gatifloxacin

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Dose	Unit	Route
0.40	g	O
0.40	g	P

Property	Value	Reference
BA (Bioavailability)	96 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	1.70 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	2.80 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.80 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	10 hours	Lombardo F, Berellini G, Obach RS
S (Water solubility)	60 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Bocci G, Oprea TI, Benet LZ

Property	Description	Value	Unit	Confidence	Similarity
azlogd74	LogD at pH 7.4	-0.665		High	1
caco2-efflux	Caco-2 efflux ratio (BA/AB)	3.451		High	1
caco2-intrinsic-papp	Caco-2 intrinsic apparent permeability	4.943	10^-6 cm/s	High	1
dh-clint	Dog hepatocyte intrinsic clearance	1.104	uL/min/10^6 cells	High	1
dppb	Dog plasma protein binding (% unbound)	87.350	%	High	1
fcs-ppb	Fetal calf serum protein binding (% unbound)	85.820	%	High	1
herg	hERG pIC50	4.291	pIC50	High	1
hh-clint	Human hepatocyte intrinsic clearance	0.879	uL/min/10^6 cells	High	1
hlm-clint	Human liver microsomal intrinsic clearance	2.938	uL/min/mg protein	High	1
hppb	Human plasma protein binding (% unbound)	89.740	%	High	1
kinase-safety-class	GRK2,PDK1,PDK2,PDK4	4
kinase-selectivity-class	AXL,DYRK1B,EIF2AK3,GRK2,MAPK7,PDK4,PRKDC,STK33,TTK	9
mdck-mdr1-bcrp-efflux	MDCK-MDR1-BCRP efflux ratio	2.944		Moderate	0.72
mdck-mdr1-efflux	MDCK-MDR1 efflux ratio	10.257		High	1
mh-clint	Mouse hepatocyte intrinsic clearance	2.547		High	1
mppb	Mouse plasma protein binding (% unbound)	84.570		High	1
nih-mdck-mdr1-efflux	NIH MDCK-MDR1 efflux ratio	16.943		High	1
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
pld-class	Phospholipidosis risk class (1 = positive, 0 = negative)	0		Moderate	0.72
pppb	Pig plasma protein binding (% unbound)	89.890	%	High	1
rat-kpuu-brain	Rat brain Kpuu	0.097	%	Moderate	0.72
rh-clint	Rat hepatocyte intrinsic clearance	1.107	uL/min/10^6 cells	High	1
rh-fuinc	Rat hepatocyte fraction unbound in incubation	90.830	%	High	1
rppb	Rat plasma protein binding (% unbound)	75.170	%	High	1
solubility-dd	Solubility at pH 7.4 in DMSO	883.080	uM	High	1

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
Anaphylactic reaction	146.45	30.60	54	1373	87470	90539550
Hypoglycaemia	109.02	30.60	41	1386	69807	90557213
Drug hypersensitivity	94.65	30.60	69	1358	463540	90163480
Visual acuity reduced	68.49	30.60	22	1405	23388	90603632
Drug intolerance	57.67	30.60	51	1376	447540	90179480
Toxic anterior segment syndrome	52.20	30.60	11	1416	2239	90624781
Corneal disorder	47.47	30.60	10	1417	2032	90624988
Hyperglycaemia	45.25	30.60	20	1407	50950	90576070
Cataract	44.50	30.60	22	1405	72070	90554950
Keratitis	35.74	30.60	9	1418	3997	90623023
Endophthalmitis	34.34	30.60	9	1418	4676	90622344
Macular oedema	33.92	30.60	9	1418	4900	90622120
Conjunctival hyperaemia	32.69	30.60	8	1419	3161	90623859
Corneal oedema	31.23	30.60	7	1420	1894	90625126
Vision blurred	30.73	30.60	20	1407	110273	90516747

