Disease relevance of ALMITRINE

• Peripheral neuropathy in patients treated with almitrine dimesylate [1].
• Almitrine bismesylate improves arterial blood gas values in patients with chronic obstructive lung disease, apparently by reducing intrapulmonary ventilation-perfusion mismatching, and appears to be useful in the long-term management of these patients [2].
• Almitrine bismesylate and hypoxemia [3].
• A double blind prospective study of the effect of almitrine bismesylate and placebo on peripheral-nerve function was carried out in 12 patients with chronic bronchitis and arterial hypoxaemia (mean (SD) FEV1% predicted 38 (16), arterial oxygen tension (PaO2) 7.56 (0.76) kPa) [4].
• Almitrine bismesylate and oxygen therapy in hypoxic cor pulmonale [5].

Psychiatry related information on ALMITRINE

• Almitrine bismesylate increased PaO2 by 8.1 +/- 2.1 mm Hg (mean +/- SEM), decreased arterial carbon dioxide tension by 3.0 +/- 0.7 mm Hg (mean +/- SEM), and increased minute ventilation by 3.1 +/- 0.5 liters/minute (mean +/- SEM) during wakefulness [6].
• Plasma almitrine bismesylate levels were highly variable, and marked individual differences in peak levels and terminal phase rate constants and half lives were found [7].

High impact information on ALMITRINE

• The effect of almitrine bismesylate on hypoxemia in chronic obstructive pulmonary disease [2].
• In this double-blind, parallel, placebo-controlled study, patients with COPD received 50 mg of almitrine bismesylate (n = 9) or placebo (n = 11) twice a day for one year [6].
• Long-term effects of almitrine bismesylate on oxygenation during wakefulness and sleep in chronic obstructive pulmonary disease [6].
• Effects of almitrine bismesylate on the ionic currents of chemoreceptor cells from the carotid body [8].
• The effects of almitrine bismesylate and medroxyprogesterone acetate on oxygenation during wakefulness and sleep were compared in six patients with chronic obstructive lung disease and carbon dioxide retention [9].

Chemical compound and disease context of ALMITRINE

• The effects of almitrine bismesylate (initial intravenous dose 0.6 mg.kg-1 followed by continuous infusion of 0.4 mg.kg-1.h-1) on the ventilatory response to CO2 during hyperoxia and hypoxia were determined in 6 anaesthetized cats with the use of the dynamic end-tidal CO2 forcing technique [10].
• Inhaled NO and almitrine bismesylate in patients with acute respiratory distress syndrome: effect of noradrenalin [11].
• We studied whether exercise endurance under normobaric hypoxia can be enhanced by increasing hypoxic ventilatory sensitivity with almitrine bismesylate (ALM) [12].

Biological context of ALMITRINE

• 1. In four awake dogs we measured EMG activity of three inspiratory and four expiratory muscles during sustained central chemoreceptor stimulation (CO2 inhalation), and peripheral chemoreceptor stimulation (intravenous infusion of almitrine bismesylate (almitrine)) [13].
• High-dose almitrine bismesylate inhibits hypoxic pulmonary vasoconstriction in closed-chest dogs [14].
• INTERVENTIONS: Inhaled nitric oxide (20 parts per million for 15 mins) in the supine and prone position, and intravenous almitrine bismesylate while prone (1 mg/kg/hr for 60 mins), alone or combined with nitric oxide [15].
• Low dose almitrine bismesylate improves pulmonary gas exchange during canine one-lung hypoxia [16].
• Almitrine bismesylate decreased the alveolar-arterial oxygen difference vs. baseline from 406 +/- 124 torr (53.9 +/- 16.5 kPa) to 386 +/- 112 torr (51.3 +/- 14.8 kPa) and vs. nitric oxide and supine position from 406 +/- 111 torr (53.9 +/- 14.7 kPa) to 386 +/- 112 torr (51.3 +/- 14.8 kPa) (p < .05) [15].

Anatomical context of ALMITRINE

• Almitrine bismesylate is a peripheral chemoreceptor agonist that improves arterial oxygen tension (PaO2) in patients with COPD during wakefulness [6].
• Some authors have observed an increase in pulmonary artery pressure (Ppa) after single doses of almitrine bismesylate (A) [17].
• We conclude that almitrine bismesylate during normoxia enhances the CO2 sensitivity of the peripheral chemoreflex loop and decreases the apneic threshold due to an action located outside the brain stem [18].
• Almitrine bismesylate at a dose of 0.5 mg kg-1 of body weight was injected intravenously in the intact animals and following bilateral vagotomy which spared the right recurrent laryngeal nerve [19].
• Almitrine bismesylate disposition in the human digestive tract [20].

Associations of ALMITRINE with other chemical compounds

• In a porcine model of oleic acid-induced lung injury, the effects of inhaled nitric oxide (iNO) and intravenous almitrine bismesylate (ivALM), which enhances the hypoxic pulmonary vasoconstriction on the distribution of regional pulmonary blood flow (PBF), were assessed [21].
• 2. Animals with innervated chemoreceptors (n = 16) reacted to almitrine bismesylate with a significant (P <0.05) increase in both ACTH and cortisol [22].
• Effect of arterial chemoreceptor stimulation with almitrine bismesylate on plasma renin activity, aldosterone, ACTH and cortisol in anaesthetized, artificially ventilated cats [22].
• Plasma vasopressin levels in healthy young men in response to stimulation of the peripheral arterial chemoreceptors by almitrine bismesylate [23].
• Influence of infusion of deoxycorticosterone acetate on the responses of kidney function elicited by stimulation of the peripheral arterial chemoreceptors with almitrine bismesylate in anaesthetized rats [24].

Gene context of ALMITRINE

• STUDY OBJECTIVE: Assessment of acute and chronic effects of low-dose almitrine bismesylate (AB) in stable chronic obstructive pulmonary disease (COPD) [25].
• The purpose of this study was to investigate the possible participation of atrial natriuretic factor (ANF) in the natriuretic and diuretic response occurring after stimulation of the peripheral arterial chemoreceptors by almitrine bismesylate in normoxic humans [26].
• To validate a recently developed liquid chromatography/ultraviolet (LC/UV) method in a pharmacokinetic study of Vectarion (almitrine) where the unchanged drug, its five metabolites and an internal standard are analysed, on-line fast atom bombardment liquid chromatography/mass spectrometry (FAB LC/MS) with a moving belt interface has been used [27].

Analytical, diagnostic and therapeutic context of ALMITRINE

• Almitrine bismesylate was studied for its effects on hypoxemia in 67 patients with chronic obstructive lung disease in a placebo-controlled, double-blind study [2].
• The effects of low dose almitrine bismesylate on pulmonary gas exchange, venous admixture, and pulmonary perfusion were examined in a canine one-lung hypoxic model [16].
• Dose-response and pharmacokinetic study with almitrine bismesylate after single oral administrations in COPD patients [28].
• Intubation and mechanical ventilation avoided by using almitrine bismesylate in an acute hypoxemic pneumonia [29].
• OBJECTIVES: To determine possible additive effects of combined high-dose partial liquid ventilation (PLV) and almitrine bismesylate (ALM) on pulmonary gas exchange and hemodynamics in an animal model of acute lung injury (ALI) [30].

References