Ketotifen (Fumarate)
Ketotifen (Fumarate) is potent antihistaminic agent which exhibit strong H1 receptor blocking activity. Ketotifen (Fumarate) is prepared synthetically. Ketotifen (Fumarate) is effective in the preventive management for asthma and in the treatment of allergic conditions such as rhinitis and conjunctivitis. Ketotifen (Fumarate) is administered orally.
Primary Characteristics
It is of Synthetic origin and belongs to Piperidylbenzocycloheptane.
It belongs to H1-antagonist pharmacological group on the basis of mechanism of action and also classified in Antihistamine, H1 Blocker, Opthalmic pharmacological group.
Molecular Weight: 425.5 · pKa: 8.43 · Solubility in Water: sparingaly soluble · Solubility in Alcohol: soluble · Non-proprietary name: Ketotifen (Fumarate).
Pharmacokinetics
Absorption: Ketotifen (Fumarate) has an oral bioavailability is 50%.
Distribution: Ketotifen (Fumarate) has a plasma protein binding is >75%.
Elimination: it is metabolised via Hepatic (extensively), plasma half-life is 21 hr, renal excretion is 40%.
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Indications
Ketotifen (Fumarate) is primarily indicated in conditions like Allergic conjunctivitis, Allergic rhinitis, Prophylaxis of asthma.
Ketotifen (Fumarate) is also indicated for secondary conditions like Dysfunctional uterine bleeding, menorrhagia.
Contraindications
Ketotifen (Fumarate) is contraindicated in conditions like Impaired alertness, Hypersensitivity.
Dosage
Ketotifen (Fumarate)'s dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 0.025 % | 0.025 % | Every 12h | Opthalmic | With food. |
| 1.5 mg | 1.5 mg | Every 12h | PO | |
| Paediatric Dosage (20kg) | ||||
| 0.025 % | 0.025 % | — | Opthalmic | From 3 year of age. |
| 500 ug | 500 ug | Every 12h | Oral | Recommended in Paeds over 2 Years of Age |
| Neonatal Dosage (3kg) | ||||
| 0 – 0 | — | — | Not recommended in this age group | |
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
The signs and symptoms that are produced after acute overdosage of Ketotifen (Fumarate) are Bradycardia, Tachycardia , Convulsions , Drowsiness, Drowsiness, Confusion , Hyperactive reflexes, Cyanosis, Hyperexcitability , Dyspnea.
Ketotifen (Fumarate) is known to cause more or less tolerable side effects which are usually transient. These include Dizziness, Drowsiness, Dry mouth, Lethargy, Weight gain.
Warnings / Precautions
Interference in Pathology
Ketotifen (Fumarate) may interfere in the diagnosis of Elevated liver enzymes.
Available Brands
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Single Ingredient
Storage Conditions
Drug Classification
- 1.25.1.1 — Oral/Parenteral antiasthmatics