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

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 cyclic adenosine monophosphate (cAMP) to adenosine monophosphate 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 calcium ions-the calmodulin complex, as a result of which the inactivated form of CLCM supports muscular relaxation. cAMP, 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 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:

Bioavailability is 100%. Drotaverine and its metabolites can penetrate the placental barrier. Does not penetrate the blood-brain barrier. Communication with plasma proteins is 95-97%. For 72 hours almost completely eliminated from the body.

With parenteral administration, the drug appears after 2-4 minutes. The maximum effect occurs in 30 minutes. It is released from the connection with blood 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 in diseases of bile ducts: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis.

Spasms of smooth muscles of the urinary tract: nephrolithiasis, urolithiasis, pyelitis, cystitis, bladder tenesmus.

As an auxiliary therapy (when the form of tablets can not be applied): with spasms of smooth muscles of the gastrointestinal tract: peptic ulcer of stomach and duodenum, gastritis, spasm of cardia and pylorus, enteritis, colitis, irritable bowel syndrome; with gynecological diseases: dysmenorrhea; at carrying out of some instrumental researches, including at cholecystography.

Contraindications:

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

- hypersensitivity to sodium disulfite;

- severe hepatic or renal insufficiency;

- severe chronic heart failure;

- AV-blockade II-III degree;

- childhood;

- the period of childbirth;

- the period of lactation.

If you have one of the listed diseases (conditions), before taking the drug always consult a doctor.

Carefully:

With arterial hypotension, pronounced arteriosclerosis of the coronary arteries, prostate adenoma, glaucoma, pregnancy.

Pregnancy and lactation:

The use of the drug during pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.

If it is necessary to use the drug during breastfeeding, it is necessary to resolve the issue of stopping breastfeeding.

Dosing and Administration:

Intramuscularly 2-4 ml (40-80 mg) 1-3 times a day. The course of treatment is 1-2 weeks. If necessary, prolonged treatment, they switch to taking the drug inside in the dosage form of the tablet.In acute colic (renal or cholelithiasis) - 2-4 ml (40-80 mg) in 10-20 ml 0.9% sodium chloride solution or 5% dextrose solution intravenously slowly (duration of administration is approximately 30 seconds). Do not mix in one syringe with a solution of aminophylline.

Side effects:

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

From the cardiovascular system: tachycardia, decrease arterial pressure, arrhythmia, collapse (with intravenous administration).

From the digestive system: nausea, vomiting, constipation.

Allergic reactions: angioedema, urticaria, rash, itching, anaphylactic shock.

Local reactions: reaction at the site of administration.

Other: feeling of heat, sweating.

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, inform the doctor about it.

Overdose:

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

Symptoms: atrioventricular blockade, cardiac arrest, paralysis of the respiratory center.

Treatment: In case of an overdose, patients should be careful medical supervision and they should conduct symptomatic therapy and treatment aimed at maintaining the basic functions of the body.

Interaction:

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

Strengthens (especially with intravenous administration) the spasmolytic effect of papaverine, bendazole and other antispasmodics, including m-holinoblokatory. Strengthens the hypotension caused by tricyclic antidepressants, quinidine, procainamide.

Reduces the spasmogenic activity of morphine.

Phenobarbital enhances the spasmolytic effect of drotaverine.

Special instructions:

The drug contains disulfite, which can cause allergic reactions, including anaphylactic symptoms and bronchospasm in sensitive individuals, especially in people with asthma or allergic diseases in history. In case of hypersensitivity to disulfite, parenteral administration of the drug should be avoided (see "Contraindications").

When intravenously administered drotaverina in patients with low blood pressure, the patient should be in a horizontal position in connection with the risk of collapse.

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

During the period of treatment it is not recommended to operate vehicles, mechanisms or engage in activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Solution for intravenous and intramuscular administration, 20 mg / ml.

Packaging:

To 2 ml in glass syringes of neutral glass with Luer Lock lock, with a hard cap and accessories. 1 syringe per contour cell packaging made of polyvinyl chloride or polyethylene terephthalate film. On 1 contour acheikova packing together with a needle injecting and the instruction on application in a pack from cardboard box.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

1 year.

The drug should not be used after the expiry date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:PL-004469

Date of registration:19.09.2017

Expiration Date:19.09.2022

The owner of the registration certificate:FARMZASCHITA NPC, FSUE FARMZASCHITA NPC, FSUE Russia

Manufacturer: & nbsp

FARMZASCHITA NPC, FSUE Russia

Information update date: & nbsp06.10.2017

Illustrated instructions

Instructions

Drotaverine (Drotaverine)