Comparative evaluation of cardioselectivity of metoprolol OROS and atenolol: A double-blind, placebo-controlled crossover study

Tantucci, Claudio; Bruni, B; Dottorini, Maurizio; Peccini, F.; Motolese, M; Lecaillon, J. B.; Sorbini, C. A.; Grassi, Vittorio

doi:10.1016/0002-8703(90)90106-8

Cited by 14 publications

(6 citation statements)

References 20 publications

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“…Another single-dose study in 12 asthmatic patients showed similar results in postmedication baseline sGaw after 14/190 mg metoprolol oros, whereas after 100 mg atenolol postmedication baseline sGaw was significantly lower than after placebo. 12 In that study single doses of both metoprolol oros and atenolol blunted the salbutamol-induced A U Q c values, with no significant difference between the drugs. 12 These conflicting results on the bronchial effects of single doses of cardioselective ^-adrenergic receptor antagonists indicate a different sensitivity to 0-adrenergic receptor antagonism in different groups of mild to moderate asthmatic patients.…”

Section: Effects On Ft-adrenergic Receptors Of Bronchial Smooth Musclementioning

confidence: 83%

“…12 In that study single doses of both metoprolol oros and atenolol blunted the salbutamol-induced A U Q c values, with no significant difference between the drugs. 12 These conflicting results on the bronchial effects of single doses of cardioselective ^-adrenergic receptor antagonists indicate a different sensitivity to 0-adrenergic receptor antagonism in different groups of mild to moderate asthmatic patients. 20 Therefore, in the treatment of hypertensive asthmatic patients, it would seem sensible to avoid /3-adrenergic receptor antagonists, as alternative forms of antihypertensive therapy are likely to be as effective and at least as well tolerated.…”

Section: Effects On Ft-adrenergic Receptors Of Bronchial Smooth Musclementioning

confidence: 83%

See 1 more Smart Citation

Osmotic release oral drug delivery system of metoprolol in hypertensive asthmatic patients. Pharmacodynamic effects on beta 2-adrenergic receptors.

Bauer

Kaik

1994

Hypertension

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This study investigated the effects of an osmotic release oral drug delivery system of metoprolol on the changes induced by cumulative doses of inhaled salbutamol on bronchomotor tone, skeletal muscle, and the circulatory system after single (day 1) and multiple (day 7) dosing in 18 hypertensive asthmatic patients (forced expiratory volume in 1 second >50% predicted; diastolic blood pressure >90 mm Hg). The patients were given 14/190 mg metoprolol, 100 mg atenolol, and placebo once daily for a 7-day period each in a randomized, double-blind, crossover design. At the estimated time of peak plasma concentrations, cumulative doses of salbutamol (12.5, 37.5, 112.5, 412.5, 812.5, and 1612.5 fig) were applied every 20 minutes. Specific airway conductance, finger tremor amplitude, heart rate, and blood pressure were registered at baseline and at each dose increment. The slopes of the salbutamol dose-response curves of specific airway conductance did not differ on day 1 (P>.05). On day 7, atenolol caused a shift of the dose-response curves of specific airway conductance to the right (P<.05), whereas metoprolol M etoprolol, introduced in 1975, has been described as an effective, well-tolerated, cardioselective ^-adrenergic receptor antagonist without significant partial agonist activity used extensively in the treatment of hypertension and angina pectoris. "3 Its efficacy in the secondary prevention of myocardial infarction and reduction of the incidence of ventricular fibrillation, 4 reinfarction, 3 and sudden death 4 -6 has suggested cardioprotective properties. The oral osmotic (oros) release drug delivery system of metoprolol (Alza Corp) consists of an osmotically active core, made up mainly of active drug, surrounded by a semipermeable membrane.7 A small hole is drilled through this membrane with a high-speed laser beam. Osmotic pressure causes the passage of water into the drug reservoir, resulting in a slow, continuous release of active material. The oros system is designed to release Received January 17, 1994; accepted in revised form June 1, 1994.From the University of Vienna Medical School, Clinical Pharmacology, and the Kaiser Franz-Josef-Hospital, Department of Internal Medicine 2, Vienna, Austria.Presented in part at the 2nd International Symposium on Heart Failure: Mechanisms and Management, Geneva, Switzerland, May 16-20, 1993.Reprint requests to Karin Bauer, MD, University of Vienna Medical School, Clinical Pharmacology, AKH-Ebene 6, Wahringer Gurtel 18-20, A-1090 Vienna, Austria.Correspondence to G.

