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Biomedical subjects

D R Jasinski

Publications and source records attributed to D R Jasinski.

At least 37 records · Page 2Linked to original sources
PubMed1991

History of abuse liability testing in humans.

Clinical testing for drug abuse liability began as part of a collaborative effort to develop non-addicting substitutes for morphine. Physical dependence capacity and euphorigenic potential were identified as the potent effects of morphine leading to abuse; quantitative measures were developed for these effects. Drugs were evaluated for morphine-like effects using principles of bioassay. In recent years, the alterations in mood, feeling, thinking, and perception induced by drugs (subjective effects) are viewed as the effects leading to reinforcement of drug-taking behavior and to abuse. The same procedures and methods developed for assessing these effects with opioids have subsequently been applied to other classes of drugs. At present, human drug abuse liability testing methods exist for opioids, stimulants, sedative hypnotics, serotonin agonist and antagonists, nicotine, alcohol, and caffeine.

Drug Evaluation↗
PubMed1991

Intravenous methylphenidate abuse. Prototype for prescription drug abuse.

Data are presented from a case series of 22 patients who abused methylphenidate hydrochloride (Ritalin-SR). The abuse pattern and symptoms of toxicity were similar to that seen with cocaine hydrochloride and amphetamine sulfate addiction; yet, the morbidity and mortality seen in this case series were greater than usual for a group of patients involved in intravenous drug abuse. We describe the characteristics of the methylphenidate abuse syndrome in terms of the pharmacology of methylphenidate, the constituents of the Ritalin-SR preparation, and the disease of chemical dependence. We propose solutions to the problem of methylphenidate abuse.

Adult↗
PubMed1990

Learning disabilities in alcohol-dependent adults: a preliminary study.

To determine if neuropsychological deficits, known to precede alcohol use in those genetically predisposed to alcoholism, were present in an alcoholic population, 25 male alcoholics (mean age 41.1) were interviewed concerning alcohol usage, educational difficulties in elementary school, and family history of alcoholism. Using a regression table, discrepancies between current IQ on the Wechsler Adult Intelligence Scale-Revised (WAIS-R) (Wechsler, 1981) and achievement on the Woodcock-Johnson Psycho-Educational Battery (WJB) (Woodcock & Johnson, 1977) were calculated to determine present learning status. Forty percent of the alcoholics were found to have had special education, remedial services, or repeated grade failure concurrent with a familial history of alcoholism and current discrepancies indicative of learning disability. There were no significant differences on intelligence, years of drinking, or mean grades completed in school between this group and the rest of the subjects who did not receive services in school. Conclusions were that childhood learning disorders may be related to the development of alcoholism, particularly when alcoholism is in the family, and that special educators have a role to play in the prevention and treatment of alcoholism.

Adult↗
PubMed1989

Sublingual versus subcutaneous buprenorphine in opiate abusers.

To compare the pharmacologic profiles of sublingually and subcutaneously administered buprenorphine, 10 healthy male subjects with histories of opiate abuse were given sublingually administered buprenorphine (1, 2, and 4 mg), subcutaneously administered buprenorphine (1 and 2 mg), and placebo in a double-blind, double-dummy, placebo-controlled study. All active buprenorphine dosages produced a significant degree of miosis but no significant changes in body temperature, blood pressure, or respiratory or heart rate. Buprenorphine produced varying degrees of euphoria related to dose and route of administration but little dysphoria and sedation, as assessed by subscales of the Addiction Research Center Inventory. Subject "liking" for buprenorphine was reported by both observers and subjects. The relative potency of sublingually to subcutaneously administered buprenorphine was calculated for both physiologic and behavioral parameters and found to be approximately two thirds. The results indicated that both sublingual and subcutaneous buprenorphine have a similar profile of effects in opiate abusers.

Administration, Sublingual↗
PubMed1988

The psychopharmacologic and prolactin response after large doses of naloxone in man.

Large doses of naloxone (150-300 mg), placebo, and morphine (15-30 mg) were given intramuscularly to human volunteers and compared using measures of subjective feeling states, physiological measures and discriminative features. Plasma prolactin responses after naloxone 210 mg and placebo were compared. The subjective measures and discriminative features of naloxone revealed that the drug is subtly psychoactive but the stimulus is vague and cannot be identified clearly as an opioid agonist or antagonist in nondependent opioid-using volunteers. The physiologic and prolactin responses closely resembled opiate agonist activity. We conclude that naloxone in this dose range may act as an opiate agonist in man.

Adult↗
PubMed1988

Naloxone fails to alter local cerebral glucose utilization in the rat.

The autoradiographic, 2-deoxy-D-[1-14C]glucose ([14C]DG) method was used to map the effects of intravenous (IV) naloxone (1.0, 10.0, and 20.0 mg/kg) on local cerebral glucose utilization (LCGU), an index of local brain function. Naloxone injected 5 min before [14C]DG did not alter LCGU in any of the fifty-six brain regions examined. Our findings suggest that acute naloxone at these doses does not significantly affect cerebral metabolism.

Animals↗
PubMed1988

A clinical trial of buprenorphine: comparison with methadone in the detoxification of heroin addicts.

