*** CHEMICAL IDENTIFICATION ***

RTECS NUMBER            : XI0194000
CHEMICAL NAME           : 4-Thia-1-azabicyclo(3.2.0)hept-2-ene-2-carboxylic
                          acid, 3-(((aminocarbonyl)oxy)methyl)-6-
                          (1-hydroxyethyl)-7-oxo-, (acetyloxy)methyl ester,
                          (5R-(5-alpha,6-beta(R*)))-
CAS REGISTRY NUMBER     : 99376-22-4
LAST UPDATED            : 199606
DATA ITEMS CITED        : 9
MOLECULAR FORMULA       : C13-H16-N2-O8-S
MOLECULAR WEIGHT        : 360.37
COMPOUND DESCRIPTOR     : Drug
SYNONYMS/TRADE NAMES :
   * RIPM-AC
   * Ritipenem acetoxymethyl ester
   * Ritipenem Acoxil
 
                       *** HEALTH HAZARD DATA ***
 
                        ** ACUTE TOXICITY DATA **
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 7230 mg/kg
TOXIC EFFECTS :
   Behavioral - altered sleep time (including change in righting reflex)
   Behavioral - somnolence (general depressed activity)
   Gastrointestinal - hypermotility, diarrhea
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: 29,3329,1995
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intraperitoneal
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 239 mg/kg
TOXIC EFFECTS :
   Behavioral - altered sleep time (including change in righting reflex)
   Behavioral - somnolence (general depressed activity)
   Kidney, Ureter, Bladder - changes in tubules (including acute renal failure,
   acute tubular necrosis)
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: 29,3329,1995
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Subcutaneous
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 353 mg/kg
TOXIC EFFECTS :
   Behavioral - altered sleep time (including change in righting reflex)
   Behavioral - somnolence (general depressed activity)
   Kidney, Ureter, Bladder - changes in tubules (including acute renal failure,
   acute tubular necrosis)
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: 29,3329,1995
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : >7200 mg/kg
TOXIC EFFECTS :
   Behavioral - altered sleep time (including change in righting reflex)
   Behavioral - somnolence (general depressed activity)
   Gastrointestinal - hypermotility, diarrhea
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: 29,3329,1995
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intraperitoneal
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 326 mg/kg
TOXIC EFFECTS :
   Behavioral - altered sleep time (including change in righting reflex)
   Behavioral - somnolence (general depressed activity)
   Kidney, Ureter, Bladder - changes in tubules (including acute renal failure,
   acute tubular necrosis)
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: 29,3329,1995
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Subcutaneous
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 465 mg/kg
TOXIC EFFECTS :
   Behavioral - altered sleep time (including change in righting reflex)
   Behavioral - somnolence (general depressed activity)
   Kidney, Ureter, Bladder - changes in tubules (including acute renal failure,
   acute tubular necrosis)
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: 29,3329,1995
 
TYPE OF TEST            : LD - Lethal dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rabbit
DOSE/DURATION           : >2 gm/kg
TOXIC EFFECTS :
   Kidney, Ureter, Bladder - changes in tubules (including acute renal failure,
   acute tubular necrosis)
   Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)
   Nutritional and Gross Metabolic - changes in potassium
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: 29,3475,1995
 
                 ** OTHER MULTIPLE DOSE TOXICITY DATA **
 
TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 36400 mg/kg/13W-I
TOXIC EFFECTS :
   Cardiac - changes in heart weight
   Kidney, Ureter, Bladder - other changes
   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: 29,3341,1995
 
TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rabbit
DOSE/DURATION           : 2100 mg/kg/7D-I
TOXIC EFFECTS :
   Kidney, Ureter, Bladder - other changes in urine composition
   Nutritional and Gross Metabolic - weight loss or decreased weight gain
   Biochemical - Enzyme inhibition, induction, or change in blood or tissue
   levels - transaminases
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: 29,3459,1995
 
                            *** END OF RECORD ***