But spa is a producing country. No-Shpa during breastfeeding. What is No-Shpa for injectable form?

Tradename: NO-SHPA ®

International (nonproprietary) name: Drotaverine

Dosage form: pills

Compound:

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.

Description

Round biconvex tablets, yellow with a greenish or orangish tint, with spa engraving on one side.

Pharmacotherapeutic group:

Antispasmodic.

ATX code: A03A D02

Pharmacological properties:

Pharmacodynamics

Drotaverine is an isoquinoline derivative that exhibits a powerful antispasmodic effect on smooth muscle due to inhibition of the enzyme phosphodiesterase (PDE). The enzyme phosphodiesterase is necessary for the hydrolysis of cyclic adenosine monophosphate (cAMP) to adenosine monophosphate (AMP). Inhibition of the phosphodiesterase enzyme leads to increased concentrations 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 Ca 2+ -calmodulin complex, resulting in an inactivated form of MLCK supporting muscle relaxation. cAMP also affects the cytosolic concentration of Ca 2+ ion by stimulating the transport of Ca 2+ into the extracellular space and the sarcoplasmic reticulum. This lowering Ca 2+ ion concentration effect of drotaverine through cAMP explains the antagonistic effect of drotaverine towards Ca 2+.

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

The hydrolysis of cAMP in the myocardium and vascular smooth muscle occurs mainly with the help of the PDE III isoenzyme, which explains the fact that with high antispasmodic activity, drotaverine has no serious side effects on the heart and blood vessels and no pronounced effects on the cardiovascular system.

Drotaverine is effective against 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 genitourinary system.

Pharmacokinetics

Absorption:

After oral administration, drotaverine is quickly and completely absorbed. After first-pass metabolism, 65% of the administered 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 plasma binding (95-98%), especially with albumin γ and β-globumin.

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

Metabolism

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

Removal

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

Within 72 hours, drotaverine is almost completely eliminated 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 found in the 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, bladder tenesmus.

As an adjuvant therapy:

For spasms of smooth muscles of the gastrointestinal tract: peptic ulcer of the stomach and duodenum, gastritis, spasms of the cardia and pylorus, enteritis, colitis, spastic, colitis with constipation and irritable bowel syndrome with flatulence after excluding diseases manifested by “acute abdomen” syndrome (appendicitis , peritonitis, ulcer perforation, acute pancreatitis, etc.).
For tension headaches.
For dysmenorrhea.

Contraindications

hypersensitivity to the active substance or to any of the excipients of the drug
Severe liver or kidney failure
Severe heart failure (low cardiac output syndrome)
Children under 6 years old
Breastfeeding period (no clinical data).
Rare hereditary galactose intolerance, lactase deficiency and glucose-galactose malabsorption syndrome (due to the presence of lactose in the drug).

Carefully:

For arterial hypotension.

In children (lack of clinical experience with use).

In pregnant women (see section “Pregnancy and lactation”).

Directions for use and doses

Adults

Typically, 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

There have been no clinical studies using drotaverine in children.

In case of prescribing drotaverine to children:

For children from 6 to 12 years of age, the maximum daily dose is 80 mg, divided into 2 doses.

For children over 12 years of age, 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 pain does not decrease during this period, the patient should consult a doctor to clarify the diagnosis and, if necessary, change therapy. In cases where drotaverine is used as an adjuvant therapy, the duration of treatment without consulting a doctor may be longer (2-3 days).

Performance Evaluation 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, can also be 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 decrease significantly after taking the maximum daily dose, it is recommended to consult a doctor.

Side effect

Below are the adverse reactions observed in clinical studies, divided by organ system, indicating the frequency of their occurrence in accordance with the following gradations: very common (≥ 10%), frequent (≥ 1%,<10); нечастые (≥0,1%, < 1%); редкие (≥0,01%, < 0,1%) и очень редкие, включая отдельные сообщения (< 0,01%), неизвестная частота (по имеющимся данным частоту определить нельзя).

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

Interaction with other drugs

With levodopa

Phosphodiesterase inhibitors like papaverine reduce the antiparkinsonian effect of levodopa. When prescribing drotaverine simultaneously with levodopa, increased rigidity and tremor may occur. With other antispasmodics, including m-anticholinergics Mutual enhancement of antispasmodic action.

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

Drotaverine binds significantly to plasma proteins, mainly albumin,

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

special instructions

No-shpa® 40 mg tablets contain 52 mg of lactose. This may cause gastrointestinal complaints in individuals who are lactose intolerant. This form is unacceptable for patients suffering from lactose deficiency, galactosemia or impaired glucose/galactose absorption syndrome (see section “Contraindications”).

