Pharmacodynamics. Drotaverine - an isoquinoline derivative with an antispasmodic effect on smooth muscles by inhibiting the action of the enzyme pde-4 - increases the concentration of camp and, due to inactivation of myosin light chain kinase, leads to relaxation of smooth muscles.
In vitro, drotaverine inhibits the action of PDE-4 and inhibits the isoenzymes PDE-3 and -5. PDE-4 is of great functional importance for reducing the contractile activity of smooth muscles, therefore, selective inhibitors of this enzyme can be effective for the treatment of disorders accompanied by hyperperistalsis, as well as various diseases in which spasms of the gastrointestinal tract occur.
In the cells of smooth muscles of the myocardium and blood vessels, cAMP is hydrolyzed mainly by the isoenzyme PDE-3, therefore drotaverine does not have significant side effects on the part of the cardiovascular system and a strong therapeutic effect on the circulatory system.
Drotaverine is effective for smooth muscle spasms of both nervous and muscle origin. Regardless of the type of autonomic innervation, drotaverine acts on the smooth muscles of the gastrointestinal tract, biliary, urogenital and vascular systems.
Drotaverine enhances blood circulation in tissues due to vasodilation.
The action of drotaverine is more pronounced than the action of papaverine, absorption is faster and more complete, it binds less to blood plasma proteins. Unlike papaverine, drotaverine after parenteral administration does not cause such side effects as breathing stimulation.
Pharmacokinetics. Drotaverine is rapidly and completely absorbed after oral administration. In many ways (95–98%) it binds to blood plasma proteins, especially albumin, gamma and beta globulins. Cmax is achieved within 45-60 minutes after oral administration. Approximately 65% of the dose enters the bloodstream unchanged.
Within 72 hours, drotaverine is almost completely excreted from the body: more than 50% - with urine, 30% - with feces. It is mainly excreted in the form of metabolites, unchanged in the urine is not detected.
Treatment for:
As an adjuvant for:
Adults: the average daily dose is 120-240 mg in 2-3 divided doses.
Children over 12 years of age: the maximum daily dose is 160 mg (½ tablet 2–4 times a day).
The duration of treatment is determined by the doctor individually.
Hypersensitivity to the components of the preparation. severe hepatic, renal, or heart failure (small cardiac output syndrome). hereditary lactase deficiency, galactosemia or glucose-galactose malabsorption syndrome. age up to 12 years. av-blockade ii and iii degrees. lactation period.
Side effects
Which were observed during clinical studies and, possibly, were caused by drotaverine, distributed by organ systems and frequency of occurrence: very often (1/10), often (1/100, 1/10), infrequently (1/1000, 1/100 ), rarely (1/10 000, 1/1000), very rarely (1/10 000).
From the immune system. Rarely: allergic reactions, including angioedema, urticaria, rash, itching, skin flushing, fever, weakness.
On the part of the cardiovascular system. Rarely: tachycardia, arterial hypotension.
From the nervous system. Rarely: headache, dizziness, insomnia.
From the gastrointestinal tract. Rarely: nausea, constipation, vomiting.
Use with extreme caution in case of arterial hypotension. do not use for the treatment of patients with lactase deficiency, galactosemia or glucose-galactose malabsorption syndrome.
Use during pregnancy and lactation. Due to the lack of clinical data, it is possible to prescribe to pregnant women only if the benefits of use outweigh the risks. The active substance crosses the placenta. The preparation should not be used during childbirth due to the increased risk of bleeding in the postpartum period.
Since drotaverine passes into breast milk, the use of the preparation is not recommended during breastfeeding.
Children. The use of the preparation in children under 12 years of age is contraindicated.
The ability to influence the reaction rate when driving or operating other mechanisms. In therapeutic doses for oral administration, drotaverine does not affect the reaction rate when driving or operating other mechanisms. The patient should be informed that in case of dizziness, avoid driving or working with mechanisms that require increased attention.
It should be used with caution simultaneously with levodopa, since the severity of the antiparkinsonian effect of the latter decreases, and the rigidity and tremor increase.
Symptoms: With a significant overdose of drotaverine, studies have noted violations of the heart rhythm and conduction, including complete blockade of the bundle of the bundle and cardiac arrest, which can be fatal.
In case of a significant overdose, the patient should be under close medical supervision. It is recommended to induce vomiting and / or gastric lavage, symptomatic and supportive treatment.
At a temperature not higher than 30 ° C.
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