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telithromycin
Overview
What is Ketek?
KETEK tablets contain telithromycin, a semisynthetic antibacterial in the ketolide class for oral administration. Chemically, telithromycin is designated as Erythromycin, 3-de[(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribo-hexopyranosyl)oxy]-11,12-dideoxy-6-O-methyl-3-oxo-12,11-[oxycarbonyl[[4-[4-(3-pyridinyl)-1H-imidazol-1-yl]butyl]imino]]-.
Telithromycin, a ketolide, differs chemically from the macrolide group of antibacterials by the lack of α-L-cladinose at position 3 of the erythronolide A ring, resulting in a 3-keto function. It is further characterized by a C11-12 carbamate substituted by an imidazolyl and pyridyl ring through a butyl chain. Its empirical formula is CHNOand its molecular weight is 812.03. Telithromycin is a white to off-white crystalline powder. The following represents the chemical structure of telithromycin.
KETEK tablets are available as light-orange, oval, film-coated tablets, each containing 400 mg or 300 mg of telithromycin, and the following inactive ingredients: croscarmellose sodium, hypromellose, magnesium stearate, microcrystalline cellulose, polyethylene glycol, povidone, red ferric oxide, talc, titanium dioxide, and yellow ferric oxide.
What does Ketek look like?
What are the available doses of Ketek?
Sorry No records found.
What should I talk to my health care provider before I take Ketek?
Sorry No records found
How should I use Ketek?
The dose of KETEK tablets is 800 mg (2 tablets of 400 mg) taken orally once every 24 hours, for 7–10 days. KETEK tablets can be administered with or without food.
KETEK may be administered without dosage adjustment in the presence of hepatic impairment.
In the presence of severe renal impairment (CL < 30 mL/min), including patients who need dialysis, the dose should be reduced to KETEK 600 mg once daily. In patients undergoing hemodialysis, KETEK should be given after the dialysis session on dialysis days. (See .)
In the presence of severe renal impairment (CL < 30 mL/min), with coexisting hepatic impairment, the dose should be reduced to KETEK 400 mg once daily. (See .)
What interacts with Ketek?
KETEK is contraindicated in patients with myasthenia gravis.
KETEK is contraindicated in patients with previous history of hepatitis and/or jaundice associated with the use of KETEK tablets, or any macrolide antibiotic.
KETEK is contraindicated in patients with a history of hypersensitivity to telithromycin and/or any components of KETEK tablets, or any macrolide antibiotic.
Concomitant administration of KETEK with cisapride or pimozide is contraindicated. (See and .)
Concomitant administration of KETEK and colchicine is contraindicated in patients with renal or hepatic impairment. (See and .)
What are the warnings of Ketek?
Hepatotoxicity
QTc prolongation
Telithromycin has the potential to prolong the QTc interval of the electrocardiogram in some patients. QTc prolongation may lead to an increased risk for ventricular arrhythmias, including torsades de pointes. Thus, telithromycin should be avoided in patients with congenital prolongation of the QTc interval, and in patients with ongoing proarrhythmic conditions such as uncorrected hypokalemia or hypomagnesemia, clinically significant bradycardia, and in patients receiving Class IA (e.g., quinidine and procainamide) or Class III (e.g., dofetilide) antiarrhythmic agents.
Cases of torsades de pointes have been reported post-marketing with KETEK. In clinical trials, no cardiovascular morbidity or mortality attributable to QTc prolongation occurred with telithromycin treatment in 4780 patients in clinical trials, including 204 patients having a prolonged QTc at baseline.
Visual disturbances*
KETEK may cause visual disturbances particularly in slowing the ability to accommodate and the ability to release accommodation.
Loss of Consciousness*
Drug Interactions
Serious adverse reactions have been reported in patients taking KETEK concomitantly with CYP 3A4 substrates. These include colchicine toxicity with colchicine; rhabdomyolysis with simvastatin, lovastatin, and atorvastatin; and hypotension with calcium channel blockers metabolized by CYP 3A4 (e.g., verapamil, amlodipine, diltiazem). (See .)
Life-threatening and fatal drug interactions have been reported in patients treated with colchicine and strong CYP 3A4 inhibitors. Telithromycin is a strong CYP 3A4 inhibitor and this interaction may occur while using both drugs at their recommended doses. If co-administration of telithromycin and colchicine is necessary in patients with normal renal and hepatic function, the dose of colchicine should be reduced. Patients should be monitored for clinical symptoms of colchicine toxicity. Concomitant administration of KETEK and colchicine is contraindicated in patients with renal or hepatic impairment. (See and .)
