Effect of histamine-2 receptor antagonists on blood alcohol levels

Abstract

OBJECTIVE:To determine the effect, if any, of histamine type 2 receptor antagonists (H 2 RAs) on serum alcohol levels under various conditions including type of H 2 RA receptor antagonist, alcohol dose, and fed status of the subject. STUDY DESIGN:Meta-analysis of the published literature.DATA SOURCES: Studies were identified by MEDLINE (January 1982 through December 1997) using the key words H 2 receptor antagonists and alcohol. Other studies were identified by reviewing bibliographies of retrieved articles and by discussion with colleagues. STUDY SELECTION:Studies were selected if they involved the coadministration of H 2 RAs and alcohol in healthy, human volunteers. Studies that may have addressed this goal but were performed in another context, for instance the measurement of ulcer healing, were excluded. DATA EXTRACTION:Data were extracted on the design, number of participants, participant characteristics, type and dose of H 2 RA administered, serum alcohol levels (measured as C max ) along with standard deviations, dose of alcohol received, and fed or fasted status of participants. Alcohol dose was arbitrarily divided into low dose ( Յ 0.5 g/kg body weight) versus high dose ( Ͼ 0.5 g/kg body weight). In addition, studies involving ranitidine and cimetidine were stratified by sample size into small ( n Յ 10) versus not small ( n Ͼ 10). MEASUREMENTS AND MAIN RESULTS:

Alcohol, microbiome, life style influence alcohol and non-alcoholic organ damage

“…Central nervous system agents were the most common medications (59.1% mainly opioids and psychotherapeutic agents, including antidepressants; Neuman et al, 2006). There is a potential interaction between alcohol and H2 receptor antagonists such as cimetidine (Weinberg et al, 1998). The inhibition of the metabolism of acetaldehyde may cause disulfiram-like reactions.…”

Alcoholic Liver Disease: A Synopsis of the Charles Lieber's Memorial Symposia 2009-2012

“…Cimetidine and ranitidine, which are H 2 RA, can increase the peak levels of alcohol and the area under the alcohol concentration curve (DiPadova et al, 1992). It was subsequently determined that the resulting elevations in blood alcohol levels were unlikely to exceed legal limits or be clinically relevant in individuals with adequate nutrition and with moderate social alcohol consumption (Raufman et al, 1993;Weinberg et al, 1998). A recent in vitro study and computer simulation confirmed that cimetidine can act either as a competitive or a non-competitive inhibitor, depending on the class of ADH isozyme.…”

Commentary

“…9 In addition, alcohol can affect the pharmacokinetics of drugs by delaying gastric emptying time and inducing enzyme cytochrome p450 CY2E1 in the liver. For example, it is well known that some antibiotics such as metronidazole, cephamandole, cefoperazone, griseofulvin, and procarbazine can cause disulfiram-like reactions by inhibiting metabolism of acetaldehyde.…”

“…8 H 2 receptor antagonists such as ranitidine inhibit gastric ADH (alcohol dehydrogenase), and it is possible that coadministration of alcohol and H 2 receptor antagonists may cause unexpectedly high blood alcohol concentrations. 9 In addition, alcohol can affect the pharmacokinetics of drugs by delaying gastric emptying time and inducing enzyme cytochrome p450 CY2E1 in the liver. 8 Inducing cytochrome p450 CY2E1 affects var-ious compounds such as acetaminophen, which can be metabolized to toxic compounds and cause liver toxicity.…”