Identification
- Summary
Ofloxacin is an antibacterial agent used for the treatment of bacterial infections in many parts of the body, including the respiratory tract, kidney, skin, soft tissue, and urinary tract.
- Brand Names
- Ocuflox
- Generic Name
- Ofloxacin
- DrugBank Accession Number
- DB01165
- Background
A synthetic fluoroquinolone (fluoroquinolones) antibacterial agent that inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Ofloxacin (DB01165)
- Weight
- Average: 361.3675
Monoisotopic: 361.143784348 - Chemical Formula
- C18H20FN3O4
- Synonyms
- 8-Fluoro-3-methyl-9-(4-methyl-piperazin-1-yl)-6-oxo-2,3-dihydro-6H-1-oxa-3a-aza-phenalene-5-carboxylic acid
- Ofloxacin
- Ofloxacine
- Ofloxacino
- Ofloxacinum
- OFLX
- External IDs
- DL-8280
- HOE 280
- HOE-280
Pharmacology
- Indication
For the treatment of infections (respiratory tract, kidney, skin, soft tissue, UTI), urethral and cervical gonorrhoea.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Acute bacterial exacerbation of chronic bronchitis •••••••••••• Treatment of Acute otitis media •••••••••••• Treatment of Bacterial infections •••••••••••• Treatment of Cervicitis •••••••••••• Treatment of Community-acquired pneumonia •••••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Ofloxacin is a quinolone/fluoroquinolone antibiotic. Ofloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase, which allows the untwisting required to replicate one DNA double helix into two. Notably the drug has 100 times higher affinity for bacterial DNA gyrase than for mammalian. Ofloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria.
- Mechanism of action
Ofloxacin acts on DNA gyrase and toposiomerase IV, enzymes which, like human topoisomerase, prevents the excessive supercoiling of DNA during replication or transcription. By inhibiting their function, the drug thereby inhibits normal cell division.
Target Actions Organism ADNA gyrase subunit A inhibitorHaemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd) ADNA topoisomerase 4 subunit A inhibitorHaemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd) UDNA topoisomerase 2-alpha inhibitorHumans - Absorption
Bioavailability of ofloxacin in the tablet formulation is approximately 98%
- Volume of distribution
Not Available
- Protein binding
32%
- Metabolism
Hepatic
- Route of elimination
Ofloxacin is mainly eliminated by renal excretion, where between 65% and 80% of an administered oral dose of ofloxacin is excreted unchanged via urine within 48 hours of dosing. About 4-8% of an ofloxacin dose is excreted in the feces and the drug is minimally subject to biliary excretion.
- Half-life
9 hours
- Clearance
Not Available
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
LD50=5450 mg/kg (orally in mice)
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAcarbose The therapeutic efficacy of Acarbose can be increased when used in combination with Ofloxacin. Aceclofenac Aceclofenac may increase the neuroexcitatory activities of Ofloxacin. Acemetacin Acemetacin may increase the neuroexcitatory activities of Ofloxacin. Acenocoumarol The therapeutic efficacy of Acenocoumarol can be increased when used in combination with Ofloxacin. Acetohexamide The therapeutic efficacy of Acetohexamide can be increased when used in combination with Ofloxacin. - Food Interactions
- Limit caffeine intake.
