Drugs online research references









Gen Pharmacol. 1988;19(2):201-4.
Anorectic and behavioural effects of bupropion.

Zarrindast MR, Hosseini-Nia T.

Department of Pharmacology, Faculty of Medicine, University of Tehran, Iran.

1. Bupropion (12.5-75 mg kg-1) was given intraperitoneally to rats and was found to decrease the food consumption of the animals dose-dependently. While phenoxybenzamine, propranolol and methergoline failed to antagonize the anorectic effect of the drug; pimozide a dopamine receptor blocker decreased anorexia induced by bupropion. 2. Bupropion (12.5-50 mg kg-1) also caused a marked increase in locomotor activity of the rats. The increase in locomotion produced by bupropion was completely antagonized by pretreatment of the animals with pimozide and reserpine plus a-methyl-p-tyrosine, but not by pretreatment with phenoxybenzamine, propranolol or methergoline. 3. Taking into considerations the evidences of dopaminergic properties of bupropion shown by the others, it could be suggested that the anorexia and hyperactivity produced by bupropion may be induced through the indirect dopaminergic mechanism.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3127269&dopt=Abstract

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Farmakol Toksikol. 1988 Jan-Feb;51(1):14-7.
[Bupropion activation of memory trace retrieval in amnesia and forgetting]

[Article in Russian]

Il'iuchenok RIu, Dubrovina NI, Vinnitskii IM.

The effect of a new antidepressant bupropion on the processes of retrieval of the conditioned response of passive avoidance in mice under amnesia of different genesis and spontaneous forgetting was studied. The drug was shown to exert the antiamnesic effect and to facilitate retrieval of amnesia-affected or forgotten memory trace. The maximal effect of bupropion was observed at the dosage of 30 mg/kg. At the use of bupropion on the 2nd day after exertion of amnesic influences there was registered the tendency to prolongation of preservation of the conditioned habit enhanced retrieval as compared with greater time periods. The drug effect under memory trace retrieval impaired by cycloheximide-induced amnesia was similar in the action but more pronounced than that under "psychogenic" amnesia. The data obtained testify in favour of an active involvement of the brain dopaminergic system in the processes of memory trace retrieval.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3129303&dopt=Abstract

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Eur J Drug Metab Pharmacokinet. 1988 Jul-Sep;13(3):149-53.
Effect of hepatic and renal dysfunction on disposition of bupropion in rats.

Kaka JS, Al-Khamis KI, Tanira MO.

Department of Clinical Pharmacy, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.

Disposition of bupropion after oral administration was investigated in carbon tetrachloride (CCl4) and gentamicin treated rats. Bupropion exhibits extensive first-pass effect and is mainly cleared by hepatic route. In rats with hepatic damage, maximum plasma concentration (Cmax) was approximately 3 times higher and area under the plasma concentration-time curve up to 6 h (AUC 0-6) and AUC 0-infinity increased on an average 4 and 5 times respectively compared to the control. The half-life was doubled with hepatic dysfunction. These findings suggest that hepatic impairment in rats causes a decrease in first pass effect as well as an increase in the half-life of the drug. Rats with renal impairment, exhibited a significant increase in Cmax, AUC 0-6 and AUC 0-infinity of bupropion approximately 3-fold as compared to the control, no change in half life of the drug was observed. This indicates that rats with renal impairment show less efficient first-pass effect which may lead to increase in systemic bioavailability. The time to peak observed in all treated animals was not significantly different from the control. The percentage of bound bupropion did not differ either in CCl4 or gentamicin treated plasma as compared to the control.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3149241&dopt=Abstract

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