No-shpa, 40 mg tablets 6 pcs

Pharmgroup:

The antispasmodic agent.

Pharmic action:

No-spa is a myotropic antispasmodic, isoquinoline derivative. It has a powerful antispasmodic effect on smooth muscles by inhibiting the enzyme FDE. PDE enzyme is required for hydrolysis of cAMP to AMP. Inhibition of FDE 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 (CLKM).

Phosphorylation of CLSM leads to a decrease in its affinity for the Ca2+-calmodulin complex; as a result, the inactivated form of CLSM maintains muscle relaxation. In addition, cAMP affects the cytosolic concentration of Ca2+ ion by stimulating Ca2+ transport into the extracellular space and the sarcoplasmic reticulum. This lowering of Ca2+-ion concentration by drotaverine through the cAMP explains the antagonistic effect of drotaverine with respect to Ca2+.

In vitro, drotaverine inhibits the FDE4 isoenzyme without inhibiting the FDE3 and FDE5 isoenzymes. Therefore, the effectiveness of drotaverine depends on the concentration of FDE4 in tissues (FDE4 content varies in different tissues). FDE4 is most important for inhibition of contractile activity of smooth muscles, therefore selective inhibition of FDE4 may be useful for treatment of hyperkinetic dyskinesias and various diseases accompanied by spastic state of GIT.

The hydrolysis of CAMP in the myocardium and vascular smooth muscle occurs primarily through the FDE3 isoenzyme, which explains the fact that with high antispasmodic activity, drotaverine has no serious cardiovascular side effects 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.

Indications

Active ingredient

Composition

Active ingredient:

drotaverine hydrochloride;

Additives:

Magnesium stearate;

Talc;

Povidone;

Corn starch;

Lactose monohydrate;

How to take, the dosage

Ingestion.

The average daily dose is usually 120-240 mg (the daily dose is divided into 2-3 doses).

Interaction

Levodopa. When used concomitantly, drotaverine may weaken the anti-Parkinsonian effect of levodopa, i.e., increase stiffness and tremor.

Papaverine, bendazole and other antispasmodics (including m-cholinolytics). Increased antispasmodic action.

Morphine. Reduction of the spasmogenic activity of morphine.

Phenobarbital. Enhancement of the antispasmodic action of drotaverine.

Special Instructions

The use of the drug in case of arterial hypotension requires increased caution.

Each tablet contains 104 mg of lactose.

Lactose can take up to 156 mg (1.5 tablets) when taken, which can cause GI disorders in patients who are lactose intolerant.

The tablets are not appropriate for patients with lactose deficiency, galactosemia, or impaired glucose/galactose absorption syndrome (see Contraindications).

Impact on the ability to drive a car or perform work requiring increased speed of physical and mental reactions.

When taken orally in therapeutic doses, drotaverine has no effect on the ability to drive and perform work requiring increased attention.

If any side effects occur, driving and operating machinery require individual consideration.

In case of dizziness, potentially hazardous activities such as driving and operating machinery should be avoided.

Contraindications

With caution: arterial hypotension.

Side effects

Systemic system disorders: rarely – palpitations, decreased blood pressure.

CNS disorders: rarely – headache, dizziness, insomnia.

Gastrointestinal disorders: rarely – nausea, constipation.

The immune system: rare – allergic reactions (angioedema, urticaria, rash, itching); unknown frequency – when using the drug it was reported the development of anaphylactic shock with fatal and non-fatal outcome.

Overdose

Symptoms: cardiac rhythm and conduction disorders, including complete Gis bundle leg block and cardiac arrest, which can be fatal.

Treatment: In cases of overdose, patients should be under medical supervision and, if necessary, they should be given symptomatic and supportive treatment for basic body functions, including induction of vomiting or gastric lavage.

Pregnancy use

During pregnancy and lactation can be used when indicated.

It is contraindicated in children under 6 years of age.

Similarities