- Take with or without food. The absorption is unaffected by food.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Ofloxacin hydrochloride I2UWV315WA 118120-51-7 CAOOISJXWZMLBN-UHFFFAOYSA-N - Product Images
- International/Other Brands
- Floxstat / Zanocin
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Floxin Tablet, coated 400 mg/1 Oral Ortho Mc Neil Pharmaceuticals 1990-12-28 2009-01-31 US 
Floxin Tablet, coated 200 mg/1 Oral Physicians Total Care, Inc. 1993-08-03 2011-05-31 US Floxin Tablet, coated 300 mg/1 Oral Ortho Mc Neil Pharmaceuticals 1990-12-28 2009-01-31 US Floxin Tablet, coated 400 mg/1 Oral Physicians Total Care, Inc. 1992-12-08 2011-05-31 US Floxin Tablet, coated 200 mg/1 Oral Ortho Mc Neil Pharmaceuticals 1990-12-28 2009-01-31 US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Apo-ofloxacin Solution 0.3 % Ophthalmic Apotex Corporation 2004-01-22 Not applicable Canada 
Floxin Otic Solution / drops 3 mg/1mL Auricular (otic) ALMATICA PHARMA INC. 2016-07-25 2019-11-15 US Novo-ofloxacin Tablet 300 mg Oral Novopharm Limited 2004-06-11 2012-05-08 Canada Novo-ofloxacin Tablet 200 mg Oral Novopharm Limited 2004-06-11 2012-05-08 Canada Novo-ofloxacin Tablet 400 mg Oral Novopharm Limited 2004-06-11 2012-05-08 Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image EXOPRED (OPHTHALMIC SUSPENSION) Ofloxacin (3 MG/1ML) + Prednisolone (10 MG/1ML) Suspension Ophthalmic บริษัท แอลเลอร์แกน (ประเทศไทย) จำกัด 2016-07-14 Not applicable Thailand 
Categories
- ATC Codes
- J01MA01 — Ofloxacin
- J01MA — Fluoroquinolones
- J01M — QUINOLONE ANTIBACTERIALS
- J01 — ANTIBACTERIALS FOR SYSTEMIC USE
- J — ANTIINFECTIVES FOR SYSTEMIC USE
- J01RA — Combinations of antibacterials
- J01R — COMBINATIONS OF ANTIBACTERIALS
- J01 — ANTIBACTERIALS FOR SYSTEMIC USE
- J — ANTIINFECTIVES FOR SYSTEMIC USE
- Drug Categories
- Agents Causing Muscle Toxicity
- Anti-Bacterial Agents
- Anti-Infective Agents
- Anti-Infective Agents, Urinary
- Antibacterials for Systemic Use
- Antiinfectives for Systemic Use
- BSEP/ABCB11 Substrates
- Cytochrome P-450 CYP1A2 Inhibitors
- Cytochrome P-450 CYP1A2 Inhibitors (strength unknown)
- Cytochrome P-450 Enzyme Inhibitors
- Enzyme Inhibitors
- Fluoroquinolones
- Heterocyclic Compounds, Fused-Ring
- Moderate Risk QTc-Prolonging Agents
- OAT1/SLC22A6 inhibitors
- Ophthalmologicals
- Otologicals
- QTc Prolonging Agents
- Quinolines
- Quinolone Antimicrobial
- Quinolones
- Sensory Organs
- Topoisomerase II Inhibitors
- Topoisomerase Inhibitors
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as quinoline carboxylic acids. These are quinolines in which the quinoline ring system is substituted by a carboxyl group at one or more positions.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Quinolines and derivatives
- Sub Class
- Quinoline carboxylic acids
- Direct Parent
- Quinoline carboxylic acids
- Alternative Parents
- Fluoroquinolones / N-arylpiperazines / Haloquinolines / Hydroquinolones / Aminoquinolines and derivatives / Benzoxazines / Hydroquinolines / Pyridinecarboxylic acids / Dialkylarylamines / N-methylpiperazines show 15 more
- Substituents
- 1,4-diazinane / Alkyl aryl ether / Amine / Amino acid / Amino acid or derivatives / Aminoquinoline / Aromatic heteropolycyclic compound / Aryl fluoride / Aryl halide / Azacycle show 34 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- N-arylpiperazine, organic heterotricyclic compound, N-alkylpiperazine, quinolone antibiotic, fluoroquinolone antibiotic, 3-oxo monocarboxylic acid, oxazinoquinoline (CHEBI:7731)
- Affected organisms
- Enteric bacteria and other eubacteria
Chemical Identifiers
- UNII
- A4P49JAZ9H
- CAS number
- 82419-36-1
- InChI Key
- GSDSWSVVBLHKDQ-UHFFFAOYSA-N
- InChI
- InChI=1S/C18H20FN3O4/c1-10-9-26-17-14-11(16(23)12(18(24)25)8-22(10)14)7-13(19)15(17)21-5-3-20(2)4-6-21/h7-8,10H,3-6,9H2,1-2H3,(H,24,25)
- IUPAC Name
- 7-fluoro-2-methyl-6-(4-methylpiperazin-1-yl)-10-oxo-4-oxa-1-azatricyclo[7.3.1.0^{5,13}]trideca-5(13),6,8,11-tetraene-11-carboxylic acid
- SMILES
- CC1COC2=C3N1C=C(C(O)=O)C(=O)C3=CC(F)=C2N1CCN(C)CC1
References
- Synthesis Reference
- US4382892
- General References
- Not Available
- External Links
- Human Metabolome Database
- HMDB0015296
- KEGG Drug
- D00453
- KEGG Compound
- C07321
- PubChem Compound
- 4583
- PubChem Substance
- 46507574
- ChemSpider
- 4422
- BindingDB
- 50045004
- 7623
- ChEBI
- 7731
- ChEMBL
- CHEMBL4
- Therapeutic Targets Database
- DAP000655
- PharmGKB
- PA450684
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Ofloxacin
- FDA label
- Download (198 KB)
- MSDS
- Download (73.9 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Corneal Transplant / Grafting, Corneal / Keratoplasty, Lamellar / Transplantation, Cornea 1 4 Completed Other Infection 1 4 Completed Supportive Care Amoxicillin / Metronidazole / Ofloxacin / Periodontitis / Root Planing 1 4 Completed Treatment Cataracts 1 4 Completed Treatment Fever / Urinary Tract Infection 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Akorn Inc.
