EMADINE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for EMADINE (EMADINE).
Emedastine is a selective histamine H1 receptor antagonist that inhibits histamine-induced vascular permeability, edema, and pruritus.
| Metabolism | Hepatic via CYP450 enzymes, primarily CYP3A4 and CYP2D6 |
| Excretion | Renal: approximately 60% as unchanged drug and metabolites; fecal: approximately 15% |
| Half-life | Terminal elimination half-life: 4–6 hours; clinically, dosing every 4–6 hours as needed for symptom relief |
| Protein binding | Approximately 50% bound to plasma proteins |
| Volume of Distribution | Not well defined; estimated around 1.2 L/kg, suggesting distribution into total body water |
| Bioavailability | Ophthalmic: systemic bioavailability < 10% due to local administration and low absorption |
| Onset of Action | Ophthalmic: approximately 3–5 minutes after instillation |
| Duration of Action | Ophthalmic: up to 8–12 hours; prolonged effect due to local binding in conjunctival tissue |
| Action Class | Calcium channel blockers- Dihydropyridines (DHP) |
| Brand Substitutes | Amlin 5mg Tablet, Amset 5mg Tablet, Amlip 5 Tablet, Amcard 5 Tablet, Camlodip 5mg Tablet, Lupidip 10mg Tablet, Amlokind 10mg Tablet, Amcard 10 Tablet, Amlip 10 Tablet, Primodil 10 Tablet |
1 drop of 0.05% ophthalmic solution in the affected eye(s) twice daily, approximately 8 hours apart.
| Dosage form | SOLUTION/DROPS |
| Renal impairment | No dosage adjustment required for renal impairment. |
| Liver impairment | No dosage adjustment required for hepatic impairment. |
| Pediatric use | Safety and efficacy in pediatric patients below 3 years have not been established. For children 3 years and older, same as adult dosing. |
| Geriatric use | No specific dosage adjustment recommended, but caution advised due to possible increased sensitivity. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for EMADINE (EMADINE).
| Breastfeeding | Unknown if excreted in human breast milk. M/P ratio not available. Caution advised; use only if clearly needed. |
| Teratogenic Risk | FDA Pregnancy Category B. No evidence of teratogenicity in animal studies; insufficient human data. Avoid use in first trimester unless benefit outweighs risk. |
| Fetal Monitoring | Monitor maternal liver function and renal function; assess fetal growth if used long-term. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to emedastine or any components of the formulation"]
| Precautions | ["Not for injection","Should not be used to treat contact lens related irritation","Patients should not wear contact lenses if eyes are red"] |
Loading safety data…
| Fertility Effects | No known adverse effects on fertility in animal studies; no human data. |