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Section: Effects On Ft-adrenergic Receptors Of Bronchial Smooth Musclementioning

confidence: 83%

Section: Effects On Ft-adrenergic Receptors Of Bronchial Smooth Musclementioning

confidence: 83%

Osmotic release oral drug delivery system of metoprolol in hypertensive asthmatic patients. Pharmacodynamic effects on beta 2-adrenergic receptors.

Bauer

Kaik

1994

Hypertension

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“…Analysis of change in FEV 1 associated with the use of cardioselective betablockers in double-blind studies has recently been performed and mean results, both statistically and clinically, have been minimal (28). Consequently, we examined these same double-blind studies for evidence of either symptoms or marked decline in FEV 1 in individual patients due to cardioselective beta-blocker -induced bronchospasm (Table 1) (26,(31)(32)(33)(34)(35)(36)(37)(38)(39)(40)(41)(42)(43)(44)(45)(46)(47)(48)(49)(50). Because the focus of this article concerns patients with heart failure or a history of MI, any patients in these reports with bronchospasm due to agents with intrinsic sympathomimetic activity were not included.…”

Section: Evidence For Cardioselective Beta-blocker -Induced Bronchospasmmentioning

confidence: 99%

Cardioselective Beta‐Blockers in Patients with Asthma and Concomitant Heart Failure or History of Myocardial Infarction: When Do Benefits Outweigh Risks?

et al. 2003

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“…Its role in relation to ~-blockers has been discussed by Kendall and John (1985). More recently, its advantages in terms of ~l-selectivity based on a study in patients with reversible obstructive airways disease have been presented (Tantucci et al 1990). In a replicate design study the CR and 'Oros' formulations were compared, and both gave similarly even plasma concentration profiles (Abrahamsson et al 1990b).…”

Section: Comparison With Other Extended Release Preparationsmentioning

confidence: 99%

Controlled Release Metoprolol

Kendall

Maxwell

Sandberg

et al. 1991

Clinical Pharmacokinetics

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Metoprolol is a relatively beta 1-selective beta-blocker used extensively to treat hypertension and angina and as a prophylaxis after myocardial infarction. Conventional formulations are usually administered twice daily and the drug has a tendency to lose its selectivity of action at higher plasma concentrations. Two controlled release formulations, metoprolol CR and metoprolol 'Oros', have made it possible to achieve sustained beta 1-blockade over an entire 24h period and to minimise the loss of selectivity associated with higher plasma concentrations. The CR formulation has been extensively investigated and is the major subject of this review. The 'Oros' formulation is pharmaceutically different from the CR, yet both produce similar plasma concentration profiles and comparable beta 1-blocking effects. The availability of these preparations occurs at a time when increasingly persuasive data are becoming available on the cardioprotective or coronary preventive action of metoprolol.

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Comparative evaluation of cardioselectivity of metoprolol OROS and atenolol: A double-blind, placebo-controlled crossover study

Cited by 14 publications

References 20 publications

Osmotic release oral drug delivery system of metoprolol in hypertensive asthmatic patients. Pharmacodynamic effects on beta 2-adrenergic receptors.

Osmotic release oral drug delivery system of metoprolol in hypertensive asthmatic patients. Pharmacodynamic effects on beta 2-adrenergic receptors.

Cardioselective Beta‐Blockers in Patients with Asthma and Concomitant Heart Failure or History of Myocardial Infarction: When Do Benefits Outweigh Risks?

Controlled Release Metoprolol

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