1 The effects of concurrent administration of cotrimoxazole on the plasma concentration-time profiles of loperamide and its oxide were investigated in two separate studies in healthy male volunteers. Cotrimoxazole (960 mg, twice daily) was administered for 24 h before and 48 h after an oral dose of loperamide oxide (4 mg) or loperamide (4 mg). 2 Coadministration of cotrimoxazole with loperamide oxide did not alter the t max' C max and AUC of loperamide oxide, whereas the C max (0.32 ± 0.14 ng ml -1 without cotrimoxazole; 0.45 ± 0.18 ng ml -1 with cotrimoxazole; P -1 h without cotrimoxazole; 12.50 ± 4.60 ng ml -1 h with cotrimoxazole; P 3 Coadministration of cotrimoxazole with loperamide significantly increased the C max (0.74 ± 0.22 ng ml -1 without cotrimoxazole; 1.49 ± 0.81 ng ml -1 with cotrimoxazole; P -1 h without cotrimoxazole; 25.30 ± 11.10 ng ml -1 h with cotrimoxazole; P max and t 1/2, z were not significantly altered. 4 The increase in loperamide AUC, following coadministration of either loperamide oxide or loperamide with cotrimoxazole, may be due to reduced first pass metabolism of loperamide.
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机译：1 在两项针对健康男性志愿者的独立研究中，研究了同时给予复方新诺明对洛哌丁胺及其氧化物血浆浓度-时间曲线的影响。复方新诺明（960mg，每日两次）在口服洛哌丁胺氧化物（4mg）或洛哌丁胺（4mg）之前和之后48小时施用。2 复方新诺明与氧化洛哌丁胺联合给药不会改变氧化洛哌丁胺的 t max' C max 和 AUC，而 C max（0.32 ± 0.14 ng ml -1 不含复方新诺明;0.45 ± 0.18 ng ml -1 与复方新诺明;P -1 h，不含复方新诺明;12.50±4.60ng ml-1小时与复方新诺明;P 3复方新诺明与洛哌丁胺联合给药显著增加C max（0.74±0.22ng ml-1，不复方新诺明;1.49±0.81ngml-1与复方新诺明;P -1 h，不含复方新诺明;25.30±11.10ng ml-1小时与复方新诺明;P max和t 1/2，z无显著变化。4 洛哌丁胺氧化物或洛哌丁胺与复方新诺明合用后，洛哌丁胺AUC的增加可能是由于洛哌丁胺的首过代谢降低。
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