Levofloxacin 500mg tablets
Prescription only
Requires a prescription from a doctor or prescriber
Tablet
500mg
Oral
Antibacterial drugs
Active ingredients:
Levofloxacin
No active safety alerts
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Source: MHRA Products DatabaseOGL 3.0
Updated 3 months ago(16 Jan 2026)Safety monitoring data
Yellow Card reports
MHRA
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Data from the MHRA Yellow Card scheme. A reported reaction does not necessarily mean the medicine caused it. Contains public sector information licensed under the Open Government Licence v3.0.
EudraVigilance
EMA
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Suspected adverse reactions reported for Levofloxacin
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26 branded products available
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26 products
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Levofloxacin 500mg tablets
Levofloxacin 500mg tablets
Levofloxacin 500mg tablets
Levofloxacin 500mg tablets
Levofloxacin 500mg tablets
Levofloxacin 500mg tablets
Levofloxacin 500mg tablets
Levofloxacin 500mg tablets
Levofloxacin 500mg tablets
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£6.40indicative price
This is the NHS Drug Tariff indicative price used for reimbursement purposes. It may not reflect the price paid by patients or pharmacies.
View full Drug TariffSource: NHS Drug Tariff via NHSBSA. Derived from dm+d VMPP (Virtual Medicinal Product Pack) pricing data. Contains public sector information licensed under the Open Government Licence v3.0.
WHO defined daily dose (DDD)
500 mg
Not a recommended dose. The DDD is the assumed average maintenance dose per day for a drug used for its main indication in adults. It is a statistical measure used for research and comparison purposes only.
Source: WHO Collaborating Centre for Drug Statistics Methodology, distributed via NHS dm+d BNF mapping files. Contains public sector information licensed under the Open Government Licence v3.0.
Therapeutically similar medicines
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Ciprofloxacin 200mg/100ml infusion polyethylene bottles
Infusion
200mg/100ml
Same therapeutic group
Ciprofloxacin 400mg/200ml infusion polyethylene bottles
Infusion
400mg/200ml
Same therapeutic group
Moxifloxacin 400mg/250ml infusion polyethylene bottles
Infusion
400mg/250ml
Same therapeutic group
Levofloxacin 500mg/100ml infusion polyethylene bottles
Infusion
500mg/100ml
Same therapeutic group
Levofloxacin 125mg/5ml oral solution
Oral solution
125mg/5ml
Same therapeutic group
Similarity based on WHO Anatomical Therapeutic Chemical (ATC) classification and NHS BNF section grouping. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
NHS prescribing volume and spending trends
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Clinical guidelines and formulary information
British National Formulary
Levofloxacin
BNF
Drug monograph — bnf.nice.org.ukSource: British National Formulary, NICE. Joint Formulary Committee. Contains public sector information licensed under the Open Government Licence v3.0.
NICE clinical guidance(11)
Prostatitis (acute): antimicrobial prescribing (NG110)
NG110
Guidance
Updated Oct 2018Bronchiectasis (non-cystic fibrosis), acute exacerbation: antimicrobial prescribing (NG117)
NG117
Guidance
Updated Dec 2018Pyelonephritis (acute): antimicrobial prescribing (NG111)
NG111
Guidance
Updated Oct 2018Gastro-oesophageal reflux disease and dyspepsia in adults: investigation and management (CG184)
CG184
Clinical guideline
Updated Oct 2019Antimicrobial prescribing: delafloxacin for community-acquired pneumonia (ES37)
ES37
Evidence summary
Updated Aug 2021Chronic obstructive pulmonary disease (acute exacerbation): antimicrobial prescribing (NG114)
NG114
Guidance
Updated Dec 2018Pneumonia: diagnosis and management (NG250)
NG250
NICE guideline
Updated Sept 2025Cellulitis and erysipelas: antimicrobial prescribing (NG141)
NG141
Guidance
Updated Sept 2019Urinary tract infection (lower): antimicrobial prescribing (NG109)
NG109
Guidance
Updated Oct 2018Otitis media (acute): antimicrobial prescribing (NG91)
NG91
Guidance
Updated Mar 2022Boston Keratoprosthesis Type I for corneal blindness (MIB91)
MIB91
Guidance
Updated Jan 2017Source: National Institute for Health and Care Excellence (NICE). Contains public sector information licensed under the Open Government Licence v3.0.
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Supply & product information
Official product databases and supply status monitoring
Pharmacy links redirect to the retailer's own search and do not represent real-time stock levels. emc (electronic medicines compendium) is operated by Datapharm Ltd. Shortage information sourced from NHS Specialist Pharmacy Service (SPS), sps.nhs.uk.
Codes for healthcare professionals and prescribing systems
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These codes are used by healthcare IT systems and prescribers to identify this medicine.
NHS UK identifiers
Browse tools
SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF codes from NHS Business Services Authority (NHSBSA). ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
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Searching UK clinical trials...
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
None known
Half-life
6-8 hours
Mechanism
Levofloxacin, like other fluoroquinolone antibiotics, exerts its antimicrobial a…
Food interactions
1 warning
Human targets
None mapped
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
99%
Absorption of levofloxacin following oral administration is rapid and essentially complete, with an oral bioavailability of approximately 99%.
[L11638]…
[L11638]…
Half-life
6-8 hours
The average terminal elimination half-life of levofloxacin is 6-8 hours.
[A190663][L11638]
[A190663][L11638]
Protein binding
24-38%
Levofloxacin is 24-38% protein-bound in plasma, primarily to albumin.…
Volume of distribution
1.09-1.26 L/kg
Levofloxacin is widely distributed in the body, with an average volume of distribution following oral administration between 1.09-1.26…
Metabolism
5%
Only 2 metabolites, desmethyl-levofloxacin and levofloxacin-N-oxide, have been identified in humans, neither of which appears to carry any relevant pharmacological activity.
[L11638]…
[L11638]…
Elimination
87%
The majority of administered levofloxacin is excreted unchanged in the urine.
[L11638]…
[L11638]…
Clearance
8.64-13.56 L/h
The average apparent total body clearance of levofloxacin ranges from 8.64-13.56…
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Status:
Approved
Investigational
Small molecule
About this compound
Levofloxacin is a fluoroquinolone antibiotic and the optical S-(-) isomer of racemic [ofloxacin].[A190663] It reportedly carries 8 to 128-fold more activity against both gram-negative and gram-positive bacteria compared to R-(+)-ofloxacin[A190663] and remains stereochemically stable following administration (i.e. it does not invert to the inactive isomer).[L11638] Levofloxacin, along with other quinolones such as [gatifloxacin] and [moxifloxacin], is a member of the third generation of fluoroquinolones, colloquially referred to as the "respiratory quinolones" due to improved activity against gram-positive bacteria commonly implicated in respiratory infections.[A31453][A190756]
Levofloxacin was first approved by the FDA in 1996, and was approved in Canada and several South American countries soon after.[A190663]
Levofloxacin was first approved by the FDA in 1996, and was approved in Canada and several South American countries soon after.[A190663]
Properties:
View FDA drug labelsolid
Avg. mass: 361.37 Da
DrugBank indication
In oral and intravenous formulations, levofloxacin is indicated in adults for the treatment of various infections caused by susceptible bacteria, including infections of the upper respiratory tract, lower respiratory tract, skin, skin structures, urinary tract, and prostate.
