The tetracyclines are broad-spectrum, bacteriostatic antibiotics that are active against many pathogens including gram positive and gram negative bacteria, spirochetes, chlamydia, leptospira, mycoplasma and rickettsia. They are widely used in medical practice, but currently have restricted usefulness. Tetracyclines act by binding to bacterial ribosomes inhibiting protein synthesis. Bacterial resistance is common and is usually caused by plasmids that decrease the bacterial cell wall permeability. At least eight different tetracyclines are currently available in the United States: tetracycline, doxycycline, minocycline, tigecycline, sarecycline, omadacycline, eravacycline and demeclocycline. Several others tetracyclines have been used in the past in the United States or Europe, but have been withdrawn (chlortetracycline, aureomycin, triacetyloleandomycin, rolitetracycline, oxytetracycline). While all tetracyclines are capable of causing a distinctive form of acute fatty liver disease when given intravenously in high doses, liver injury from oral forms tetracyclines vary greatly in frequency and clinical features. Minocycline is the most commonly implicated tetracycline in causing liver injury and generally ranks within the 10 most common causes of drug induced liver injury in developed nations. Minocycline hepatotoxicity generally presents with a long latency, hepatocellular enzyme elevations, prominent autoimmune features, apparent response to corticosteroid therapy and relatively bengn course. Doxycycline, in contrast, usually presents with a short latency (within 60 days), a cholestatic course, mild immunoallergic or autoimmune features and sometimes prolonged, but ultimately benign course. The other tetracyclines have had limited clinical use and are generally suspected but unproven potential causes of liver injury. References updated: 10 April 2019
四环素是广谱抑菌性抗生素,对许多病原体具有活性,包括革兰氏阳性菌和革兰氏阴性菌、螺旋体、衣原体、钩端螺旋体、支原体和立克次氏体。它们在医学实践中广泛使用,但目前用途有限。四环素通过与细菌核糖体结合来抑制蛋白质合成发挥作用。细菌耐药性很常见,通常是由降低细菌细胞壁通透性的质粒引起的。目前美国至少有八种不同的四环素:四环素、多西环素、米诺环素、替加环素、沙瑞环素、奥马环素、依拉环素和地美环素。过去在美国或欧洲还使用过其他几种四环素,但已被撤市(金霉素、土霉素、醋竹桃霉素、罗利环素、氧四环素)。虽然所有四环素静脉高剂量给药时都能引起一种独特形式的急性脂肪性肝病,但口服四环素引起的肝损伤在频率和临床特征上差异很大。米诺环素是引起肝损伤最常见的四环素,在发达国家通常位列药物性肝损伤最常见的10大病因之中。米诺环素肝毒性通常潜伏期长,肝细胞酶升高,有明显的自身免疫特征,对皮质类固醇治疗有明显反应,病程相对良性。相比之下,多西环素通常潜伏期短(60天内),呈胆汁淤积病程,有轻度免疫过敏或自身免疫特征,有时病程延长,但最终为良性病程。其他四环素临床应用有限,一般被怀疑是肝损伤的潜在原因,但未经证实。参考文献更新日期:2019年4月10日