- Alcon Laboratories
- Allergan Inc.
- American Regent
- Apotex Inc.
- AQ Pharmaceuticals Inc.
- A-S Medication Solutions LLC
- Bausch & Lomb Inc.
- Cipla Ltd.
- Daiichi Sankyo
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- Doctor Reddys Laboratories Ltd.
- Falcon Pharmaceuticals Ltd.
- H.J. Harkins Co. Inc.
- Hi Tech Pharmacal Co. Inc.
- Innoviant Pharmacy Inc.
- Janssen-Ortho Inc.
- Lake Erie Medical and Surgical Supply
- Novex Pharma
- Nucare Pharmaceuticals Inc.
- Ortho Mcneil Janssen Pharmaceutical Inc.
- Pacific Pharma Lp
- Pack Pharmaceuticals
- Par Pharmaceuticals
- PD-Rx Pharmaceuticals Inc.
- Pharmaceutical Utilization Management Program VA Inc.
- Pharmaforce Inc.
- Physicians Total Care Inc.
- Preferred Pharmaceuticals Inc.
- Prescript Pharmaceuticals
- Ranbaxy Laboratories
- Rebel Distributors Corp.
- Redpharm Drug
- Sandhills Packaging Inc.
- Santen Inc.
- Teva Pharmaceutical Industries Ltd.
- Dosage Forms
Form Route Strength Solution / drops Auricular (otic) Ointment Ophthalmic 0.3 % Solution / drops Ophthalmic 3 MG/ML Suspension Ophthalmic Tablet Oral Tablet Oral 400.00 mg Tablet, film coated Oral 200.00 MG Ointment Ophthalmic Tablet, coated Oral 200 mg/1 Tablet, coated Oral 300 mg/1 Tablet, coated Oral 400 mg/1 Liquid Intravenous 20 mg / mL Tablet Oral 300 mg Tablet Oral 400 mg Solution Intravenous 400 mg Tablet, coated Oral 400 mg Solution / drops Auricular (otic) 0.3 % Tablet, coated Oral 100 mg Tablet Oral 400.000 mg Solution Auricular (otic) Injection, solution Intravenous 200 mg/100ml Solution / drops Ophthalmic 0.3 % Solution Ophthalmic 0.3 % Solution Ophthalmic 3.000 mg Tablet Oral 200 mg Solution Auricular (otic) 3 mg Injection Intravenous 200 mg/100ml Tablet, coated Oral Solution Conjunctival; Ophthalmic 3 mg Solution Auricular (otic) 3 mg/1mL Solution Ophthalmic 3 mg/1mL Solution / drops Auricular (otic) 3 mg/1mL Solution / drops Ophthalmic 3 mg/1mL Tablet Oral 200 mg/1 Tablet Oral 300 mg/1 Tablet Oral 400 mg/1 Tablet, film coated Oral 200 mg/1 Tablet, film coated Oral 300 mg/1 Tablet, film coated Oral 400 mg/1 Tablet, film coated Oral Solution / drops Ophthalmic Injection Intravenous Solution Oral 3 mg Tablet, film coated Oral 200 mg Injection, solution Intravenous Tablet, film coated Oral 400 mg Solution Auricular (otic) Solution Auricular (otic) 3 mg/ml Solution Intravenous 200 mg Tablet, coated Oral 300 mg Liquid Auricular (otic) 3 mg/1ml Liquid Ophthalmic 3 mg/1ml Tablet, coated Oral 200 mg Tablet, film coated Oral 100 mg Tablet Oral 100 mg Solution 2 mg/1ml Capsule 100 mg - Prices
