*** CHEMICAL IDENTIFICATION ***
RTECS NUMBER : UU8815500
CHEMICAL NAME : 7H-Pyrido(1,2,3-de)-1,4-benzoxazine-6-carboxylic
acid, 2,3-dihydro-9-fluoro-3-methyl-10-
(4-methyl-1-piperazinyl)-7-oxo-, (+-)-
CAS REGISTRY NUMBER : 82419-36-1
OTHER CAS REGISTRY NOS. : 83380-47-6
BEILSTEIN REFERENCE NO. : 3657947
LAST UPDATED : 199806
DATA ITEMS CITED : 28
MOLECULAR FORMULA : C18-H20-F-N3-O4
MOLECULAR WEIGHT : 361.41
COMPOUND DESCRIPTOR : Drug
Mutagen
Reproductive Effector
Human
SYNONYMS/TRADE NAMES :
* DL-8280
* HOE 280
* Oflocet
* Ofloxacin
* (+-)-Ofloxacin
* Ofloxacine
* ORF 18489
* Oxaldin
* PT 01
* Tarivid
* Visiren
*** HEALTH HAZARD DATA ***
** ACUTE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - man
DOSE/DURATION : 17 mg/kg/3D-I
TOXIC EFFECTS :
Behavioral - excitement
Blood - changes in cell count (unspecified)
Skin and Appendages - dermatitis, allergic (after systemic exposure)
REFERENCE :
IEDIEP Internal Medicine. (The Japanese Society of Internal Medicine, 34-3,
3-chome, Hongo, Bunkyo-ku, Tokyo 113, Japan) V.31- 1992-
Volume(issue)/page/year: 34,872,1995
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - woman
DOSE/DURATION : 24 mg/kg/3D-I
TOXIC EFFECTS :
Behavioral - hallucinations, distorted perceptions
Behavioral - toxic psychosis
Behavioral - irritability
REFERENCE :
JCLPDE Journal of Clinical Psychiatry. (Physicians Postgraduate Press,
Inc., POB 240008, Memphis, TN 38124) V.39- 1978-
Volume(issue)/page/year: 53,137,1992
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - man
DOSE/DURATION : 51428 ug/kg
TOXIC EFFECTS :
Gastrointestinal - hypermotility, diarrhea
Nutritional and Gross Metabolic - body temperature increase
REFERENCE :
AJMEAZ American Journal of Medicine. (Technical Pub., 875 Third Ave., New
York, NY 10022) V.1- 1946- Volume(issue)/page/year: 87,479,1989
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 3590 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
Behavioral - ataxia
Lungs, Thorax, or Respiration - respiratory depression
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year:
32(Suppl 1),1084,1984
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 7070 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
Behavioral - ataxia
Lungs, Thorax, or Respiration - respiratory depression
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year:
32(Suppl 1),1084,1984
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 273 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
Behavioral - coma
Lungs, Thorax, or Respiration - respiratory depression
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year:
32(Suppl 1),1084,1984
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 3266 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
ZKZAEY Zhongguo Kangshengsu Zazhi. Chinese Journal of Antibiotics.
(Zhongguo Kangshengsu Zazhi Bianjibu, 9 Shanbanqiaolu, Chenqdu, 610051 Peop.
Rep. China) V.13- 1988- Volume(issue)/page/year: 18,218,1993
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 805 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ENSHEE Ensho. Japanese Journal of Inflammation. (The Japanese Society of
Inflammation, 4-5-505 Iidabashi, 4-Chrome, Chiyoda-ku, Tokyo 102, Japan)
V.1- 1981- Volume(issue)/page/year: 11,343,1991
TYPE OF TEST : LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 7690 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year:
32(Suppl 1),1084,1984
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 208 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
Behavioral - coma
Lungs, Thorax, or Respiration - respiratory depression
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year:
32(Suppl 1),1084,1984
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intramuscular
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : >600 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
ZKZAEY Zhongguo Kangshengsu Zazhi. Chinese Journal of Antibiotics.
(Zhongguo Kangshengsu Zazhi Bianjibu, 9 Shanbanqiaolu, Chenqdu, 610051 Peop.
