Нош-Бра®

General characteristics. Structure:

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

Excipients: potato starch, sugar milk (lactoses monohydrate), polyvinylpirrolidone low-molecular (povidone), talc, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Drotaverinum - a myotropic spasmolysant, derivative isoquinoline. On chemical structure and pharmacological properties it is close to a papaverine, but has more expressed and long effect. Drotaverinum is effective at spasms of smooth muscles of both a neurogenic, and muscular origin.

Spasmolytic action on smooth muscles is caused at the expense of phosphodiesterase inhibition 4 types (FDE-4). FDE-4 hydrolyzes cyclic adenosinemonophosphate (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 muscular relaxation. tsAMF, besides, influences cytosolic concentration of Sa2+, thanks to stimulation of transport of Sa2 + in extracellular space and a sarcoplasmic reticulum.

In vitro Drotaverinum inhibits FDE-4 isoenzyme without inhibition 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, mainly, by means of FDE-3 therefore Drotaverinum influences cardiovascular system less.

Pharmacokinetics. At oral administration it is quickly and completely absorbed in digestive tract. Is exposed to effect of "the first passing" through a liver (the quantity Defined in a system blood-groove makes 65% of the accepted dose). Time of achievement of the maximum concentration (TCmax) - 45-60 min.

Communication with proteins of plasma - 95-97%, are preferential with albumine, scale and beta globulins, and also lipoproteids of high density. It is evenly distributed on fabrics, gets into smooth muscle cells. Does not get through a blood-brain barrier. Drotaverinum and/or its metabolites can slightly get through a placental barrier.

Almost it is completely metabolized in a liver by O-dezetilirovaniya. Metabolites quickly conjugate with glucuronic acid. The main metabolite - 4-dezetildrotaverin, other metabolites - 6-dezetildrotaverin and 4-dezetildrotaveraldin. An elimination half-life (T1/2) - 8-10 h. For 72 h more than 50% by kidneys (it is preferential in the form of metabolites) and about 30% intestines are practically brought out of an organism. Not changed Drotaverinum in urine is not found.

Indications to use:

Spasm of smooth muscles at zayobolevaniye of biliary tract: the cholecystolithiasis, a cholangiolithiasis, cholecystitis, a pericholecystitis, holanyogit, an inflammation of a nipple of a 12-perstny gut.

Spasm of smooth muscles at diseases of urinary tract: нефроуролитиаз, уретролити­аз, pyelitis, cystitis, bladder spasm. As auxiliary therapy: at spasms of a smooth muskuyolatura of a GIT: a peptic ulcer a zheyoludka 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.

During the carrying out some tool issleyodovaniye, including cholecystography.

Route of administration and doses:

Inside, it is not dependent on meal. The adult on 40-80 mg to 3 times a day, the maximum daily dose - 240 mg. The maximum daily dose for children at the age of 3-6 years makes 40 mg, divided into 2 receptions; for children from 6 to 12 years - 80 mg, divided into two receptions; for children over 12 years - 160 mg, divided into 2 - 4 receptions.

Features of use:

Pregnancy and lactation. Use of drug during pregnancy is recommended only if the estimated advantage for mother exceeds potential risk for a fruit.

Due to the lack of necessary clinical data, it is not recommended to appoint Drotaverinum in the period of a lactation (breastfeeding).

At patients with the low and unstable ABP treatment should be carried out under control of the ABP.

Influence on ability to manage vehicles and mechanisms. During treatment it is necessary to abstain from control of vehicles and occupations other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Dizziness, heartbeat, lowering of arterial pressure, feeling of heat, perspiration, allergic skin reactions.

Interaction with other medicines:

At simultaneous use weakens protivoparkinsonichesky effect of a levodopa (strengthening of rigidity and a tremor).

Strengthens spasmolytic action of a papaverine, Bendazolum and other spasmolysants (including m-holinoblokatorov).

Reduces spazmogenny activity of morphine. Phenobarbital strengthens spasmolytic action of Drotaverinum.

Contraindications:

Hypersensitivity to active ingredient or to any of drug excipients. Heavy liver or renal failure. Heavy chronic heart failure. Children's age up to 3 years. Feeding period breast.

With care. With care appoint to patients with the expressed atherosclerosis of coronary arteries, a prostate hyperplasia, glaucoma, during pregnancy and breastfeeding.

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.

Assistance measures at overdose: drug withdrawal, a gastric lavage, reception of absorbent carbon, giving to the patient of horizontal position with the raised legs, a symptomatic treatment (the measure directed to maintenance of the ABP).

Storage conditions:

In the dry, protected from light place at a temperature not above 30 °C. To store in the place, unavailable to children. A period of validity - 3 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

Without recipe

Packaging:

Tablets on 40 mg. Packaging: on 10 or 20 tablets in a blister strip packaging from a film of polyvinyl chloride and flexible packaging on the basis of aluminum foil for medicines or in a blister strip packaging from flexible packaging on the basis of aluminum foil for medicines. On 10,20, 30,40, 50,100 tablets in banks polymeric with the screwed covers. To bank or 1, 2, 3, 4, 5, 10 blister strip packagings together with the application instruction place in a pack from a cardboard.