Myotropic antispasmodic. In chemical structure and pharmacological properties it is close to papaverine, but it has a stronger and longer lasting effect. Its action is stronger than that of papaverine, and absorption is faster and more complete, it binds less to plasma proteins.
Drotaverin is an isoquinoline derivative that has an antispasmodic effect on smooth muscle by suppressing the phosphodiesterase IV (PDE IV) enzyme without inhibiting the PDE III and PDE V isoenzymes. Inhibition of the phosphodiesterase IV enzyme leads to an increased concentration of cAMP, which inactivates the light chain MLC , which, in turn, leads to relaxation of smooth muscles.
The enzyme that hydrolyzes cAMP in smooth muscle cells of the myocardium and blood vessels is mainly an isoenzyme of PDE III, which explains that drotaverin is an effective antispasmodic agent without cardiovascular side effects and a pronounced effect on the cardiovascular system. The drug is effective for smooth muscle spasms caused by impaired nervous regulation and self-regulation of both nervous and muscular etiology. Regardless of the type of autonomic innervation, drotaverin acts on the smooth muscles located in the gastrointestinal, biliary, urogenital and vascular systems. Due to its vasodilating effect, it improves the blood circulation of tissues.
With oral administration, the drug is rapidly absorbed from the digestive tract. In small concentrations binds to albumin, α- and β-plasma globulins. The maximum concentration (Cmax) in serum upon oral administration is recorded at 45-60 minutes. The metabolism of the drug occurs in the liver. The half-life (T1/2) is 16-22 hours. For 72 hours, it is practically excreted from the body, about 50% with urine, 30% with feces. It is excreted mainly in the form of metabolites, unchanged in urine is not observed. Passes through the placenta.
Indications for use
– spasm of smooth muscles in diseases of the biliary system (cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis);
– spasm of smooth muscles of the urinary system (nephrolithiasis, urethrolithiasis, pyelitis, cystitis, tenesmus of the bladder);
As an aid:
– with spasms of the smooth muscles of the digestive tract (stomach ulcer and duodenal ulcer, gastritis, enteritis, colitis, spasm of the cardiac sphincter of the stomach and pylorospasm, irritable bowel syndrome, accompanied by flatulence);
– with tension headache;
– with gynecological diseases (aldismenorrhea), to reduce the increased tone of the uterus during pregnancy, with threatening abortion.
Dosage and administration
Inside, adults are prescribed 40-80 mg (1-2 tablets of 40 mg) 3 times a day.
For children under the age of 6 years, the drug is prescribed in a single dose of 10-20 mg, the maximum daily dose is 120 mg, at the age of 6 to 12 years, 20 mg, the maximum daily dose is 200 mg. Multiplicity of appointment 1-2 times a day.
The duration of use is determined by the doctor.
From the digestive system: (> 1/10000, <1/1000) – nausea, constipation;
From the side of the nervous system: (> 1/10000, <1/1000) – headache, dizziness, insomnia;
From the cardiovascular system: (> 1/10000, <1/1000) – accelerated heartbeat, arterial hypotension, arrhythmia, sensation of heat;
From the respiratory system: bronchospasm, swelling of the nasal mucosa;
Very rarely there is allergic dermatosis, excessive sweating, Quincke’s edema.
If any adverse reactions occur, consult a doctor.
Hypersensitivity to drotaverine or to any other component of the drug. Severe violations of the liver, kidneys and heart failure, atrioventicular block II-III degree, arterial hypotension, glaucoma, lactose deficiency, galactosemia or glucose-galactose malabsorption syndrome. Children’s age up to 1 year.
The simultaneous administration of drotaverine hydrochloride with morphine reduces the spasmogenic activity of the latter, with levodopa – it reduces its antiparkinsonian effect, increases rigidity, tremor. The drug enhances the effect of antispasmodics (including m-anticholinergics); enhances arterial hypotension caused by tricyclic antidepressants, quinidine, procainamide. Concomitant use with phenobarbital enhances the antispasmodic effect of drotaverine.
If it is necessary to use the drug with other medicines, it is necessary to consult a doctor.
With caution, the drug is prescribed during pregnancy and lactation, as well as in patients with severe coronary arteriosclerosis and low blood pressure.
Due to the fact that the drug acts directly on smooth muscle, it can be used as an antispasmodic in cases when medicines from the group of anticholinergics are contraindicated (glaucoma, prostatic hypertrophy, etc.)
In case of side effects, it is necessary to cancel the drug.
The use of drotaverine during pregnancy does not lead to teratogenic and embryotoxic effects. However, caution is required when prescribing a drug during pregnancy.
Due to the lack of necessary clinical data during lactation, it is not recommended to prescribe.
If patients experience dizziness after using the drug, they should avoid potentially dangerous activities, such as driving a car and performing work that requires increased attention.
The drug should be stored out of the reach of children and do not use the drug after the expiration date indicated on the package.
Symptoms: side effects of the drug are amplified, atrioventricular block, heart failure, respiratory center paralysis are possible.
Treatment: induce vomiting and rinse the stomach. The use of laxatives. The patient should be under medical supervision. Therapy is symptomatic.
Tablets, 40 mg in blister packs.
In a dry, dark place at a temperature of no higher than 25ºС.
Pharmacy sales terms