Drotaverin tablets 0.04 g. №30

Description

Drotaverin №30 Composition
active substance: drotaverine;

1 tablet contains 40 mg drotaverine hydrochloride;

Drotaverin №30 excipients:

lactose monohydrate, corn starch, microcrystalline cellulose, colloidal anhydrous silicon dioxide, magnesium stearate.

Drotaverin №30 Dosage form
Pills.

Basic physical and chemical properties: tablets of light yellow or dark yellow color interspersed, flat-cylindrical, with a chamfer and a line.

Pharmacotherapeutic group
Drugs used for functional gastrointestinal disorders. ATX code A03A D02.

Pharmacodynamics
Drotaverin-Darnitsa is an isoquinoline derivative that has an antispasmodic effect on smooth muscles by inhibiting the action of the enzyme phosphodiesterase IV (PDE IV), which causes an increase in the concentration of cAMP and, due to inactivation of the light chain of myosin kinase (MLCK), leads to relaxation of smooth muscles.

In vitro, drotaverine inhibits the action of the PDE IV enzyme and inhibits the isoenzymes of phosphodiesterase III (PDE III) and phosphodiesterase V (PDE V). PDE IV is of great functional importance for reducing the contractile activity of smooth muscles, therefore, selective inhibitors of this enzyme can be useful for the treatment of diseases that are accompanied by hypermobility, as well as various diseases during which spasms of the gastrointestinal tract occur.

In the cells of smooth muscles of the myocardium and blood vessels, cAMP is hydrolyzed to a greater extent by the isoenzyme PDE III, therefore drotaverine is an effective antispasmodic agent that does not have significant side effects on the part of the cardiovascular system and a strong therapeutic effect on this system.

Drotaverin-Darnitsa is effective for smooth muscle spasms of both nervous and muscular origin. Drotaverin-Darnitsa acts on the smooth muscles of the gastrointestinal, biliary, urogenital and vascular systems, regardless of the type of their autonomous innervation. The drug increases blood circulation in tissues due to its ability to dilate blood vessels.

The action of drotaverine is stronger than that of papaverine, absorption is faster and more complete, it binds less to blood plasma proteins. The advantage of drotaverine is that, in contrast to papaverine, after its parenteral administration, no such side effect as breathing stimulation was noted.

Pharmacokinetics
Drotaverin-Darnitsa is rapidly and completely absorbed after oral administration. To a high degree (95-98%) it binds to blood plasma proteins, especially albumin, gamma and beta globulins. The maximum concentration in the blood after oral administration is reached after 45-60 minutes. After primary metabolism, 65% of the dose taken enters the bloodstream unchanged. Metabolized in the liver. The half-life is 8-10 hours. Within 72 hours, drotaverine is almost completely excreted from the body, more than 50% is excreted in the urine and approximately 30% in the feces. Basically, drotaverine is excreted in the form of metabolites; it is not detected in the unchanged form in the urine.

Indications
For therapeutic purposes with:

spasms of smooth muscles associated with diseases of the biliary tract: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis;
spasms of smooth muscles in diseases of the urinary tract: nephrolithiasis, urethrolithiasis, pyelitis, cystitis, tenesmus of the bladder.
As an adjunct treatment for:

spasms of smooth muscles of the gastrointestinal tract: gastric ulcer and duodenal ulcer, gastritis, cardio and / or pylorospasm, enteritis, colitis, spastic colitis with constipation and irritable bowel syndrome accompanied by flatulence;
tension headaches;
gynecological diseases (dysmenorrhea).

Contraindications
Hypersensitivity to drotaverine or other components of the drug; severe hepatic, renal, or heart failure (small cardiac output syndrome).