[L11638][L11692]
The oral formulation is also indicated in both adults and children 6 months of age and older for the post-exposure management of inhalational anthrax caused by Bacillus anthracis and for the treatment and/or prophylaxis of plague caused by Yersinia pestis.
[L11638]
In its ophthalmic formulation, levofloxacin is indicated for the treatment of bacterial conjunctivitis caused by susceptible organisms.
[L11641]
An inhalational solution available in Canada is indicated for the management of cystic fibrosis patients aged 18 years or older with chronic pulmonary Pseudomonas aeruginosa infections.
[L11689]
[L11638][L11692]
The oral formulation is also indicated in both adults and children 6 months of age and older for the post-exposure management of inhalational anthrax caused by Bacillus anthracis and for the treatment and/or prophylaxis of plague caused by Yersinia pestis.
[L11638]
In its ophthalmic formulation, levofloxacin is indicated for the treatment of bacterial conjunctivitis caused by susceptible organisms.
[L11641]
An inhalational solution available in Canada is indicated for the management of cystic fibrosis patients aged 18 years or older with chronic pulmonary Pseudomonas aeruginosa infections.
[L11689]
Also known as(79)
(-)-Ofloxacin
(3S)-(-)-9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid
(S)-(-)-9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzooxazine-6-carboxylic acid
(S)-9-Fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido(1,2,3-de)-1,4-benzoxazine-6-carboxylic acid
(S)-Ofloxacin
L-Ofloxacin
Levofloxacin
Levofloxacin anhydrous
Dosage forms(114)
Tablet (Oral) — 500.000 mg
Tablet, coated (Oral) — 768.75 mg
Tablet, film coated (Oral) — 250.0 mg
Tablet (Oral) — 512.466 mg
Solution (Ophthalmic) — 5 mg
Tablet (Oral) — 768.636 mg
Solution (Intravenous) — 500.000 mg
Tablet (Oral) — 768.700 mg
Molecular properties(19)
Drug interactions(1432)
Known interactions with other medications. Always consult a healthcare professional.
Ivabradine
Moderate
Ivabradine may increase the QTc-prolonging activities of Levofloxacin.
Didanosine
Moderate
Didanosine can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Quinapril can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium acetate
Moderate
Calcium acetate can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sevelamer can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Iron Dextran
Moderate
Iron Dextran can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lanthanum carbonate
Moderate
Lanthanum carbonate can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric carboxymaltose
Moderate
Ferric carboxymaltose can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Iron sucrose
Moderate
Iron sucrose can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric pyrophosphate
Moderate
Ferric pyrophosphate can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric sulfate
Moderate
Ferric sulfate can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric cation
Moderate
Ferric cation can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Tetraferric tricitrate decahydrate can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lanthanum III cation
Moderate
Lanthanum III cation can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric oxyhydroxide
Moderate
Ferric oxyhydroxide can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sucralfate
Moderate
Sucralfate can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zolmitriptan
Moderate
The metabolism of Zolmitriptan can be decreased when combined with Levofloxacin.
Nitrofurantoin
Moderate
The therapeutic efficacy of Levofloxacin can be decreased when used in combination with Nitrofurantoin.
Picosulfuric acid
Moderate
The therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Levofloxacin.
Insulin human
Moderate
The therapeutic efficacy of Insulin human can be increased when used in combination with Levofloxacin.
Insulin lispro
Moderate
The therapeutic efficacy of Insulin lispro can be increased when used in combination with Levofloxacin.
Insulin pork
Moderate
The therapeutic efficacy of Insulin pork can be increased when used in combination with Levofloxacin.
Troglitazone
Moderate
The therapeutic efficacy of Troglitazone can be increased when used in combination with Levofloxacin.
Glimepiride
Moderate
The therapeutic efficacy of Glimepiride can be increased when used in combination with Levofloxacin.
Sulfisoxazole
Moderate
The therapeutic efficacy of Sulfisoxazole can be increased when used in combination with Levofloxacin.
The therapeutic efficacy of Acarbose can be increased when used in combination with Levofloxacin.
Sulfadiazine
Moderate
The therapeutic efficacy of Sulfadiazine can be increased when used in combination with Levofloxacin.
Rosiglitazone
Moderate
The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Levofloxacin.
Acetohexamide
Moderate
The therapeutic efficacy of Acetohexamide can be increased when used in combination with Levofloxacin.
The therapeutic efficacy of Miglitol can be increased when used in combination with Levofloxacin.
Chlorpropamide
Moderate
The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Levofloxacin.
Nateglinide
Moderate
The therapeutic efficacy of Nateglinide can be increased when used in combination with Levofloxacin.
Pentamidine
Moderate
The therapeutic efficacy of Pentamidine can be increased when used in combination with Levofloxacin.
Tolazamide
Moderate
The therapeutic efficacy of Tolazamide can be increased when used in combination with Levofloxacin.
Repaglinide
Moderate
The therapeutic efficacy of Repaglinide can be increased when used in combination with Levofloxacin.
Phenformin
Moderate
The therapeutic efficacy of Phenformin can be increased when used in combination with Levofloxacin.
Sulfamethoxazole
Moderate
The therapeutic efficacy of Sulfamethoxazole can be increased when used in combination with Levofloxacin.
The therapeutic efficacy of Glyburide can be increased when used in combination with Levofloxacin.
The therapeutic efficacy of Glipizide can be increased when used in combination with Levofloxacin.
Gliclazide
Moderate
The therapeutic efficacy of Gliclazide can be increased when used in combination with Levofloxacin.
Tolbutamide
Moderate
The therapeutic efficacy of Tolbutamide can be increased when used in combination with Levofloxacin.
Pioglitazone
Moderate
The therapeutic efficacy of Pioglitazone can be increased when used in combination with Levofloxacin.
Gliquidone
Moderate
The therapeutic efficacy of Gliquidone can be increased when used in combination with Levofloxacin.
Mitiglinide
Moderate
The therapeutic efficacy of Mitiglinide can be increased when used in combination with Levofloxacin.
Sitagliptin
Moderate
The therapeutic efficacy of Sitagliptin can be increased when used in combination with Levofloxacin.
The therapeutic efficacy of Sunitinib can be increased when used in combination with Levofloxacin.
The therapeutic efficacy of Exenatide can be increased when used in combination with Levofloxacin.
Mecasermin
Moderate
The therapeutic efficacy of Mecasermin can be increased when used in combination with Levofloxacin.
Pramlintide
Moderate
The therapeutic efficacy of Pramlintide can be increased when used in combination with Levofloxacin.
Showing 50 of 1432 interactions
Food & lifestyle interactions
Advice
Take with or without food. Food slightly alters kinetics but not to any clinically significant extent.
Toxicity & overdose
The LD50 following oral administration in mice and rats is 1803 mg/kg and 1478 mg/kg, respectively.
