TELITHROMYCIN

TELITHROMYCIN
(tel-i-thro-my'sin)
Ketek
Classifications: antibiotic; ketolide;
Therapeutic: antibiotic; ketolide

Prototype: Erythromycin
Pregnancy Category: C

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 7–10 d

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 QTc 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.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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