776f5421a107f171db76f55adbb3fff0

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776f5421a107f171db76f55adbb3fff0

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Spasmolytic agent
Dosage form
Tablets from light yellow with a greenish shade to yellow with a greenish tint of color with a risk on one side and a facet.
Composition
1 tab.

Drotaverina hydrochloride 40 mg

Excipients: lactose monohydrate (sugar milk) — 16.6 mg, microcrystalline cellulose — 20 mg, corn starch — 10 mg, croscarmellose sodium — 4 mg, povidone K25 — 3.5 mg, magnesium stearate — 0.9 mg.
pharmachologic effect
Spasmolytic agent, isoquinoline derivative. Has a powerful spasmolytic effect on smooth muscle by inhibiting the enzyme PDE. Enzyme PDE is necessary for the hydrolysis of cAMP to AMP. Inhibition of PDE leads to an increase in the concentration of cAMP, which triggers the following cascade reaction: high concentrations of cAMP activate cAMP-dependent phosphorylation of myosin light chain kinase (CMLC). Phosphorylation of CMLC leads to a decrease in its affinity for the Ca2 + -culmodulin complex, as a result of which the inactivated form of CLCM supports muscular relaxation. In addition, cAMP influences the cytosolic concentration of the Ca2 + ion by stimulating Ca2 + transport into the extracellular space and the sarcoplasmic reticulum. This lowering concentration of the Ca2 + ion, the drotaverin effect through cAMP, explains the antagonistic effect of drotaverine relative to Ca2 +.

In vitro, drotaverin inhibits the PDE4 isoenzyme without inhibiting the isoenzymes PDE3 and PDE5. Therefore, the effectiveness of drotaverine depends on the concentration of PDE4 in the tissues (the PDE4 content varies in different tissues). PDE4 is most important for suppressing the contractile activity of smooth muscle, and therefore selective inhibition of PDE4 can be useful for the treatment of hyperkinetic dyskinesias and various diseases accompanied by spastic condition of the gastrointestinal tract.

The hydrolysis of cAMP in the myocardium and smooth muscles of the vessels is mainly due to the isoenzyme of PDE3, which explains the fact that with high spasmolytic activity, drotaverin has no serious side effects from the heart and vessels and the pronounced effects on the cardiovascular system.

Drotaverine is effective in spasms of smooth muscles of both neurogenic and muscular origin. Regardless of the type of vegetative innervation, drotaverin relaxes the smooth musculature of the digestive tract, the biliary tract, the genitourinary system.

Dosage
Inside to 40-80 mg 1-3 times / day, the maximum single dose of 80 mg, the maximum daily 240 mg. For children aged 6-12 years — 20 mg, frequency of application 1-2 times / day.