Pseudomembranous colitis
What are the precautions of Ketek?
General
Prescribing KETEK in the absence of a proven or strongly suspected bacterial infection or a prophylactic indication is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria.
Telithromycin is principally excreted via the liver and kidney. Telithromycin may be administered without dosage adjustment in the presence of hepatic impairment. In the presence of severe renal impairment (CL < 30 mL/min), a reduced dosage of KETEK is recommended. (See )
Information for patients
Because of potential visual difficulties, loss of consciousness, confusion or hallucinations, patients should attempt to minimize activities such as driving a motor vehicle, operating heavy machinery or engaging in other hazardous activities during treatment with KETEK.
- Because of potential visual difficulties, loss of consciousness, confusion or hallucinations, patients should attempt to minimize activities such as driving a motor vehicle, operating heavy machinery or engaging in other hazardous activities during treatment with KETEK.
- patients should seek advice from their physician before taking another dose
- patients should not drive a motor vehicle, operate heavy machinery, or engage in otherwise hazardous activities.
Ketek is contraindicated in patients with myasthenia gravis.
Array
CONTRAINDICATIONS
- Array
- of the possibility of liver injury, associated with KETEK, which in rare cases may be severe. Symptoms of liver injury may include nausea, fatigue, anorexia, jaundice, dark urine, light-colored stools, pruritus, or tender abdomen. Ketek must not be taken by patients with a previous history of hepatitis/jaundice associated with the use of KETEK or macrolide antibiotics.(See and )
- antibacterial drugs including KETEK should only be used to treat bacterial infections. They do not treat viral infections (e.g., the common cold). When KETEK is prescribed to treat a bacterial infection, patients should be told that although it is common to feel better early in the course of therapy, the medication should be taken exactly as directed. Skipping doses or not completing the full course of therapy may (1) decrease the effectiveness of the immediate treatment and (2) increase the likelihood that bacteria will develop resistance and will not be treatable by KETEK or other antibacterial drugs in the future.
- KETEK has the potential to produce changes in the electrocardiogram (QTc interval prolongation) and that they should report any fainting occurring during drug treatment.
- KETEK should be avoided in patients receiving Class 1A (e.g., quinidine, procainamide) or Class III (e.g., dofetilide) antiarrhythmic agents.
- to inform their physician of any personal or family history of QTc prolongation or proarrhythmic conditions such as uncorrected hypokalemia, or clinically significant bradycardia.
- diarrhea is a common problem caused by antibiotics which usually ends when the antibiotic is discontinued. Sometimes after starting treatment with antibiotics, patients can develop watery and bloody stools (with or without stomach cramps and fever) even as late as two or more months after having taken the last dose of the antibiotic. If this occurs, patients should contact their physician as soon as possible
- simvastatin, lovastatin, or atorvastatin should be avoided in patients receiving KETEK. If KETEK is prescribed, therapy with simvastatin, lovastatin, or atorvastatin should be stopped during the course of treatment. (See )
- colchicine should be avoided in patients receiving KETEK. If KETEK is prescribed in patients with normal kidney and liver function, the dose is colchicine should be reduced. Concomitant treatment with KETEK and colchicine is contraindicated in patients with kidney or liver impairment. (See )
- KETEK tablets can be taken with or without food.
- to inform their physician of any other medications taken concurrently with KETEK, including over-the-counter medications and dietary supplements.
A Medication Guide is provided to patients when Ketek is dispensed. Patients should be instructed to read the MedGuide when Ketek is received. In addition, the complete text of the MedGuide is reprinted at the end of this document.
The following information and instructions should be communicated to the patient.
Patients should be advised that avoiding quick changes in viewing between objects in the distance and objects nearby may help to decrease the effects of these visual difficulties.
If patients experience visual difficulties, loss of consciousness / fainting, confusion or hallucination
Patients should also be advised:
Drug interactions
Telithromycin is a strong inhibitor of the cytochrome P450 3A4 system. Co-administration of KETEK tablets and a drug primarily metabolized by the cytochrome P450 3A4 enzyme system may result in increased plasma concentration of the drug co-administered with telithromycin that could increase or prolong both the therapeutic and adverse effects. Therefore, appropriate dosage adjustments may be necessary for the drug co-administered with telithromycin.