Unit description Cost Unit Floxin Otic 0.3% Solution 10ml Bottle 142.91USD bottle Ofloxacin 10ml Otic (ear) Solution 132.19USD bottle Ofloxacin 10ml. Ophthalmic (eye) Solution 87.6USD bottle Floxin Otic 0.3% Solution 5ml Bottle 86.49USD bottle Ofloxacin 5ml Otic (ear) Solution 77.21USD bottle Ofloxacin 5ml. Ophthalmic (eye) Solution 43.86USD bottle Ocuflox 0.3% eye drops 11.35USD ml Floxin 400 mg tablet 9.55USD tablet Ofloxacin 0.3% eye drops 8.08USD ml Floxin 200 mg tablet 6.6USD tablet Ofloxacin 400 mg tablet 6.12USD tablet Ofloxacin 300 mg tablet 5.81USD tablet Floxin 300 mg tablet 5.61USD tablet Ofloxacin 200 mg tablet 4.88USD tablet Floxin otic singles 4.28USD each Ocuflox 0.3 % Solution 2.75USD ml Apo-Ofloxacin 0.3 % Solution 1.04USD ml Pms-Ofloxacin 0.3 % Solution 1.04USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5401741 No 1995-03-28 2012-03-27 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 254 dec °C PhysProp water solubility 28.3 mg/mL Not Available logP -0.39 HANSCH,C ET AL. (1995) - Predicted Properties
Property Value Source Water Solubility 1.44 mg/mL ALOGPS logP -0.02 ALOGPS logP 0.09 Chemaxon logS -2.4 ALOGPS pKa (Strongest Acidic) 5.35 Chemaxon pKa (Strongest Basic) 6.72 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 7 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 73.32 Å2 Chemaxon Rotatable Bond Count 2 Chemaxon Refractivity 94.94 m3·mol-1 Chemaxon Polarizability 36.69 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9545 Blood Brain Barrier - 0.9659 Caco-2 permeable + 0.8867 P-glycoprotein substrate Substrate 0.7862 P-glycoprotein inhibitor I Non-inhibitor 0.8782 P-glycoprotein inhibitor II Non-inhibitor 0.8383 Renal organic cation transporter Non-inhibitor 0.7489 CYP450 2C9 substrate Non-substrate 0.8468 CYP450 2D6 substrate Non-substrate 0.9116 CYP450 3A4 substrate Non-substrate 0.6386 CYP450 1A2 substrate Non-inhibitor 0.9045 CYP450 2C9 inhibitor Non-inhibitor 0.907 CYP450 2D6 inhibitor Non-inhibitor 0.9268 CYP450 2C19 inhibitor Non-inhibitor 0.9026 CYP450 3A4 inhibitor Non-inhibitor 0.8309 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.7726 Ames test AMES toxic 0.7844 Carcinogenicity Non-carcinogens 0.9033 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 2.1639 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.8402 hERG inhibition (predictor II) Non-inhibitor 0.866
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 195.5502641 predictedDarkChem Lite v0.1.0 [M-H]- 184.60565 predictedDeepCCS 1.0 (2019) [M+H]+ 196.2312641 predictedDarkChem Lite v0.1.0 [M+H]+ 187.25964 predictedDeepCCS 1.0 (2019) [M+Na]+ 195.8325641 predictedDarkChem Lite v0.1.0 [M+Na]+ 194.42082 predictedDeepCCS 1.0 (2019)
Targets
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- Kind
- Protein
- Organism
- Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Dna topoisomerase type ii (atp-hydrolyzing) activity
- Specific Function
- DNA gyrase negatively supercoils closed circular double-stranded DNA in an ATP-dependent manner and also catalyzes the interconversion of other topological isomers of double-stranded DNA rings, inc...
