Drotaverin-Borimed

General characteristics. Structure:

Active ingredient: 40 mg of Drotaverinum of a hydrochloride in 2 ml of solution.

Excipients: sodium pyrosulphite, sodium acetic 3-water, acetic acid, alcohol, water for injections.

Pharmacological properties:

Pharmacodynamics. Drotaverinum represents derivative isoquinoline which shows spasmolytic action on smooth muscles by suppression of enzyme of phosphodiesterase IV (FDE IV). The inhibition of enzyme of phosphodiesterase IV results in the increased concentration of tsAMF that inactivates an easy chain of a kinase of a myosin (MLCK) that, in turn, leads to relaxation of smooth muscles.

Drotaverinum inhibits enzyme (FDE) IV phosphodiesterase without inhibition of FDE III and FDE V isoenzymes. FDE IV is functionally very important for decrease in sokratitelny ability of unstriated muscles and the FDE IV selection inhibitors can be useful at treatment of the hyperkinetic diseases and various states connected with spastic conditions of digestive tract.

The enzyme hydrolyzing tsAMF in cells of smooth muscles a miokardiya and vessels, generally is FDE III isoenzyme, it explains that Drotaverinum is an effective spasmolytic agent without serious cardiovascular side effects and the expressed action on cardiovascular system.

Drotaverinum is effective at the spasms of smooth muscles caused by disturbance of nervous control and self-control of both a nervous, and muscular etiology. Irrespective of type of a vegetetivny innervation, Drotaverinum affects the unstriated muscles which are in gastrointestinal, bilious, urogenital and vascular systems.

Thanks to the vasodilating action it improves blood circulation of fabrics.

Action of Drotaverinum is stronger, than at a papaverine, and absorption - more bystry and full, it contacts proteins of plasma less. Advantage of Drotaverinum is that it does not possess a promoting effect on respiratory system which was observed after parenteral administration of a papaverine.

Pharmacokinetics. Bioavailability – 100%. It is evenly distributed on fabrics, gets into smooth muscle cells. Time of achievement of the maximum concentration of drug in a blood plasma (Cmax) - 2 h. Communication with proteins of plasma – 95 - 98%. It is metabolized in a liver. An elimination half-life of medicine (T1/2) – 2,4 h later in/in introductions. It is generally removed by kidneys, to a lesser extent - with excrements. Does not get through a blood-brain barrier.

Indications to use:

• the spasms of smooth muscles connected with diseases of a biliary path: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis;

• spasms of smooth muscles of urinary tract: nephrolithiasis, ureterolithiasis, pyelitis, cystitis, bladder tenesmus;

• at physiological childbirth - shortening of a phase of disclosure of a neck of uterus and by that reduction of the general duration of delivery.

As auxiliary therapy (when the form of tablets cannot be applied):

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

• at gynecologic diseases: dysmenorrhea;

• strong labor pains.

Route of administration and doses:

The average daily dose for adults makes 40 – 240 mg of Drotaverinum of a hydrochloride (divided into 1 - 3 introductions a day) intramusculary.

At acute gripes (renal or bilious) - 40 - 80 mg (2 - 4 ml of medicine) intravenously slowly.

For shortening of a phase of disclosure of a neck of uterus during physiological childbirth at the beginning of the period of stretching of 40 mg (2 ml) intramusculary that at unsatisfactory effect 1 time within 2 hours can be repeated.

Features of use:

At hypotension use of medicine demands the increased care.

At intravenous maintaining Drotaverinum – in connection with danger of a collapse – the patient has to lie!

In case of hypersensitivity to sodium pyrosulphite of parenteral use of medicine it is necessary to avoid. Medicine contains sodium pyrosulphite which can cause reactions of allergic type, including anafilaktichsky symptoms and a bronchospasm in sensitive persons, especially in persons with asthma or allergic diseases in the anamnesis.

Pregnancy and lactation. Parenteral use of Drotaverinum during pregnancy does not lead to teratogenic and embriotoksichesky actions. However, at prescription of medicine during pregnancy care is necessary.

Due to the lack of necessary clinical data in the period of a lactation it is not recommended to appoint.

Influence on ability to driving of motor transport and to control of mechanisms. After parenteral, and especially intravenous administration of medicine, patients are recommended to refrain from driving of vehicles and occupations potentially dangerous types of activity demanding speed of physical and mental reactions during 1 h after parenteral administration.

Side effects:

• from digestive tract: seldom (<1/10000) - nausea, a lock;

• from the central nervous system: seldom (<1/10000) - a headache, dizziness, sleeplessness;

• from cardiovascular system: seldom (<1/10000) - tachycardia, hypotension;

• disturbances of immune system: seldom (<1/10000) – allergic reactions, especially at the patients having hypersensitivity to sodium pyrosulphite).

Interaction with other medicines:

Drotaverinum can weaken antiparkinsonichesky effect of a levodopa.

Drotaverinum strengthens action of a papaverine, Bendazolum, etc. spasmolysants (including m-holinoblokatorov).

At simultaneous use with Drotaverinum of tricyclic antidepressants, quinidine and procaineamide hypotensive action amplifies.

Drotaverinum reduces spazmogenny activity of morphine.

Phenobarbital increases expressiveness of spasmolytic action of Drotaverinum.

Contraindications:

Hypersensitivity to active agent or to any of medicine excipients (in particular to sodium pyrosulphite), heavy liver, renal or heart failure (a syndrome of low cordial emission), children's age.

With care it is necessary to appoint at arterial hypotension, the expressed atherosclerosis of coronary arteries, during pregnancy.

Overdose:

Symptoms: in high doses breaks atrioventricular conductivity, reduces excitability of a cardiac muscle, can cause a cardiac standstill and paralysis of a respiratory center.

Treatment: symptomatic.

Storage conditions:

In the place protected from light, at a temperature from 15 to 25 ºС. To store in the place, unavailable to children. A period of validity - 2 years. Medicine cannot be used after the termination of a period of validity.

Issue conditions:

According to the recipe

Packaging:

In ampoules on 2 ml in packaging No. 10, No. 10 x 1.