Drotaverinum

General characteristics. Structure:

Active ingredient: 20 mg of Drotaverinum of a hydrochloride (in terms of 100% substance) in 1 ml of solution.

Excipients: sodium disulphite (sodium metabisulphite), ethanol (alcohol) of 95%, water for injections

Pharmacological properties:

Pharmacodynamics. Drotaverinum - derivative isoquinoline, on chemical structure and pharmacological properties is close to a papaverine, but renders more expressed and long deyyostviye. Drotaverinum possesses the expressed spasmolytic action on unstriated muscles at the expense of inhibition of phosphodiesterase-4 (FDE-4). FDE-4 hydrolyzes tsAMF to AMF. The inhibition of FDE-4 leads to increase in concentration of tsAMF which activates tsAMF - dependent phosphorylation of the kinase of light chains of a myosin (KLCM).

Phosphorylation of KLTsM leads to decrease in its affinity to Sa2+-to a kalmodulinovy complex therefore the inactivated KLTsM form supports myshechyony relaxation. tsAMF, besides influences cytosolic concentration of Sa2+, благо­даря to stimulation of transport of Sa2 + in extracellular space and a sarcoplasmic reticulum. In vitro Drotaverinum inhibits FDE-4 isoenzyme without ingibirovayoniya of isoenzymes of FDE-3 and FDE-5 therefore efficiency of Drotaverinum depends on activity of FDE-4, which content in different fabrics various. High content of FDE-4 is noted in zhelche-and urinary tract, a uterus, digestive tract.

Hydrolysis of tsAMF in a myocardium and unstriated muscles of blood vessels happens, a glavyony image, by means of FDE-3 therefore Drotaverinum influences cordial vascular system less. Drotaverinum is effective at spasms of smooth muscles of both a neurogenic, and muscular origin.

Pharmacokinetics. At parenteral administration effect of drug is shown in 2-4 minutes. The maximum effect occurs in 30 minutes. It is released from communication with proteins of plasma gradually, providing long action. Elimination half-life 2-4 hours. Metabolism is carried out in a liver, the main part of metabolites is allocated with kidneys.

Indications to use:

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

Spasm of smooth muscles of urinary tract: nephrolithiasis, ureterolithiasis, pyelitis, cystitis, bladder tenesmus.

As auxiliary therapy (when the form of tablets cannot be applied): at spasms of smooth muscles of a gastrointestinal origin: ulcer бо­лезнь stomach and duodenum, gastritis, spasm of the cardia and gatekeeper, enteritis, colitis.

At gynecologic diseases: dysmenorrhea.

Route of administration and doses:

Adults: the average daily dose makes 40-240 mg of Drotaverinum of a hydrochloride (razyodelenny on 1-3 doses a day) intramusculary; at acute gripes (renal and cholelithic) 40-80 mg intravenously slowly (duration of introduction about 30 seconds).

Features of use:

Pregnancy and lactation. Use at pregnancy is possible only when the potential advantage for mother exceeds potential risk for a fruit.

At treatment of a peptic ulcer of a stomach and duodenum apply in combination with other antiulcerous medicines. At intravenous administration the patient has to be in horizontal position (risk of a collapse).

Drug contains disulphite which can cause reactions of allergic type, including an acute anaphylaxis and a bronchospasm in persons, sensitive to sulfites, osoyobenno in the presence in the anamnesis of bronchial asthma and allergic diseases; in case of hypersensitivity to disulphite parenteral administration of drug is contraindicated.

Influence on ability to manage vehicles and mechanisms. During treatment it is necessary to abstain from driving of motor transport and occupations other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions (within 1 hour after intravenous administration).

Side effects:

Side reactions with the indication of frequency of their emergence are given below: very much час­то - more than 1/10, it is frequent - more than 1/100 and less than 1/10, infrequently - more than 1/1000 and less than 1/100, is rare - more than 1/10000 and less than 1/1000, is very rare - more than 1/10000, including separate messages, the unknown frequency (according to the available data frequency cannot be determined).

From a nervous system: seldom - a headache, dizziness, sleeplessness.

From cardiovascular system: seldom - heartbeat increase, a lowering of arterial pressure.

From the alimentary system: seldom - nausea, a lock.

From immune system: seldom - allergic reactions (a Quincke's disease, a small tortoiseshell, rash, an itch).

Unknown frequency: at use of drug it was reported about development of anafilakticheyosky shock from the death and without death.

Local reactions: seldom - reactions in an injection site.

Interaction with other medicines:

- phosphodiesterase inhibitors, similar to a papaverine, weaken protivoparkinsonichesky effect of a levodopa;

- at simultaneous use with drug a levodopa strengthening of rigidity and a tremor is possible;

- Drotaverinum strengthens spasmolytic action of a papaverine, Bendazolum and other spasmolysants, including m-holinoblokatory;

- strengthens the hypotension caused by tricyclic antidepressants, quinidine and procaineamide;

- reduces spazmogenny activity of morphine; phenobarbital strengthens spasmolytic action of Drotaverinum.

Contraindications:

• Hypersensitivity to active ingredient or to any of drug excipients;
• Hypersensitivity to sodium to disulphite;
• Heavy liver or renal failure;
• Children's age;
• Feeding period breast;
• Period of childbirth.

With care apply at arterial hypotension, during pregnancy.

Overdose:

At overdose strengthening of dozozavisimy side effects is possible.

Treatment: symptomatic.

Storage conditions:

To store in the place protected from light at a temperature from 5 to 25 °C. To store in the place, unavailable to children. A period of validity - 2 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Solution for intravenous and intramuscular administration of 20 mg/ml in ampoules on 2 ml. Packaging: on 5 ampoules of light-protective glass in a blister strip packaging from a film of polyvinyl chloride and aluminum foil (or without foil). 1 or 2 blister strip packagings with the scarificator ampoule ceramic or a knife for opening of ampoules and the application instruction place in a pack from a cardboard. When using ampoules with a ring of a break or a point of a break the knife or the scarificator do not put.