Nosh-Bra - instructions for use, doses, side effects, contraindications

Potato starch is 37.98 mg, milk sugar (lactose monohydrate) is 56.00 mg, low molecular weight polyvinylpyrrolidone (povidone) is 3.36 mg, talc is 1.40 mg, magnesium stearate is 1.26 mg.

Description:

Ploskotsilindricheskie tablets of yellow or yellow with a greenish shade of color with a facet and a risk. "Marble" is allowed.

Pharmacotherapeutic group:Spasmolytic agent

ATX: & nbsp

A.03.A.D.02 Drotaverine

Pharmacodynamics:

Drotaverin is a myotropic antispasmodic, an isoquinoline derivative. The chemical structure and pharmacological properties are close to papaverine, but it has a more pronounced and long-lasting effect. Drotaverine Effective in spasms of smooth muscles, both neurogenic and muscular.

Spasmolytic effect on smooth muscle is due to inhibition of type 4 phosphodiesterase (PDE-4). PDE-4 hydrolyses cyclic adenosine monophosphate (cAMP) to AMP. Inhibition of PDE-4 leads to an increase in the concentration of cAMP, which activates cAMP-dependent phosphorylation of myosin light chain kinase (CMLC). Phosphorylation of CMLC leads to a decrease in its affinity for Ca²⁺- calmodulin complex, as a result of which the inactivated form of CLCM supports muscular relaxation. cAMP, in addition, affects the cytosolic concentration of Ca²⁺, due to the stimulation of transport of Ca²⁺ in the extracellular space and sarcoplasmic reticulum.

In vitro drotaverin inhibits PDE-4 isoenzyme without inhibition of PDE-3 isoenzymes and PDE-5, so the effectiveness of drotaverine depends on the activity of PDE-4, the content of which in different tissues is different. High content of PDE-4 is noted in the bile and urinary tract, uterus, gastrointestinal tract. The hydrolysis of cAMP in the myocardium and smooth muscles of blood vessels is mainly due to PDE-3, therefore drotaverine less affects the cardiovascular system.

Pharmacokinetics:

When taken orally, it is quickly and completely absorbed in the gastrointestinal tract. It is affected by the effect of "first passage" through the liver (the amount determined in the systemic blood flow is 65% of the dose taken). Time to reach the maximum concentration (TCmah) - 45-60 minutes.

Communication with plasma proteins - 95-97%, mainly with albumin, gamma and beta-globulins, as well as high-density lipoproteins. Evenly distributed on the tissues, penetrates into the smooth muscle cells. Does not penetrate the blood-brain barrier. Drotaverine and / or its metabolites can penetrate insignificantly through the placental barrier.

Almost completely metabolized in the liver by O-de-ethylation. Metabolites are rapidly conjugated with glucuronic acid. The main metabolite is 4'-desethyltraderin, the other metabolites are 6-deethyldrothaverin and 4'-deethyldrothaveraldin. The half-life period (T1 / 2) is 8-10 hours. For 72 hours it is practically eliminated from the body, more than 50% by the kidneys (mainly in the form of metabolites) and about 30% by the intestine. Unchanged drotaverine in the urine is not found.

Indications:

Spasm of smooth muscles in diseases of bile ducts: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, inflammation of the papilla of the duodenum.Spasm of smooth muscles in diseases of the urinary tract: nephrourolythiasis, urethrolithiasis, pyelitis, cystitis, bladder spasm. As an auxiliary therapy: with spasms of smooth muscles of the gastrointestinal tract: stomach ulcer and duodenal ulcer, gastritis, cardia and pyloric spasm, enteritis, colitis, spastic colitis with constipation and irritable bowel syndrome with flatulence; tensor headache; dysmenorrhea. In carrying out some instrumental research, incl. cholecystography.

Contraindications:

Hypersensitivity to the active ingredient or to any of the excipients of the drug. Severe hepatic or renal insufficiency. Severe chronic heart failure. Children under 3 years. The period of breastfeeding.

Carefully:

With caution appoint patients with severe coronary artery disease, prostatic hyperplasia, glaucoma, during pregnancy and breastfeeding.

Pregnancy and lactation:

The use of the drug during pregnancy is recommended only if the intended benefit to the mother exceeds the potential risk to the fetus.

Due to the lack of necessary clinical data, drotaverine it is not recommended to appoint during lactation (breast-feeding).

Dosing and Administration:

Inside, regardless of food intake.

Adults on 40-80 mg up to 3 times a day, the maximum daily dose - 240 mg. The maximum daily dose for children aged 3-6 years is 40 mg divided into 2 divided doses; for children from 6 to 12 years - 80 mg, divided into two doses; for children older than 12 years - 160 mg, divided into 2-4 admission.

Side effects:

Dizziness, palpitation, lowering blood pressure, feeling hot, sweating, allergic skin reactions.

Overdose:

Symptoms: in large doses violates atrioventricular conduction, reduces the excitability of the heart muscle, can cause heart failure and paralysis of the respiratory center.

Measures to assist with overdose: cancellation of the drug, gastric lavage, reception of activated charcoal, giving the patient a horizontal position with elevated legs, symptomatic treatment (measures aimed at maintaining blood pressure).

Interaction:

With simultaneous application weaken the antiparkinsonian effect of levodopa (increased rigidity andtremors).

Enhances the spasmolytic effect of papaverine, bendazole and other antispasmodics (including m-holinoblokatorov).

Reduces the spasmogenic activity of morphine.

Phenobarbital enhances the spasmolytic effect of drotaverine.

Special instructions:

In patients with low and unstable blood pressure, treatment should be performed under the control of blood pressure.

Effect on the ability to drive transp. cf. and fur:During the treatment period, it is necessary to refrain from driving vehicles and practicing other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Tablets of 40 mg.

Packaging:

For 10 or 20 tablets in a contour mesh package made of a polyvinylchloride film and flexible packaging based on aluminum foil for medicinal products or in a contour mesh package made of flexible packaging on the basis of aluminum foil for medicinal preparations.

For 10,20, 30,40, 50,100 tablets in cans of polymeric with screw caps. The bank or 1, 2, 3, 4, 5, 10 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Storage conditions:

In dry, the dark place at a temperature of no higher than 30 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:P N000335 / 02

Date of registration:31.07.2008 / 02.08.2013

The owner of the registration certificate:BRYNTSALOV-A, CJSC BRYNTSALOV-A, CJSC Russia

Manufacturer: & nbsp

BRYNTSALOV-A, CJSC Russia

Information update date: & nbsp21.01.2016

Illustrated instructions

Instructions

Нош-Бра® (Nos-Bra®)