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Almitrine
Systematic (IUPAC) name
6-[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl]- N,N'-
diprop-2-enyl-1,3,5-triazine-2,4-diamine
Identifiers
CAS number 27469-53-0
ATC code R07AB07
PubChem 33887
ChemSpider 31235
Chemical data
Formula C 26H29F2N7  
Mol. mass 477.552 g/mol
SMILES eMolecules & PubChem
Physical data
Melt. point 181 °C (358 °F)
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?
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Almitrine (Duxil) is a piperazine classified as a respiratory stimulant by the ATC. It enhances respiration by acting as an agonist of peripheral chemoreceptors located on the carotid bodies. The drug increases arterial oxygen tension while decreasing arterial carbon dioxide tension in patients with chronic obstructive pulmonary disease. It may also prove useful in the treatment of nocturnal oxygen desaturation without impairing the quality of sleep.

Different pharmacological properties of almitrine-raubasine show that this combination may be a good therapy for the treatment of age-related cerebral disorders and functional rehabilitation after stroke. Many clinical studies have been carried out in France and in the rest of Europe, confirming the value of this compound in such situations. Without discussing the complexity of clinical trials in both the areas of cognitive disorders and stroke, we shall present two studies demonstrating the beneficial effects of almitrine-raubasine against cognitive impairments. The first is a double-blind controlled study versus placebo with a 3-month follow-up period involving patients (aged between 60 and 85) with memory loss, lack of concentration, impaired mental alertness, and emotional instability. The second is a controlled multi-center study of 155 outpatients (age 70-85) presenting with cognitive decline (assessed by MMSE, SCAG). In both these studies, almitrine-raubasine significantly improved symptomatology and was superior to placebo, especially in the vascular cases. This confirms the validity of previous studies and justifies the indication of these compounds in the treatment of age-related cognitive disorders. Other studies also demonstrated the beneficial effect of this compound on neurosensory vascular disorders, with specific studies carried out on chorioretinal dysfunctions (visual symptomatology) and in vestibular disorders (vertigo associated with electronystagmographic modifications). The appropriate and usual dosage (2 tablets per day) and the good tolerance of the compound have been confirmed in a French multi-centric study in 5,361 outpatients.

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