Pregnancy and lactation

As animal reproduction experiments and retrospective studies of clinical data have shown, 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 carefully weighing the balance of benefits and risks.
Due to the lack of necessary clinical data, it is not recommended to prescribe during lactation.

Impact on the ability to drive a car and other mechanisms

When taken orally in therapeutic doses, drotaverine does not affect the ability to drive a car or perform work that requires increased attention. If any side effects occur, the issue of driving and operating machinery requires individual consideration. If dizziness occurs after taking the drug, you should avoid engaging in potentially hazardous activities, such as driving a car or operating machinery.

Release form

Tablets 40 mg.

6, 10 or 20 tablets in a PVC/Aluminium blister.

1, 2,4 or 5 blisters of 6 tablets each with instructions for use in a cardboard box.

3 blisters of 10 tablets each 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/Aluminium (laminated with polymer).

2 blisters with instructions for use in a cardboard box.

60 or 64 tablets in a polypropylene bottle with a polyethylene stopper,

equipped with a piece dispenser.

100 tablets in a polypropylene bottle with a polyethylene stopper.

1 bottle with instructions for use in a cardboard box.

Best before date

For tablets in Aluminum/Aluminium blisters: 5 years. For tablets in PVC/Aluminium blisters: 3 years.

For tablets in bottles: 5 years.

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

Storage conditions

For tablets in Aluminum/Aluminium blisters: store at a temperature not exceeding 30 °C.

For tablets in PVC/Aluminium blisters: store at a temperature not exceeding 25 °C. For tablets in vials: store in a place protected from light at a temperature of 15°C to 25°C. Keep out of the reach of children.

Conditions for dispensing from pharmacies

Over the counter

Manufacturer
Hinoin Pharmaceutical and Chemical Products Plant JSC, Hungary st. Levay 5,2112 Veresedház, Hungary.

Consumer complaints should be sent to the following address in Russia:

115035, Moscow, st. Sadovnicheskaya, 82, building 2.

pharmachologic effect

Antispasmodic agent, isoquinoline derivative. It has a powerful antispasmodic effect on smooth muscles due to inhibition of the PDE enzyme. The enzyme PDE is necessary for the hydrolysis of cAMP to AMP. Inhibition of PDE leads to an increase in cAMP concentration, 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 Ca 2+ -calmodulin complex, as a result of which the inactivated form of MLCK maintains muscle relaxation. In addition, cAMP affects the cytosolic concentration of Ca 2+ ion by stimulating the transport of Ca 2+ into the extracellular space and the sarcoplasmic reticulum. This lowering Ca 2+ ion concentration effect of drotaverine through cAMP explains the antagonistic effect of drotaverine in relation to Ca 2+.

In vitro, drotaverine inhibits the PDE4 isoenzyme without inhibiting the PDE3 and PDE5 isoenzymes. Therefore, the effectiveness of drotaverine depends on the concentration of PDE4 in tissues (the content of PDE4 in different tissues varies). PDE4 is most important for suppressing the contractile activity of smooth muscles, and therefore selective inhibition of PDE4 may be useful for the treatment of hyperkinetic dyskinesias and various diseases accompanied by a spastic state of the gastrointestinal tract.

The hydrolysis of cAMP in the myocardium and vascular smooth muscle occurs mainly with the help of the PDE3 isoenzyme, which explains the fact that with high antispasmodic activity, drotaverine has no serious side effects on the heart and blood vessels and no pronounced effects on the cardiovascular system.

Pharmacokinetics

Suction

Distribution

In vitro, drotaverine is highly bound to plasma proteins (95-98%), especially albumin, β- and γ-globulins.

Drotaverine is evenly distributed in tissues and penetrates smooth muscle cells. Does not penetrate the BBB. Drotaverine and/or its metabolites are able to slightly penetrate the placental barrier.

Metabolism

Removal

In humans, a two-chamber mathematical model was used to assess the pharmacokinetics of drotaverine. The final T1/2 of plasma radioactivity was 16 hours.

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

Indications

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

- spasms of smooth muscles of the urinary system: nephrolithiasis, urethrolithiasis, pyelitis, cystitis, bladder spasms; bladder tenesmus (parenteral).

As an adjuvant therapy:

- for spasms of smooth muscles of the gastrointestinal tract: peptic ulcer of the stomach and duodenum, gastritis, spasms of the cardia and pylorus, enteritis, colitis, spastic colitis with constipation and irritable bowel syndrome with flatulence after excluding diseases manifested by the "acute abdomen" syndrome (appendicitis, peritonitis, ulcer perforation, acute pancreatitis);

- tension headaches (for oral administration);

- dysmenorrhea.

