Instructions for No-Spa (Drotaverine)
Current substances:
Drotaverin
Release Form:
Pills
Composition:
1 tab. dtrotaverine hydrochloride 40 mg;
Auxiliary substances:
magnesium stearate - 3 mg,
talc - 4 mg,
povidon - 6 mg,
starch corn - 35 mg,
lactose monohydrate - 52 mg;
Pharmaceutical effect:
Drotaverin is a derivative of isochinolin. It exhibits a powerful spaszprama action on smooth musculature due to the inhibition of FDE IV type (FDE IV). FTE IV is necessary for the hydrolysis of the cAMF to AMF. Inflexing of enzyme FDE IV leads to an increase in the concentration of AMF, which triggers the following cascading reaction: High concentrations of CAMF activate CAMF dependent phosphorysis of myozine lung circuits (CLCM). Phosphorization of the CLCM leads to a decrease in its affinity to calcium (Ca2+)-modulin complex, as a result of which the inactivated form of the CLCMM supports muscle relaxation. CAMF also influences Ca2+ cytozolic concentration by promoting Ca2+ transport to the extracellular space and sarcoplasmic reticulum. This decreasing concentration of ion Ca2+ the effect of the dtrotaverin through the AMF explains the antagonistic effect of the drotaverin in relation to Ca2+.;In vitro dartaverin ingibates the enzyme of the FDE IV without inhibition of isoferments of FDE III and FDE V. Therefore, the effectiveness of the dartaverine depends on the concentrations of the FDE IV in tissues, which differ in different tissues. FTE IV is most important for the suppression of the contractionary activity of smooth musculature, therefore selective inhibition of FDE IV can be useful for the treatment of hyperkinetic diskinesis and various diseases associated with the spastic condition of the LCD. ;CAMF hydrolysis in myocardium and smooth vascular musculature occurs mainly through the isoensim FDE III, which explains the fact that in the case of high spaspram activity, the dartaverin has no serious side effects on the heart and blood vessels and expressed effects with respect to SSS.;Drotaverine is effective in smooth muscle spasms
Pharmacokinetics:
Absorption. Compared to papaverin, the dartaverine is more quickly and more completely absorbed from the LCD. After a repressive metabolism, 65% of the dosage taken is absorbed into the system blood flow. Cmax in plasma is reached in 45-60 minutes;Distribution. In vitro dartaverin has a high connection with plasma proteins (95-98%), especially with albumin, α and α-globulins.;Drotaverin is evenly distributed across tissues, penetrates into smooth muscular cells. It doesn't get through the GAB. Drotaverine and/or its metabolites can penetrate slightly through the placental barrier.;Metabolism. In man, the dartaverine is almost completely metabolized in the liver.;Injection. T1/2 is 8-10 h.;During 72 h, the dartaverine is almost completely removed from the body. About 50% of the dartaverine is excreted with kidneys and about 30% through LCD (bile excretion). Drotaverine is mainly excreted as metabolites, unmodified dartaverine in the urine is not detected;
Indications:
- Spasma of smooth musculature, in the case of diseases of the bile tract
- cholecystytiasis
- cholangiolithiasis
- cholecystitis
- pericolecystitis
- holangitis
- papillite
- smooth musculature spasma of the urinary tract
- petrolithiasis
- uretrolithiasis
- pielitis
- cystitis
- bladder spasms
- As a auxiliary therapy: LCD smooth musculature spasms: ulcerous stomach disease and duodenal intestine, gastritis, cardiac and gatekeeper spasma, enteritis, colitis, constipated spastic colitis and irritated intestine syndrome with meteorism; voltage headaches; Dismenorea (menstrual pain);
Contraindications:
Increased sensitivity to >span class="token_created">active substance or any of >span class="token_created">auxiliary substances of >span class="token_created">drug; Severe liver or kidney failure; severe heart failure (low-heart-emitting syndrome); Children under 6 years of age; Breastfeeding period (without clinical trials); rare hereditary intolerability of galactose, lactase deficit and halactose glucose malabsorption syndrome (due to lactose in >span class="token_created">drug).;With caution: arterial hypotension; Children's patients (insufficient clinical experience); pregnancy
Use in pregnancy and breastfeeding
How to use and dose:
Adults are given 1-2 pills. 2-3 times a day. >span class="token_created">maximum daily dose is 6 tablets. (which corresponds to 240 mg). No drotaverine clinical trials were conducted with children.; For No-Spa for children aged 6 to 12 - 40 mg (1 tablet) 1 - 2 times per day, for children aged 12 years - 4 mg (1 tablet) 1 - 4 times per day or 80 mg (2 tablet) 1 - 2 times/day
Side effects:
The following are adverse reactions observed in clinical studies, divided by organ systems, indicating the frequency of their occurrence according to 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 available data, the frequency cannot be determined).; From the CCC: rarely - sensation of heartbeat, decrease in BP.; From the CNS: rarely - headache, dizziness, insomnia.; From the GI: rarely - nausea, constipation.; From the immune system: rarely - allergic reactions (angioedema, cornea
Overdose:
Symptoms: heart rhythm and conduction disorders, including complete blockade of the legs of the Gis 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 given symptomatic and aimed at maintaining the basic functions of the body treatment;
Interaction with other drugs No-Spa:
Levodopa. FDE inhibitors like papaverin reduce the anti-parkinsonic effect of the levodope. When assigning a dartaverin simultaneously with the leopard, it is possible to increase the rigidity and tremor.;Other spasmyllic remedies, including m-cholinocolators. Mutual strengthening of spasma action;
Special Instructions
It is used with care in patients with atherosclerosis of coronary arteries, in the case of arterial gtipotensia.;Drotaverine can be used in the combination therapy to bathe hypertonic crisis;
