*** CHEMICAL IDENTIFICATION ***
RTECS NUMBER : DE8260000
CHEMICAL NAME : 10H-Benzo(4,5)cyclohepta(1,2-b)thiophen-10-one,
4,9-dihydro-4-(1-methyl-4- piperidinylidene)-,
(E)-2-butenedioate (1:1)
CAS REGISTRY NUMBER : 34580-14-8
LAST UPDATED : 199409
DATA ITEMS CITED : 14
MOLECULAR FORMULA : C19-H19-N-O-S.C4-H4-O4
MOLECULAR WEIGHT : 425.53
COMPOUND DESCRIPTOR : Drug
Human
SYNONYMS/TRADE NAMES :
* HC 20-511 fumarate
* Ketotifen fumarate
* Zaditen
*** HEALTH HAZARD DATA ***
** ACUTE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - woman
DOSE/DURATION : 500 ug/kg
TOXIC EFFECTS :
Behavioral - general anesthetic
Behavioral - convulsions or effect on seizure threshold
Lungs, Thorax, or Respiration - respiratory depression
REFERENCE :
DRSAEA Drug Safety. (Adis International Ltd., Private Bag 65901, Mairangi
Bay, Auckland 10, New Zealand) V.5- 1990- Volume(issue)/page/year:
7,387,1992
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - man
DOSE/DURATION : 286 ug/kg
TOXIC EFFECTS :
Behavioral - hallucinations, distorted perceptions
Cardiac - pulse rate
REFERENCE :
DRSAEA Drug Safety. (Adis International Ltd., Private Bag 65901, Mairangi
Bay, Auckland 10, New Zealand) V.5- 1990- Volume(issue)/page/year:
7,387,1992
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - child
DOSE/DURATION : 200 ug/kg
TOXIC EFFECTS :
Lungs, Thorax, or Respiration - dyspnea
Lungs, Thorax, or Respiration - respiratory stimulation
Nutritional and Gross Metabolic - body temperature increase
REFERENCE :
DRSAEA Drug Safety. (Adis International Ltd., Private Bag 65901, Mairangi
Bay, Auckland 10, New Zealand) V.5- 1990- Volume(issue)/page/year:
7,387,1992
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - child
DOSE/DURATION : 500 ug/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity)
REFERENCE :
DRSAEA Drug Safety. (Adis International Ltd., Private Bag 65901, Mairangi
Bay, Auckland 10, New Zealand) V.5- 1990- Volume(issue)/page/year:
7,387,1992
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - child
DOSE/DURATION : 500 ug/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - effect, not otherwise specified
Cardiac - pulse rate increase, without fall in BP
Lungs, Thorax, or Respiration - respiratory stimulation
REFERENCE :
DRSAEA Drug Safety. (Adis International Ltd., Private Bag 65901, Mairangi
Bay, Auckland 10, New Zealand) V.5- 1990- Volume(issue)/page/year:
7,387,1992
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - child
DOSE/DURATION : 1 mg/kg
TOXIC EFFECTS :
Lungs, Thorax, or Respiration - cyanosis
REFERENCE :
DRSAEA Drug Safety. (Adis International Ltd., Private Bag 65901, Mairangi
Bay, Auckland 10, New Zealand) V.5- 1990- Volume(issue)/page/year:
7,387,1992
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 360 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity)
Behavioral - convulsions or effect on seizure threshold
Lungs, Thorax, or Respiration - respiratory depression
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: 13,4069,1979
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 370 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - chromodacryorrhea
Behavioral - ataxia
Lungs, Thorax, or Respiration - dyspnea
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: 13,4069,1979
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 5100 ug/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis
Behavioral - ataxia
Lungs, Thorax, or Respiration - dyspnea
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: 13,4069,1979
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 585 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex)
Behavioral - convulsions or effect on seizure threshold
Behavioral - ataxia
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: 13,4069,1979
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 820 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
Behavioral - ataxia
Blood - changes in spleen
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: 13,4069,1979
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 18800 ug/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
Lungs, Thorax, or Respiration - dyspnea
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: 13,4069,1979
** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 4500 mg/kg/5W-I
TOXIC EFFECTS :
Liver - other changes
Biochemical - Enzyme inhibition, induction, or change in blood or tissue
levels - phosphatases
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: 13,4069,1979
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 4680 mg/kg/26W-I
TOXIC EFFECTS :
Liver - other changes
Biochemical - Enzyme inhibition, induction, or change in blood or tissue
levels - phosphatases
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: 13,4069,1979
*** END OF RECORD ***