PAZUFLOXACIN MESILATE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C16H15FN2O4.CH4O3S
Molecular Weight	414.405
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CS(O)(=O)=O.C[C@H]1COC2=C(C(F)=CC3=C2N1C=C(C(O)=O)C3=O)C4(N)CC4

InChI

InChIKey=UDHGFPATQWQARM-FJXQXJEOSA-N

InChI=1S/C16H15FN2O4.CH4O3S/c1-7-6-23-14-11(16(18)2-3-16)10(17)4-8-12(14)19(7)5-9(13(8)20)15(21)22;1-5(2,3)4/h4-5,7H,2-3,6,18H2,1H3,(H,21,22);1H3,(H,2,3,4)/t7-;/m0./s1

HIDE SMILES / InChI

Molecular Formula	C16H15FN2O4
Molecular Weight	318.2997
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Molecular Formula	CH4O3S
Molecular Weight	96.106
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: http://www.japi.org/october_2009/article_14.pdf
Curator's Comment: description was created based on several sources, including, http://www.mt-pharma.co.jp/e/release/nr/mpc/2002/pdf/e020902.pdf

Pazufloxacin is a fused tricyclic quinolone derivative that has a broad spectrum of anti-bacterial activity. Pazufloxacin inhibits bot DNA gyrase and topoisomerase IV and has shown in vitro activity against Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Klebsiella, Enterobacter, Hafnia, Citrobacter, Proteus, Providencia, Serratia, Shigella, Salmonella, Aeromonas and Yersinia. The drug is used for the treatment of infectious diseases such as abdominal infections, genital infections, urinary tract infections, respiratory tract infections, etc.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Bacterial DNA gyrase 66 Target ID: CHEMBL2311224 Sources: http://www.japi.org/october_2009/article_14.pdf	Inhibitor 8504
Topoisomerase IV 62 Target ID: CHEMBL2363076 Sources: http://www.japi.org/october_2009/article_14.pdf	Inhibitor 8504

Conditions

Condition	Modality	Highest Phase	Product
Abdominal infections 2 Sources: http://www.japi.org/october_2009/article_14.pdf	Curative	Approved 8583	PASIL Approved Use Unknown Launch Date 2002
Genital infections 3 Sources: http://www.japi.org/october_2009/article_14.pdf	Curative	Approved 8583	PASIL Approved Use Unknown Launch Date 2002
Urinary tract infections 207 Sources: http://www.japi.org/october_2009/article_14.pdf	Curative	Approved 8583	PASIL Approved Use Unknown Launch Date 2002
Respiratory tract infections 85 Sources: http://www.japi.org/october_2009/article_14.pdf	Curative	Approved 8583	PASIL Approved Use Unknown Launch Date 2002
Secondary infections after injuries, burns and post-operative 2 Sources: http://www.japi.org/october_2009/article_14.pdf	Curative	Approved 8583	PASIL Approved Use Unknown Launch Date 2002

