Drotaverin - instructions for use, dose, side effects, contraindications

Excipients: milk sugar (lactose monohydrate) - 58.4 mg; potato starch - 32.5 mg; calcium stearate - 1.4 mg, talc - 1.4 mg, polyvinylpyrrolidone (povidone) - 5.9 mg.

Description:Tablets of round shape yellow or yellow with a greenish tint of color.

Pharmacotherapeutic group:Spasmolytic agent

ATX: & nbsp

A.03.A.D.02 Drotaverine

Pharmacodynamics:

Drotaverin is a derivative of isoquinoline, it is close in chemical structure and pharmacological properties to papaverine, but it has a more pronounced and prolonged effect. Drotaverine has a pronounced antispasmodic effect on smooth muscles due to inhibition of phosphodiesterase (PDE-4). PDE-4 hydrolyses cyclic adenosine monophosphate (cAMP) to adenosine monophosphate (AMP).Inhibition of PDE-4 leads to an increase in the concentration of cAMP, which activates cAMP-dependent phosphorylation of myosin light chain kinase (CMLC). Phosphorylation of CMLC leads to a decrease in its affinity for the Ca2 + - calmodulin complex, as a result of which the inactivated form of CLCM supports muscular relaxation of cAMP, in addition it affects the cytosolic concentration of Ca2 +, by stimulating the Ca2 + transport into the extracellular space and the sarcoplasmic reticulum.

In vitro drotaverin inhibits the isoenzyme PDE-4 without inhibiting the isoenzymes PDE-3 and PDE-5, therefore the effectiveness of drotaverin depends on the activity of PDE-4, the content of which in different tissues is different. High content of PDE-4 is noted in the bile and urinary tract, uterus, gastrointestinal tract (GIT). The hydrolysis of cAMP in the myocardium and smooth muscles of blood vessels is mainly due to PDE-3, therefore drotaverine less affects the cardiovascular system. Drotaverine Effective in spasms of smooth muscles, both neurogenic and muscular.

Pharmacokinetics:

When taken orally, absorption is high, the half-absorption period is 12 min.Bioavailability is 100%. Evenly distributed to tissues, penetrates into smooth muscle cells. Time to reach the maximum concentration in the blood (TCmoh) -2 hours. The connection with plasma proteins is 95-98%. It is mainly excreted by the kidneys, to a lesser extent - with bile. Does not penetrate the blood-brain barrier (BBB).

Indications:

Spasm of smooth muscles in diseases of the bile ducts: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, inflammation of the papilla of the duodenum.

Spasm of smooth muscles in diseases of the urinary tract: nephrourolythiasis, urethrolithiasis, pyelitis, cystitis, bladder spasm.

As an auxiliary therapy: with spasms of smooth muscles of the gastrointestinal tract: stomach ulcer and duodenal ulcer, gastritis, cardia and pyloric spasm, enteritis, colitis, spastic colitis with constipation and irritable bowel syndrome with flatulence; tensor headache; Algodismenorea, threatening miscarriage, threatening premature birth; spasm of the throat of the uterus during labor, prolonged opening of the throat, postnatal fights.

In carrying out some instrumental studies, including cholecystography.

Contraindications:

Hypersensitivity to the components of the drug, expressed by hepatic, renal, heart failure, atrioventricular blockade of 2-3 degrees, cardiogenic shock, arterial hypotension, lactase deficiency, lactose intolerance, glucose-galactose malabsorption, children under 6 years (solid indivisible dosage form).

Carefully:

Pronounced atherosclerosis of the coronary arteries, prostatic hyperplasia, angle-closure glaucoma, pregnancy and lactation.

Pregnancy and lactation:

Drotaverine does not have teratogenic and embryotoxic effects. However, the use of the drug is recommended only if the potential benefit to the mother exceeds the potential risk to the fetus.

Due to the lack of necessary clinical data drotaverine it is not recommended to use during lactation (breastfeeding).

Dosing and Administration:Inside, adults - 40-80 mg (1-2 tablets) 2-3 times a day. The maximum daily dose is 240 mg.
Children aged 6-12 years - 40 mg (1 tablet) per day.
Children aged 12-18 years 40 mg 2-3 times a day. The maximum daily dose is 200 mg.

Side effects:

Dizziness, palpitations, a feeling of heat, increased sweating, lowering blood pressure (BP), allergic skin reactions.

Overdose:

Symptoms: in high doses violates atrioventricular conduction, reduces the excitability of the heart muscle, can cause heart failure and respiratory center paralysis.

In order to facilitate atrioventricular blockade (AV-blocks) are used atropine and isoprenaline intravenously, to resume the rhythm of the heart - atropine or epinephrine intravenously with a temporary pacemaker, respiratory center paralysis is the artificial ventilation of the lungs.

Interaction:

With simultaneous application drotaverine mMay weaken the antiparkinsonian effect of levodopa.

Strengthens the effect of papaverine, bendazole and other antispasmodics (including M-holinoblokatorov), a decrease in blood pressure, caused by tricyclic antidepressants, quinidine and procainamide.

Phenobarbital increases the severity of spasmolytic action of drotaverine. Reduces the spasmogenic activity of morphine.

Special instructions:

In the treatment of gastric ulcer and duodenal ulcer are used in combination with other antiulcermedicinal preparations.

Effect on the ability to drive transp. cf. and fur:

During the treatment period it is necessary to refrain from driving motor vehicles and practicing other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Tablets of 40 mg.

Packaging:

10 tablets per contour cell pack.

By 20.30, 50 or 100 tablets in a jar of polymer materials.

Each bank or 2, 3, 5 or 10 contour cell packs of 10 tablets together with the instruction for use are placed in a pack.

A polymer-free can is supplied with a glue instruction for use and placed in a group package.

Storage conditions:

In dry, protected from light, out of the reach of children.

Shelf life:

2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LS-001332

Date of registration:22.07.2011

The owner of the registration certificate:PHARMACY 36.6, CJSC PHARMACY 36.6, CJSC Russia

Manufacturer: & nbsp

VEROPHARM SA Russia

Information update date: & nbsp04.01.2016

Illustrated instructions

Instructions

Drotaverine (Drotaverine)