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Biomedical subjects

D R Jasinski

Publications and source records attributed to D R Jasinski.

At least 73 records · Page 4Linked to original sources

Human pharmacology of narcotic antagonists.

1 Human studies at the Addiction Research Center enable narcotic antagonists to be classified into three subgroups: (1) nalorphine-like agents; (2) pure antagonists; and (3) morphine-like agents. 2 Six narcotic antagonists (pentazocine, nalbuphine, cyclazocine, butorphanol, propiram and buprenorphine) developed in recent years seem to have a lesser abuse potential than codeine or propoxyphene. 3 When adjusted for relative availability of the agents, epidemiological data shows that pentazocine is abused less than codeine or propoxyphene in the US. 4 Recent studies with buprenorphine indicate that this agent would find application both as an analgesic of low abuse potential and as a new type of drug for the treatment of addiction.

Humans↗

Human pharmacology and abuse potential of the analgesic buprenorphine: a potential agent for treating narcotic addiction.

Buprenorphine was evaluated for its abuse potential and utility in treating narcotic addiction. The drug was morphine-like but was 25 to 50 times more potent than morphine and was longer-acting. Little if any physical dependence of clinical significance was produced by buprenorphine. The effects of morphine to 120-mg doses were blocked by buprenorphine, a blockade that persisted for 29 1/2 hours. In man, buprenorphine has less intrinsic activity than morphine, and as such, as a low abuse potential. Moreover, the drug has potential for treating narcotic addiction since it is acceptable to addicts, is long-acting, produces a low level of physical dependence such that patients may be easily detoxified, is less toxic than drugs used for maintenance therapy, and blocks the effects of narcotics.

Adult↗

Abrupt withdrawal from therapeutically administered diazepam. Report of a case.

Subjective, behavioral, and physiologic changes followed abrupt withdrawal of diazepam (Valium) in a patient who had been treated with 30 to 45 mg of diazepam daily for 20 months. Precipitous weight loss and orthostatic pulse rate increase were a part of the abstinence syndrome, which occurred between the fifth and ninth days of withdrawal. Accompanying these changes in physiologic measures were discomforting symptoms and dysphoria that were aversive and reinforcing to drug taking since the patient sought diazepam administration. These observations suggest that changes in mood, feeling states, and behavior may be the most prominent characteristics of the abstinence syndrome associated with physical dependence on this dose level of diazepam.

Adult↗

Lithium: effects on subjective functioning and morphine-induced euphoria.

The therapeutic usefulness of lithium in decreasing the euphoria and other symptoms associated with manic behavior and the hypothesis of a common final mechanism for elevations in mood have led to speculation that lithium may block the euphoria induced by drugs of abuse. In this study, lithium alone was antieuphoric in drug-free opiate addicts and, further, did not block morphine-induced euphoria.

Clinical Trials as Topic↗

Therapeutic usefulness of propoxyphene napsylate in narcotic addiction.

The maximum doses of propoxyphene napsylate used to treat heroin addicts produce a degree of morphine-like activity equal to that produced by 20 to 25 mg/day of subcutaneously given morphine or 10 mg/day orally given methadone. This degree of activity wound be sufficient to ameliorate abstinence even in patients dependent on large doses of narcotics--an observation that supports the utility of propoxyphene napsylate in detoxification. On the other hand, only patients taking 10 mg/day or less of parenterally administered heroin could be maintained on maximum subtoxic levels of propoxyphene napsylate without abstinence signs or symptoms suggesting that propoxyphene napsylate would be less useful in maintenance therapy.

Administration, Oral↗

Azidomorphine: subjective effects and suppression of morphine abstinence.

In man, azidomorphine, a new morphine congener, constricted pupils, produced morphine-like subjective effects and euphoria, and suppressed the morphine abstinence syndrome. Azidomorphine was 10 to 50 times as potent as morphine. It is concluded that in man azidomorphine is a typical morphine-like drug.

Azides↗

Etorphine in man. I. Subjective effects and suppression of morphine abstinence.

The effects of etorphine, a potent morphine-like drug, were qualitatively and quantitatively compared to those of morphine. In nondependent subjects, etorphine in doses of 0.025, 0.050, and 0.100 mg produced pupillary constriction and morphine-like subjective effects and euphoria. Etorphine was 500 times as potent as morphine, with a very rapid onset and short duration of action. In morphine-dependent subjects, etorphine suppressed abstinence but for a shorter period than morphine. These studies indicate that in man etorphine is a morphine-like drug with a high abuse potential.

Clinical Trials as Topic↗

A comparison of fenfluramine and amphetamine in man.

dl-Fenfluramine hydrochloride (60, 120, 240 mg), d-amphetamine sulfate (20, 40 mg), and placebo were compared in 8 postaddict volunteers, each dose given orally in random sequence at weekly intervals using a double-blind crossover design. Fenfluramine had little effect on blood pressure and temperature, but caused a marked dilation of pupils, whereas amphetamine was a potent vasopressor and a weak mydriatic. While fenfluramine produced euphoria in some subjects, its overall effects were unpleasant, sedative, and qualitatively different from amphetamine. Three subjects given 240 mg of fenfluramine experienced brief but vivid hallucinogenic episodes characterized by olfactory, visual, and somatic hallucinations, abrupt polar changes in mood, time distortion, fleeting paranoia, and sexual ideation. These observations indicate that fenfluramine is a hallucinogenic agent with a pharmacologic profile in man that is not amphetamine-like.

Adult↗