*** CHEMICAL IDENTIFICATION ***
RTECS NUMBER : XI0330600
CHEMICAL NAME : 5-Thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic
acid, 7-(((4-(2-amino-1-carboxy-
2-oxoethyl)-1,3-dithietan-2-yl)carbonyl)amino)-7-meth
oxy-3-(((1-methyl-1H- tetrazol-5-yl)
thio)methyl)-8-oxo-, disodium salt, (6R-cis)-
CAS REGISTRY NUMBER : 74356-00-6
LAST UPDATED : 199806
DATA ITEMS CITED : 19
MOLECULAR FORMULA : C17-H15-N7-O8-S4.2Na
MOLECULAR WEIGHT : 619.61
COMPOUND DESCRIPTOR : Drug
Reproductive Effector
Human
SYNONYMS/TRADE NAMES :
* Apatef
* Cefotetan disodium salt
* Cefotetan sodium
* Ceftenon
* Cepan
* Darvilen
* ICI 156834 disodium
* Yamatetan
* YM 09330
*** HEALTH HAZARD DATA ***
** ACUTE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Human - man
DOSE/DURATION : 800 mg/kg/4W-I
TOXIC EFFECTS :
Lungs, Thorax, or Respiration - other changes
REFERENCE :
AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200
Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year:
116,522,1992
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Human - man
DOSE/DURATION : 814 mg/kg/18D-C
TOXIC EFFECTS :
Kidney, Ureter, Bladder - interstitial nephritis
Skin and Appendages - dermatitis, allergic (after systemic exposure)
Nutritional and Gross Metabolic - body temperature increase
REFERENCE :
AJKDDP American Journal of Kidney Diseases. (Grune & Stratton, Inc.,
Journal Subscription Dept., POB 6280, Duluth, MN 55806) V.1- 1981-
Volume(issue)/page/year: 16,259,1990
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : >10 gm/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: -,565,1990
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 8250 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis
Behavioral - altered sleep time (including change in righting reflex)
Behavioral - changes in motor activity (specific assay)
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year:
30(Suppl 1),208,1982
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : >10 gm/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: -,565,1990
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 6790 mg/kg
TOXIC EFFECTS :
Behavioral - tremor
Behavioral - convulsions or effect on seizure threshold
Lungs, Thorax, or Respiration - acute pulmonary edema
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year:
30(Suppl 1),208,1982
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : >10 gm/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: -,565,1990
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 8120 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis
Behavioral - altered sleep time (including change in righting reflex)
Behavioral - changes in motor activity (specific assay)
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year:
30(Suppl 1),208,1982
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : >10 gm/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: -,565,1990
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 4990 mg/kg
TOXIC EFFECTS :
Behavioral - tremor
Behavioral - convulsions or effect on seizure threshold
Lungs, Thorax, or Respiration - acute pulmonary edema
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year:
30(Suppl 1),208,1982
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : >6 gm/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: -,661,1995
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : >6 gm/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: -,565,1990
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Primate - monkey
DOSE/DURATION : >6 gm/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: -,661,1995
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - rabbit
DOSE/DURATION : >6 gm/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: -,565,1990
** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 182 gm/kg/26W-C
TOXIC EFFECTS :
Liver - changes in liver weight
Kidney, Ureter, Bladder - urine volume decreased
Kidney, Ureter, Bladder - changes in bladder weight
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda
Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960-
Volume(issue)/page/year: 16,98,1982
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 35 gm/kg/5W-I
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting
Liver - changes in liver weight
Endocrine - changes in spleen weight
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda
Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960-
Volume(issue)/page/year: 16,15,1982
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 91 gm/kg/13W-I
TOXIC EFFECTS :
Gastrointestinal - hypermotility, diarrhea
Gastrointestinal - nausea or vomiting
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda
Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960-
Volume(issue)/page/year: 16,69,1982
** REPRODUCTIVE DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - rat
DOSE : 5460 mg/kg
SEX/DURATION : male 26 week(s) pre-mating
TOXIC EFFECTS :
Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland,
accessory glands
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda
Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960-
Volume(issue)/page/year: 16,98,1982
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - rat
DOSE : 2700 mg/kg
SEX/DURATION : female 17-22 day(s) after conception
lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Maternal Effects - parturition
Reproductive - Effects on Newborn - behavioral
Reproductive - Effects on Newborn - physical
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 23,767,1982
*** END OF RECORD ***