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

Myotropic antispasmodic, isoquinoline derivative. By chemical structure and pharmacological properties close to papaverine; but has a stronger and longer action. Reduces the intake of calcium ions (Ca²⁺) in smooth muscle cells (inhibits phosphodiesterase (PDE), leads to the accumulation of intracellular cyclic adenosine monophosphate (cAMP)) and as a consequence to the inactivation of the light chain of myosin kinase,resulting in a relaxation of smooth muscles.

Reduces the tone of the smooth muscles of internal organs and intestinal motility, dilates the blood vessels. Does not affect the autonomic nervous system, does not penetrate the central nervous system (CNS). The presence of a direct effect on smooth muscles can be used as an antispasmodic in cases where drugs are contraindicated. (LS) from the group of m-holinoblokatorov (zakratougolnaya, glaucoma, prostatic hypertrophy).

Pharmacokinetics:

Suction: when taken orally, absorption is high; the half-absorption period is 12 min. Bioavailability is 100%. Time to reach the maximum concentration of the drug in the blood plasma (Tcmah) -2 hours.

Distribution: communication with plasma proteins - 95-98%, mainly with albumin, gamma and beta globulins, as well as lipoproteins, high density (HDL)., evenly distributed in tissues, penetrates smooth muscle cells. Does not penetrate the blood-brain barrier (BBB). Drotaverine and / or its metabolites can penetrate insignificantly through the placental barrier.

Metabolism: the half-life (T1 / 2) is 8-10 hours.Almost completely metabolized in the liver by O-de-ethylation. Metabolites are rapidly conjugated with glucuronic acid. The main metabolite is 4'-desethyltraderin, the other metabolites are 6-deethyldrothaverin and 4'-deethyldrothaveraldin.

Excretion: for 72 hours almost completely eliminated from the body. It is mainly excreted by the kidneys (mainly in the form of metabolites) and to a lesser extent - with bile. Unaltered drotaverine in the urine is not found.

Indications:

Spasm of smooth muscles in diseases of the 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 the 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. In carrying out some instrumental research; in t.ch. cholecystography.

Contraindications:

Hypersensitivity to the drug components, expressed by hepatic, renal, cardiac, insufficiency, atrioventricular block II-III degree, cardiogenic shock, arterial hypotension, lactation, children under 6 years.

In connection with the presence of lactose monohydrate in the formulation, its administration is contraindicated for patients suffering from lactase deficiency, galactosemia or the syndrome of impaired glucose / galactose absorption.

Carefully:Arterial hypotension, severe coronary atherosclerosis, arteries, prostatic hyperplasia, closed angle glaucoma, gestational period.

Pregnancy and lactation:See the sections "Contraindications" and "With caution".

Dosing and Administration:

The dosage regimen is individual and is prescribed by the doctor depending on the patient's condition and the clinical picture of the disease.

Inside, adults and children over 12 years - 40-80 mg (1-2 tablets) 2-3 times a day. Children aged 6 to 12 years - 40 mg (1 tablet) 1-2 times a day.

Side effects:

Classification of the incidence of adverse events (WHO):

very often> 1/10

often from> 1/100 to <1/10

infrequently from> 1/1000 to <1/100

rarely from> 1/10000 to <1/1000

very rarely from <1/10000, including individual messages.

Allergic reactions: infrequently - angioedema, urticaria, rash, itching.

From the side of the central nervous system: infrequently - headache, dizziness, insomnia.

From the digestive system: infrequently - nausea, constipation.

From the cardiovascular system: infrequently - tachycardia, lowering blood pressure.

If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:

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

Treatment: discontinuation of the drug, the patient should be under close medical supervision and receive symptomatic and supportive treatment. It is recommended to induce vomiting and / or rinse the stomach. There is no specific antidote.

Interaction:

With simultaneous application drotaverine can weaken the antiparkinsonian effect of levodopa (increased rigidity and tremor).

Strengthens the spasmolytic effect of papaverine, bendazole and other antispasmodics (incl.m-holinoblokatorov), arterial hypotension caused by tricyclic antidepressants, quinidine and pocaineamide.

Reduces the spasmogenic activity of morphine.

Phenobarbital increases the severity of spasmolytic action of drotaverine.

Special instructions:

In the treatment of gastric ulcer and duodenal ulcer are used in combination with other antiulcer drugs.

Tablets contain lactose monohydrate. This can cause gastrointestinal complaints of persons suffering from intolerance to lactose.

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

When administered orally in therapeutic doses drotaverine does not affect the ability to drive and perform work requiring increased attention. If there are any side effects, the question of driving and working on machines requires individual consideration.

Form release / dosage:Tablets of 40 mg.

Packaging:

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

Storage conditions:

In a dry place protected from light.

Keep out of the reach of children.

Shelf life:

3 years.

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

Terms of leave from pharmacies:Without recipe

Registration number:LS-002099

Date of registration:26.04.2012

The owner of the registration certificate:MOSCOW ENDOCRINE FACTORY, FSUE MOSCOW ENDOCRINE FACTORY, FSUE Russia

Manufacturer: & nbsp

MOSCOW ENDOCRINE FACTORY, FSUE Russia

Information update date: & nbsp29.11.2015

Illustrated instructions

Instructions

Drotaverine (Drotaverine)