

Papaverine hydrochloride is a myotropic antispasmodic. Inhibits phosphodiesterase, causes accumulation of cyclic 3,5-adenosine monophosphate (AMP) in the cell and a decrease in calcium content. Relaxes smooth muscles of internal organs (gastrointestinal tract, respiratory tract, urogenital system) and blood vessels. In large doses, reduces the excitability of the heart muscle and slows intracardiac conduction. The effect of papaverine on the central nervous system is weakly expressed, but in large doses it has a sedative effect.
Pharmacokinetics
The bioavailability of papaverine after rectal administration (according to preclinical studies) is about 25%. Communication with plasma proteins 90%. Well distributed, penetrates histohematogenous barriers. Metabolized in the liver. The elimination half-life (T1 / 2) is 0.5-2 hours (an increase up to 24 hours is possible). Excreted by the kidneys as metabolites.
Spasm of smooth muscles: abdominal organs (with cholecystitis, pylorospasm, spastic colitis); with renal colic; peripheral vessels (with endarteritis); cerebral vessels (with migraine); heart (with angina - as part of complex therapy); bronchi (with bronchospasm).
The composition of one suppository: active ingredient: papaverine hydrochloride - 20 mg; excipients: solid fat (Witepsol (mark H 15, W 35), Supposir (mark NA 15, NAS 50)) - to obtain a suppository weighing 1.25 g
Papaverine is marketed under different brands and generic names, and comes in different dosage forms:
Brand name | Manufacturer | Country | Dosage form |
---|---|---|---|
Papaverine | Nizhpharm | Russia | rectal suppositories |
Papaverine | PFK Obnovlenie | Russia | pills |
Papaverine | Pharmstandard | Russia | pills |
Papaverine | PFK Obnovlenie | Russia | solution |
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Rectally. Having released the suppository from the contour packaging, it is introduced into the anus. Apply 1 suppository 2 to 3 times a day after spontaneous bowel movements or cleansing enemas.
Allergic reactions, atrioventricular block, ventricular premature beats, increased activity of liver transaminases, lowering blood pressure, drowsiness, constipation, and eosinophilia are possible.
Hypersensitivity to the components of the drug, atrioventricular block, glaucoma, severe liver failure, old age (risk of developing hyperthermia), children's age, because the dosing regimen in children is not specified.
Carefully
With caution and in small doses used in the state after traumatic brain injury, chronic renal failure, insufficiency of adrenal function, hypothyroidism, prostatic hyperplasia, supraventricular tachycardia, shock conditions.
Reduces the effect of Dopegyt®a.
When smoking is reduced.
During pregnancy and lactation (breastfeeding), the safety and efficacy of papaverine has not been established.
With caution and in small doses should be used in elderly and debilitated patients, as well as in patients with traumatic brain injury, impaired liver and kidney function, hypothyroidism, adrenal insufficiency, prostatic hypertrophy, with supraventricular tachycardia and shock.
Studies and clinical trials of Papaverine (Click to expand)