性格和新陈代谢后可待因的单剂量和长期在一个贫穷和七metabolisers广泛。

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陈锆、索莫吉AA,雷诺兹G,博赫纳F

性格和新陈代谢后可待因的单剂量和长期在一个贫穷和七metabolisers广泛。

Br中国新药杂志。1991年4月,31 (4):381 - 90。

PubMed ID

2049245 (在PubMed

]

文摘

1。药物动力学、代谢和部分间隙吗啡,可待因norcodeine codeine-6-glucuronide后单(30毫克)和慢性(七剂量30毫克8 h)管理可待因研究八个学科(7广泛和一个右美沙芬代谢差)。可待因、codeine-6-glucuronide吗啡和norcodeine由高效液相色谱分析测定。2。单剂量后,时间达到最大等离子可待因浓度为0.97 + / - 0.31 h(意思是南达科他州+ / -)和codeine-6-glucuronide是1.28 + / - 0.49 h。codeine-6-glucuronide的等离子体AUC是15.8 + / - 4.5倍的可待因。可待因的AUC唾液是3.4 + / - 1.1倍,在等离子体。可待因的消除半衰期为3.2 + / - 0.3 h和codeine-6-glucuronide为3.2 + / - 0.9 h。3。可待因的肾清除率是183 + / - 59毫升最低为1和尿液pH值呈负相关(r = 0.81)。这些数据表明,可待因经过肾小球滤过,肾小管分泌和被动重吸收。codeine-6-glucuronide的肾清除率是55 + / - 21毫升最低为1,并没有与尿液博士其绑定到人血浆不到10%。 These data suggest that codeine-6-glucuronide undergoes filtration at the glomerulus and tubular reabsorption. This latter process is unlikely to be passive. 4. After chronic dosing, the pharmacokinetics of codeine and codeine-6-glucuronide were not significantly different from the single dose pharmacokinetics. 5. After the single dose, 86.1 +/- 11.4% of the dose was recovered in urine, of which 59.8 +/- 10.3% was codeine-6-glucuronide, 7.1 +/- 1.1% was total morphine, 6.9 +/- 2.1% was total norcodeine and 11.8 +/- 3.9% was unchanged codeine. These recoveries were not significantly different (P greater than 0.05) after chronic administration. 6. After the single dose, the partial clearance to morphine was 137 +/- 31 ml min-1 in the seven extensive metabolisers and 8 ml min-1 in the poor metaboliser; to norcodeine the values were 103 +/- 33 ml min-1 and 90 ml min-1; to codeine-6-glucuronide the values were 914 +/- 129 ml min-1 and 971 ml min-1; and intrinsic clearance was 1568 +/- 103 ml min-1 and 1450 ml min-1. These values were not significantly (P greater than 0.05) altered by chronic administration.(ABSTRACT TRUNCATED AT 400 WORDS)

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药物

可待因