When used as an adjuvant, the drug is administered parenterally if it is not possible to use tablets.

Dosage regimen

Clinical studies using drotaverine involving children was not carried out.

If the drug No-shpa ® is prescribed, the maximum daily dose when taken orally for children in ages 6 to 12 years is 80 mg (divided into 2 doses), for children over 12 years of age- 160 mg (divided into 2-4 doses).

Duration of treatment without consulting a doctor

Performance Evaluation Method

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

When using a bottle with a polyethylene 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 your palm 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 at the bottom.

Side effect

Below are the adverse reactions observed in clinical studies, divided by organ system, indicating the frequency of their occurrence in accordance with the following gradations: very common (≥10%), common (≥1%,<10), нечастые (≥0.1%, <1%), редкие (≥0.01%, <0.1%), очень редкие, включая отдельные сообщения (<0.01%), частота неизвестная (по имеющимся данным частоту определить нельзя).

From 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, itching, rash); frequency unknown - fatal and non-fatal anaphylactic shock has been reported.

Local reactions: rare - reactions at the injection site.

Contraindications for use

- severe renal failure;

- severe liver failure;

- severe heart failure (low cardiac output syndrome);

- children under 6 years of age (for tablets);

- children's age (for parenteral administration, since clinical studies have not been conducted in children);

- breastfeeding period (no clinical data);

- rare hereditary galactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome (for tablets, due to the presence of lactose in their composition);

- hypersensitivity to the components of the drug;

- hypersensitivity to sodium disulfite (for solution for intravenous and intramuscular administration).

WITH caution the drug is used for arterial hypotension (due to the risk of collapse), during pregnancy; in children (for tablets).

Use during pregnancy and breastfeeding

As studies of reproduction in animals and retrospective data on the clinical use of drotaverine have shown, the use of drotaverine during pregnancy had neither teratogenic nor embryotoxic effects. Despite this, when prescribing drotaverine to pregnant women, caution should be exercised and it should be used only in cases where the potential benefit to the mother outweighs the potential risk to the fetus, while prescribing the injectable dosage form of the drug No-shpa ® in pregnant women should be avoided.

The drug should not be used during childbirth (potential risk of developing postpartum atonic hemorrhage).

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

Use in children

Parenteral use in children is contraindicated.

Taking the drug orally is contraindicated for children under 6 years of age.

Overdose

Drotaverine overdose has been associated with cardiac rhythm and conduction disturbances, including complete bundle branch block and cardiac arrest, which can be fatal.

Treatment: in case of overdose, patients should be under medical supervision. If necessary, symptomatic treatment aimed at maintaining basic body functions should be carried out, including artificial induction of vomiting or gastric lavage.

Drug interactions

PDE inhibitors like papaverine reduce the antiparkinsonian effect of levodopa. When No-shpa ® is prescribed simultaneously with levodopa, rigidity and tremor may increase.

With the simultaneous use of drotaverine with other antispasmodics, including m-anticholinergics, a mutual enhancement of the antispasmodic effect occurs.

Drotaverine for IM and IV administration increases arterial hypotension caused by tricyclic antidepressants, quinidine and procainamide.

Drotaverine for IM and IV administration reduces the spasmogenic activity of morphine.

Phenobarbital enhances the antispasmodic effect of drotaverine.

Drotaverine binds significantly to plasma proteins, mainly albumin, β- and γ-globulins. There are no data on the interaction of drotaverine with drugs that are significantly bound to plasma proteins. However, we can assume the possibility of their interaction with drotaverine at the level of binding to plasma proteins - the displacement of one of the drugs by the other from the binding sites and an increase in the concentration of the free fraction in the blood of the drug with weaker binding to proteins. This could hypothetically increase the risk of pharmacodynamic and/or toxic side effects of this drug.

Conditions for dispensing from pharmacies

The drug in tablet form is approved for use as an over-the-counter product.

The drug in the form of a solution for intravenous and intramuscular administration is available with a prescription.

Storage conditions and periods

Tablets in PVC/Aluminum blisters should be stored at a temperature not exceeding 25°C. Shelf life - 3 years.

Tablets in Aluminum/Aluminium blisters should be stored at a temperature not exceeding 30°C. Shelf life - 5 years.

Tablets in polypropylene bottles and solution for intravenous and intramuscular administration should be stored in a place protected from light at a temperature of 15° to 25°C. Shelf life - 5 years.

The drug should be stored out of the reach of children.

Use for liver dysfunction

Use is contraindicated in severe liver failure.

Use for renal impairment

Use is contraindicated in severe renal failure.

special instructions

The 40 mg tablets contain 52 mg of lactose, as a result of which complaints from the digestive system are possible in patients with lactose intolerance. This form is not intended for patients with lactase deficiency, galactosemia or impaired glucose/galactose absorption syndrome.

