No-spa pills 40mg, 24pcs

Composition

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

Pharmacological action

Drotaverine is an isoquinoline derivative that has a powerful antispasmodic effect on smooth muscle by inhibiting 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 an increase in cAMP concentration, which triggers the following cascade reaction: high cAMP concentrations activate cAMP-dependent phosphorylation of myosin light chain kinase (MLCM). Phosphorylation of CLCM leads to a decrease in its affinity for the Ca2+ – calmodulin complex, as a result of which the inactivated form of CLCM supports muscle relaxation. cAMP also affects the cytosolic concentration of the Ca2+ ion by stimulating the transport of Ca2+ into the extracellular space and sarcoplasmic reticulum. This Ca2+ – lowering effect of drotaverine via cAMP explains the antagonistic effect of drotaverinate with respect to Ca2+.

In vitro, drotaverine inhibits the PDE IV isoenzyme 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 varies 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.

cAMP hydrolysis 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 from the heart and blood vessels and pronounced effects on the cardiovascular system.

Drotaverine is effective in treating smooth muscle spasms of both neurogenic and muscular origin. Regardless of the type of vegetative innervation, drotaverine relaxes the smooth muscles of the gastrointestinal tract, biliary tract, and genitourinary system.

Pharmacokinetics

Absorption rate:

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

In vitro Distribution drotaverine has a high association with plasma proteins (95-98%), especially with albumin γ and β-globumins.

Drotaverine is evenly distributed throughout the tissues, penetrates into smooth muscle cells. It does not cross the blood-brain barrier. Drotaverine and / or its metabolites may only slightly cross the placental barrier.

Metabolism

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

Deduction

In humans, a two-chamber mathematical model was used to evaluate the pharmacokinetics of drotaverine. The final 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 (bile excretion). Drotaverine is mainly excreted as metabolites; unchanged drotaverine is not detected in the urine.

Indications

• smooth muscle spasms 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 an adjunct therapy:

• With 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, etc. ).
• For tension headaches.
• For dysmenorrhea.

Contraindications

• hypersensitivity to the Active ingredient 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 of age
• Breast-feeding period (no clinical data available).
• Rare hereditary problems of galactose intolerance, lactase deficiency, and glucose-galactose malabsorption syndrome (due to the presence of lactose in the drug).

With caution:

– With arterial hypotension.

– In children (lack of clinical experience).

– In pregnant women

Side effects

Below are the adverse reactions observed in clinical trials, divided by system, organ, and frequency of occurrence in accordance with the following gradations: very frequent (≥ 10%), frequent (≥1%, <10); infrequent (≥0,1%, < 1%); rare (≥0.01%, < 0.1%) and very rare, including individual reports (

From the cardiovascular system

Rare – increased heart rate, decreased blood pressure.

Nervous system disorders

Rare – headache, dizziness, insomnia.

From the gastrointestinal tract

Rare – nausea, constipation.

From the immune system

Rare-allergic reactions (angioedema, urticaria, rash, pruritus)

Interaction

With levodopa

Phosphodiesterase inhibitors, such as papaverine, reduce the antiparkinsonian effect of levodopa. When drotaverine is administered simultaneously with levodopa, it is possible to increase rigidity and tremor. With other antispasmodic agents, including m-holinoblokatorov Mutual strengthening of antispasmodic action.

Drugs that significantly bind 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 significantly bind to plasma proteins, however, there is a hypothetical possibility of their interaction with drotaverin at the protein binding level (displacement of one of the drugs by another from the protein binding and an increase in the concentration of the free fraction in the blood of the drug with a less strong protein binding), which hypothetically may increase the risk of pharmacodynamic and/or toxic side effects of this drug.

How to take, course of use 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

No clinical trials involving drotaverine have been conducted in children.

If drotaverine is prescribed 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 the pain syndrome 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 adjunctive 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, is also easily assessed by the patient. If there is a moderate reduction in pain or no reduction in pain within a few hours after taking the maximum single dose, or if the pain does not significantly decrease after taking the maximum daily dose, it is recommended to consult a doctor.

Overdose

There are no data on overdose of the drug.

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 vomiting or gastric lavage.

Special instructions

No-shpa 40 mg tablets contain 52 mg of lactose. This can cause gastrointestinal complaints in people who are lactose intolerant. This form is not acceptable for patients suffering from lactose deficiency, galactosemia, or impaired glucose/galactose absorption syndrome.

Pregnancy and lactation

Animal reproduction experiments and retrospective studies of clinical data have shown that 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 benefit-risk ratio. Due to the lack of necessary clinical data, it is not recommended to prescribe during lactation.

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

Active ingredient

Drotaverine

Dosage form

Tablets