Overview
| Generic Names: | telithromycin |
|---|---|
| Trade Names: | Ketek |
| PharmGKB Accession Id: | PA10202 |
Description
Telithromycin is a semi-synthetic erythromycin derivative. It is used to treat mild to moderate respiratory infections. Telithromycin prevents bacteria from growing, by interfering with their protein synthesis. Telithromycin binds to the subunit 50S of the bacterial ribosome, and blocks the progression of the growing polypeptide chain. In addition, telithromycin binds simultaneously to two domains of 23S RNA of the 50 S ribosomal subunit, where older macrolides bind only to one. (source: Drug Bank)
Indication
For the treatment of <i>Pneumococcal</i> infection, acute sinusitis, acute bacterial tonsillitis, acute bronchitis and bronchiolitis, lower respiratory tract infection and lobar (pneumococcal) pneumonia. (source: Drug Bank)
ATC Therapeutic Category
- J01FA:Macrolides
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
Telithromycin acts by binding to domains II and V of 23S rRNA of the 50S ribosomal subunit. By binding at domain II, telithromycin retains activity against gram-positive cocci (e.g., <i>Streptococcus pneumoniae</i>) in the presence of resistance mediated by methylases (erm genes) that alter the domain V binding site of telithromycin. Telithromycin may also inhibit the assembly of nascent ribosomal units. (source: Drug Bank)
Pharmacology
Telithromycin is a macrolide antibiotic which has an antimicrobial spectrum similar or slightly wider to that of penicillin, and is often used for people who have an allergy to penicillins. For respiratory tract infections, it has better coverage of atypical organisms, including mycoplasma. It is also used to treat outbreaks of chlamydia, syphilis, and gonorrhea. Telithromycin prevents bacteria from growing, by interfering with their protein synthesis. Telithromycin binds to the subunit 50S of the bacterial ribosome, and thus inhibits the translocation of peptides. (source: Drug Bank)
Food Interactions
Take without regard to meals. (source: Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic (source: Drug Bank)
Protein Binding
60%-70% (source: Drug Bank)
Toxicity
LD<sub>50</sub>>2000 mg/kg (PO in rats) (source: Drug Bank)
Isomeric SMILES Code:
CC[C@H]1[C@@]2([C@@H]([C@@H](C(=O)[C@@H](C[C@]([C@@H]([C@H](C(=O)[C@H](C(=O)O1)C)C)O[C@H]3[C@@H]([C@H](C[C@H](O3)C)N(C)C)O)(C)OC)C)C)N(C(=O)O2)CCCCN4C=C(N=C4)C5=CN=CC=C5)C (source: Drug Bank)
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
|
CYP2C8 |
|
Publications |
|
CYP3A4 |
|
Publications |
|
|
KCNH2 |
|
Publications |
A list of non-curated publications that mention this drug along with other genes is available.
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| acenocoumarol |
|
Telithromycin increases the anticoagulant effect (source: Drug Bank) |
| alprazolam |
|
Telithromycin increases the effect/toxicity of the benzodiazepine (source: Drug Bank) |
| amiodarone |
|
Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank) |
| astemizole |
|
Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank) |
| atorvastatin |
|
Telithromycin may possibly increase statin toxicity (source: Drug Bank) |
| bretylium |
|
Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank) |
| carbamazepine |
|
Telithromycin may possibly increase this agent effect/toxicity (source: Drug Bank) |
| cisapride |
|
Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank) |
| colchicine |
|
Severe colchicine toxicity can occur (source: Drug Bank) |
| cyclosporine |
|
Telithromycin may possibly increase this agent effect/toxicity (source: Drug Bank) |
| dasatinib |
|
Increased levels/toxicity of dasatinib (source: Drug Bank) |
| dicumarol |
|
Telithromycin increases the anticoagulant effect (source: Drug Bank) |
| digoxin |
|
Telithromycin may increase levels of digoxin (source: Drug Bank) |
| disopyramide |
|
Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank) |
| dofetilide |
|
Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank) |
| erlotinib |
|
This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank) |
| lovastatin |
|
Telithromycin may possibly increase statin toxicity (source: Drug Bank) |
| metoprolol |
|
Telithromycin may possibly increase metoprolol effect (source: Drug Bank) |
| midazolam |
|
Telithromycin increases the effect/toxicity of the benzodiazepine (source: Drug Bank) |
| phenytoin |
|
Telithromycin may possibly increase this agent effect/toxicity (source: Drug Bank) |
| pimozide |
|
Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank) |
| quinidine |
|
Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank) |
| rifampin |
|
Rifampin decreases the effect of telithromycin (source: Drug Bank) |
| simvastatin |
|
Telithromycin may possibly increase statin toxicity (source: Drug Bank) |
| sotalol |
|
Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank) |
| sunitinib |
|
Possible increase in sunitinib levels (source: Drug Bank) |
| tacrolimus |
|
This antibiotic increases the effect and toxicity of tacrolimus (source: Drug Bank) |
| terfenadine |
|
Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank) |
| triazolam |
|
Telithromycin increases the effect/toxicity of the benzodiazepine (source: Drug Bank) |
| verapamil |
|
Telithromycin may possibly increase verapamil effect/toxicity (source: Drug Bank) |
| warfarin |
|
Telithromycin increases the anticoagulant effect (source: Drug Bank) |
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
|
|
Drug Toxicity |
|
Publications |
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.