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Mecamylamine modifies the pharmacokinetics and reinforcing effects of alcohol.
Alcohol Clin Exp Res. 2002 Mar; 26(3):326-31.AC

Abstract

BACKGROUND

Central nicotinic cholinergic receptors modify alcohol-induced mesolimbic dopamine activation, which seems to be important in the reinforcing properties of alcohol. Consistent with this model, acute administration to rats of the tertiary nicotinic receptor antagonist mecamylamine blocks both alcohol consumption and alcohol-induced dopamine release in the nucleus accumbens. This study was conducted to test the hypothesis that, during the ascending limb of the blood alcohol concentration curve, mecamylamine would reduce the stimulating and pleasurable effects of an intoxicating dose of alcohol in humans.

METHODS

Ten female and 10 male volunteers with no history of alcohol or substance use disorders, including nicotine dependence, completed the study. During two laboratory sessions, subjects consumed three aliquots of an alcohol-containing drink, with a total ethanol content of 0.7 g/kg (in women) or 0.8 g/kg (in men), over a 30-min period. Two hours before the first drink, subjects were pretreated with mecamylamine or placebo, with the order of sessions counterbalanced. Primary outcome measures included the Drug Effect Questionnaire, the central stimulation subscale of the Alcohol Sensation Scale, and the stimulant subscale of the Biphasic Alcohol Effects Scale. Breath alcohol level (BAL) was examined to identify the ascending and descending limbs of the blood alcohol curve and to assess pharmacokinetic interactions between alcohol and mecamylamine.

RESULTS

Significant effects of time, study drug, and their interaction were observed. Compared with placebo, mecamylamine reduced BAL. After controlling for BAL at each time point, mecamylamine also reduced the Drug Effect Questionnaire and Alcohol Sensation Scale stimulant subscale scores, with a trend for a similar effect on the Biphasic Alcohol Effects Scale score.

CONCLUSIONS

Mecamylamine seems to modify both the pharmacokinetic profile of alcohol and the rewarding effects of alcohol in healthy volunteers.

Authors+Show Affiliations

Alcohol Research Center, Department of Psychiatry, University of Connecticut School of Medicine, 263 Farmington Avenue, Farmington, CT 06030-2103, USA.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't
Research Support, U.S. Gov't, P.H.S.

Language

eng

PubMed ID

11923584

Citation

Blomqvist, Ola, et al. "Mecamylamine Modifies the Pharmacokinetics and Reinforcing Effects of Alcohol." Alcoholism, Clinical and Experimental Research, vol. 26, no. 3, 2002, pp. 326-31.
Blomqvist O, Hernandez-Avila CA, Van Kirk J, et al. Mecamylamine modifies the pharmacokinetics and reinforcing effects of alcohol. Alcohol Clin Exp Res. 2002;26(3):326-31.
Blomqvist, O., Hernandez-Avila, C. A., Van Kirk, J., Rose, J. E., & Kranzler, H. R. (2002). Mecamylamine modifies the pharmacokinetics and reinforcing effects of alcohol. Alcoholism, Clinical and Experimental Research, 26(3), 326-31.
Blomqvist O, et al. Mecamylamine Modifies the Pharmacokinetics and Reinforcing Effects of Alcohol. Alcohol Clin Exp Res. 2002;26(3):326-31. PubMed PMID: 11923584.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Mecamylamine modifies the pharmacokinetics and reinforcing effects of alcohol. AU - Blomqvist,Ola, AU - Hernandez-Avila,Carlos A, AU - Van Kirk,Jeffrey, AU - Rose,Jed E, AU - Kranzler,Henry R, PY - 2002/3/30/pubmed PY - 2002/7/26/medline PY - 2002/3/30/entrez SP - 326 EP - 31 JF - Alcoholism, clinical and experimental research JO - Alcohol Clin Exp Res VL - 26 IS - 3 N2 - BACKGROUND: Central nicotinic cholinergic receptors modify alcohol-induced mesolimbic dopamine activation, which seems to be important in the reinforcing properties of alcohol. Consistent with this model, acute administration to rats of the tertiary nicotinic receptor antagonist mecamylamine blocks both alcohol consumption and alcohol-induced dopamine release in the nucleus accumbens. This study was conducted to test the hypothesis that, during the ascending limb of the blood alcohol concentration curve, mecamylamine would reduce the stimulating and pleasurable effects of an intoxicating dose of alcohol in humans. METHODS: Ten female and 10 male volunteers with no history of alcohol or substance use disorders, including nicotine dependence, completed the study. During two laboratory sessions, subjects consumed three aliquots of an alcohol-containing drink, with a total ethanol content of 0.7 g/kg (in women) or 0.8 g/kg (in men), over a 30-min period. Two hours before the first drink, subjects were pretreated with mecamylamine or placebo, with the order of sessions counterbalanced. Primary outcome measures included the Drug Effect Questionnaire, the central stimulation subscale of the Alcohol Sensation Scale, and the stimulant subscale of the Biphasic Alcohol Effects Scale. Breath alcohol level (BAL) was examined to identify the ascending and descending limbs of the blood alcohol curve and to assess pharmacokinetic interactions between alcohol and mecamylamine. RESULTS: Significant effects of time, study drug, and their interaction were observed. Compared with placebo, mecamylamine reduced BAL. After controlling for BAL at each time point, mecamylamine also reduced the Drug Effect Questionnaire and Alcohol Sensation Scale stimulant subscale scores, with a trend for a similar effect on the Biphasic Alcohol Effects Scale score. CONCLUSIONS: Mecamylamine seems to modify both the pharmacokinetic profile of alcohol and the rewarding effects of alcohol in healthy volunteers. SN - 0145-6008 UR - https://www.unboundmedicine.com/medline/citation/11923584/Mecamylamine_modifies_the_pharmacokinetics_and_reinforcing_effects_of_alcohol_ L2 - http://ovidsp.ovid.com/ovidweb.cgi?T=JS&PAGE=linkout&SEARCH=11923584.ui DB - PRIME DP - Unbound Medicine ER -