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

Excipients: sodium disulfite (sodium metasulfite) - 0.001 g; ethyl alcohol 95% - 0.069 g; sodium sulfite anhydrous - 0.0002 g; disodium edetate dihydrate 0.0001 g; benzethonium chloride 0.0001 g; citric acid monohydrate - 0.000825 g; sodium citrate pentasecylhydrate 0.00165 g; water for injection - up to 1 ml.

Description:Transparent or slightly opalescent liquid from light yellow to intensely yellow or from greenish-yellow to intensely yellow with a green tinge.

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. Phosphodiesterase hydrolyses cyclic adenosine monophosphate. Inhibition of phosphodiesterase leads to an increase in the concentration of cyclic adenosine monophosphate, which activates cyclic adenosine monophosphate-dependent phosphorylation of myosin light chain kinase (CLCM). Phosphorylation of myosin light chain kinase (CMLC) leads to a decrease in its affinity for the Calcademulinum complex, resulting in inactivated form of lung kinase Myosin chains (KLMC) support muscular relaxation. Cyclic adenosine monophosphate, in addition, affects the cytosolic concentration of calcium ions by stimulating the transport of calcium ions into the extracellular space and the sarcoplasmic reticulum.

In a process in an artificial environment drotaverine 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.Hydrolysis of cyclic adenosine monophosphate in the myocardium and smooth muscles of blood vessels is mainly due to PDE-3, therefore drotaverine less affects the cardiovascular system.

Drotaverine is effective in spasms of smooth muscles of both neurogenic and muscular origin.

Pharmacokinetics:

Quickly and well absorbed in the gastrointestinal tract. Absorption - 100%. However, 65% of the accepted dose (the "first pass" effect through the liver) enters the systemic circulation. Time to reach the maximum concentration of the drug in the plasma - 45-60 minutes.

The connection with plasma proteins is 95-97%, mainly with albumin, gamma and beta-globulin, as well as high-density lipoproteins. Evenly distributed on the tissues, penetrates into the smooth muscle cells. Does not penetrate the blood-brain barrier. Drotaverine 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, the other metabolites are 6-desethyltraderin and 4'-deethyldrothaveraldine.

The half-life of the preparation is 8-10 hours. For 72 hours it is almost completely removed from the body, more than 50% by the 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 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: gastric 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.

In carrying out some instrumental research, incl. cholecystography.

Contraindications:

Hypersensitivity, marked hepatic and renal insufficiency, severe chronic heart failure, lactation period; Children under 18 years of age (for a dosage of 80 mg), hypersensitivity to sulfites.

Carefully:Arterial hypotension due to the risk of collapse, pregnancy.

Pregnancy and lactation:

Drotaverin does not have teratogenic and embryotoxic effects, however its use in pregnancy is recommended only after a careful weighing of the benefit benefit ratio.

Due to the lack of necessary clinical data Drotaverine it is not recommended to appoint during breastfeeding.

Dosing and Administration:

Adults intramuscularly or subcutaneously - 40-240 mg per 1-3 hours per day;

To remove acute renal and gallstone colic - intravenously slowly, 40-80 mg;

Other abdominal spastic pains: 40-80 mg intramuscularly or subcutaneously, if necessary up to 3 times a day (no more);

Spasm of cardia or esophagus: 80 mg intramuscularly.

Side effects:

Frequency: very often - more than 1/10, often - more than 1/100 and less than 1/10, infrequently - more than 1/1000 and less than 1/100, rarely - more than 1/10000 and less than 1/1000, very rarely - more 1/10000, including individual messages.

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

From the cardiovascular system: infrequently - tachycardia, lowering of arterial pressure, collapse (with intravenous administration).

From the digestive system: infrequently - nausea, constipation.

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

Overdose:

In high doses, it breaks AV- Conductivity, reduces the excitability of the heart muscle, can cause heart failure and paralysis of the respiratory center.

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:

The administration of the drug to patients with arterial hypotension is performed in the "lying" position because of the danger of development of collapse.

The solution contains sodium sulfite, which can cause allergic reactions, including anaphylactic shock and bronchospasm, in sensitive individuals (especially in persons with bronchial asthma or allergic reactions in the anamnesis).

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

During the treatment period, it is necessary to refrain from driving and other potentially hazardous activities,requiring an increased concentration of attention and speed of psychomotor reactions (within 1 h after parenteral, especially intravenous administration).

Form release / dosage:

Solution for injection 20 mg / ml.

Packaging:

2 ml of preparation in ampoules of light-protective glass.

5 ampoules are placed in a contiguous cell pack of a polyvinylchloride film without coating.

1 or 2 contour mesh packages are placed in a pack of cardboard for consumer containers.

5.10 ampoules are placed in a pack of cardboard for consumer containers with partitions or grilles, or a paperboard separator for consumer packaging or sack paper.

10 ampoules are placed in a box of cardboard for consumer containers and with a loose leaf of paper paste. The box is pasted with a label-parcel of paper label or coated.

Each instruction pack or box is supplied with instructions for use, an ampoule knife or ampoule scarifier.

When using ampoules with incisions, break rings or break points, the ampoule knife or the ampoule scapegrator is not inserted.

Packs and boxes are placed in a group package.

Storage conditions:

In a place protected from light and inaccessible to children at a temperature of no higher than 25 ° C.Do not freeze.

Shelf life:

2 years.

Do not use the product after the expiration date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-001642

Date of registration:29.12.2011

The owner of the registration certificate:Promomed Rus, Open CompanyPromomed Rus, Open Company Russia

Manufacturer: & nbsp

BIOCHEMIST, OJSC Russia

Information update date: & nbsp29.11.2015

Illustrated instructions

Instructions

Drotaverine (Drotaverine)