No-spa solution for intravenous and intramuscular injection of ampoules 2 ml 25 pcs.
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Active ingredients
Drotaverine
Release form
Solution
Composition
In 1 amp. Drotaverine Hydrochloride 40 mg. Excipients: sodium disulfite (sodium metabisulfite) - 2 mg, ethanol 96% - 132 mg, water d / and - up to 2 ml. ;
Pharmacological effect
Drotaverine is an isoquinoline derivative. It has a strong antispasmodic effect on smooth muscles due to inhibition of type 4 PDE (PDE IV). PDE IV is required for the hydrolysis of cAMP to AMP. Inhibition of the PDE IV enzyme leads to an increase in the concentration of cAMP, which triggers the following cascade reaction: high concentrations of cAMP activate cAMP dependent phosphorylation of the myosin light chain kinase (MLCC). Phosphorylation of MLCC leads to a decrease in its affinity to calcium (Ca2 +), a calmodulin complex, as a result of which the inactivated form of MLCC supports muscle relaxation. CAMP also affects the cytosolic concentration of Ca2 + by stimulating the transport of Ca2 + into the extracellular space and the sarcoplasmic reticulum. This dropping effect of the Ca2 + ion effect of drotaverine through cAMP explains the antagonistic effect of drotaverine in relation to Ca2 + .; In vitro, Drotaverine inhibits the enzyme PDE IV without inhibiting the isoenzymes of PDE III and PDE V. Therefore, the effectiveness of drotaverine depends on the concentrations of PDE IV in tissues, which differ in different tissues. PDE IV is most important for suppressing the contractile activity of smooth muscles, and therefore selective inhibition of PDE IV may be useful for the treatment of hyperkinetic dyskinesias and various diseases involving the spastic condition of the gastrointestinal tract. ; Hydrolysis of cAMP in the myocardium and vascular smooth muscle occurs mainly through the use of PDE III isoenzyme, which explains the fact that, with high spasmolytic activity, drotaverine does not have serious side effects from the heart and blood vessels and pronounced effects on CVS .; Drotaverine is effective in spasms of smooth muscles of both neurogenic and muscular origin. Regardless of the type of vegetative innervation, drotaverine relaxes the smooth muscles of the gastrointestinal tract, biliary tract, urinary system;
Pharmacokinetics
Absorption.Compared with papaverine, drotaverine when administered orally is faster and more fully absorbed from the gastrointestinal tract. After the presystemic metabolism, 65% of the dose of drotaverine injected into the systemic circulation. Cmax in plasma is reached in 45–60 minutes; Distribution. In vitro, drotaverine has a high binding to plasma proteins (95–98%), especially with albumin, γ and β-globulins .; Drotaverine is evenly distributed in the tissues, penetrates into the smooth muscle cells. Does not penetrate the BBB. Drotaverine and / or its metabolites may slightly penetrate the placental barrier .; Metabolism. In humans, drotaverine is almost completely metabolized in the liver .; Inference. D1 / 2 Drotaverine makes 8–10 h; Within 72 hours, drotaverine is almost completely eliminated from the body. About 50% of Drotaverine is excreted by the kidneys and about 30% through the gastrointestinal tract (excretion into bile). Drotaverine is mainly excreted as metabolites, unchanged drotaverine is not detected in the urine;
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, spasms of the bladder .; As an adjuvant therapy: gastrointestinal smooth muscle spasms: gastric ulcer and duodenal ulcer, gastritis, cardia and pylorus spasms, enteritis, colitis, spastic colitis with constipation and irritable bowel syndrome with flatulence; tension headaches; dysmenorrhea (menstrual pain) .;
Contraindications
Hypersensitivity to the active substance or to any of the excipients of the drug; severe hepatic or renal failure; severe heart failure (low cardiac output syndrome); children's age (the use of drotaverine in children in clinical studies has not been studied); breastfeeding period (no clinical studies); rare hereditary intolerance to galactose, lactase deficiency and glucose-galactose malabsorption syndrome (due to the presence of lactose in the formulation) .; With care: arterial hypotension; pediatric patients (lack of clinical experience); pregnancy;
Use during pregnancy and lactation
In the conducted studies, no teratogenic and embryotoxic effect of Drotaverine was detected, as well as an adverse effect on the course of pregnancy. However, if necessary, the use of the drug No-spa during pregnancy, care should be taken, and prescribe the drug only after assessing the ratio of the potential benefits to the mother and the possible risk to the fetus .; In the absence of the necessary clinical data during breastfeeding is not recommended;
Dosage and administration
V / m, in / in or p / to adults - 40-80 mg 1-3 times / day. With hepatic and renal colic, it is recommended to introduce IV slowly in a dose of 40-80 mg. For spasms of the peripheral arteries, drotaverine can be administered in / a;
Side effects
Below are the adverse reactions observed in clinical studies, divided by organ systems, indicating the frequency of their occurrence in accordance with the following gradation: very often (≥10%), often (≥1, <10%); infrequently (≥0.1, <1%); rarely (≥0.01, <0.1%); very rarely, including individual messages (<0.01%); unknown frequency (according to the available data it is impossible to determine the frequency) .; From the side of the cardiovascular system: rarely - a feeling of heartbeat, lowering blood pressure .; From the side of the central nervous system: rarely - headache, dizziness, insomnia .; On the part of the digestive tract: rarely - nausea, constipation .; On the part of the immune system: rarely - allergic reactions (angioedema, urticaria, rash, itching);
Overdose
Symptoms: disturbances of heart rhythm and conduction, including complete blockade of the bundle of the His bundle and cardiac arrest, which can be fatal .; Treatment: in case of overdose, patients should be under medical supervision, and if necessary, they should be symptomatic and aimed at maintaining the main functions of the body treatment;
Interaction with other drugs
Levodopa. PDE inhibitors, like papaverine, reduce the antiparkinsonic action of levodopa. With the appointment of drotaverine simultaneously with levodopa may increase rigidity and tremor .; Other antispasmodics, including m-anticholinergics. Mutual enhancement of antispasmodic action;
special instructions
It is used with caution in patients with severe atherosclerosis of the coronary arteries, with arterial hypertension .; Drotaverine can be used as part of a combination therapy to relieve a hypertensive crisis;