Drugs online research references
Pharmazie. 1990 Nov;45(11):847-9.
The influence of ethanol on the distribution of amitriptyline and nortriptyline in rats.
Negrusz A, Brandys J, Piekoszewski W.
Toxicological Department, Medical Academy Cracov, Krakow, Poland.
The influence of ethanol in single and multiple doses on concentration-time profile of amitriptyline (1) and nortriptyline (2) in rat serum, brain, heart, and liver was studied. AUC0-6 values were calculated and statistically compared as well as cmax values in serum and tissues. Ethanol inhibited N-demethylation of 1 and therefore 2 has not been detected in biological material. AUC0-6 and cmax values were less than in control group. All AUC0-6 and cmax values for 1 in ethanol treated groups of rats were statistically significant compared with the control group.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2100338&dopt=Abstract
Zhongguo Yao Li Xue Bao. 1989 Sep;10(5):465-9.
Effects of nortriptyline on the activities of human and rat liver microsome bufuralol 1'-hydroxylase in vitro.
Tu ZG, Seddon CE, Boobis AR, Davies DS.
The effects of nortriptyline in vitro on the activities of optical isomer and racemate bufuralol 1'-hydroxylase in man and Wistar rat liver microsomal fractions were studied. There was a dose-dependent inhibitory effect of nortriptyline on bufuralol 1'-hydroxylase in both species. While the concentration of nortriptyline greater than or equal to 0.32 mumol/L and greater than or equal to 1.6 mumol/L, the activities of (+), (-) and (+/-) bufuralol 1'-hydroxylase were significantly reduced in man and rat, respectively. The values of inhibitor concentration causing 50% reduction (IC50) to (+), (-) and (+/-) bufuralol 1'-hydroxylase were 10, 19 and 14 mumol/L for human and 4, 10, 6 mumol/L for rat, respectively. It was shown by improved Dixon's plot that the inhibitory type was competitive, and the inhibitory constant (Ki) values to (+), (-) and (+/-) bufuralol 1'-hydroxylase were 5, 3, 4 mumol/L for human and 55, 29, 43 mumol/L for rat, respectively. These results indicate that nortriptyline is a very potent competitive inhibitor to bufuralol 1'-hydroxylase in man and Wistar rat.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2618737&dopt=Abstract
Ther Drug Monit. 1988;10(2):231-3.
Alprazolam does not inhibit the metabolism of nortriptyline in depressed patients or inhibit the metabolism of desipramine in human liver microsomes.
Bertilsson L, Aberg-Wistedt A, Liden A, Otani K, Spina E.
Department of Clinical Pharmacology, Karolinska Institute, Huddinge Hospital, Sweden.
In 10 patients treated with nortriptyline, the steady-state plasma concentrations of the parent drug and the active 10-hydroxy metabolite were very similar before and during concomitant treatment with alprazolam (0.5 mg orally t.i.d.). In human liver microsomes the 2-hydroxylation of desipramine was not inhibited by alprazolam. The absence of an inhibition by alprazolam on the hydroxylations of nortriptyline in vivo and of desipramine in vitro indicates that alprazolam is not metabolized by the debrisoquine hydroxylase.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3381243&dopt=Abstract
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