Document Detail


Cardiovascular safety profile of almotriptan, a new indolic derivative for the treatment of migraine.
MedLine Citation:
PMID:  11134656     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Almotriptan is a new 5-HT(1B/1D) receptor agonist effective for treating acute migraine attacks with or without aura. As 3-5% of patients treated with sumatriptan experience chest symptoms thought to be of cardiac origin, we investigated the cardiovascular safety profile of almotriptan in comparison with that of sumatriptan in six animal models. Almotriptan did not modify blood pressure or heart rate in conscious telemetered normotensive Wistar rats (p.o.), in anaesthetised beagle dogs (i.v.), or in conscious beagle dogs (i.v.), and only produced transient increases when administered (s.c.) to telemetered cynomolgus monkeys. Almotriptan did not consistently affect the duration of the electrocardiogram (ECG) intervals in anaesthetised beagle dogs even when the drug was administered into the coronary artery, nor was ECG morphology altered in telemetered cynomolgus monkeys. In contrast, sumatriptan i.v. consistently increased mean blood pressure and heart rate in conscious beagle dogs. Finally, almotriptan did not modify coronary blood flow at a dose of up to 0.3 mg/kg i.v. in conscious beagle dogs. Thus, almotriptan has a favourable cardiovascular safety profile.
Authors:
J Gras; I Cardelús; J Llenas; J M Palacios
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Publication Detail:
Type:  Comparative Study; Journal Article    
Journal Detail:
Title:  European journal of pharmacology     Volume:  410     ISSN:  0014-2999     ISO Abbreviation:  Eur. J. Pharmacol.     Publication Date:  2000 Dec 
Date Detail:
Created Date:  2001-01-31     Completed Date:  2001-02-15     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  1254354     Medline TA:  Eur J Pharmacol     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  53-9     Citation Subset:  IM    
Affiliation:
Pharmacological Development Department, Almirall Prodesfarma, Research Center, Cardener 68-74, 08024-, Barcelona, Spain. jgras@almirallprodesfarma.com
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MeSH Terms
Descriptor/Qualifier:
Animals
Blood Pressure / drug effects
Cardiovascular System / drug effects*
Cats
Coronary Circulation / drug effects
Coronary Vessels / drug effects
Dogs
Electrocardiography
Female
Guinea Pigs
Heart Rate / drug effects
Indoles / pharmacology*
Injections, Subcutaneous
Macaca fascicularis
Male
Migraine Disorders / drug therapy*
Rats
Rats, Wistar
Receptor, Serotonin, 5-HT1B
Receptor, Serotonin, 5-HT1D
Receptors, Serotonin / metabolism
Safety
Serotonin Agonists / pharmacology*
Sumatriptan / pharmacology
Tryptamines
Chemical
Reg. No./Substance:
0/Indoles; 0/Receptor, Serotonin, 5-HT1B; 0/Receptor, Serotonin, 5-HT1D; 0/Receptors, Serotonin; 0/Serotonin Agonists; 0/Tryptamines; 103628-46-2/Sumatriptan; 154323-57-6/almotriptan

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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