TELITHROMYCIN (tel-i-thro-my'sin)
Ketek Classifications: antibiotic; ketolide; Therapeutic: antibiotic; ketolide Prototype: Erythromycin Pregnancy Category: C
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Availability
400 mg tablets
Action
Telithromycin binds to bacterial ribosomal RNa site of the 50S subunit; this action results in inhibition of RNA-dependent
protein synthesis of bacteria, thus resulting in cell death. Telithromycin concentrates in phagocytes where it works against
intracellular respiratory pathogens.
Therapeutic Effect
Its broad spectrum of activity is effective against respiratory pathogens, including erythromycin- and penicillin-resistant
pneumococci.
Uses
Treatment of mild to moderate community-acquired pneumonia.
Contraindications
Macrolide antibiotic hypersensitivity; QT prolongation; ongoing proarrhythmic conditions such as hypokalemia, hypomagnesemia,
significant bradycardia, concurrent administration of Class IA or Class III antiarrhythmic drugs; myasthenia gravis, unless
no other therapeutic option is available; severe renal impairment or renal failure; concurrent administration with terfenadine
or pimozide; viral infections; pregnancy (category C). Safety and efficacy in children <18 y are not established.
Cautious Use
History of GI disease; hepatic disease; history of hepatitis or jaundice; lactation.
Route & Dosage
Community-Acquired Pneumonia Adult: PO 800 mg once daily for 710 d
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Administration
Oral
- Do not administer concurrently with simvastatin, lovastatin, atorvastatin, Class 1A (e.g., quinidine, procainamide) or Class
III (e.g., dofetilide) antiarrhythmic agents. See drug interactions for other prohibited drug combinations.
- Store at 15°30° C (59°86° F). Keep container tightly closed. Protect from light.
Adverse Effects (≥1%)
CNS: Headache, dizziness.
CV: Potential to cause QT
c prolongation.
GI: Diarrhea, nausea, vomiting, loose stools, dysgeusia.
Metabolic: Elevated LFTs, liver failure.
Musculoskeletal: May exacerbate myasthenia gravis.
Special Senses: Blurred vision, diplopia, difficulty focusing.
Interactions
Drug: Pimozide or
class ia or
class iii antiarrhythmics may cause life-threatening arrhythmias; may increase concentrations of
atorvastatin, lovastatin, simvastatin, benzodiazepines;
rifampin decreases telithromycin levels;
ergot derivatives (ergotamine, dihydroergotamine) may cause severe peripheral vasospasm;
theophylline may exacerbate adverse GI effects.
Food: Grapefruit juice (>1 qt/d) may increase
plasma concentrations and adverse effects.
Pharmacokinetics
Absorption: 57% bioavailable.
Peak: 1 h.
Metabolism: 50% in liver (CYP3A4), 50% by CYP-independent mechanisms.
Elimination: In urine and feces.
Half-Life: 10 h.
Nursing Implications
Assessment & Drug Effects
- Monitor ECG in patients at risk for QTc interval prolongation (i.e., bradycardia).
- Withhold drug and notify physician for S&S of QTc interval prolongation such as dizziness or fainting; liver dysfunction.
- Lab tests: baseline LFTs, BUN and creatinine, serum potassium.
Patient & Family Education
- Stop taking drug and notify physician for episodes of dizziness or fainting; jaundice (yellow color of the skin and/or eyes).
- Exercise caution when engaging in potentially hazardous activities; visual disturbances (e.g., blurred vision, difficulty
focusing, double vision) are potential side effects of this drug. If visual problems occur, avoid quick changes in viewing
between close and distant objects.