The solution for intravenous and intramuscular administration contains sodium bisulfite, which can cause allergic reactions, including anaphylactic and bronchospasm, in sensitive individuals (especially in individuals with bronchial asthma or a history of allergic reactions). In case of hypersensitivity to sodium metabisulfite, parenteral use of the drug should be avoided.

When administering the drug intravenously to patients with low blood pressure, the patient should be in a horizontal position due to the risk of collapse.

Impact on the ability to drive vehicles and operate machinery

When taken orally in therapeutic doses, drotaverine does not affect the ability to drive vehicles or perform work that requires increased concentration.

If any adverse reactions occur, the issue of driving and operating machinery requires individual consideration. If dizziness occurs after taking the drug, you should avoid engaging in potentially hazardous activities, such as driving vehicles and working with machinery.

After parenteral administration of the drug, it is recommended to refrain from driving vehicles and engaging in other potentially hazardous activities that require high concentration and speed of psychomotor reactions.

Release form:

Tablets 6, 10 pcs. - PVC/Aluminium blisters (1, 2, 3, 4, 5) - cardboard packs.

Tablets 60, 100 pcs. - polypropylene bottles (1) with a polyethylene stopper, equipped with a piece dispenser - cardboard packs.

Solution for intravenous and intramuscular administration 2 ml - dark glass ampoules (5) - contour plastic cell packaging (1, 5) - cardboard packs.

Compound:

One tablet contains

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.

One ampoule of solution for intravenous and intramuscular administration contains

Active substance: drotaverine hydrochloride 40 mg

Excipients: sodium disulfite (sodium metabisulfite) - 2 mg, ethanol 96% - 132 mg, water for injection - up to 2 ml.

Description:

Injection: transparent liquid of greenish-yellow color.

Pills: round, biconvex, yellow, with a greenish or orange tint, with “spa” engraved on one side.

Pharmacotherapeutic group:

Organotropic agents

Pharmacological properties:

Pharmacodynamics

Myotropic antispasmodic, isoquinoline derivative. It has a powerful antispasmodic effect on smooth muscles due to inhibition of the PDE enzyme. The enzyme PDE is necessary for the hydrolysis of cAMP to AMP. Inhibition of PDE leads to an increase in cAMP concentration, 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 Ca 2+ -calmodulin complex, as a result of which the inactivated form of MLCK maintains muscle relaxation. In addition, cAMP affects the cytosolic concentration of Ca 2+ ion by stimulating the transport of Ca 2+ into the extracellular space and the sarcoplasmic reticulum. This lowering Ca 2+ ion concentration effect of drotaverine through cAMP explains the antagonistic effect of drotaverine in relation to Ca 2+.

Pharmacokinetics

Absorption. After oral administration, drotaverine is quickly and completely absorbed. After first-pass metabolism, 65% of the administered dose of drotaverine enters the systemic circulation. Cmax in plasma is reached within 45–60 minutes.

Distribution. In vitro drotaverine has a high binding to plasma proteins (95–98%), especially albumin, γ and β-globulins.

Drotaverine is evenly distributed throughout the tissues and penetrates smooth muscle cells. Does not penetrate the BBB. Drotaverine and/or its metabolites may slightly penetrate the placental barrier.

Metabolism. In humans, drotaverine is almost completely metabolized in the liver by O-desethylation. Its metabolites quickly conjugate with glucuronic acid. The main metabolite is 4"-desethyldrotaverine, in addition to which 6-desethyldrotaverine and 4"-desethyldrotaveraldine have been identified.

Excretion. In humans, a two-chamber mathematical model was used to assess the pharmacokinetics of drotaverine. The final T1/2 of plasma radioactivity was 16 hours.

Indications for use:

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

Spasms of smooth muscles of the urinary system: nephrolithiasis, urethrolithiasis, pyelitis, cystitis, bladder spasms;

As an adjuvant therapy:

For spasms of smooth muscles of the gastrointestinal tract: peptic ulcer of the stomach and duodenum, gastritis, spasms of the cardia and pylorus, enteritis, colitis, spastic colitis with constipation and irritable bowel syndrome with flatulence after excluding diseases manifested by the "acute abdomen" syndrome (appendicitis, peritonitis, perforation ulcers, acute pancreatitis);

Tension headaches (for oral administration);

Algodismenorrhea.

When used as an adjuvant, the drug is administered parenterally if it is not possible to use tablets.

