Drugs online research references









Neuropharmacology. 1986 Feb;25(2):199-202.
Effect of plasma from patients containing bupropion and its metabolites on the uptake of norepinephrine.

Perumal AS, Smith TM, Suckow RF, Cooper TB.

The uptake of norepinephrine into cortical punches from the brain of the rat was studied in the presence of buffer and plasma from patients containing bupropion and its metabolites. Even though bupropion and its metabolite (compound II) were equipotent in inhibiting the uptake of NE in buffer, compound II was twice as active as bupropion in the presence of human plasma. When the inhibition of uptake of NE in the presence of plasma, obtained from patients on bupropion on steady-state, was correlated with levels of bupropion and its metabolites (II, III, IV) a highly significant correlation was seen in the presence of compound II. Since this compound accumulated in plasma from patients 20-100 times that of the parent compound, the mode of action of bupropion may in part be due to the effect of this compound on the uptake of NE.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3084990&dopt=Abstract

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J Pharmacol Exp Ther. 1981 Jun;217(3):602-10.
Radioimmunoassay and pharmacokinetic profile of bupropion in the dog.

Butz RF, Schroeder DH, Welch RM, Mehta NB, Phillips AP, Findlay JW.

A radioimmunoassay (RIA) procedure for the quantification of bupropion (dl-2-tert-butylamino-3'-chloropropiophenone) in biological fluids is described. Immunization of rabbits with conjugates of bovine serum albumin and p-succinoyl propylbupropion or p-carbomethoxybupropion resulted in the production of antisera which are capable of detecting less than 1 ng ml-1 (100 pg actual mass) of bupropion in the RIA, utilizing [6-3H] bupropion as radioligand. The antisera used in these studies have low cross-reaction (approximately 0.1% or less) with known side chain metabolites of bupropion, but exhibit significant cross-reaction with p-hydroxybupropion (30.3%). Excellent agreement was obtained between RIA and high-pressure liquid chromatography determinations of bupropion concentrations in human plasma samples, but plasma or serum from bupropion-treated dogs, rats and mice required extraction from basic medium to remove some interference before RIA. The assay was applied to a study of bupropion disposition in two beagles of each sex after i.v. and p.o. administrations of bupropion hydrochloride (100 mg). The pharmacokinetic profile in dogs was best described by an open two-compartment model after either route of drug administration. Peak plasma bupropion levels after oral dosing were highly variable, ranging from 12.9 to 63.5 ng ml-1 at 26 to 32 min after drug administration. The mean terminal phase half-life of bupropion was calculated to be 1.73 hr after either route and the absolute oral bioavailability of the drug varied from 2.0 to 6.5%.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6785419&dopt=Abstract

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J Clin Psychiatry. 1984 Jul;45(7 Pt 2):29-36.
Delineation of anxiety and phobic disorders responsive to monoamine oxidase inhibitors: implications for classification.

Sheehan DV.

Studies of the treatment of panic anxiety and various other states with monoamine oxidase (MAO) inhibitors are critically reviewed. It is concluded that MAOIs have differential effects on several dimensions of pathologic anxiety. The association between depression and anxiety states is also reviewed; it is observed that MAOIs effectively treat severe anxiety and phobic disorders without operating strictly via their antidepressant mechanism. In addition, it is proposed that biologic depression and biologic anxiety should be considered to have some independence from one another. Guidelines for the clinical delineation of anxiety disorders are provided, and the clinical and research implications of the proposal for revision of DSM-III anxiety and phobic disorders section, are outlined in detail. It is suggested that anxiety and phobic disorders be classified into endogenous (disease) and exogenous (nondisease) types.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6429129&dopt=Abstract

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