Drotaverin forte tablets 80 mg. №10

Description

Drotaverin tablets Storage
active substance: drotaverine;

1 tablet contains drotaverine hydrochloride 80 mg;

Drotaverin tablets excipients: lactose monohydrate; potato starch; povidone; magnesium stearate; croscarmellose sodium.

Drotaverin tablets Dosage form
Tablets.

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

Pharmacotherapeutic group
Remedies used in functional gastrointestinal disorders. Code ATX A0ZA D02.

Pharmacological properties

Pharmacodynamics.

Drotaverine, an isoquinoline derivative, has an antispasmodic effect directly on smooth muscle by inhibiting the action of the enzyme phosphodiesterase IV (PDE IV), which causes an increase in the concentration of cyclic adenosine monophosphate (cAMP) and by inactivation of light chain kinases.

In vitro, drotaverine inhibits the action of the enzyme PDE IV and does not inhibit the enzymes phosphodiesterase III (PDE III) and phosphodiesterase V (PDE V). PDE IV is of great functional importance for reducing the contractile activity of smooth muscle, so selective inhibitors of this enzyme may be useful in the treatment of diseases accompanied by hypermobility, as well as various diseases in which spasms of the gastrointestinal tract occur.

In myocardial and vascular smooth muscle cells, cAMP is mostly hydrolyzed by the PDE III isoenzyme, so drotaverine is an effective antispasmodic that has no significant cardiovascular side effects and a strong therapeutic effect on this system.

Drotaverine is effective in smooth muscle spasms of both nervous and muscular origin. Drotaverine acts on the smooth muscles of the gastrointestinal, biliary, genitourinary and vascular systems, regardless of the type of their autonomic innervation.

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

Drotaverine is stronger than papaverine, is more rapidly and completely absorbed, and is less bound to serum proteins. The advantage of drotaverine is also that, unlike papaverine, after its parenteral administration there is no such side effect as respiratory stimulation.

Pharmacokinetics.

Drotaverine is rapidly and completely absorbed after oral administration. It is highly (95-98%) bound to plasma albumin, gamma and beta globulins. The maximum concentration in the blood is reached within 45-60 minutes after oral administration. 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 eliminated from the body, approximately 50% is excreted in the urine and approximately 30% – in the feces. Drotaverine is mainly excreted in the form of metabolites, in unchanged form in the urine is not detected.

Indication
For therapeutic purposes in:

smooth muscle spasms 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 in:

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

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