[L11725]
Levofloxacin exhibits low potential for acute toxicity - following a single high dose of levofloxacin in several different test animals (e.g. mice, rats, monkeys) observed symptoms included ataxia, ptosis, decreased motor activity, dyspnea, tremors, and convulsions.
[L11638]
Treatment of acute overdosage should involve stomach emptying (e.g. with activated charcoal) and general supportive measures. Consider monitoring of the patient's ECG to ensure QTc values remain within range.
[L11692]
Levofloxacin is not efficiently removed by dialysis (peritoneal or hemodialysis) and is therefore of little benefit in cases of overdose.
[L11638]
[L11725]
Levofloxacin exhibits low potential for acute toxicity - following a single high dose of levofloxacin in several different test animals (e.g. mice, rats, monkeys) observed symptoms included ataxia, ptosis, decreased motor activity, dyspnea, tremors, and convulsions.
[L11638]
Treatment of acute overdosage should involve stomach emptying (e.g. with activated charcoal) and general supportive measures. Consider monitoring of the patient's ECG to ensure QTc values remain within range.
[L11692]
Levofloxacin is not efficiently removed by dialysis (peritoneal or hemodialysis) and is therefore of little benefit in cases of overdose.
[L11638]
How it works
Mechanism of action
Levofloxacin, like other fluoroquinolone antibiotics, exerts its antimicrobial activity via the inhibition of two key bacterial enzymes: DNA gyrase and topoisomerase IV.[L11638] Both targets are type II topoisomerases, but have unique functions within the bacterial cell. DNA gyrase is an enzyme found only in bacteria that introduces negative supercoils into DNA during replication - this helps to relieve torsional strain caused by the introduction of positive supercoils during replication, and these negative supercoils are essential for chromosome condensation and the promotion of transcription initiation.[A31453] It is comprised of four subunits (two A subunits and two B subunits) of which the A subunits appear to be the target of fluoroquinolone antibiotics.[A190663] Bacterial topoisomerase IV, in addition to contributing to the relaxation of positive supercoils, is essential at the terminal stages of DNA replication and functions to “unlink” newly replicated chromosomes to allow for the completion of cell division.[A31453]
Inhibition of these enzymes by levofloxacin likely occurs via complexation with the topoisomerase enzymes.[A31453] The end result is a blockade of DNA replication, thus inhibiting cell division and resulting in cell death.
Inhibition of these enzymes by levofloxacin likely occurs via complexation with the topoisomerase enzymes.[A31453] The end result is a blockade of DNA replication, thus inhibiting cell division and resulting in cell death.
Pharmacodynamics
Levofloxacin is bactericidal and exerts its antimicrobial effects via inhibition of bacterial DNA replication.[L11638] It has a relatively long duration of action in comparison with other antibiotics that allows for once or twice daily dosing. Levofloxacin is associated with QTc-interval prolongation and should be used with caution in patients with other risk factors for prolongation (e.g. hypokalemia, concomitant medications).[L11638]
Levofloxacin has demonstrated in vitro activity against a number of aerobic gram-positive and gram-negative bacteria and may carry some activity against certain species of anaerobic bacteria[L11638] and other pathogens such as Chlamydia and Legionella.[A190663] Resistance to levofloxacin may develop, and is generally due to mutations in DNA gyrase or topoisomerase IV, or via alterations to drug efflux.[L11638][A31453] Cross-resistance may occur between levofloxacin and other fluoroquinolones, but is unlikely to develop between levofloxacin and other antibiotic classes (e.g. macrolides) due to significant differences in chemical structure and mechanism of action.[L11638]
As antimicrobial susceptibility patterns are geographically distinct, local antibiograms should be consulted to ensure adequate coverage of relevant pathogens prior to use.
Levofloxacin has demonstrated in vitro activity against a number of aerobic gram-positive and gram-negative bacteria and may carry some activity against certain species of anaerobic bacteria[L11638] and other pathogens such as Chlamydia and Legionella.[A190663] Resistance to levofloxacin may develop, and is generally due to mutations in DNA gyrase or topoisomerase IV, or via alterations to drug efflux.[L11638][A31453] Cross-resistance may occur between levofloxacin and other fluoroquinolones, but is unlikely to develop between levofloxacin and other antibiotic classes (e.g. macrolides) due to significant differences in chemical structure and mechanism of action.[L11638]
As antimicrobial susceptibility patterns are geographically distinct, local antibiograms should be consulted to ensure adequate coverage of relevant pathogens prior to use.
Pharmacokinetics
How the body processes this drug — absorption, distribution, metabolism, and elimination
Absorption
Absorption of levofloxacin following oral administration is rapid and essentially complete, with an oral bioavailability of approximately 99%.
[L11638]
Due to its nearly complete absorption, the intravenous and oral formulations of levofloxacin may be interchangeable.
[L11692]
The Tmax is generally attained 1-2 hours following administration and the Cmax is proportional to the given dose - an intravenous dose of 500mg infused over 60 minutes resulted in a Cmax of 6.2 ± 1.0 µg/mL whereas a 750mg dose infused over 90 minutes resulted in a Cmax of 11.5 ± 4.0 µg/mL.
[L11638]
Oral administration with food prolongs the Tmax by approximately 1 hour and slightly decreases the Cmax, but these changes are not likely to be clinically significant.
[L11638]
Systemic absorption following oral inhalation is approximately 50% lower than that observed following oral administration.
[L11689]
[L11638]
Due to its nearly complete absorption, the intravenous and oral formulations of levofloxacin may be interchangeable.
[L11692]
The Tmax is generally attained 1-2 hours following administration and the Cmax is proportional to the given dose - an intravenous dose of 500mg infused over 60 minutes resulted in a Cmax of 6.2 ± 1.0 µg/mL whereas a 750mg dose infused over 90 minutes resulted in a Cmax of 11.5 ± 4.0 µg/mL.
[L11638]
Oral administration with food prolongs the Tmax by approximately 1 hour and slightly decreases the Cmax, but these changes are not likely to be clinically significant.
[L11638]
Systemic absorption following oral inhalation is approximately 50% lower than that observed following oral administration.
[L11689]
Half-life
The average terminal elimination half-life of levofloxacin is 6-8 hours.
[A190663][L11638]
[A190663][L11638]
Protein binding
Levofloxacin is 24-38% protein-bound in plasma, primarily to albumin. The extent of protein-binding is independent of its plasma concentration.
[L11638]
[L11638]
Volume of distribution
Levofloxacin is widely distributed in the body, with an average volume of distribution following oral administration between 1.09-1.26 L/kg (~89-112 L).
[A190663][L11638]
Concentrations in many tissues and fluids may exceed those observed in plasma.
[A190663]
Levofloxacin is known to penetrate well into skin tissue, fluids (e.g. blisters), lung tissue, and prostatic tissue, amongst others.
[A190663]
[A190663][L11638]
Concentrations in many tissues and fluids may exceed those observed in plasma.
[A190663]
Levofloxacin is known to penetrate well into skin tissue, fluids (e.g. blisters), lung tissue, and prostatic tissue, amongst others.
