TOSUFLOXACIN

Possibly Marketed Outside US

Details

Stereochemistry	RACEMIC
Molecular Formula	C19H15F3N4O3
Molecular Weight	404.3426
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

NC1CCN(C1)C2=NC3=C(C=C2F)C(=O)C(=CN3C4=CC=C(F)C=C4F)C(O)=O

InChI

InChIKey=WUWFMDMBOJLQIV-UHFFFAOYSA-N

InChI=1S/C19H15F3N4O3/c20-9-1-2-15(13(21)5-9)26-8-12(19(28)29)16(27)11-6-14(22)18(24-17(11)26)25-4-3-10(23)7-25/h1-2,5-6,8,10H,3-4,7,23H2,(H,28,29)

HIDE SMILES / InChI

Description

Tosufloxacin is a fluoroquinolone antibacterial agent. Tosufloxacin is an inhibitor of bacterial DNA gyrase and topoisomerase IV. Tosufloxacin is indicated for the treatment of various infections such as skin, respiratory, urinary, gynecologic, ophthalmologic, otolaryngologic, dental infections. Fluoroquinolones including tosufloxacin have a potential risk of inducing cartilage and joint toxicity in children. It is also associated with severe thrombocytopenia and nephritis, and hepatotoxicity.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Bacterial DNA gyrase	Inhibitor
Topoisomerase IV	Inhibitor

Conditions

Condition	Modality	Highest Phase	Product
Infectious enteritis	Curative	Approved	Ozex
Cystitis	Curative	Approved	Ozex
Prostatitis	Curative	Approved	Ozex
Pneumonia	Curative	Approved	Ozex

C_max

Value	Dose	Analyte	Population
0.45 μg/L	150 mg 3 times / day multiple, oral	TOSUFLOXACIN plasma	Homo sapiens
0.6 μg/L	150 mg 3 times / day multiple, oral	TOSUFLOXACIN plasma	Homo sapiens
0.83 μg/L	150 mg single, oral	TOSUFLOXACIN plasma	Homo sapiens
0.62 μg/L	150 mg single, oral	TOSUFLOXACIN plasma	Homo sapiens
0.73 μg/L	150 mg single, oral	TOSUFLOXACIN plasma	Homo sapiens
0.82 μg/L	150 mg single, oral	TOSUFLOXACIN plasma	Homo sapiens

AUC

Value	Dose	Co-administered	Analyte	Population
4.09 μg × h/mL	150 mg 3 times / day multiple, oral		TOSUFLOXACIN plasma	Homo sapiens
3.84 μg × h/mL	150 mg 3 times / day multiple, oral		TOSUFLOXACIN plasma	Homo sapiens

T_1/2

Value	Dose	Analyte	Population
4.5 h	150 mg 3 times / day multiple, oral	TOSUFLOXACIN plasma	Homo sapiens
3.59 h	150 mg 3 times / day multiple, oral	TOSUFLOXACIN plasma	Homo sapiens
3.85 h	150 mg single, oral	TOSUFLOXACIN plasma	Homo sapiens
4 h	150 mg single, oral	TOSUFLOXACIN plasma	Homo sapiens
9.8 h	150 mg single, oral	TOSUFLOXACIN plasma	Homo sapiens
10.5 h	150 mg single, oral	TOSUFLOXACIN plasma	Homo sapiens

Doses

Show entries

Dose	Population	Adverse events
200 mg 3 times / day multiple, oral Recommended	unhealthy, ADULT	Disc. AE: Anaphylactoid shock, Toxic epidermal necrolysis...
300 mg 2 times / day multiple, oral Recommended	unhealthy, ADULT

Showing 1 to 2 of 2 entries

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AEs

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AE	Significance	Dose	Population
Acute renal failure	Disc. AE	200 mg 3 times / day multiple, oral Recommended	unhealthy, ADULT
Anaphylactoid shock	Disc. AE	200 mg 3 times / day multiple, oral Recommended	unhealthy, ADULT
Consciousness abnormal	Disc. AE	200 mg 3 times / day multiple, oral Recommended	unhealthy, ADULT
Convulsion	Disc. AE	200 mg 3 times / day multiple, oral Recommended	unhealthy, ADULT
Interstitial nephritis	Disc. AE	200 mg 3 times / day multiple, oral Recommended	unhealthy, ADULT

Showing 1 to 5 of 8 entries

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PubMed

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Title	Date	PubMed
In-vitro activity of quinolones and macrolides against mycobacteria.	1994 Sep	7829409
Trovafloxacin is active against Toxoplasma gondii.	1996 Aug	8843293
Therapeutic effect of the quinolone prodrug prulifloxacin against experimental urinary tract infections in mice.	1996 Dec	9006794
[In vitro anti-MAC activities of new quinolones in focus (2)].	1996 Sep	8999137
History of quinolones and their side effects.	2001	11549783

Showing 1 to 5 of 22 entries

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Patents

Sample Use Guides

In Vivo Use Guide

In general, for adults, take 2 to 3 tablets (300 to 450 mg of the active ingredient) a day, in 2 to 3 divided doses. The dosage may be adjusted according to disease, symptoms, etc. of the patient. If symptoms are severe or the effect is insufficient, take 4 tablets (600 mg) a day. Osteomyelitis, arthritis: In general, for adults, take 1 tablet (150 mg of the active ingredient) at a time, 3 times a day. The dosage may be adjusted according to disease, symptoms, etc. of the patient. If symptoms are severe or the effect is insufficient, take 4 tablets (600 mg) a day. Typhoid/paratyphoid fever: In general, for adults, take 1 tablet (150 mg of the active ingredient) at a time, 4 times a day for 14 days.

Route of Administration: Oral

In Vitro Use Guide

The MIC90s of tosufloxacin among the 27 isolates of macrolide-resistant Mycoplasma pneumoniae (MRMP) was 0.25 ug/ml and those among the 23 isolates of macrolide-sensitive Mycoplasma pneumoniae (MSMP) was 0.5 μg/ml.

Show entries

Name

Type

Language

TOSUFLOXACIN

Official Name

English

Tosufloxacin [WHO-DD]

Common Name

English

A 67107

Code