Terfenadine is an antihistamine formerly used for the treatment of allergic conditions. It was brought to market by Hoechst Marion Roussel (now Sanofi-Aventis) and was marketed under various brand names, including Seldane in the United States, Triludan in the United Kingdom, and Teldane in Australia. It was superseded by fexofenadine in the 1990s due to the risk of a particular type of disruption of the electrical rhythms of the heart (specifically cardiac arrhythmia caused by QT interval prolongation) and has been withdrawn from markets worldwide.:53; Terfenadine is a prodrug, generally completely metabolized to the active form fexofenadine in the liver by the enzyme cytochrome P450 3A4. Due to its near complete metabolism by the liver immediately after leaving the gut, terfenadine normally is not measurable in the plasma. Terfenadine itself, however, is cardiotoxic at higher doses, while its major active metabolite is not. Terfenadine, in addition to its antihistamine effects, also acts as a potassium channel blocker (Kv11.1 encoded by the gene hERG). Since its active metabolite is not a potassium channel blocker, no cardiotoxicity is associated with fexofenadine. Toxicity is possible after years of continued use with no previous problems as a result of an interaction with other medications such as erythromycin, or foods such as grapefruit. The addition of, or a dosage increase in, these CYP3A4 inhibitors makes it harder for the body to metabolize and remove terfenadine. In larger plasma concentrations, it may lead to toxic effects on the heart's rhythm (e.g. ventricular tachycardia and torsades de pointes).

CAS：50679-08-8
中文别名：Α-[4-(1,1-二甲基乙基)苯基]-4-(羟基二苯甲基)-1-哌啶丁醇;叔哌丁醇;Α-[4-叔丁基苯基]-4-(羟基二苯基甲基)-1-哌啶丁醇;α-[4-(1,1-Dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol;alpha-[4-叔丁基苯基]-4-(羟基二苯基甲基)-1-哌啶丁醇;
英文别名：Triludan;[3H]-Terfenadine;Aldaban;Teldane;Terfenadina;Ternadin;Seldane;terfenadine;Terdin;Teldanex;Terfenadine;Allerplus;[14C]-Terfenadine;
分子式：C32H41NO2
分子量：471.673
精确质量：471.314
Psa：43.7
Logp：6.3837

UNII：7BA5G9Y06Q

外观与性状：固体结晶粉末
密度：1.088 g/cm3
沸点：626.8ºC at 760 mmHg
熔点：145-152 °C
闪点：306.9ºC
水溶解性：0.001 g/100 mL (30 ºC)
储存条件：2-8ºC

RTECS号：TM4969000
安全说明：S24/25
WGK Germany：2
海关编码：2933399090
危险性描述：H413

生产方法
α，α-二苯基-4-哌啶基甲醇(107g，0.4m 新型抗组胺药，有特异的外周H1受体拮抗作用，且没有抗5-羟色胺、抗胆碱能和抗肾上腺素能的作用。适用于季节性过敏性鼻炎(花粉症)、常年性过敏鼻炎、急慢性荨麻疹等的治疗。
用途
新型抗组胺药，有特异的外周H1受体拮抗作用，且没有抗5-羟色胺、抗胆碱能和抗肾上腺素能的作用。适用于季节性过敏性鼻炎(花粉症)、常年性过敏鼻炎、急慢性荨麻疹等的治疗。