[A190663]
Metabolism
Only 2 metabolites, desmethyl-levofloxacin and levofloxacin-N-oxide, have been identified in humans, neither of which appears to carry any relevant pharmacological activity.
[L11638]
Following oral administration, less than 5% of the administered dose was recovered in the urine as these metabolites, indicating very little metabolism of levofloxacin in humans.
[L11638]
The specific enzymes responsible for the demethylation and oxidation of levofloxacin have yet to be ascertained.
[L11638]
Following oral administration, less than 5% of the administered dose was recovered in the urine as these metabolites, indicating very little metabolism of levofloxacin in humans.
[L11638]
The specific enzymes responsible for the demethylation and oxidation of levofloxacin have yet to be ascertained.
Route of elimination
The majority of administered levofloxacin is excreted unchanged in the urine.
[L11638]
Following the administration of a single oral dose of levofloxacin, approximately 87% was eliminated unchanged in the urine within 48 hours and less than 4% was eliminated in the feces within 72 hours.
[L11638]
[L11638]
Following the administration of a single oral dose of levofloxacin, approximately 87% was eliminated unchanged in the urine within 48 hours and less than 4% was eliminated in the feces within 72 hours.
[L11638]
Clearance
The average apparent total body clearance of levofloxacin ranges from 8.64-13.56 L/h, and its renal clearance ranges from 5.76-8.52 L/h.
[A190663][L11638]
The relative similarity of these ranges indicates a small degree of non-renal clearance.
[A190663]
[A190663][L11638]
The relative similarity of these ranges indicates a small degree of non-renal clearance.
[A190663]
Metabolizing enzymes(1)
Enzymes involved in drug metabolism — important for understanding drug interactions
Enzyme activity key
substrate
inhibitor
inducer
CYP2C9Cytochrome P450 2C9
inhibitor
Transporters(8)
Proteins that transport this drug across cell membranes
ATP-dependent translocase ABCB1
ABCB1
substrate
inhibitor
Specific functionABC-type xenobiotic transporter activity
Cellular location
Cell membrane
General function & pharmacology
Translocates drugs and phospholipids across the membrane .
PMID:2897240 PMID:35970996 PMID:8898203 PMID:9038218 PMID:35507548
Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins .
PMID:8898203
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells PMID:2897240 PMID:35970996 PMID:9038218
PMID:2897240 PMID:35970996 PMID:8898203 PMID:9038218 PMID:35507548
Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins .
PMID:8898203
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells PMID:2897240 PMID:35970996 PMID:9038218
Multidrug and toxin extrusion protein 1
SLC47A1
substrate
inhibitor
Specific functionantiporter activity
Cellular location
Cell membrane
General function & pharmacology
Multidrug efflux pump that functions as a H(+)/organic cation antiporter .
PMID:16330770 PMID:17509534
Plays a physiological role in the excretion of cationic compounds including endogenous metabolites, drugs, toxins through the kidney and liver, into urine and bile respectively .
PMID:16330770 PMID:17495125 PMID:17509534 PMID:17582384 PMID:18305230 PMID:19158817 PMID:21128598 PMID:24961373
Mediates the efflux of endogenous compounds such as creatinine, vitamin B1/thiamine, agmatine and estrone-3-sulfate .
PMID:16330770 PMID:17495125 PMID:17509534 PMID:17582384 PMID:18305230 PMID:19158817 PMID:21128598 PMID:24961373
May also contribute to regulate the transport of cationic compounds in testis across the blood-testis-barrier (Probable)
PMID:16330770 PMID:17509534
Plays a physiological role in the excretion of cationic compounds including endogenous metabolites, drugs, toxins through the kidney and liver, into urine and bile respectively .
PMID:16330770 PMID:17495125 PMID:17509534 PMID:17582384 PMID:18305230 PMID:19158817 PMID:21128598 PMID:24961373
Mediates the efflux of endogenous compounds such as creatinine, vitamin B1/thiamine, agmatine and estrone-3-sulfate .
PMID:16330770 PMID:17495125 PMID:17509534 PMID:17582384 PMID:18305230 PMID:19158817 PMID:21128598 PMID:24961373
May also contribute to regulate the transport of cationic compounds in testis across the blood-testis-barrier (Probable)
Multidrug and toxin extrusion protein 2
SLC47A2
inhibitor
Specific functionantiporter activity
Cellular location
Cell membrane
General function & pharmacology
Multidrug efflux pump that functions as a H(+)/organic cation antiporter. Mediates the efflux of cationic compounds, such as the model cations, tetraethylammonium (TEA) and 1-methyl-4-phenylpyridinium (MPP+), the platinum-based drug oxaliplatin or weak bases that are positively charged at physiological pH, cimetidine, the platinum-based drugs cisplatin and oxaliplatin or the antidiabetic drug metformin. Mediates the efflux of endogenous compounds such as, creatinine, thiamine and estrone-3-sulfate.
Plays a physiological role in the excretion of drugs, toxins and endogenous metabolites through the kidney
Plays a physiological role in the excretion of drugs, toxins and endogenous metabolites through the kidney
Solute carrier family 22 member 1
SLC22A1
inhibitor
Specific function(R)-carnitine transmembrane transporter activity
Cellular location
Basolateral cell membrane
General function & pharmacology
Electrogenic voltage-dependent transporter that mediates the transport of a variety of organic cations such as endogenous bioactive amines, cationic drugs and xenobiotics .
PMID:11388889 PMID:11408531 PMID:12439218 PMID:12719534 PMID:15389554 PMID:16263091 PMID:16272756 PMID:16581093 PMID:19536068 PMID:21128598 PMID:23680637 PMID:24961373 PMID:34040533 PMID:9187257 PMID:9260930 PMID:9655880
Functions as a pH- and Na(+)-independent, bidirectional transporter (By similarity). Cation cellular uptake or release is driven by the electrochemical potential (i.e. membrane potential and concentration gradient) and substrate selectivity (By similarity). Hydrophobicity is a major requirement for recognition in polyvalent substrates and inhibitors (By similarity).
Primarily expressed at the basolateral membrane of hepatocytes and proximal tubules and involved in the uptake and disposition of cationic compounds by hepatic and renal clearance from the blood flow (By similarity). Most likely functions as an uptake carrier in enterocytes contributing to the intestinal elimination of organic cations from the systemic circulation .
PMID:16263091
Transports endogenous monoamines such as N-1-methylnicotinamide (NMN), guanidine, histamine, neurotransmitters dopamine, serotonin and adrenaline .
PMID:12439218 PMID:24961373 PMID:35469921 PMID:9260930
Also transports natural polyamines such as spermidine, agmatine and putrescine at low affinity, but relatively high turnover .
PMID:21128598
Involved in the hepatic uptake of vitamin B1/thiamine, hence regulating hepatic lipid and energy metabolism .
PMID:24961373
Mediates the bidirectional transport of acetylcholine (ACh) at the apical membrane of ciliated cell in airway epithelium, thereby playing a role in luminal release of ACh from bronchial epithelium .