The use of KETEK is contraindicated with cisapride. (See and )
The use of KETEK is contraindicated with pimozide. Although there are no studies looking at the interaction between KETEK and pimozide, there is a potential risk of increased pimozide plasma levels by inhibition of CYP 3A4 pathways by KETEK as with macrolides. (See )
In a pharmacokinetic study, simvastatin levels were increased due to CYP 3A4 inhibition by telithromycin. (See ) Similarly, an interaction may occur with lovastatin or atorvastatin but not with statins which are not metabolized by CYP3A4.
High levels of HMG-CoA reductase inhibitors increase the risk of myopathy and rhabdomyolysis. Use of simvastatin, lovastatin, or atorvastatin concomitantly with KETEK should be avoided. If KETEK is prescribed, therapy with simvastatin, lovastatin, or atorvastatin should be suspended during the course of treatment. Patients concomitantly treated with statins should be carefully monitored for signs and symptoms of myopathy and rhabdomyolysis.
Colchicine is a substrate for both CYP 3A4 and the efflux transporter, P-glycoprotein (P-gp), and a significant increase in colchicine plasma concentration is anticipated when co-administered with strong CYP 3A4 inhibitors such as telithromycin. (See and
Monitoring of digoxin side effects or serum levels should be considered during concomitant administration of digoxin and KETEK. (See
Hypotension, bradyarrhythmia and loss of consciousness have been observed in patients receiving concomitant treatment with calcium channel blockers that are substrates of CYP 3A4 (e.g., verapamil, amlodipine, diltiazem).
Patients should be monitored with concomitant administration of midazolam and dosage adjustment of midazolam should be considered if necessary. Precaution should be used with other benzodiazepines, which are metabolized by CYP 3A4 and undergo a high first-pass effect (e.g., triazolam). (See )
Concomitant treatment of KETEK with rifampin, a CYP 3A4 inducer, should be avoided. Concomitant administration of other CYP 3A4 inducers such as phenytoin, carbamazepine, or phenobarbital is likely to result in subtherapeutic levels of telithromycin and loss of effect. (See .)
In patients treated with metoprolol for heart failure, the increased exposure to metoprolol, a CYP 2D6 substrate, may be of clinical importance. Therefore, co-administration of KETEK and metoprolol in patients with heart failure should be considered with caution. (See )
Spontaneous post-marketing reports suggest that administration of KETEK and oral anticoagulants concomitantly may potentiate the effects of the oral anticoagulants. Consideration should be given to monitoring prothrombin times/INR while patients are receiving KETEK and oral anticoagulants simultaneously.
No specific drug interaction studies have been performed to evaluate the following potential drug-drug interactions with KETEK. However, these drug interactions have been observed with macrolide products.
Drugs metabolized by the cytochrome P450 system such as carbamazepine, cyclosporine, tacrolimus, sirolimus, hexobarbital, and phenytoin: elevation of serum levels of these drugs may be observed when co-administered with telithromycin. As a result, increases or prolongation of the therapeutic and/or adverse effects of the concomitant drug may be observed.
Ergot alkaloid derivatives (such as ergotamine or dihydroergotamine): acute ergot toxicity characterized by severe peripheral vasospasm and dysesthesia has been reported when macrolide antibiotics were co-administered. Without further data, the co-administration of KETEK and these drugs is not recommended.
Laboratory test interactions
There are no reported laboratory test interactions.
Carcinogenesis, mutagenesis, impairment of fertility
Long-term studies in animals to determine the carcinogenic potential of KETEK have not been conducted.
Telithromycin showed no evidence of genotoxicity in four tests: gene mutation in bacterial cells, gene mutation in mammalian cells, chromosome aberration in human lymphocytes, and the micronucleus test in the mouse.
No evidence of impaired fertility in the rat was observed at doses estimated to be 0.61 times the human daily dose on a mg/m basis. At doses of 1.8–3.6 times the human daily dose, at which signs of parental toxicity were observed, moderate reductions in fertility indices were noted in male and female animals treated with telithromycin.
