Sign Out
Cough Suppressant.
Pharmacology: Pharmacodynamics: Levodropropizine has antitussive effects in particular on the peripheral type at the tracheobronchial level, accompanied by anti-allergy and anti-biochemical effects. In animals, the product also exhibited local anesthetic activity.
Mechanism of action: Levodropropizine acts antitussively via inhibition at the C-fiber level.
In vitro, it has been shown to be capable of inhibiting the release of neuropeptides from C-fibers. In cats in anesthesia, levodropropizine significantly reduces activation of C-fibers and prevents associated reflexes.
Levodropropizine acts on the bronchopulmonary system by inhibiting bronchospasm induced by histamine, serotonin or bradykinin.
In animals, levodropropizine does not induce attenuation of respiratory function, does not have significant cardiovascular effects, nor does it cause constipation.
In humans, levodropropizine does not inhibit respiratory function or mucociliary clearance.
The antitussive effect of levodropropizineis comparable to the effect of centrally acting medicinal products, but levodropropizine exhibits better tolerability, particularly with respect to central sedative effects.
Pharmacokinetics: In humans, levodropropizine is rapidly absorbed and rapidly distributed throughout the body after oral administration.
Biological half-life is approximately 1-2 hours. Excretion takes place via the primary urine. The preparation is eliminated in unchanged form and at the same time in the form of metabolites such as conjugated levodropropizine and free or conjugated p-hydroxyleodropropizine. Excretion of the product and its metabolites in urine accounts for approximately 35% of the administered dose within 48 hours.
Pharmacokinetic studies were conducted in rats, dogs and humans. It has been shown that absorption, distribution, metabolism and excretion are very similar in all three species, with a bioavailability exceeding 75% when administered per os.
Binding to blood plasma proteins in humans is insignificant (11-14%) and is comparable to the values observed in dogs and rats.
Tests in which the drug has been repeatedly administered indicate that treatment for eight days (3 times a day) does not affect the absorption and excretion characteristics of the product. The cumulative effect and metabolic autoinduction can therefore be ruled out.
Recovery of radioactivity after oral administration was 93%.
No significant changes in the pharmacokinetic properties of the product in children, elderly patients with moderate or severe renal insufficiency were observed.
The pharmacokinetics and bioavailability of the drop formulation are the same as the syrup dosage form.
