No-Spa Forte 80mg 24 tablets

NO-SPA® forte Trade name: NO-SPA® forte / NO-SPA® forte International Nonproprietary Name: Drotaverine / Drotaverine Dosage form: Tablets. Composition One tablet contains: Active substance: 80 mg drotaverine hydrochloride. Excipients: magnesium stearate (E470), talc (E553), povidone (E1201), corn starch, lactose monohydrate. Description Yellow, biconvex, oblong tablets with a greenish or orange tint. Marked "~NOshPA~" on one side, a dividing line on the other. Pharmacotherapeutic group: Agent for the treatment of functional disorders of the gastrointestinal tract. Papaverine and its derivatives. ATC code: A03AD02 See also: NOSPA - Noshpa 40mg 24 tablets Pharmacological properties Pharmacodynamics: Mechanism of action Drotaverine is an isoquinoline derivative that exhibits antispasmodic action on smooth muscles by inhibiting the enzyme phosphodiesterase IV (PDE IV). Inhibition of phosphodiesterase IV leads to an increased concentration of cAMP, which inactivates the light chain of myosin kinase, causing relaxation of smooth muscles. Drotaverine inhibits PDE IV in vitro without inhibiting the isoenzymes PDE III and PDE V. PDE IV is functionally very important for reducing the contractility of smooth muscles; its selective inhibitors may be useful for treating hyperkinetic diseases and various symptoms caused by spasmodic conditions of the gastrointestinal tract. The PDE-III isoenzyme hydrolyzes cAMP in the myocardium and smooth muscles of blood vessels, which explains why drotaverine is an effective antispasmodic without serious cardiovascular side effects and strong cardiovascular therapeutic activity. The drug is effective in spasms of smooth muscles of both nervous and muscular etiology, caused by impaired nervous regulation and self-regulation. Regardless of the type of vegetative innervation, drotaverine acts on the smooth muscles of the gastrointestinal, biliary, urogenital, and vascular systems. Compared to papaverine, its action is stronger, absorption is faster and more complete, and it binds less to plasma proteins. The advantage of drotaverine is that it does not have a stimulating effect on the respiratory system, which was observed after parenteral administration of papaverine. See blog: Noshpa - what you need to know about the drug's side effects Pharmacokinetics: Absorption Drotaverine is rapidly and completely absorbed after both oral administration and intramuscular injection. Maximum plasma concentration is reached 45-60 minutes after oral administration. Distribution Drotaverine is highly bound to plasma proteins, especially albumin (95-98%), alpha- and beta-globulins. Biotransformation and elimination Drotaverine is metabolized in the liver; its half-life is 8-10 hours. After the first pass through the liver, 65% of the dose remains unchanged in the blood. Within 72 hours, drotaverine is practically completely eliminated from the body, with over 50% excreted in the urine and approximately 30% in the feces. Drotaverine is mainly excreted in the form of metabolites; the parent compound is not detected in the urine. Indications · Spasm of smooth muscles caused by diseases of the biliary tract: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis; · Spasm of smooth muscles of the urinary tract: nephrolithiasis, ureterolithiasis, pyelitis, cystitis, urinary bladder tenesmus; · For spasms of smooth muscles of the gastrointestinal tract: peptic ulcer disease of the stomach and duodenum, gastritis, spasm of the pyloric and cardiac parts of the stomach, enteritis, colitis, spastic colitis with constipation and meteorism; · Tension-type headache; · In gynecology: dysmenorrhea. Contraindications · Hypersensitivity to the active substance or any of the excipients; · Severe hepatic or renal insufficiency; · Severe heart failure (low cardiac output syndrome). Dosage and administration The drug is intended for oral administration. Always take the drug in strict accordance with the instructions in the leaflet or the doctor's recommendation. Adults The usual daily dose is 120-240 mg, i.e., 1.5-3 tablets per day, taken in 2-3 divided doses. The single dose for adults is 40-80 mg (0.5-1 tablet). Children Clinical trials on the use of drotaverine in children have not been conducted. If drotaverine administration is necessary in children: Children over 12 years of age: The usual daily dose is 160 mg, i.e., 2 tablets, taken in 2-4 divided doses. The single dose for children over 12 years of age is 40-80 mg (0.5-1 tablet). Adverse reactions · Gastrointestinal disorders: rarely: nausea, constipation · Nervous system disorders: rarely: headache, dizziness, insomnia · Cardiovascular system disorders: rarely: palpitations, hypotension · Immune system disorders: rarely: allergic reaction (angioedema, urticaria, rash, itching) (see section ~Contraindications~). If any of the listed side effects or side effects not described in the leaflet occur, consult a doctor! Overdose Overdose with drotaverine can cause disorders of cardiac rhythm and conduction, including complete blockade of the bundle branches of His and cardiac arrest, which can lead to a fatal outcome. In case of overdose, the patient should be under observation and receive symptomatic and supportive treatment. Inducing vomiting and/or gastric lavage is recommended. Special warnings and precautions Use of the drug requires caution in case of hypotension. One tablet of the drug contains 104 mg of lactose. When taken at the recommended dosage, each dose contains up to 156 mg of lactose. In patients with lactose intolerance, this may cause undesirable gastrointestinal reactions. This dosage form should not be taken by patients with lactose deficiency, galactosemia, or glucose/galactose malabsorption syndrome. Clinical studies on the use of the drug by children have not been conducted. Pregnancy, lactation and fertility According to retrospective clinical studies and animal studies, oral drotaverine during pregnancy does not have a direct or indirect harmful effect on the course of pregnancy, embryonic development, childbirth, and postnatal development. However, caution is required when prescribing the drug during pregnancy. Due to the lack of adequate clinical data, administration of the drug during lactation is not recommended. There is no information on the effect of the drug on fertility. Interactions with other drugs Phosphodiesterase inhibitors, such as papaverine, reduce the antiparkinsonian effect of levodopa. Caution should be exercised when using the drug simultaneously with levodopa, as the antiparkinsonian effect of levodopa is reduced and tremor and rigidity are increased. Effect on ability to drive or operate machinery If dizziness occurs after taking the drug, refrain from driving or operating other potentially hazardous machinery. Shelf life: 3 years. Do not use after the expiry date. Dosage form: 24 tablets in PVC/aluminum blisters. 1 blister in a cardboard box with an insert. Storage conditions: Keep out of reach of children! Store at a temperature not exceeding 25°C, protected from light. Dispensing category: Pharmaceutical product group III, available without a prescription