Drotaverin forte tablets 80 mg. №20

Description

Drotaverin Composition
active substance: drotaverine;

1 tablet contains 80 mg drotaverine hydrochloride;

Drotaverin excipients:

lactose monohydrate, potato starch; povidone, magnesium stearate, croscarmellose sodium.

Drotaverin Dosage form
Pills.

Basic physical and chemical properties: tablets from light yellow to yellowish green color.

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

Pharmacodynamics
Drotaverine, an isoquinoline derivative, has an antispasmodic effect directly on smooth muscles by inhibiting the action of the enzyme phosphodiesterase IV (PDE IV), which leads to an increase in the concentration of cyclic adenosine monophosphate (cAMP) and, due to inactivation of myosin light chain kinase (CLM).

In vitro, drotaverine inhibits the action of the PDE IV enzyme and does not inhibit the isoenzymes of phosphodiesterase II (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 mainly by the isoenzyme PDE III, therefore drotaverine is an effective antispasmodic agent, does not have significant side effects from the cardiovascular system and has a strong therapeutic effect on this system.

Drotaverine is effective for smooth muscle spasms of both nervous and muscle origin. Drotaverine acts on the smooth muscles of the gastrointestinal, biliary, urogenital and vascular systems, regardless of the type of their autonomous innervation.

It enhances blood circulation in tissues due to its ability to dilate blood vessels.

The action of drotaverine is stronger than the action of papaverine, absorption is faster and more complete, it binds less to blood plasma proteins. The advantage of drotaverine is also the fact that, unlike papaverine, after its parenteral administration, there is no such side effect as breathing stimulation.

Pharmacokinetics
Drotaverine is rapidly and completely absorbed after oral administration. It binds to a high degree (95-98%) with plasma albumin, gamma and beta globulins. The maximum concentration in the blood is reached within 45-60 minutes after ingestion. After primary metabolism, 65% of the administered dose 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, about 50% is excreted in the urine, 30% in the feces. Basically, drotaverine is excreted in the form of metabolites, unchanged in the urine is not detected.

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 to any component of the drug. Severe hepatic, renal, or heart failure (small cardiac output syndrome). Lactase deficiency, galactosemia or glucose-galactose malabsorption syndrome.

Interaction with other medicinal products and other forms of interaction
Phosphodiesterase inhibitors such as papaverine reduce the antiparkinsonian effect of levodopa. The drug should be used with caution at the same time as levodopa, since the antiparkinsonian effect of the latter decreases, and the rigidity and tremor increase.