Drotaverine solution for intravenous and intramuscular injection 20mg/ml in ampoules 2ml №10

Name:
Drotaverine-Borimed solution d-i 2% 2ml №10
Description:
Transparent liquid from yellow to yellowish-green color. The presence of the smell of acetic acid is allowed. One ampoule (2 ml of solution) contains: active ingredient – drotaverine hydrochloride – 40 mg; excipients: sodium metabisulphite, sodium acetate trihydrate, glacial acetic acid, ethyl alcohol, water for injection. Pharmacotherapeutic group Drug for the treatment of functional disorders of the gastrointestinal tract. Papaverine and its derivatives. ATX code: A03AD02. Pharmacological properties Pharmacodynamics Drotaverine is an isoquinoline derivative that exhibits an antispasmodic effect on smooth muscles by inhibiting the enzyme phosphodiesterase IV (PDE IV). Inhibition of the enzyme phosphodiesterase IV leads to an increased concentration of cAMP, which inactivates the myosin kinase (MLCK) light chain, which in turn leads to smooth muscle relaxation. Drotaverine inhibits the PDE IV enzyme without inhibiting the isoenzymes PDE III and PDE V. PDE IV is functionally very important in reducing smooth muscle contractility and selective PDE IV inhibitors may be useful in the treatment of hyperkinetic diseases and various conditions associated with spastic conditions of the gastrointestinal tract. The enzyme that hydrolyzes cAMP in myocardial and vascular smooth muscle cells is mainly a PDE III isoenzyme, which explains why drotaverine is an effective antispasmodic agent without serious cardiovascular side effects and a pronounced effect on the cardiovascular system. Drotaverine is effective in spasms of smooth muscles caused by impaired nervous regulation and self-regulation of both nervous and muscular etiology. Regardless of the type of autonomic innervation, drotaverine acts on smooth muscles located in the gastrointestinal, biliary, urogenital and vascular systems. Due to its vasodilating effect, it improves tissue circulation. The action of drotaverine is stronger than that of papaverine, and absorption is faster and more complete, 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. Pharmacokinetics Drotaverine is rapidly and completely absorbed both after oral administration and after parenteral administration. It is highly (95–98%) bound to plasma proteins, especially albumin, gamma and beta globulins. After the primary metabolism, 65% of the administered dose enters the bloodstream unchanged. The peak in serum after oral administration is reached after 45-60 minutes. Metabolized in the liver. The biological half-life is 8-10 hours. For 72 hours, drotaverine is almost completely excreted from the body, more than 50% is excreted in the urine, 30% in the feces. Basically, drotaverine is excreted in the form of metabolites, unchanged in the urine is not detected. Indications for use: spasms of smooth muscles associated with diseases of the biliary tract: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis; spasms of smooth muscles of the urinary tract: nephrolithiasis, urethrolithiasis, pyelitis, cystitis, bladder tenesmus. cannot be used): 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; with gynecological diseases: dysmenorrhea. Contraindications Hypersensitivity to the active substance or to any of the excipients drugs (especially to sodium methylbisulfite), severe hepatic, renal or heart failure (low cardiac output syndrome), childhood. Precautions Caution should be prescribed for arterial hypotension, severe atherosclerosis of the coronary arteries, during pregnancy. With intravenous administration of drotaverine – due to the danger of collapse – the patient must lie down! In case of hypersensitivity to sodium methylbisulfite, parenteral use of the drug should be avoided. The medicinal product contains sodium methyl bisulfite, which may cause allergic-type reactions, including anaphylactic shock and bronchospasm in susceptible individuals, especially those with a history of asthma or allergic diseases. Clinical studies on the use of the drug in children have not been conducted. Pregnancy, breastfeeding and fertility Parenteral use of drotaverine during pregnancy does not lead to teratogenic and embryotoxic effects. However, when prescribing the drug during pregnancy, caution is necessary. Drotaverine should not be used during childbirth. Due to the lack of necessary clinical data during breastfeeding, it is not recommended to prescribe. Data on the effect of the drug on fertility are not available. Influence on the ability to drive vehicles or other mechanisms After parenteral, and especially intravenous administration of the drug, patients are advised to refrain from driving vehicles and engaging in potentially hazardous activities that require quick physical and mental reactions. Dosage and administration The average daily dose for adults is 40-240 mg of drotaverine hydrochloride (divided into 1-3 injections per day) intramuscularly. In acute colic (biliary and urolithiasis) – 40-80 mg (2-4 ml of the drug) intravenously slowly. Side effects In the event of adverse reactions, you should consult a doctor. The evaluation of adverse effects is based on the following data on the frequency of occurrence: very often (?1/10), often (?1/100 to <1/10), infrequently (?1/1000 to <1/100), rarely (?1 /10,000 to <1/1000), very rare (<1/10,000), not known (cannot be estimated from the available data). From the gastrointestinal tract: rarely - nausea, constipation. From the side of the central nervous system: rarely - headache, dizziness, insomnia. Since the cardiovascular system: rarely - palpitations, hypotension. From the immune system: rarely - allergic reactions, including angioedema, urticaria, rash, itching, fever, chills, fever, weakness, especially in patients with hypersensitivity to metabisulphite. General diseases and local reactions: reactions at the injection site. The frequency is unknown - there have been reports of cases of anaphylactic shock with fatal and non-fatal consequences when using the injectable form. Interaction with other drugs Drotaverine may weaken the antiparkinsonian effect of levodopa. Drotaverine enhances the effect of papaverine, bendazole and other antispasmodics (including m-anticholinergics). With the simultaneous use of tricyclic antidepressants, quinidine and procainamide with drotaverine, the hypotensive effect is enhanced. Drotaverine reduces the spasmogenic activity of morphine. Phenobarbital increases the severity of the antispasmodic effect of drotaverine. OverdoseSymptoms: In high doses, it can cause cardiac arrhythmias and conduction disturbances, including complete bundle branch block and cardiac arrest, which can be fatal. Treatment: observation, symptomatic and supportive treatment. UpakovkaPo 2 ml in glass ampoules. 10 ampoules, together with instructions for medical use, are placed in a cardboard box (No. 10). 10 ampoules, together with instructions for medical use, are placed in a pack with a cardboard insert for fixing ampoules (No. 10). Storage conditions In a place protected from light, at a temperature of 15? C to 25? C. Keep out of the reach of children. Shelf life 2 years. The medicinal product must not be used after the expiration date. Terms of dispensing from pharmacies By prescription. Buy Drotaverine solution for intravenous and intramuscular injection 20mg/ml in ampoules 2ml №10 and intramuscular injections 20mg/ml in ampoules 2ml №10