Ketotifen hydrogen fumarate is a chemical compound, a type of drug used to treat asthma and allergies.

Take only under medical supervision

The name describes the structure of the molecule:

• "Ketotifen" is a type of medication known as a mast cell stabilizer, which works by blocking the release of certain chemical messengers that cause symptoms of asthma and allergies.
• "Hydrogen fumarate" indicates that the ketotifen is in the form of a salt with fumaric acid. This is a common form of the drug because it is stable and easy to manufacture and store.

The synthesis process takes place in different steps:

• The first step involves the reaction of 4-chloroquinoline with sodium azide to produce 4-azidoquinoline.
• The 4-azidoquinoline is then reacted with ethyl propiolate in the presence of a base to produce a compound known as a cycloaddition product.
• This cycloaddition product is then reacted with hydrochloric acid to produce ketotifen.
• Finally, the ketotifen is reacted with fumaric acid to produce ketotifen hydrogen fumarate.

Studies

Ketotifen hydrogen fumarate is able to inhibit the release of histamine, other basophil and mast cell relays. It causes a long-lasting inhibition of histamine reactions. It is effective in the treatment of allergic diseases and asthma. It is used to prevent asthma attacks caused by allergy, but also acts as an anti-anaphylactic (1).

Ketotifene hydrogen fumarate has shown some characteristics of a serotoninolytic (2), inhibits the release of mediators from cells involved in hypersensitivity reactions. decreases chemotaxis and eosinophil activation (3).

Like all drugs it can cause side effects. Always ask the physician.

References_____________________________________________________________________

(1) Wyszomirska E, Czerwińska K, Kublin E, Mazurek AP. Identification and determination of ketotifen hydrogen fumarate, azelastine hydrochloride, dimetindene maleate and promethazine hydrochloride by densitometric method. Acta Pol Pharm. 2013 Nov-Dec;70(6):951-9. 

Abstract. Conditions for determination of: ketotifen hydrogen fumarate, azelastine hydrochloride, dimetindene maleate and promethazine hydrochloride by densitometric method in substances and pharmaceuticals were provided. Maximum wavelenghts were: 228 nm for ketotifen hydrogen fumarate, 295 nm for azelastine hydrochloride, 265 nm for dimetindene maleate and 255 nm for promethazine hydrochloride. The limits of quantification were in the ranges of 0.2-5 microg/spot. The statistical data showed adequate accuracy and precision of developed methods.

(2) Rogóz Z, Skuza G, Sowińska H. Central action of ketotifen. Pol J Pharmacol Pharm. 1981;33(5):503-15. 

Abstract. Ketotifen (4-/1-methyl-4-piperidylidene/-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-10(9H)-one hydrogen fumarate) inhibited spontaneous locomotor activity and amphetamine hypermotility in mice and rats, as well as L-DOPA-induced motor stimulation in mice. It produced in mice a slight hypothermia and did not prevent reserpine-induced hypothermia; thus, it does not posses properties or tricyclic antidepressants. Ketotifen showed some features of serotoninolytic: it inhibited the head twitch response to 5-hydroxytryptophan in mice, depressed tryptamine-induced clonic convulsions in rats, antagonized fenfluramine-induced hyperthermia in rats at high ambient temperature and showed weak antiserotonin action in the flexor reflex preparation. Ketotifen did not affect spiperone- or reserpine-induced catalepsy and showed no cholinolytic activity. LD50 of ketotifen (after 24 h) was 122.5 mg/kg ip in mice and 62.6 mg/kg ip in rats.

(3) Ghoreishi, S. M., Behpour, M., Zahrani, H. A., & Golestaneh, M. (2010). Preparation and optimization of a ketotifen sensor and its pharmaceutical applications. Anal. Bioanal. Electrochem, 2(3), 112-124.

Abstract. Ketotifen hydrogen fumarate (KET-C4H4O4) [4-(1-Methyl-4-piperidylidene)-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-10(9H)-one hydrogen fumarate] is a relatively selective, non competitive histamine antagonist (H1-receptore) and mast cell stabilizer. Ketotifen inhibits the release of mediators from cells involved in hypersensitivity reactions. Decrease chemotaxis and activation of eosinophils has also been demonstrated...