Abstract
This study addressed the assumption that rate of onset affects the euphorigenic effects of drugs. Drugs with rapid onset are commonly thought to be more euphorigenic than drugs with slower onset, but this idea has rarely been studied directly. Nine healthy male social drinkers, with no history of drug- or alcohol-related problems, participated in three sessions. On each session they received oral doses of placebo (PLAC), diazepam in a rapid onset condition (FAST), or diazepam in a slow onset condition (SLOW). In the FAST condition, they received a single 20 mg dose, whereas in the SLOW condition they received six 4 mg doses administered at 30-min intervals. Plasma levels of diazepam and desmethyldiazepam, subjective effects (including measures of euphoria), psychomotor performance and vital signs were monitored throughout each session. Although the FAST and SLOW conditions led to similar peak plasma levels of drug, the peak was attained earlier in the FAST condition (61 min versus 220 min). Subjects' scores on a measure of euphoria (MBG scale of the ARCI) were significantly higher in the FAST condition compared to the SLOW and PLAC conditions. Subjects exhibited significantly more behavioral signs of intoxication and greater psychomotor impairment in the FAST condition. Sedative effects of the drug were similar in magnitude, but the effects lasted slightly longer in the FAST condition. On several measures diazepam produced similar effects in the two conditions (e.g., ratings of strength of drug effect). These data provide limited support for the notion that a faster rate of onset of drug effects is associated with greater euphoria.
MeSH Terms
Adult
Affect/drug effects
Alcohol Drinking/psychology
Behavior/drug effects
Breath Tests
Cognition/drug effects
Diazepam/blood,pharmacokinetics,pharmacology
Double-Blind Method
Euphoria/drug effects
Humans
Male
Nordazepam/blood
Psychomotor Performance/drug effects
Sleep/drug effects
Chemicals
Nordazepam
Diazepam
Authors & Affiliations
3 authors, click to expand affiliations / ORCID
de Wit H
Department of Psychiatry, University of Chicago, IL 60637.
Dudish S
Ambre J
References (27)
27 references, click to expand
-
Brain uptake of benzodiazepines: effects of lipophilicity and plasma protein binding.
J Pharmacol Exp Ther. 1988 Jun;245(3):816-22
PMID: 3385643
-
Drug preference in humans: double-blind choice comparison of pentobarbital, diazepam and placebo.
J Pharmacol Exp Ther. 1980 Dec;215(3):649-61
PMID: 7441524
-
Pharmacodynamics of benzodiazepines after single oral doses: kinetic and physiochemical correlates.
Psychopharmacology Suppl. 1984;1:92-7
PMID: 6147845
-
Benzodiazepine concentrations in brain directly reflect receptor occupancy: studies of diazepam, lorazepam, and oxazepam.
Psychopharmacology (Berl). 1990;102(3):373-8
PMID: 1979181
-
Entry of diazepam and its major matabolite into cerebrospinal fluid.
Psychopharmacology (Berl). 1980;70(1):89-93
PMID: 6775342
-
Drug preference and mood in humans: diazepam.
Psychopharmacology (Berl). 1980;71(3):269-73
PMID: 6779334
-
Relative abuse liability of lorazepam and diazepam: an evaluation in 'recreational' drug users.
Drug Alcohol Depend. 1988 Dec;22(3):215-22
PMID: 3234245
-
Benzodiazepines and human memory: a review.
Anesthesiology. 1990 May;72(5):926-38
PMID: 1971164
-
Importance of genetic factors in the regulation of diazepam metabolism: relationship to S-mephenytoin, but not debrisoquin, hydroxylation phenotype.
Clin Pharmacol Ther. 1989 Apr;45(4):348-55
PMID: 2495208
-
Absorption rate, blood concentrations, and early response to oral chlordiazepoxide.
Am J Psychiatry. 1977 May;134(5):559-62
PMID: 848586
-
Reinforcing and subjective effects of diazepam in nondrug-abusing volunteers.
Pharmacol Biochem Behav. 1989 May;33(1):205-13
PMID: 2780778
-
A methodological comparison of two formulations of temazepam in pharmacokinetic and pharmacodynamic aspects.
Pharmacol Toxicol. 1989 Jan;64(1):28-32
PMID: 2569191
-
Six weeks of diazepam treatment in normal women: effects on psychomotor performance and psychophysiology.
J Clin Psychopharmacol. 1988 Apr;8(2):83-99
PMID: 3372718
-
Pharmacokinetic determinants of drug abuse and dependence. A conceptual perspective.
Clin Pharmacokinet. 1986 Mar-Apr;11(2):144-53
PMID: 3514044
-
A large-sample study of diazepam pharmacokinetics.
Ther Drug Monit. 1989 Nov;11(6):652-7
PMID: 2512694
-
Relative abuse liability of different benzodiazepines in drug abusers.
J Clin Psychopharmacol. 1990 Aug;10(4):237-43
PMID: 1981067
-
Testing the abuse liability of anxiolytic and hypnotic drugs in humans.
Drug Alcohol Depend. 1991 Jun;28(1):83-111
PMID: 1679388
-
Pharmacokinetic profile of diazepam in man following single intravenous and oral and chronic oral administrations.
J Pharm Sci. 1973 Nov;62(11):1789-96
PMID: 4758075
-
Rate of increase of plasma drug level influences subjective response in humans.
Psychopharmacology (Berl). 1992;107(2-3):352-8
PMID: 1615136
-
Pharmacokinetic considerations in abuse liability evaluation.
Br J Addict. 1991 Dec;86(12):1601-6
PMID: 1786493
-
Effects of different rates of absorption of two benzodiazepins on subjective and objective parameters. Significance for clinical use and risk of abuse.
Eur J Clin Pharmacol. 1974;7(3):201-11
PMID: 4851741
-
A comparison of the soft gelatin capsule and the tablet form of temazepam.
Acta Pharmacol Toxicol (Copenh). 1986 Jan;58(1):49-54
PMID: 2869638
-
Acute and subacute effects of diazepam on human performance: comparison of plain tablet and controlled release capsule.
Pharmacol Toxicol. 1988 Nov;63(5):369-74
PMID: 3070520
-
Comparison of diazepam and oxazepam: preference, liking and extent of abuse.
J Pharmacol Exp Ther. 1984 May;229(2):501-8
PMID: 6716272
-
Physiologic, subjective, and behavioral effects of amphetamine, methamphetamine, ephedrine, phenmetrazine, and methylphenidate in man.
Clin Pharmacol Ther. 1971 Mar-Apr;12(2):245-58
PMID: 5554941
-
The Leeds Sleep Evaluation Questionnaire in psychopharmacological investigations - a review.
Psychopharmacology (Berl). 1980;71(2):173-9
PMID: 6777817
-
Diazepam preference in males with and without an alcoholic first-degree relative.
Alcohol Clin Exp Res. 1991 Aug;15(4):593-600
PMID: 1928632