telithromycin


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telithromycin

(te-lith-roe-mye-sin) ,

Ketek

(trade name)

Classification

Therapeutic: anti infectives
Pharmacologic: ketolides
Pregnancy Category: C

Indications

Community-acquired pneumonia.

Action

Blocks bacterial protein synthesis at the level of the 50S ribosomal subunit.

Therapeutic effects

Resolution of infection.
Active against the following organisms: Staphylococcus aureus (methicillin and erythromycin susceptible strains only), Streptococcus pneumoniae (including multidurg-resistant strains), Haemophilus influenzae, Moraxella catarrhalis, Chlamydophila pneumoniae, and Mycoplasma pneumoniae.

Pharmacokinetics

Absorption: 57% absorbed following oral administration; unaffected by food.
Distribution: Concentrates in bronchial mucosa, epithelial lining fluid and alveolar macrophages.
Metabolism and Excretion: 70% metabolized by the liver (50% by CYP3A4), 13% excreted unchanged in urine, 7% excreted unchanged via biliary/intestinal elimination.
Half-life: 10 hr.

Time/action profile (blood levels)

ROUTEONSETPEAKDURATION
POrapid1 hr24 hr

Contraindications/Precautions

Contraindicated in: Hypersensitivity; History of hepatitis or jaundice associated with use of telithromycin; Hypersensitivity to macrolides (erythromycin, azithromycin, clarithromycin); Concurrent use of pimozide, ergot alkaloids, simvastatin, lovastatin, atorvastatin, or rifampin; Congenital QTc prolongation, uncorrected hypokalemia or hypomagnesemia, bradycardia, concurrent use of Class IA (quinidine, procainamide) or Class III antiarrhythmics (dofetilide); Concurrent use of colchicine in patients with renal or hepatic impairment; Myasthenia gravis; Lactation: Excreted in breast milk; consider alternative to breastfeeding.
Use Cautiously in: CCr <30 mL/min (dosage not established); Concurrent use of midazolam and other benzodiazpines; Obstetric: Use only if benefits outweigh risks to fetus; Pediatric: Safety not established.

Adverse Reactions/Side Effects

Central nervous system

  • confusion
  • hallucinations
  • loss of consciousness

Ear, Eye, Nose, Throat

  • visual disturbances

Cardiovascular

  • arrhythmias
  • QTc interval prolongation

Gastrointestinal

  • pseUdomembranous colitis (life-threatening)
  • diarrhea (most frequent)
  • hepatitis
  • HEPATotoxicity (life-threatening)
  • nausea

Neurologic

  • exacerbation of myasthenia gravis

Interactions

Drug-Drug interaction

Blood levels are ↑ by ketoconazole and itraconazole.↑ levels and risk of myopathy from simvastatin, lovastatin, and atorvastatin ; avoid concurrent use.↑ levels and risk of toxicity with colchicine ; avoid concurrent use in patients with renal or hepatic impairment; ↓ dose of colchicine if patients have normal renal and hepatic function.↑ levels and risk of excessive sedation with midazolam ; careful titration is required. Similar effects may occur with triazolam.↑ levels of metoprolol ; use caution in patients with HF.May also ↑ levels, effects and risk of toxicity from ergot derivatives (ergotamine, dihydroergotamine ); concurrent use not recommended; similar effects may occur with carbamazepine, cyclosporine, tacrolimus, sirolimus, hexobarbital, or phenytoin.Rifampin ↓ levels and effectiveness; avoid concurrent use. Similar effects may occur with phenytoin, carbamazepine, or phenobarbital.

Route/Dosage

Oral (Adults) community-acquired pneumonia—800 mg once daily for 7–10 days.

Availability

Tablets: 300 mg, 400 mg

Nursing implications

Nursing assessment

  • Assess for infection (vital signs; sputum, WBC) at beginning of and during therapy.
  • Obtain specimens for culture and sensitivity before initiating therapy. First dose may be given before receiving results.
  • Determine any family history of QTc prolongation or proarrythmic conditions (hypokalemia, bradycardia).
  • Monitor for signs or symptoms of hepatitis (fatigue, malaise, anorexia, nausea, jaundice, bilirubinuria, acholic stools, liver tenderness or hepatomegaly). If these occur, discontinue telithromycin immediately and monitor liver function; do not re-administer telithromycin.
  • Lab Test Considerations: May cause ↑ platelet count.
    • Monitor liver function periodically during therapy and if signs of hepatitis occur.

