Description of the medicine: Papaverinum (Papaverinum)

PAPAVERIN (Papaverinum).

The alkaloid contained in the opium. Currently, they are produced synthetically. Produced in the form of papaverine hydrochloride (Rarverini hoodrochloridum).

By chemical structure is 6, 7-dimethoxy-1- (3,4-dimethoxybenzyl) -isoquinoline hydrochloride.

White crystalline powder slightly bitter taste. Slowly soluble in water (1:40), little - in alcohol. Aqueous solutions (pH 3, 0 - 4, 5) are sterilized at + 100 ° C for 30 minutes.

Papaverin is a myotropic antispasmodic. It lowers the tone and reduces the contractile activity of smooth muscles and therefore has a vasodilating and spasmolytic effect.

In large doses reduces the excitability of the heart muscle and slows intracardiac conduction.

The mechanism of action of papaverine is not clear enough. In recent years, it has been found that it is an inhibitor of the enzyme phosphodiesterase and causes intracellular accumulation of cyclic 3 ', 5'-adenosine monophosphate (see Theophylline).

The accumulation of cAMP ultimately leads to a violation of contractility of smooth muscles and their relaxation in spastic states.

The effect on the central nervous system is poorly expressed, only in large doses, it has some sedative effect.

Papaverine is widely used as a spasmolytic agent for spasms of smooth muscles of the abdominal cavity organs (with pilorospasm, cholecystitis, spastic colitis, urinary tract spasms), bronchus (usually in combination with other bronchodilators), as well as spasms of peripheral vessels (endarteritis, etc.) And vessels of the brain.

Previously, papaverine was relatively widely used internally for the prevention of angina attacks. The drug has some effect, but now more effective anti-anginal drugs are used for this purpose.

Sometimes papaverine is used parenterally (under the skin, intramuscularly, rarely in a vein) in combination with promedol or other analgesic and antispasmodic drugs for arresting angina attacks.

Assign papaverine hydrochloride inside, under the skin, intramuscularly, intravenously and rectally.

Inside adults take on 0,04 - 0,08 g (40 - 80 mg) 3 - 4 times a day; Children - also 3-4 times a day: at the age of 6 months to 2 years - 0,005 grams (5 mg) per reception, 3 to 4 years - 0,005 to 0,01 g, 5 to 6 years to 0, 01 g, 7 - 9 years - 0,01 - 0,015 g, 10 - 14 years - 0,015 - 0,02 g per reception.

When vomiting or difficulty swallowing appoint in the form of suppositories of 0,02 - 0,04 g 2 - 3 times a day (adults).

Under the skin and intramuscularly administered to adults 1 to 2 ml (usually 2 ml) 2% solution, and intravenously - in the same dose (very slowly!), Diluting 2% solution papaverine hydrochloride in 10 - 20 ml isotonic sodium chloride solution. Children are given in smaller doses according to age.

Higher doses for adults inside: single 0.2 g, daily 0.6 g; Under the skin, intramuscularly and in a vein: single 0.1 g, daily 0.3 g.