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

Excipients: sodium disulfite - 1 mg, ethanol 95 % - 61 mg, disodium edetate dihydrate 0.1 mg, benzethonium chloride 0.1 mg, sodium sulfite anhydrous 0.2 mg, citric acid monohydrate 0.825 mg, sodium citrate pentasecylhydrate 1.65 mg, water for injection up to 1 ml .

Description:Transparent or slightly opalescent. liquid of light yellow or greenish-yellow 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 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 KLTSM 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, 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 PDE-4 isoenzyme without inhibition of isoenzymes PDE-3 and PDE-5, therefore the effectiveness of drotaverine 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 cAMP in myocardium and smooth muscleblood vessels occurs mainly with the help of PDE-3; so drotaverine less affects the cardiovascular system. Drotaverine Effective for spasms of smooth muscles, both neurogenic andof muscular origin.

Pharmacokinetics:

Quickly and well absorbed in the gastrointestinal tract.

Absorption - 100 %. However, the systemic blood flow is 65 % the accepted dose (the effect of "first passage" through the liver). Time to reach the maximum concentration (TCmah) 45-60 minutes. The connection with plasma proteins is 95-97%, mainly with albumin, - gamma and beta globins, 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; other metabolites are 6-deethyldroverine and 4-desethylditaveraldin. The half-life period (T1 / 2) is 8-10 hours. For 72 hours it is almost completely eliminated from the body, more than 50 % kidneys (mainly in the form of metabolites) and about 30% of the intestines. Unchanged drotaverine in the urine is not found.

Indications:

Spasms smooth musculature at 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 used): with spasms of smooth muscles of gastrointestinal origin: ulcerative disease of the 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;

- severe chronic heart failure;

- childhood;

- the period of lactation.

Carefully:With arterial hypotension (danger of collapse, see section Special instructions).

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 you need to use the drug during breastfeeding, you need to resolve the issue of stopping breastfeeding.

Dosing and Administration:

Adults: The daily average dose is 40-240 mg of drotaverine hydrochloride (divided by 1-3 doses per day) intramuscularly, subcutaneously.

With acute colic (renal or cholelithiasis) - 40-80 mg intravenously slowly (duration of administration is approximately 30 seconds).

Side effects:

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

From the cardiovascular system: tachycardia, reduction: blood pressure, collapse (with intravenous administration).

From the digestive system: nausea, constipation.

Allergic reactions: angioedema, urticaria, rash, itching.

Local reactions: reactions at the site of administration.

Overdose:

Atrioventricular blockade, cardiac arrest, paralysis of the respiratory center.

In case of an overdose, patients should be under close medical supervision and should be given 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, novocainamide.
Reduces the spasmogenic activity of morphine.
Phenobarbital enhances the spasmolytic effect of drotaverine.

Special instructions:

The drug contains a disulfite that can cause allergic reactions, including anaphylactic symptoms and bronchospasm in sensitive individuals, especially in people with asthma or allergic diseases in the anamnesis. In the case of increased sensitivity to disulfite parenteral use of the drug should be avoided (see Contraindications section).

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

Effect on the ability to drive transp. cf. and fur:During the treatment period, it is necessary to refrain from driving and other potentially dangerous speciesactivities that require increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Solution for injection 20 mg / ml.

Packaging:

2 ml into the ampoules of the light-protective glass.

For 5 or 10 ampoules, together with the instructions for use, they are placed in a pack of cardboard with a liner of paper or corrugated, ribbon, or with special nests, and paste a label-parcel of paper. It is allowed to put the text of the label-parcel directly on the packet.

5 ampoules are placed in a contour mesh package from a polyvinyl chloride film and foil aluminum lacquered or without foil.

For 1 or 2 contour packagings together with the instruction for use, place in a pack of cardboard and paste a label of paper. The text of the package label is allowed apply directly to the pack.

In each pack insert knife ampoule or scarifier. When you pack the ampoules with a break point or a fracture ring, the ampoule knife or scarifier does not insert.

Storage conditions:

In dry, 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 expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-000697

Date of registration:28.09.2011

The owner of the registration certificate:Armavir Biofactory, FKPArmavir Biofactory, FKP Russia

Manufacturer: & nbsp

ARMAVIRSK BIOLOGICAL FACTORY, FSUE Russia

Information update date: & nbsp02.12.2015

Illustrated instructions

Instructions

Drotaverine (Drotaverine)