Pregnancy
Pregnancy Category C
Telithromycin was not teratogenic in the rat or rabbit. Reproduction studies have been performed in rats and rabbits, with effect on pre-post natal development studied in the rat. At doses estimated to be 1.8 times (900 mg/m) and 0.49 times (240 mg/m) the daily human dose of 800 mg (492 mg/m) in the rat and rabbit, respectively, no evidence of fetal terata was found. At doses higher than the 900 mg/m and 240 mg/m in rats and rabbits, respectively, maternal toxicity may have resulted in delayed fetal maturation. No adverse effects on prenatal and postnatal development of rat pups were observed at 1.5 times (750 mg/m/d) the daily human dose.
There are no adequate and well-controlled studies in pregnant women. Telithromycin should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Nursing mothers
Telithromycin is excreted in breast milk of rats. Telithromycin may also be excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when KETEK is administered to a nursing mother.
Pediatric use
The safety and effectiveness of KETEK in pediatric patients has not been established.
Geriatric use
In all Phase III clinical trials (n=4,780), KETEK was administered to 694 patients who were 65 years and older, including 231 patients who were 75 years and older. Efficacy and safety in elderly patients ≥ 65 years were generally similar to that observed in younger patients; however, greater sensitivity of some older individuals cannot be ruled out. No dosage adjustment is required based on age alone. (See and )
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What are the side effects of Ketek?
In Phase III clinical trials, 4,780 patients (n=2702 in controlled trials) received daily oral doses of KETEK 800 mg once daily for 5 days or 7 to 10 days. Most adverse events were mild to moderate in severity. In the combined Phase III studies, discontinuation due to treatment-emergent adverse events occurred in 4.4% of KETEK-treated patients and 4.3% of combined comparator-treated patients. Most discontinuations in the KETEK group were due to treatment-emergent adverse events in the gastrointestinal body system, primarily diarrhea (0.9% for KETEK vs. 0.7% for comparators), nausea (0.7% for KETEK vs. 0.5% for comparators).
All and possibly related treatment-emergent adverse events (TEAEs) occurring in controlled clinical studies in ≥ 2.0% of all patients are included below:
The following events judged by investigators to be at least possibly drug related were observed infrequently (≥ 0.2% and < 2%), in KETEK-treated patients in the controlled Phase III studies.
Gastrointestinal system:
Liver and biliary system:
Nervous system:
Body as a whole:
Special senses:
Females and patients under 40 years old experienced a higher incidence of telithromycin-associated visual adverse events. (See .)
Urogenital system:
Skin:
Hematologic:
Other possibly related clinically-relevant events occurring in <0.2% of patients treated with KETEK from the controlled Phase III studies included:
| Adverse Event | All TEAEs | Possibly-Related TEAEs | |||
|---|---|---|---|---|---|
| KETEKn= 2702 | Comparator n= 2139 | KETEKn= 2702 | Comparator n= 2139 | ||
| Diarrhea | 10.8% | 8.6% | 10.0% | 8.0% | |
| Nausea | 7.9% | 4.6% | 7.0% | 4.1% | |
| Headache | 5.5% | 5.8% | 2.0% | 2.5% | |
| Dizziness (excl. vertigo) | 3.7% | 2.7% | 2.8% | 1.5% | |
| Vomiting | 2.9% | 2.2% | 2.4% | 1.4% | |
| Loose Stools | 2.3% | 1.5% | 2.1% | 1.4% | |
| Dysgeusia | 1.6% | 3.6% | 1.5% | 3.6% |
Post-Marketing Adverse Event Reports
In addition to adverse events reported from clinical trials, the following events have been reported from worldwide post-marketing experience with KETEK.
Allergic: face edema, rare reports of severe allergic (hypersensitivity) reactions, including angioedema and anaphylaxis
Cardiovascular: atrial arrhythmias, palpitations
Gastrointestinal system: pancreatitis
Liver and biliary system: Hepatic dysfunction has been reported.
Severe and in some cases fatal hepatotoxicity, including fulminant hepatitis, hepatic necrosis and hepatic failure have been reported in patients treated with KETEK. These hepatic reactions were observed during or immediately after treatment. In some of these cases, liver injury progressed rapidly and occurred after administration of only a few doses of KETEK. (See and .) Severe reactions, in some but not all cases, have been associated with serious underlying diseases or concomitant medications.
Data from post-marketing reports and clinical trials show that most cases of hepatic dysfunction were mild to moderate. (See .)
Musculoskeletal: muscle cramps, rare reports of exacerbation of myasthenia gravis. (See ) arthralgia, myalgia
Nervous system: loss of consciousness, in some cases associated with vagal syndrome.