Rep. China) V.13- 1988- Volume(issue)/page/year: 18,218,1993
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : >200 mg/kg
TOXIC EFFECTS :
Gastrointestinal - changes in structure or function of salivary glands
Gastrointestinal - hypermotility, diarrhea
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year:
32(Suppl 1),1084,1984
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : >70 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo,
Japan) Volume(issue)/page/year: -,291,1995
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Primate - monkey
DOSE/DURATION : 500 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year:
32(Suppl 1),1084,1984
** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 7560 mg/kg/4W-I
TOXIC EFFECTS :
Behavioral - fluid intake
Kidney, Ureter, Bladder - other changes in urine composition
Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year:
32(Suppl 1),1091,1984
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : 5600 mg/kg/4W-I
TOXIC EFFECTS :
Gastrointestinal - other changes
Musculoskeletal - joints
Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year:
32(Suppl 1),1105,1984
** REPRODUCTIVE DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 990 mg/kg
SEX/DURATION : female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death,
e.g., stunted fetus)
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag,
Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951-
Volume(issue)/page/year: 36,1244,1986
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 1620 mg/kg
SEX/DURATION : female 9-10 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight
gain)
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag,
Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951-
Volume(issue)/page/year: 36,1244,1986
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 8910 mg/kg
SEX/DURATION : female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4
per # born alive)
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag,
Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951-
Volume(issue)/page/year: 36,1244,1986
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rabbit
DOSE : 2080 mg/kg
SEX/DURATION : female 6-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetal death
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag,
Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951-
Volume(issue)/page/year: 36,1244,1986
** MUTATION DATA **
TYPE OF TEST : Mutation in microorganisms
TEST SYSTEM : Bacteria - Salmonella typhimurium
DOSE/DURATION : 50 ng/plate
REFERENCE :
MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE
Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 248,135,1991
TYPE OF TEST : Mutation test systems - not otherwise specified
TEST SYSTEM : Bacteria - Escherichia coli
DOSE/DURATION : 200 ug/L
REFERENCE :
AMACCQ Antimicrobial Agents and Chemotherapy. (American Soc. for
Microbiology, 1913 I St., NW, Washington, DC 20006) V.1- 1972-
Volume(issue)/page/year: 37,213,1993
TYPE OF TEST : DNA inhibition
TEST SYSTEM : Bacteria - Escherichia coli
DOSE/DURATION : 25 mg/L
REFERENCE :
AMACCQ Antimicrobial Agents and Chemotherapy. (American Soc. for
Microbiology, 1913 I St., NW, Washington, DC 20006) V.1- 1972-
Volume(issue)/page/year: 34,1955,1990
TYPE OF TEST : Phage inhibition capacity
TEST SYSTEM : Bacteria - Escherichia coli
DOSE/DURATION : 100 ug/L
REFERENCE :
AMACCQ Antimicrobial Agents and Chemotherapy. (American Soc. for
Microbiology, 1913 I St., NW, Washington, DC 20006) V.1- 1972-
Volume(issue)/page/year: 37,213,1993
TYPE OF TEST : DNA repair
TEST SYSTEM : Bacteria - Bacillus subtilis
DOSE/DURATION : 20 mg/L
REFERENCE :
AMACCQ Antimicrobial Agents and Chemotherapy. (American Soc. for
Microbiology, 1913 I St., NW, Washington, DC 20006) V.1- 1972-
Volume(issue)/page/year: 37,213,1993
TYPE OF TEST : DNA damage
TEST SYSTEM : Human Lymphocyte
DOSE/DURATION : 80 mg/L
REFERENCE :
MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE
Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 211,171,1989
TYPE OF TEST : Unscheduled DNA synthesis
TEST SYSTEM : Rodent - rat Liver
DOSE/DURATION : 1100 umol/L
REFERENCE :
MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE
Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 221,263,1989
TYPE OF TEST : DNA inhibition
TEST SYSTEM : Mammal - domestic Cells - not otherwise specified
DOSE/DURATION : 27 mg/L
REFERENCE :
AMACCQ Antimicrobial Agents and Chemotherapy. (American Soc. for
Microbiology, 1913 I St., NW, Washington, DC 20006) V.1- 1972-
Volume(issue)/page/year: 34,1955,1990
*** END OF RECORD ***