フェノキシベンズアミン塩酸塩 化学特性,用途語,生産方法
外観
白色～ほとんど白色粉末～結晶
効能
血圧降下薬, 血管拡張薬, αアドレナリン受容体拮抗薬
説明
Phenoxybenzamine hydrochloride (dibenzyline) is an orally effective, long-acting non-selective (alpha1 and alpha2) alpha-adrenoceptor blocking agent. It is used for the control of episodes of hypertension associated withpheochromocytoma. It literally produces a "chemical sympathectomy". It increases blood flow to the skin, mucosa and abdominal viscera, and lowers both supine and erect blood pressures. It has no effect on the parasympathetic system. The initialdose is 10 mg/day, increased by 10 mg every 4 days till the desired response is attained.The usual dosage range is 20-60mg/day.
化学的特性
white crystalline solid or powder. Odorless. soluble in ethanol, chloroform, propylene glycol, slightly soluble in benzene, slightly soluble in cold water. The melting point of its free base is 38-40 ° C, and it is soluble in benzene.
使用
Phenoxybenzamine (5.0 to 60.0 mg/day) is used in order to control episodes of hypertension and sweating, it has a relatively slow onset and prolonged effect when compared to alternative α-blockers. If tachycardia is excessive, it may also be necessary to use a betablocker concomitantly. In addition, phenoxybenzamine has been tested for its efficacy in micturition disorders resulting from neurogenic bladder, functional outlet obstruction, and partial prostatic obstruction.
一般的な説明
Phenoxybenzamine hydrochloride is a white crystalline powder. Melting point 137.5-140°C. Used as an antihypertensive drug.
空気と水の反応
Light sensitive and may be sensitive to exposure to air . Insoluble in water.
作用機序
Phenoxybenzamine hydrochloride is a noncompetitive alpha-adrenergicreceptor blocker, and its action cannot be nullified by increasing the amount of agonist, or agonists. It causes epinephrine reversal in that the administration of epinephrine after pretreatment with phenoxybenzamine elicits vasodilation, and, conversely, phenoxybenzamine reverses epinephrine-mediated vasoconstriction to vasodilation. It may inhibit neuronal and extraneuronal uptake mechanisms of norepinephrine. At higher concentrations, it inhibits responses to 5-HT, histamine and acetylcholine.
臨床応用
Oral phenoxybenzamine is used for the preoperativemanagement of patients with pheochromocytoma and in thechronic management of patients whose tumors are notamenable to surgery. Only about 20% to 30% of an oraldose is absorbed.
副作用
The adverse effects of phenoxybenzamine include nasal congestion, miosis, postural hypotension, tachycardia, and inhibition of ejaculation.
安全性プロファイル
Confumed carcinogen
with experimental carcinogenic and
teratogenic data. Poison by intraperitoneal,intravenous, and subcutaneous routes.
Human systemic effects by ingestion:
changes in tubules, including acute renal
failure, acute tubular necrosis. Moderately
toxic by ingestion. Other experimental
reproductive effects. Mutation data
reported. A long-acting adrenergic blocker.
When heated to decomposition it emits very
toxic fumes of NOx and Cl-.
発がん性
Phenoxybenzamine hydrochloride is reasonably anticipated to be a human carcinogen based on sufficient evidence of carcinogenicity from studies in experimental animals.
Dosage
Initially, 10 mg of Dibenzyline (phenoxybenzamine hydrochloride) twice a day. Dosage should be increased every other day, usually to 20 to 40 mg 2 or 3 times a day, until an optimal dosage is obtained, as judged by blood pressure control.
フェノキシベンズアミン塩酸塩 上流と下流の製品情報
原材料
準備製品