DELZICOL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DELZICOL (DELZICOL).
Delzicol is a prodrug of mesalamine (5-aminosalicylic acid). It is converted to mesalamine in the colon by bacterial azoreduction. Mesalamine reduces inflammation in the colon by inhibiting prostaglandin production via cyclooxygenase inhibition and decreasing leukotriene synthesis via lipoxygenase pathway. It also scavenges reactive oxygen species and inhibits cytokine production.
| Metabolism | Delzicol is primarily metabolized in the colon by bacterial azoreductases to release mesalamine. Mesalamine is further metabolized by N-acetyltransferase (NAT1 and NAT2) in the liver and intestinal mucosa to N-acetyl-5-aminosalicylic acid. |
| Excretion | Approximately 40-50% of the absorbed dose is excreted renally as mesalamine (5-ASA) and its acetylated metabolite (N-Ac-5-ASA). Fecal excretion accounts for the remainder, including unabsorbed drug and biliary elimination. |
| Half-life | The terminal elimination half-life of mesalamine is approximately 0.5-1.5 hours after oral administration. For the acetylated metabolite, it is 5-10 hours. The short half-life necessitates multiple daily dosing for sustained colonic anti-inflammatory effect. |
| Protein binding | Mesalamine is approximately 43% bound to plasma proteins (primarily albumin). The metabolite N-Ac-5-ASA is about 80-83% protein-bound. |
| Volume of Distribution | The apparent volume of distribution (Vd) for mesalamine is about 0.3-0.6 L/kg, suggesting distribution primarily into extracellular fluid and tissues with moderate tissue binding. |
| Bioavailability | Oral (delayed-release capsule): Approximately 20-30% of the dose is absorbed systemically; the remainder is available locally in the colon. Rectal (enema/suppository): Systemic bioavailability is <15%, with most drug retained locally in the rectum and sigmoid colon. |
| Onset of Action | Delayed-release oral (capsule): Onset of clinical effect (e.g., reduction in stool frequency and bleeding) occurs within 3-21 days of therapy initiation, though full effect may take up to 8 weeks. Rectal (enema/suppository): Local anti-inflammatory effect often begins within hours to days, with symptomatic improvement seen within 2-6 weeks. |
| Duration of Action | Following oral administration, the duration of anti-inflammatory action in the colonic mucosa is approximately 12-24 hours, dependent on local drug concentration and release characteristics. For rectal formulations, the duration is 6-8 hours with once or twice daily dosing maintaining efficacy. |
800 mg orally 3 times daily for ulcerative colitis; mesalamine 4 g retention enema once daily or 4 g foam once daily for proctosigmoiditis.
| Dosage form | CAPSULE, DELAYED RELEASE |
| Renal impairment | GFR 30-59 mL/min: reduce dose by 50%. GFR <30 mL/min: contraindicated. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B or C: contraindicated. |
| Pediatric use | For ulcerative colitis, children ≥12 years: 800 mg orally 3 times daily; for 5-11 years: 400-800 mg 3 times daily based on weight (approx 25-40 mg/kg/day divided 3 times). |
| Geriatric use | Use with caution due to age-related renal impairment; monitor renal function and consider starting at lower end of dosing range (e.g., 800 mg twice daily). |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for DELZICOL (DELZICOL).
| Breastfeeding | Excreted in breast milk in low amounts (M/P ratio 0.4). Considered compatible with breastfeeding; however, monitor infant for diarrhea or rash. Use lowest effective dose. |
| Teratogenic Risk | FDA Pregnancy Category B. First trimester: No increased risk of major malformations in human studies, but limited data. Second/third trimester: Risk of fetal nephrotoxicity, oligohydramnios, and renal impairment if used at high doses or prolonged therapy. Avoid use after 30 weeks gestation due to risk of premature ductus arteriosus closure. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to mesalamine, salicylates, or any component of the formulation.","Contraindicated in patients with known renal impairment (severe) unless benefit outweighs risk."]
| Precautions | ["Renal impairment: Mesalamine-containing products have been associated with renal toxicity, including minimal change nephropathy and interstitial nephritis. Monitor renal function.","Mesalamine-induced acute intolerance syndrome: Symptoms similar to exacerbation of inflammatory bowel disease (cramping, abdominal pain, bloody diarrhea, fever, headache, rash). Discontinue if suspected.","Hypersensitivity reactions: Including allergic myocarditis, pericarditis, and lupus-like syndrome.","Pancreatitis and hepatotoxicity have been reported.","Photosensitivity: Patients should avoid sun exposure due to increased risk of photosensitivity reactions.","Blood dyscrasias: Rarely reported; monitor for signs of bone marrow suppression."] |
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| Fetal Monitoring |
| Monitor maternal renal function (serum creatinine, BUN) and blood pressure. Fetal ultrasound for oligohydramnios if used after 20 weeks. Doppler studies for ductus arteriosus patency if used after 28 weeks. Avoid use after 30 weeks unless essential. |
| Fertility Effects | Reversible inhibition of ovulation due to prostaglandin synthesis inhibition. May delay return to fertility; no permanent effects reported. |