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
Hypoglycaemia	269.11	25.12	101	1840	59753	42559641
Hyperglycaemia	137.70	25.12	58	1883	45801	42573593
Intraocular pressure increased	95.61	25.12	27	1914	6406	42612988
Visual acuity reduced	87.13	25.12	32	1909	17518	42601876
Clostridium colitis	76.04	25.12	17	1924	1564	42617830
Blood glucose decreased	63.49	25.12	24	1917	14195	42605199
Retinal haemorrhage	50.07	25.12	16	1925	5754	42613640
Corneal oedema	44.65	25.12	11	1930	1537	42617857
Blood glucose increased	41.47	25.12	31	1910	73668	42545726
Vitreous opacities	39.33	25.12	8	1933	468	42618926
International normalised ratio increased	38.16	25.12	25	1916	48143	42571251
Eye inflammation	32.40	25.12	10	1931	3208	42616186
Corneal opacity	31.14	25.12	7	1934	658	42618736
Toxic anterior segment syndrome	30.65	25.12	8	1933	1408	42617986
Eye pain	30.26	25.12	15	1926	17015	42602379
Vitreous haemorrhage	29.63	25.12	9	1932	2738	42616656
Vision blurred	28.87	25.12	22	1919	53677	42565717
Anterior chamber cell	27.87	25.12	6	1935	462	42618932
Cataract subcapsular	26.66	25.12	6	1935	567	42618827

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gatifloxacin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Description:

Drug dosage:

ADMET properties:

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Approvals:

FDA Adverse Event Reporting System (Female)

FDA Adverse Event Reporting System (Male)

FDA Adverse Event Reporting System (Geriatric)

FDA Adverse Event Reporting System (Pediatric)

Pharmacologic Action:

Related Drugs by ATC class:

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

🐶 Veterinary Drug Use

🐶 Veterinary products

Acid dissociation constants calculated using MoKa v3.0.0

Orange Book patent data (new drug applications)

Orange Book exclusivity data (new drug applications)

Bioactivity Summary:

External reference:

Pharmaceutical products:

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
Hypoglycaemia	363.28	28.84	130	2784	115974	110470411
Hyperglycaemia	177.38	28.84	71	2843	85019	110501366
Visual acuity reduced	126.99	28.84	43	2871	32130	110554255
Intraocular pressure increased	124.10	28.84	33	2881	10843	110575542
Anaphylactic reaction	105.33	28.84	54	2860	114246	110472139
Corneal disorder	65.96	28.84	15	2899	2582	110583803
Corneal oedema	62.97	28.84	15	2899	3158	110583227
Vitreous opacities	62.91	28.84	12	2902	877	110585508
Toxic anterior segment syndrome	61.70	28.84	15	2899	3439	110582946
Blood glucose decreased	59.20	28.84	24	2890	29464	110556921
Clostridium colitis	57.20	28.84	14	2900	3301	110583084
Vision blurred	47.85	28.84	34	2880	128988	110457397
Conjunctival hyperaemia	44.88	28.84	13	2901	5818	110580567
Endophthalmitis	44.67	28.84	14	2900	8173	110578212
Corneal opacity	41.53	28.84	9	2905	1242	110585143
Drug hypersensitivity	41.18	28.84	55	2859	454035	110132350
Drug intolerance	39.58	28.84	51	2863	406461	110179924
Eye inflammation	39.08	28.84	13	2901	9158	110577227
Retinal haemorrhage	38.63	28.84	13	2901	9488	110576897
Macular oedema	38.37	28.84	12	2902	6954	110579431
Blood glucose increased	38.14	28.84	30	2884	132466	110453919
Cataract subcapsular	35.92	28.84	8	2906	1253	110585132
International normalised ratio increased	34.79	28.84	24	2890	86748	110499637
Eye pain	33.04	28.84	19	2895	50080	110536305
Keratitis fungal	31.53	28.84	6	2908	433	110585952
Corneal endotheliitis	31.52	28.84	5	2909	123	110586262

Source	Code	Description
ATC	J01MA16	ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE QUINOLONE ANTIBACTERIALS Fluoroquinolones
ATC	S01AE06	SENSORY ORGANS OPHTHALMOLOGICALS ANTIINFECTIVES Fluoroquinolones
FDA CS	M0023650	Quinolones
MeSH PA	D000890	Anti-Infective Agents
MeSH PA	D000900	Anti-Bacterial Agents
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D009883	Ophthalmic Solutions
MeSH PA	D059005	Topoisomerase II Inhibitors
CHEBI has role	CHEBI:33231	antitubercular agent
CHEBI has role	CHEBI:33281	antimicrobial agent
CHEBI has role	CHEBI:33282	antibacterial agent
CHEBI has role	CHEBI:35441	antiinfective agent
CHEBI has role	CHEBI:49201	anti-ulcer drug
CHEBI has role	CHEBI:50750	EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
CHEBI has role	CHEBI:66981	ophthalmology drug
FDA EPC	N0000175937	Quinolone Antimicrobial