PMID:15817714
Transports dopaminergic neuromodulators cyclo(his-pro) and salsolinol with lower efficency .
PMID:17460754
Also capable of transporting non-amine endogenous compounds such as prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) .
PMID:11907186
May contribute to the transport of cationic compounds in testes across the blood-testis-barrier (Probable). Also involved in the uptake of xenobiotics tributylmethylammonium (TBuMA), quinidine, N-methyl-quinine (NMQ), N-methyl-quinidine (NMQD) N-(4,4-azo-n-pentyl)-quinuclidine (APQ), azidoprocainamide methoiodide (AMP), N-(4,4-azo-n-pentyl)-21-deoxyajmalinium (APDA) and 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP) PMID:11408531 PMID:15389554 PMID:35469921 PMID:9260930
PMID:11388889 PMID:11408531 PMID:12439218 PMID:12719534 PMID:15389554 PMID:16263091 PMID:16272756 PMID:16581093 PMID:19536068 PMID:21128598 PMID:23680637 PMID:24961373 PMID:34040533 PMID:9187257 PMID:9260930 PMID:9655880
Functions as a pH- and Na(+)-independent, bidirectional transporter (By similarity). Cation cellular uptake or release is driven by the electrochemical potential (i.e. membrane potential and concentration gradient) and substrate selectivity (By similarity). Hydrophobicity is a major requirement for recognition in polyvalent substrates and inhibitors (By similarity).
Primarily expressed at the basolateral membrane of hepatocytes and proximal tubules and involved in the uptake and disposition of cationic compounds by hepatic and renal clearance from the blood flow (By similarity). Most likely functions as an uptake carrier in enterocytes contributing to the intestinal elimination of organic cations from the systemic circulation .
PMID:16263091
Transports endogenous monoamines such as N-1-methylnicotinamide (NMN), guanidine, histamine, neurotransmitters dopamine, serotonin and adrenaline .
PMID:12439218 PMID:24961373 PMID:35469921 PMID:9260930
Also transports natural polyamines such as spermidine, agmatine and putrescine at low affinity, but relatively high turnover .
PMID:21128598
Involved in the hepatic uptake of vitamin B1/thiamine, hence regulating hepatic lipid and energy metabolism .
PMID:24961373
Mediates the bidirectional transport of acetylcholine (ACh) at the apical membrane of ciliated cell in airway epithelium, thereby playing a role in luminal release of ACh from bronchial epithelium .
PMID:15817714
Transports dopaminergic neuromodulators cyclo(his-pro) and salsolinol with lower efficency .
PMID:17460754
Also capable of transporting non-amine endogenous compounds such as prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) .
PMID:11907186
May contribute to the transport of cationic compounds in testes across the blood-testis-barrier (Probable). Also involved in the uptake of xenobiotics tributylmethylammonium (TBuMA), quinidine, N-methyl-quinine (NMQ), N-methyl-quinidine (NMQD) N-(4,4-azo-n-pentyl)-quinuclidine (APQ), azidoprocainamide methoiodide (AMP), N-(4,4-azo-n-pentyl)-21-deoxyajmalinium (APDA) and 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP) PMID:11408531 PMID:15389554 PMID:35469921 PMID:9260930
Solute carrier family 22 member 2
SLC22A2
inhibitor
Specific functionacetylcholine transmembrane transporter activity
Cellular location
Basolateral cell membrane
General function & pharmacology
Electrogenic voltage-dependent transporter that mediates the transport of a variety of organic cations such as endogenous bioactive amines, cationic drugs and xenobiotics .
PMID:9260930 PMID:9687576
Functions as a Na(+)-independent, bidirectional uniporter .
PMID:21128598 PMID:9687576
Cation cellular uptake or release is driven by the electrochemical potential, i.e. membrane potential and concentration gradient .
PMID:15212162 PMID:9260930 PMID:9687576
However, may also engage electroneutral cation exchange when saturating concentrations of cation substrates are reached (By similarity). Predominantly expressed at the basolateral membrane of hepatocytes and proximal tubules and involved in the uptake and disposition of cationic compounds by hepatic and renal clearance from the blood flow .
PMID:15783073
Implicated in monoamine neurotransmitters uptake such as histamine, dopamine, adrenaline/epinephrine, noradrenaline/norepinephrine, serotonin and tyramine, thereby supporting a physiological role in the central nervous system by regulating interstitial concentrations of neurotransmitters .
PMID:16581093 PMID:17460754 PMID:9687576
Also capable of transporting dopaminergic neuromodulators cyclo(his-pro), salsolinol and N-methyl-salsolinol, thereby involved in the maintenance of dopaminergic cell integrity in the central nervous system .
PMID:17460754
Mediates the bidirectional transport of acetylcholine (ACh) at the apical membrane of ciliated cell in airway epithelium, thereby playing a role in luminal release of ACh from bronchial epithelium .
PMID:15817714
Also transports guanidine and endogenous monoamines such as vitamin B1/thiamine, creatinine and N-1-methylnicotinamide (NMN) .
PMID:12089365 PMID:15212162 PMID:17072098 PMID:24961373 PMID:9260930
Mediates the uptake and efflux of quaternary ammonium compound choline .
PMID:9260930
Mediates the bidirectional transport of polyamine agmatine and the uptake of polyamines putrescine and spermidine .
PMID:12538837 PMID:21128598
Able to transport non-amine endogenous compounds such as prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) .
PMID:11907186
Also involved in the uptake of xenobiotic 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP) .
PMID:12395288 PMID:16394027
May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
PMID:9260930 PMID:9687576
Functions as a Na(+)-independent, bidirectional uniporter .
PMID:21128598 PMID:9687576
Cation cellular uptake or release is driven by the electrochemical potential, i.e. membrane potential and concentration gradient .
PMID:15212162 PMID:9260930 PMID:9687576
However, may also engage electroneutral cation exchange when saturating concentrations of cation substrates are reached (By similarity). Predominantly expressed at the basolateral membrane of hepatocytes and proximal tubules and involved in the uptake and disposition of cationic compounds by hepatic and renal clearance from the blood flow .
PMID:15783073
Implicated in monoamine neurotransmitters uptake such as histamine, dopamine, adrenaline/epinephrine, noradrenaline/norepinephrine, serotonin and tyramine, thereby supporting a physiological role in the central nervous system by regulating interstitial concentrations of neurotransmitters .
PMID:16581093 PMID:17460754 PMID:9687576
Also capable of transporting dopaminergic neuromodulators cyclo(his-pro), salsolinol and N-methyl-salsolinol, thereby involved in the maintenance of dopaminergic cell integrity in the central nervous system .
PMID:17460754
Mediates the bidirectional transport of acetylcholine (ACh) at the apical membrane of ciliated cell in airway epithelium, thereby playing a role in luminal release of ACh from bronchial epithelium .
PMID:15817714
Also transports guanidine and endogenous monoamines such as vitamin B1/thiamine, creatinine and N-1-methylnicotinamide (NMN) .
PMID:12089365 PMID:15212162 PMID:17072098 PMID:24961373 PMID:9260930
Mediates the uptake and efflux of quaternary ammonium compound choline .