Refers to diseases:

Contraindications:

The drug should not be used if any of the conditions listed below are present:

Severe renal failure;

Severe liver failure;

Severe heart failure (low cardiac output syndrome);

Children under 6 years of age (for tablets);

Children's age (for parenteral administration, since clinical studies have not been conducted in children);

Breastfeeding period (no clinical data);

Rare hereditary galactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome (for tablets, due to the presence of lactose in their composition);

Hypersensitivity to the components of the drug;

Hypersensitivity to sodium disulfite (for solution for intravenous and intramuscular administration).

WITH caution: the drug is used for arterial hypotension (due to the risk of collapse), during pregnancy; in children (for tablets).

Directions for use and dosage:

The average daily dose for intramuscular administration in adults is 40-240 mg (divided into 1-3 administrations/day). For acute colic (renal or biliary), the drug is administered intravenously slowly at a dose of 40-80 mg (duration of administration is approximately 30 seconds).

Clinical studies with the use of drotaverine have not been conducted in children.

When prescribing the drug No-shpa, the maximum daily dose when taken orally for children aged 6 to 12 years is 80 mg in 2 divided doses, for those over 12 years old - 160 mg in 2-4 divided doses.

Duration of treatment without consulting a doctor:

Efficiency evaluation method:

Side effect:

Determination of the frequency of adverse reactions: very often (≥10%), often (≥1%,<10); нечасто (≥ 0.1%, < 1%); редко (≥ 0.01%, < 0.1%), очень редко, включая отдельные сообщения (< 0.01%), частота неизвестная (по имеющимся данным частоту определить нельзя.

From the cardiovascular system: rarely – rapid heartbeat, decreased blood pressure.

From the nervous system: rarely – headache, dizziness, insomnia.

From the digestive system: rarely – nausea, constipation.

Allergic reactions: rarely - itching, rash, urticaria, angioedema.

Local reactions: rarely - reactions at the injection site.

Overdose:

There are no data on overdose of the drug No-shpa.

Treatment: in case of overdose, patients should be under medical supervision. If the drug has recently been taken orally, you can artificially induce vomiting or flush the stomach. If necessary, symptomatic treatment aimed at maintaining the basic functions of the body should be carried out.

Use during pregnancy and breastfeeding:

As studies of reproduction in animals and retrospective data on the clinical use of drotaverine have shown, the use of drotaverine during pregnancy had neither teratogenic nor embryotoxic effects.

During pregnancy, the drug should be used with caution and only in cases where the potential benefit of therapy for the mother outweighs the possible risk to the fetus.

Due to the lack of necessary clinical data, the drug is contraindicated during lactation (breastfeeding).

Interaction with other drugs:

PDE inhibitors like papaverine reduce the antiparkinsonian effect of levodopa. When No-shpa ® is prescribed simultaneously with levodopa, rigidity and tremor may increase.

When used simultaneously with drotaverine, the antispasmodic effect of papaverine, bendazole and other antispasmodics, including m-anticholinergics, is mutually enhanced.

No-spa increases arterial hypotension caused by tricyclic antidepressants, quinidine and procainamide.

No-spa reduces the spasmogenic activity of morphine.

Phenobarbital enhances the antispasmodic effect of drotaverine.

Special instructions and precautions:

The tablets contain 52 mg of lactose, as a result of which complaints from the digestive system are possible in patients suffering from lactose intolerance. Therefore, the drug in tablet form is not prescribed to patients with lactase deficiency, galactosemia or impaired glucose/galactose absorption syndrome.

When administering the drug intravenously to patients with low blood pressure, the patient should be in a horizontal position due to the risk of collapse.

When taken orally in therapeutic doses, drotaverine does not affect the ability to drive vehicles or perform work that requires increased concentration.

Storage conditions:

Tablets in aluminum/aluminium blisters should be stored at a temperature not exceeding 30°C.

Tablets in PVC/aluminum blisters should be stored at a temperature not exceeding 25°C.

Tablets in bottles and solution for intravenous and intramuscular administration should be stored in a place protected from light at a temperature of 15° to 25°C.

Best before date:

Tablets in aluminum/aluminium blisters, tablets in bottles and solution for intravenous and intramuscular administration - 5 years. Tablets in PVC/aluminum blisters - 3 years.

A drug that has a vasodilator, antispasmodic, and hypotensive effect.

Regulations for the industrial production of the drug drotaverine were developed in 1961 in Hungary, its authors were the research group of the pharmaceutical plant "Hinoin". The plant has been producing the most popular painkiller, papaverine, for over 100 years.

In the course of regular working studies, a substance was discovered that was much superior to papaverine in terms of potency and prolongation of effect. Called drotaverine, this substance became the active component of the new myotropic antispasmodic no-spa (translated from Latin as “no spasm”).

