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The Sound of Evolution
Ketotifen
酮替酚
Mechanism of action:
Ketotifen 是一種第二代 H₁ 受體拮抗劑（H₁ receptor antagonist），同時具有肥大細胞（mast cell）穩定作用（mast cell stabilizer）。Ketotifen 可拮抗 H₁ 受體，阻止組織胺與受體結合，從而減少因組織胺釋放所造成的鼻癢、流鼻水、結膜紅腫、搔癢、支氣管收縮。Ketotifen 也能抑制肥大細胞與嗜鹼性球的去顆粒作用（degranulation），減少多種過敏介質的釋放。
Reference(s):
1. Hawes EM et al. (1998). N⁺-glucuronidation, a common pathway in human metabolism of drugs with a tertiary amine group. Drug Metab Dispos.
2. Kato Y et al. (2013). Human UDP-glucuronosyltransferase (UGT) 2B10 in drug N-glucuronidation: substrate screening and comparison with UGT1A3 and UGT1A4. Drug Metab Dispos.
3. Sokol KC et al. (2013). Ketotifen in the management of chronic urticaria: resurrection of an old drug. Ann Allergy Asthma Immunol.
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