- Gene Name
- gyrA
- Uniprot ID
- P43700
- Uniprot Name
- DNA gyrase subunit A
- Molecular Weight
- 97817.145 Da
References
- Schmitz FJ, Hofmann B, Hansen B, Scheuring S, Luckefahr M, Klootwijk M, Verhoef J, Fluit A, Heinz HP, Kohrer K, Jones ME: Relationship between ciprofloxacin, ofloxacin, levofloxacin, sparfloxacin and moxifloxacin (BAY 12-8039) MICs and mutations in grlA, grlB, gyrA and gyrB in 116 unrelated clinical isolates of Staphylococcus aureus. J Antimicrob Chemother. 1998 Apr;41(4):481-4. [Article]
- Cambau E, Sougakoff W, Besson M, Truffot-Pernot C, Grosset J, Jarlier V: Selection of a gyrA mutant of Mycobacterium tuberculosis resistant to fluoroquinolones during treatment with ofloxacin. J Infect Dis. 1994 Nov;170(5):1351. [Article]
- Shi R, Zhang J, Li C, Kazumi Y, Sugawara I: Emergence of ofloxacin resistance in Mycobacterium tuberculosis clinical isolates from China as determined by gyrA mutation analysis using denaturing high-pressure liquid chromatography and DNA sequencing. J Clin Microbiol. 2006 Dec;44(12):4566-8. Epub 2006 Oct 11. [Article]
- Kind
- Protein
- Organism
- Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Dna topoisomerase type ii (atp-hydrolyzing) activity
- Specific Function
- Topoisomerase IV is essential for chromosome segregation. It relaxes supercoiled DNA. Performs the decatenation events required during the replication of a circular DNA molecule.
- Gene Name
- parC
- Uniprot ID
- P43702
- Uniprot Name
- DNA topoisomerase 4 subunit A
- Molecular Weight
- 83366.24 Da
References
- Turner AK, Nair S, Wain J: The acquisition of full fluoroquinolone resistance in Salmonella Typhi by accumulation of point mutations in the topoisomerase targets. J Antimicrob Chemother. 2006 Oct;58(4):733-40. Epub 2006 Aug 8. [Article]
- Chau TT, Campbell JI, Galindo CM, Van Minh Hoang N, Diep TS, Nga TT, Van Vinh Chau N, Tuan PQ, Page AL, Ochiai RL, Schultsz C, Wain J, Bhutta ZA, Parry CM, Bhattacharya SK, Dutta S, Agtini M, Dong B, Honghui Y, Anh DD, Canh do G, Naheed A, Albert MJ, Phetsouvanh R, Newton PN, Basnyat B, Arjyal A, La TT, Rang NN, Phuong le T, Van Be Bay P, von Seidlein L, Dougan G, Clemens JD, Vinh H, Hien TT, Chinh NT, Acosta CJ, Farrar J, Dolecek C: Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones. Antimicrob Agents Chemother. 2007 Dec;51(12):4315-23. Epub 2007 Oct 1. [Article]
- Ishiguro F, Toho M, Yamazaki M, Matsuyuki S, Moriya K, Tanaka D, Isobe J, Kyota Y, Muraoka M: [Mutations of gyrA gene and parC gene in fluoroquinolone-resistant Escherichia coli isolates from sporadic diarrheal cases]. Kansenshogaku Zasshi. 2006 Sep;80(5):507-12. [Article]
- Drlica K, Zhao X: DNA gyrase, topoisomerase IV, and the 4-quinolones. Microbiol Mol Biol Rev. 1997 Sep;61(3):377-92. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Ubiquitin binding
- Specific Function
- Control of topological states of DNA by transient breakage and subsequent rejoining of DNA strands. Topoisomerase II makes double-strand breaks. Essential during mitosis and meiosis for proper segr...
- Gene Name
- TOP2A
- Uniprot ID
- P11388
- Uniprot Name
- DNA topoisomerase 2-alpha
- Molecular Weight
- 174383.88 Da
References
- Divo AA, Sartorelli AC, Patton CL, Bia FJ: Activity of fluoroquinolone antibiotics against Plasmodium falciparum in vitro. Antimicrob Agents Chemother. 1988 Aug;32(8):1182-6. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- Curator comments
- This drug is a fluoroquinolone, and these agents are known to inhibit CYP1A2.
