药物动力学的oxicam非甾体类抗炎药物。
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Olkkola KT,布鲁内托AV,马提拉乔丹
药物动力学的oxicam非甾体类抗炎药物。
Pharmacokinet。1994年2月,26 (2):107 - 20。
- PubMed ID
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8162655 (在PubMed]
- 文摘
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Oxicam非甾体类抗炎药(非甾体抗炎药)是一组结构密切相关的物质与抗炎、止痛和退热的活动。他们有一个弱酸性的性格和广泛被血浆蛋白。使用最广泛的oxicam吡罗昔康,口服后吸收良好。药物的血浆浓度峰值(Cmax)在2到4小时内到达。吡罗昔康的小体积分布和低血浆清除率。它经历了肝代谢和只有5 - 10%是尿液排泄不变。消除半衰期不同30至70小时。病人的年龄和肾或肝功能障碍似乎没有任何重大影响吡罗昔康的药物动力学。肾排泄的药物可以减少锂临床上重要的程度,但piroxicam-aspirin的临床意义(乙酰水杨酸)和piroxicam-acenocoumarol交互尚未建立。Ampiroxicam, droxicam pivoxicam高活性化合物合成的吡罗昔康减少piroxicam-related胃肠刺激。 All prodrugs are well absorbed, but Cmax values are reached later than those following administration of piroxicam. Tenoxicam is used in the management of rheumatic and inflammatory diseases. Mean Cmax values are achieved 2 hours postdose. Food reduces the rate but not the extent of absorption. The oral bioavailability of tenoxicam is 100% and rectal bioavailability is 80%. Like piroxicam, tenoxicam has a low volume of distribution and low plasma clearance. It is eliminated through hepatic metabolism. The mean elimination half-life is 60 to 75 hours. The pharmacokinetics of tenoxicam are independent of patient age, or concurrent liver or renal diseases. High doses of aspirin have been shown to increase the elimination of tenoxicam, but this has little clinical significance. Isoxicam was in widespread clinical use until its worldwide marketing was suspended because of fatal skin reactions. Isoxicam is completely absorbed, but Cmax values are not reached until 10 hours postdose. It has a low plasma clearance, approximately 5 ml/min (0.3 L/h), and low volume of distribution. The mean elimination half-life is 30 hours and does not appear to be affected by the age of the patient. Isoxicam potentiated the anticoagulant effect of warfarin, necessitating a 20% dosage reduction. Lornoxicam differs from other oxicam NSAIDs because it has a short elimination half-life of 3 to 4 hours. On the basis of limited data, some individuals seem to eliminate lornoxicam very slowly, suggesting the presence of polymorphic metabolism. The pharmacokinetics of cinnoxicam and sudoxicam have not been studied thoroughly.(ABSTRACT TRUNCATED AT 400 WORDS)
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