No-shpa forte, tablets 80 mg 10 pcs

Drotaverine is an isoquinoline derivative with chemical structure and pharmacological properties similar to papaverine, but with stronger and more prolonged action. It has a powerful antispasmodic effect on smooth muscles by inhibiting the enzyme FDE. PDE enzyme is necessary for hydrolysis of cAMP to AMP.

PDE inhibition 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 cytosolic Ca²⁺ ion concentration by stimulating Ca²⁺ transport into the extracellular space and the sarcoplasmic reticulum. This decreasing Ca²⁺ ion concentration effect of drotaverine via 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 no pronounced cardiovascular effects.

Intake

In comparison with papaverine, drotaverine is more rapidly and completely absorbed from the gastrointestinal tract when taken orally. Absorption is 100%. After metabolism during “first passage” through the liver, 65% of the administered dose of drotaverine enters the systemic bloodstream. C_max in plasma is reached after 45-60 min.

Distribution

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

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

Metabolism

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

Excretion

T_1/2 is 8-10 h.

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

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 urogenital system.

Due to its vasodilator effect, drotaverine improves blood supply to tissues.

Indications

Urolithiasis, Colitis, Headache, Pain, Menstrual pain (algodysmenorrhea), Painful menstruation (algodysmenorrhea), Gallstones, Colic, Gallstone disease

Auxiliary therapy:

• in spasms of the smooth muscles of the gastrointestinal tract: gastric and duodenal ulcer, gastritis, cardiac and gateway spasms, enteritis, colitis, spastic colitis with constipation and irritable bowel syndrome with flatulence;
• tension headaches;
• algodysmenorrhea.

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Active ingredient

Drotaverine

Composition

1 tablet contains drotaverine hydrochloride 80 mg;

How to take, the dosage

The drug is prescribed orally.

Average daily dose is usually 120-240 mg in 2-3 doses.

Interaction

Concomitant use with drotaverine may decrease the antiparkinsonian effect of levodopa, i.e., increase stiffness and tremor.

Concomitant use of drotaverine increases the antispasmodic effect of papaverine, bendazole and other antispasmodics (including m-cholinoblockers).

In concomitant use drotaverine reduces the antispasmodic activity of morphine.

Concomitant use of phenobarbital increases the spasmolytic effect of drotaverine.

Special Instructions

When using the drug in patients with arterial hypotension, increased caution is required.

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

Impact on ability to drive and operate machinery

Drotaverine does not affect the ability to drive and perform work requiring increased concentration when taken orally in therapeutic doses.

If any adverse reactions occur, driving and operating machinery requires individual consideration. If dizziness occurs after taking the drug, the patient should avoid potentially hazardous activities, such as driving and operating machinery.

Contraindications

• expressed renal failure;
• expressed hepatic failure;
• severe heart failure (decreased cardiac output);
• period of breastfeeding;
• childhood (no clinical studies in children);
• hereditary lactose intolerance, lactase deficiency, galactosemia, glucose-galactose malabsorption syndrome (due to the presence of lactose in the tablets);
• high sensitivity to drotaverine and/or excipients.

The drug is used with caution in case of arterial hypotension and pregnancy.

Side effects

The side effects listed below, which have been considered in clinical trials to be at least possibly related to drotaverine, are listed according to the following frequency of occurrence: Very common (≥1/10), common (≥1/100, <1/10); rare (≥1/1000, <1/100); sometimes (≥1/10,000, <1/1000); very rare, including individual reports (<1/10,000); frequency unknown (the incidence cannot be determined from available data).

Nervous system disorders: sometimes – headache, dizziness, insomnia.

Cardiovascular system disorders: sometimes – palpitations, decreased blood pressure.

The digestive system: sometimes – nausea, constipation.

The immune system: sometimes – allergic reactions (itching, rash, urticaria, angioedema).

Overdose

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

Treatment: In case of overdose, patients should be under medical supervision. If necessary, symptomatic and aimed at maintenance of basic body functions should be carried out.

Similarities

No-shpa, Drotaverine, Spasmonet, Drotaverine-Teva