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

Excipients: lactose monohydrate 52.0 mg, potato starch 35.0 mg, povidone (low molecular weight polyvinylpyrrolidone) 6.0 mg, talc 4.0 mg, calcium stearate 3.0 mg.

Description:

Round, flat-cylindrical tablets of light yellow with greenish openck or yellow with greenish openck color with impregnations from light yellow to yellow with greenish color of the color on the surface and in the mass of the tablet.

Pharmacotherapeutic group:Spasmolytic agent

ATX: & nbsp

A.03.A.D.02 Drotaverine

Pharmacodynamics:

Drotaverin is an isoquinoline derivative that exhibits a powerful antispasmodic effect on smooth muscles due to inhibition of the enzyme, phosphodiesterase (PDE). Inhibition of the enzyme PDE leads to an increase in the concentration of cyclic adenosine monophosphate (cAMP), which inactivates the light chain of myosin kinase (MLCK), which, in turn, leads to relaxation of smooth muscles.

Drotaverine inhibits the isoenzyme PDE-4 in vitro without inhibiting the isoenzymes PDE-3 and PDE-5. Therefore, the effectiveness of drotaverine depends on the concentration of PDE-4 in tissues, the content of which differs in different tissues. PDE-4 is most important for suppressing the contractile activity of smooth muscle, and therefore selective inhibition of PDE-4 can be useful for the treatment of hyperkinetic diseases and various diseases accompanied by the spastic state of the gastrointestinal tract.

The hydrolysis of cAMP in the myocardium and smooth muscle of blood vessels is mainly due to the isoenzyme PDE-3, therefore drotaverine less affects the cardiovascular system.

Drotaverine is effective in spasms of smooth muscles of both neurogenic and muscular origin. Regardless of the type of autonomic innervation drotaverine relaxes the smooth musculature of the gastrointestinal tract, biliary tract, urogenital system.

Pharmacokinetics:

Suction. When taken orally drotaverine quickly and completely absorbed. Bioavailability is 100%. The maximum concentration of the drug in the blood plasma (C_m_Oh) is reached after 45-60 minutes.

Distribution. The connection with blood plasma proteins is 95-98%, mainly with albumin, γ and β-globulins. 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.

Metabolism. Metabolised in the liver.

Excretion. The half-life (T1/2) - 16-22 hours. Within 72 hours drotaverine almost completely eliminated from the body mainly in the form of metabolites, more than 50% is excreted by the kidneys and about 30% - through the intestine (with bile).

Indications:

- spasms of smooth muscles associated with diseases of the biliary tract: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis;

- spasms of smooth muscles associated with diseases of the urinary tract: nephrolithiasis, urethrolithiasis, pyelitis, cystitis, bladder spasm.

As an auxiliary therapy:

- spasms of smooth muscles of the gastrointestinal tract: peptic ulcer of stomach and duodenum, gastritis, spasms of cardia and pylorus, enteritis, colitis, accompanied by constipation and flatulence;

- tensor headache;

- Dysmenorrhea.

Contraindications:

- hypersensitivity to drotaverine or other components of the drug;

- severe hepatic or renal insufficiency;

- severe heart failure (low cardiac output syndrome);

- atrioventricular block II-III degree, arterial hypotension, cardiogenic shock;

- lactose intolerance, lactase deficiency, glucose-galactose malabsorption (due to the presence of lactose in the formulation);

- the period of breastfeeding;

- children's age till 6 years.

Carefully:

Carefully patients with severe atherosclerosis of the coronary arteries, prostatic hyperplasia, glaucoma, during pregnancy, simultaneous administration with levodopa.

Pregnancy and lactation:

In pregnancy drotaverine Should be used 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.

Dosing and Administration:

Inside, with enough liquid.

Adults appoint 40-80 mg (1-2 tablets) 2-3 times a day, the maximum daily dose is 240 mg.

Children aged 6 to 12 years appoint a single dose of 40 mg 1-2 times a day, the maximum daily dose is 80 mg.

Children over 12 years old appoint 40-80 mg (1-2 tablets) 2-4 times a day, the maximum daily dose is 160 mg.

The recommended duration of treatment without a doctor's consultation is 1-2 days.

Side effects:

The frequency of unwanted reactions is given in accordance with the following scale: very often (> 10%); often (> 1% and <10%); infrequently (> 0.1 % and <1 %); rarely (>0,01 % and <01 %); very rarely (<0.01 %).

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

From the cardiovascular system: rarely - increased heart rate, very rarely - lowering blood pressure.

From the digestive system: rarely - nausea, constipation.

Allergic reactions: infrequently - itchy skin, rash, angioedema, hives.

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:

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

Treatment: induction of vomiting, gastric lavage, symptomatic therapy. There is no specific antidote.

Interaction:

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

Enhances the spasmolytic effect of papaverine, bendazole and other antispasmodics (including m-holinoblokatorov).

Reduces the spasmogenic activity of morphine.

Phenobarbital increases the severity of spasmolytic action of drotaverine.

Special instructions:

Care should be taken when using the drug in patients with severe arterial hypotension.

The composition of the tablets includes lactose, so the drug is not prescribed for patients with lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome.

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

When administered orally in therapeutic doses, the drug does not affect the ability to drive vehicles and engage in other potentially hazardous Activities that require increased concentration and speed of psychomotor reactions.If you have any side effects from the nervous system (headache, dizziness), you should avoid practicing potentially hazardous activities, such as driving and handling machinery.

Form release / dosage:Tablets of 40 mg.

Packaging:

For 10 tablets in a contour mesh package, 20 or 100 tablets per vial of polymer.

2 contour squares or 1 bottle of polymer together with instructions for use in a pack of cardboard.

Storage conditions:

In the dark place at a temperature of no higher than 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:Without recipe

Registration number:P N001658 / 01

Date of registration:24.12.2007 / 07.09.2015

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

Manufacturer: & nbsp

FARMPROJECT, CJSC Russia

Information update date: & nbsp16.06.2016

Illustrated instructions

Instructions

Drotaverine (Drotaverine)