塩酸 パパベリン

用途ホスホジエステラーゼ阻害作 用を示します。

用途ホスホジエステラーゼ阻害作 用を示します。

説明Papaverine Hydrochloride, USP, is the hydrochloride of an alkaloid obtained from opium or prepared synthetically. It belongs to the benzylisoquinoline group of alkaloids. It does not contain a phenanthrene group as do morphine and codeine.Papaverine Hydrochloride, USP, is 6,7-dimethoxy-1-veratrylisoquinoline hydrochloride and contains, on the dried basis, not less than 98.5% of CHNO.HCI. The molecular weight is 375.85. The structural formula is as shown.Papaverine Hydrochloride occurs as white crystals or white crystalline powder. One gram dissolves in about 30 mL of water and in 120 mL of alcohol. It is soluble in chloroform and practically insoluble in ether.Papaverine Hydrochloride Injection, USP, is a clear, colorless to pale-yellow solution.Papaverine Hydrochloride, for parenteral administration, is a smooth-muscle relaxant that is available in vials containing 30 mg/mL. Each vial also contains edetate disodium 0.005%. The 10 mL vials also contain chlorobutanol 0.5% as a preservative. pH may be adjusted with sodium citrate and/or citric acid.

来歴Human beings have a long history of using opium poppy as food and narcotics, which can be dated back to the Neolithic age. The opium, which is the dried product of the opium poppy juice, is widely used as analgesics in the old and new civilizations of the old continent except the Chinese civilization. In 1848, German chemist Georg Merck successfully isolated a new alkaloid from the opium liquor for the first time and named it as “papaverine” . He also determined the correct molecular formula of papaverine as C20 H21NO4 and prepared the papaverine hydrochloride and nitrate by recrystallization method. Then, Goldschmiedt etal. put forward the molecular structure of papaverine by studying its oxidation products in 1883 and determined the isoquinoline ring as the core structure of papaverine in 1888 . Since the content of papaverine in plants is very low (less than 1%) and can hardly meet the clinical needs, so Pictet and Gams proposed a synthetic method of papaverine in 1909, which makes the large-scale industrialized production of papaverine possible . Study on the pharmacology of papaverine was first published in 1914 by Professor Pal of Vienna, who found that papaverine possessed smooth muscle relaxation effect without causing smooth muscle paralysis and can be used for the treatment of hypertension, angina, and acute uremia .

使用Papaverine hydrochloride is as effective as sodium diclofenac for the short-term relief of acute renal colic pain and may be advantageous in patients with contraindications for nonsteroidal anti-inflammatory drugs. However, sodium diclofenac appears to provide a longer effective analgesia.Papaverine hydrochloride belongs to the group of benzylisoquinoline alkaloid. It is obtained from opium poppy.Papaverine hydrochloride has been used:in oxygenated Krebs solution for tissue mechanics analysisas a vasodilator in heparinized horse serum in tissue uptake techniqueas an inhibitor of H-MPP+ uptake into stably transfected 293 cells expressing either extraneuronal monoamine transporter (EMT) human or EMT rat