Disease	Relation	SNOMED_ID	DOID
Acute gonococcal cervicitis	indication	20943002	DOID:10615
Staphylococcal pneumonia	indication	22754005
Acute gonococcal urethritis	indication	29864006
Pneumonia due to Streptococcus	indication	34020007
Gonorrhea of rectum	indication	42746002
Pneumonia due to Mycoplasma pneumoniae	indication	46970008
Bacterial pneumonia	indication	53084003	DOID:874
Klebsiella cystitis	indication	60867007
Haemophilus influenzae pneumonia	indication	70036007
Acute bacterial sinusitis	indication	75498004
Bacterial conjunctivitis	indication	128350005	DOID:9700
Pneumococcal pneumonia	indication	233607000
Chlamydial pneumonia	indication	233609002
Escherichia coli urinary tract infection	indication	301011002
Proteus urinary tract infection	indication	301012009
Bacterial urinary infection	indication	312124009
Infection due to Staphylococcus aureus	indication	406602003
Acute exacerbation of chronic bronchitis	indication	425748003
Urinary tract infection caused by Klebsiella	indication	369001000119100
Moraxella Catarrhalis Chronic Bronchitis	indication
E. Coli Pyelonephritis	indication
Haemophilus Parainfluenzae Chronic Bronchitis	indication
Legionella Pneumophila Pneumonia	indication
Moraxella Catarrhalis Pneumonia	indication
Staphylococcus Chronic Bronchitis	indication
Complicated Proteus UTI	indication
Streptococcus Pneumoniae Chronic Bronchitis	indication
Skin and Skin Structure Streptococcus Infection	indication
Haemophilus Influenzae Chronic Bronchitis	indication
Haemophilus Parainfluenzae Pneumonia	indication
Acute tuberculosis	off-label use	25629007
Pulmonary tuberculosis	off-label use	154283005	DOID:2957

Target	Class	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
DNA topoisomerase 4	Enzyme	PARC_STRPN PARE_STRPN	INHIBITOR			CHEMBL	CHEMBL
DNA gyrase	Enzyme	GYRB_STRPN GYRA_STRPN	INHIBITOR			CHEMBL	CHEMBL
DNA topoisomerase 4 subunit A	Enzyme	PARC_STAAU		IC50	5.92	CHEMBL
DNA gyrase subunit A	Enzyme	GYRA_MYCTU		IC50	5.03	CHEMBL
DNA gyrase	Enzyme	GYRA_ECOLI GYRB_ECOLI		IC50	6.30	CHEMBL

ID	Source
4021187	VUID
N0000148634	NUI
D00589	KEGG_DRUG
180200-66-2	SECONDARY_CAS_RN
4021187	VANDF
CHEBI:5280	CHEBI
GFN	PDB_CHEM_ID
CHEMBL31	ChEMBL_ID
10816	IUPHAR_LIGAND_ID
DB01044	DRUGBANK_ID
L4618BD7KJ	UNII
1546025	RXNORM
8587	MMSL
d04504	MMSL
007995	NDDF
116349004	SNOMEDCT_US
371238005	SNOMEDCT_US
C0753645	UMLSCUI
D000077734	MESH_DESCRIPTOR_UI
7423	INN_ID
5379	PUBCHEM_CID

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
ZYMAXID	HUMAN PRESCRIPTION DRUG LABEL	1	0023-3615	SOLUTION/ DROPS	5 mg	OPHTHALMIC	NDA	25 sections
Gatifloxacin	HUMAN PRESCRIPTION DRUG LABEL	1	50383-189	SOLUTION/ DROPS	5 mg	OPHTHALMIC	ANDA	23 sections
ZYMAXID	HUMAN PRESCRIPTION DRUG LABEL	1	54868-6303	SOLUTION/ DROPS	5 mg	OPHTHALMIC	NDA	25 sections
Gatifloxacin	HUMAN PRESCRIPTION DRUG LABEL	1	61314-672	SOLUTION/ DROPS	5 mg	OPHTHALMIC	ANDA	23 sections
Gatifloxacin Ophthalmic Solution 0.5%	Human Prescription Drug Label	1	65145-207	SOLUTION	5 mg	OPHTHALMIC	ANDA	22 sections
GATIFLOXACIN	HUMAN PRESCRIPTION DRUG LABEL	1	69315-331	SOLUTION	5 mg	OPHTHALMIC	ANDA	23 sections

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	6.23	acidic
pKa2	8.39	Basic
pKa3	1.22	Basic