮质激素会抑制宿主的抵抗力从而导致对真菌、细菌和病毒的易感性增加。逐渐递减用药量可减少因用药而产生的肾上腺皮质机能不全现象。这种现象可在停药后持续数月，因而在此期间一旦出现紧急情况应恢复服药。由于盐皮质激素的分泌也可能被抑制，应同时补充盐分和/或给予盐皮质激素。甲状腺功能减退和肝硬化会增强皮质类固醇的作用。皮质类固醇应慎用于眼部单纯疱疹患者，以免引发角膜穿孔。应采用尽可能低的皮质类固醇剂量控制病情。若要减量，应逐渐递减。 服用皮质类固醇可能出现下列精神紊乱的症状：欣快感、失眠、情绪变化、个性改变及重度抑郁直至明显的精神病表现。已有的情绪不稳和精神病倾向可能会因服用皮质类固醇而加重。对凝血酶原过少的患者，皮质类固醇与阿司匹林及非甾体类抗炎药的联用应谨慎。 若有下列情况应慎用皮质类固醇： 可能立即穿孔的非特异性溃疡性结肠炎、脓肿或其它化脓性感染、憩室炎、刚行肠吻合术、消化道溃疡活动期或潜伏期、肾功能不良、高血压、骨质疏松、重症肌无力。 因糖皮质激素治疗的并发症与用药的剂量和时间有关，所以对每个病例均需就剂量，疗程和每天给药还是间隔给药作出风险/利益评价。 致癌性、致突变性和生育力 证据表明皮质类固醇会致癌、致突变和抑制生育能力。 孕妇及哺乳期妇女用药 一些动物试验表明，母亲服用大剂量皮质类固醇可能引起胎儿畸形。因未作过足够的人类生殖研究，因而当皮质类固醇用于孕妇、哺乳妇女或可能怀孕的妇女时，应仔细衡量它对母亲、胚胎或胎儿的利弊，因为没有足够的人类怀孕安全性方面的证据，因此只有当确实需要时，皮质类固醇才可用于孕妇。因皮质类固醇很容易透过胎盘，故对怀孕期间用过大量皮质类固醇的母亲生育的婴儿，应仔细观察和评价是否有肾上腺皮质功能减退的迹象，未见皮质类固醇对分娩有影响。皮质类固醇随乳汁分泌。 药物过量 未发现本药急性过量引起的综合征，长期重复服药（每天一次或每周数次）可能导致柯兴氏症和其它长期激素治疗引发的并发症。 包装规格： 16mg *28片 4mg *100片 8mg*28 片 MEDROL (methylprednisolone) tablet [Pharmacia & Upjohn Company] For Oral Use In Dogs and Cats Caution Federal (USA) law restricts this drug to use by or on the order of a licensed veterinarian. DESCRIPTION Methylprednisolone, a potent anti-inflammatory steroid synthesized and developed in the Research Laboratories of The Upjohn Company is the 6-methyl derivative of prednisolone. It has a greater anti-inflammatory potency than prednisolone and even less tendency than prednisolone to induce sodium and water retention. Its advantage over the older corticoids lies in its ability to achieve equal anti-inflammatory effect with lower dose, while at the same time enhancing the split between anti-inflammatory and mineralocorticoid activities. INDICATIONS The indications for MEDROL Tablets are the same as those for other anti-inflammatory steroids and comprise the various collagen, dermal, allergic, ocular, otic, and musculoskeletal conditions known to be responsive to the anti-inflammatory corticosteroids. Representative of the conditions in which the use of steroid therapy and the benefits to be derived therefrom have had repeated confirmation in the veterinary literature are: (1) dermal conditions, such as non-specific eczema, summer dermatitis, and burns; (2) allergic manifestations, such as acute urticaria, allergic dermatitis, drug and serum reactions, bronchial asthma, and pollen sensitivities; (3) ocular conditions, such as iritis, iridocyclitis, secondary glaucoma, uveitis, and chorioretinitis; (4) otic conditions, such as otitis externa; (5) musculoskeletal conditions, such as myositis, rheumatoid arthritis, osteoarthritis, and bursitis; (6) various chronic or recurrent diseases of unknown etiology such as ulcerative colitis and nephrosis. In acute adrenal insufficiency, MEDROL may be effective because of its ability to correct the defect in carbohydrate metabolism and relieve the impaired diuretic response to water characteristic of primary or secondary adrenal insufficiency. However, because this agent lacks significant mineralocorticoid activity, the parent hormones, SOLU-CORTEF® containing hydrocortisone sodium succinate, CORTEF® containing hydrocortisone, or cortisone should be used when salt retention is indicated. CONTRAINDICATIONS MEDROL Tablets like prednisolone, are contraindicated in animals with arrested tuberculosis, peptic ulcer, acute psychoses, and Cushingoid syndrome. The presence of diabetes, osteoporosis, chronic psychotic reactions, predisposition to thrombophlebitis, hypertension, congestive heart failure, renal insufficiency, and active tuberculosis necessitates carefully controlled use. Some of the above conditions occur only rarely in dogs and cats but should be kept in mind. WARNINGS Not for human use. Clinical and experimental data have demonstrated that corticosteroids administered orally or parenterally to animals may induce the first stage of parturition when administered during the last trimester of pregnancy and may precipitate premature parturition followed by dystocia, fetal death, retained placenta, and metritis. Additionally, corticosteroids administered to dogs, rabbits and rodents during pregnancy have resulted in cleft palate in offspring. Corticosteroids administered to dogs during pregnancy have also resulted in other congenital anomalies including deformed forelegs, phocomelia, and anasarca. PRECAUTIONS Because of its inhibitory effect on fibroplasia, methylprednisolone may mask the signs of infection and enhance dissemination of the infecting organism. Hence, all animal patients receiving methylprednisolone should be watched for evidence of intercurrent infection. Should infection occur, it must be brought under control by use of appropriate antibacterial measures, or administration of methylprednisolone should be discontinued. MEDROL Tablets, like prednisolone and other adrenocortical steroids is a potent therapeutic agent influencing the biochemical behavior of most, if not all, tissues of the body. Because this anti-inflammatory steroid manifests little sodium-retaining activity, the usual early sign of cortisone or hydrocortisone overdosage (ie, increase in body weight due to fluid