- Tablets 300 mg
- Tablets 400 mg
Interferes with microbial protein synthesis.
Bioavailability 57%. C max approximately 2 mcg/mL after an 800 mg oral dose; peak level is reached in about 1 h. Steady-state plasma level reached in 2 to 3 days.
Protein binding is 60% to 70%. Vd is 2.9 L/kg.
Approximately 70% of dose is metabolized. About 50% of metabolism is mediated by CYP3A4.
Terminal elimination t ½ is about 10 h. Elimination consists of 7% unchanged in feces, 13% unchanged in the urine, and 37% metabolized by the liver.
Indications and Usage
Treatment of community-acquired pneumonia of mild to moderate severity caused by Streptococcus pneumoniae (including multi-drug resistant isolates), Haemophilus influenzae , Moraxella catarrhalis , Chlamydophila pneumoniae , or Mycoplasma pneumoniae .
Coadministration of cisapride or pimozide; history of hepatitis, jaundice, or hypersensitivity to any macrolide antibiotic or any component of this product; myasthenia gravis.
Dosage and AdministrationAdults
PO 800 mg daily for 7 to 10 days.Severe Renal Function Impairment
PO In severe renal function impairment (CrCl less than 30 mL/min), including patients on dialysis, reduce the dosage to 600 mg once daily. In patients undergoing hemodialysis, give the drug after the dialysis session on dialysis days. In severe renal function impairment with coexisting hepatic function impairment, reduce the dosage to 400 mg once daily.
Store tablets at controlled room temperature (59° to 86°F).
Drug InteractionsAtorvastatin, lovastatin, simvastatin
Telithromycin may elevate plasma levels of these agents, increasing the risk of adverse reactions (eg, myopathy).Carbamazepine, cyclosporine, hexobarbital, metoprolol, midazolam, phenytoin, ranolazine, sirolimus, tacrolimus
Telithromycin may elevate plasma levels of these agents, increasing the pharmacologic and adverse reactions.Carbamazepine, phenobarbital, phenytoin, rifampin
May decrease telithromycin plasma concentrations, resulting in subtherapeutic levels and loss of efficacy.Cisapride, pimozide
Concurrent use of these agents with telithromycin is contraindicated.Class IA (eg, procainamide, quinidine) and class III (eg, dofetilide) antiarrhythmic agents
Because telithromycin has the potential to prolong the QTc interval, avoid coadministration of telithromycin and agents in these classes.Digoxin
Digoxin peak plasma concentrations may be elevated.Ergot alkaloid derivatives (eg, dihydroergotamine, ergotamine)
Acute ergot toxicity characterized by severe peripheral vasospasm and dysesthesia may occur.Itraconazole, ketoconazole
May increase telithromycin plasma concentrations.Midazolam, triazolam
Elevated plasma concentrations of these drugs may occur, increasing the therapeutic and adverse reactions.Sotalol
Sotalol plasma levels may be decreased by telithromycin.Theophylline
Theophylline plasma concentrations may be elevated, increasing the risk of adverse reactions.Verapamil
Risk of cardiotoxicity may be increased.Warfarin
There have been postmarketing reports of potentiation of the effects of oral anticoagulants.
Laboratory Test Interactions
None well documented.
Atrial arrhythmias, palpitations (postmarketing).
Headache (6%); dizziness (4%); fatigue, insomnia, somnolence, vertigo (less than 2%); loss of consciousness (sometimes associated with vagal syndrome), syncope (postmarketing).
Increased sweating, rash (less than 2%).
Visual adverse reactions, including blurred vision, difficulty focusing, and diplopia (less than 2%).
Diarrhea (11%); nausea (8%); vomiting (3%); dysgeusia, loose stools (2%); abdominal distension, abdominal pain, anorexia, constipation, dry mouth, dyspepsia, flatulence, gastritis, gastroenteritis, GI upset, glossitis, oral candidiasis, stomatitis, upper abdominal pain, watery stools (less than 2%); pancreatitis (postmarketing).
Vaginal candidiasis, vaginal fungal infection, vaginitis (less than 2%).
Increased platelet count (less than 2%).
Abnormal LFTs, increased liver enzymes (eg, ALT, AST), increased transaminases (less than 2%); hepatic function impairment, including fulminent hepatitis, hepatic failure, and hepatic necrosis (postmarketing).
Exacerbation of myasthenia gravis, muscle cramps (postmarketing).
Allergy, including anaphylaxis, angioedema, and face edema (postmarketing).
There have been reports of fatal and life-threatening respiratory failure in patients with myasthenia gravis associated with telithromycin administration.
Monitor for signs or symptoms of hepatitis such as anorexia, fatigue, jaundice, malaise, or nausea.
Category C .
Safety and efficacy not established.
Dosage reduction required in severe renal function impairment.
Prolonged use of antibiotics may result in bacterial or fungal overgrowth of nonsusceptible microorganisms.
Acute hepatic failure and severe liver injury, sometimes fatal, may occur. Do not administer to patients with a history of hepatitis and/or jaundice associated with telithromycin use.
Loss of consciousness
Has been reported and in some cases has been associated with vagal syndrome.
Consider possibility in patients who develop diarrhea.
May be prolonged in some patients.
Ability to accommodate and ability to release accommodation may be slowed.
Carefully monitor ECG and electrolytes.
- Caution patient that the drug may cause fainting and impact the ability to drive, especially if patient is experiencing severe nausea, vomiting, or lightheadedness. Caution patient to avoid driving, operating heavy machinery, and engaging in hazardous tasks if these symptoms are experienced.
- Instruct patient to take exactly as prescribed and not to change the dose or discontinue therapy unless advised by health care provider.
- Instruct patient to take prescribed dose at the same time once daily. Advise patient that medication can be taken without regard to meals, but to take with food if stomach upset occurs.
- Instruct patient to complete entire course of therapy, even if symptoms of infection have disappeared.
- Instruct patient to notify health care provider if infection does not appear to be improving or appears to be getting worse.
- Advise patient to discontinue therapy and contact health care provider immediately if fainting, hives, itching, palpitations, shortness of breath, or skin rash occur.
- Advise patient to discontinue therapy and contact health care provider immediately if signs or symptoms of liver disease (eg, dark urine, itchy skin, light-colored stools, nausea, stomach pains, yellowing of skin or eyes) occur.
- Advise patient to report the following signs of superinfection to health care provider: black, “furry” tongue; foul-smelling stools; vaginal itching or discharge; white patches in mouth.
- Warn patient that diarrhea containing blood or pus may be a sign of a serious disorder and to seek medical care if noted and to not treat at home. Caution patient that this may occur even weeks after completing therapy.
- Caution patient that drug may cause visual disturbances (eg, blurred vision, difficulty focusing, double vision) and to use caution while driving or performing other potentially hazardous activities until tolerance is determined. If visual problems develop, advise patient that avoiding quick changes in viewing distant and nearby objects may help decrease the effects. Advise patient to contact health care provider if visual difficulties interfere with daily activities.
- Advise patient to report any other bothersome adverse reactions to health care provider.
Copyright © 2009 Wolters Kluwer Health.
More about telithromycin
- Other brands: Ketek