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

Description:Transparent or slightly opalescent liquid from light yellow to intensely yellow or from greenish-yellow to intensely yellow with a greenish 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-4 (PDE-4). PDE-4 hydrolyses cAMP to 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 Ca²⁺- calmodulin complex, as a result of which the inactivated form of CLCM supports muscular relaxation. cAMP, in addition it affects the cytosolic concentration of Ca²⁺, due to the stimulation of transport of Ca²⁺ in the extracellular space and 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 PDE-4 is noted in the biliary and urinary tract, uterus, gastrointestinal tract. Hydrolysis of cAMP in the myocardium and smooth muscle of blood vessels occurs, mainly way, with the help of PDE-3, therefore drotaverine less affects the cardiovascular system. Drotaverine Effective in spasms of smooth muscles as a neurogenic, and of a muscular origin.

Pharmacokinetics:

With parenteral administration, the drug appears after 2-4 minutes. The maximum effect occurs in 30 minutes. It is released from the connection with plasma proteins gradually, providing a lasting effect. Half-life is 2-4 hours. Metabolism is carried out in the liver, most of the metabolites are excreted by the kidneys.

Indications:

Spasms of smooth muscles associated with diseases of the biliary tract: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis.

Spasm of smooth musculature of the urinary tract: nephrolithiasis, urethrolithiasis, pyelitis, cystitis, bladder tenesmus.

As an auxiliary therapy (when the form of tablets can not be used): with spasms of smooth muscles of gastrointestinal origin: peptic ulcer of stomach and duodenum, gastritis, spasm of cardia and pylorus, enteritis, colitis.

With gynecological diseases: dysmenorrhea.

Contraindications:

Hypersensitivity to the active substance or to any of the excipients of the drug;

Hypersensitivity to sodium disulfite;

Severe hepatic or renal insufficiency;

Childhood;

Breastfeeding period;

Period of delivery.

Carefully:Use with caution in arterial hypotension, during pregnancy.

Pregnancy and lactation:Application in pregnancy is possible only in cases where the potential benefit to the mother exceeds the potential risk to the fetus.

Dosing and Administration:

Adults: The average daily dose is 40 - 240 mg of drotaverine hydrochloride (divided by 1 to 3 doses per day) by intramuscular injection; with acute colic (renal and cholelithiasis) 40 - 80 mg intravenously slowly (duration of administration is approximately 30 seconds).

Side effects:

Below are the side reactions with the frequency of their occurrence: 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 than 1/10000, including individual messages, an unknown frequency (according to the available data, the frequency can not be determined).

From the nervous system: rarely - headache, dizziness, insomnia.

From the side of the cardiovascular system: rarely - increased heart rate, lower blood pressure.

From the digestive system: rarely - nausea, constipation.

From the immune system: rarely - allergic reactions (angioedema, urticaria, rash, itching).

Unknown frequency: When using the drug, the development of anaphylactic shock with a fatal outcome and without a fatal outcome has been reported.

Local Reactions: rarely - reactions at the injection site.

Overdose:

In case of an overdose, dose-dependent side effects may be increased.

Treatment: symptomatic.

Interaction:Phosphodiesterase inhibitors like papaverine weaken the anti-Parkinsonian effect of levodopa; with simultaneous use with the drug levodopa possibly increased rigidity and tremor; drotaverine enhances the spasmolytic effect of papaverine, bendazole and other antispasmodics, including m-holinoblokatory; increases hypotension caused by tricyclic antidepressants, quinidine and procainamide; reduces the spasmogenic activity of morphine; phenobarbital enhances the spasmolytic effect of drotaverine.

Special instructions:

In the treatment of gastric ulcer and duodenal ulcer used in combination with other antiulcer drugs.When administered intravenously, the patient should be in a horizontal position (risk of collapse).

The drug contains disulfite, which can cause allergic reactions, including anaphylactic shock and bronchospasm in persons susceptible to sulfites, especially if there is an anamnesis of bronchial asthma and allergic diseases; In the case of hypersensitivity to disulfite, parenteral administration of the drug is contraindicated.

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 hazardous activities that require increased concentration and the speed of psychomotor reactions (within 1 hour after intravenous Introduction).

Form release / dosage:Solution for intravenous and intramuscular injection of 20 mg / ml in ampoules of 2 ml.

Packaging:5 ampoules of light-protective glass in a contour mesh box made of polyvinylchloride film and aluminum foil (or without foil). 1 or 2 contour mesh packages with a scarifier ampoule ceramic or knife for opening ampoules and instructions for use are placed in a pack of cardboard.When using ampoules with a break ring or break point, the knife or scarifier is not inserted.

Storage conditions:Store in a dark place at a temperature of 5 to 25 ° C. Keep out of the reach of children.

Shelf life:2 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-001487

Date of registration:08.02.2012

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

Manufacturer: & nbsp

BINNOFARM, CJSC Russia

GosMPS, FSUE Russia

"MEDICAL-TECHNOLOGICAL HOLDING" "MTX", CJSC " Russia

Information update date: & nbsp29.11.2015

Illustrated instructions

Instructions

Drotaverine (Drotaverine)