But-x-sha tab. of 0.04 g No. 30

Structure and form of release

Structure

Active ingredient: drotaverine;

1 tablet contains

: Drotaverinum a hydrochloride in terms of dry matter of 40 mg (0.04 g);

excipients: lactoses monohydrate, starch corn, magnesium stearate, talc.

release Form

Tablet.

Pharmacological properties

Pharmacodynamics.

Drotaverinum — derivative isoquinoline which has spasmolytic effect directly on smooth muscles by oppression of effect of enzyme of ІV phosphodiesterase (FDE ІV) that attracts increase in concentration of tsAMF and thanks to an inactivation of an easy link of a kinase of myosin (MLCK) leads

to relaxation of an unstriated muscle.

In vitro Drotaverinum oppresses effect of FDE ІV enzyme and phosphodiesterase ІІІ (FDE ІІІ) and phosphodiesterase V (FDE V) does not influence action of isoenzymes. FDE ІV has great functional value for decrease in sokratitelny activity of unstriated muscles therefore selective inhibitors of this enzyme can be useful to treatment of diseases which are followed by hyper mobility and also for treatment of various diseases at which there are digestive tract spasms.

In cells of unstriated muscles of a myocardium and vessels of tsAMF it is hydrolyzed generally by FDE isoenzyme ІІІ therefore Drotaverinum is effective antispasmodic which has no considerable side effects from a cardiovascular system and strong therapeutic impact on this system.

Drotaverinum is effective

at spasms of smooth muscles of both nervous, and muscular origin. Drotaverinum affects smooth muscles of gastrointestinal, biliary, urinogenital and vascular systems irrespective of type of their autonomous innervation.

It strengthens

krovoobmen in fabrics thanks to the ability to expand vessels.

Pharmacokinetics.

Effect of Drotaverinum is stronger, than action of a papaverine, absorption faster and full, it contacts serum proteins less. Advantage of Drotaverinum is also that, unlike a papaverine, after its parenteral administration such side effect as breath stimulation is not observed.

Drotaverinum is quickly and completely absorbed by

after oral administration. It highly (95–98%) contacts albumine of blood plasma, gamma and beta globulins. The maximum concentration in blood serum is reached within 45–60 minutes after oral administration. After primary metabolism of 65% of the entered dose comes to a blood-groove in not changed look.

by

It is metabolized in a liver. Elimination half-life makes 8–10 hours.

Drotaverinum is almost completely removed by

In 72 hours from an organism, more than 50% are removed with urine and about 30% — with a stake. Generally Drotaverinum is removed in the form of metabolites, in not changed form in urine is not defined.

Indication

With the medical purpose at:

• spasms of smooth muscles connected with diseases of a biliary path: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis;
• spasms of smooth muscles at diseases of an uric path: nephrolithiasis, ureterolithiasis, pyelitis, cystitis, bladder tenesmus.

As auxiliary treatment at:

• spasms of smooth muscles of digestive tract: a peptic ulcer of a stomach and a duodenum, gastritis, kardio and/or a pylorospasm, enteritis, colitis, a spastic colitis with a constipation and a syndrome of the angry intestines which are followed by a meteorism;
• a headache of tension;
• gynecologic diseases (dysmenorrhea).

Contraindication

Hypersensitivity to Drotaverinum or to any component of medicine. heavy liver, renal or heart failure (syndrome of small warm emission).

Route of administration and doses

Adult: the usual average dose makes 120–240 mg a day in 2–3 receptions.

in case of use of Drotaverinum to children:

for children of 6-12 years the maximum daily dose makes 80 mg (divided into 2 receptions);

for children from 12 years the maximum daily dose makes 160 mg (divided into 2–4 receptions).

to Apply

Feature of application

with extra care at arterial hypotension.

Tablet of medicine of No-H-sha of ^® contain lactose. Not to apply to treatment of the patients having rare hereditary diseases, such as intolerance of a galactose, deficiency of Lappa lactase or a glucose galactose sprue.

Use during pregnancy or feeding by a breast

Pregnancy. As showed results of retrospective clinical trials and researches on animals, oral administration of medicine did not cause any signs of any direct or indirect impact on pregnancy, embryonic development, childbirth or postnatal development. However pregnant women need to appoint medicine with care. Feeding by a breast. Due to the lack of data during feeding by a breast use of medicine is not recommended.

by

to Drivers

If at patients after use of medicine observes dizziness, they have to avoid potentially dangerous occupations, such as driving and performance of work which require special attention.

Children to

to Children up to 6 years the use of medicine is contraindicated to

. Drotaverinum use to children was not estimated in clinical trials.

Overdose

Symptoms: at considerable overdose of Drotaverinum, violations of a warm rhythm and conductivity, including a total block of a ventriculonector and cardiac arrest which can be lethal were observed.

At overdose the patient has to be under careful observation of the doctor and receive symptomatic treatment, including calling of vomiting and/or gastric lavage.

Side reactions

Side effect which was observed during clinical trials and, perhaps, was caused by Drotaverinum, distributed on the system of bodies.

from the immune system: allergic reactions, including a Quincke's disease, a small tortoiseshell, rash, the naggers, a dermahemia, fever, a fever, fervescence, weakness.

from a cardiovascular system: cardiopalmus, arterial hypotension.

from nervous system: headache, dizziness, insomnia.

from digestive tract: nausea, lock, vomiting.

Interaction

phosphodiesterase Inhibitors, such as papaverine, reduce antiparkinsonichesky effect of a levodopa.

Should use with care medicament No-H-sha ^® along with a levodopa as the antiparkinsonichesky effect of the last decreases, and the rigidity and a tremor amplify.

Storage conditions

to Store

in original packing at a temperature not above 25 °C. To store out of children's reach. An expiration date - 5 years.