No-spa Forte tablets 80mg, No. 24

• Spasms of smooth muscles in diseases of the biliary tract: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, inflammation of the duodenal papilla.

• Spasms of smooth muscles in diseases of the urinary tract: nephrolithiasis, urethrolithiasis, pyelitis, cystitis, bladder spasms.

As adjunctive therapy:

• with spasms of smooth muscles of the gastrointestinal tract: gastric ulcer and duodenal ulcer, gastritis, spasms of the cardia and pylorus, enteritis, colitis, spastic colitis with constipation and irritable bowel syndrome with flatulence;

• with tensor headaches (tension headaches); with algodismenorrhea.

The drug is taken orally. Usually, the average daily dose is 120-240 mg (the daily dose is divided into 2-3 doses).

1 tablet contains:

active substance : drotaverine hydrochloride - 80 mg;

excipients : magnesium stearate, talc, povidone, corn starch, lactose monohydrate.

• Hypersensitivity to drotaverine and / or excipients that make up the drug.

• Severe hepatic or renal impairment.

• Severe heart failure (decreased cardiac output).

• Breastfeeding period (see section 'Pregnancy and lactation').

• Children's age (no clinical studies have been conducted in children).

• Hereditary lactose intolerance, lactase deficiency, galactosemia or glucose / galactose malabsorption syndrome (due to the presence of lactose in the preparation) (see 'Special instructions').

Carefully

With arterial hypotension.

In pregnant women (see section 'Pregnancy and lactation'). Pregnancy and lactation

According to the limited amount of retrospective data on the use of the drug in humans and data from studies in animals when taking drotaverine orally, there was no evidence of its teratogenic or embryotoxic effect, as well as an adverse effect on the course of pregnancy. Despite this, when using the drug in pregnant women, caution should be exercised and the drug should be prescribed only after careful weighing of the balance of benefits and risks for the mother and risks for the child.

Studies on the excretion of drotaverine into breast milk in animals have not been carried out. Due to the lack of such studies in animals and clinical data, it is not recommended to prescribe drotaverine during lactation.

Trade name : NO-SHPAЃ forte

International (non-proprietary) name : drotaverin

Chemical rational name : 1- (3,4-Diethoxyphenyl) methylene-6,7-diethoxy-1,2,3,4-tetrahydroisoquinoline (as hydrochloride)

Dosage form : tablets

Composition

1 tablet contains:

active substance : drotaverine hydrochloride - 80 mg;

excipients : magnesium stearate, talc, povidone, corn starch, lactose monohydrate.

Description

Oblong biconvex tablets, yellow with a greenish or orange tinge, engraved with 'NOSPA' on one side and a fracture line on the other side.

Pharmacotherapeutic group : antispasmodic agent

ATX code : A03AD02

Pharmacological properties

Pharmacodynamics

Drotaverine is an isoquinoline derivative, which is similar in chemical structure and pharmacological properties to papaverine, but has a stronger and longer-lasting effect. Drotaverine has a powerful antispasmodic effect on smooth muscles by inhibiting the enzyme phosphodiesterase (PDE). The enzyme phosphodiesterase is required for the hydrolysis of cAMP (cyclic adenosine-3 ', 5'-monophosphate) to AMP (adenosine-5'-monophosphate). Inhibition of the enzyme phosphodiesterase leads to an increase in the concentration of cAMP, which triggers the following cascade reaction: high concentrations of cAMP activate cAMP-dependent phosphorylation of myosin light chain kinase (MLCK). Phosphorylation of MLCK leads to a decrease in its affinity for the Ca2 + -calmodulin complex,as a result, the inactivated form of MLCK maintains muscle relaxation. cAMP, in addition, affects the cytosolic concentration of the Ca2 + ion by stimulating the transport of Ca2 + into the extracellular space and the sarcoplasmic reticulum. This effect of drotaverine on a decrease in the cytosolic concentration of the Ca2 + ion through cAMP explains its antagonistic effect with respect to Ca2 +.

In vitro, drotaverine inhibits the PDE IV isozyme without inhibiting the PDE III and PDE V isoenzymes. Therefore, the effectiveness of drotaverine depends on the concentrations of PDE IV in tissues, the content of which differs in different tissues. PDE IV is most important for suppressing the contractile activity of smooth muscles, and therefore selective inhibition of PDE IV can be useful for the treatment of hyperkinetic dyskinesias and various diseases accompanied by a spastic state of the gastrointestinal tract.

Hydrolysis of cAMP in the myocardium and vascular smooth muscle occurs mainly with the help of the isoenzyme PDE III, which explains the fact that with high antispasmodic activity, drotaverine does not have serious side effects from the heart and blood vessels and pronounced effects on the cardiovascular system.

Drotaverine is effective for smooth muscle spasms of both neurogenic and muscular origin. Regardless of the type of autonomic innervation, drotaverine relaxes the smooth muscles of the gastrointestinal tract, biliary tract, genitourinary system, and blood vessels.

Due to its vasodilating action, drotaverine improves tissue blood supply.

Pharmacokinetics

Compared with papaverine, when taken orally, drotaverine is absorbed faster and more completely from the gastrointestinal tract. Absorption is 100%. However, after metabolism during the 'first pass through the liver', 65% of the dose taken enters the systemic circulation. The maximum plasma concentration (Cmax) is reached after 45-60 minutes.

In vitro, drotaverine has a high binding to plasma proteins (95-97%), especially albumin,? and? - globulins.

