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

Excipients: sodium disulfite - 1 mg, sodium acetate trihydrate - 6.8 mg, acetic acid 99.8% - 0.0196 ml, ethanol 96.3% - 65.9 mg, water for injection - up to 1.0 ml.

Description:Transparent liquid from yellow to yellow with a greenish shade 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-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⁺ -kalmodulin complex, resulting in Inactivated form of KLMC supports muscular relaxation. cAMP, in addition, 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 of PDE-4 is noted in the bile and urinary tract, uterus, gastrointestinal tract. 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:

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.

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

As an auxiliary therapy (when the form of tablets can not be used): with spasms of smooth muscles of the gastrointestinal tract (peptic ulcer of stomach and duodenum, gastritis, spasms of cardia and pylorus, enteritis, colitis, spastic colitis with constipation, irritable bowel syndrome with meteorism) with gynecological diseases: dysmenorrhea.

In carrying out some instrumental studies, including cholecystography.

Contraindications:

Hypersensitivity to drotaverine or to any of the components of the drug. Severe hepatic or renal insufficiency. Severe chronic heart failure. AV- blockade II-III degree. Lactation period, childbirth period, children's age.

Carefully:

The drug is used with caution in the expressed atherosclerosis of the coronary arteries, prostate adenoma, glaucoma, arterial hypotension, 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. Due to the lack of necessary clinical data drotaverine it is not recommended to appoint during breastfeeding. If you need to use the drug during lactation, you must stop breastfeeding.

Dosing and Administration:

Intramuscularly or subcutaneously - 2-4 ml (40-80 mg) 1-3 times a day. The course of treatment is 1-2 weeks or more. If necessary, prolonged treatment is transferred to taking the drug inside.

In cases where a rapid effect is needed, 2-4 ml of the drug in 10-20 ml of a 0.9% solution of sodium chloride or 5 % solution of dextrose.

Do not mix in one syringe with a solution of aminophylline.

Side effects:

The incidence of side effects is given in accordance with the classification of the World Health Organization: Often - not less than 10%; often - not less than 1% and less than 10%; infrequently - not less than 0.1% and less than 1%; rarely - not less than 0,01% and less than 0,1%; rarely - less than 0.01%, including isolated cases.

From the side of the cardiovascular system: infrequently - palpitation, arrhythmia, arterial hypotension;

From the digestive system: infrequently - nausea, vomiting, constipation;

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

From the immune system: rarely - angioedema, urticaria; frequency unknown - anaphylactic shock;

Local reactions: rarely - reactions at the site of administration;

Other: rarely - a feeling of heat, sweating, the development of allergic dermatitis, with intravenous injection - collapse.

Overdose:

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

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

Treatment: symptomatic.

Interaction:

With simultaneous application drotaverine can reduce the antiparkinsonian effect of levodopa (increased rigidity and tremor). Enhances the antispasmodic effect of papaverine, bendazole and other antispasmodics, including m-holinoblokatory. Reduces the spasmogenic activity of morphine. Phenobarbital enhances the spasmolytic effect of drotaverine. Increases the risk of arterial hypotension caused by tricyclic antidepressants, quinidine and procainamide.

Special instructions:

When administered intravenously, the patient should be in a horizontal position (risk of collapse).

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

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 (within 1 hour after parenteral, especially intravenous administration).

Form release / dosage:

A solution for intravenous and intramuscular administration of 20 mg / ml.

Packaging:

2 ml per ampoule of glass.

For 10 ampoules together with a knife for opening ampoules and instructions for medical use are placed in a box of cardboard.

10 ampoules are placed in a blister pack. 1 blister pack together with a knife for opening ampoules and instructions for medical use are placed in a pack of cardboard.

For 10 ampoules together with a knife for opening ampoules and instructions for medical use are placed in a pack with a cardboard insert for fixing ampoules from cardboard.

In case of using ampoules with a break ring or a notch and a break point, the insertion of the knife for opening ampoules is not provided.

Storage conditions:

In the dark place at a temperature of 15 to 25 ° C.

Keep out of the reach of children.

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

Terms of leave from pharmacies:On prescription

Registration number:LP-002590

Date of registration:20.08.2014

The owner of the registration certificate:BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus

Manufacturer: & nbsp

BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus

Information update date: & nbsp29.11.2015

Illustrated instructions

Instructions

Drotaverine (Drotaverine)