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Papaverine hydrochloride - antispasmodic, hypotensive.
Papaverine has hypotensive and antispasmodic action.
The mechanism of action is associated with papaverine ability to block the activity of phosphodiesterase type IV. Blockade of the enzyme results in termination of the hydrolysis and increased cAMP concentration in the cells, vascular smooth muscle, internal organs. cAMP restricts the flow of calcium ions into the cell and inactivates muscle myosin light chain kinase - contractile protein that provides contraction of the muscle.
Papaverine reduces the tone and relaxes the smooth muscles of internal organs (gastrointestinal tract, respiratory tract, genitourinary system) and vessels. Papaverine extends predominantly arterial vessels and increases blood flow, including cerebral.
After subcutaneous and intramuscular rapidly and completely absorbed. A therapeutically effective drug concentration in plasma is 0.2-2.0 ug / ml. Repeated use of the drug does not change the pharmacokinetics.
Associated with the plasma protein by 90%. Easily it passes through the blood-tissue barriers. In the liver and adipose tissue depot forms. Treated biotransformation in the liver. Elimination half (t½) of papaverine is 0.5-2.0 hours. Displays in the form of metabolites in the urine, small amounts (less than 0.5%) in an unchanged form.
Inside, adults - 40-60 mg 3-4 times a day. The highest single dose - 0.2 g; daily - 0,6 g Children from 6 months to 14 years - 5-20 mg (depending on age).
N / k / m - 1-2 ml of 2% solution (20-40 mg) 2-4 times a day; w / w, slowly - 1 ml (20 mg) c preliminary dilution of 2% solution in 10-20 ml of isotonic sodium chloride solution.
Rectal, 1-2 supp. (20-40 mg) 2-3 times a day (for adults).
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