Almitrine

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
Clinical data
AHFS/Drugs.com	International Drug Names
Pregnancy cat.	?
Legal status	?
Identifiers
CAS number	27469-53-0
ATC code	R07AB07
PubChem	CID 33887
DrugBank	DB01430
ChemSpider	31235 Y
UNII	9A1222NBG4 Y
KEGG	D07126 Y
ChEBI	CHEBI:53778 Y
Chemical data
Formula	C26H29F2N7
Mol. mass	477.552 g/mol
SMILES	eMolecules & PubChem
InChI InChI=1S/C26H29F2N7/c1-3-13-29-24-31-25(30-14-4-2)33-26(32-24)35-17-15-34(16-18-35)23(19-5-9-21(27)10-6-19)20-7-11-22(28)12-8-20/h3-12,23H,1-2,13-18H2,(H2,29,30,31,32,33) Y Key:OBDOVFRMEYHSQB-UHFFFAOYSA-N Y
Physical data
Melt. point	181 °C (358 °F)
Y(what is this?)  (verify)

Almitrine (marketed as Duxil by Servier) is a diphenylmethylpiperazine derivative 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.

See also

• Diphenylmethylpiperazine
• Servier