Papaverine
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Clinical Pharmacology
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.
Indications
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).
Composition
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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Dosage and Administration
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.
Adverse reactions
Allergic reactions, atrioventricular block, ventricular premature beats, increased activity of liver transaminases, lowering blood pressure, drowsiness, constipation, and eosinophilia are possible.
Contraindications
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.
Drug interactions
Reduces the effect of Dopegyt®a.
When smoking is reduced.
Pregnancy and Lactation
During pregnancy and lactation (breastfeeding), the safety and efficacy of papaverine has not been established.
Special instructions
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.
- Brand name: Papaverine
- Active ingredient: Papaverine
- Dosage form: Rectal suppositories
- Manufacturer: Nizhpharm
- Country of Origin: Russia
Studies and clinical trials of Papaverine (Click to expand)
- Comparison of intravenous adenosine to intracoronary papaverine for calculation of pressure-derived fractional flow reserve
- Drug-induced vasodilation: In vitro and in vivo study on the effects of lidocaine and papaverine on rabbit carotid artery
- Oxidation and Degradation Products of Papaverine. Part I: Gadamer and Schulemann's Papaverinol Synthesis Revisited
- Papaverine PVC Membrane Ion-Selective Electrodes Based on its Ion-Exchangers with Tetraphenylborate and Tetrathiocyanate Anions
- Does papaverine affect brain dopamine?
- Response of C-6 glioma to isoproterenol and papaverine in vivo depends on β-adrenergic receptor density
- Does papaverine interact with levodopa in Parkinson's disease?
- Papaverine Crown Ethers
- Retinal cell death occurs in the absence of retinal disc invagination: Experimental evidence in papaverine-treated chicken embryos
- Oxidation and Degradation Products of Papaverine, Part II[1]: Investigations on the Photochemical Degradation of Papaverine Solutions
- Pharmacokinetics and bioavailability of papaverine HCl following intravenous, peroral, rectal, vaginal, topical and buccal administration in beagle dogs
- Effect of mode of application of papaverine on the contractile response of the internal mammary artery
- Papavine: The ideal coronary vasodilator for investigating coronary flow reserve? A study of timing, magnitude, reproducibility, and safety of the coronary hyperemic response after intracoronary papaverine
- Unfavorable interaction of hexabrix and papaverine
- Does intracoronary papaverine dilate epicardial coronary arteries? implications for the assessment of coronary flow reserve
- Changes in epicardial coronary arterial diameter following intracoronary papaverine in man
- Intracoronary electrocardiogram during torsade des pointes secondary to intracoronary papaverine
- Ventricular arrhythmia due to intracoronary papaverine: Analysis of QT intervals and coronary vasodilatory reserve
- ChemInform Abstract: Synthesis of Isoquino[1,2-a][2]benzazepines and Biochemical Testing of Isomeric Homoberbines and Related Papaverine-Derivatives for the Inhibition of Phosphodiesterases.
- Oxidation and Degradation Products of Papaverine. Part 1. Gadamer and Schulemann′s Papaverinol Synthesis Revisited.
- Synthesis and Antispasmodic Activity Evaluation of Bis-(Papaverine) Analogues.
- Synthesis of Pyrroloisoquinolines from Papaverine
- ChemInform Abstract: New Synthesis of 1-[(3,4-Dimethoxyphenyl)methoxymethyl]-6,7-dimethoxyisoquinoline (Setigerine), a Naturally Occurring Alkaloid, and Some Derivatives of Papaverine.
- Papaverine inhibits transcytotic vesicle transport and lipid excretion into bile in isolated perfused rat liver