Naranjo C A, Poulos C X, Lanctôt K L, Bremner K E, Kwok M, Umana M
Psychopharmacology Research Program, Sunnybrook Health Science Centre, University of Toronto, Ontario, Canada.
Addiction. 1995 Jul;90(7):893-905. doi: 10.1046/j.1360-0443.1995.9078933.x.
Ritanserin, a 5-HT2 receptor antagonist, decreased alcohol intake in some, but not all, animal studies and in an open clinical study. We tested the short-term effects of ritanserin in 39 (35 male, four female) heavy social drinkers (consuming at least 28 drinks/week), aged 19-63 years, who were not seeking treatment. After an intake assessment, they received placebo for 7 days in a single-blind baseline. They were then randomly assigned to one of three double-blind treatments for 14 days: ritanserin 5 mg/day (n = 12), ritanserin 10 mg/day (n = 13) or placebo (n = 14). Subjects recorded daily outpatient alcohol intake. Feelings of intoxication and interest, desire, craving and liking for alcohol were rated retrospectively at each weekly study visit. Experimental drinking sessions were conducted after baseline (EDS1) and treatment (EDS2); in each session subjects were offered 18 mini-drinks (total = six standard) and rated their desire to drink, intoxication and mood (POMS). Outpatient results: ritanserin 5 mg/day decreased desire and craving for alcohol (vs. baseline, p < 0.05) but not alcohol intake. Liking of alcohol decreased from baseline with ritanserin 10 mg/day (p = 0.01) and placebo (p = 0.05). Changes in alcohol intake from baseline with ritanserin 10 mg/day (increase, p > 0.05) and placebo (decrease, p > 0.05) were different (p < 0.05). EDS results: in EDS2, desire ratings for the first three mini-drinks were lower after ritanserin 5 mg/day than after ritanserin 10 mg/day (p < 0.05), but the decreases were not statistically significant when EDS1 desire ratings were controlled for. Ritanserin 10 mg/day increased alcohol-induced feelings of intoxication and friendliness, compared with placebo (p < 0.05). Both ritanserin 5 mg/day and 10 mg/day enhanced alcohol-induced decreases in fatigue, compared with placebo (p < 0.05). These results indicate that ritanserin may have differential effects on alcohol intake, desire, craving and liking, intoxication and some of alcohol's effects on mood. However, they suggest that ritanserin has limited efficacy in reducing alcohol intake in heavy drinkers.
利坦色林是一种5-羟色胺2（5-HT2）受体拮抗剂，在部分（而非全部）动物研究及一项开放性临床研究中可减少酒精摄入量。我们对39名（35名男性，4名女性）年龄在19至63岁之间、未寻求治疗的重度社交饮酒者（每周至少饮用28杯酒）进行了利坦色林短期效果测试。在进行摄入量评估后，他们在单盲基线期接受了7天的安慰剂治疗。随后，他们被随机分配至三种双盲治疗方案之一，为期14天：利坦色林5毫克/天（n = 12）、利坦色林10毫克/天（n = 13）或安慰剂（n = 14）。受试者记录每日门诊酒精摄入量。在每周的研究访视时，回顾性评估醉酒感以及对酒精的兴趣、欲望、渴望和喜好程度。在基线期（EDS1）和治疗后（EDS2）进行实验性饮酒环节；在每个环节中，为受试者提供18小杯酒（总计六标准杯），并让他们对饮酒欲望、醉酒感和情绪（POMS）进行评分。门诊结果：利坦色林5毫克/天可降低对酒精的欲望和渴望（与基线相比，p < 0.05），但并未减少酒精摄入量。利坦色林10毫克/天和安慰剂组中，对酒精的喜好程度均较基线期有所下降（分别为p = 0.01和p = 0.05）。利坦色林10毫克/天组与安慰剂组相比，酒精摄入量相对于基线期的变化情况不同（利坦色林组增加，p > 0.05；安慰剂组减少，p > 0.05）（p < 0.05）。实验性饮酒环节结果：在EDS2中，利坦色林5毫克/天组在前三杯小酒的欲望评分低于利坦色林10毫克/天组（p < 0.05），但在控制了EDS1欲望评分后，这种下降无统计学意义。与安慰剂相比，利坦色林10毫克/天组增强了酒精引起的醉酒感和友好感（p < 0.05）。与安慰剂相比，利坦色林5毫克/天和10毫克/天组均增强了酒精引起的疲劳感下降（p < 0.05）。这些结果表明，利坦色林可能对酒精摄入量、欲望、渴望和喜好、醉酒感以及酒精对情绪的某些影响具有不同作用。然而，研究结果表明利坦色林在减少重度饮酒者酒精摄入量方面的疗效有限。
