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ofloxacin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
antibacterials, nalidixic acid derivatives	1981	82419-36-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: gailuoxian ofloxacine oxaldin prifloxcin prifloxin ofloxacin ofloxacin hydrochloride ofloxacin HCl	A synthetic fluoroquinolone antibacterial agent that inhibits the supercoiling activity of bacterial DNA GYRASE, halting DNA REPLICATION. Molecular weight: 361.37 Formula: C18H20FN3O4 CLOGP: -0.26 LIPINSKI: 0 HAC: 7 HDO: 1 TPSA: 73.32 ALOGS: -2.40 ROTB: 2 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

gailuoxian
ofloxacine
oxaldin
prifloxcin
prifloxin
ofloxacin
ofloxacin hydrochloride
ofloxacin HCl

A synthetic fluoroquinolone antibacterial agent that inhibits the supercoiling activity of bacterial DNA GYRASE, halting DNA REPLICATION.

Molecular weight: 361.37
Formula: C18H20FN3O4
CLOGP: -0.26
LIPINSKI: 0
HAC: 7
HDO: 1
TPSA: 73.32
ALOGS: -2.40
ROTB: 2

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.40	g	O
0.40	g	P

ADMET properties:

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Property	Value	Reference
t_half (Half-life)	8.90 hours	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	64 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	31.62 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
S (Water solubility)	3.54 mg/mL	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	2.50 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	1.60 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.75 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Dec. 28, 1990	FDA

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Endophthalmitis	106.47	15.71	32	7554	3560	63477876
Toxic anterior segment syndrome	94.55	15.71	25	7561	1746	63479690
Acute kidney injury	78.06	15.71	124	7462	263291	63218145
Hypopyon	72.69	15.71	17	7569	715	63480721
Corneal perforation	66.59	15.71	15	7571	533	63480903
Drug reaction with eosinophilia and systemic symptoms	65.19	15.71	44	7542	33792	63447644
Cholestasis	60.86	15.71	40	7546	29394	63452042
Eye pain	53.50	15.71	39	7547	33815	63447621
Rash maculo-papular	53.28	15.71	38	7548	31858	63449578
Eosinophilia	52.16	15.71	33	7553	22723	63458713

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Drug reaction with eosinophilia and systemic symptoms	156.51	15.95	93	7197	32919	34916722
Type 2 lepra reaction	79.66	15.95	16	7274	179	34949462
Tendonitis	77.71	15.95	38	7252	9102	34940539
Cholestasis	73.97	15.95	54	7236	26894	34922747
Hepatocellular injury	71.35	15.95	49	7241	22162	34927479
Rash maculo-papular	62.64	15.95	50	7240	28401	34921240
Agranulocytosis	59.25	15.95	45	7245	23776	34925865
Toxic epidermal necrolysis	58.54	15.95	43	7247	21603	34928038
Endophthalmitis	57.07	15.95	23	7267	3485	34946156
Eosinophilia	55.42	15.95	45	7245	26177	34923464

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Drug reaction with eosinophilia and systemic symptoms	208.44	13.83	132	13422	64112	79666722
Endophthalmitis	150.05	13.83	52	13502	6376	79724458
Cholestasis	125.46	13.83	89	13465	52020	79678814
Acute kidney injury	115.73	13.83	265	13289	519139	79211695
Rash maculo-papular	112.93	13.83	86	13468	55992	79674842
Toxic anterior segment syndrome	107.82	13.83	33	13521	2731	79728103
Corneal oedema	101.01	13.83	31	13523	2589	79728245
Eosinophilia	98.99	13.83	73	13481	45272	79685562
Tendonitis	97.88	13.83	57	13497	23773	79707061
Type 2 lepra reaction	92.59	13.83	18	13536	210	79730624

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	J01MA01	ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE QUINOLONE ANTIBACTERIALS Fluoroquinolones
ATC	J01RA09	ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE COMBINATIONS OF ANTIBACTERIALS Combinations of antibacterials
ATC	S01AE01	SENSORY ORGANS OPHTHALMOLOGICALS ANTIINFECTIVES Fluoroquinolones
ATC	S02AA16	SENSORY ORGANS OTOLOGICALS ANTIINFECTIVES Antiinfectives
CHEBI has role	CHEBI:35441	antiinfective agents
CHEBI has role	CHEBI:36047	antibacterial drugs
CHEBI has role	CHEBI:50750	inhibitors of type II topoisomerase
CHEBI has role	CHEBI:53559	topoisomerase IV inhibitors
CHEBI has role	CHEBI:59517	DNA synthesis inhibitors
FDA CS	M0023650	Quinolones

