QuickView for levofloxacin (compound)

Summary
General Info

DrugBank

Identification

Name:	Levofloxacin
Name (isomeric):	DB01137
Drug Type:	small molecule
Synonyms:	L-Ofloxacin
Brand:	Levoxacin, Mosardal, Nofaxin, Levox, Cravit Ophthalmic, Levokacin, Lesacin, Tavanic, Quixin, Cravit, Reskuin, Iquix, Levaquin, Floxel, Leroxacin, Volequin, Elequine
Category:	Anti-Bacterial Agents, Quinolones, Anti-Infective Agents, Urinary, Nucleic Acid Synthesis Inhibitors
CAS number:	100986-85-4

Pharmacology

Indication:	For the treatment of bacterial conjunctivitis caused by susceptible strains of the following organisms: <i>Corynebacterium</i> species, <i>Staphylococus aureus</i>, <i>Staphylococcus epidermidis</i>, <i>Streptococcus pneumoniae</i>, <i>Streptococcus</i> (Groups C/F/G), Viridans group streptococci, <i>Acinetobacter lwoffii</i>, <i>Haemophilus influenzae</i>, <i>Serratia marcescens</i>.
Pharmacology:	Levofloxacin, a fluoroquinolone antiinfective, is the optically active L-isomer of ofloxacin. Levofloxacin is used to treat bacterial conjunctivitis, sinusitis, chronic bronchitis, community-acquired pneumonia and pneumonia caused by penicillin-resistant strains of Streptococcus pneumoniae, skin and skin structure infections, complicated uri... show more » Levofloxacin, a fluoroquinolone antiinfective, is the optically active L-isomer of ofloxacin. Levofloxacin is used to treat bacterial conjunctivitis, sinusitis, chronic bronchitis, community-acquired pneumonia and pneumonia caused by penicillin-resistant strains of Streptococcus pneumoniae, skin and skin structure infections, complicated urinary tract infections and acute pyelonephritis. show less «
Mechanism of Action:	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.
Absorption:	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.
Protein binding:	24-38% (to plasma proteins)
Biotransformation:	Mainly excreted as unchanged drug (87%); undergoes limited metabolism in humans.
Route of elimination:	Mainly excreted as unchanged drug in the urine.
Half Life:	6-8 hours
Toxicity:	Side effects include disorientation, dizziness, drowsiness, hot and cold flashes, nausea, slurring of speech, swelling and numbness in the face
Affected organisms:	Enteric bacteria and other eubacteria

Interactions

Food interaction:

Take without regard to meals. Take with water, drink lliberally. Taking this product with orange juice can result in reduced quinolone plasma levels.

Drug interaction:

Erythromycin	Increased risk of cardiotoxicity and arrhythmias
Promazine	Increased risk of cardiotoxicity and arrhythmias
Disopyramide	Increased risk of cardiotoxicity and arrhythmias
Anisindione	The quinolone antibiotic, levofloxacin, may increase the anticoagulant effect of anisindione.
Triflupromazine	Increased risk of cardiotoxicity and arrhythmias

Erythromycin	Increased risk of cardiotoxicity and arrhythmias
Promazine	Increased risk of cardiotoxicity and arrhythmias
Disopyramide	Increased risk of cardiotoxicity and arrhythmias
Anisindione	The quinolone antibiotic, levofloxacin, may increase the anticoagulant effect of anisindione.
Triflupromazine	Increased risk of cardiotoxicity and arrhythmias
Iron	Formation of non-absorbable complexes
Procainamide	Levofloxacin may increase the effect of procainamide.
Chlorpromazine	Increased risk of cardiotoxicity and arrhythmias
Calcium	Formation of non-absorbable complexes
Bretylium	Increased risk of cardiotoxicity and arrhythmias
Magnesium oxide	Formation of non-absorbable complexes
Zinc	Formation of non-absorbable complexes
Sucralfate	Formation of non-absorbable complexes
Thiethylperazine	Increased risk of cardiotoxicity and arrhythmias
Lumefantrine	Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
Magnesium	Formation of non-absorbable complexes
Dihydroquinidine barbiturate	Increased risk of cardiotoxicity and arrhythmias
Warfarin	The quinolone antibiotic, levofloxacin, may increase the anticoagulant effect of warfarin.
Zuclopenthixol	Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Promethazine	Increased risk of cardiotoxicity and arrhythmias
Perphenazine	Increased risk of cardiotoxicity and arrhythmias
Josamycin	Increased risk of cardiotoxicity and arrhythmias
Methotrimeprazine	Increased risk of cardiotoxicity and arrhythmias
Sotalol	Increased risk of cardiotoxicity and arrhythmias
Mesoridazine	Increased risk of cardiotoxicity and arrhythmias
Thiothixene	May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
Aluminium	Formation of non-absorbable complexes
Thioridazine	Increased risk of cardiotoxicity and arrhythmias
Vorinostat	Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Bepridil	Increased risk of cardiotoxicity and arrhythmias
Prochlorperazine	Increased risk of cardiotoxicity and arrhythmias
Quinidine barbiturate	Increased risk of cardiotoxicity and arrhythmias
Propiomazine	Increased risk of cardiotoxicity and arrhythmias
Ziprasidone	Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
Quinupristin	This combination presents an increased risk of toxicity
Artemether	Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
Tacrolimus	Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
Amiodarone	Increased risk of cardiotoxicity and arrhythmias
Calcium Acetate	Calcium salts such as calcium acetate may decrease the absorption of quinolone antibiotics such as levofloxacin. Of concern only with oral administration of both agents. Interactions can be minimized by administering oral quinolone at least 2 hours before, or 6 hours after, the dose of an oral calcium supplement. Monitor for decreased therapeutic effects of oral quinolones if administered with oral calcium supplements.
Toremifene	Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.
Quinidine	Increased risk of cardiotoxicity and arrhythmias
Dicumarol	The quinolone antibiotic, levofloxacin, may increase the anticoagulant effect of dicumarol.
Fluphenazine	Increased risk of cardiotoxicity and arrhythmias
Iron Dextran	Formation of non-absorbable complexes
Trimipramine	Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
Trifluoperazine	Increased risk of cardiotoxicity and arrhythmias
Acenocoumarol	The quinolone antibiotic, levofloxacin, may increase the anticoagulant effect of acenocoumarol.
Voriconazole	Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).

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Targets

DNA topoisomerase 4 subunit A

DNA gyrase subunit A

DNA topoisomerase 2-alpha

Enzymes

Cytochrome P450 1A2

Cytochrome P450 3A4

Transporters

Multidrug resistance protein 1

Solute carrier family 22 member 6

Solute carrier family 22 member 2

Organic cation/carnitine transporter 1