ACUVUE THERAVISION WITH KETOTIFEN
Clinical safety rating: safe
CNS depressants may enhance sedative effects For ophthalmic use only may cause transient stinging.
Ketotifen is a selective histamine H1-receptor antagonist and mast cell stabilizer that inhibits the release of inflammatory mediators such as histamine and leukotrienes from mast cells.
| Metabolism | Not significantly metabolized in the eye; systemic absorption is minimal. After systemic absorption, it is metabolized primarily via glucuronidation and oxidation, with a half-life of approximately 12 hours. |
| Excretion | Renal (approximately 50% as unchanged drug, 30% as metabolites); biliary/fecal elimination accounts for <10%. |
| Half-life | 12 hours (terminal elimination half-life; clinical context: twice-daily dosing needed for continuous effect). |
| Protein binding | 99% (primarily albumin and alpha-1-acid glycoprotein). |
| Volume of Distribution | 2.4 L/kg (high tissue distribution, including ocular tissues). |
| Bioavailability | Ocular topical: ~0.1% systemic; oral: 70% (not relevant for contact lens application). |
| Onset of Action | Ocular: within 5 minutes after instillation (peak effect at 15 minutes). |
| Duration of Action | Up to 8 hours (symptom relief from ocular itching with twice-daily dosing). |
| Molecular Weight | 309.4 |
| Action Class | Antihistamine / Mast Cell Stabilizer |
One drop in each affected eye twice daily (approximately 8 hours apart) as needed. The lens should be removed prior to instillation and can be reinserted after at least 10 minutes.
| Dosage form | DRUG-ELUTING CONTACT LENS |
| Renal impairment | No dosage adjustment required based on renal function; systemic absorption is minimal. |
| Liver impairment | No dosage adjustment required based on hepatic function; systemic absorption is minimal. |
| Pediatric use | Safety and efficacy in pediatric patients below 3 years of age have not been established. For children 3 years and older, administer one drop in each affected eye twice daily. |
| Geriatric use | No specific dosage adjustment is required for elderly patients; use same dosing as for adults. |
| 1st trimester | Limited data; systemic absorption from ophthalmic use is minimal (<10 ng/mL). No known risk in T1 based on animal studies. |
| 2nd trimester | Minimal systemic absorption; unlikely to pose risk. No known adverse effects. |
| 3rd trimester | Minimal systemic absorption; unlikely to pose risk near term. |
Clinical note
CNS depressants may enhance sedative effects For ophthalmic use only may cause transient stinging.
| FDA category | Animal |
| Placental transfer | Not studied; due to low systemic bioavailability (<10 ng/mL) from ophthalmic use, significant placental transfer is unlikely. |
| Breastfeeding |
■ FDA Black Box Warning
None
| Common Effects | Drowsiness |
| Serious Effects | Hypersensitivity reactions (e.g., angioedema, urticaria, rash), Ocular irritation or burning on instillation, Corneal abrasion or epithelial defect (rare), Increased intraocular pressure (rare) |
Hypersensitivity to ketotifen or any component of the product
| Precautions | For topical ophthalmic use only; not for injection., Contains benzalkonium chloride; soft contact lens wearers should remove lenses before application and wait at least 10 minutes before reinserting., May cause transient stinging or burning upon instillation., Use with caution in patients with known hypersensitivity to any component. |
| Food/Dietary | None reported. |
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| Systemic absorption is negligible; not expected to cause adverse effects in breastfed infants. Use caution if eyes or nasolacrimal system are inflamed. |
| Lactation Rating | L1: Safe |
| Teratogenic Risk | Ketotifen ophthalmic solution has minimal systemic absorption (approximately 0.1% of administered dose). No adequate well-controlled studies in pregnant women. Animal studies showed no teratogenicity at doses up to 50 mg/kg/day orally. Risk to fetus is considered low when used topically as directed. |
| Fetal Monitoring | No specific monitoring required beyond routine prenatal care due to minimal systemic exposure. |
| Fertility Effects | No known adverse effects on fertility from ophthalmic ketotifen based on limited systemic absorption. |
| Clinical Pearls | Ketotifen is a mast cell stabilizer and antihistamine; contact lens must be removed before instillation and may be reinserted after 10 minutes. Do not use while wearing contact lenses. Advise patient to wait at least 5 minutes between different eye drops. The preservative benzalkonium chloride may be absorbed by soft contact lenses. |
| Patient Advice | Remove contact lenses before using the drops and wait at least 10 minutes before reinserting. · Wash hands before use. Do not touch the dropper tip to any surface, including the eye. · Do not use if the solution changes color or becomes cloudy. · Use exactly as prescribed; do not use more often than directed. · If you miss a dose, use it as soon as possible. If it is almost time for the next dose, skip the missed dose and resume your regular schedule. Do not double the dose. · Contact your doctor if you experience eye pain, vision changes, or if symptoms persist or worsen. |