Psychiatric disorders: confusion, hallucinations (mostly visual)
Special senses: taste/smell perversion and/or loss
What should I look out for while using Ketek?
KETEK is contraindicated in patients with myasthenia gravis.
KETEK is contraindicated in patients with previous history of hepatitis and/or jaundice associated with the use of KETEK tablets, or any macrolide antibiotic.
KETEK is contraindicated in patients with a history of hypersensitivity to telithromycin and/or any components of KETEK tablets, or any macrolide antibiotic.
Concomitant administration of KETEK with cisapride or pimozide is contraindicated. (See and .)
Concomitant administration of KETEK and colchicine is contraindicated in patients with renal or hepatic impairment. (See and .)
What might happen if I take too much Ketek?
In the event of acute overdosage, the stomach should be emptied by gastric lavage. The patient should be carefully monitored (e.g., ECG, electrolytes) and given symptomatic and supportive treatment. Adequate hydration should be maintained. The effectiveness of hemodialysis in an overdose situation with KETEK is unknown.
How should I store and handle Ketek?
Protect from light. Keep covered in carton until time of use. Store at 20˚-25˚C (68˚-77˚F), excursions permitted to 15˚-30˚C (59˚-86˚F) [See USP Controlled Room Temperature].To report SUSPECTED ADVERSE REACTIONS, contact West-Ward Pharmaceutical Corp. at 1-877-845-0689, or the FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.For Product Inquiry call 1-877-845-0689.Manufactured by:WEST-WARD PHARMACEUTICALSRevised May 2011462-220-01Repackaged by: REBEL DISTRIBUTORS CORPThousand Oaks, CA 91320Protect from light. Keep covered in carton until time of use. Store at 20˚-25˚C (68˚-77˚F), excursions permitted to 15˚-30˚C (59˚-86˚F) [See USP Controlled Room Temperature].To report SUSPECTED ADVERSE REACTIONS, contact West-Ward Pharmaceutical Corp. at 1-877-845-0689, or the FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.For Product Inquiry call 1-877-845-0689.Manufactured by:WEST-WARD PHARMACEUTICALSRevised May 2011462-220-01Repackaged by: REBEL DISTRIBUTORS CORPThousand Oaks, CA 91320Protect from light. Keep covered in carton until time of use. Store at 20˚-25˚C (68˚-77˚F), excursions permitted to 15˚-30˚C (59˚-86˚F) [See USP Controlled Room Temperature].To report SUSPECTED ADVERSE REACTIONS, contact West-Ward Pharmaceutical Corp. at 1-877-845-0689, or the FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.For Product Inquiry call 1-877-845-0689.Manufactured by:WEST-WARD PHARMACEUTICALSRevised May 2011462-220-01Repackaged by: REBEL DISTRIBUTORS CORPThousand Oaks, CA 91320Protect from light. Keep covered in carton until time of use. Store at 20˚-25˚C (68˚-77˚F), excursions permitted to 15˚-30˚C (59˚-86˚F) [See USP Controlled Room Temperature].To report SUSPECTED ADVERSE REACTIONS, contact West-Ward Pharmaceutical Corp. at 1-877-845-0689, or the FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.For Product Inquiry call 1-877-845-0689.Manufactured by:WEST-WARD PHARMACEUTICALSRevised May 2011462-220-01Repackaged by: REBEL DISTRIBUTORS CORPThousand Oaks, CA 91320Protect from light. Keep covered in carton until time of use. Store at 20˚-25˚C (68˚-77˚F), excursions permitted to 15˚-30˚C (59˚-86˚F) [See USP Controlled Room Temperature].To report SUSPECTED ADVERSE REACTIONS, contact West-Ward Pharmaceutical Corp. at 1-877-845-0689, or the FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.For Product Inquiry call 1-877-845-0689.Manufactured by:WEST-WARD PHARMACEUTICALSRevised May 2011462-220-01Repackaged by: REBEL DISTRIBUTORS CORPThousand Oaks, CA 91320Protect from light. Keep covered in carton until time of use. Store at 20˚-25˚C (68˚-77˚F), excursions permitted to 15˚-30˚C (59˚-86˚F) [See USP Controlled Room Temperature].To report SUSPECTED ADVERSE REACTIONS, contact West-Ward Pharmaceutical Corp. at 1-877-845-0689, or the FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.For Product Inquiry call 1-877-845-0689.Manufactured by:WEST-WARD PHARMACEUTICALSRevised