No-spa tablets 40mg, No. 100

• Spasms of smooth muscles, in diseases of the biliary tract: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis;

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

As adjunctive therapy:

• 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;

• tension headaches;

• dysmenorrhea (menstrual pain).

Inside.

Adults. 1-2 tables. at one time 2-3 times a day. The maximum daily dose is 6 tablets. (which corresponds to 240 mg).

Children. Clinical studies using drotaverine with the participation of children have not been conducted.

In the case of the appointment of drotaverine to children:

- for children 6-12 years old, 1 table. at one time 1-2 times a day. The maximum daily dose is 2 tablets. (which corresponds to 80 mg).

- for children over 12 years old, 1 table. at one time 1-4 times a day or 2 tables. at one time 1-2 times a day. The maximum daily dose is 4 tablets. (which corresponds to 160 mg).

Duration of treatment without consulting a doctor. When taking the drug without consulting a doctor, the recommended duration of taking the drug is usually 1Ц2 days. If during this period the pain syndrome does not decrease, the patient should consult a doctor to clarify the diagnosis and, if necessary, change the therapy. In cases where drotaverine is used as an adjunctive therapy, the duration of treatment without consulting a doctor may be longer (2-3 days).

When using a bottle with a PE stopper equipped with a piece dispenser. Before use, remove the protective strip from the top of the bottle and the sticker from the bottom of the bottle. Place the bottle in the palm of your hand so that the dispensing hole on the bottom does not rest against your palm. Then press on the top of the bottle, causing one tablet to fall out of the dispensing hole on the bottom.

Efficiency assessment method. If the patient can easily independently diagnose the symptoms of his disease, because they are well known to him, the effectiveness of the treatment, namely the disappearance of pain, is also easily assessed by the patient. If, within a few hours after taking the maximum single dose, there is a moderate decrease in pain or no decrease in pain, or if the pain does not significantly decrease after taking the maximum daily dose, it is recommended to consult a doctor.

active substance: drotaverine hydrochloride - 40 mg;

excipients: magnesium stearate - 3 mg, talc - 4 mg, povidone - 6 mg,

corn starch - 35 mg, lactose monohydrate - 52 mg.

• Hypersensitivity to the active substance or any of the excipients of the drug;

• severe hepatic or renal impairment;

• severe heart failure (low cardiac output syndrome);

• children under 6 years of age;

• the period of breastfeeding (there are no clinical studies);

• rare hereditary galactose intolerance, lactase deficiency and glucose-galactose malabsorption syndrome (due to the presence of lactose in the preparation).

With care: arterial hypotension; pediatric patients (lack of clinical experience of use); pregnancy (see 'Application during pregnancy and lactation').

Trade name : NO-SHPAЃ

International (non-proprietary) name : Drotaverin

Dosage form : tablets

Ingredients :

Active ingredient: drotaverine hydrochloride - 40 mg;

Excipients: magnesium stearate - 3 mg, talc - 4 mg, povidone - 6 mg,

corn starch - 35 mg, lactose monohydrate - 52 mg.

Description

Round biconvex tablets of yellow with a greenish or orange tinge, with spa engraving on one side.

Pharmacotherapeutic group :

Antispasmodic agent.

ATX code : A03A D02

Pharmacological properties :

Pharmacodynamics

Drotaverine is an isoquinoline derivative that exhibits a potent antispasmodic effect on smooth muscle by inhibiting an enzyme, phosphodiesterase (PDE). The enzyme phosphodiesterase is required for the hydrolysis of cyclic adenosine monophosphate (cAMP) to adenosine monophosphate (AMP). 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 of which the inactivated form of MLCK maintains muscle relaxation. cAMP also affects the cytosolic concentration of the Ca2 + ion,by stimulating the transport of Ca2 + into the extracellular space and the sarcoplasmic reticulum. This Ca2 + ion concentration-lowering effect of drotaverin through cAMP explains the antagonistic effect of drotaverinate on Ca2 +.

In vitro, drotaverine inhibits the PDE IV isozyme without inhibiting the PDE III and PDEV isoenzymes. Therefore, the effectiveness of drotaverine depends on the concentration 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, and the genitourinary system.

Pharmacokinetics

Absorption:

After oral administration, drotaverine is rapidly and completely absorbed. After presystemic metabolism, 65% of the taken dose of drotaverine enters the systemic circulation. The maximum plasma concentration (Cmax) is reached after 45-60 minutes.

Distribution

In vitro, drotaverine has a high association with plasma transactions (95-98%), especially with albumin? and? - globumin.

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.

Metabolism

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.

Withdrawal

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

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

Indications for use

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

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

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 after exclusion of diseases manifested by the syndrome of 'acute abdomen' (appendicitis , peritonitis, ulcer perforation, acute pancreatitis, etc.).

• With tension headaches.

• With dysmenorrhea.

Contraindications

• hypersensitivity to the active substance or to any of the excipients of the drug

• Severe hepatic or renal impairment

• Severe heart failure (low cardiac output syndrome)

• Children under 6 years of age

• Breastfeeding period (lack of clinical data).

• Rare hereditary galactose intolerance, lactase deficiency and glucose-galactose malabsorption syndrome (due to the presence of lactose in the preparation).