PMID:9260930
Mediates the bidirectional transport of polyamine agmatine and the uptake of polyamines putrescine and spermidine .
PMID:12538837 PMID:21128598
Able to transport non-amine endogenous compounds such as prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) .
PMID:11907186
Also involved in the uptake of xenobiotic 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP) .
PMID:12395288 PMID:16394027
May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
Solute carrier family 22 member 4
SLC22A4
inhibitor
Specific functionacetylcholine transmembrane transporter activity
Cellular location
Apical cell membrane
General function & pharmacology
Transporter that mediates the transport of endogenous and microbial zwitterions and organic cations .
PMID:10215651 PMID:15107849 PMID:15795384 PMID:16729965 PMID:20601551 PMID:22206629 PMID:22569296 PMID:29530864
Functions as a Na(+)-dependent and pH-dependent high affinity microbial symporter of potent food-derived antioxidant ergothioeine .
PMID:15795384 PMID:29530864 PMID:33124720
Transports one sodium ion with one ergothioeine molecule (By similarity). Involved in the absorption of ergothioneine from the luminal/apical side of the small intestine and renal tubular cells, and into non-parenchymal liver cells, thereby contributing to maintain steady-state ergothioneine level in the body .
PMID:20601551
Also mediates the bidirectional transport of acetycholine, although the exact transport mechanism has not been fully identified yet .
PMID:22206629
Most likely exports anti-inflammatory acetylcholine in non-neuronal tissues, thereby contributing to the non-neuronal cholinergic system .
PMID:22206629 PMID:22569296
Displays a general physiological role linked to better survival by controlling inflammation and oxidative stress, which may be related to ergothioneine and acetycholine transports .
PMID:15795384 PMID:22206629
May also function as a low-affinity Na(+)-dependent transporter of L-carnitine through the mitochondrial membrane, thereby maintaining intracellular carnitine homeostasis .
PMID:10215651 PMID:15107849 PMID:16729965
May contribute to regulate the transport of cationic compounds in testis across the blood-testis-barrier PMID:35307651
PMID:10215651 PMID:15107849 PMID:15795384 PMID:16729965 PMID:20601551 PMID:22206629 PMID:22569296 PMID:29530864
Functions as a Na(+)-dependent and pH-dependent high affinity microbial symporter of potent food-derived antioxidant ergothioeine .
PMID:15795384 PMID:29530864 PMID:33124720
Transports one sodium ion with one ergothioeine molecule (By similarity). Involved in the absorption of ergothioneine from the luminal/apical side of the small intestine and renal tubular cells, and into non-parenchymal liver cells, thereby contributing to maintain steady-state ergothioneine level in the body .
PMID:20601551
Also mediates the bidirectional transport of acetycholine, although the exact transport mechanism has not been fully identified yet .
PMID:22206629
Most likely exports anti-inflammatory acetylcholine in non-neuronal tissues, thereby contributing to the non-neuronal cholinergic system .
PMID:22206629 PMID:22569296
Displays a general physiological role linked to better survival by controlling inflammation and oxidative stress, which may be related to ergothioneine and acetycholine transports .
PMID:15795384 PMID:22206629
May also function as a low-affinity Na(+)-dependent transporter of L-carnitine through the mitochondrial membrane, thereby maintaining intracellular carnitine homeostasis .
PMID:10215651 PMID:15107849 PMID:16729965
May contribute to regulate the transport of cationic compounds in testis across the blood-testis-barrier PMID:35307651
Solute carrier organic anion transporter family member 1A2
SLCO1A2
substrate
Specific functionbile acid transmembrane transporter activity
Cellular location
Cell membrane
General function & pharmacology
Na(+)-independent transporter that mediates the cellular uptake of a broad range of organic anions such as the endogenous bile salts cholate and deoxycholate, either in their unconjugated or conjugated forms (taurocholate and glycocholate), at the plasmam membrane .
PMID:19129463 PMID:7557095
Responsible for intestinal absorption of bile acids (By similarity). Transports dehydroepiandrosterone 3-sulfate (DHEAS), a major circulating steroid secreted by the adrenal cortex, as well as estrone 3-sulfate and 17beta-estradiol 17-O-(beta-D-glucuronate) .
PMID:11159893 PMID:12568656 PMID:19129463 PMID:23918469 PMID:25560245 PMID:9539145
Mediates apical uptake of all-trans-retinol (atROL) across human retinal pigment epithelium, which is essential to maintaining the integrity of the visual cycle and thus vision .
PMID:25560245
Involved in the uptake of clinically used drugs .
PMID:17301733 PMID:20686826 PMID:27777271
Capable of thyroid hormone transport (both T3 or 3,3',5'-triiodo-L-thyronine, and T4 or L-tyroxine) .
PMID:19129463 PMID:20358049
Also transports prostaglandin E2 .
PMID:19129463
Plays roles in blood-brain and -cerebrospinal fluid barrier transport of organic anions and signal mediators, and in hormone uptake by neural cells (By similarity). May also play a role in the reuptake of neuropeptides such as substance P/TAC1 and vasoactive intestinal peptide/VIP released from retinal neurons .
PMID:25132355
May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drugs methotrexate and paclitaxel .
PMID:23243220
Shows a pH-sensitive substrate specificity which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment .
PMID:19129463
Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions .
PMID:19129463
May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
PMID:19129463 PMID:7557095
Responsible for intestinal absorption of bile acids (By similarity). Transports dehydroepiandrosterone 3-sulfate (DHEAS), a major circulating steroid secreted by the adrenal cortex, as well as estrone 3-sulfate and 17beta-estradiol 17-O-(beta-D-glucuronate) .
PMID:11159893 PMID:12568656 PMID:19129463 PMID:23918469 PMID:25560245 PMID:9539145
Mediates apical uptake of all-trans-retinol (atROL) across human retinal pigment epithelium, which is essential to maintaining the integrity of the visual cycle and thus vision .
PMID:25560245
Involved in the uptake of clinically used drugs .
PMID:17301733 PMID:20686826 PMID:27777271
Capable of thyroid hormone transport (both T3 or 3,3',5'-triiodo-L-thyronine, and T4 or L-tyroxine) .
PMID:19129463 PMID:20358049
Also transports prostaglandin E2 .
PMID:19129463
Plays roles in blood-brain and -cerebrospinal fluid barrier transport of organic anions and signal mediators, and in hormone uptake by neural cells (By similarity). May also play a role in the reuptake of neuropeptides such as substance P/TAC1 and vasoactive intestinal peptide/VIP released from retinal neurons .
PMID:25132355
May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drugs methotrexate and paclitaxel .
PMID:23243220
Shows a pH-sensitive substrate specificity which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment .
PMID:19129463
Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions .
PMID:19129463
May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
Solute carrier organic anion transporter family member 4C1
SLCO4C1
inhibitor
Specific functionorganic anion transmembrane transporter activity
Cellular location
Basolateral cell membrane
General function & pharmacology
Mediates the transport of organic anions such as steroids (estrone 3-sulfate, chenodeoxycholate, glycocholate) and thyroid hormones (3,3',5-triiodo-L-thyronine (T3), L-thyroxine (T4)), in the kidney .
