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Generic Name and Formulations:
Diclofenac sodium 75mg (e-c), misoprostol 200mcg; tabs.
Company:
Pfizer Inc.
Indications for ARTHROTEC 75:
Osteoarthritis (OA) or rheumatoid arthritis (RA) in patients at high risk for developing NSAID-induced gastric or duodenal ulcers.
Adult Dose for ARTHROTEC 75:
Swallow whole; food may reduce diarrhea. ≥18yrs: OA: one Arthrotec 50 tab 3 times daily. RA: one Arthrotec 50 tab 3–4 times daily. Both: if not tolerated, may reduce to one Arthrotec 50 or one Arthrotec 75 tablet twice daily (this may be less effective in preventing ulcers). Concomitant CYP2C9 inhibitors: max Arthrotec 50mg twice daily. See full labeling.
Children's Dose for ARTHROTEC 75:
<18yrs: not established.
See Also:
ARTHROTEC 50
Pharmacological Class:
NSAID + prostaglandin E1 analogue.
Contraindications:
Pregnancy (Cat.X). Aspirin allergy. Coronary artery bypass graft surgery.
Warnings/Precautions:
For women of childbearing potential: obtain negative serum pregnancy test within 2 weeks before start of therapy; begin Arthrotec therapy on 2nd or 3rd day of menstrual period; maintain contraception during therapy; give oral and written warnings on risks in pregnancy. Increased risk of serious cardiovascular events, MI, and stroke. Increased risk of serious GI adverse events (eg, bleeding, ulceration, perforation). Advanced renal disease: not recommended. History of ulcer disease or GI bleeding. Edema. Heart failure. Hypertension. Pre-existing asthma. Hepatic or renal dysfunction. Monitor BP, CBCs, blood chemistry, hepatic and renal function. Check ALT (SGPT) within 4–8 wks then periodically. Discontinue if signs/symptoms of liver or renal disease develop, or if abnormal liver function tests persist or worsen. Hepatic porphyria. Dehydration. SLE. Elderly. Debilitated. Labor & delivery. Avoid in late pregnancy. Nursing mothers: not recommended.
Interactions:
Avoid magnesium-containing antacids, salicylates, aspirin, other NSAIDs. May be potentiated by CYP2C9 inhibitors (eg, voriconazole); caution. May be antagonized by CYP2C9 inducers (eg, rifampin); caution. May antagonize ACE-inhibitors, diuretics. Monitor for digoxin, methotrexate, cyclosporine, lithium, warfarin toxicity. Hyper- or hypoglycemia possible with insulin, oral hypoglycemic agents. Increased risk of GI bleed with oral corticosteroids, anticoagulants (monitor), alcohol, smoking, prolonged NSAID therapy. Increased serum potassium with K+-sparing diuretics. Caution with concomitant drugs that are known to be hepatotoxic (eg, antibiotics, anti-epileptics).
Adverse Reactions:
Abdominal pain, diarrhea, dyspepsia, nausea, flatulence, GI bleed/ulcer, other GI disturbances, rash (may be serious, eg, Stevens Johnson Syndrome; discontinue if occurs), elevated transaminase levels, anemia; anaphylactic reactions, aseptic meningitis (rare). See full labeling re: risk of cardiovascular or GI events.
