Effect of chronic ketanserin treatment on serotonin-induced platelet aggregation in patients with Raynaud's phenomenon

Marasini, Bianca; Biondi, Maria Luisa; Mollica, R.

doi:10.1007/bf00315113

Cited by 3 publications

(6 citation statements)

References 8 publications

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“…There have been no data published about the relationship between ketanserin-induced vasodilation and ketanserin-induced 5-HT2 platelet receptor blockade in patients with Raynaud's phenomenon. This study shows that the two events are independent and confirms our previous finding of discrepancies between subjective improvement and platelet inhibition after chronic ketanserin intake (Marasini et al, 1990).…”

Section: Discussionsupporting

confidence: 92%

“…This study shows that the two events are independent and confirms our previous finding of discrepancies between subjective improvement and platelet inhibition after chronic ketanserin intake (Marasini et al, 1990).…”

Section: Discussionsupporting

confidence: 80%

“…In acute studies 20 mg ketanserin have been used to limit the cases of complete blockade of platelet aggregation, as we previously observed with a dose of 40 mg (Marasini et al, 1990), and…”

Section: Measurementsmentioning

confidence: 99%

“…Furthermore, the recent finding of dissociation between 5-HT2 platelet receptor inhibition and clinical benefit after chronic ketanserin treatment (Marasini et al, 1990), casts some doubts on the mechanism of the drug against this particular vasospasm. In this study we investigated whether ketanserin-induced digital vasodilation paralleled the inhibitory effect of the drug on platelet response to 5-HT in patients with Raynaud's phenomenon, to investigate further the importance of 5-HT2 receptor blockade in the vasodilatory effect of ketanserin in Raynaud's phenomenon.…”

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Digital blood flow and 5‐hydroxytryptamine receptor blockade after ketanserin in patients with Raynaud's phenomenon.

Marasini

Bassani

1990

Brit J Clinical Pharma

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1 The effect of ketanserin on digital blood flow and 5-hydroxytryptamine (5-HT)-induced platelet aggregation was studied in 18 patients with Raynaud's phenomenon. 2 Measurements were made before and after a single dose of 20 mg ketanserin and again after 1 month of continuous treatment with 20 mg ketanserin three times a day. 3 Digital blood flow was assessed by changes in digital pulse volume; platelet aggregation by changes in light transmission after challenge with 10-5 M 5-HT.4 Ketanserin induced a rise in digital blood flow and blocked the platelet response to 5-HT; the two events were not correlated and were independent of subjective improvement. 5 These data do not support the suggestion that 5-HT2-receptor blockade is of major importance in the dilatory effect of ketanserin in Raynaud's phenomenon.

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Section: Discussionsupporting

confidence: 92%

Section: Discussionsupporting

confidence: 80%

Section: Measurementsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Digital blood flow and 5‐hydroxytryptamine receptor blockade after ketanserin in patients with Raynaud's phenomenon.

Marasini

Bassani

1990

Brit J Clinical Pharma

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Serotonin and Serotonin Antagonism in Cardiovascular and Non‐Cardiovascular Disease

Frishman

Huberfeld

Okin

et al. 1995

The Journal of Clinical Pharma

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Serotonin, or 5-hydroxytryptamine, is a naturally-occurring vasoactive substance found primarily in the brain, enterochromaffin tissue, and blood platelets. It has diffuse cardiophysiologic effects. The multiple effects of serotonin on blood vessels can be explained by the existence of 2 serotonergic receptor subtypes (the S1 receptor mediates vasodilation, and the S2 receptor vasoconstriction). Serotonin via the S2 receptor also augments the actions of several other vasoconstricting substances. Serotonin may be responsible for causing, or at least perpetuating, some forms of systemic hypertension through peripheral and central nervous system (CNS) actions. Ketanserin is a highly selective S2-serotonergic antagonist with additional alpha-adrenergic blocking activity, which has been proposed as a therapy for various cardiovascular diseases including hypertension. It has been shown to be more effective than placebo in treating hypertension and comparable in effectiveness to other antihypertensive drugs. Its major side effects relate to the CNS, and prolongation of the electrocardiogram QT interval has been described. Caution must be used when using ketanserin in patients receiving potassium- and magnesium-losing agents, because of the risk of torsades de pointes. Ketanserin has potential utility in the treatment of eclampsia, peripheral vascular disease, carcinoid syndrome, and "shock lung." The drug is not yet approved for clinical use in the United States.

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The effects of a selective 5‐HT2 receptor antagonist (ICI 170,809) on platelet aggregation and pupillary responses in healthy volunteers.

Millson¹,

Jessup²,

Swaisland³

et al. 1992

Brit J Clinical Pharma

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Europe, Crawley, Sussex RH10 2NJ 1 ICI 170,809 (2-(2-dimethylamino-2-methylpropylthio)-3-phenylquinoline hydrochloride)is a potent 5-hydroxytryptamine (5-HT) type 2 postsynaptic receptor antagonist. depression of the dose-response curve to 5-HT at all concentrations of 5-HT and with no evidence for a parallel shift. 5 The ex vivo platelet 5-HT response demonstrated a dose related significant (P < 0.02) decrease in aggregation reaching a maximum at 2 h after dosing with the effect persisting for at least 8 h after dosing with the 7 and 15 mg doses. 6 Resting pupil diameter (RPD), and light induced pupillary responses in the dark adapted pupil, showed a significant (P < 0.01) dose related reduction with significant (P < 0.05) effects still present with the 15 and 30 mg doses at 8 h after dosing. 7 We conclude that, changes in both ex vivo platelet aggregation to 5-HT and dark adapted pupil size, are significantly correlated (P < 0.0001) with log plasma concentrations (ng ml-) of ICI 170,809, enabling the assessment of 5-HT2-receptor antagonism in man.

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Effect of chronic ketanserin treatment on serotonin-induced platelet aggregation in patients with Raynaud's phenomenon

Cited by 3 publications

References 8 publications

Digital blood flow and 5‐hydroxytryptamine receptor blockade after ketanserin in patients with Raynaud's phenomenon.

Digital blood flow and 5‐hydroxytryptamine receptor blockade after ketanserin in patients with Raynaud's phenomenon.

Serotonin and Serotonin Antagonism in Cardiovascular and Non‐Cardiovascular Disease

The effects of a selective 5‐HT2 receptor antagonist (ICI 170,809) on platelet aggregation and pupillary responses in healthy volunteers.

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