No-shpa - instructions for use, doses, side effects, contraindications

In one ampoule (2 ml) contains the active substance: drotaverina hydrochloride - 40 mg; auxiliary substances: sodium disulfite (sodium metabisulphite) -2.0 mg, ethanol 96% - 132.0 mg, water for injection up to 2.0 ml.

Description:

Transparent liquid is greenish-yellow in color.

Pharmacotherapeutic group:antispasmodic

ATX: & nbsp

A.03.A.D.02 Drotaverine

Pharmacodynamics:

Drotaverin is a derivative of isoquinoline, which exhibits a powerful spasmolytic effect on smooth muscle by inhibiting the enzyme phosphodiesterase (PDE). The enzyme phosphodiesterase is necessary for the hydrolysis of c-AMP to AMP. Inhibition of the enzyme phosphodiesterase leads to an increase in the concentration of c-AMP, which triggers the following cascade reaction: high concentrations of c-AMP activate c-AMP dependent phosphorylation of myosin light chain kinase (CMLC).Phosphorylation of CMLC leads to a decrease in its affinity for calcium (Ca2 +) - calmodulin complex, as a result of which the inactivated form of CLCM supports muscular relaxation. c-AMP also affects the cytosolic Ca2 + concentration, by stimulating the transport of Ca2 + into the extracellular space and the sarcoplasmic reticulum. This C2 + -reducing effect of drotaverin via c-AMP explains the antagonistic effect of drotaverin relative to Ca2 +.

In vitro drotaverin inhibits the isoenzyme PDE-4, without inhibiting the isoenzymes PDE-3 and PDE-5. Therefore, the effectiveness of drotaverine depends on the concentrations of PDE-4 in tissues, the content of which differs in different tissues. PDE-4 is most important for suppressing the contractile activity of smooth muscle, and therefore selective inhibition of PDE-4 can be useful for the treatment of hyperkinetic dyskinesias and various diseases accompanied by the spastic state of the gastrointestinal tract.

The hydrolysis of c-AMP in the myocardium and smooth musculature of the vessels occurs mainly with the use of isoenzyme PDE-3, which explains the fact,that at a high spasmolytic activity in drotaverine there are no serious side effects from the heart and vessels and pronounced effects on the cardiovascular system.

Drotaverine is effective in spasms of smooth muscles of both neurogenic and muscular origin. Regardless of the type of vegetative innervation, drotaverine has a relaxing effect on the smooth musculature of the gastrointestinal tract, biliary tract, urogenital system.

Pharmacokinetics:

Drotaverin and / or its metabolites can penetrate insignificantly through the placental barrier.

In vitro - drotaverine has a high bond with plasma proteins (95-97%), especially with albumin, y and β-globulin, as well as a-HDL (high-density lipoproteins). In humans drotaverine almost completely metabolized by O-de-ethylation. Its metabolites are rapidly conjugated to glucuronic acid. The main metabolite is 4'-desethyltraderin, in addition to which 6-deethyldrothaverin and 4'-deethyldrothaveraldin were identified.

In humans, a two-chamber mathematical model was used to evaluate the pharmacokinetics of drotaverin.The final half-life of plasma radioactivity was 16 hours.

The half-life is 8-10 hours. For 72 hours almost completely eliminated from the body, more than 50% through the kidneys (mainly in the form of metabolites) and about 30% through the intestine. Unaltered drotaverine in the urine is not found.

Indications:

- spasms of smooth muscles associated with diseases of the biliary tract: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis.

- spasms of smooth musculature of the urinary tract: nephrolithiasis, urethrolithiasis, pyelitis, cystitis, bladder tenesmus.

As an auxiliary therapy (when the tablet form can not be used):

- with spasms of smooth muscles of gastrointestinal origin: peptic ulcer of stomach and duodenum, gastritis, spasms of cardia and pylorus, enteritis, colitis

- with gynecological diseases: dysmenorrhea.

Contraindications:

Hypersensitivity to the active ingredient or to any of the excipients of the drug.

Hypersensitivity to sodium disulfite (see section "Special instructions").

Severe hepatic or renal insufficiency.

Severe chronic heart failure.

Children's age (the use of drotaverin in children in clinical studies has not been studied).

The period of breastfeeding.