How Supplied:
Arthrotec 50—60, 90; Arthrotec 75—60
部分中文ARTHROTEC信息资料（仅供参考）
药理作用
本药含双氯芬酸钠和米索前列醇，前者有抗炎、止痛和解热作用，后者对胃和十二指肠黏膜有保护作用。双氯芬酸钠为苯乙酸类非甾体抗炎药，主要通过抑制环氧化酶来阻断花生四烯酸合成前列腺素，也可抑制脂氧化酶来阻断花生四烯酸转化为白三烯，从而发挥抗炎作用。但同其他抗炎药一样，双氯芬酸钠的不良反应以胃肠道症状和黏膜损伤居首位，原因在于双氯芬酸钠抑制胃肠黏膜生理性环氧酶-1，导致对局部有保护作用的前列腺素合成减少。本药中的米索前列醇是一种合成的前列腺素E1类似物，具有抑制胃酸分泌，增加重碳酸盐和黏液含量，及增加胃黏膜血流量等作用，因而对胃黏膜有保护作用。补充这种外源性前列腺素，可预防或减少双氯芬酸钠对胃黏膜产生的不良影响，且不影响双氯芬酸钠的抗炎、止痛和解热作用。有研究表明，本药的疗效与双氯芬酸、吡罗昔康及萘普生相当，但对胃、十二指肠黏膜的保护作用则优于这三种药物。
药动学
本药单次或多次使用，双氯芬酸钠和米索前列醇之间不产生药动学的相互影响。本药生物效应与两种成分单独运用时相当：空腹口服双氯芬酸钠在胃肠道吸收完全。单剂口服50mg后，达峰时间为1～2h，血药浓度峰值为1.5μg/ml。血浆蛋白结合率达90%以上，在肝、肾及血液中浓度高。进入关节滑膜液后，其清除速度比血浆中慢，呈现滑膜液药物浓度高于血浆浓度的现象。双氯芬酸钠的半衰期为1～2h，主要在肝内代谢，然后以葡萄糖醛酸或硫酸结合物的形式排出体外，其中2/3经肾，1/3经胆汁和粪便排出。未发现双氯芬酸钠的吸收、代谢或排泄过程与年龄有关。肾功能受损者，按常规剂量单次给药不会引起蓄积。双氯芬酸钠的药动学在肝功能受损者和非肝病患者之间无差异。米索前列醇口服能迅速吸收，经去脂化成为有活性的代谢物米索前列醇酸。该成分在血浆中易发现。达峰时间约为10min，与血浆蛋白结合率不足90%。口服米索前列醇的80%经尿排出，清除半衰期为30min。米索前列醇不影响动物肝脏的细胞色素P450酶系统。
适应证
本药为抗风湿药，可用于各种急、慢性关节炎、类风湿性关节炎、增生性骨关节病、强直性脊椎炎、软组织风湿病、各种急性疼痛等。由于本药含胃肠黏膜保护剂，故对以往有消化性溃疡伴或不伴出血、穿孔，有较严重慢性胃炎史，以往用非甾体类抗炎药后有胃肠不良反应的患者特别适用，可防止发生胃肠黏膜损伤。
禁忌证
1.对双氯芬酸钠和其他非甾体类抗炎药，或前列腺素过敏者。
2.活动性消化性溃疡和胃肠道出血者。
3.严重肾功能损害或肾功能进行性恶化者(肌酐清除率每分钟小于30ml)。
4.肝功明显受损者。
5.孕妇、哺乳妇女禁用。
注意事项
1.慎用：
(1)肝、肾或心脏病患者。
(2)正在接受锂剂治疗的患者。
(3)凝血功能障碍或血友病患者(因本药抗血小板效应可能使病情恶化)。
(4)脱水的患者：使用本药有增加肾毒性的危险。
(5)有高血压或其他易引起体液潴留疾病的患者。
2.用药前后应监测肝肾功能、血细胞及血电解质。
3.不要与其他非甾体类抗炎药同用。
4.不要咀嚼或咬碎药片。
不良反应
主要引起胃肠道不良反应，表现为腹痛、腹泻、恶心、消化不良、胃肠胀气、呕吐、胃炎、便秘、嗳气；也可引起头痛、头晕和皮疹等。尚可引起过敏反应、水肿、月经障碍、白带增多、痛经、绝经后阴道出血及肝功能异常等。
用法用量
口服给药：每次1片，每天2～3次。
药物相应作用
参见：双氯芬酸钠
专家点评
本药含双氯芬酸钠和米索前列醇，前者有抗炎、止痛和解热作用，后者对胃和十二指肠黏膜有保护作用。有研究表明，本药的疗效与双氯芬酸、吡罗昔康及萘普生相当，但对胃、十二指肠黏膜保护作用则优于这三种药物。
生产厂家：辉瑞制药 |
