| 药品名称 |
Clemastine
|
| 分子靶点 |
Histamine H1 receptor
|
| 酶 |
Cytochrome P450 2D6
|
| 药物类型 |
Small Molecule
|
| 研发阶段 |
Approved, Investigational
|
| 药物描述 |
An ethanolamine-derivative, first generation histamine H1 antagonist used in hay fever, rhinitis, allergic skin conditions, and pruritus. It causes drowsiness.
|
| 结构式 |
 |
| 药物别名 |
(+)-(2R)-2-(2-(((R)-p-chloro-α-methyl-α-phenylbenzyl)oxy)ethyl)-1-methylpyrrolidine;(+)-(2R)-2-[2-[[(R)-p-chloro-α-methyl-α-phenylbenzyl]oxy]ethyl]-1-methylpyrrolidine;Clemastina;Clemastine;Clemastinum
|
| 治疗类别 |
Aminoalkyl Ethers;Anti-Allergic Agents;Antihistamines for Systemic Use;Antihistamines for Topical Use;Antipruritics;Antipruritics, Incl. Antihistamines, Anesthetics, Etc.;Central Nervous System Depressants;Cytochrome P-450 CYP2D6 Inhibitors;Cytochrome P-450 CYP2D6 Inhibitors (moderate);Cytochrome P-450 Enzyme Inhibitors;Dermatologicals;Highest Risk QTc-Prolonging Agents;Histamine Agents;Histamine Antagonists;Histamine H1 Antagonists;Neurotransmitter Agents;Pyrrolidines;QTc Prolonging Agents
|
| UNII号 |
95QN29S1ID
|
| CAS号 |
15686-51-8
|
| 分子量 |
343.89
|
| 分子式 |
C21H26ClNO
|
| 适应症 |
For the relief of symptoms associated with allergic rhinitis such as sneezing, rhinorrhea, pruritus and acrimation. Also for the management of mild, uncomplicated allergic skin manifestations of urticaria and angioedema. Used as self-medication for temporary relief of symptoms associated with the common cold.
|
| 药效学 |
Clemastine is an antihistamine that also induces anticholinergic and sedative effects. Antihistamines competitively antagonize various physiological effects of histamine including increased capillary permeability and dilatation, the formation of edema, the "flare" and "itch" response, and gastrointestinal and respiratory smooth muscle constriction. Within the vascular tree, H1- receptor antagonists inhibit both the vasoconstrictor and vasodilator effects of histamine. Depending on the dose, H1- receptor antagonists can produce CNS stimulation or depression. Most antihistamines exhibit central and/or peripheral anticholinergic activity. Antihistamines act by competitively blocking H1- receptor sites. Antihistamines do not pharmacologically antagonize or chemically inactivate histamine, nor do they prevent the release of histamine.
|
| 作用机制 |
Clemastine is a selective histamine H1 antagonist and binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine.
|
| 吸收 |
Rapidly absorbed from the gastrointestinal tract.
|
| 代谢 |
Antihistamines appear to be metabolized in the liver chiefly via mono- and didemethylation and glucuronide conjugation.
|
| 排泄 |
Urinary excretion is the major mode of elimination.
|
| 毒理 |
Oral LD in rat and mouse is 3550 mg/kg and 730 mg/kg, respectively. Antihistamine overdosage reactions may vary from central nervous system depression to stimulation. In children, stimulation predominates initially in a syndrome which may include excitement, hallucinations, ataxia, incoordination, muscle twitching, athetosis, hyperthermia, cyanosis convulsions, tremors, and hyperreflexia followed by postictal depression and cardio-respiratory arrest. Convulsions in children may be preceded by mild depression. Dry mouth, fixed dilated pupils, flushing of the face, and fever are common. In adults, CNS depression, ranging from drowsiness to coma, is more common.
|
| ATC代码 |
D04AA14
|
