Short description Pharmacological action - antispasmodic, myotropic, hypotensive. Indications: Spasm of smooth muscles of internal organs (hepatic colic, cholelithiasis and urolithiasis, pylorospasm) and vessels (cerebral, coronary and peripheral); peptic ulcer of the stomach and duodenum, hyperactivity of the myometrium. Inside, 0.04-0.08 g 2-3 times a day. Children under 6 years old - 0.01-0.02 g each; children from 6 to 12 years old - 0.02 g 1-2 times a day. pharmachologic effect Antispasmodic isoquinoline derivative. It has a powerful antispasmodic effect on smooth muscles by inhibiting the PDE4 type enzyme (PDE4). Inhibition of PDE4 leads to an increase in the concentration of cAMP, inactivation of myosin light chain kinase, which further causes relaxation of smooth muscles. The effect of drotaverine through cAMP, which reduces the concentration of Ca2 + ion, explains the antagonistic effect of drotaverine in relation to Ca2 +. In vitro, drotaverine inhibits the PDE4 isozyme without inhibiting the PDE3 and PDE5 isoenzymes. Therefore, the effectiveness of drotaverine depends on the concentration of PDE4 in different tissues. 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. Hydrolysis of cAMP in the myocardium and vascular smooth muscle occurs mainly with the help of the isoenzyme PDE3, which explains the fact that with high antispasmodic activity, drotaverine does not have serious side effects from the heart and blood vessels 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, and the genitourinary system. Due to its vasodilating action, drotaverine improves tissue blood supply. Thus, the above mechanisms of action of drotaverine eliminate smooth muscle spasm, which leads to a decrease in pain. Indications - spasms of smooth muscles in diseases of the biliary tract: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis; - spasms of smooth muscles of the urinary tract: nephrolithiasis, urethrolithiasis, pyelitis, cystitis, bladder spasms. As an auxiliary therapy: - for spasms of smooth muscles of the gastrointestinal tract: gastric ulcer and duodenal ulcer, gastritis, spasms of the cardia and pylorus, enteritis, colitis, spastic colitis with constipation and irritable bowel syndrome with flatulence; - with tension headaches; - with dysmenorrhea (menstrual pain). Method of administration and dosage Adults are prescribed 1-2 tablets. at a time 2-3 times / day. The maximum daily dose is 6 tab. (which corresponds to 240 mg). Clinical studies with the use of drotaverine with the participation of children have not been conducted. In the case of prescribing No-shpa for children aged 6 to 12 years - 40 mg (1 tab.) 1-2 times / day, for children over 12 years old - 4 mg (1 tab.) 1 -4 times / day or 80 mg (2 tab.) 1-2 times / day. The maximum daily dose is 160 mg (4 tab.). When taking the drug without consulting a doctor, the recommended duration of taking the drug is usually 1-2 days. In cases where drotaverine is used as an auxiliary therapy, the duration of treatment without consulting a doctor may be longer (2-3 days). If pain persists, the patient should see a doctor. Efficiency assessment method If the patient can easily diagnose the symptoms of his disease independently, because they are well known to him, the effectiveness of the treatment, namely the disappearance of pain, is also easily assessed by the patient. If, within a few hours after taking the drug at the maximum single dose, there is a moderate decrease in pain or no decrease in pain, or if the pain does not decrease significantly after taking the maximum daily dose, it is recommended to consult a doctor. When using a bottle with a polyethylene stopper equipped with a piece dispenser: before use, remove the protective strip from the top of the bottle and the sticker from the bottom of the bottle. Place the bottle in the palm of your hand so that the dispensing hole on the bottom does not rest on the palm. Then press on the top of the bottle, causing one tablet to fall out of the dispensing hole on the bottom. Side effects Below are the adverse reactions observed in clinical trials, divided by organ systems, indicating the frequency of their occurrence in accordance with the following gradations recommended by the WHO: very often (?10%), often (?1%, 10), infrequently (?0.1 %, 1%), rarely (?0.01%, 0.1%), very rare, including individual messages ( 0.01%), the frequency is unknown (the frequency cannot be determined from the available data). From the side of the nerve Noah system: rarely - headache, dizziness, insomnia. From the side of the cardiovascular system: rarely - a feeling of palpitations, a decrease in blood pressure. From the digestive system: rarely - nausea, constipation. From the immune system: rarely - allergic reactions (angioedema, urticaria, itching, rash). Contraindications - severe hepatic or renal impairment; - severe heart failure (low cardiac output syndrome); - children under 6 years old; - period of breastfeeding (clinical data are not available); - hereditary galactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome; - hypersensitivity to the components of the drug. The drug should be used with caution in case of arterial hypotension, during pregnancy, in children. Overdose Drotaverine overdose has been associated with cardiac arrhythmias 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 and maintenance of basic body functions should be carried out, including artificial induction of vomiting or gastric lavage. special instructions The 40 mg tablets contain 52 mg of lactose monohydrate, as a result of which complaints from the digestive system in patients with lactose intolerance are possible. This form is not intended for patients with lactase deficiency, galactosemia, or impaired glucose / galactose absorption syndrome. Influence on the ability to drive vehicles and control 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 side reactions manifest, the question of driving a vehicle and working with mechanisms requires individual consideration. In case of dizziness after taking the drug, you should avoid engaging in potentially hazardous activities, such as driving and working with machinery. Interaction with other drugs PDE inhibitors, like papaverine, weaken the antiparkinsonian effect of levodopa. When prescribing No-shpa simultaneously with levodopa, an increase in rigidity and tremor is possible. With the simultaneous use of drotaverine with other antispasmodic agents, including m-anticholinergics, there is a mutual enhancement of the antispasmodic effect. Structure 1 tablet contains 40 mg drotaverine hydrochloride Storage conditions Tablets in PVC / Aluminum blisters should be stored at a temperature not exceeding 25 C. Shelf life is 3 years. The tablets in aluminum / aluminum blisters should be stored at a temperature not exceeding 30 C. The shelf life is 5 years. Tablets in vials should be stored in their original packaging at temperatures between 15 and 25 C. The shelf life is 5 years. The drug should be kept out of the reach of children.