*** CHEMICAL IDENTIFICATION ***
RTECS NUMBER : VB2002000
CHEMICAL NAME : 3-Quinolinecarboxylic acid,
1,4-dihydro-1-ethyl-6-fluoro-7-(4-methyl-1-piperaziny
l)-4-oxo-
CAS REGISTRY NUMBER : 70458-92-3
BEILSTEIN REFERENCE NO. : 0567618
REFERENCE : 5-23-03-00135 (Beilstein Handbook Reference)
LAST UPDATED : 199806
DATA ITEMS CITED : 9
MOLECULAR FORMULA : C17-H20-F-N3-O3
MOLECULAR WEIGHT : 333.40
WISWESSER LINE NOTATION : T66 BN VVJ B2 DVQ HF I- AT6N DNTJ D1
COMPOUND DESCRIPTOR : Drug
Mutagen
Reproductive Effector
Human
SYNONYMS/TRADE NAMES :
* AM-725
* AM 725
* 1-Ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(4-methyl-1-piperazinyl)-3-quinolin
ecarboxylic acid
* Pefloxacin
* Pefloxacine
* 1584RB
*** HEALTH HAZARD DATA ***
** ACUTE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - man
DOSE/DURATION : 1714 mg/kg/21W-I
TOXIC EFFECTS :
Peripheral Nerve and Sensation - paresthesis
Peripheral Nerve and Sensation - structural change in nerve or sheath
REFERENCE :
LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823-
Volume(issue)/page/year: 340,126,1992
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - man
DOSE/DURATION : 343 mg/kg/30D-I
TOXIC EFFECTS :
Musculoskeletal - joints
Musculoskeletal - other changes
REFERENCE :
DRSAEA Drug Safety. (Adis International Ltd., Private Bag 65901, Mairangi
Bay, Auckland 10, New Zealand) V.5- 1990- Volume(issue)/page/year:
7,310,1992
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Human - woman
DOSE/DURATION : 16 mg/kg
TOXIC EFFECTS :
Behavioral - hallucinations, distorted perceptions
Behavioral - muscle contraction or spasticity
REFERENCE :
AMDIBO Annales de Medecine Interne. (Masson Abonnements, B.P.22, F-41354
Vineuil Cedex, France) V.120- 1969- Volume(issue)/page/year:
144,495,1993
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : >4 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
USXXAM United States Patent Document. (U.S. Patent Office, Box 9,
Washington, DC 20231) Volume(issue)/page/year: #4530930
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 225 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
EPXXDW European Patent Application. (U.S. Patent and Trademark Office,
Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #0047005
TYPE OF TEST : LD - Lethal dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : >50 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
USXXAM United States Patent Document. (U.S. Patent Office, Box 9,
Washington, DC 20231) Volume(issue)/page/year: #4292317
** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 7500 mg/kg/30D-C
TOXIC EFFECTS :
Liver - changes in liver weight
Kidney, Ureter, Bladder - other changes in urine composition
Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 25,475,1983
** REPRODUCTIVE DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 30 gm/kg
SEX/DURATION : male 30 day(s) pre-mating
TOXIC EFFECTS :
Reproductive - Paternal Effects - testes, epididymis, sperm duct
Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland,
accessory glands
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 25,475,1983
** MUTATION DATA **
TYPE OF TEST : Unscheduled DNA synthesis
TEST SYSTEM : Rodent - rat Liver
DOSE/DURATION : 780 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
*** END OF RECORD ***