Each ml contains: Active ingredient: Ketotifen fumarate 0.345 mg, corresponding to 0.25 mg of ketotifen.
Excipients/Inactive Ingredients: Glycerol 21.25 mg, sodium hydroxide 1 N q.s., water for injections to 1 ml.
Zaditen: Preservative: Benzalkonium chloride 0.1 mg.
Zaditen SDU: Preservative free.
Pharmacology: Pharmacodynamics: Ketotifen is a histamine H1-receptor antagonist. Ketotifen also inhibits the release of mediators (e.g. histamine, leukotrienes, prostaglandins, PAF) from cells involved in type 1, or immediate allergic reactions (mast cells, eosinophils, basophils and neutrophils). Ketotifen also reduces chemotaxis, activation and degranulation of eosinophils. cAMP levels increased by phosphodiesterase inhibition can contribute to the cell-stabilising effect of ketotifen.
The antihistamine effect of Zaditen/Zaditen SDU eye drops has a rapid onset following instillation into the eye and persists for 8-12 hours.
Zaditen/Zaditen SDU eye drops alleviate the symptoms of allergic conjunctivitis, such as pruritus and hyperaemia.
Pharmacokinetics: In a pharmacokinetics study conducted in 18 healthy volunteers with Zaditen/Zaditen SDU eye drops plasma levels of ketotifen after repeated ocular administration for 14 days were in most cases below the limit of quantitation (20 pg/ml).
After oral administration, ketotifen is eliminated biphasically with an initial half-life of 3 to 5 hours and a terminal half-life of 21 hours. About 1% of the substance is excreted unchanged in the urine within 48 hours and 60 to 70% as metabolites. The main metabolite is the practically inactive ketotifen N-glucuronide.
Treatment of signs and symptoms of allergic conjunctivitis.
Adults, elderly and children (age 3 and older): Instill 1 drop twice a day into the conjunctival sac.
To avoid contamination of the solution do not allow the tip of the bottle to touch any surface.
Zaditen SDU: The contents of a single dose unit are sufficient for one administration into both eyes.
To date, there have been no reports of overdoses with Zaditen/Zaditen SDU eye drops.
One 5 ml bottle contains 1.25 mg ketotifen (≅ 1.725 mg ketotifen fumarate). Drinking one whole bottle would result in the ingestion of 60% of the recommended daily dose for a 3-year-old child.
Hypersensitivity to ketotifen or to any of the excipients.
Effects on ability to drive and use machines: Any patient who experiences blurred vision or somnolence should not drive or operate machines.
Zaditen: Zaditen eye drops in bottles of 5 ml contain benzalkonium chloride as preservative, contact lenses must be taken out before applying Zaditen eye drops solution and not replaced for at least 15 minutes.
For Zaditen/Zaditen SDU eye drops, no clinical data on use during pregnancy are available. Oral animal studies using maternally toxic doses showed increased pre and postnatal mortality, but no teratogenicity. Systemic levels of ketotifen after ocular use are generally below the limit of quantitation. Caution should be exercised when prescribing to pregnant women.
Although animal data following oral administration show excretion into breast milk, topical administration to human is unlikely to produce detectable quantities in breast milk. Nursing mothers receiving Zaditen/Zaditen SDU eye drops can breastfeed.
At the recommended dose, the following undesirable effects have been reported: Ocular side effects:
Between 1% and 2%: Burning/stinging, punctate corneal epithelial erosion.
<1%: Blurring of vision upon drug instillation, dry eyes, eyelid disorder, conjunctivitis, eye pain, photophobia, subconjunctival haemorrhage.
Systemic side effects:
<1%: Headache, somnolence, skin rash, eczema, urticaria, dry mouth and allergic reaction.
If several medicines are to be administered into the eye, there should be an interval of at least 5 minutes between each application.
Incompatibilities: None known to date.
Zaditen: Close the bottle immediately after use.
Zaditen SDU: For single use only.
Discard the Zaditen SDU container immediately after use. Do not save unused contents.
Store below 25°C.
Zaditen: May be used up to 1 month after first opening.
Zaditen SDU: Discard one month after first opening of the pouch.
After opening of the single dose unit container: Use immediately.
S01GX08 - ketotifen ; Belongs to the class of other ophthalmologic antiallergics.
Zaditen: Eye drops 0.025% x 5 mL.
Zaditen SDU: Ophth eye drops 0.25 mg/mL x 0.4 mL x 10's.