Description
Top Gene Interactions
Related Pathways
General Information
- Metabolism: Hepatic - estimated 50% metabolized by CYP3A4 and 50% metabolized independent of cytochrome P450 Route of Elimination: The systemically available telithromycin is eliminated by multiple pathways as follows: 7% of the dose is excreted unchanged in feces by biliary and/or intestinal secretion; 13% of the dose is excreted unchanged in urine by renal excretion; and 37% of the dose is metabolized by the liver. Half Life: Main elimination half-life is 2-3 hours; terminal elimination half-life is 10 hours
- Uses/Sources: For the treatment of Pneumococcal infection, acute sinusitis, acute bacterial tonsillitis, acute bronchitis and bronchiolitis, lower respiratory tract infection and lobar (pneumococcal) pneumonia.
- Symptoms: Most common side-effects are gastrointestinal, including diarrhea, nausea, abdominal pain and vomiting. Headache and disturbances in taste also occur. Less common side-effects include palpitations, blurred vision and rashes. [Wikipedia]
- Route of Exposure: Absolute bioavailability is approximately 57%. Maximal concentrations are reached 0.5 - 4 hours following oral administration. Food intake does not affected absorption.
Toxicity
- Carcinogenicity: No indication of carcinogenicity to humans (not listed by IARC).
- Toxicity: LD50>2000 mg/kg (PO in rats).
Mechanism of Action
Target Name | Mechanism of Action | References |
---|---|---|
Cytochrome P450 3A3 | 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., Streptococcus pneumoniae) 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. |
11601667 12149046 15792396 15598962 16199242 |
Cytochrome P450 3A4 Cytochrome P450 3A5 Cytochrome P450 3A7 Cytochrome P450 2D6 Cytochrome P450 1A2 |
11601667 12149046 15792396 19934256 2007 15598962 16199242 |
Telithromycin Interacts with Diseases
Disease | Inference Score | References/Inference Genes |
Manganese Poisoning | 16.35 |
|
Anthracosis | 13.49 |
|
HIV Wasting Syndrome | 12.24 |
|
Chlamydia Infections | 11.44 |
|
Arthritis, Infectious | 10.75 |
|
Oral Submucous Fibrosis | 10.75 |
|
Radiation Injuries, Experimental | 10.75 |
|
Mitochondrial Myopathies | 10.52 |
|
Burns | 10.3 |
|
Dermatitis, Allergic Contact | 10.08 |
|
Breast carcinoma | 9.94 |
|
Dermatomyositis | 9.89 |
|
Polymyositis | 9.89 |
|
Leishmaniasis | 9.85 |
|
Leishmaniasis, Cutaneous | 9.85 |
|
Heat Stroke | 9.75 |
|
Visceral leishmaniasis | 9.42 |
|
Fever | 9.27 |
|
Hernia, Diaphragmatic | 9.19 |
|
Hepatitis C | 9.04 |
|