Apomorphine administered in reserpine-induced as well as in restraint ulcers in rats, failed to afford protection. Pimozide, moperone, trifluperidol and chlorpromazine fail to influence the development of the experimental ulcers. Pimozide and moperone although antagonizing the behavioral changes of amphetamine, maintained its antiulcer activity. Amitryptiline, cocaine and morphine had a protective activity. L-Dopa afforded a significant protection which was abolished if this compound was administered together with FLA-63, a specific dopamine-β-hydroxilase inhibitor. These results were explained by admitting that not dopamine, but noradrenaline was responsible for the antiulcer activity. α-Methyl-dopa produced a significant protection in both experimental models.
Background: Opioid use disorder continues to have a significant impact on public health morbidity and mortality throughout the United States and elsewhere. Managing opioid withdrawal is a critical treatment goal in individuals entering treatment with an active opioid use.Study Question: What are the milestones of the changes in the expert approach to the pharmacological management of heroin withdrawal syndrome in the past century?Study Design: To determine the changes in the expert approach to the management of heroin withdrawal syndrome, as presented in a widely used textbook in the United States.Data Sources: The chapters on opioid dependence in the 26 editions of Cecil Textbook of Medicine published from 1927 through 2020.Results: Opioid replacement taper with morphine (1927-1947), codeine (1931-1943), and methadone (1951-present) administered for 3-10 days has remained the main intervention. The anticholinergic drugs, scopolamine and atropine, were recommended from 1927 to 1943, but their use has never been backed by scientific evidence. Newer approaches relied on clonidine, an alpha-2 receptor agonist used since 1982, and buprenorphine, an opioid agonist/antagonist endorsed for the treatment of heroin withdrawal in 2000.
Conclusions:The pharmacological management of heroin withdrawal syndrome in the past century has progressed from the introduction of methadone to the utilization of clonidine and buprenorphine. More recent advances in treating opioid use disorder have changed the goals of opioid withdrawal management to achievement of abstinence from all opioids to facilitation of long-term treatment with medications for opioid use disorder.
In reserpine-induced ulcers in rats, the centrally acting sympathomimetic amines (amphetamine, mephentermine and ephedrine) produced a significant protection. Only amphetamine had a beneficial effect in restraint ulcers. Tyramine, a preponderant peripherally acting sympathomimetic amine, was inefficient in both experimental models. It is suggested that the protective activity is due to the influence of these amines on the adrenergic structures, mainly at central level.
α-Methyldopamine and α-methylnoradrenaline administered intraperitoneally afforded significant protection in reserpine-induced ulcers in rats. The optimal doses were 2 and 4 mg/kg. Lower and higher doses were less effective. α-Methyldopamine and α-methylnoradrenaline probably act by reestablishing the normal adrenergic tone which is diminished in reserpine-induced ulcers.
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