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

Myotropic antispasmodic, isoquinoline derivative. Inhibits phosphodiesterasePDE-4, which leads to the accumulation of intracellular cyclic adenosine monophosphate (cAMP) and, as a consequence, to the inactivation of myosin light chain kinase, resulting in relaxation of smooth muscle.

Regardless of the type of vegetative innervation, drotaverine It acts on smooth muscles in the gastrointestinal tract, bile ducts, genitourinary and cardiovascular systems. In the myocardium and vessels, the enzyme that hydrolyses cAMP is PDE-3, which explains the absence of serious side effects from the cardiovascular system and the unexplained therapeutic effect on the cardiovascular system.

Pharmacokinetics:

Quickly and well absorbed in the gastrointestinal tract. Absorption - 100 %. However, the systemic blood flow is 65 % the accepted dose (the effect of "first passage" through the liver). The time to reach the maximum concentration is 45-60 minutes.

The connection with plasma proteins is 95-97%, mainly with albumin, gamma and beta-globulins, as well as high-density lipoproteins. Evenly distributed on the tissues, penetrates into the smooth muscle cells. Does not penetrate the blood-brain barrier. Drotaverin and / or its metabolites can penetrate insignificantly through the placental barrier. Almost completely metabolized in the liver by O-de-ethylation. Metabolites are rapidly conjugated with glucuronic acid. The main metabolite is 4-desethyltraderin,other metabolites are 6-deethyldroverine and 4-desethylditaveraldin.

Half-life is 8-10 hours. For 72 hours it is almost completely eliminated from the body, more than 50 % kidneys (mainly in the form of metabolites) and about 30 % intestines. Unchanged drotaverine in the urine is not found.

Indications:

Spasm of smooth muscles in diseases of biliary tract: 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: gastric ulcer and duodenal ulcer, gastritis, cardia and pyloric spasm, enteritis, colitis, spastic colitis with constipation and irritable bowel syndrome with flatulence; tensor headache; dysmenorrhea, threatening miscarriage, threatening premature birth, prolonged opening of the throat of the uterus, postnatal fights. In carrying out some instrumental studies, including cholecystography.

Contraindications:

- hypersensitivity;

- marked hepatic and renal insufficiency;

- severe chronic heart failure;

- lactose intolerance, lactase deficiency or glucose-galactose malabsorption;

- children's age up to 3 years.

Carefully:Be wary of patients with arterial hypotension, prostatic hypertrophy, closed-angle glaucoma.

Pregnancy and lactation:

During pregnancy, use with caution (on the advice of a doctor); during the lactation drug is contraindicated.

Dosing and Administration:

Drotaverin is taken internally.

Adults on 40-80 mg (1-2 tablets) 3 times a day.

Children aged 3-6 years - 40-120 mg (1-3 tablets) in 2-3 divided doses, the maximum daily dose - 120 mg; 6-18 years - 80-200 mg (2-5 tablets) in 2-5 receptions; the maximum daily dose is 240 mg.

Side effects:

From the cardiovascular system: palpitation, tachycardia, lowering blood pressure.

From the central nervous system: dizziness, headache, insomnia.

From the gastrointestinal tract: nausea, constipation.

Allergic reactions: angioedema, urticaria, rash, itching.

Overdose:

Symptoms of overdose: weakness, lowering blood pressure.

Treatment: symptomatic (maintenance of arterial pressure).

Interaction:

Relieves the antiparkinsonian effect of levodopa (increased rigidity and tremor).

Strengthens the spasmolytic effect of papaverine, bendazole and other antispasmodics, including m-holinoblokatory.

Reduces the spasmogenic activity of morphine.

Phenobarbital enhances the spasmolytic effect of drotaverine.

Special instructions:

When treating gastric ulcer and duodenal ulcer are used in combination with other antiulcer drugs.

Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased concentration and speed of psychomotor reactions, with the appearance of dizziness

Form release / dosage:Tablets of 40 mg.

Packaging:

For 10 tablets in a contoured cell pack of a polyvinyl chloride film and aluminum foil printed lacquered or paper with a polymer coating.

1, 2, 5 or 10 contour mesh packages together with the instruction for use are placed in a pack of cardboard for consumer containers.

Contoured packages, together with an equal number of instructions for use, are placed in a group package.

Storage conditions:

In a dry place protected from light.

In a place inaccessible to children.

Shelf life:

3 years.

Do not use the product after the expiry date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:P N001563 / 01-2002

Date of registration:16.03.2009

The owner of the registration certificate:MEDISORB, CJSC MEDISORB, CJSC Russia

Manufacturer: & nbsp

MEDISORB, CJSC Russia

Information update date: & nbsp16.06.2016

Illustrated instructions

Instructions

Drotaverin MS (Drotaverine MS)