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Otitis externa	indication	3135009
Typhoid fever	indication	4834000	DOID:13258
Septicemia due to Escherichia coli	indication	9323009
Prostatitis	indication	9713002	DOID:14654
Infection due to Pseudomonas aeruginosa	indication	11218009
Gonorrhea	indication	15628003	DOID:7551
Enteric campylobacteriosis	indication	18081009
Infectious diarrheal disease	indication	19213003	DOID:13250
Infection of skin AND/OR subcutaneous tissue	indication	19824006
Acute gonococcal cervicitis	indication	20943002	DOID:10615

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

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Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	6.12	acidic
pKa2	8.29	Basic
pKa3	1.12	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		IC50	4.54	WOMBAT-PK
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		IC50	4.41	WOMBAT-PK
Histamine H3 receptor	GPCR	Q9Y5N1	HRH3_HUMAN		IC50	4.55	WOMBAT-PK
Gamma-aminobutyric acid receptor subunit alpha-2	Ion channel	P47869	GBRA2_HUMAN		IC50	4.23	WOMBAT-PK
DNA gyrase subunit A	Enzyme		GYRA_ECOLI	INHIBITOR	IC50	5.28	WOMBAT-PK	CHEMBL
DNA gyrase subunit B	Enzyme		GYRB_ECO57				WOMBAT-PK
Gag-Pro-Pol polyprotein	Polyprotein		POL_HTL1A		IC50	4.82	WOMBAT-PK
GABA-A receptor; anion channel	Ion channel		GBRP_RAT GBRB1_RAT GBRD_RAT GBRG2_RAT GBRA5_RAT GBRA3_RAT GBRG1_RAT GBRA2_RAT GBRA4_RAT GBRG3_RAT GBRA6_RAT GBRA1_RAT GBRB3_RAT GBRB2_RAT Q91ZM7_RAT GBRE_RAT		IC50	4.96	CHEMBL
CAAX prenyl protease 1	Enzyme		STE24_YEAST		AC50	5.71	CHEMBL
Trypsin	Enzyme		TRYP_PIG		AC50	5.03	CHEMBL

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External reference:

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ID	Source
003563	NDDF
004136	NDDF
10918	IUPHAR_LIGAND_ID
118120-51-7	SECONDARY_CAS_RN
387551000	SNOMEDCT_US
4019567	VUID
4019567	VANDF
441553007	SNOMEDCT_US
4583	PUBCHEM_CID
47400	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
OCUFLOX	HUMAN PRESCRIPTION DRUG LABEL	1	11980-779	SOLUTION/ DROPS	3 mg	OPHTHALMIC	NDA	22 sections
OCUFLOX	HUMAN PRESCRIPTION DRUG LABEL	1	11980-779	SOLUTION/ DROPS	3 mg	OPHTHALMIC	NDA	22 sections
Ofloxacin	HUMAN PRESCRIPTION DRUG LABEL	1	0404-7189	SOLUTION/ DROPS	3 mg	OPHTHALMIC	ANDA	24 sections
Ofloxacin	HUMAN PRESCRIPTION DRUG LABEL	1	0517-0760	SOLUTION/ DROPS	3 mg	OPHTHALMIC	ANDA	22 sections
Ofloxacin	HUMAN PRESCRIPTION DRUG LABEL	1	0517-0761	SOLUTION/ DROPS	3 mg	OPHTHALMIC	ANDA	22 sections
Ofloxacin	HUMAN PRESCRIPTION DRUG LABEL	1	13985-602	SOLUTION/ DROPS	3 mg	OPHTHALMIC	ANDA	25 sections
OFLOXACIN	HUMAN PRESCRIPTION DRUG LABEL	1	16590-175	SOLUTION/ DROPS	3 mg	OPHTHALMIC	ANDA	10 sections
OFLOXACIN	HUMAN PRESCRIPTION DRUG LABEL	1	16590-931	SOLUTION/ DROPS	3 mg	AURICULAR (OTIC)	ANDA	11 sections
Ofloxacin	HUMAN PRESCRIPTION DRUG LABEL	1	17478-713	SOLUTION/ DROPS	3 mg	OPHTHALMIC	ANDA	23 sections
Ofloxacin	HUMAN PRESCRIPTION DRUG LABEL	1	17478-713	SOLUTION/ DROPS	3 mg	OPHTHALMIC	ANDA	23 sections

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