retention) is not a reliable index of overdosage. Hence, recommended dose levels should not be exceeded, and all animal patients receiving MEDROL should be under close medical supervision. All precautions pertinent to the use of prednisolone apply to methylprednisolone. Moreover, the veterinarian should endeavor to keep informed of current studies with MEDROL as they are reported in the veterinary literature. ADVERSE REACTIONS With therapeutically equivalent doses, the likelihood of occurrence of troublesome side effects is less with methylprednisolone than with prednisolone; moreover, side effects actually have been conspicuously absent during clinical trials with MEDROL Tablets in dogs and cats. However, methylprednisolone is similar to prednisolone in regard to kinds of side effects and metabolic alterations to be anticipated when treatment is intensive or prolonged. In animal patients with diabetes mellitus, use of methylprednisolone may be associated with an increase in the insulin requirement. Negative nitrogen balance may occur, particularly in animals that require protracted maintenance therapy; measures to counteract persistent nitrogen loss include a high protein intake and the administration when indicated, of a suitable anabolic agent. Excessive loss of potassium, like excessive retention of sodium, is not likely to be induced by effective maintenance doses of MEDROL. However, these effects should be kept in mind and the usual regulatory measures employed as indicated. Ecchymotic manifestations, while not noted during the clinical evaluation in dogs and cats, may occur. If such reactions do occur and are serious, reduction in dosage or discontinuance of methylprednisolone therapy may be indicated. Concurrent use of daily oral supplements of ascorbic acid may be of value in helping to control ecchymotic tendencies. Since methylprednisolone, like prednisolone, suppresses endogenous adrenocortical activity, it is highly important that the animal patient receiving MEDROL be under careful observation, not only during the course of treatment but for some time after treatment is terminated. Adequate adrenocortical supportive therapy with cortisone or hydrocortisone, and including ACTH, must be employed promptly if the animal is subjected to any unusual stress such as surgery, trauma, or severe infection. DOSAGE AND ADMINISTRATION The keystone of satisfactory therapeutic management with MEDROL Tablets, as with its steroid predecessors, is individualization of dosage in reference to the severity of the disease, the anticipated duration of steroid therapy, and the animal patient's threshold or tolerance for steroid excess. The prime objective of steroid therapy should be to achieve a satisfactory degree of control with a minimum effective daily dose. The dosage recommendations are suggested average total daily doses and are intended as guides. As with other orally administered corticosteroids, the total daily dose of MEDROL should be given in equally divided doses. The initial suppressive dose level is continued until a satisfactory clinical response is obtained, a period usually of 2 to 7 days in the case of musculoskeletal diseases, allergic conditions affecting the skin or respiratory tract, and ocular inflammatory diseases. If a satisfactory response is not obtained in 7 days, reevaluation of the case to confirm the original diagnosis should be made. As soon as a satisfactory clinical response is obtained, the daily dose should be reduced gradually, either to termination of treatment in the case of acute conditions (eg, seasonal asthma, dermatitis, acute ocular inflammations) or to the minimal effective maintenance dose level in the case of chronic conditions (eg, rheumatoid arthritis). In chronic conditions, and in rheumatoid arthritis especially, it is important that the reduction in dosage from initial to maintenance dose levels be accomplished slowly. The maintenance dose level should be adjusted from time to time as required by fluctuation in the activity of the disease and the animal's general status. Accumulated experience has shown that the long-term benefits to be gained from continued steroid maintenance are probably greater the lower the maintenance dose level. In rheumatoid arthritis in particular, maintenance steroid therapy should be at the lowest possible level. Important: In the therapeutic management of animal patients with chronic diseases such as rheumatoid arthritis, methylprednisolone should be regarded as a highly valuable adjunct, to be used in conjunction with but not as replacement for standard therapeutic measures. Average total daily oral doses for dogs and cats: 5 to 15 lb body wt 2 mg 15 to 40 lb body wt 2 to 4 mg 40 to 80 lb body wt 4 to 8 mg The total daily dose should be given in divided doses, 6 to 10 hours apart. HOW SUPPLIED Veterinary MEDROL Tablets are compressed cross-scored tablets available in bottles of 500. Each 4 mg tablet contains 4 mg methylprednisolone. Store at controlled room temperature 20° to 25° C (68° to 77° F).