Drotaverin-Darnitsa

General characteristics. Structure:

Active ingredient: drotaverine; 1 ml of solution contains hydrochloride Drotaverinum in recalculation for 100% dry matter – 20 mg;

excipients: ethanol (96%), sodium metabisulphite (E 223), water for injections.

Pharmacological properties:

Pharmacodynamics. Drotaverinum has myotropic spasmolytic (papaverinopodobny) effect. The mechanism of action is caused by decrease in intake of calcium in cells of unstriated muscles by oppression of phosphodiesterase and intracellular accumulation of tsAMF. It is expressed and for a long time relaxes smooth muscles of internals and blood vessels, reduces arterial pressure.

Pharmacokinetics. At parenteral not vascular administration the elimination half-life (T1/2) of Drotaverinum makes 10–12 h of a blood plasma, almost full elimination of substance is noted for 72 h. Accumulates in high concentration in TsNS, fatty tissue, a myocardium, kidneys and lungs, the lowest concentration are noted in a liver and a stomach. Linkng with proteins of plasma – 95–98%. An insignificant part – in shape sulfate conjugates is removed by kidneys and bile in the form of conjugates with glucuronic acid (89–99%).

 

Pharmaceutical characteristics.

Main physical and chemical properties: transparent chartreuse or yellow liquid.

Indications to use:

The spasms of smooth muscles connected with diseases of a biliary path: cholecystolithiasis, cholangiolithiasis, cholecystitis, cholangitis, papillitis.

Spasms of smooth muscles at diseases of an uric path: nephrolithiasis, ureterolithiasis, pyelitis, cystitis, bladder tenesmus.

At physiological childbirth for reduction of a phase of disclosure of a neck of uterus and a duration of delivery.

As auxiliary treatment (when use of drug in the form of tablets is not possible):

- at spasms of smooth muscles of digestive tract: peptic ulcer of a stomach and duodenum, gastritis, spasms of the cardia and pylorus, enteritis, colitis;

- at gynecologic diseases: dysmenorrhea, strong labor pains.

Route of administration and doses:

Apply the adult. The usual daily dose makes 40–240 mg (2–12 ml) in 1–3 introductions intramusculary.

At hepatic or renal colic about 2-4 ml (40–80 mg) of drug are recommended to enter slowly intravenously.

For reduction of a phase of disclosure of a neck of uterus at the beginning of the disclosure period at physiological childbirth – 40 mg intramusculary. If this dose not effective, in 2 h enter 40 more mg of drug Drotaverin-Darnitsa.

Features of use:

To apply with care at arterial hypotension.

At intravenous administration of drug Drotaverin-Darnitsa the patient has to be in horizontal position!

Drug contains metabisulphite which can cause allergic reactions, including anaphylactic symptoms and a bronchospasm in sensitive patients, especially in patients with asthma and with allergic reactions in the anamnesis.

With care to apply at the expressed atherosclerosis of coronary arteries, prostate adenoma.

It is necessary to be careful at parenteral administration to pregnant women.

Drug contains ethanol (96%).

Ability to influence speed of response at control of motor transport or work with other mechanisms. During treatment it is recommended to abstain from control of motor transport or work with other mechanisms after parenteral (especially intravenous) introduction.

Side effects:

From a digestive tract: nausea, lock.

From a nervous system: headache, dizziness, sleeplessness.

From cardiovascular system: development of AV blockade, arrhythmia, arterial hypotension.

From immune system: reactions of allergic character, including anaphylactic symptoms and a bronchospasm, especially at patients with hypersensitivity to meta bisulphite; allergic dermatosis.

Interaction with other medicines:

Increases effect of other spasmolysants. Strengthens the arterial hypotension caused by tricyclic antidepressants, quinidine, novokainamidy. Reduces spazmogenny activity of morphine and antiparkinsonichesky action of a levodopa.

Phenobarbital increases expressiveness of spasmolytic action of Drotaverinum.

Contraindications:

Hypersensitivity to active ingredient or any component of drug (especially to sodium metabisulphite).

Heavy abnormal liver functions, kidneys and heart failure, AV blockade of II-III of degree, arterial hypotension, glaucoma. Feeding period breast. Children's age.

Use during pregnancy or feeding by a breast. Drug with care is used during pregnancy. Due to the lack of sufficient experimental data during feeding by a breast use of drug is not recommended.

Children. Drug is not used to children.

Overdose:

Symptoms. At overdose side effects of drug amplify, AV blockade, a cardiac standstill, paralysis of a respiratory center is possible.

Treatment. For the purpose of simplification of AV blockade apply atropine and изопреналин intravenously, to recovery of a heart rhythm – atropine or adrenaline intravenously with temporary cardiostimulation, at paralysis of a respiratory center artificial ventilation of the lungs is carried out.

Storage conditions:

Period of validity 2 years. To store in the place, unavailable to children, in original packaging at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 2 ml in an ampoule; on 5 or 10 ampoules in packaging.