クロルフェニラミン 化学特性,用途語,生産方法
解説
3-(4-chlorophenyl)-N,N-dimethyl-3-(2-pyridyl)propylamine．C16H19ClN2(274.79)．クロルフェニラミンは，4-クロロベンジルシアニドと2-クロロピリジンとを縮合させ，これに2-(ジメチルアミノ)エチルクロリドを反応させ，80％ H2SO4と加熱すると得られる．油状の液体．沸点142 ℃(0.13 kPa)．マレイン酸塩：C16H19ClN2·C4H4O4(390.87)が実用化されている．白色の微細な結晶．融点130～135 ℃．λmax 261 nm．水，エタノール，クロロホルムに可溶．2％ 水溶液の pH は約5．強力な抗ヒスタミン薬である．じんましん，枯草熱，皮膚疾患に伴う掻痒(そうよう)，アレルギー性鼻炎，血管運動性鼻炎などに投与する．LD50 162 mg/kg(マウス，経口)．[CAS 132-22-9][CAS 113-92-8:マレイン酸塩] 森北出版「化学辞典（第2版）
効能
抗アレルギー薬, H1受容体拮抗薬
化学的特性
BP
使用
Chlorpheniramine is a drug in the class of first-generation
antihistamines, used to help alleviate symptoms of allergic
reactions potentiated by histamine release. Though it is
included in many multisymptom over-the-counter cold relief
medications, the Food and Drug Administration (FDA) issued
a safety alert in March 2011 detailing some risks associated
with these medications. The safety alert also indicated that
increased enforcement of FDA laws governing the marketing
of these drugs would occur, as many of the products had not
been approved in their current formulations for safety, effectiveness,
and quality.
Chlorpheniramine is commonly used in small-animal
veterinary medicine for its antihistaminic/antipruritic effects,
especially for the treatment of pruritus in cats, and occasionally
as a mild sedative.
環境運命予測
Toxicity of antihistamines is usually related to their anticholinergic
effects and may include loss of appetite, nausea,
vomiting, diarrhea or constipation, and other GI effects, as well
as dizziness, tinnitus, lassitude, incoordination, fatigue, blurred
vision, diplopia, euphoria, nervousness, insomnia, and
tremors. Acetylcholine is competitively blocked at muscarinic
receptors, resulting in symptoms of anticholinergic poisoning.
Concurrent use of alcohol, tricyclic antidepressants, monoamine
oxidase inhibitors, or other central nervous system
(CNS) depressants along with antihistamines may exaggerate
and extend the anticholinergic and CNS depressant effects of
antihistamines; concurrent use is not recommended.
Products that were marketed prior to the FDA safety alert
but not approved by the FDA included multisymptom cold
medications comprised of drug combinations of chlorpheniramine
with decongestants, antitussives, and analgesics. Risks
associated with the use of these products included improper
use in children and infants, potentially risky combination of
ingredients, and patients receiving too much or too little
medication because of problems with the way some ‘extendedrelease’
products were made. Newborn and premature infants
are even more prone to anticholinergic side effects and an
increased susceptibility toward convulsions; thus, this drug is
not recommended at all in this age group. Geriatric patients are
also more prone to anticholinergic effects, and a paradoxical
reaction characterized by hyperexcitability may occur in some
children taking antihistamines. Overdosage may also produce
central excitation resulting in convulsions.
クロルフェニラミン 上流と下流の製品情報
原材料
準備製品