Potential Nursing Diagnoses

Risk for infection (Indications)
Noncompliance (Patient/Family Teaching)

Implementation

  • Oral: Administer with or without food. Swallow tablets whole; do not crush, break, or chew.

Patient/Family Teaching

  • Instruct patient to take medication as directed and to finish medication completely, even if feeling better. Take missed doses as soon as remembered, but do not take more than one dose in a 24–hr period. Advise patient to read Patient Information Sheet prior to starting therapy.
  • May cause visual disturbances (blurred vision, difficulty focusing, diplopia). Caution patient to avoid driving or other activities requiring visual acuity until response to medication is known. Advise patient to notify health care professional if visual disturbances interfere with daily activities.
  • Instruct patient to notify health care professional if fainting occurs.
  • Advise patient to report the signs of superinfection (black, furry overgrowth on the tongue; vaginal itching or discharge; loose or foul-smelling stools).
  • Instruct patient to notify health care professional if fever and diarrhea develop, especially if stool contains blood, pus, or mucus. Advise patient not to treat diarrhea without consulting health care professional.
  • Advise patient to discontinue telithromycin and notify health care professional immediately if signs of liver injury (nausea, fatigue, anorexia, jaundice, dark urine, light-colored stools, pruritus, or tender abdomen) occur.
  • Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
  • Advise patient to notify health care professional if pregnancy is planned or suspected or if breast feeding.

Evaluation/Desired Outcomes

  • Resolution of the signs and symptoms of infection. Length of time for complete resolution depends on the organism and site of infection.

telithromycin

an antiinfective.
indications This drug is used to treat acute bacterial exacerbation of chronic bronchitis caused by Streptococcus pneumoniae, Haemophilus influenzae, and Moraxella catarrhalis; acute bacterial sinusitis caused by S. pneumoniae, H. influenzae, M catarrhalis, and Staphylococcus aureus; and community-acquired pneumonia.
References in periodicals archive ?
A case report to highlight the above statement; one in which an individual case report identified the hepatotoxicity of telithromycin - an FDA approved drug - and underpinned poor drug testing practices.
Including itraconazole, ketoconazole, erythromycin, clarithromycin, telithromycin, nefazodone, HIV protease inhibitors and regular ingestion of grapefruit juice.
Some examples of strong CYP3A4 inhibitors are ketoconazole, itraconazole, posaconazole, clarithromycin, nefazodone, ritonavir, saquinavir, nelflnavir, indinavir, boceprevir, telaprevir, telithromycin, and conivaptan.
However, evidence for moxifloxacin and telithromycin suggests that a shorter course of 5-7 days is clinically and/or bacteriologically equivalent to a 10-day course.
Elevated hepatic transaminases associated with telithromycin therapy: A case report and literature review.
Predicting drug interaction potential with a physiologically based pharmacokinetic model: a case study of telithromycin, a time-dependent CYP3A inhibitor.
Options Other antibiotics in the same class (macrolides) include clarithromycin (Biaxin) and telithromycin (Ketek); however antibiotic choice depends on the infection itself and the pattern of antibiotic resistance in your area.
Resistance to erythromycin and telithromycin in Streptococcus pyogenes isolates obtained between 1999 and 2002 from Greek children with tonsillopharyngitis: phenotypic and genotypic analysis.
Disposition of oral telithromycin in foals and in vitro activity of the drug against macrolide-susceptible and macrolide-resistant Rhodococcus equi isolates.
Emergence of a Streptococcus pneumoniae clinical isolate highly resistant to telithromycin and fluoroquinolones.
The agency also noted that simvastatin should not be used along with the following drugs, which can increase the risk of myopathy: itraconazole, ketoconazole, posaconazole, erythromycin, clarithromycin, telithromycin, HIV protease inhibitors, nefazodone, gemfibrozil, cyclosporin and danazol.