ベタネコール塩化物

外観

白色～ほとんど白色粉末～結晶

効能

消化管運動改善薬, ムスカリン受容体作動薬

商品名

ベサコリン (サンノーバ)

説明

Bethanechol is an agonist of muscarinic acetylcholine receptors with IC₅₀ values of 1,837, 25, 631, 317, and 393 μM for M_1-5, respectively, in a radioligand binding assay using CHO cells expressing the human receptors. It inhibits M₂-mediated increases in cyclic AMP induced by isoproterenol in isolated guinea pig small intestine (IC₅₀ = 127 μM). Bethanechol increases basal tone of isolated porcine intravesical ureter (EC₅₀ = 4.27 μM). It also induces fluid secretion in the ileum, duodenum, and jejunum of anesthetized rats when administered at a dose of 60 μg/kg. Formulations containing bethanechol have been used to increase urination and improve smooth muscle tone in the gastrointestinal tract.

化学的特性

White Solid

使用

cholinergic

定義

ChEBI: The chloride salt of bethanechol. A slowly hydrolysed muscarinic agonist with no nicotinic effects, it is used to increase smooth muscle tone, as in the gastrointestinal tract following abdominal surgery, treatment of gastro-oesophageal reflux disease, and as an alternative to catheterisation in the treatment of non-obstructive urinary retention.

一般的な説明

Bethanechol, β-methylcholinechloride carbamate, (2-hydroxypropyl)trimethylammoniumchloride carbamate, carbamylmethylcholinechloride (Urecholine), is nonspecific in its action on muscarinicreceptor subtypes but appears to be more effective ateliciting pharmacological action of M3 receptors. It haspharmacological properties similar to those of methacholine.Both are esters of β-methylcholine and have feeblenicotinic activity. Bethanechol is inactivated more slowlyby AChE in vivo than is methacholine. It is a carbamyl esterand is expected to have stability in aqueous solutions similarto that of carbachol.

危険性

Headache, flushing, gastrointestinal distress, diarrhea, hypotension, excessive salivation, sweating, hypersensitivity.

作用機序

Bentanechol is a drug, which has structurally unique qualities of both methacholine and carbachol, i.e. it contains both β-methyl and carbamate functional groups, and quite logically exhibits pharmacological properties of both the drugs. It is resistant to hydrolysis by cholinesterases and has a very minor effect on nicotinic receptors of the autonomic ganglia and neuromuscular junctions. Betanechol has more of a selective action on muscarinic receptors of the gastrointestinal tract and the bladder than do other cholinic esters.

臨床応用

The main use of bethanechol chloride is in the relief ofurinary retention and abdominal distention after surgery.The drug is used orally and by subcutaneous injection. Itmust never be administered by intramuscular or intravenousinjection because of the danger from cholinergic overstimulationand loss of selective action. Proper administration ofthe drug is associated with low toxicity and no serious sideeffects. Bethanechol chloride should be used with caution inasthmatic patients; when used for glaucoma, it producesfrontal headaches from the constriction of the sphinctermuscle in the eye and from ciliary muscle spasms. Its durationof action is 1 hour.