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一种新型抗心绞痛药物胺碘酮对心肌的作用。

The effect of amiodarone, a new anti-anginal drug, on cardiac muscle.

作者信息

Singh B N, Vaughan Williams E M

出版信息

Br J Pharmacol. 1970 Aug;39(4):657-67. doi: 10.1111/j.1476-5381.1970.tb09891.x.

Abstract
  1. Amiodarone (2-butyl, 3-(4-diethylaminoethoxy, 3,5-diiodo, benzoyl) benzofuran hydrochloride), an anti-anginal drug which causes coronary dilatation and depresses myocardial oxygen consumption, was found to protect anaesthetized guinea-pigs against ouabain-induced ventricular fibrillation.2. A 5% (73.4 mM) solution of amiodarone had no local anaesthetic action on guinea-pig skin.3. Amiodarone, 20 mg/kg (29.4 mumol/kg) given daily for 6 weeks intraperitoneally, had no effect on the resting potential or action potential height, and only a small effect on the maximum rate of depolarization, of isolated rabbit atrial or ventricular muscle fibres as shown by intracellular recording. It caused a considerable prolongation of the action potential in both tissues.4. Simultaneous administration of thyroxine (5 mug; 6.26 nmol), given daily for 3 weeks intraperitoneally, prevented the prolongation by amiodarone of the duration of the action potential.5. Treatment of rabbits with 20 mg/kg of amiodarone daily intraperitoneally for 6 weeks had no effect on the weight of the thyroid gland, but was associated with a reduction in body growth rate.6. Treatment of rabbits with 10 mg/kg (60.3 mumol/kg) of potassium iodide (equal in its iodine content to that of 20 mg/kg of amiodarone), given daily for 6 weeks intraperitoneally, had no effect on body growth rate or the duration of cardiac action potentials.7. It was concluded that amiodarone had effects on cardiac action potentials similar to those which occur after thyroidectomy.
摘要
  1. 胺碘酮(2 - 丁基 - 3 -(4 - 二乙氨基乙氧基)- 3,5 - 二碘苯甲酰基苯并呋喃盐酸盐)是一种抗心绞痛药物,可引起冠状动脉扩张并降低心肌耗氧量,已发现它能保护麻醉的豚鼠免受哇巴因诱导的心室颤动。

  2. 5%(73.4 mM)的胺碘酮溶液对豚鼠皮肤无局部麻醉作用。

  3. 如细胞内记录所示,腹腔内每日给予20 mg/kg(29.4 μmol/kg)胺碘酮,持续6周,对离体兔心房或心室肌纤维的静息电位或动作电位高度无影响,对最大去极化速率仅有轻微影响。它使两种组织的动作电位显著延长。

  4. 腹腔内每日同时给予甲状腺素(5 μg;6.26 nmol),持续3周,可防止胺碘酮引起的动作电位持续时间延长。

  5. 腹腔内每日用20 mg/kg胺碘酮治疗家兔6周,对甲状腺重量无影响,但与体重生长速率降低有关。

  6. 腹腔内每日用10 mg/kg(60.3 μmol/kg)碘化钾(碘含量与20 mg/kg胺碘酮相等)治疗家兔6周,对体重生长速率或心脏动作电位持续时间无影响。

  7. 得出的结论是,胺碘酮对心脏动作电位的影响与甲状腺切除术后出现的影响相似。

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