COLOCORT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for COLOCORT (COLOCORT).
Colocort (hydrocortisone acetate) is a corticosteroid that binds to the glucocorticoid receptor, leading to inhibition of inflammatory mediators such as prostaglandins and leukotrienes, and suppression of immune responses.
| Metabolism | Primarily hepatic via CYP3A4; also metabolized locally in the colon. |
| Excretion | Renal: ~30% as metabolites; fecal/biliary: ~20% as metabolites; remainder metabolized with minimal unchanged drug excreted. |
| Half-life | Terminal elimination half-life: 2.5–3.5 hours (mean ~3 hours). No active metabolites, so duration of action correlates with half-life. |
| Protein binding | ~85% bound to albumin and corticosteroid-binding globulin (CBG). |
| Volume of Distribution | 1.4–2.3 L/kg (approx 100–160 L in 70 kg adult). Indicates extensive tissue distribution. |
| Bioavailability | Oral: ~20–25% (first-pass metabolism); Rectal enema: ~15–20% (avoidance of first-pass but incomplete absorption); Rectal foam: ~10–15% (limited retention). |
| Onset of Action | Oral: 3–5 hours; Rectal enema: 1–3 hours; Rectal foam: 2–4 hours. Clinical effect onset delayed due to time required for mucosal healing. |
| Duration of Action | Oral: 12–24 hours (single dose); Rectal enema/foam: 12–24 hours; Duration limited by half-life but once-daily dosing effective due to local effects. |
| Molecular Weight | 521.04 |
10 mg rectally administered once daily, preferably at bedtime, as a retention enema.
| Dosage form | ENEMA |
| Renal impairment | No dose adjustment required for renal impairment. |
| Liver impairment | No specific guidelines; use with caution in severe hepatic impairment due to potential for increased systemic exposure. |
| Pediatric use | Safety and efficacy not established in pediatric patients below 18 years. |
| Geriatric use | No specific dose adjustment; use with caution due to potential for increased sensitivity and adverse effects. |
| 1st trimester | Avoid due to risk of cleft palate and suppressed fetal growth; limited data, but corticosteroids are generally not recommended in first trimester unless essential. |
| 2nd trimester | Use only if benefit outweighs risk; may cause adrenal suppression in fetus; monitor for intrauterine growth restriction (IUGR). |
| 3rd trimester | Use with caution; prolonged use may lead to neonatal adrenal insufficiency; associated with preterm premature rupture of membranes (PPROM) and low birth weight. |
Clinical note
Comprehensive clinical and safety monograph for COLOCORT (COLOCORT).
| Placental transfer | Beclomethasone dipropionate crosses the placenta to a limited extent; its active metabolite, beclomethasone-17-monopropionate, has higher systemic activity but placental transfer is minimal after inhalation due to low bioavailability; animal studies show some transfer. |
| Breastfeeding | Corticosteroids like beclomethasone (active component of COLOCORT) are excreted into breast milk in low amounts; risk of infant adrenal suppression is minimal with inhaled or topical use; systemic absorption is low; however, monitor infant for signs of adrenal suppression if maternal dose is high. |
■ FDA Black Box Warning
There is no FDA black box warning for Colocort.
| Serious Effects |
Hypersensitivity to beclomethasone dipropionate or any excipientUntreated systemic bacterial, fungal, or viral infectionsSevere bronchiectasisStatus asthmaticus (acute severe asthma requires systemic corticosteroids)
| Precautions | Local irritation or burning sensation, Systemic absorption may cause adrenal suppression, especially with prolonged use or large doses, Increased risk of infection, Masking of infection symptoms, Perforation risk in severe inflammatory bowel disease, Use with caution in patients with diverticulitis, fistulas, or intestinal anastomoses |
| Food/Dietary | Avoid grapefruit and grapefruit juice during treatment as they inhibit CYP3A4 and may increase budesonide systemic levels. No other specific food restrictions; however, a low-residue diet may be recommended during acute flare-ups to reduce bowel irritation. |
Loading safety data…
| Lactation Rating | L2 (Safer) |
| Teratogenic Risk | COLOCORT (budesonide) is a corticosteroid. In pregnancy, oral budesonide is not associated with a significant increase in major congenital malformations based on population-based cohort studies. First trimester exposure does not show increased risk of orofacial clefts. Second and third trimester exposure may be associated with reduced fetal growth and increased risk of neonatal adrenal suppression if used chronically at high doses. No documented fetal risk in inhaled form at recommended doses. |
| Fetal Monitoring | Monitor maternal blood pressure, blood glucose, and signs of infection. For prolonged use, assess fetal growth via ultrasound every 4-6 weeks. Neonates exposed to high doses in third trimester should be monitored for adrenal suppression (e.g., hypoglycemia, hypotension). |
| Fertility Effects | No evidence of impaired fertility in humans. In animal studies, high doses caused reduced fertility. In patients with inflammatory bowel disease, improved disease control may enhance fertility. No known direct adverse effect on spermatogenesis or ovulatory function. |
| Clinical Pearls | COLOCORT (budesonide) is a locally-acting corticosteroid for induction of remission in mild-to-moderate ulcerative colitis. It undergoes extensive first-pass hepatic metabolism, reducing systemic bioavailability. Administer as a retention enema, typically at bedtime after bowel evacuation. Patients should retain the enema for at least 8 hours. Monitor for hypothalamic-pituitary-adrenal axis suppression if switching from systemic corticosteroids. |
| Patient Advice | Use exactly as prescribed; do not use more often or for longer than directed. · Shake the enema bottle well before use. Lie on your left side to administer, then remain lying for 30 minutes. · Try to retain the enema for at least 8 hours, preferably overnight. · Do not use if you have a bowel obstruction or perforation, or if you have an active infection. · Contact your doctor if symptoms do not improve within 2 weeks or worsen. · Inform your doctor about all medications you take, especially other corticosteroids, antifungals, or HIV medications (protease inhibitors). · Report any signs of infection (fever, sore throat) or unusual bruising/bleeding. |