May 2011462-220-01Repackaged by: REBEL DISTRIBUTORS CORPThousand Oaks, CA 91320Protect from light. Keep covered in carton until time of use. Store at 20˚-25˚C (68˚-77˚F), excursions permitted to 15˚-30˚C (59˚-86˚F) [See USP Controlled Room Temperature].To report SUSPECTED ADVERSE REACTIONS, contact West-Ward Pharmaceutical Corp. at 1-877-845-0689, or the FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.For Product Inquiry call 1-877-845-0689.Manufactured by:WEST-WARD PHARMACEUTICALSRevised May 2011462-220-01Repackaged by: REBEL DISTRIBUTORS CORPThousand Oaks, CA 91320Protect from light. Keep covered in carton until time of use. Store at 20˚-25˚C (68˚-77˚F), excursions permitted to 15˚-30˚C (59˚-86˚F) [See USP Controlled Room Temperature].To report SUSPECTED ADVERSE REACTIONS, contact West-Ward Pharmaceutical Corp. at 1-877-845-0689, or the FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.For Product Inquiry call 1-877-845-0689.Manufactured by:WEST-WARD PHARMACEUTICALSRevised May 2011462-220-01Repackaged by: REBEL DISTRIBUTORS CORPThousand Oaks, CA 91320KETEK 400 mg tablets are supplied as light-orange, oval, film-coated tablets, imprinted "H3647" on one side and "400" on the other side. These are packaged in bottles or blister cards (Ketek Pak™ and unit dose) as follows:
Clinical Information
Chemical Structure
No Image foundClinical Pharmacology
Non-Clinical Toxicology
KETEK is contraindicated in patients with myasthenia gravis.KETEK is contraindicated in patients with previous history of hepatitis and/or jaundice associated with the use of KETEK tablets, or any macrolide antibiotic.
KETEK is contraindicated in patients with a history of hypersensitivity to telithromycin and/or any components of KETEK tablets, or any macrolide antibiotic.
Concomitant administration of KETEK with cisapride or pimozide is contraindicated. (See and .)
Concomitant administration of KETEK and colchicine is contraindicated in patients with renal or hepatic impairment. (See and .)
Telithromycin is a strong inhibitor of the cytochrome P450 3A4 system. Co-administration of KETEK tablets and a drug primarily metabolized by the cytochrome P450 3A4 enzyme system may result in increased plasma concentration of the drug co-administered with telithromycin that could increase or prolong both the therapeutic and adverse effects. Therefore, appropriate dosage adjustments may be necessary for the drug co-administered with telithromycin.
The use of KETEK is contraindicated with cisapride. (See and )
The use of KETEK is contraindicated with pimozide. Although there are no studies looking at the interaction between KETEK and pimozide, there is a potential risk of increased pimozide plasma levels by inhibition of CYP 3A4 pathways by KETEK as with macrolides. (See )
In a pharmacokinetic study, simvastatin levels were increased due to CYP 3A4 inhibition by telithromycin. (See ) Similarly, an interaction may occur with lovastatin or atorvastatin but not with statins which are not metabolized by CYP3A4.
High levels of HMG-CoA reductase inhibitors increase the risk of myopathy and rhabdomyolysis. Use of simvastatin, lovastatin, or atorvastatin concomitantly with KETEK should be avoided. If KETEK is prescribed, therapy with simvastatin, lovastatin, or atorvastatin should be suspended during the course of treatment. Patients concomitantly treated with statins should be carefully monitored for signs and symptoms of myopathy and rhabdomyolysis.
Colchicine is a substrate for both CYP 3A4 and the efflux transporter, P-glycoprotein (P-gp), and a significant increase in colchicine plasma concentration is anticipated when co-administered with strong CYP 3A4 inhibitors such as telithromycin. (See and
Monitoring of digoxin side effects or serum levels should be considered during concomitant administration of digoxin and KETEK. (See
Hypotension, bradyarrhythmia and loss of consciousness have been observed in patients receiving concomitant treatment with calcium channel blockers that are substrates of CYP 3A4 (e.g., verapamil, amlodipine, diltiazem).
