ALAMAST
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ALAMAST (ALAMAST).
Mast cell stabilizer; inhibits release of histamine and other inflammatory mediators from mast cells.
| Metabolism | Primarily excreted unchanged in urine; minimal hepatic metabolism. |
| Excretion | Primarily renal excretion of unchanged drug (approximately 70-80% of dose); biliary/fecal elimination accounts for the remainder (20-30%). |
| Half-life | Terminal elimination half-life is 12-15 hours in healthy adults; steady-state achieved within 2-3 days; prolonged in renal impairment. |
| Protein binding | Approximately 85-90% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Mean Vd is approximately 1.0-1.5 L/kg, indicating extensive distribution into tissues. |
| Bioavailability | Intranasal: systemic bioavailability is low (approximately 5-10%) due to local administration and first-pass metabolism; oral bioavailability is <1%. |
| Onset of Action | Intranasal: clinical effects (sneezing, rhinorrhea) begin within 1-2 hours; maximal effect after 3-5 days of regular use. |
| Duration of Action | Duration of action is approximately 12 hours; twice-daily dosing maintains therapeutic effect. |
1 or 2 drops (0.025% or 0.05% solution) in each affected eye four times daily.
| Dosage form | SOLUTION/DROPS |
| Renal impairment | No dosage adjustment required for systemic absorption is negligible. |
| Liver impairment | No dosage adjustment required for systemic absorption is negligible. |
| Pediatric use | Safety and efficacy in pediatric patients below 3 years of age have not been established; for children 3 years and older, same as adult dose. |
| Geriatric use | No specific geriatric dose adjustment; use same dosing as adults. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ALAMAST (ALAMAST).
| Breastfeeding | It is unknown whether pemirolast is excreted in human milk. No M/P ratio available. Because many drugs are excreted in human milk, caution should be exercised when ALAMAST is administered to a nursing woman. |
| Teratogenic Risk | Pregnancy Category C. No adequate well-controlled studies in pregnant women. In animal studies, pemirolast (the active ingredient) administered intravenously at doses up to 100 mg/kg/day (approximately 200 times the maximum recommended human ocular dose) during organogenesis produced maternal toxicity and increased fetal resorptions in rabbits. No teratogenic effects were observed in rats or rabbits. Risk cannot be ruled out; use only if potential benefit justifies potential risk to the fetus. |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to cromolyn sodium or any component.
| Precautions | Not for acute bronchospasm; caution in hepatic impairment; rare hypersensitivity reactions. |
| Food/Dietary | No significant food interactions. Avoid rubbing eyes after instillation to prevent drug loss and irritation. |
| Clinical Pearls | ALAMAST (pemirolast potassium) is a mast cell stabilizer indicated for allergic conjunctivitis. Administer as one drop in each affected eye four times daily. Shake well before use. Effectiveness may take several weeks. Do not wear contact lenses during treatment if eyes are red. May be used with other ophthalmic medications separated by at least 5 minutes. |
Loading safety data…
| Fetal Monitoring | No specific routine monitoring recommended. General pregnancy monitoring per standard obstetric care. Monitor for maternal hypersensitivity reactions, which could affect pregnancy outcomes. |
| Fertility Effects | No human data on fertility effects. In animal studies, no impairment of fertility was observed in rats at intravenous doses up to 100 mg/kg/day (approximately 200 times the maximum recommended human ocular dose). |
| Patient Advice | Do not touch the dropper tip to any surface to avoid contamination. · Remove contact lenses before instillation and wait at least 10 minutes before reinserting. · Do not use while wearing contact lenses if eyes are red. · Shake the bottle well before each use. · Use exactly as prescribed; do not skip doses. · Report any worsening of symptoms or signs of infection (e.g., eye pain, discharge). · Store at room temperature, away from light and moisture. |