The drug NO-SPA was patented in 1962, and in 1970 its creators received a state prize. Currently, Hinoin is part of the pharmaceutical company Sanofi-Sintelabo, therefore the NO-SPA trademark, certified in many countries around the world, belongs to this company.

The Hinoin plant prepares raw materials for production independently; the plant equipment meets the requirements of European quality standards.

The high safety profile and consistently high quality of the original drug are confirmed by clinical and post-marketing studies. Safety monitoring was carried out between 1964 and 1998.

The analysis, which included results from 37 group clinical trials, assessed the effectiveness and side effects of the drug. Along with high efficiency and safety, the medicine is characterized by cost-effectiveness during long-term use.

Thanks to the combination of such advantages, the drug has confidently held the leadership among over-the-counter antispasmodics since its appearance on the pharmaceutical markets of the world.

According to statistics provided by the marketing company "Business Credit", in the group of drugs for the treatment of diseases accompanied by hypertonicity of smooth muscles, NO-SPA has for many years occupied the first position in terms of demand as a remedy with a universal spectrum of action.

Instructions for use

Clinical and pharmacological group: Myotropic antispasmodic.

Latin name: No-Spa.

Trade name (name of the drug assigned by the developer): NO-SHPA.

International nonproprietary name: Drotaverine.

Code according to the Anatomical-Therapeutic-Chemical Classification (ATC): A03A D02.

Active ingredient: drotaverine (Drotaverinum), a derivative of the heterocyclic organic compound isoquinoline.

Chemical formula: 1-(3,4-diethoxybenzylidene)-6,7-diethoxy-1,2,3,4-tetrahydroisoquinoline hydrochloride.

Gross formula: C 24 H 31 NO 4

Release forms

Pills. Biconvex tablets with an orange or green tint and one-sided engraving “spa”. One tablet contains 40 mg of drotaverine hydrochloride. Additional (auxiliary) substances: polyvinylpyrrolidone, talc, magnesium stearate, starch, lactose. Types of packaging:

Aluminum or aluminum-polyvinyl chloride blisters of 6, 20 or 24 tablets;

polypropylene bottles of 60 or 100 tablets.

Solution for intravenous and intramuscular injections. Hydrolytic class ampoules with a capacity of 2 ml made of dark glass with a printed break point. 1 ml of solution contains 20 mg of drotaverine hydrochloride. Excipients are: sodium metabisulfite, 96% ethyl alcohol, water for injection.

pharmachologic effect

In terms of pharmacological properties, No-Shpa is close to papaverine, but has a longer and stronger effect. It inhibits the entry of Ca2+ into smooth muscle cells, dilates blood vessels, and has a powerful antispasmodic effect in cases of spasms of both neurogenic and muscle origin.

The mechanism of bioaction is based on the ability of drotoverine to reduce the activity of the PDE4 enzyme. This selective inhibition allows the drug to be used for the treatment of diseases accompanied by spasms of the gastrointestinal tract, genitourinary system and biliary tract.

This same factor ensures a minimum of side effects from the cardiovascular system, since another representative of the phosphodiesterase group, PDE3, is responsible for myocardial resistance to ischemia.

It can be used as an antispasmodic when other drugs that reduce smooth muscle tone cannot be used (for example, m-anticholinergic drugs are contraindicated in glaucoma and prostate hypertrophy). No-Spa does not penetrate the central nervous system and does not affect the autonomic nervous system, does not mask the symptom of “acute abdomen”. Tolerance to the action of the drug does not occur.

Pharmacological kinetics

Compared to other myotropic antispasmodics, NO-SPA acts on the body quite gently and is well absorbed by it. The drug exhibits its effect 3-5 minutes after intramuscular administration, 2-4 minutes. after intravenous administration, and after 10–12 minutes. after taking the pill.

The maximum effect is achieved after 30 minutes; about 65% of the dose taken orally enters the circulatory system. The drug is distributed fairly evenly throughout the tissues and penetrates slightly into the fetal blood through the histohematic barrier.

Drotaverine is almost completely decomposed in the liver and is excreted from the body within 72 hours. More than 50% of metabolites are removed through the kidneys, about 30% through the gastrointestinal tract. The drug does not have cumulative properties.

Indications for use and dosage regimen

No-Shpa is indicated for:

diseases of the biliary tract (cholecystitis, papillitis, gallbladder dyskinesia, cholangitis, etc.);
diseases of the urinary tract accompanied by smooth muscle spasms (cystitis, pyelitis, nephrolithiasis, bladder tenesmus, etc.);
spastic constipation;
irritable bowel syndrome, accompanied by pain and qualitative and quantitative changes in stool;
spasm of the uterine pharynx during childbirth;
increased tone of the uterus during pregnancy;
pain due to dysmenorrhea;
tension-type headaches (“tension headache”);
attacks of hemicrania (migraine);
hypertensive crisis to lower blood pressure;
obliterating endarteritis to improve blood supply to ischemic areas;
as an adjuvant therapy for gastrointestinal diseases (gastritis, enteritis, colitis, peptic ulcer)
conducting instrumental examinations and cholecystography.

