Telithromycin

CLINICAL USE

Antibacterial agent

DOSE IN NORMAL RENAL FUNCTION

800 mg daily

PHARMACOKINETICS

Molecular weight :812

%Protein binding :60–70

%Excreted unchanged in urine : 12

Volume of distribution (L/kg) :1.9–3.9

half-life – normal/ESRD (hrs) :2–3/14.64

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

30–50 Dose as in normal renal function 10–30 600 mg daily (given as 800 mg/400 mg alternating days)

<10 : 600 mg daily (given as 800 mg/400 mg alternating days)

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD :Unknown dialysability. Dose as in GFR <10 mL/min

HD :Dialysed. Dose as in GFR <10 mL/min . (Give 800 mg dose after dialysis sessios)

HDF/high flux :Dialysed. Dose as in GFR <10 mL/min . (Give 800 mg dose after dialysis session)

CAV/VVHD :Dialysed. Dose as in GFR 10 to 20 mL/min

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Antibacterials: concentration reduced by rifampicin – avoid during and for 2 weeks after rifampicin therapy

Antidepressants: concentration reduced by St John’s wort – avoid during and for 2 weeks after St John’s wort therapy

Anti-epileptics: concentration reduced by carbamazepine, phenytoin, phenobarbital and primidone – avoid during and for 2 weeks after treatment

Antifungals: avoid in combination with ketoconazole in severe renal and hepatic impairment

Antipsychotics: increased risk of ventricular arrhythmias with pimozide – avoid concomitant use

Antivirals: avoid concomitant use with amprenavir, atazanavir, indinavir, lopinavir, nelfinavir, ritonavir, saquinavir and tipranavir in severe renal and hepatic impairmentAnxiolytics and hypnotics: inhibits metabolism of midazolam (increased sedation)

Ciclosporin: possibly increased ciclosporin levels

Diuretics: increased eplerenone concentration – avoid concomitant useTelithromycin and ergot derivatives should not be co-administered due to possibility of ergotismIvabradine: possibly increased ivabradine concentration – avoid concomitant useLipid-regulating drugs: increased risk of myopathy with atorvastatin and simvastatin – avoid concomitant useSirolimus: increased sirolimus levels – avoid concomitant use

Tacrolimus: possibly increased tacrolimus levels

ADMINISTRATION

Reconstition

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Route

Oral

Rate of Administration

–

Comments

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OTHER INFORMATION

Do not give to people at risk of QT interval prolongation due to its potential to prolong the QT intervalOral bioavailability is approximately 57% after a single dose of 800 mgIn patients with renal and hepatic impairment the dose should be reduced to 400 mg dailyMonitor for signs of liver toxicity AUC increased 2-fold if GFR<30 mL/min .

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