Carefully:

With arterial hypotension (danger of collapse, see section "Special instructions");

In pregnant women (see the section "Pregnancy and lactation period")

Pregnancy and lactation:

As studies on reproductive toxicity in animals and retrospective studies of clinical data have shown, the use of drotaverine during pregnancy did not have teratogenic or embryotoxic effects. Nevertheless, with the administration of drotaverin, pregnant women should be cautious and apply it only when the potential benefit to the mother exceeds the potential risk to the fetus, while the prescription of an injectable dosage form of No-shpa® in pregnant women should be avoided. The drug should not be used during labor (the potential risk of postpartum atonic bleeding).

Due to the lack of the necessary clinical data during lactation, it is not recommended to prescribe the drug.

Dosing and Administration:

Adults:

The daily average dose is 40-240 mg of drotaverine hydrochloride (divided by 1-3 doses per day) by intramuscular injection.

In acute colic (renal or cholelithic) - 40-80 mg intravenously-slow (duration of administration is approximately 30 seconds).

Side effects:

Below are the adverse reactions observed in clinical trials, divided by organ systems, indicating the frequency of their occurrence in accordance with the following grades: very frequent (> 10%), frequent (> 1% and <10%); infrequent (> 0,1 and <1%); rare (> 0.01% and <0.1%) and very rare, including individual messages (<0.01%), unknown frequency (according to the available data, the frequency can not be determined).

From the side of the cardiovascular system

Rare - increased heart rate, lower blood pressure.

From the nervous system

Rare - headache, dizziness, insomnia.

From the gastrointestinal tract

Rarely - nausea, constipation.

From the immune system

Rare - allergic reactions (angioedema, urticaria, rash, itching) (see the section "Contraindications").

Unknown frequency

When the drug was used, it was reported about the development of anaphylactic shock with a fatal outcome and without a fatal outcome.

Local Reactions

Rare - reactions at the injection site.

Overdose:

The overdose of drotaverin was associated with cardiac rhythm and conduction disorders, including a complete blockade of the bundle's legs and cardiac arrest, which can be fatal.

In case of an overdose, patients should be under close medical supervision and should be given symptomatic therapy and treatment aimed at maintaining the basic functions of the body.

Interaction:

FROM levodopa

Phosphodiesterase inhibitors like papaverine weaken the antiparkinsonian effect of levodopa. When administering drotaverin simultaneously with levodopa possibly increased rigidity and tremor.

FROM papaverine, bendazole and other antispasmodics (including m-cholinolytics) Drotaverin enhances the spasmolytic effect of papaverine, bendazole and other antispasmodics, including m-holinoblokatory.

With tricyclic antidepressants, quinidine and procainamide

Enhances hypotension caused by tricyclic antidepressants, quinidine and procainamide.

FROM morphine

Reduces the spasmogenic activity of morphine.

FROM phenobarbital

Phenobarbital enhances the spasmolytic effect of drotaverine.

Special instructions:

The drug contains disulfite, which can cause allergic reactions, including anaphylactic symptoms and bronchospasm in sensitive individuals, especially in people with asthma or allergic diseases in history. In case of hypersensitivity to disulfite, parenteral administration of the drug should be avoided (see the section "Contraindications").

When intravenously administered drotaverina in patients with low blood pressure, the patient should be in a horizontal position in connection with the risk of collapse.

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:

A solution for intravenous and intramuscular administration of 20 mg / ml.

Packaging:

2 ml per ampoule of dark glass (hydrolytic class, type I) with a broken fracture point.

5 ampoules per plastic contour pack without cover (pallet).

For 1 or 5 pallets with instructions for use in a cardboard box.

Storage conditions:

Store in a dark place at a temperature of 15-25 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use after the expiration date stated on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N011854 / 01

Date of registration:27.07.2010

The owner of the registration certificate:HINOIN Pharmaceutical and Chemical Products Plant, ZAO HINOIN Pharmaceutical and Chemical Products Plant, ZAO Hungary

Manufacturer: & nbsp

CHINOIN Pharmaceutical and Chemical Works, Co. Ltd. Hungary

Representation: & nbspSanofi Russia, JSCSanofi Russia, JSCRussia

Information update date: & nbsp05.07.2013

Illustrated instructions

Instructions

No-spa® (No-Spa®)