Drotaverinum

General characteristics. Structure:

International and chemical names: drotaverine; 1-[(3,4 diethoxy-phenyl) marked] - 6,7-diethoxy-3,4-dihydroisoquinoline a hydrochloride; main physical and chemical properties: transparent liquid of chartreuse or yellow color; structure: 1 ml of solution contains Drotaverinum of a hydrochloride 20 mg; excipients: alcohol of ethyl 96%, sodium metabisulphite, water for injections.

Pharmacological properties:

Pharmacodynamics. Spasmolytic, vasodilating, antihypertensive. A spasmolysant of myotropic action which mechanism is caused by reduction of intake of calcium in smooth muscle cells as a result of inhibition of phosphodiesterase and intracellular accumulation of tsAMF. Vyrazhenno it is also long expands smooth muscles of internals and vessels, reduces their physical activity, lowers arterial pressure, increases the minute volume of heart. On a chemical structure and pharmacological properties it is close to a papaverine, however surpasses it in efficiency and duration of action.

Pharmacokinetics. At parenteral administration Drotaverinum is quickly soaked up. Action comes in 2-4 min. after intravenous administration and in 5-10 min. – after intramuscular. The maximum concentration in plasma – in 30-40 min. The elimination half-life (T1/2) of Drotaverinum from a blood plasma is equal to 10-12 h, almost full elimination of substance is noted during 72 h. Linkng with proteins of plasma – 95-98%. Accumulates in high concentration in fatty tissue, a myocardium, kidneys and lungs, the lowest concentration are noted in a liver and a stomach. Does not get through a blood-brain barrier. It is metabolized in a liver, 50% with urine and 20% with a stake in the form of conjugates with glucuronic acid, an insignificant part of  in shape sulfate conjugates are removed.

Indications to use:

The functional disturbances and pain syndrome caused by a spasm of unstriated muscles of internals including at a chronic gastroduodenit, a peptic ulcer of a stomach and duodenum, a zhelchekamenny disease, chronic cholecystitis, a postcholecystectomy syndrome, hyper motor dyskinesia of biliary tract, spastic dyskinesia of intestines (intestinal colic), at postoperative colic owing to a delay of gases, spastic locks, a spastic colitis, a proctitis, tenesmus, a meteorism, an urolithiasis (renal colic), a pyelitis. Spasm of coronary and peripheral arteries, brain vessels. For decrease in excitability of a uterus at pregnancy, at a spasm of a neck of uterus in labor, long disclosure of a neck, at puerperal pains, the menacing abortion. When carrying out tool interventions.

Route of administration and doses:

Appoint the adult usually intramusculary, 2-4 ml (40-80 mg) 1-3 times a day. For removal of hepatic or renal colic it is recommended to enter intravenously, slowly. At disturbances of peripheric circulation it is possible to enter vnutriarterialno, slowly.
To children 12 years drug are more senior appoint intramusculary, 1-2 ml (20-40 mg) 1-3 times a day.

Features of use:

At intravenous administration of the patient has to be in lying situation. With care appoint the patient with suspicion of atherosclerosis of coronary arteries, and also during the periods of pregnancy and a lactation.
It is necessary to refrain from the activity requiring special attention, bystry mental and motor reactions within an hour after parenteral (especially intravenous) introduction.

Side effects:

Dizziness, sweating strengthening, heart consciousness, feeling of heat; at intravenous administration – a lowering of arterial pressure. Sometimes – development of AV-blockade, arrhythmia, at intravenous administration – oppression of a respiratory center, allergic dermatitis.

Interaction with other medicines:

Strengthens effect of other spasmolysants (including m-holinoblokatorov) and the hypotension caused by tricyclic antidepressants, quinidine, novokainamidy. Reduces antiparkinsonichesky action of a levodopa. Reduces spazmogenny activity of morphine

Contraindications:

The increased individual sensitivity to drug components. Heavy liver, renal or heart failure. AV blockade of the II-III degree, glaucoma; children up to 12 years.

Overdose:

AV blockade, decrease in excitability of a cardiac muscle, arrhythmia, oppression of a respiratory center are possible.
Treatment: drug withdrawal, symptomatic therapy. The specific antidote does not exist.

Storage conditions:

To store in protected from light, the place, unavailable to children, at a temperature not above 25 °C.

Period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

On 2 ml of solution in an ampoule; on 5 ampoules in the cartridge, on 2 or 4 cartridges in a pack.