Comparison of antianginal activity of nicorandil, propranolol and diltiazem with reference to the antianginal mechanism

Kinoshita, Masahiko; Hashimoto, Kenji; Ohbayashi, Yasunori; Inoue, Tohru; Taguchi, Hisao; Mitsunami, Kenichi

doi:10.1016/0002-9149(89)90209-9

Cited by 16 publications

(1 citation statement)

References 15 publications

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“…In a single-blind study the effects of single-dose nicorandil 30 mg, was compared with those of propranolol 40 mg, diltiazem 60 and 120 mg, and placebo in 12 patients with chronic stable angina pectoris (Kinoshita et al 1989). All patients performed 6 full exercise tests on separate days.…”

Section: Clinical Applicationangina Pectorismentioning

confidence: 99%

Clinical Pharmacology of Potassium Channel Openers

Andersson

1992

Pharmacology & Toxicology

138

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Opening of K+ channels in cell membranes with resulting increase in K+ conductance, shifts the membrane potential in a hyperpolarizing direction towards the K+ equilibrium potential. Hyperpolarization reduces the opening probability of ion channels involved in membrane depolarization and excitation is reduced. K+ channel openers are believed to hyperpolarize smooth muscle cells by a direct action on the cell membrane. The best known members of the group are cromakalim, nicorandil and pinacidil, but several new compounds are being evaluated. In addition, it has recently been shown that also clinically well-known drugs like, e.g. diazoxide and minoxidil exhibit K+ channel opening properties. Nicorandil and new compounds containing nitro groups have a dual mechanism of action, also activating guanylate cyclase, an effect that contributes to their cardiovascular effect profile. K+ channel openers have a wide range of effects. Some of their properties and actions are summarized, and their present applications and/or potential for future application, in e.g. hypertension, angina pectoris, asthma, bladder instability, and several other disorders are discussed. It is concluded that K+ channel openning represents an interesting pharmacological principle with many potential clinical applications. However, most available drugs do not seem to have a sufficient tissue selectivity to be useful therapeutic alternatives. Before the potential of the new members of the group on clinical trials can be properly evaluated, clinical experiences are needed.

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Section: Clinical Applicationangina Pectorismentioning

confidence: 99%

Clinical Pharmacology of Potassium Channel Openers

Andersson

1992

Pharmacology & Toxicology

138

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Nicorandil: A Potassium Channel Opening Drug for Treatment of Ischemic Heart Disease

Goldschmidt

Landzberg

Frishman

1996

The Journal of Clinical Pharma

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Nicorandil is the first oral potassium channel activating drug to be used for the treatment of symptomatic coronary artery disease. It appears to relax vascular smooth muscle through membrane hyperpolarization via increased transmembrane potassium conductance and, like nitrates, through an increase in intracellular cyclic GMP. In addition, nicorandil, in a nitrate-like manner, dilates normal and stenotic coronary arteries and reduces both ventricular preload and afterload. In contrast to nitrates, however, nicorandil does not appear to cause tolerance with long-term administration. In placebo and comparison clinical trials, nicorandil has demonstrated some efficacy and safety in patients with both stable and vasospastic angina pectoris, and it was found to be a myocardial protective agent in animal studies. The antianginal activity of nicorandil, however, is relatively short lived after dosing, which will necessitate the development of extended-release formulations of the drug.

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Is There a Potential Role for KATP Openers in the Treatment of Angina?

Opie

1995

Myocardial Protection and the KATP Channel

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Comparison of antianginal activity of nicorandil, propranolol and diltiazem with reference to the antianginal mechanism

Cited by 16 publications

References 15 publications

Clinical Pharmacology of Potassium Channel Openers

Clinical Pharmacology of Potassium Channel Openers

Nicorandil: A Potassium Channel Opening Drug for Treatment of Ischemic Heart Disease

Is There a Potential Role for KATP Openers in the Treatment of Angina?

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