No-spa forte pills 80mg, 24pcs

Composition

1 tablet contains: Active ingredient: 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. Drotaverine has a powerful antispasmodic effect on smooth muscle by inhibiting the enzyme phosphodiesterase (PDE). The enzyme phosphodiesterase is necessary for the hydrolysis of cAMP (cyclic adenosine-3′,5 ‘- monophosphate) to AMP (adenosine-5′-monophosphate). 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 MLCM leads to a decrease in its affinity for the Ca2+ – calmodulin complex, as a result of which the inactivated form of MLCM 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 effect of drotaverine on lowering the cytosolic concentration of the Ca2+ ion via cAMP explains its antagonistic effect with respect to Ca2+. In vitro, drotaverine inhibits the PDE IV isoenzyme without inhibiting the PDE III and PDE V isoenzymes. Therefore, the effectiveness of drotaverine depends on the concentrations 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, genitourinary system, and blood vessels. Due to its vasodilating effect, drotaverine improves blood supply to tissues. Pharmacokinetics Compared to papaverine, drotaverine is absorbed more quickly and completely from the gastrointestinal tract when taken orally. The absorption rate is 100%. However, after metabolism, during the “first pass through the liver”,65% of the dose taken enters the systemic bloodstream. The maximum plasma concentration (Cmax) is reached after 45-60 minutes. In vitro, drotaverine is highly bound to plasma proteins (95-97%), especially to albumin, γ and β – globulins. 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. 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. The elimination half-life of drotaverine is 8-10 hours. In 72 hours, drotaverine is almost completely eliminated from the body, more than 50% of the drug is excreted by the kidneys (mainly in the form of metabolites) and about 30% through the gastrointestinal tract (excretion in bile). Unchanged drotaverine is not detected in the urine.

Indications

• Spasms of smooth muscles in diseases of the biliary tract: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, inflammation of the duodenal papilla.
• Smooth muscle spasms in diseases of the urinary tract: nephrolithiasis, urethrolithiasis, pyelitis, cystitis, bladder spasms.

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;
• with tensor headaches (tension headaches); with algodismenorrhea.

Contraindications

• Hypersensitivity to drotaverine and / or excipients included in the preparation.
• Severe hepatic or renal failure.
• Severe heart failure (decreased cardiac output).
• The period of breast-feeding (see the section “Pregnancy and lactation”).
• Children’s age (no clinical studies have been conducted in children).
• Hereditary lactose intolerance, lactase deficiency, galactosemia, or glucose / galactose malabsorption syndrome (due to the presence of lactose in the drug) (see “Special instructions”).

With caution

With arterial hypotension.

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

Based on the limited number of retrospective data on the use of the drug in humans and data from studies in animals, when taking drotaverine orally, there was no evidence of its teratogenic or embryotoxic effects, as well as adverse effects on the course of pregnancy. Despite this, caution should be exercised when using the drug in pregnant women and prescribe the drug only after careful weighing of the benefit-risk ratio for the mother and the risk to the child.

Studies on the excretion of drotaverine in human milk in animals have not been conducted. Due to the lack of such studies in animals and clinical data, it is not recommended to prescribe drotaverine during lactation.

Side effects

The following side effects, which were considered at least possibly related to drotaverine in clinical trials, are given according to the following frequency gradations: very common ( 1/10), common (≥1/100,1/10); rare (≥1/1000,1/100); sometimes (≥1/10000,1/1000); very rare (including individual reports) ( 1/10000); unknown frequency (it is impossible to determine the frequency of occurrence from available data) and grouped by organ system. From the nervous system Sometimes: headache, dizziness, insomnia. From the cardiovascular systemin some cases: rapid heartbeat, decreased blood pressure. From the gastrointestinal tract Sometimes: nausea, constipation. From the immune system, sometimes-allergic reactions (angioedema, urticaria, rash, pruritus) (see the section “Contraindications”).

Interaction

With Levodopa, when used concomitantly, drotaverine may weaken the antiparkinsonian effect of levodopa, that is, increase rigidity and tremor. With papaverine, bendazole and other antispasmodics (including m-holinoblokatorami)Increased antispasmodic effect. With morphine, a decrease in the spasmodic activity of morphine. With phenobarbital Strengthening of the antispasmodic action of drotaverine.

How to take, course of use and dosage

The drug is taken orally. Usually, the average daily dose is 120-240 mg (the daily dose is divided into 2-3 doses).

Overdose

In case of overdose, patients should be under medical supervision and, if necessary, they should be treated symptomatically and aimed at maintaining the basic functions of the body.

There are no data on overdose of the drug.

Special instructions

The use of the drug for arterial hypotension requires increased caution. 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 suffering from lactase deficiency, galactosemia or glucose/galactose malabsorption syndrome. 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 vehicles and perform work that requires increased attention. If any side effects occur, the question of driving vehicles or engaging in other potentially dangerous activities requires individual consideration. In case of dizziness, you should avoid engaging in potentially dangerous activities, such as driving vehicles and working with mechanisms.

Storage conditions

Store at a temperature not exceeding 25 °C. Keep out of reach of children.

Shelf

life is 5 years.

Active ingredient

Drotaverine

Dosage form

Tablets

Purpose

For adults

Indications

Enteritis, Cholecystitis, Gastric and Duodenal Ulcers, Colitis, Cholelithiasis, Spasm of the gastrointestinal tract, Threatened Miscarriage, Gastritis, Gastroduodenitis, Urolithiasis