APRISO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for APRISO (APRISO).
Mesalamine, the active ingredient, is a 5-aminosalicylic acid (5-ASA) that acts locally in the colon to reduce inflammation by inhibiting prostaglandin and leukotriene synthesis, scavenging free radicals, and activating peroxisome proliferator-activated receptor-gamma (PPAR-γ).
| Metabolism | Primarily metabolized in the liver via N-acetylation to N-acetyl-5-aminosalicylic acid; also undergoes acetylation in the gut wall and by gut bacteria. |
| Excretion | Renal (primarily as acetylated metabolite, ~80%) and fecal (~20%). |
| Half-life | 8.6 ± 4.2 hours for mesalamine; after multiple dosing, effective half-life ~12 hours. Clinical context: allows twice-daily dosing. |
| Protein binding | ~40% bound to plasma proteins (primarily albumin). |
| Volume of Distribution | 0.13 L/kg (approximately 9 L in 70 kg adult), indicating low tissue distribution. |
| Bioavailability | Oral: ~28% (delayed-release formulation; undergoes extensive presystemic metabolism). |
| Onset of Action | Oral: 3-21 days for symptomatic improvement in ulcerative colitis. |
| Duration of Action | Sustained release over 24 hours with once-daily dosing; clinical effect persists during trough concentrations. |
1.5 g (3 capsules) orally once daily in the morning. Each capsule contains 0.5 g mesalamine.
| Dosage form | CAPSULE, EXTENDED RELEASE |
| Renal impairment | Contraindicated in patients with severe renal impairment (eGFR <30 mL/min/1.73 m²). For mild to moderate impairment (eGFR 30-89 mL/min/1.73 m²), use with caution; no specific dose adjustment recommended, but monitor renal function. |
| Liver impairment | No specific dose adjustment for hepatic impairment. Use with caution in severe hepatic disease (Child-Pugh C) due to limited data. |
| Pediatric use | Safety and efficacy not established in pediatric patients (<18 years). No standard dosing available. |
| Geriatric use | No specific dose adjustment. Use with caution due to higher risk of renal impairment; monitor renal function regularly. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for APRISO (APRISO).
| Breastfeeding | Mesalamine is excreted into breast milk in low concentrations. The milk-to-plasma (M/P) ratio is approximately 0.08–0.14. At therapeutic maternal doses, the estimated infant dose is less than 10% of the maternal weight-adjusted dose, which is generally considered safe. However, caution is advised in neonates with glucose-6-phosphate dehydrogenase (G6PD) deficiency due to potential hemolysis. Diarrhea in the infant has been reported. |
| Teratogenic Risk | APRISO (mesalamine) is classified as FDA Pregnancy Category B. Data from human studies do not indicate an increased risk of major congenital anomalies in the first trimester. However, mesalamine is absorbed systemically, and there is a potential for fetal renal impairment, particularly in the third trimester, as it may cause oligohydramnios due to reduced fetal renal blood flow. Cases of neonatal renal dysfunction have been reported with maternal use of mesalamine products. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Hypersensitivity to mesalamine, salicylates, or any component of the formulation"]
| Precautions | ["Renal impairment (acute interstitial nephritis, nephrotoxicity)","Hypersensitivity reactions (e.g., pericarditis, myocarditis, colitis exacerbation)","Hepatic failure (in patients with pre-existing liver disease)","Photosensitivity","Pyloric stenosis (may cause prolonged gastric retention)"] |
| Food/Dietary | No significant food interactions. Take with or without food. Avoid concomitant use with magnesium trisilicate-containing antacids. |
| Clinical Pearls |
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| Fetal Monitoring | Monitor maternal renal function, hepatic function, and complete blood count periodically. During pregnancy, assess for signs of drug-induced hypersensitivity reactions. In the third trimester, monitor fetal urine output and amniotic fluid volume via ultrasound due to risk of oligohydramnios. Newborns should be observed for hypoglycemia, hemolytic anemia, and renal impairment after delivery. |
| Fertility Effects | No specific adverse effects on human fertility have been reported with mesalamine. Animal studies show no impairment of fertility. Inflammatory bowel disease itself can affect fertility, and controlling disease activity may improve reproductive outcomes. |
| APRISO is a once-daily, delayed-release formulation of mesalamine (5-aminosalicylic acid) designed for maintenance of remission in ulcerative colitis. The capsules contain polymer-coated beads that release mesalamine throughout the colon. Do not cut, crush, or chew capsules. Avoid co-administration with antacids containing magnesium trisilicate due to premature release. Monitor renal function in patients with pre-existing renal disease. |
| Patient Advice | Take APRISO once daily in the morning, with or without food. · Swallow capsules whole; do not cut, crush, or chew. · Avoid antacids containing magnesium trisilicate (e.g., Gaviscon) within 2 hours of taking APRISO. · Report worsening gastrointestinal symptoms, unexplained bruising, or bleeding. · Drink adequate fluids to prevent crystallization in urine. · Store at room temperature, away from moisture and heat. |