Drotaverin ampoules 2% 2 ml. №5

Description

Drotaverin Storage
active substance: drotaverine;

1 ml of solution contains drotaverine hydrochloride 20 mg;

Drotaverin Excipients: ethanol (96%), sodium metabisulphite (E 223), water for injections.

Drotaverin Dosage form
Solution for injection.

Basic physical and chemical properties: transparent greenish-yellow or yellow liquid.

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

Pharmacological properties

Pharmacodynamics.

Drotaverine, an isoquinoline derivative, has an antispasmodic effect on smooth muscle by inhibiting the action of the enzyme phosphodiesterase IV (PDE IV), which causes an increase in cAMP concentration and, by inactivating the myosin kinase light chain (MLCK), leads to relaxation of muscles.

In vitro, drotaverine inhibits the action of the enzyme PDE IV and inhibits 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, urogenital and vascular systems, regardless of the type of their autonomic innervation. The drug enhances blood circulation in the tissues due to its ability to dilate blood vessels.

The effect of drotaverine is stronger than the effect of papaverine, absorption is faster and more complete, it is less bound to plasma 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, with greater (95-98%) binding to plasma proteins, especially albumin, gamma and beta globulins. After primary metabolism, 65% of the dose enters the bloodstream unchanged. Metabolized in the liver. The half-life is 8-10 hours. In 72 hours, drotaverine is almost completely excreted from the body, more than 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
Smooth muscle spasms associated with biliary tract diseases such as cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis;

Smooth muscle spasms in diseases of the urinary tract: nephrolithiasis, urethrolithiasis, pyelitis, cystitis, tenesmus of the bladder.

As adjunctive treatment (when the use of the drug in the form of tablets is not possible) in:

with spasms of smooth muscles of the gastrointestinal tract: peptic ulcer of the stomach and duodenum, gastritis, cardio- and / or pylorospasm, enteritis, colitis;
in gynecological diseases (dysmenorrhea).

Contraindication
Hypersensitivity to drotaverine or to other components of the drug (especially to sodium metabisulfite). Hypersensitivity to sodium disulfite. Severe hepatic, renal or heart failure (low cardiac output syndrome).