Almitrine (marketed as Duxil by
Servier
Servier Laboratories (French: Laboratoires Servier, often abbreviated to Servier) is an international pharmaceutical company governed by a non-profit foundation, with its headquarters in France (Suresnes).
The consolidated turnover for the 2018 ...
) is a
diphenylmethylpiperazine
1-(Diphenylmethyl)piperazine, also known as benzhydrylpiperazine, is a chemical compound and piperazine derivative. It features a piperazine ring with a benzhydryl (diphenyl methyl) group bound to one of the nitrogen
Nitrogen is the chemical ...
derivative
In mathematics, the derivative of a function of a real variable measures the sensitivity to change of the function value (output value) with respect to a change in its argument (input value). Derivatives are a fundamental tool of calculus. F ...
classified as a
respiratory stimulant
Stimulants (also often referred to as psychostimulants or colloquially as uppers) is an overarching term that covers many drugs including those that increase activity of the central nervous system and the body, drugs that are pleasurable and inv ...
by the
ATC. It enhances respiration by acting as an
agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the ago ...
of peripheral
chemoreceptors
A chemoreceptor, also known as chemosensor, is a specialized sensory receptor which transduces a chemical substance (endogenous or induced) to generate a biological signal. This signal may be in the form of an action potential, if the chemorecept ...
located on the
carotid bodies
The carotid body is a small cluster of chemoreceptor cells, and supporting sustentacular cells. The carotid body is located in the adventitia, in the bifurcation (fork) of the common carotid artery, which runs along both sides of the neck.
The ca ...
. The drug increases arterial oxygen tension while decreasing arterial carbon dioxide tension in patients with
chronic obstructive pulmonary disease
Chronic obstructive pulmonary disease (COPD) is a type of progressive lung disease characterized by long-term respiratory symptoms and airflow limitation. The main symptoms include shortness of breath and a cough, which may or may not produce ...
. It may also prove useful in the treatment of nocturnal oxygen desaturation without impairing the quality of sleep.
A significant literature exists for this compound, including over 60 papers that Medline labels as reviews.
The clinical efficacy of almitrine-
raubasine
Ajmalicine, also known as δ-yohimbine or raubasine, is an antihypertensive drug used in the treatment of high blood pressure. It has been marketed under numerous brand names including Card-Lamuran, Circolene, Cristanyl, Duxil, Duxor, Hydroxysarp ...
combination therapy for age related cerebral disorders and functional rehabilitation after
stroke
A stroke is a medical condition in which poor blood flow to the brain causes cell death. There are two main types of stroke: ischemic, due to lack of blood flow, and hemorrhagic, due to bleeding. Both cause parts of the brain to stop functionin ...
has been reviewed by Allain and Bentué-Ferrer. They summarize two studies in which almitrine-raubasine improved some symptoms significantly more than placebo, especially in vascular cases. Their paper also suggests that other studies have shown a beneficial effect of this compound on neurosensory vascular disorders, specifically chorioretinal dysfunctions (visual symptomatology) and vertigo associated with electronystagmographic modifications. This paper further claims that the dosage and tolerance of the compound have been confirmed in a French multi-center study of 5,361 outpatients.
Under the brand names Albasine, Aruxil, and Truxil, almitrine-raubasine has been marketed for rehabilitation after stroke, age related neurological disorders, visual disorders related to circulation, and
tinnitus in
Bangladesh
Bangladesh (}, ), officially the People's Republic of Bangladesh, is a country in South Asia. It is the eighth-most populous country in the world, with a population exceeding 165 million people in an area of . Bangladesh is among the mos ...
.
Synthesis

The reaction between 1-
is(4-fluorophenyl)methyliperazine
7469-60-9(1) and Cyanuric Chloride
08-77-0(2) gives 2-
-[Bis(4-fluorophenyl)methyliperazin-1-yl">is(4-fluorophenyl)methyl.html" ;"title="-[Bis(4-fluorophenyl)methyl">-[Bis(4-fluorophenyl)methyliperazin-1-yl4,6-dichloro-1,3,5-triazine
CID:134990507(3). Reaction with Allylamine [107-11-9] (4) completes the synthesis of Almitrine (5).
See also
*Flunarizine
* Diphenylmethylpiperazine
*
Servier
Servier Laboratories (French: Laboratoires Servier, often abbreviated to Servier) is an international pharmaceutical company governed by a non-profit foundation, with its headquarters in France (Suresnes).
The consolidated turnover for the 2018 ...
References
Piperazines
Triazines
Respiratory agents
Fluoroarenes
{{respiratory-system-drug-stub