Ketotifen; Uses, Dosage, Side Effects, Drug Interactions

Ketotifen; Uses, Dosage, Side Effects, Drug Interactions

Ketotifen is a cycloheptathiophene derivative with anti-allergic activity. Ketotifen selectively blocks histamine (H1) receptors and prevents the typical symptoms caused by histamine release. This agent also interferes with the release of inflammatory mediators from mast cells involved in hypersensitivity reactions, thereby decreasing chemotaxis and activation of eosinophils. Ketotifen is a cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators. It has been proposed for the treatment of asthma, rhinitis, skin allergies, and anaphylaxis.

Ketotifen is a first-generation noncompetitive H1-antihistamine and mast cell stabilizer. It is most commonly sold as a salt with a fumaric acid, ketotifen fumarate, and is available in two forms. In its ophthalmic form, it is used to treat allergic conjunctivitis. In its oral form, it is used to prevent asthma attacks or Anaphylaxis, as well as various mast cell, allergic-type disorders cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators. It has been proposed for the treatment of asthma, rhinitis, skin allergies, and anaphylaxis.

Mechanism of action  of Ketotifen

Ketotifen is a relatively selective, non-competitive histamine antagonist (H1-receptor) and mast cell stabilizer. Ketotifen inhibits the release of mediators from mast cells involved in hypersensitivity reactions. Decreased chemotaxis and activation of eosinophils have also been demonstrated. Ketotifen also inhibits cAMP phosphodiesterase. Properties of ketotifen which may contribute to its antiallergic activity and its ability to affect the underlying pathology of asthma include inhibition of the development of airway hyperactivity associated with activation of platelets by PAF (Platelet Activating Factor), inhibition of PAF-induced accumulation of eosinophils and platelets in the airways, suppression of the priming of eosinophils by human recombinant cytokines and antagonism of bronchoconstriction due to leukotrienes. Ketotifen inhibits of the release of allergic mediators such as histamine, leukotrienes C4 and D4(SRS-A) and PAF.

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Indications of Ketotifen

Contra-Indications of Ketotifen

  • No Disease Contraindications
Allergies
  • Ketotifen
  • Antihistamines
  • Antihistamines – Piperidine
  • Mast Cell Stabilizer

Dosage of Ketotifen

Allergic Conjunctivitis

  • Instill 1 drop in the affected eye(s) 2 times a day

Allergic Conjunctivitis

  • Age: 3 years and older
  • Instill 1 drop in the affected eye(s) 2 times a day

Side Effects of Ketotifen

The most common

Opthalmic 

More common

Less common

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Drug Interactions

Tell your doctor of all nonprescription and prescription medication you may use, especially of: oral drugs used for diabetes. Also report drugs that may cause drowsiness such as sleeping pills, anti-anxiety drugs, psychiatric medicines, certain antihistamines (e.g., diphenhydramine), muscle relaxants, narcotic pain relievers (e.g., codeine), anti-seizure drugs. Certain cough-and-cold preparations may also make you drowsy. Consult your pharmacist. Do not start or stop any medicine without doctor or pharmacist approval.

  • benzphetamine
  • brompheniramine
  • buprenorphine
  • buprenorphine buccal
  • butabarbital
  • butalbital
  • butorphanol
  • caffeine
  • carbinoxamine
  • carisoprodol
  • chloral hydrate
  • chlordiazepoxide
  • chlorpheniramine
  • chlorpromazine
  • chlorpropamide
  • chlorzoxazone
  • cinnarizine
  • clemastine
  • clomethiazole

Pregnancy and Lactation

FDA Pregnancy Category  C

Pregnancy

Ketotifen should not be used by anyone who is pregnant or breastfeeding.

Lactation

Ketotifen should not be used by anyone who is pregnant or breastfeeding. Pregnancy

References

Ketotifen

 

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