With care :

- With arterial hypotension.

- In children (lack of clinical experience of use).

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

Method of administration and dosage

Adults

Usually, the average daily dose in adults is 120-240 mg (the daily dose is divided into 2-3 doses). The maximum single dose is 80 mg. The maximum daily dose is 240 mg.

Children

clinical studies using drotaverine with the participation of children have not been conducted.

In the case of the appointment of drotaverine to children:

- for children from 6 to 12 years old, the maximum daily dose is 80 mg, divided into 2 doses.

- for children over 12 years old, the maximum daily dose is 160 mg, divided into 2-4 doses. Duration of treatment without consulting a doctor

When taking the drug without consulting a doctor, the recommended duration of taking the drug is usually 1-2 days. If during this period the pain syndrome does not decrease, the patient should consult a doctor to clarify the diagnosis and, if necessary, change the therapy. In cases where drotaverine is used as an adjunct therapy, the duration of treatment without consulting a doctor may be longer (2-3 days).

Efficiency assessment method

If the patient can easily independently diagnose the symptoms of his disease, since they are well known to him, then the effectiveness of treatment, namely the disappearance of pain, is also easy to assess by the patient. If, within a few hours after taking the maximum single dose, there is a moderate decrease in pain or no decrease in pain, or if the pain does not significantly decrease after taking the maximum daily dose, it is recommended to consult a doctor.

Side effect

On the part of the cardiovascular system

Rare - increased heart rate, decreased blood pressure.

From the nervous system

Rare - headache, dizziness, insomnia.

From the gastrointestinal tract

Rare - nausea, constipation.

From the immune system

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

Overdose

There are no data on drug overdose.

In case of an overdose, patients should be under medical supervision and, if necessary, they should be treated symptomatic and aimed at maintaining basic body functions, including artificial induction of vomiting or gastric lavage.

Interaction with other medicinal products

With levodopa

Phosphodiesterase inhibitors like papaverine reduce the antiparkinsonian effect of levodopa. When drotaverine is prescribed simultaneously with levodopa, an increase in rigidity and tremor is possible. With other antispasmodics, including m-anticholinergics. Mutual enhancement of antispasmodic action.

Drugs that significantly bind to plasma proteins (more than 80%)

Drotaverine binds significantly to plasma proteins, mainly albumin,

Y and B-globulins (see section 'Pharmacokinetics'). There is no data on the interaction of drotaverine. with drugs that significantly bind to plasma proteins, however, there is a hypothetical possibility of their interaction with drotaverine at the level of protein binding (displacement of one of the drugs by another from the bond with the protein and an increase in the concentration of the free fraction in the blood of a drug with a less strong bond with protein), which is hypothesized may increase the risk of pharmacodynamic and / or toxic side effects of this drug.

special instructions

No-shpaЃ 40 mg tablets contain 52 mg of lactose. It can cause gastrointestinal complaints in individuals with lactose intolerance. This form is unacceptable for patients suffering from lactose deficiency, galactosemia or impaired glucose / galactose absorption syndrome (see section 'Contraindications').

Pregnancy and lactation

As shown by animal reproduction experiments and retrospective studies of clinical data, the use of drotaverine during pregnancy does not lead to either teratogenic or embryotoxic effects. However, the use of the drug is recommended only after careful weighing of the balance of benefits and risks.
Due to the lack of the necessary clinical data during lactation, it is not recommended to prescribe.

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 and perform work that requires increased attention. If any side effects appear, the question of driving transport and working with mechanisms requires individual consideration. In case of dizziness after taking the drug, you should avoid engaging in potentially hazardous activities, such as driving and working with machinery.

Release form

Tablets 40 mg.

6, 10 or 20 tablets per PVC / Aluminum blister.

1, 2.4 or 5 blisters of 6 tablets with instructions for use in a cardboard box.

3 blisters of 10 tablets with instructions for use in a cardboard box.

1 blister of 20 tablets with instructions for use in a cardboard box.

10 tablets per blister Aluminum / Aluminum (polymer laminated).

ѕо 2 блистера с инструкцией по применению в картонную пачку.

ѕо 60 или 64 таблетки во флакон из полипропилена с полиэтиленовой пробкой,

снабженной штучным дозатором.

ѕо 1 флакону с инструкцией по применению в картонную пачку.

ѕо 100 таблеток во флакон из полипропилена с полиэтиленовой пробкой.

ѕо 1 флакону с инструкцией по применению в картонную пачку.

—рок годности

?л¤ таблеток в блистерах јлюминий/јлюминий: 5 лет. ?л¤ таблеток в блистерах ѕ¬’/јлюминий: 3 года.

?л¤ таблеток во флаконах: 5 лет.

Ќе примен¤ть препарат после истечени¤ срока годности, указанного на упаковке.

”слови¤ хранени¤

?л¤ таблеток в блистерах јлюминий/јлюминий: хранить при температуре не выше 30 ?—.

?л¤ таблеток в блистерах ѕ¬’/јлюминий: хранить при температуре не выше 25 ?—. ?л¤ таблеток во флаконах: хранить в защищенном от света месте при температуре от 15?— до 25?—. ’ранить в недоступном дл¤ детей месте.

”слови¤ отпуска из аптек

Ѕез рецепта