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Ketotifen- first-generation noncompetitive H1-antihistamine and mast cell stabilizer.

Ketotifen is a first-generation noncompetitive H1-antihistamine and mast cell stabilizer. It is most commonly sold as a salt with fumaric acid More

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Description

Ketotifen is a first-generation noncompetitive H1-antihistamine and mast cell stabilizer. It is most commonly sold as a salt with fumaric acid

Generic Name

Ketotifen- first-generation noncompetitive H1-antihistamine and mast cell stabilizer.

Chemical names

Ketotifen; Ketotifene; Zaditor; Ketotifeno

Brand names

Albalon, Airyfen, Asthafen, Azofen, Azofen-T, Ketasma, Ketorid, Ketotif, Ketovent, Mastifen, Mastifen-C, Mastifen-S, Privent, Privent DPS, Tritofen, Zaditen, Zerosma, Zetiffen.

IUPAC name

2-(1-methylpiperidin-4-ylidene)-6-thiatricyclo[8.4.0.0³,?]tetradeca-1(14),3(7),4,10,12-pentaen-8-one

Pharmacokinetics

Actions

Ketotifen is a fast acting non-competitive histamine antagonist. It inhibits the mediators release from mast cells. It is a non-bronchodilator antiasthmatic drug (when taken orally).

Dosage/Dosage form

  • 0.025% solution for allergic conjunctivitis.
  • 1 mg twice daily for asthma as oral.

Therapeutic uses

Antihistamine prescribed for asthma, allergic conjunctivitis and other allergic reactions.

Adverse effects/Side effects

  • GI ulcer, drowsiness, bleeding and perforation, rash, hypotension, bronchospasm, psychosis, dry mouth, fever, bradycardia, chest pain, dizziness, headache, sweating, oedema, pallor, liver function changes.
  •  Anaphylaxis.
  • MI, stroke, GI bleeding.
  • Severe skin reactions.
  • Transient stinging and local irritation (ophthalmic).

Interaction

  • May reduce effects of antihypertensives (e.g. ACE inhibitors or angiotensin II receptor antagonists).
  • Increased adverse effects with aspirin or other NSAIDs.
  • Increased risk of renal toxicity with ACE inhibitors, diuretics.
  • Hallucinations may occur when used with fluoxetine, thiothixene, alprazolam.
  • May increase toxicity of methotrexate and lithium.
  • Increased risk of GI bleeding with warfarin.
  • Increased plasma concentrations with probenecid.

Contraindications

Hypersensitivity to aspirin or other NSAIDs, asthma. Hypovolaemia or dehydration. Do not give postoperatively to patients with high risk of haemorrhage. History of peptic ulcer or coagulation disorders. Nasal polyps, angioedema, bronchospasm. Labour. Moderate to severe renal impairment. GI bleeding, cerebrovascular bleeding. As prophylactic analgesic before surgery. Pregnancy, lactation.

Storage

Store at 15-25°C

Information

Molecular weight

309.425

Molecular formula

C19H19NOS

CAS number

34580-13-7

Precautions

  • Monitor renal function closely.
  • Elderly, patients weighing <50 kg, hepatic dysfunction, heart failure, predisposition to reduced blood volume or renal blood flow.