The ketolide class of antibiotics was first introduced in 2004. At this time, telithromycin (Ketek) is the only approved drug in the class.
酮内酯类抗生素首次引入是在2004年，当时，泰利霉素（Ketek）为唯一获批药物。
Therapeutic Actions and Indications 治疗作用与适应症
The ketolides block protein synthesis within susceptible bacteria, leading to cell death, which makes them structurally related to the macrolide antibiotics. Telithromycin binds to specific ribosome subunits, leading to cell death in susceptible bacteria, which includes several strains resistant to other antibiotics. Telithromycin is effective against S. pneumoniae, including certain multidrugresistant strains, H. influenzae, M. catarrhalis, Chlamydophila pneumoniae, and Mycoplasma pneumoniae. It is only approved for use in treating mild to moderate community-acquired pneumonia.
Telithromycin is available as an oral drug only. It is rapidly absorbed through the GI tract, reaching peak levels in 1 hour. The drug is widely distributed, may cross the placenta, and does pass into breast milk. It is metabolized in the liver with a half-life of 10 hours. It is excreted in the urine and feces.
泰利霉素只有口服剂型。该药经胃肠道迅速吸收，1小时后达峰。药物分布广泛，可穿过胎盘，可进入母乳。经肝代谢，半衰期10小时。经尿和粪便排出。 Contraindications and Cautions 禁忌症和注意事项
Telithromycin is contraindicated with known allergy to any component of the drug or to macrolide antibiotics to avoid hypersensitivity reactions; with known congenital prolonged QT interval, bradycardia, or any proarrhythmic condition such as hypokalemia to avoid potentially serious cardiac effects; with concurrent use of pimozide, cardiac antiarrhythmics, simvastatin, atorvastatin, or lovastatin because of the risk of serious adverse effects if these are combined; and with myasthenia gravis, which is a black box warning with this Drug because of the risk of potentially fatal respiratory failure.
泰利霉素禁忌对象：已知药物成份过敏或对大环内酯类抗生素过敏的患者，应避免超敏反应；已知的先天性QT间期延长或心律失常疾病患者，如低钾血症，避免潜在的心脏影响；同步使用匹莫齐特、抗心律不齐药、辛伐他汀、阿托伐他汀、洛伐他汀，因为与这些药物结合会引起严重的不良效应风险；重症肌无力患者，该症被列为该药的黑箱警示范畴，因为有潜在的致命性呼吸衰竭风险。
Use with caution in cases of renal or hepatic impairment because this could alter the metabolism and excretion of the drug, leading to serious adverse effects. Use with caution with pregnant and lactating patients because of the potential for toxic effects on the fetus or infant.
肾、肝受损患者慎用，因为可能出现药物代谢和排泄改变，导致严重的不良效应。孕妇和哺乳患者慎用，因为可能对胎儿和婴儿产生毒性效应。
Perform culture and sensitivity testing to ensure that the drug is used appropriately.
进行细菌培养和敏感性试验，确保药物使用适当。 Adverse Effects 不良效应
The adverse effects associated with telithromycin are largely secondary to toxic effects on the GI tract: nausea, vomiting, taste alterations, and the potential for pseudomembranous colitis. Superinfections are common, related to the loss of normal flora bacteria. Serious hypersensitivity reactions, including anaphylaxis, have occurred.
ketolide – n. 酮内酯类抗生素
telithromycin – n. 泰利霉素 Ketek --泰利霉素商标名
ribosome – n. 核糖体
subunit – n. 亚单位
multidrugresistant – n. 多重耐药 M. catarrhalis – n. 卡他莫拉氏菌
proarrhythmic – a. 致心律失常的
pimozide – n. 匹莫齐特
Test 1. Which laboratory result should a nurse monitor more frequently when a patient is receiving clarithromycin (Biaxin) and warfarin (Coumadin)?
A. Activated partial thromboplastin time (aPTT)
B. Platelet count
C. Erythrocyte sedimentation rate (ESR)
D. International normalized ratio (INR)
2. A patient who has a vancomycin-resistant enterococci (VRE) infection is receiving linezolid (Zyvox). Which laboratory result indicates that the patient is having an adverse effect?
A. White blood cell (WBC) count of 1200 units/L
B. Hemoglobin (Hgb) level of 18 g/dL
C. Potassium level of 3.0 mEq/dL
D. Glucose level of 200 mg/dL
本期ISPN Review答案： 1. D. International normalized ratio (INR)
Clarithromycin is a macrolide similar to erythromycin and can inhibit hepatic metabolism of medications such as warfarin and theophylline. The INR is the blood test used to evaluate warfarin ranges. The aPTT is the blood test used in monitoring heparin. The platelet count and ESR are not affected by clarithromycin.
2. A. White blood cell (WBC) count of 1200 units/L
Linezolid can cause reversible myelosuppression, manifesting as anemia, leukopenia, or even pancytopenia. The potassium and blood glucose levels are not affected by linezolid.
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