Drotaverine is evenly distributed throughout the tissues, penetrates into smooth muscle cells. Does not penetrate the blood-brain barrier. Drotaverine and / or its metabolites can slightly penetrate the placental barrier.

In humans, drotaverine is almost completely metabolized in the liver by O-desethylation. Its metabolites are rapidly conjugated with glucuronic acid. The main metabolite is 4'-desethyldrotaverine, in addition to which 6-desethyldrotaverine and 4'-desethyldrotaverine have been identified.

The half-life of drotaverine is 8-10 hours.

Within 72 hours, drotaverine is almost completely excreted from the body, more than 50% of the drug is excreted by the kidneys (mainly in the form of metabolites) and about 30% through the gastrointestinal tract (excretion into bile). Unchanged drotaverine is not detected in urine.

Indications for use

• Spasms of smooth muscles in diseases of the biliary tract: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, inflammation of the duodenal papilla.

• Spasms of smooth muscles in diseases of the urinary tract: nephrolithiasis, urethrolithiasis, pyelitis, cystitis, bladder spasms.

As adjunctive therapy:

• with spasms of smooth muscles of the gastrointestinal tract: gastric ulcer and duodenal ulcer, gastritis, spasms of the cardia and pylorus, enteritis, colitis, spastic colitis with constipation and irritable bowel syndrome with flatulence;

• with tensor headaches (tension headaches); with algodismenorrhea.

Contraindications

• Hypersensitivity to drotaverine and / or excipients that make up the drug.

• Severe hepatic or renal impairment.

• Severe heart failure (decreased cardiac output).

• Breastfeeding period (see section 'Pregnancy and lactation').

• Children's age (no clinical studies have been conducted in children).

• Hereditary lactose intolerance, lactase deficiency, galactosemia or glucose / galactose malabsorption syndrome (due to the presence of lactose in the preparation) (see 'Special instructions').

Carefully

With arterial hypotension.

In pregnant women (see section 'Pregnancy and lactation'). Pregnancy and lactation

According to the limited amount of retrospective data on the use of the drug in humans and data from studies in animals when taking drotaverine orally, there was no evidence of its teratogenic or embryotoxic effect, as well as an adverse effect on the course of pregnancy. Despite this, when using the drug in pregnant women, caution should be exercised and the drug should be prescribed only after careful weighing of the balance of benefits and risks for the mother and risks for the child.

Studies on the excretion of drotaverine into breast milk in animals have not been carried out. Due to the lack of such studies in animals and clinical data, it is not recommended to prescribe drotaverine during lactation.

Method of administration and dosage

The drug is taken orally. Usually, the average daily dose is 120-240 mg (the daily dose is divided into 2-3 doses).

Side effect

The following side effects, which in clinical studies were regarded as at least possibly associated with drotaverine, are given in accordance with the following gradation of frequency of their occurrence: very often (1/10), often (? 1/100, 1/10) ; rarely (? 1/1000, 1/100); sometimes (? 1/10000, 1/1000); very rare (including isolated messages) (1/10000); unknown frequency (it is impossible to determine the frequency of occurrence from the available data) and are grouped by organ systems.

From the nervous system

Sometimes: headache, dizziness, insomnia.

On the part of the cardiovascular system

Sometimes: rapid heartbeat, decreased blood pressure.

From the gastrointestinal tract

Sometimes: nausea, constipation.

From the immune system

- Sometimes - allergic reactions (angioedema, urticaria, rash, itching) (see section 'Contraindications').

Overdose

In the event of an overdose, patients should be under medical supervision and, if necessary, they should be treated symptomatic and aimed at maintaining the basic functions of the body.

There are no data on drug overdose.

Interaction with other medicinal products

With levodopa

With simultaneous use, drotaverine can weaken the antiparkinsonian effect of levodopa, that is, increase rigidity and tremor.

With papaverine, bendazole and other antispasmodics (including m-anticholinergics)

Strengthening the antispasmodic action.

With morphine

Reducing the spasmogenic activity of morphine. With phenobarbital

Strengthening the antispasmodic effect of drotaverine.

special instructions

The use of the drug for arterial hypotension requires increased caution.

Each No-shpaЃ forte tablet contains 104 mg of lactose. When taken according to the recommended dosing regimen, up to 156 mg of lactose (1.5 No-shpaЃ forte tablets) can be supplied with each dose, which can cause gastrointestinal disturbances in patients suffering from lactose intolerance. This form of the drug is unacceptable for patients suffering from lactase deficiency, galactosemia or glucose / galactose malabsorption syndrome.

Influence on the ability to drive a car and other mechanisms

When taken orally in therapeutic doses, drotaverine does not affect the ability to drive vehicles and perform work that requires increased attention. If any side effects appear, the question of driving a vehicle or engaging in other potentially hazardous activities requires individual consideration. If dizziness occurs, you should avoid engaging in potentially hazardous activities, such as driving and working with machinery.

Release form

Tablets 80 mg.

10 tablets in a blister of aluminum foil / aluminum foil laminated with polymer.

10 tablets in a PVC / aluminum foil blister.

2 blisters with instructions for use in a cardboard box.

24 tablets in a PVC / aluminum foil blister.

1 blister with instructions for use in a cardboard box.

Storage conditions

Store at a temperature not exceeding 25 ? C. Keep out of the reach of children.

Shelf life

For tablets in blister aluminum foil / aluminum foil laminated with polymer: 5 years.

For tablets in PVC / aluminum foil blisters: 3 years.

Do not use the drug after the expiry date indicated on the package.

Conditions of dispensing from pharmacies

Without recipe.