Ketotifen fumarate

Modify Date: 2024-01-02 12:24:40

Ketotifen fumarate Structure
Ketotifen fumarate structure
Common Name Ketotifen fumarate
CAS Number 34580-14-8 Molecular Weight 425.497
Density 0.968 g/mL at 25 °C(lit.) Boiling Point 250-263 °C(lit.)
Molecular Formula C23H23NO5S Melting Point -43°C
MSDS Chinese USA Flash Point 96-98°C/5mm
Symbol GHS07
GHS07
Signal Word Warning

 Use of Ketotifen fumarate


Ketotifen (fumarate) is a second-generation noncompetitive H1-antihistamine and mast cell stabilizer, which is used to prevent asthma attacks.Target: Histamine Receptor Ketotifen is a second-generation noncompetitive H1-antihistamine and mast cell stabilizer. It is most commonly sold as a salt of fumaric acid,ketotifen fumarate, and is available in two forms. In its ophthalmic form, it is used to treat allergic conjunctivitis, or the itchy red eyes caused by allergies. In its oral form, it is used to prevent asthma attacks. Side effects include drowsiness, weight gain, dry mouth, irritability, and increased nosebleeds.Ketotifen relieves and prevents eye itchiness and/or irritation associated with most seasonal allergies. It starts working within minutes after administering the drops. The drug has not been studied in children under three. The mean elimination half life is 12 hours. Besides its anti-histaminic activity, it is also a functional leukotriene antagonist and a phosphodiesterase inhibitor. The drug may also help relieve the symptoms of Irritable bowel syndrome.

 Names

Name (E)-but-2-enedioic acid,10-(1-methylpiperidin-4-ylidene)-5H-benzo[1,2]cyclohepta[3,4-b]thiophen-4-one
Synonym More Synonyms

 Ketotifen fumarate Biological Activity

Description Ketotifen (fumarate) is a second-generation noncompetitive H1-antihistamine and mast cell stabilizer, which is used to prevent asthma attacks.Target: Histamine Receptor Ketotifen is a second-generation noncompetitive H1-antihistamine and mast cell stabilizer. It is most commonly sold as a salt of fumaric acid,ketotifen fumarate, and is available in two forms. In its ophthalmic form, it is used to treat allergic conjunctivitis, or the itchy red eyes caused by allergies. In its oral form, it is used to prevent asthma attacks. Side effects include drowsiness, weight gain, dry mouth, irritability, and increased nosebleeds.Ketotifen relieves and prevents eye itchiness and/or irritation associated with most seasonal allergies. It starts working within minutes after administering the drops. The drug has not been studied in children under three. The mean elimination half life is 12 hours. Besides its anti-histaminic activity, it is also a functional leukotriene antagonist and a phosphodiesterase inhibitor. The drug may also help relieve the symptoms of Irritable bowel syndrome.
Related Catalog
References

[1]. Klooker TK, et al. The mast cell stabiliser ketotifen decreases visceral hypersensitivity and improves intestinal symptoms in patients with irritable bowel syndrome. Gut. 2010 Sep;59(9):1213-21.

 Chemical & Physical Properties

Density 0.968 g/mL at 25 °C(lit.)
Boiling Point 250-263 °C(lit.)
Melting Point -43°C
Molecular Formula C23H23NO5S
Molecular Weight 425.497
Flash Point 96-98°C/5mm
Exact Mass 425.129700
PSA 123.15000
LogP 3.66410
Index of Refraction n20/D 1.522(lit.)
Storage condition Store at RT

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
DE8260000
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

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

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
Precautionary Statements P301 + P312 + P330
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Faceshields;Gloves
Hazard Codes Xn:Harmful
Risk Phrases R22
Safety Phrases S36
RIDADR NONH for all modes of transport
WGK Germany 3
RTECS DE8260000
HS Code 2934999090

 Customs

HS Code 2934999090
Summary 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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 Synonyms

Ketotifen hydrogen fumarate
Zaditor
4-(1-methylpiperidin-4-ylidene)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one (2E)-but-2-enedioate
acide (2E)-but-2-ènedioïque - 4-(1-méthylpipéridin-4-ylidène)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophén-10-one (1:1)
Ketotifen fumarate
4-(1-Methylpiperidin-4-ylidene)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one (2E)-but-2-enedioate (1:1)
UNII:HBD503WORO
Ketotifen fumarate salt
Alaway
10H-Benzo[4,5]cyclohepta[1,2-b]thiophen-10-one, 4,9-dihydro-4-(1-methyl-4-piperidinylidene)-, (2E)-2-butenedioate (1:1)
(2E)-But-2-endisäure--4-(1-methylpiperidin-4-yliden)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-on(1:1)
Zaditen
UNII-HBD503WORO
MFCD00079394
4-(1-Methyl-4-piperidinylidene)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one (2E)-2-butenedioate (1:1)
EINECS 252-100-0
Ketotifen (fumarate)
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