For adults, the maximum single dose of the drug is 80 mg. Recommended daily dose:

for adults 120-240 mg,
for children over 12 years old 160 mg,
for children from 6 to 12 years old 80 mg,
for children aged 1 to 6 years, no more than 120 mg.

The daily dose for children under 12 years of age is divided into 4–5 doses, for people of other age groups into 2–4 doses.

If, when taking No-Shpa without a doctor's prescription, the symptoms of spasm or pain do not subside within 2 days, the drug should not be continued. It is necessary to consult a doctor to clarify the diagnosis and the correct choice of medication.

Contraindications

hypersensitivity to drotaverine or any excipient included in the composition of the drug NO-SPA,
genetically determined galactose intolerance (malabsorption syndrome);
severe renal or liver failure;
severe heart failure;

The drug should be used with caution during arterial hypotension, pregnancy and lactation. Intramuscular and intravenous administration of the drug is not recommended for children under 18 years of age.

Side effects

The undoubted advantage of the drug is the minimal number of side effects. The drug has been used in clinical practice since 1961, and during this time not a single case of serious adverse reaction has been recorded. Today, this is one of the best indicators for drugs in the group of myotropic antispasmodics.
In 0.9% of cases of drug use, the following side effects were noted:

disorders of the nervous system in the form of headache, insomnia, dizziness;
gastrointestinal disorders - constipation, nausea;
cardiovascular disorders - rapid pulse, moderate hypotension (especially with intravenous administration), feeling of heat, increased sweating;
allergic skin reactions in the form of itching, urticaria or angioedema.

Overdose

A significant overdose of drotaverine can cause paralysis of the respiratory center, arrhythmia or serious disturbances in cardiac conduction, up to complete blockade of the bundle branches and cardiac arrest.

If an overdose is suspected, the patient should be left under medical supervision and, if necessary, artificially induce vomiting, perform gastric lavage and symptomatic treatment aimed at restoring impaired body functions.

Interaction of the drug with other drugs

Simultaneous use with other antispasmodics, including m-anticholinergics, mutually enhances their effect. Phenobarbital also enhances its antispasmodic effect.

NO-SPA does not cause side effects when used simultaneously with analgesics (paracetamol, ibuprofen, acetylsalicylic acid, diclofenac). This allows, if necessary, to carry out combination therapy, combining a vasodilator effect with an analgesic.

No-Spa, administered intramuscularly or intravenously, reduces the activity of morphine. It is necessary to combine levodopa with the antiparkinsonian drug with caution, since when used simultaneously, the effect of the latter is reduced, and, as a result, the patient experiences increased rigidity and tremor.

Drotaverine actively binds to β- and γ-globulin proteins and albumin. There is a possibility of interaction of No-Shpa with other drugs that interact with plasma proteins. When taken together, the stronger drug may displace the drug with a weaker bond, increasing its level in the blood and increasing the risk of side effects.

Precautions when taking the drug

For intravenous and intramuscular administration, it should be taken into account that injection solutions contain sodium metabisulfite, which can cause allergic reactions. Sodium pyrosulphide is included in medications as an excipient, and in people with allergic diseases or asthma it can provoke bronchospasm or anaphylactic symptoms.

When administering the drug intravenously to patients with hypotension, the patient should be placed in a horizontal position and blood pressure should be periodically monitored due to the risk of angiogenic collapse.

Since use may cause short-term dizziness or a drop in blood pressure, during the first period of taking the drug it is not recommended to drive vehicles or engage in other potentially dangerous types of work that require rapid physical reaction and increased attention. Not everyone experiences such an adverse reaction, so the degree of restrictions in each case depends on the individual characteristics of the patient’s body.

Tablets should be prescribed with caution to patients suffering from lactose intolerance, since taking the drug can cause gastrointestinal disorders in them.

If you abruptly stop taking it, a “withdrawal syndrome” typical of fast-acting drugs may occur, manifested by an exacerbation of the underlying disease. Therefore, it is recommended to discontinue the drug gradually.

In the context of compatibility with alcohol, it should be noted that alcohol significantly reduces muscle tone, distorting the effect of the active substance No-Shpa - drotaverine.

Conditions for dispensing from pharmacies

Drugs in tablet form are available over-the-counter in many countries. Drugs in the form of solutions for intravenous and intramuscular injections are available with a prescription.

