Acute Antianginal Effect of Tiapamil

Gasić, S

doi:10.1159/000173557

Cited by 6 publications

(3 citation statements)

References 6 publications

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“…(Table 2) (21). These findings are relevant to the antianginal effects of tiapamil (19), especially in the variant (vasospastic) form of angina (1 1).…”

Section: Hemodynamic Analysismentioning

confidence: 87%

“…was shown to have a definite antianginal effect in 19 of 22 patients undergoing a bicycle exercise test (19). In 8 of 10 patients studied with thallium-201 myocardial imaging, intravenous tiapamil caused a significant increase in regional myocardial perfusion (19,20), supporting the notion of an increase in regional oxygen supply to the ischemic myocardium. The effect of acute oral tiapamil (600 or 800 mg) on exercise performance in patients with exertional angina pectoris has been demonstrated in a double-blind, placebo-controlled study (42).…”

Section: Antianginal Effectsmentioning

confidence: 90%

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Tiapamil

Hoick

Osterrieder

1987

Cardiovascular Drug Reviews

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Tiapamil is a Ca2+ entry blocker that is under development for the treatment of mild to moderate hypertension and angina pectoris. It also possesses antiarrhythmic properties. This review focuses on the pharmacological, toxicological, and clinical properties of tiapamil. A comparison is made of the effects of tiapamil with the effects of some other Ca2+ entry blockers. CHEMISTRYTiapamil (Ro 1 1-178 1 , Larocord) is the hydrochloride monohydrate of N-(3,4-dimethoxyphenethy1)-2-(3,4-dimethoxyphenyl)-N-methyl-rn-dithiane-2-propylamine 1,1,3,3-tetraoxide; it was synthesized by Ramuz (47,48) ( Fig. 1). With a molecular weight of 610.18, it is an odorless white crystalline powder with a bitter taste. It is moderately soluble in water (-1.7% at 25°C) and is a weak base with a pKa of 8.35 at 25°C. Tiapamil lacks an asymmetrical carbon atom; it is thus a single chemical entity. In this respect tiapamil differs from other phenylalkylamine derivatives, which are available only as racemic mixtures. PHARMACOLOGYTiapamil inhibits depolarization-induced transmembrane Ca2+ influx and interferes with excitation-contraction coupling in the heart and vascular smooth muscle (15,27). Inhibitory effects of tiapamil have been demonstrated in isolated vascularpreparations, including rabbit main pulmonary artery, dog coronary artery, and rat mesenteric and renal arteries (15,27,29). Tiapamil was most effective in relaxing high K+ (150 mM) induced contractures of isolated dog coronary artery strips, with a potency (ICSO 0.22 FM) only slightly lower than that of verapamil (ICSO 0.17 p~) . Both compounds also inhibited 45Ca influx induced by K+ depolarization in rabbit main pulmonary artery at concentrations similar to those required for relaxation of contracture. In isolated, depolarized renal arteries of the rat, tiapamil 77

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“…(Table 2) (21). These findings are relevant to the antianginal effects of tiapamil (19), especially in the variant (vasospastic) form of angina (1 1).…”

Section: Hemodynamic Analysismentioning

confidence: 87%

Section: Antianginal Effectsmentioning

confidence: 90%

Tiapamil

Hoick

Osterrieder

1987

Cardiovascular Drug Reviews

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“…6. 11, 13] and as an antianginal agent [1,2,12,16] and preliminary trials have been conducted to determine whether it can effectively reduce the size of an acute infarct [8]. In spite of the very encouraging results in several areas, the acceptance of tia pamil for clinical use has been hampered by the theoretical possibility that its intrinsic negative inotropic effects [3] may preclude its use in patients with coronary artery disease (CAD).…”

Section: Introductionmentioning

confidence: 99%

Effects of Tiapamil on Myocardial Performance in Coronary Artery Disease

Braun¹,

Miller²,

Terdiman³

et al. 1982

Cardiology

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Tiapamil has been extensively investigated for treatment of cardiac arrhythmias. Concern persists, however, that, as a calcium antagonist, it may seriously depress myocardial function. To investigate this possibility, 20 patients were given tiapamil intravenously and studied by radionuclide ventriculography. Tiapamil markedly lowered arterial pressure. Left ventricular ejection fraction increased from 54 ± 3.3 to 57 ± 3.3%. No significant change in heart rate was noted. Tiapamil did not increase the extent of left ventricular asynergy. The potent vasodilator properties of tiapamil compensate for any intrinsic decrease in left ventricular contractibility, and therefore overall cardiac function is not worsened by the drug in patients with normal or moderately reduced resting ventricular ejection fractions.

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Pharmacokinetics and Hemodynamic Effects of Tiapamil: Exercise Performance, Thallium Stress Scintigraphy, and Radionuclide Ventriculography

Eckert

Pozenel²,

Pillat

1984

The Journal of Clinical Pharma

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The pharmacokinetic behavior and hemodynamic effects of tiapamil, a calcium antagonist, were studied in 16 cardiac patients during an eight-day treatment course, giving oral doses of 600 mg daily. The hemodynamic effects were investigated using exercise performance tests, thallium stress scintigraphy, and radionuclide ventriculography. The areas under the plasma concentration-time curve after the final dose were greater than after the first dose for both tiapamil (+53 per cent) and its metabolite (+24 per cent). One possible explanation is that tiapamil undergoes saturable intestinal wall metabolism. Alternatively, like verapamil, it may undergo a saturable hepatic elimination process. The hemodynamic test series showed that, despite increasing the exercise tolerance, tiapamil significantly reduced the rate-pressure product, an index of myocardial oxygen requirement. Regional myocardial perfusion clearly improved. Ventriculography showed a significant increase in ejection fraction (+18 per cent), cardiac index (+12 per cent), and stroke volume index (+19 per cent). At the same time, the measured mean arterial pressure decreased significantly by about 10 per cent and the calculated peripheral vascular resistance, by about 19 per cent.

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Acute Antianginal Effect of Tiapamil

Cited by 6 publications

References 6 publications

Tiapamil

Tiapamil

Effects of Tiapamil on Myocardial Performance in Coronary Artery Disease

Pharmacokinetics and Hemodynamic Effects of Tiapamil: Exercise Performance, Thallium Stress Scintigraphy, and Radionuclide Ventriculography

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