Drotaverinum

General characteristics. Structure:

Active ingredient: 40 mg of Drotaverinum of a hydrochloride in 1 tablet.

Excipients: lactoses monohydrate, potato starch, povidone (polyvinylpirrolidone low-molecular medical 12600±2700), кросповидон (полипласдон XL-10), magnesium stearate, talc.

Pharmacological properties:

Pharmacodynamics. Myotropic spasmolysant, derivative isoquinoline. On chemical structure and pharmacological, to properties it is close to a papaverine; but possesses stronger and long action. Reduces receipt of calcium ions (Sa2+) in smooth muscle cells (inhibits phosphodiesterase (FDE), leads to accumulation of intracellular cyclic adenosinemonophosphate (tsAMF)) and as a result to an inactivation of a light chain of a kinase of a myosin therefore occurs rasslableyony smooth muscles.

Reduces a tone of unstriated muscles of internals and a peristaltics of intestines, expands blood vessels. Does not influence the autonomic nervous system, does not get into the central nervous system (CNS). Existence of direct influence on smooth muscles allows to use as a spasmolysant in cases when the medicines. (M.) from group of m-holinoblokatorov are contraindicated (closed-angle, glaucoma, a hypertrophy of a prostatic zheyoleza).

Pharmacokinetics. Absorption: at oral administration absorption - high; the semi-absorption period - 12 min. Bioavailability - 100%. Time of achievement of the maximum concentration - drug in a blood plasma (Tcmax) of-2 h.

Distribution: communication with proteins of plasma - 95-98%, are preferential with albumine, gamma and beta globulins, and also lipoproteins, the high density (LPVP)., it is Evenly distributed on fabrics, gets into smooth muscle cells. Does not get through a blood-brain barrier (GEB). Drotaverinum and/or its metabolites can slightly get through a placental barrier.

Metabolism: an elimination half-life (T1/2) - 8-10 h. Almost it is completely metabolized in a liver by O-dezetilirovaniya. Metabolites quickly conjugate with glucuronic acid. The main metabolite - 4-dezetildrotaverin, other metaboyolita - 6-dezetildrotaverin and 4-dezetildrotaveraldin.

Removal: for 72 h it is almost completely brought out of an organism. It is generally removed by kidneys (preferential in the form of metabolites) and to a lesser extent - with bile. Invariable Drotaverinum in urine is not found.

Indications to use:

Spasm of smooth muscles at diseases of biliary tract: cholecystolithiasis; cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, inflammation of a nipple of a 12-perstny gut. A spasm of smooth muscles at diseases of urinary tract: нефроуролитиаз, ureterolithiasis, pyelitis, cystitis, bladder spasm.

In a kayochestvo, auxiliary therapy: at spasms of smooth muscles of digestive tract: a peptic ulcer of a stomach and a 12-perstny gut, gastritis, a spasm of the cardia and the gatekeeper, enteritis, colitis, a spastic colitis with a lock, and a syndrome of the angry intestines with a meteorism; tensor, headache; dysmenorrhea. When carrying out some tool researches; including cholecystographies.

Route of administration and doses:

The dosing mode individual is also appointed by the doctor depending on a sostoyayoniya of the patient and a clinical picture of a disease.

Inside, to adults and children 12 years - on 40-80 mg (1-2 tablets) 2-3 times a day are more senior. To children aged from 6 up to 12 years - on 40 mg (1 tablet) 1-2 times a day.

Features of use:

At treatment of a peptic ulcer of a stomach and a 12-perstny gut apply in a sochetayoniya with other antiulcerous medicines.

Tablets contain lactoses monohydrate. It can cause gastrointestinal complaints in the persons having a lactose intolerance.

Influence on ability to manage vehicles and mechanisms. At intake in therapeutic doses Drotaverinum does not exert impact on ability to drive the car and to perform the works requiring special attention. At emergence of any side effects, the question of driving of transport and work on machines demands individual consideration.

Side effects:

Classification of frequency of development of side effects (WHO): very often> 1/10, it is frequent from> 1/100 to <1/10, infrequently from> 1/1000 to <1/100, is rare from> 1/10000 to <1/1000, is very rare from <1/10000, including separate messages.

Allergic reactions: infrequently - a Quincke's disease, a small tortoiseshell, rash, an itch.

From the central nervous system: infrequently - a headache, golovokruzheyony, sleeplessness.

From the alimentary system: infrequently - nausea, locks.

From cardiovascular system: infrequently - tachycardia, a lowering of arterial pressure.

If any of the side effects specified in the instruction are aggravated, or you noticed any other side effects which are not specified in the instruction, report about it to the doctor.

Interaction with other medicines:

At simultaneous use Drotaverinum can weaken protivoparkinsonichesky effect of a levodopa (strengthening of rigidity and a tremor).

Strengthens spasmolytic action of a papaverine, Bendazolum and other spasmolysants (including m-holinoblokatorov), the arterial hypotension caused by tritsikliyochesky antidepressants, quinidine and pokainamidy.

Reduces spazmogenny activity of morphine.

Phenobarbital increases expressiveness of spasmolytic action of Drotaverinum.

Contraindications:

Hypersensitivity to drug components, expressed hepatic, renal, cordial, insufficiency, an atrioventricular block of the II-III degree, cardiogenic shock arterial hypotension, the lactation period, children's age up to 6 years.

Due to the existence in composition of drug of lactose of monohydrate, its reception is contraindicated for the patients suffering from deficit of lactase, a galactosemia or a syndrome of the broken absorption of a glucose/galactose.

With care. Arterial hypotension, the expressed atherosclerosis coronary, arteries, a prostate hyperplasia, closed-angle glaucoma, the pregnancy period.

Overdose:

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

Treatment: drug withdrawal, the patient has to be under careful nablyudeyoniy the doctor and receive the symptomatic and supporting treatment. Rekomenduyotsya to cause vomiting and/or to wash out a stomach. Does not sushchestvuyot a specific antidote.

Storage conditions:

In the dry, protected from light place. To store in the places unavailable to children. A period of validity - 3 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets of 40 mg. Packaging: on 10 tablets in a blister strip packaging. 1, 2 or 5 konyoturny strip packagings together with the application instruction place in a pack from a cardboard.