Definition
The L-isomer of Ofloxacin.
Levofloxacin is a synthetic fluoroquinolone antibacterial agent that inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication. Levofloxacin is marketed by Ortho-McNeil under the trade name Levaquin. Chemically, levofloxacin is the S-enantiomer (L-isomer) of ofloxacin. -- Wikipedia [HMDB]
Description
Levofloxacin is a synthetic fluoroquinolone antibacterial agent that inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication. Levofloxacin is marketed by Ortho-McNeil under the trade name Levaquin. Chemically, levofloxacin is the S-enantiomer (L-isomer) of ofloxacin.
Top Gene Interactions
Related Pathways
General Information
- Metabolism: Mainly excreted as unchanged drug (87%); undergoes limited metabolism in humans. Levofloxacin is rapidly and essentially completely absorbed after oral administration. It is distributed into body tissues, especially in the skin and lung tissues. Levofloxacin is stereochemically stable in plasma and urine and does not invert metabolically to its enantiomer, D-ofloxacin. Levofloxacin undergoes limited metabolism in humans and is primarily excreted as unchanged drug in the urine. Following oral administration, approximately 87% of an administered dose was recovered as unchanged drug in urine within 48 hours, whereas less than 4% of the dose was recovered in feces in 72 hours. Less than 5% of an administered dose was recovered in the urine as the desmethyl and N-oxide metabolites, the only metabolites identified in humans. These metabolites have little relevant pharmacological activity. Levofloxacin is excreted largely as unchanged drug in the urine (L1009). Route of Elimination: Mainly excreted as unchanged drug in the urine. Half Life: 6-8 hours
- Uses/Sources: For the treatment of bacterial conjunctivitis caused by susceptible strains of the following organisms: Corynebacterium species, Staphylococus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus (Groups C/F/G), Viridans group streptococci, Acinetobacter lwoffii, Haemophilus influenzae, Serratia marcescens. Levofloxacin is a synthetic chemotherapeutic agent used to treat severe and life threatening bacterial infection (L1009).
- Health Effects: Irreversible peripheral neuropathy, central nervous system toxicity, cardiovascular toxicity, tendon / articular toxicity, and hepatic toxicity. Toxic epidermal necrolysis, coagulation abnormalities and pancytopenia are other possible adverse effect of levofloxacin. Administration of commercial levofloxin (Levaquin), increased risk of tendinitis and tendon rupture in all ages. This adverse reaction most frequently involves the Achilles tendon (L1009, L1017).
- Symptoms: Side effects include disorientation, dizziness, drowsiness, hot and cold flashes, nausea, slurring of speech, swelling and numbness in the face.
- Treatment: In the event of an acute overdosage, the stomach should be emptied. The patient should be observed and appropriate hydration maintained. Levofloxacin is not efficiently removed by hemodialysis or peritoneal dialysis. (L1009)
- Route of Exposure: Ingestion; injection; skin contact (L1017). Absorption of ofloxacin after single or multiple doses of 200 to 400 mg is predictable, and the amount of drug absorbed increases proportionately with the dose.
Toxicity
- Carcinogenicity: No indication of carcinogenicity to humans (not listed by IARC).
- Toxicity: LD50: 640 mg/kg (Oral, Rat)
Mechanism of Action
Target Name | Mechanism of Action | References |
---|---|---|
DNA topoisomerase 2-alpha | Levofloxacin inhibits bacterial type II topoisomerases, topoisomerase IV and DNA gyrase. Levofloxacin, like other fluoroquinolones, inhibits the A subunits of DNA gyrase, two subunits encoded by the gyrA gene. This results in strand breakage on a bacterial chromosome, supercoiling, and resealing; DNA replication and transcription is inhibited. |
18048412 11752352 |
Potassium voltage-gated channel subfamily H member 2 Multidrug and toxin extrusion protein 1 |
18448342 23241029 15911273 12873512 |
Levofloxacin Interacts with Diseases
Disease | Inference Score | References/Inference Genes |
Liver Cirrhosis, Experimental | 51.29 |
|
Mammary Neoplasms, Animal | 19.17 |
|
Mammary Neoplasms, Experimental | 15.92 |
|
Hepatocellular carcinoma | 14.2 |
|
Carcinoma | 13.51 |
|
Prostatic Neoplasms | 12.21 |
|
Drug-induced liver injury | 11.46 |
|
Mesothelioma, Malignant | 11.05 |
|
Job Syndrome | 9.72 |
|
Breast carcinoma | 9.08 |
|
Carcinoma, Non-Small-Cell Lung | 8.91 |
|
Lipidoses | 8.46 |
|
Liver Cirrhosis | 7.7 |
|
Acute coronary syndrome | 7.57 |
|
Lymphatic Metastasis | 7.17 |
|
Stomach Neoplasms | 6.97 |
|
Autoimmune disease | 6.92 |
|
Colonic neoplasm | 6.62 |
|
Atopic eczema | 6.43 |
|
Squamous cell carcinoma | 6.31 |
|