Responsiveness of Various Symptoms of Vascular Disorders to Calcium Antagonists

Verhaegen, H.; Reyntjens, A.; Hörig, C; Pötsch, W.

doi:10.1177/000331977903000703

Cited by 6 publications

(3 citation statements)

References 2 publications

(1 reference statement)

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“…It is a difluorated piperazine derivative that is available in several countries in Europe for the treatment of vascular disorders, including those of the brain. 1 This drug is a potent, long-acting antivasoconstrictor agent which inhibits the influx of calcium into vascular smooth muscle cells. 2 In a screening program for drugs which may protect against brain hypoxia, flunarizine was found to be a powerful agent.…”

Section: Introductionmentioning

confidence: 99%

A Double‐blind Placebo‐controlled Prophylactic Study of Flunarizine (Sibelium®) in Migraine

1981

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SYNOPSIS The potential prophylactic value of a daily dose of 10 mg flunarizine, a calcium antagonist with anti‐vasospastic properties was studied in a 3‐month double‐blind placebo‐controlled trial in 58 migraineurs. With an almost perfect mutual correlation, both the patients' overall appreciation of the treatment and the reduction of migraine attacks proved flunarizine to be effective (p<0.001). Half of the flunarizine‐patients considered the treatment certainly beneficial in contrast to none of the placebo‐patients. In 21 of the 29 flunarizine‐patients the attack rate was lower than expected in 20 of the 29 controls it was not. Younger patients appeared to respond better to the treatment. Flunarizine displayed a gradually increasing effect; during the third month 83% of the treated patients were completely attack‐free. The drug did not appear to influence the severity and duration of attacks, however. Treatment was very well tolerated. Flunarizine, therefore, appears to be a very suitable agent for migraine prophylaxis but it should be given for more than two months in order to obtain full effectiveness with this dosage.

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Section: Introductionmentioning

confidence: 99%

A Double‐blind Placebo‐controlled Prophylactic Study of Flunarizine (Sibelium®) in Migraine

1981

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“…2,3 However, calcium channel antagonists are also effective in the treatment of cerebral vasospasm following subarachnoid hemorrhage 4,5 and peripheral vascular disease. 6 In addition, calcium blockers appear to be effective in the treatment of both common and classic migraine. [7][8][9] In the present report, the pharmacologic effects of the calcium channel antagonists are reviewed.…”

Section: Introductionmentioning

confidence: 99%

“…2,3 Flunarizine and cinnarizine, on the other hand, have been used in the treatment of peripheral vascular disorders. 6 The non-specific calcium antagonists are a group of drugs which have previously been described in terms of their actions in other physiologic systems. In addition, each of these agents is capable of blocking calcium channels.…”

Section: Introductionmentioning

confidence: 99%

The Pharmacology of Calcium Channel Antagonists: a Novel Class of Anti‐migraine Agents?

Peroutka

1983

Headache

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SYNOPSIS, The calcium channel antagonists are a recently developed class of vasodilators that prevent the influx of calcium into vascular smooth muscle. The unique pharmacologic effects of these agents provide a theoretical basis for their use in the treatment of migraine. First, the calcium channel antagonists inhibit the actions of all vasoactive substances on intracerebral smooth muscle via a blockade of the "final common pathway" of cellular contraction. Secondly, the vascular effects of the calcium channel antagonists are selective for intracerebral versus peripheral vessels. Clinically, two specific calcium antagonists (flunarizine, cinnarizine) and two non‐specific antagonists (cyproheptadine, amitriptyline) are effective in the treatment of migraine. Further studies will determine whether the calcium channel antagonists, as a class of agents, are effective in the treatment of migraine and other forms of vascular headache. This novel class of vasodilators also provides a powerful tool for the critical evaluation of the vascular theory of migraine.

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1,4‐Dihydropyridine Ca²⁺channel antagonists and activators: A comparison of binding characteristics with pharmacology

Janis

Triggle

1984

Drug Development Research

240

125

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This comparison of the binding characteristics and pharmacology of 1,4-dihydropyridines indicates that the high-affinity binding sites studied in cardiac and smooth muscle cells represent a major site of action of these drugs, and that this site is the Ca2+ channel or a closely related protein. Electrophysiological studies suggest that the effects of both Ca2+ channel inhibitors and activators are voltage dependent. The apparent lack of agreement between the equilibrium dissociation constants for [3H]1 ,4-dihydropyridines and their potency in cardiac muscle may be due to conformational modifications that occur in the 1,4-dihydropyridine binding site as a result of voltage or other changes during membrane isolation. The selective effect of 1 ,4-dihydropyridines for vascular smooth muscle relative to cardiac muscle may be explained, in part, by differences in membrane potentials and Ca2+ channel regulatory mechanisms and, in part, by differences in receptor structure. 1,4-Dihydropyridine antagonists and activators appear to bind to a common site that is not the same as the binding site for nondihydropyridine Ca2+ channel antagonists.

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Responsiveness of Various Symptoms of Vascular Disorders to Calcium Antagonists

Cited by 6 publications

References 2 publications

A Double‐blind Placebo‐controlled Prophylactic Study of Flunarizine (Sibelium®) in Migraine

A Double‐blind Placebo‐controlled Prophylactic Study of Flunarizine (Sibelium®) in Migraine

The Pharmacology of Calcium Channel Antagonists: a Novel Class of Anti‐migraine Agents?

1,4‐Dihydropyridine Ca²⁺channel antagonists and activators: A comparison of binding characteristics with pharmacology

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Responsiveness of Various Symptoms of Vascular Disorders to Calcium Antagonists

Cited by 6 publications

References 2 publications

A Double‐blind Placebo‐controlled Prophylactic Study of Flunarizine (Sibelium®) in Migraine

A Double‐blind Placebo‐controlled Prophylactic Study of Flunarizine (Sibelium®) in Migraine

The Pharmacology of Calcium Channel Antagonists: a Novel Class of Anti‐migraine Agents?

1,4‐Dihydropyridine Ca2+channel antagonists and activators: A comparison of binding characteristics with pharmacology

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1,4‐Dihydropyridine Ca²⁺channel antagonists and activators: A comparison of binding characteristics with pharmacology