Ketotifen fumarate

Synonym(s):Ketotifen fumarate salt

CAS NO.：34580-14-8
Empirical Formula: C23H23NO5S
Molecular Weight: 425.5
MDL number: MFCD00079394
EINECS: 252-100-0
SAFETY DATA SHEET (SDS)
Update Date: 2024-11-08 20:21:46

What is Ketotifen fumarate ?

Description

Ketotifen is a histamine H₁ receptor antagonist (K_i = 1.3 nM) and mast cell stabilizer. It is selective for H₁ receptors over H₂ and H₃ receptors (K_is = 987 and 2,500 nM, respectively). Ketotifen (50 and 100 μM) inhibits degranulation of rat peritoneal mast cells induced by compound 48/80 . It inhibits the passive cutaneous anaphylaxis (PCA) reaction in rats by 54.6% when administered orally at a dose of 20 mg/kg. Ketotifen (30 mg/kg) inhibits the quick phase airway response in a rat ovalbumin-induced immediate airway response model. Formulations containing ketotifen have been used in the treatment of itching associated with allergic conjunctivitis.

Chemical properties

Off-White Solid

The Uses of Ketotifen fumarate

vasodilator

The Uses of Ketotifen fumarate

Ketotifen fumarate salt has been used: for mast cell product antagonism, as a positive control in β-hexosaminidase release assay, as mast cell stabilizer to treat pregnant dams added to ad libitum drinking water

The Uses of Ketotifen fumarate

Antiasthmatic; antiallergic.

The Uses of Ketotifen fumarate

Ketotifen, C19H19NOS, is also a piperidine derivative; like oxatomide, it has mast cell stabilizing actions besides its antihistamine properties.

brand name

Zaditor (Novartis).

General Description

Ketotifen fumarate, 4-(1-methyl-4-piperidylidene)-4Hbenzo[4,5]cyclohepta[1,2-b]thiophen-10(9H)-one hydrogenfumarate (Zaditor), is a fine crystalline powder.Ketotifen is a ketothiophene isostere analog of the dibenzocycloheptaneantihistamines. The solution contains0.345 mg of ketotifen fumarate, which is equivalent to0.25 mg of ketotifen. The solution also contains the preservativebenzalkonium chloride (0.01%) as well as glycerol,sodium hydroxide and/or hydrochloric acid (to adjust pH),and purified water. It has a pH of 4.4 to 5.8 and an osmolalityof 210 to 300 mOsm/kg.
The recommended dose of ketotifen solution is 1 drop instilledinto each affected eye every 8 to 12 hours. The mostfrequently reported adverse reactions are conjunctival infection,headaches, and rhinitis. This drug product is for ocularadministration only and not for injection or oral use.Ketotifen solution should be used with caution during pregnancyor while nursing, because its safety has not been studiedunder these circumstances.

Biological Activity

An H 1 receptor antagonist.

storage

Store at RT

Properties of Ketotifen fumarate

Melting point:	192 C
storage temp.	2-8°C
solubility	Sparingly soluble in water, slightly soluble in methanol, very slightly soluble in acetonitrile.
form	neat
form	Solid
color	White to Pale Beige
PH	pH (10g/l, 25℃) : 3.0～4.0
Water Solubility	Soluble in water (10 mg/ml), DMSO (100 mM), and methanol.
λmax	297nm(MeOH)(lit.)
Merck	14,5307
CAS DataBase Reference	34580-14-8(CAS DataBase Reference)

Safety information for Ketotifen fumarate

Signal word	Warning
Pictogram(s)	Exclamation Mark Irritant GHS07
GHS Hazard Statements	H302:Acute toxicity,oral H319:Serious eye damage/eye irritation
Precautionary Statement Codes	P264:Wash hands thoroughly after handling. P264:Wash skin thouroughly after handling. P270:Do not eat, drink or smoke when using this product. P280:Wear protective gloves/protective clothing/eye protection/face protection. P301+P312:IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. P337+P313:IF eye irritation persists: Get medical advice/attention.