No-spa forte, pills 80mg, 10pcs

Composition

1 tab. contains drotaverine hydrochloride 80 mg; Excipients: magnesium stearate, talc, povidone, corn starch, lactose monohydrate.

Pharmacological action

Drotaverine is a derivative of isoquinoline, similar in chemical structure and pharmacological properties to papaverine, but with a stronger and longer-lasting effect. 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 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, and as a result, the inactivated form of CLCM supports muscle relaxation. In addition, cAMP 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 drotaverine with respect to Ca2+.

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 the 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 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 PDE3 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.

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

Indications

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;
• tension headaches;
• algodismenorrhea.

Contraindications

• severe renal insufficiency;
• severe hepatic impairment;
• severe heart failure (reduced cardiac output);
• breastfeeding;
• children’s age (clinical trials in children have not been carried out);
• hereditary lactose intolerance, lactase deficiency, galactosemia, a syndrome of malabsorption of glucose-galactose (due to the presence in the composition of the tablets of lactose);
• hypersensitivity to drotaverine and/or auxiliary components of the drug.

With caution, the drug is used for arterial hypotension, during pregnancy.

Side effects

The following side effects, which were considered at least possibly related to drotaverine in clinical trials, 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 isolated reports (

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

From the cardiovascular system:  sometimes-rapid heartbeat, decreased blood pressure.

From the digestive system:  sometimes – nausea, constipation.

From the immune system:  sometimes-allergic reactions (pruritus, rash, urticaria, angioedema).

Interaction

When used concomitantly with drotaverine, it is possible to reduce the antiparkinsonian effect of levodopa, i. e., increase rigidity and tremor.

When used concomitantly, drotaverine enhances the antispasmodic effect of papaverine, bendazole and other antispasmodics (including m-holinoblockers).

When used concomitantly, drotaverine reduces the spasmogenic activity of morphine.

When used concomitantly, phenobarbital increases the severity of the antispasmodic effect of drotaverine.

How to take, course of use and dosage

The drug is prescribed inside.

Usually, the average daily dose is 120-240 mg in 2-3 divided doses.

Overdose

Overdose of drotaverine has been associated with cardiac arrhythmia and conduction disorders, 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 should be carried out and aimed at maintaining the basic functions of the body.

Functional features

Suction

Compared to papaverine, drotaverine is absorbed faster and more completely from the gastrointestinal tract when taken orally. The absorption rate is 100%. After metabolism, during the” first pass ” through the liver,65% of the accepted dose of drotaverine enters the systemic bloodstream. C_max in blood plasma is reached in 45-60 minutes.

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

Drotaverine is evenly distributed in the tissues, penetrates into smooth muscle cells. It does not penetrate the BBB. Drotaverine and / or its metabolites can 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.

Elimination

of T_1/2 is 8-10 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 in bile). Drotaverine is mainly excreted as metabolites; unchanged drotaverine is not detected in the urine.

Special instructions

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

Each tablet of No-spa® forte contains 104 mg of lactose. When taken according to the recommended dosage regimen, each dose may contain up to 156 mg of lactose (1.5 tablets of No-spa ® forte), which may cause gastrointestinal disorders in patients suffering from lactose intolerance. This form of the drug is unacceptable for patients with lactase deficiency, galactosemia or glucose / galactose malabsorption syndrome.

Influence on the ability to drive motor vehicles and manage mechanisms

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

If any adverse reactions occur, the question of driving vehicles and working with mechanisms requires individual consideration. In case of dizziness after taking the drug, the patient should avoid engaging in potentially dangerous activities, such as driving vehicles and working with mechanisms.

Storage conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C.

Active ingredient

Drotaverine

Dosage form

Tablets

Description

For adults, Pregnant women as prescribed by a doctor

Indications

Gastrointestinal Spasm, Colitis, Threatened Miscarriage, Cholecystitis, Cholelithiasis, Urolithiasis