Drotaverinum hydrochloride

General characteristics. Structure:

Active ingredient: 40 mg of Drotaverinum of a hydrochloride in each tablet.

Excipients: lactose monohydrate, potato starch, talc, stearic acid.

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 cardiovascular side effects and the expressed action on cardiovascular system. Drug 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. Its action 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. Absorption. At intake of Drotaverinum the hydrochloride is quickly absorbed from digestive tract, the semi-absorption period - 12 min. Bioavailability - about 100%. Cmax in serum is reached in 45 - 60 min.

Distribution. Drotaverinum the hydrochloride does not get through a blood-brain barrier.

Metabolism. Drotaverinum the hydrochloride biotransformirutsya in a liver.

Removal. In 72 h it is practically brought out of an organism in the form of metabolites - for 50% with urine and for 30% - with a stake.

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.

As auxiliary therapy:

- at spasms of smooth muscles of a gastrointestinal origin: a peptic ulcer of a stomach and duodenum, gastritis, spasms of the cardia and the gatekeeper, enteritis, colitis, a spastic colitis with a lock and meteoristichesky forms of mucous colitis;

- headaches of tenzionny type;

- in obstetrics and gynecology: альдисменорея, for reduction of the raised uterus tone during pregnancy, at the menacing abortion.

Route of administration and doses:

Inside, the adult appoint 40-80 mg (1 - 2 tablets) 3 times a day; to children at the age of 1 - 6 years appoint in a single dose 10-20 mg (1/4-1/2 tablets), the maximum daily dose – 120 mg (3 tablets); aged from 6 up to 12 years – a single dose - 20 mg (1/2 tablets), the maximum daily dose – 200 mg (5 tablets). Frequency rate of appointment - 2 - 3 in days.

Features of use:

Use of medicine at hypotension demands the increased care.

Tablets of Drotaverinum contain 53 mg of lactose, At reception according to the recommended dosage each dose contains up to 159 mg of lactose. It can cause gastrointestinal frustration in the persons having a lactose intolerance. This dosage form is unacceptable for the patients suffering from deficit of lactase, a galactosemia or a syndrome of the broken absorption of a glucose / galactose.

Pregnancy and lactation. 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 management to mechanisms. Patients should be informed that at display of dizziness they have to avoid potentially dangerous actions, such as management of transport and potentially dangerous mechanisms.

Side effects:

• from digestive tract: seldom (> 1/10000, <1/1000) - nausea, a lock;

• from a nervous system: seldom (> 1/10000, <1/1000) - a headache, dizziness, sleeplessness;

• from cardiovascular system: seldom (> 1/10000, <1/1000) - tachycardia, hypotension.

Interaction with other medicines:

At simultaneous use Drotaverinum can weaken protivoparkinsonichesky effect of a levodopa.

Contraindications:

- hypersensitivity to active agent or to any of medicine excipients;

- heavy liver and renal failure;

- heavy heart failure (syndrome of low cordial emission);

- children's age till 1 year.

With care it is necessary to appoint at arterial hypotension, the expressed atherosclerosis of coronary arteries, during pregnancy, at children from 1 year to 6 years.

Overdose:

So far about cases of overdose it was not reported.

Storage conditions:

In the place protected from light and moisture, at a temperature not over 25 ºС. A period of validity - 2 years. Medicine cannot be used after the termination of the period of validity specified on packaging.

Issue conditions:

Without recipe

Packaging:

On 10 tablets in a blister strip packaging; on 2 planimetric packagings in a pack from a cardboard.