PMID:14993604 PMID:19129463 PMID:20610891
Capable of transporting cAMP and pharmacological substances such as digoxin, ouabain and methotrexate .
PMID:14993604
Transport is independent of sodium, chloride ion, and ATP .
PMID:14993604
Transport activity is stimulated by an acidic extracellular environment due to increased substrate affinity to the transporter .
PMID:19129463
The driving force for this transport activity is currently not known (By similarity). The role of hydrogencarbonate (HCO3(-), bicarbonate) as the probable counteranion that exchanges for organic anions is still not well defined .
PMID:19129463
Functions as an uptake transporter at the apical membrane, suggesting a role in renal reabsorption (By similarity). Involved in the renal secretion of the uremic toxin ADMA (N(omega),N(omega)-dimethyl-L-arginine or asymmetrical dimethylarginine), which is associated to cardiovascular events and mortality, and the structurally related amino acids L-arginine and L-homoarginine (a cardioprotective biomarker) .
PMID:30865704
Can act bidirectionally, suggesting a dual protective role of this transport protein; exporting L-homoarginine after being synthesized in proximal tubule cells, and mediating uptake of ADMA from the blood into proximal tubule cells where it is degraded by the enzyme dimethylarginine dimethylaminohydrolase 1 (DDAH1) .
PMID:30865704 PMID:32642843
May be involved in sperm maturation by enabling directed movement of organic anions and compounds within or between cells (By similarity).
This ion-transporting process is important to maintain the strict epididymal homeostasis necessary for sperm maturation (By similarity). May have a role in secretory functions since seminal vesicle epithelial cells are assumed to secrete proteins involved in decapacitation by modifying surface proteins to facilitate the acquisition of the ability to fertilize the egg (By similarity)
PMID:14993604 PMID:19129463 PMID:20610891
Capable of transporting cAMP and pharmacological substances such as digoxin, ouabain and methotrexate .
PMID:14993604
Transport is independent of sodium, chloride ion, and ATP .
PMID:14993604
Transport activity is stimulated by an acidic extracellular environment due to increased substrate affinity to the transporter .
PMID:19129463
The driving force for this transport activity is currently not known (By similarity). The role of hydrogencarbonate (HCO3(-), bicarbonate) as the probable counteranion that exchanges for organic anions is still not well defined .
PMID:19129463
Functions as an uptake transporter at the apical membrane, suggesting a role in renal reabsorption (By similarity). Involved in the renal secretion of the uremic toxin ADMA (N(omega),N(omega)-dimethyl-L-arginine or asymmetrical dimethylarginine), which is associated to cardiovascular events and mortality, and the structurally related amino acids L-arginine and L-homoarginine (a cardioprotective biomarker) .
PMID:30865704
Can act bidirectionally, suggesting a dual protective role of this transport protein; exporting L-homoarginine after being synthesized in proximal tubule cells, and mediating uptake of ADMA from the blood into proximal tubule cells where it is degraded by the enzyme dimethylarginine dimethylaminohydrolase 1 (DDAH1) .
PMID:30865704 PMID:32642843
May be involved in sperm maturation by enabling directed movement of organic anions and compounds within or between cells (By similarity).
This ion-transporting process is important to maintain the strict epididymal homeostasis necessary for sperm maturation (By similarity). May have a role in secretory functions since seminal vesicle epithelial cells are assumed to secrete proteins involved in decapacitation by modifying surface proteins to facilitate the acquisition of the ability to fertilize the egg (By similarity)
Carriers(1)
Proteins that carry this drug through the body
Albumin
ALB
substrate
Specific functionantioxidant activity
Cellular location
Secreted
General function & pharmacology
Binds water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs (Probable). Its main function is the regulation of the colloidal osmotic pressure of blood (Probable). Major zinc transporter in plasma, typically binds about 80% of all plasma zinc .
PMID:19021548
Major calcium and magnesium transporter in plasma, binds approximately 45% of circulating calcium and magnesium in plasma (By similarity).
Potentially has more than two calcium-binding sites and might additionally bind calcium in a non-specific manner (By similarity). The shared binding site between zinc and calcium at residue Asp-273 suggests a crosstalk between zinc and calcium transport in the blood (By similarity). The rank order of affinity is zinc > calcium > magnesium (By similarity).
Binds to the bacterial siderophore enterobactin and inhibits enterobactin-mediated iron uptake of E.coli from ferric transferrin, and may thereby limit the utilization of iron and growth of enteric bacteria such as E.coli .
PMID:6234017
Does not prevent iron uptake by the bacterial siderophore aerobactin PMID:6234017
PMID:19021548
Major calcium and magnesium transporter in plasma, binds approximately 45% of circulating calcium and magnesium in plasma (By similarity).
Potentially has more than two calcium-binding sites and might additionally bind calcium in a non-specific manner (By similarity). The shared binding site between zinc and calcium at residue Asp-273 suggests a crosstalk between zinc and calcium transport in the blood (By similarity). The rank order of affinity is zinc > calcium > magnesium (By similarity).
Binds to the bacterial siderophore enterobactin and inhibits enterobactin-mediated iron uptake of E.coli from ferric transferrin, and may thereby limit the utilization of iron and growth of enteric bacteria such as E.coli .
PMID:6234017
Does not prevent iron uptake by the bacterial siderophore aerobactin PMID:6234017
Scientific references(8)
Fish D.N., Chow A.T.
The clinical pharmacokinetics of levofloxacin.
Clinical Pharmacokinetics
1997 Feb32(2):101-19. doi: 10.2165/00003088-199732020-00002
Giri P., Naidu S., Patel N., Patel H., Srinivas N.R.
Evaluation of In Vitro Cytochrome P450 Inhibition and In Vitro Fate of Structurally Diverse N-Oxide Metabolites: Case Studies with Clozapine, Levofloxacin, Roflumilast, Voriconazole and Zopiclone.
European Journal Drug Metabolism Pharmacokinetics
2017 Aug42(4):677-688. doi: 10.1007/s13318-016-0385-7
Sato T., Mishima E., Mano N., Abe T., Yamaguchi H.
Potential Drug Interactions Mediated by Renal Organic Anion Transporter OATP4C1.
Journal of Pharmacology and Experimental Therapeutics
2017 Aug362(2):271-277. doi: 10.1124/jpet.117.241703. Epub 2017 May 26
Parvez M.M., Kaisar N., Shin H.J., Jung J.A., Shin J.G.
Inhibitory Interaction Potential of 22 Antituberculosis Drugs on Organic Anion and Cation Transporters of the SLC22A Family.
Antimicrob Agents Chemother
2016 Oct 2160(11):6558-6567. doi: 10.1128/AAC.01151-16. Print 2016 Nov
Maeda T., Takahashi K., Ohtsu N., Oguma T., Ohnishi T., Atsumi R., Tamai I.
Identification of influx transporter for the quinolone antibacterial agent levofloxacin.
