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* This is the Professional Version. *

Telithromycin

By Hans P. Schlecht, MD, MSc; Christopher Bruno, MD

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Patient Education

Telithromycin is a ketolide antibiotic. Ketolides are chemically related to macrolides (see Macrolides) and inhibit bacterial ribosomal protein synthesis without inducing resistance to macrolides, clindamycin, or streptogramins. Telithromycin can have serious adverse effects and typically should not be selected if other, less toxic alternatives are available.

Telithromycin is rapidly absorbed orally with or without food and is metabolized primarily in the liver.

Indications

Telithromycin is active against erythromycin-susceptible staphylococci and streptococci and multidrug-resistant Streptococcus pneumoniae. Telithromycin is also active against erythromycin-susceptible enterococci, Bordetella pertussis, Haemophilus influenzae, Helicobacter pylori, Moraxella catarrhalis, Mycoplasma pneumoniae, Chlamydophila pneumoniae, and Legionella, Prevotella, and Peptostreptococcus spp.

Because of safety concerns, telithromycin is recommended only for the treatment of adults 18 yr with community-acquired mild to moderate pneumonia due to the following:

  • S. pneumoniae (including multidrug-resistant strains, ie, penicillin-resistant S. pneumoniae; isolates resistant to 2 of the following: penicillin, 2nd-generation cephalosporins [eg, cefuroxime], macrolides, tetracyclines, trimethoprim/sulfamethoxazole)

  • H. influenzae

  • M. catarrhalis

  • C. pneumoniae

  • M. pneumoniae

Contraindications

Contraindications include

  • Myasthenia gravis because telithromycin may exacerbate symptoms and fatal respiratory failure has occurred in patients with this disorder

  • Previous allergic reaction to telithromycin or any macrolide

  • Previous hepatitis or jaundice after taking telithromycin or a macrolide

  • Concurrent use of pimozide or cisapride because of cardiac arrhythmias (QT prolongation, ventricular tachycardia, ventricular fibrillation, torsades de pointes)

  • Concurrent use of colchicine in patients with renal or hepatic impairment

Use During Pregnancy and Breastfeeding

Telithromycin is in pregnancy category C because animal studies show some risk, evidence in human studies is inadequate, but clinical benefit sometimes outweighs risk.

Safety of telithromycin during breastfeeding is unknown.

Adverse Effects

Adverse effects include

  • GI disturbances

  • QT-interval prolongation

  • Severe hepatitis

Diarrhea, nausea, vomiting, and dizziness are the most common adverse effects.

Prolongation of the QT interval, hyperbilirubinemia, elevation of liver enzymes, transient loss of consciousness (sometimes associated with vagal syndrome), and visual disturbances (particularly a slowed ability to accommodate and to release accommodation) are less common. Because loss of consciousness or visual disturbance is a risk, patients should try to avoid potentially hazardous activities (eg, driving, operating dangerous equipment). Severe hepatotoxicity, which may require liver transplantation and which may be fatal, may occur.

Cross-sensitivity with macrolides can occur.

Dosing Considerations

Telithromycin inhibits cytochrome P-450 (CYP450) 3A4, increasing levels of the following drugs:

  • Digoxin: Digoxin adverse effects or serum levels should be monitored.

  • Ergot alkaloids: Concomitant use should be avoided.

  • Benzodiazepines: Concomitant use requires caution.

  • Metoprolol: Concomitant use in patients with heart failure requires caution.

  • Statins: Concomitant use of simvastatin, lovastatin, or atorvastatin (but not pravastatin or fluvastatin) should be avoided.

  • Cisapride: Concomitant use is contraindicated.

  • Pimozide: Concomitant use is contraindicated.

  • Sirolimus

  • Tacrolimus

CYP3A4 inducers such as rifampin, phenytoin, carbamazepine, and phenobarbital decrease levels of telithromycin; the CYP3A4 inhibitors itraconazole and ketoconazole increase levels of telithromycin. Telithromycin decreases absorption of sotalol.

Drugs Mentioned In This Article

  • Drug Name
    Select Trade
  • KETEK
  • CLEOCIN
  • No US brand name
  • CEFTIN, ZINACEF
  • ERY-TAB, ERYTHROCIN
  • PROPULSID
  • ORAP
  • COLCRYS
  • ZOCOR
  • BETAPACE
  • LANOXIN
  • LOPRESSOR, TOPROL-XL
  • LESCOL
  • TEGRETOL
  • PROGRAF
  • ALTOPREV
  • RIFADIN, RIMACTANE
  • LIPITOR
  • RAPAMUNE
  • NIZORAL
  • DILANTIN
  • PRAVACHOL
  • SPORANOX

* This is the Professional Version. *