Drugs online research references









Endocrinology. 1987 Jul;121(1):316-22.
Control of prolactin release induced by suckling.

de Greef WJ, Voogt JL, Visser TJ, Lamberts SW, van der Schoot P.

In the present study, the role of dopamine and TRH in suckling-induced PRL release was investigated. Bupropion, a dopamine reuptake blocker, increased hypophysial stalk dopamine levels and inhibited suckling-induced PRL release. A short period of suckling, thought to induce a transient decrease in hypothalamic dopamine release, led to higher PRL levels following an iv injection of TRH than in rats which had not nursed their young for a short period after 4- to 6-h separation. These results, in combination with previous data, suggest that a decrease in hypothalamic dopamine release is important for suckling-induced PRL release. Increased PRL release may be in part due to an augmented hypothalamic release of TRH. Since serotonergic mechanisms seem involved in TRH release, lactating rats were treated with drugs acting on serotonergic pathways. Parachlorophenylalanine and pizotifen did not alter suckling-induced PRL release. Methysergide, a serotonin receptor blocker, prevented this PRL release when administered ip but not when injected into the lateral brain ventricle. Since methysergide is converted peripherally into metabolite(s) with dopamine agonistic activity, its effect on suckling-induced PRL release may be due to this action, rather than to its action on serotonin receptors. Thus, these data do not indicate that serotonergic mechanisms are important for suckling-induced PRL release. Passive immunization against TRH inhibited suckling-induced PRL release, indicating that TRH is a hypophysiotropic mediator of this PRL release.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3109881&dopt=Abstract

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Hosp Community Psychiatry. 1985 May;36(5):513-6.
Antidepressant drug therapy: the role of the new antidepressants.

Prien RF, Blaine JD, Levine J.

Three new antidepressants have been marketed in the United States since 1980, and about two dozen more are being evaluated. In a 1983 workshop convened by the National Institute of Mental Health, participants examined the claims made for the newer antidepressants in relation to clinical efficacy, speed of onset, cardiovascular effects, and other adverse reactions. In this summary report of the workshop, primarily covering amoxapine, maprotiline, trazodone, and the investigational drug bupropion, the authors note that none of the new antidepressants demonstrate greater effectiveness than standard tricyclics, although some produce a different profile of side effects. The main benefit of the newer drugs is that they offer new options for the treatment of patients who cannot tolerate side effects of the traditional drugs or have responded unsatisfactorily to them.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3924813&dopt=Abstract

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Eur J Clin Pharmacol. 1985;29(1):97-103.
The disposition of bupropion and its metabolites in healthy male volunteers after single and multiple doses.

Posner J, Bye A, Dean K, Peck AW, Whiteman PD.

The pharmacokinetics of bupropion and 3 of its basic metabolites were determined in 8 young, healthy, male volunteers after single and multiple oral doses of bupropion. Plasma profiles were obtained: 1) after a single 100 mg oral dose of bupropion hydrochloride, 2) following administration of 100 mg 8-hourly for 14 days and 3) again after a single 100 mg dose 14 days later. Plasma concentrations of the parent drug and metabolites were determined by high-performance liquid chromatography. Saliva secretion and pupil diameters were measured, subjective assessments of sleep made using visual analogue scales and side effects, blood counts and biochemistry were monitored. After the first dose mean elimination half lives (t1/2) of bupropion, and metabolites I and II were 8, 19 and 19 h respectively. On repeated administration there was little accumulation of the parent drug and no evidence for induction of its own metabolism. Accumulation of I was consistent with its rate of elimination after single doses while that of II was greater than predicted with prolongation of t1/2 to 35 h. Metabolite III was barely detectable after single doses but its accumulation on multiple dosing was consistent with its long half life (35 h) determined on occasion 2. Saliva secretion was significantly reduced during the multiple dosing period but there were no complaints of dry mouth. Subjective assessments of sleep were not significantly altered though one subject reported vivid dreams. There were no other adverse reactions.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3932079&dopt=Abstract

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