Molecular Pharmaceutics
2007 Jan-Feb4(1):85-94. doi: 10.1021/mp060082j
Nies A.T., Damme K., Schaeffeler E., Schwab M.
Multidrug and toxin extrusion proteins as transporters of antimicrobial drugs.
Expert Opinion Drug Metabolism Toxicology
2012 Dec8(12):1565-77. doi: 10.1517/17425255.2012.722996. Epub 2012 Sep 13
Fabrega A., Madurga S., Giralt E., Vila J.
Mechanism of action of and resistance to quinolones.
Microb Biotechnol
2009 Jan2(1):40-61. doi: 10.1111/j.1751-7915.2008.00063.x. Epub 2008 Oct 13
Fish D.N.
Levofloxacin: update and perspectives on one of the original 'respiratory quinolones'.
Expert Review Anti Infectious Therapeutics
2003 Oct1(3):371-87. doi: 10.1586/14787210.1.3.371
ATC classification(5 codes)
ATC J01MA12
ATC A02BD10
ATC J04AM12
ATC J01RA05
ATC S01AE05
Affected organisms(41)
Enterococcus faecalis
Staphylococcus aureus
Staphylococcus epidermidis
Staphylococcus saprophyticus
Streptococcus pneumoniae
Streptococcus pyogenes
Enterobacter cloacae
Escherichia coli
Haemophilus influenzae
Haemophilus parainfluenzae
Klebsiella pneumoniae
Legionella pneumophila
Moraxella catarrhalis
Proteus mirabilis
Pseudomonas aeruginosa
Serratia marcescens
Chlamydophila pneumoniae
Mycoplasma pneumoniae
Staphylococcus haemolyticus
Streptococcus sp. group G
Streptococcus agalactiae
Streptococcus viridans
Bacillus anthracis
Acinetobacter baumannii
Acinetobacter lwoffii
Bordetella pertussis
Citrobacter freundii
Enterobacter aerogenes
Klebsiella oxytoca
Morganella morganii
Proteus vulgaris
Providencia rettgeri
Providencia stuartii
Pseudomonas fluorescens
Yersinia pestis
Clostridium perfringens
Group C Streptococcus sp.
Streptococcus milleri
Citrobacter koseri
Cronobacter sakazakii
Pantoea agglomerans
International brands(11)
Salt forms(1)
Levofloxacin hemihydrate(DBSALT001001)
Experimental properties(4)
Commercial products(504)
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Show
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Levofloxacin
Additional database identifiers
Drugs Product Database (DPD)
11705
ChemSpider
131410
BindingDB
50366826
PDB
LFX
ZINC
ZINC000000538273
GenBank Gene Database
L42023
GenBank Protein Database
1574722
UniProt Accession
GYRA_HAEIN
GenBank Gene Database
L42023
GenBank Protein Database
1574370
UniProt Accession
PARC_HAEIN
GenBank Gene Database
X71437
UniProt Accession
GYRB_STAAU
UniProt Accession
GYRA_STAAU
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2623
GenAtlas
CYP2C9
GeneCards
CYP2C9
GenBank Gene Database
AY341248
Guide to Pharmacology
1326
UniProt Accession
CP2C9_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:399
GenAtlas
ALB
GeneCards
ALB
GenBank Gene Database
V00494
GenBank Protein Database
28590
UniProt Accession
ALBU_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:40
GenAtlas
ABCB1
GeneCards
ABCB1
GenBank Gene Database
M14758
GenBank Protein Database
307180
Guide to Pharmacology
768
UniProt Accession
MDR1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:25588
GeneCards
SLC47A1
GenBank Gene Database
AK001709
GenBank Protein Database
7023138
Guide to Pharmacology
1216
UniProt Accession
S47A1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:26439
GeneCards
SLC47A2
Guide to Pharmacology
1217
UniProt Accession
S47A2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10963
GeneCards
SLC22A1
GenBank Gene Database
X98332
GenBank Protein Database
2511670
Guide to Pharmacology
1019
UniProt Accession
S22A1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10966
GeneCards
SLC22A2
GenBank Gene Database
X98333
GenBank Protein Database
2281942
Guide to Pharmacology
1020
UniProt Accession
S22A2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10968
GenAtlas
SLC22A4
GeneCards
SLC22A4
GenBank Gene Database
AB007448
GenBank Protein Database
2605501
UniProt Accession
S22A4_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10956
GeneCards
SLCO1A2
GenBank Gene Database
U21943
GenBank Protein Database
885978
Guide to Pharmacology
1219
UniProt Accession
SO1A2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:23612
GeneCards
SLCO4C1
GenBank Gene Database
AF401643
GenBank Protein Database
33308060
UniProt Accession
SO4C1_HUMAN
International reference pricing
11 formulations
Reference pricing from DrugBank. Prices are indicative and may not reflect current UK costs.
From $0.44/ml
To $81.68/bottle
Levaquin 500 mg/100 ml d5w
$0.44/ml
Levaquin i.v. 25 mg/ml vial
$1.94/ml
Quixin 0.5% Solution
$11.40/ml
Quixin 0.5% eye drops
$12.21/ml
Levaquin 250 mg tablet
$13.71/tablet
Source: DrugBank. Used under CC BY-NC 4.0 academic licence for non-commercial purposes.
Patent information
All patents expired, 2 expired
Approved 19 Oct 2004 · Expires 26 Aug 2022
Expired
5053407
United States
Approved 1 Oct 1991 · Expires 20 Dec 2010
Expired
Patent protection has expired — generic versions may be available.
Source: DrugBank · CC BY-NC 4.0. Patent data sourced from national patent offices. Expiry dates may not reflect extensions, regulatory exclusivity periods, or legal challenges.
DrugBank citations
If you use DrugBank data in your research, please cite the following publications:
Knox C., Wilson M., Klinger C.M., et al
DrugBank 6.
0: the DrugBank Knowledgebase for 2024
Nucleic Acids Res. 2024 Jan 552(D1):D1265-D1275
Wishart D.S., Feunang Y.D., Guo A.C., et al
DrugBank 5.
0: a major update to the DrugBank database for 2018
Nucleic Acids Res. 2017 Nov 846(D1):D1074-D1082
Show earlier publications
Law V., Knox C., Djoumbou Y., et al
DrugBank 4.
0: shedding new light on drug metabolism
Nucleic Acids Res. 2014 Jan 142(1):D1091-7
Knox C., Law V., Jewison T., et al
DrugBank 3.
0: a comprehensive resource for 'omics' research on drugs
Nucleic Acids Res. 2011 Jan39(Database issue):D1035-41
Wishart D.S., Knox C., Guo A.C., et al
DrugBank: a knowledgebase for drugs, drug actions and drug targets.
Nucleic Acids Research
2008 Jan36(Database issue):D901-6
Wishart D.S., Knox C., Guo A.C., et al
DrugBank: a comprehensive resource for in silico drug discovery and exploration.
Nucleic Acids Research
2006 Jan 134(Database issue):D668-72
Source: go.drugbank.comCC BY-NC 4.0
Updated about 1 month ago(4 Mar 2026)