- General Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58293.76 Da
References
- Zhang L, Wei MJ, Zhao CY, Qi HM: Determination of the inhibitory potential of 6 fluoroquinolones on CYP1A2 and CYP2C9 in human liver microsomes. Acta Pharmacol Sin. 2008 Dec;29(12):1507-14. doi: 10.1111/j.1745-7254.2008.00908.x. [Article]
- Zhou Q, Yan XF, Zhang ZM, Pan WS, Zeng S: Rational prescription of drugs within similar therapeutic or structural class for gastrointestinal disease treatment: drug metabolism and its related interactions. World J Gastroenterol. 2007 Nov 14;13(42):5618-28. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Symporter activity
- Specific Function
- Sodium-ion dependent, high affinity carnitine transporter. Involved in the active cellular uptake of carnitine. Transports one sodium ion with one molecule of carnitine. Also transports organic cat...
- Gene Name
- SLC22A5
- Uniprot ID
- O76082
- Uniprot Name
- Solute carrier family 22 member 5
- Molecular Weight
- 62751.08 Da
References
- Ohashi R, Tamai I, Yabuuchi H, Nezu JI, Oku A, Sai Y, Shimane M, Tsuji A: Na(+)-dependent carnitine transport by organic cation transporter (OCTN2): its pharmacological and toxicological relevance. J Pharmacol Exp Ther. 1999 Nov;291(2):778-84. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Transporter activity
- Specific Function
- Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotre...
- Gene Name
- ABCC1
- Uniprot ID
- P33527
- Uniprot Name
- Multidrug resistance-associated protein 1
- Molecular Weight
- 171589.5 Da
References
- Terashi K, Oka M, Soda H, Fukuda M, Kawabata S, Nakatomi K, Shiozawa K, Nakamura T, Tsukamoto K, Noguchi Y, Suenaga M, Tei C, Kohno S: Interactions of ofloxacin and erythromycin with the multidrug resistance protein (MRP) in MRP-overexpressing human leukemia cells. Antimicrob Agents Chemother. 2000 Jun;44(6):1697-700. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one ...
- Gene Name
- SLC22A6
- Uniprot ID
- Q4U2R8
- Uniprot Name
- Solute carrier family 22 member 6
- Molecular Weight
- 61815.78 Da
References
- Jariyawat S, Sekine T, Takeda M, Apiwattanakul N, Kanai Y, Sophasan S, Endou H: The interaction and transport of beta-lactam antibiotics with the cloned rat renal organic anion transporter 1. J Pharmacol Exp Ther. 1999 Aug;290(2):672-7. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Organic anion transmembrane transporter activity
- Specific Function
- Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
- Gene Name
- ABCC2
- Uniprot ID
- Q92887
- Uniprot Name
- Canalicular multispecific organic anion transporter 1
- Molecular Weight
- 174205.64 Da
References
- Sasabe H, Tsuji A, Sugiyama Y: Carrier-mediated mechanism for the biliary excretion of the quinolone antibiotic grepafloxacin and its glucuronide in rats. J Pharmacol Exp Ther. 1998 Mar;284(3):1033-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Symporter activity
- Specific Function
- Sodium-ion dependent, low affinity carnitine transporter. Probably transports one sodium ion with one molecule of carnitine. Also transports organic cations such as tetraethylammonium (TEA) without...
- Gene Name
- SLC22A4
- Uniprot ID
- Q9H015
- Uniprot Name
- Solute carrier family 22 member 4
- Molecular Weight
- 62154.48 Da
References
- Yabuuchi H, Tamai I, Nezu J, Sakamoto K, Oku A, Shimane M, Sai Y, Tsuji A: Novel membrane transporter OCTN1 mediates multispecific, bidirectional, and pH-dependent transport of organic cations. J Pharmacol Exp Ther. 1999 May;289(2):768-73. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Transporter activity
- Specific Function
- Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
- Gene Name
- ABCB11
- Uniprot ID
- O95342
- Uniprot Name
- Bile salt export pump
- Molecular Weight
- 146405.83 Da
References
- Pedersen JM, Matsson P, Bergstrom CA, Hoogstraate J, Noren A, LeCluyse EL, Artursson P: Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43. doi: 10.1093/toxsci/kft197. Epub 2013 Sep 6. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:54