C_max

Value	Dose	Analyte	Population
8.99 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=48	300 mg single, intravenous dose: 300 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
11 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=48	500 mg single, intravenous dose: 500 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
18.45 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=48	1000 mg single, intravenous dose: 1000 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
11 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=49 \| https://www.pmda.go.jp/drugs/2002/P200200014/48029700_21400AMZ00456_X100_1.pdf#page=28	500 mg 2 times / day multiple, intravenous dose: 500 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
13 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=49	500 mg 2 times / day multiple, intravenous dose: 500 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
11.2 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=49	500 mg 2 times / day multiple, intravenous dose: 500 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
11.6 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=49	500 mg 2 times / day multiple, intravenous dose: 500 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
12.3 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=49	500 mg 2 times / day multiple, intravenous dose: 500 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
10.9 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=49 \| https://www.pmda.go.jp/drugs/2002/P200200014/48029700_21400AMZ00456_X100_1.pdf#page=28	500 mg 2 times / day multiple, intravenous dose: 500 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
18.45 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=49	1000 mg 2 times / day multiple, intravenous dose: 1000 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
23.38 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=49	1000 mg 2 times / day steady-state, intravenous dose: 1000 mg route of administration: Intravenous experiment type: STEADY-STATE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
18.3 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=50	500 mg single, intravenous dose: 500 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
11 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=50	500 mg single, intravenous dose: 500 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
25.74 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=50	1000 mg single, intravenous dose: 1000 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
18.45 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=50	1000 mg single, intravenous dose: 1000 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
25.74 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=51	1000 mg 2 times / day multiple, intravenous dose: 1000 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
25.44 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=51	1000 mg 2 times / day multiple, intravenous dose: 1000 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
13 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=52	1000 mg 2 times / day multiple, intravenous dose: 1000 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
10.47 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=53 \| https://www.jstage.jst.go.jp/article/chemotherapy1995/56/4/56_4_462/_article/-char/en	300 mg single, intravenous dose: 300 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
13.3 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=48	300 mg single, intravenous dose: 300 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
21.7 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=48	500 mg single, intravenous dose: 500 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
59.42 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=48	1000 mg single, intravenous dose: 1000 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
21.7 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=49 \| https://www.pmda.go.jp/drugs/2002/P200200014/48029700_21400AMZ00456_X100_1.pdf#page=28	500 mg 2 times / day multiple, intravenous dose: 500 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
57.1 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=49	1000 mg 2 times / day multiple, intravenous dose: 1000 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
57.81 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=49	1000 mg 2 times / day steady-state, intravenous dose: 1000 mg route of administration: Intravenous experiment type: STEADY-STATE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
37.2 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=50	500 mg single, intravenous dose: 500 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
21.7 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=50	500 mg single, intravenous dose: 500 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
73.18 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=50	1000 mg single, intravenous dose: 1000 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
59.42 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=50	1000 mg single, intravenous dose: 1000 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
69.21 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=51	1000 mg 2 times / day multiple, intravenous dose: 1000 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
71.33 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=51	1000 mg 2 times / day multiple, intravenous dose: 1000 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
241 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=52	1000 mg 2 times / day multiple, intravenous dose: 1000 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
421 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=53 \| https://www.jstage.jst.go.jp/article/chemotherapy1995/56/4/56_4_462/_article/-char/en	300 mg single, intravenous dose: 300 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
1.65 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=48	300 mg single, intravenous dose: 300 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1.88 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=48	500 mg single, intravenous dose: 500 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=48	1000 mg single, intravenous dose: 1000 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1.88 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=49 \| https://www.pmda.go.jp/drugs/2002/P200200014/48029700_21400AMZ00456_X100_1.pdf#page=28	500 mg 2 times / day multiple, intravenous dose: 500 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=49	1000 mg 2 times / day multiple, intravenous dose: 1000 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2.9 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=49	1000 mg 2 times / day steady-state, intravenous dose: 1000 mg route of administration: Intravenous experiment type: STEADY-STATE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2.04 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=50	500 mg single, intravenous dose: 500 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1.88 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=50	500 mg single, intravenous dose: 500 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=50	1000 mg single, intravenous dose: 1000 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=50	1000 mg single, intravenous dose: 1000 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=51	1000 mg 2 times / day multiple, intravenous dose: 1000 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3.6 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=51	1000 mg 2 times / day multiple, intravenous dose: 1000 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
21.2 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=52	1000 mg 2 times / day multiple, intravenous dose: 1000 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
31.9 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=53 \| https://www.jstage.jst.go.jp/article/chemotherapy1995/56/4/56_4_462/_article/-char/en	300 mg single, intravenous dose: 300 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PAZUFLOXACIN serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
69.3% OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/400022_6241401G1020_2_006_1F.pdf#page=57			PAZUFLOXACIN serum	Homo sapiens

Doses

Dose	Population	Adverse events
1000 mg single, intravenous Highest studied dose Dose: 1000 mg Route: intravenous Route: single Dose: 1000 mg Sources: https://pubmed.ncbi.nlm.nih.gov/22809012/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/22809012/	Sources: https://pubmed.ncbi.nlm.nih.gov/22809012/
2000 mg single, intravenous Highest studied dose Dose: 2000 mg Route: intravenous Route: single Dose: 2000 mg Sources: https://www.pmda.go.jp/drugs/2010/P201000035/480297000_21400AMZ00456000_A100_1.pdf#page=27 https://www.pmda.go.jp/drugs/2010/P201000035/480297000_21400AMZ00456_K102_1.pdf#page=21	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: https://www.pmda.go.jp/drugs/2010/P201000035/480297000_21400AMZ00456000_A100_1.pdf#page=27 https://www.pmda.go.jp/drugs/2010/P201000035/480297000_21400AMZ00456_K102_1.pdf#page=21	Disc. AE: Erythema... AEs leading to discontinuation/dose reduction: Erythema (12.5%) Sources: https://www.pmda.go.jp/drugs/2010/P201000035/480297000_21400AMZ00456000_A100_1.pdf#page=27 https://www.pmda.go.jp/drugs/2010/P201000035/480297000_21400AMZ00456_K102_1.pdf#page=21
1000 mg 2 times / day multiple, intravenous Recommended\|Studied dose Dose: 1000 mg, 2 times / day Route: intravenous Route: multiple Dose: 1000 mg, 2 times / day Sources: https://www.pmda.go.jp/drugs/2010/P201000035/480297000_21400AMZ00456000_A100_1.pdf#page=27 https://www.pmda.go.jp/drugs/2010/P201000035/480297000_21400AMZ00456_K102_1.pdf#page=21	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: https://www.pmda.go.jp/drugs/2010/P201000035/480297000_21400AMZ00456000_A100_1.pdf#page=27 https://www.pmda.go.jp/drugs/2010/P201000035/480297000_21400AMZ00456_K102_1.pdf#page=21	Disc. AE: Injection site irritation, Hives... Other AEs: Erythema, Erythema... AEs leading to discontinuation/dose reduction: Injection site irritation Hives Injection site pain Other AEs: Erythema Erythema (12.5%) Sources: https://www.pmda.go.jp/drugs/2010/P201000035/480297000_21400AMZ00456000_A100_1.pdf#page=27 https://www.pmda.go.jp/drugs/2010/P201000035/480297000_21400AMZ00456_K102_1.pdf#page=21
1000 mg 2 times / day multiple, intravenous Recommended\|Studied dose Dose: 1000 mg, 2 times / day Route: intravenous Route: multiple Dose: 1000 mg, 2 times / day Sources: https://www.pmda.go.jp/drugs/2010/P201000035/480297000_21400AMZ00456000_A100_1.pdf#page=30 https://www.pmda.go.jp/drugs/2010/P201000035/480297000_21400AMZ00456_K102_1.pdf#page=130	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.pmda.go.jp/drugs/2010/P201000035/480297000_21400AMZ00456000_A100_1.pdf#page=30 https://www.pmda.go.jp/drugs/2010/P201000035/480297000_21400AMZ00456_K102_1.pdf#page=130	Disc. AE: Injection site erythema, Vomiting... Other AEs: Injection site swelling... AEs leading to discontinuation/dose reduction: Injection site erythema (2, 2.9%) Vomiting (2, 1.4%) Akathisia (2, 0.7%) Increased AST (0.7%) Increased ALT (0.7%) Dizziness (0.7%) Injection site phlebitis (0.7%) Convulsion (2, 0.7%) Asthma (3, 0.7%) Hypoesthesia (2, 0.7%) Facial edema (2, 0.7%) Edema (2, 0.7%) Discomfort (0.7%) Other AEs: Injection site swelling (2, 2.9%) Sources: https://www.pmda.go.jp/drugs/2010/P201000035/480297000_21400AMZ00456000_A100_1.pdf#page=30 https://www.pmda.go.jp/drugs/2010/P201000035/480297000_21400AMZ00456_K102_1.pdf#page=130

