Pemirolast
Class: Antiallergic Agents
VA Class: OP300
Chemical Name: 9-Methyl-3-(1H-tetrazol-5-yl)-4H-pyrido[1,2a]pyrimidin-4-one potassium salt
Molecular Formula: C10H7KN6O
CAS Number: 100299-08-9
Brands: Alamast
Introduction
Mast-cell stabilizer.
Uses for Pemirolast
Allergic Conjunctivitis
Prevention of ocular itching associated with allergic conjunctivitis.
Pemirolast Dosage and Administration
Administration
Ophthalmic Administration
Apply topically to the eye as an ophthalmic solution. Not for injection or oral use.
Avoid contamination of the solution container.
Dosage
Available as pemirolast potassium; dosage expressed in terms of the salt.
Initiate therapy before and continue throughout pollen season.
Pediatric Patients
Allergic Conjunctivitis
Ophthalmic
Children ≥3 years of age: 1 or 2 drops of a 0.1% solution in the affected eye(s) 4 times daily.
Symptomatic response (i.e., decreased itching) may be evident within a few days following initiation but frequently requires up to 4 weeks of therapy.
Adults
Allergic Conjunctivitis
Ophthalmic
1 or 2 drops of a 0.1% solution in the affected eye(s) 4 times daily.
Symptomatic response (i.e., decreased itching) may be evident within a few days following initiation but frequently requires up to 4 weeks of therapy.
Cautions for Pemirolast
Contraindications
Known hypersensitivity to pemirolast or any ingredient in the formulation.
Warnings/Precautions
Specific Populations
Pregnancy
Category C.
Lactation
Distributed into milk in rats; not known whether distributed into human milk. Caution if used in nursing women.
Pediatric Use
Safety and efficacy not established in children <3 years of age.
Common Adverse Effects
Headache, rhinitis, cold/flu symptoms.
Interactions for Pemirolast
No formal drug interaction studies to date.
Pemirolast Pharmacokinetics
Absorption
Bioavailability
Following topical application to both eyes (0.1% solution 4 times daily for 2 weeks), peak plasma concentrations were attained within about 25 minutes, but were substantially lower than those following a single (10 mg) oral dose.
Elimination
Elimination Route
10–15% of topi...