Drugs online research references
Am Heart J. 1990 Aug;120(2):490-4.
Safety and tolerability of metoprolol OROS in hypertension treatment.
Feliciano N, Kasarjian PH, McMillen JI, Grau KE, Kessler C, Stevelman HB, Hogan LB, Mroczek WJ, Goldstein RJ, Montoro R.
Cardiovascular Clinical Research, CIBA-GEIGY Corporation, Summit, NJ 07901.
One hundred twenty-six patients with mild to moderate hypertension responsive to beta-adrenergic blocking agents--alone or in combination with other antihypertensive drugs--entered this open-label, multicenter study designed to evaluate the safety and tolerability of metoprolol OROS (metoprolol fumarate). Metoprolol OROS was given once daily for 14 weeks in doses ranging from 100 to 600 mg. Satisfactory blood pressure control was achieved by 85% of the patients at doses between 100 and 400 mg. Mean diastolic blood pressure was maintained at or below 90 mm Hg. Adverse reactions were experienced by 29% of the patients; most of these reactions were mild or moderate, and none was unexpected for treatment with a beta-blocker. Only three patients withdrew because of adverse reactions. The results of this study indicate that metoprolol OROS given once daily is safe and well tolerated.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2382634&dopt=Abstract
J Pharmacol Methods. 1988 Apr;19(2):93-107.
Simultaneous assessment of membrane-stabilizing and beta-adrenoceptor blocking activity of drugs with the rat isolated left atria.
Doggrell SA.
Department of Pharmacology, School of Medicine, University of Auckland, New Zealand.
Three consecutive challenges of the rat isolated left atria with electrical stimulation and then electrical stimulation and isoprenaline were made. The responses to electrical stimulation decreased and the responses to isoprenaline increased with consecutive challenges such that the maximal combined response to electrical stimulation and isoprenaline remained constant. The sensitivity (pD2) to isoprenaline decreased with successive challenges. Thus, in studies of the effects of drugs on the responses to electrical stimulation and isoprenaline, it is necessary to perform parallel experiments with untreated atria to monitor changes in the responses unrelated to the addition of drug. Analysis of the effects of procaine, metoprolol, and propranolol on the responses to electrical stimulation and/or isoprenaline demonstrated distinct contractile manifestations of beta-adrenoceptor blocking and membrane stabilizing activity. The beta-adrenoceptor blocking activity of metroprolol at 10(-7) M and propranolol (3 X 10(-9)-10(-6) M) consisted of parallel rightward shifts of the concentration-response curves to isoprenaline alone. There were three components to the membrane-stabilizing action of drugs: first, there was a decrease in the responses to electrical stimulation alone, which was observed with procaine at greater than or equal to 10(-4) M and propranolol at greater than or equal to 3 X 10(-9) M, second, there was a small parallel rightward shift of concentration-response curve to isoprenaline alone with metoprolol at 10(-6) M and propranolol at 3 X 10(-6) M (that the inhibitory effects of metoprolol at 10(-6) M or propranolol at 3 X 10(-6) M are greater than can be explained by beta-adrenoceptor blockade only may be detected either by determining pA2 values from the formula pA2 = pAx + log(x - 1) or by Schild analysis); third, the highest concentrations of procaine (3 X 10(-4) M) and propranolol (10(-5) M) tested decreased the maximal combined response to electrical stimulation and isoprenaline.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2896276&dopt=Abstract
Nephron. 1985;39(3):175-8.
Effects of propranolol and metoprolol on glucose, cyclic AMP and insulin responses during pharmacologic hyperglucagonemia in hemodialysis patients.
Pun KK, Yeung CK, Yeung RT.
Propranolol-induced hypoglycemia in hemodialysis patients has been increasingly recognized. We studied the effects of a nonselective beta-blocker (propranolol) and a beta 1-selective-blocker (metoprolol) on glucose metabolism during pharmacologic hyperglucagonemia in these patients. cAMP and insulin responses to glucagon were noted to be significantly higher in all patients after dialysis. This may possibly be due to the removal of a dialyzable factor suppressing these responses. However, despite a similar cAMP response, patients on propranolol had significantly lower glucose response than those not receiving beta-blocker before and after dialysis. While patients on metoprolol also had impaired glucose response before dialysis, this significantly improved after dialysis possibly due to the removal of active metabolite(s). Results suggest that metoprolol has less interference on glucose response to glucagon than propranolol in hemodialysis.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2983250&dopt=Abstract
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