The efficacy of buprenorphine and methadone was compared in the outpatient detoxification of heroin addicts. Forty-five patients were randomized to receive either sublingual buprenorphine or oral methadone under double-dummy and double-blind conditions to study the pharmacology of buprenorphine in a 90-day detoxification protocol. The patients were administered either 2 mg buprenorphine or 30 mg methadone for 3 weeks followed by 4 weeks of dose reductions and 6 weeks of placebo medication. No significant between-group differences were seen on measures of treatment retention, drug use, or symptom report. During the hydromorphone challenge, methadone attenuated opioid effects to a greater extent than did buprenorphine on both physiologic (pupil constriction) and self-report measures. However, this did not result in greater abuse of illicit opioid drugs by subjects taking buprenorphine. The results of this clinical trial indicated that buprenorphine was acceptable to patients and as effective as methadone in the detoxification treatment of heroin addicts.

Adult↗
PubMed1988

Buprenorphine: dose-related blockade of opioid challenge effects in opioid dependent humans.

This study assessed the blockade of hydromorphone challenge effects (cumulative s.c. doses of 0, 6 and 18 mg) during chronic buprenorphine treatment of opioid dependent subjects. Buprenorphine was administered daily via the sublingual route in ascending doses of 2, 4, 8 and 16 mg. Hydromorphone challenges were conducted after 10 to 14 days of chronic administration of each buprenorphine dose and 24 h after the last buprenorphrine dose. Buprenorphrine itself only produced dose-related effects in respiration rate. While subjects were maintained on 2 mg of buprenorphine, the hydromorphone challenge produced dose-related changes in physiological and self-report measures. As the dose of buprenorphine was increased, hydromorphone effects on self-report measures were attenuated to a greater extent than was noted for pupil diameter. The results of this study confirm previous reports of buprenorphine blockade of opioid agonist effects in humans and extent those findings by demonstrating both a buprenorphine dose-effect function and a dissociation between the potency of buprenorphine's opioid blockade for self-report vs. physiological measures.

Adult↗
PubMed1987

Differential effects of mu and kappa opioid analgesics on cerebral glucose utilization in the rat.

The autoradiographic 2-deoxy-D-[1-(-14)C]glucose ([14C]2-DG) method was used to map the effects of subcutaneous (s.c.) morphine (8.0 mg/kg), oxymorphone (0.4 mg/kg) and nalbuphine (16.0 mg/kg) on local cerebral glucose utilization (LCGU), an index of local brain function. At the dosages administered, effects of the opioid agonists on LCGU were very restricted. The mu agonists, injected 15 min before [14C]2-DG, decreased LCGU in thalamic nuclei, including some of those which have been implicated in somatosensory processing, and in the dorsal tegmental nucleus. Nalbuphine did not produce these effects, but stimulated LCGU in nuclei of the spinal tract of the trigeminal nerve and in the globus pallidus. All of the effects on LCGU were blocked by prior administration of naloxone (1.0 or 10.0 mg/kg, s.c., 5 min before morphine or nalbuphine, respectively). Our findings suggest that different supraspinal mechanisms are involved in the actions of mu vs kappa opioids, and indicate that the [14C]2-DG procedure might be helpful in elucidating the anatomical areas involved.

Animals↗
PubMed1987

A comparative assay of nefopam, morphine and d-amphetamine.

Nefopam is a non-opioid analgesic reported to have some stimulant properties. The subjective, behavioral and physiological effects of nefopam, morphine and d-amphetamine were compared in seven non-dependent substance abusers to assess the abuse potential of nefopam. Morphine and d-amphetamine had significant effects on a number of measures generally consistent with the effects of drugs of the opioid and psychomotor stimulant drug classes. Subjects correctly discriminated between morphine and d-amphetamine. Nefopam was most frequently identified by subjects as being amphetamine-like, though several measures indicated that nefopam produced some sedation. Little or no "liking" of the effects of nefopam was reported by subjects. Overall, nefopam was one fifth as potent as morphine and one quarter as potent as d-amphetamine in producing subjective and physiological effects. The results indicate that nefopam is neither entirely morphine-like nor d-amphetamine-like. In our opinion, nefopam has a lesser potential to be abused than morphine or d-amphetamine.

Behavior↗
PubMed1987

Human pharmacology and abuse potential of meptazinol.

Meptazinol was assessed in nine opioid abusers according to a double-blind, randomized, crossover design to determine if it produced typical morphine effects. A comparison of physiologic and subjective effects was made between morphine, 7.5, 15, and 30 mg, meptazinol, 70, 140, and 280 mg, and placebo. Both drugs constricted pupils. Meptazinol, 140 and 280 mg, decreased body temperature. Valid relative potency estimates of morphine to meptazinol were obtained for self-reported liking, opiate symptoms, and pupillary constriction. Meptazinol did not increase euphoria or sedation scale scores but did increase dysphoria scale scores. In the therapeutic dose range, meptazinol produced miosis, morphine-like identification and symptoms, limited liking, and some dysphoria. Dysphoria predominated at the 280 mg dose of meptazinol. From these data, it is concluded that meptazinol is not a typical morphine-like drug and has limited abuse potential.

Adult↗