TILADE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TILADE (TILADE).
Mast cell stabilizer; inhibits release of inflammatory mediators such as histamine and leukotrienes from mast cells.
| Metabolism | Not metabolized; excreted unchanged in urine and feces. |
| Excretion | Primarily eliminated unchanged in urine (50-70%) via glomerular filtration and tubular secretion; remainder via biliary/fecal (30-50% as unchanged drug and metabolites). |
| Half-life | Terminal half-life approximately 1.5-2 hours after inhalation; systemic exposure low due to local administration and rapid clearance. |
| Protein binding | 50-60% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Vd approximately 0.5-1.0 L/kg, indicating distribution into total body water and some tissue binding. |
| Bioavailability | Inhalation: approximately 10-20% systemic bioavailability due to direct lung delivery and first-pass metabolism; oral bioavailability <1% due to poor absorption and extensive first-pass effect. |
| Onset of Action | Inhalation: 15-30 minutes; clinical effect on mast cell stabilization and airway protection. |
| Duration of Action | Duration approximately 6-8 hours; clinical notes: regular dosing four times daily required for prophylactic effect; not for acute bronchospasm. |
2 inhalations (2 mg) four times daily via oral inhalation.
| Dosage form | AEROSOL, METERED |
| Renal impairment | No dose adjustment required for renal impairment. |
| Liver impairment | No dose adjustment required for hepatic impairment. |
| Pediatric use | Children aged 2-12 years: 2 inhalations (2 mg) four times daily. |
| Geriatric use | No specific dose adjustment; use with caution due to potential comorbidities. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TILADE (TILADE).
| Breastfeeding | It is unknown if nedocromil sodium is excreted in human breast milk. The M/P ratio has not been determined. Caution should be exercised when administered to nursing women due to the potential for serious adverse reactions in nursing infants. |
| Teratogenic Risk | Tilade (nedocromil sodium) is classified as Pregnancy Category B. Animal studies have not demonstrated fetal harm, but adequate and well-controlled studies in pregnant women are lacking. No specific trimester risks have been identified; however, caution is advised throughout pregnancy. |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to nedocromil sodium or any component of the formulation.
| Precautions | Not for acute bronchospasm; may cause throat irritation, cough, and bronchospasm; renal impairment requires dose adjustment. |
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| Fetal Monitoring |
| No specific maternal or fetal monitoring is required beyond standard prenatal care. Monitor for adverse effects of the drug, such as cough or throat irritation, which may affect maternal compliance. |
| Fertility Effects | Animal studies have shown no impairment of fertility at doses up to 100 mg/kg/day (approximately 160 times the human daily inhalation dose on a mg/m² basis). Human fertility data are not available. |