Due to its high safety and minimal side effects, there is no ban on the use of the drug at the legislative level.

In some countries, for example, Great Britain and Germany, N O-SH pu forbidden Prescribed to women in the second and third trimester of pregnancy due to the risk of premature birth. These countries also restrict the use of the drug by nursing mothers. The reason is the lack of a sufficient number of clinical trials.

Storage conditions and periods

Tablets in blisters should be stored at a temperature not exceeding 25-30°C. The shelf life of the tablets, depending on the type of blister, is from 3 to 5 years.

Tablets packaged in polypropylene bottles, as well as solutions intended for intravenous and intramuscular injections, should be stored in a place protected from light at a temperature not exceeding 25°C. The shelf life of such drugs is 5 years.

Analogs

Generics, or analogues of no-shpa, are drugs registered by the manufacturer under their own name and trade name, but with the same active ingredient as in the original drug.

Generics may be inferior to the original in effectiveness due to differences in production technology and the use of different excipients. Known synonyms in which the active ingredient is drotaverine:

Drospa Forte,
No-Shpa Forte,
Ple-Spa,
Nokhshaverin,
Drotaverine Forte,
Drotaverin-Darnitsa,
Drotaverine Hydrochloride,
Drotaverine,
Spazoverin,
Spasmol,
Spasmonet,
No-H-Sha Forte,
No-H-Sha,
Spakovin,
Nosh-bra,
Drotaverine-ellara,
Drotaverine-FPO,
Drotaverine-UBF,
Drotaverin-STI,
Drotaverine-MIC,
Drotaverine-KMP
Drotaverine-AKOS
Biospa,
Bespa.

Analogues and their comparative characteristics

Drug analogues are used to treat the same diseases as the original drug, but are created on the basis of other active ingredients. Analogue drugs may have different pharmacological properties and side effects, differ in pharmacokinetics and therapeutic effect.

The most well-known analogues of No-Shpa include a group of myotropic antispasmodics, the active ingredient in which is papaverine.

Papaverine hydrochloride,
Papaverine,
Papaverine MS,
Papaverine bufus.

These drugs are the closest in pharmacological properties and are popular in the CIS countries due to their low price. However, the selectivity of the action of the original drug on smooth muscles is 5 times higher than that of papaverine drugs.

Substitutes for No-Shpa are also:

papazole (active ingredients papaverine + bendazole);
neobutin and trimedate (active ingredient trimebutin);
Niaspam, duspatalin, Sparex, mebeverine hydrochloride (active ingredient mebeverine).

These drugs are inferior in versatility in their spectrum of action. Thus, mebeverine and trimepbutine have a weak antispasmodic effect on the smooth muscles of the urinary tract and uterus.

The advantages of the mebeverine analogue include the absence of side effects such as tachycardia, dry mouth, stool disorders, and urinary retention, whereas the original drug has these side effects.

Manufacturers

Currently, NO-Shpu is produced by:

Quinoin (pharmaceutical company "Sanofi-Sintelabo", Hungary);
Niopik State Research Center (Russia);
Moskhimfarmpreparaty im. ON THE. Semashko (Russia);
Hemofarm D.D. (Yugoslavia);
Torrent Pharmaceuticals (India).

Registration of the drug and permits for its use

Issues of general regulation of the use of medicines are dealt with by an organization determined by the Federal legislation of the state. In EU member countries, procedures relating to obtaining approval for the release and use of medicinal products are carried out by the Heads of Medicines Agencies.

The sale of a medicinal product in a particular country is regulated by the Federal Law “On the Circulation of Medicines”. After receiving a certificate - an authorization document allowing the use of a drug on the territory of the state, the medicines must be:

registered with the relevant authority (in Russia this is Roszdravnadzor, in Belarus - a special commission under the Ministry of Health of the Republic of Belarus, in Ukraine - the State Expert Center of the Ministry of Health);
included in the State Register of Medicines.

The international date of first registration (IBD - International Birth Date) of No-Shpa is the date of receipt in 1961 of a certificate for the drug by the pharmaceutical company "Hinoin". In Russia, No-Shpa was last registered on July 23. 2010. Registration certificate number P N011854/02 was issued on the basis of the Order of the Ministry of Health and Medical Industry of the Russian Federation.

In Ukraine, the drug No-Shpa was produced by a pharmaceutical company GTOV "L-Pharma".However, due to the proven fact of falsification series 2V279 medicine (40 mg tablets) the sale and use of No-Shpa from this manufacturer was prohibited. Base – R Order of the State Service of Ukraine on Medicines No. 3054-1.3/2.1/17-14, dated February 17, 2014.