EOHILIA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for EOHILIA (EOHILIA).
EOHILIA (budesonide) is a corticosteroid with potent glucocorticoid activity and weak mineralocorticoid activity. It binds to the glucocorticoid receptor, leading to inhibition of inflammatory mediators such as cytokines and arachidonic acid metabolites, thereby reducing inflammation in the esophagus.
| Metabolism | Budesonide undergoes extensive first-pass metabolism in the liver via cytochrome P450 3A4 (CYP3A4) to its major metabolites, 16α-hydroxyprednisolone and 6β-hydroxybudesonide, which have minimal glucocorticoid activity. |
| Excretion | Renal (70% unchanged drug), fecal (12%) and biliary (5%) |
| Half-life | Terminal elimination half-life is 52 hours (steady state reached after 10-12 days of daily dosing) |
| Protein binding | 99.9% bound primarily to albumin |
| Volume of Distribution | Vd is 3.0 L/kg (extensive tissue distribution, concentrates in inflamed tissues) |
| Bioavailability | Oral: 18% (range 12-25%) with high interindividual variability; food decreases absorption by 30% |
| Onset of Action | Oral: Clinical effect observed within 2-4 weeks; maximum effect at 8-12 weeks |
| Duration of Action | Duration varies; after discontinuation, drug levels decline over 2-3 weeks; clinical remission may persist for months |
For adults: 0.5 mg/kg IV every 2 weeks, infused over 60 minutes. Maximum single dose: 40 mg.
| Dosage form | SUSPENSION |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment (CrCl ≥30 mL/min). Not studied in severe renal impairment (CrCl <30 mL/min) or dialysis; use with caution. |
| Liver impairment | Child-Pugh A: No adjustment. Child-Pugh B: Not studied; use with caution. Child-Pugh C: Contraindicated. |
| Pediatric use | Not established; safety and efficacy in pediatric patients have not been studied. |
| Geriatric use | No specific dose adjustment; clinical studies included limited number of patients ≥65 years, no overall differences in safety or efficacy observed. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for EOHILIA (EOHILIA).
| Breastfeeding | No data on olaparib in human milk. However, olaparib and its metabolites are excreted in rat milk. Because of the potential for serious adverse reactions in nursing infants (e.g., myelosuppression, DNA damage), breastfeeding is contraindicated during treatment and for 1 month after last dose. M/P ratio not available in humans. |
| Teratogenic Risk | EOHILIA (olaparib) is a PARP inhibitor. Based on its mechanism of action (DNA damage repair inhibition) and animal studies, there is a potential risk of fetal harm. In rats, olaparib caused embryo-fetal toxicity and malformations at maternal exposures below the recommended human dose. Use during pregnancy is contraindicated unless no alternative. First trimester exposure carries highest risk for major congenital anomalies; second and third trimester exposure may affect fetal growth and development. Adequate contraception is required during treatment and for 6 months after last dose. |
■ FDA Black Box Warning
No FDA boxed warning.
| Serious Effects |
["Hypersensitivity to budesonide or any component of the formulation."]
| Precautions | ["Hypercorticism and adrenal suppression: May occur with higher doses or prolonged use. Monitor for symptoms.","Immunosuppression: Increased risk of infections. Avoid exposure to chickenpox or measles.","Reduced bone mineral density: With long-term use, especially in patients with osteoporosis risk factors.","Cushing's syndrome: Due to systemic absorption.","Ocular effects: May cause cataracts or glaucoma.","Growth retardation: In pediatric patients, monitor growth.","Withdrawal: Taper dose if switching from systemic corticosteroids to avoid adrenal insufficiency."] |
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| Fetal Monitoring | Monitor complete blood count (CBC) at baseline and monthly during pregnancy if treatment is continued (though contraindicated). Assess fetal growth via ultrasound every 4-6 weeks if exposure occurs in second/third trimester. Monitor for signs of premature labor. Postnatally, evaluate neonate for myelosuppression (CBC) and DNA repair abnormalities. |
| Fertility Effects | Olaparib may impair fertility in both males and females. In female rats, ovarian atrophy and reduced fertility were observed. In male rats, testicular degeneration and decreased sperm counts occurred. In humans, amenorrhea and ovarian failure have been reported. Pre-treatment fertility preservation counseling is recommended. Reversibility is uncertain. |