Literature DB >> 2155948

Is metoprolol CR/ZOK more selective than conventional metoprolol and atenolol?

M Kendall1, S Akhlaghi, B Hughes, H Lewis.   

Abstract

An alternative, simple method to assess beta 1-selectivity is to establish the impact of the beta blocker on beta 2-stimulated increases in plasma glucose and decreases in plasma potassium during an intravenous infusion of terbutaline. In the present study the effects of metoprolol CR/ZOK 100 mg, conventional metoprolol 100 mg, atenolol 100 mg, and placebo on these biochemical changes have been compared. In 12 healthy volunteers, terbutaline infusion of 6 micrograms/kg was administered intravenously over 1 hour. Three and a half hours before the infusion they were given a single dose of each of the four treatments in random order, single-blind. The maximum increase in plasma above baseline occurred at the end of a 60-minute terbutaline infusion. All three-beta blockers decreased the peak plasma glucose level achieved compared with placebo (P less than .01) but this reduction was significantly less with metoprolol CR/ZOK pretreatment than with atenolol (P less than .05). Similar results were seen for the AUC values for the curves obtained from the increments over the 60 minutes of the infusion and the subsequent 120 minutes after the infusion. In addition, both the AUC values and the maximum fall in potassium were significantly reduced by all treatments (P less than .05). The metoprolol CR/ZOK preparation produced significantly less effect than atenolol with respect to both AUC (P less than .05) and maximum fall (P less than .01) and significantly less effect than conventional metoprolol tablets in maximum fall (P less than .01). In conclusion, the metoprolol CR/ZOK formulation produces lower plasma concentrations and results in less effect on potassium and glucose compared to conventional metoprolol and atenolol.(ABSTRACT TRUNCATED AT 250 WORDS)

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Year:  1990        PMID: 2155948     DOI: 10.1002/j.1552-4604.1990.tb03505.x

Source DB:  PubMed          Journal:  J Clin Pharmacol        ISSN: 0091-2700            Impact factor:   3.126


  7 in total

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Authors:  M J Kendall
Journal:  Drugs       Date:  1995-09       Impact factor: 9.546

2.  Extent of beta 1- and beta 2-receptor occupancy in plasma assesses the antagonist activity of metoprolol, pindolol, and propranolol in the elderly.

Authors:  T Kaila; E Iisalo; A Lehtonen; H Saarimaa
Journal:  Cardiovasc Drugs Ther       Date:  1993-12       Impact factor: 3.727

3.  Steady-state bioavailability and day-to-day variability of a multiple-unit (CR/ZOK) and a single-unit (OROS) delivery system of metoprolol after once-daily dosing.

Authors:  A Sandberg; B Abrahamsson; A Svenheden; B Olofsson; R Bergstrand
Journal:  Pharm Res       Date:  1993-01       Impact factor: 4.200

Review 4.  Controlled release metoprolol formulations. A review of their pharmacodynamic and pharmacokinetic properties, and therapeutic use in hypertension and ischaemic heart disease.

Authors:  G L Plosker; S P Clissold
Journal:  Drugs       Date:  1992-03       Impact factor: 9.546

Review 5.  Controlled release metoprolol. Clinical pharmacokinetic and therapeutic implications.

Authors:  M J Kendall; S R Maxwell; A Sandberg; G Westergren
Journal:  Clin Pharmacokinet       Date:  1991-11       Impact factor: 6.447

6.  Effects of Beta-Blocker Titration on Glucose Homeostasis in Heart Failure.

Authors:  Orly Vardeny; James Zebrack; Edward M Gilbert; Kai I Cheang
Journal:  J Pharm Technol       Date:  2009

Review 7.  A risk-benefit assessment of celiprolol in the treatment of cardiovascular disease.

Authors:  M J Kendall; I Rajman
Journal:  Drug Saf       Date:  1994-03       Impact factor: 5.606

  7 in total

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