Patients should be monitored with concomitant administration of midazolam and dosage adjustment of midazolam should be considered if necessary. Precaution should be used with other benzodiazepines, which are metabolized by CYP 3A4 and undergo a high first-pass effect (e.g., triazolam). (See )
Concomitant treatment of KETEK with rifampin, a CYP 3A4 inducer, should be avoided. Concomitant administration of other CYP 3A4 inducers such as phenytoin, carbamazepine, or phenobarbital is likely to result in subtherapeutic levels of telithromycin and loss of effect. (See .)
In patients treated with metoprolol for heart failure, the increased exposure to metoprolol, a CYP 2D6 substrate, may be of clinical importance. Therefore, co-administration of KETEK and metoprolol in patients with heart failure should be considered with caution. (See )
Spontaneous post-marketing reports suggest that administration of KETEK and oral anticoagulants concomitantly may potentiate the effects of the oral anticoagulants. Consideration should be given to monitoring prothrombin times/INR while patients are receiving KETEK and oral anticoagulants simultaneously.
No specific drug interaction studies have been performed to evaluate the following potential drug-drug interactions with KETEK. However, these drug interactions have been observed with macrolide products.
Drugs metabolized by the cytochrome P450 system such as carbamazepine, cyclosporine, tacrolimus, sirolimus, hexobarbital, and phenytoin: elevation of serum levels of these drugs may be observed when co-administered with telithromycin. As a result, increases or prolongation of the therapeutic and/or adverse effects of the concomitant drug may be observed.
Ergot alkaloid derivatives (such as ergotamine or dihydroergotamine): acute ergot toxicity characterized by severe peripheral vasospasm and dysesthesia has been reported when macrolide antibiotics were co-administered. Without further data, the co-administration of KETEK and these drugs is not recommended.
Prescribing KETEK in the absence of a proven or strongly suspected bacterial infection or a prophylactic indication is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria.
Telithromycin is principally excreted via the liver and kidney. Telithromycin may be administered without dosage adjustment in the presence of hepatic impairment. In the presence of severe renal impairment (CL < 30 mL/min), a reduced dosage of KETEK is recommended. (See )
In Phase III clinical trials, 4,780 patients (n=2702 in controlled trials) received daily oral doses of KETEK 800 mg once daily for 5 days or 7 to 10 days. Most adverse events were mild to moderate in severity. In the combined Phase III studies, discontinuation due to treatment-emergent adverse events occurred in 4.4% of KETEK-treated patients and 4.3% of combined comparator-treated patients. Most discontinuations in the KETEK group were due to treatment-emergent adverse events in the gastrointestinal body system, primarily diarrhea (0.9% for KETEK vs. 0.7% for comparators), nausea (0.7% for KETEK vs. 0.5% for comparators).
All and possibly related treatment-emergent adverse events (TEAEs) occurring in controlled clinical studies in ≥ 2.0% of all patients are included below:
The following events judged by investigators to be at least possibly drug related were observed infrequently (≥ 0.2% and < 2%), in KETEK-treated patients in the controlled Phase III studies.
Gastrointestinal system:
Liver and biliary system:
Nervous system:
Body as a whole:
Special senses:
Females and patients under 40 years old experienced a higher incidence of telithromycin-associated visual adverse events. (See .)
Urogenital system:
Skin:
Hematologic:
Other possibly related clinically-relevant events occurring in <0.2% of patients treated with KETEK from the controlled Phase III studies included:
Reference
This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"
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Clonazepam Description Each single-scored tablet, for oral administration, contains 0.5 mg, 1 mg, or 2 mg Clonazepam, USP, a benzodiazepine. Each tablet also contains corn starch, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and povidone. Clonazepam tablets USP 0.5 mg contain Yellow D&C No. 10 Aluminum Lake. Clonazepam tablets USP 1 mg contain Yellow D&C No. 10 Aluminum Lake, as well as FD&C Blue No. 1 Aluminum Lake. Chemically, Clonazepam, USP is 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-2H-1,4-benzodiazepin-2-one. It is a light yellow crystalline powder. It has the following structural formula: C15H10ClN3O3 M.W. 315.72Tips
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Interactions
A total of 440 drugs (1549 brand and generic names) are known to interact with Imbruvica (ibrutinib). 228 major drug interactions (854 brand and generic names) 210 moderate drug interactions (691 brand and generic names) 2 minor drug interactions (4 brand and generic names) Show all medications in the database that may interact with Imbruvica (ibrutinib).