AEs

PubMed

Title	Date	PubMed
[Drug interactions between nonsteroidal anti-inflammatory drug and pazufloxacin mesilate, a new quinolone antibacterial agent for intravenous use: convulsions in mice after intravenous or intracerebroventricular administration].	2002-06	12199111

Patents

Sample Use Guides

In Vivo Use Guide

The usually recommended dose of Pazufloxacin Injections in most infections is 500 mg twice a day administered as an I.V. infusion over 30-60 minutes. Depending on age, symptoms and severity of infection, the dose of the drug may be reduced to 300 mg twice a day.

Route of Administration: Intravenous

In Vitro Use Guide

Pazufloxacin has good antibacterial activity against variety of clinical isolates. The MICs at which 90% of the isolates were inhibited (MIC90s) of pazufloxacin were 0.2 to 0.39 ug/ml for Staphylococcus aureus and Staphylococcus epidermidis, including methicillin-resistant strains.5 Pazufloxacin has similar or 2-fold greater activity than other quinolones, against the following Enterobacteriaceae (MIC90 ≤ 0.25 ug/ml): Escherichia coli, Klebsiella, Enterobacter, Hafnia, Citrobacter, Proteus, Providencia, Serratia, Shigella, Salmonella, Aeromonas and Yersinia. Against P. aeruginosa, pazufloxacin shows more potent activity than tosufloxacin, norfloxacin and ofloxacin. Against clinical isolates of methicillin-resistant Staphylococcus aureus and P. aeruginosa, pazufloxacin has an MIC90 of 0.39 ug/ml and an MIC90 of 0.78 ug/ml respectively. MIC90 for clinical isolates of H. influenzae is ≤ 0.013 ug/l.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 19:20:55 GMT 2025` Edited by `admin` on `Mon Mar 31 19:20:55 GMT 2025`
Record UNII	2XI226J1HS
Record Status	`Validated (UNII)`
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Name

Type

Language

PAZUFLOXACIN METHANESULFONATE

Preferred Name

English

PAZUFLOXACIN MESILATE

Common Name

English

PAZUFLOXACIN MESYLATE

Common Name

English

(-)-(3S)-10-(1-AMINOCYCLOPROPYL)-9-FLUORO-2,3-DIHYDRO-3-METHYL-7-OXO-7H-PYRIDO(1,2,3-DE)-1,4-BENZOXAZINE-6-CARBOXYLIC ACID METHANESULFONATE

Systematic Name

English

Pazufloxacin mesilate [WHO-DD]

Common Name

English

PAZUFLOXACIN MESILATE [MART.]

Common Name

English

(-)-(3S)-10-(1-AMINOCYCLOPROPYL)-9-FLUORO-2,3-DIHYDRO-3-METHYL-7-OXO-7H-PYRIDO(1,2,3-DE)-1,4-BENZOXAZINE-6-CARBOXYLIC ACID METHANESULPHONATE

Systematic Name

English

NSC-759831

Code

English

PAZUFLOXACIN MESILATE [JAN]

Common Name

English

PAZUFLOXACIN METHANESULFONATE [MI]

Common Name

English

Code System Code Type Description

EVMPD

SUB16450MIG