Drugs online research references
Pharmacol Biochem Behav. 1993 Mar;44(3):611-3.
Effects of beta-adrenergic blockers on drug-induced tremors.
Iwata S, Nomoto M, Fukuda T.
Department of Pharmacology, Faculty of Medicine, Kagoshima University, Japan.
We studied the effect of various kinds of beta-adrenergic blockers on oxotremorine-, harmaline- and thyrotropin-releasing hormone (TRH)-induced tremors in mice. To investigate what property of beta-blockers plays the main role in suppressing tremor, we employed five beta-blockers (propranolol, atenolol, butoxamine, pindolol, and arotinolol). All drugs suppressed oxotremorine-induced tremors but none reduced harmaline-induced tremors. Even though TRH-induced tremors were decreased significantly only by propranolol and high doses of arotinolol, all drugs had a tendency to reduce the tremor. We concluded that neuropharmacological mechanisms underlying to harmaline-induced tremors were different from those of TRH- and oxotremorine-induced tremors and that features of beta-blockers (beta 1- or beta 2-selectivity, intrinsic sympathomimetic activity, and membrane stabilizing activity) did not primarily contribute to the suppression of tremors.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8095722&dopt=Abstract
Clin Transplant. 1997 Dec;11(6):577-81.
Elevation of cyclosporin A blood levels during carvedilol treatment in renal transplant patients.
Kaijser M, Johnsson C, Zezina L, Backman U, Dimeny E, Fellstrom B.
Department of Internal Medicine, University Hospital, Uppsala, Sweden.
In a consecutive study of 21 renal transplant patients suffering from chronic vascular rejection (CVR) we added the beta-receptor-blocking drug carvedilol to their regular medication. The purpose was to investigate possible pharmacokinetic interactions between carvedilol and cyclosporine (CsA), since carvedilol will soon be used in clinical trials in renal transplant patients with CVR. On the first day of the study the patients received 6.25 mg of carvedilol added to their daily medication. The dose was increased stepwise to 50 mg while the doses of other beta-blocking drugs were decreased. The goal was to exchange atenolol with carvedilol at a ratio of 2:1 when substituting atenolol with carvedilol. The patients' blood pressure was the final determinant of the dose of carvedilol. The trough levels of CsA were measured on days 1, 14, 30, 90 and 180. It was found that the blood levels of CsA increased when carvedilol was introduced. Thus, the doses of CsA had to be reduced in order to keep the blood levels within the therapeutic range. At 90 d, the daily doses of CsA had been reduced from 3.7 +/- 0.3 to 3.0 +/- 0.2 mg/kg BW (p < 0.001). The present results suggest an interaction between carvedilol and CsA that demands a 20% average reduction of CsA doses to maintain the CsA blood levels within the therapeutic range. However, the interaction shows a great interindividual variation, calling for careful monitoring of the CsA blood levels.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9408688&dopt=Abstract
Arch Int Pharmacodyn Ther. 1993 May-Jun;323:5-15.
Beta-blocking action of bopindolol, a new beta-blocker, and its active metabolites in open chest dogs.
Okuhira M, Nakazawa M, Kameda H, Hara K, Kawada T, Imai S.
Department of Pharmacology, Niigata University School of Medicine, Japan.
The beta-blocking activity of bopindolol, a new nonselective beta-blocker, and of its active metabolites (18-502 and 20-785) was compared with that of propranolol and atenolol in anesthetized open chest dogs. No remarkable changes in basal cardio-hemodynamic parameters were observed in all groups, except for dp/dtmax which was decreased in the bopindolol-, propranolol-and atenolol-treated groups. All beta-blockers used inhibited the isoproterenol (0.1 microgram/kg, i.v.)-induced tachycardia and the increase in myocardial oxygen consumption dose-dependently. The active metabolite 18-502 was the most potent; it was 19 times as potent as propranolol with respect to the antitachycardic action and 34 times as potent as propranolol in inhibiting the increase in oxygen consumption induced by isoproterenol (0.1 microgram/kg). The potency of bopindolol was nearly equal to that of propranolol, while the potency of atenolol and the metabolite 20-785 was weaker than that of propranolol. As 18-502 was found as a metabolite also in man, it is suggested that 18-502 is a more important active metabolite of bopindolol than 20-785 in in vivo conditions, though the metabolite 20-785 is also a potent beta-blocker.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=7902696&dopt=Abstract
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