LIALDA

Clinical safety rating: caution

Comprehensive clinical and safety monograph for LIALDA (LIALDA).

How it works

Mesalamine, the active ingredient in Lialda, is an anti-inflammatory agent that inhibits prostaglandin production and leukotriene synthesis, and reduces cytokine production in the colonic mucosa.

What the body does with it

Metabolism	Mesalamine is metabolized primarily in the liver and gut mucosa via N-acetylation to N-acetyl-5-aminosalicylic acid by N-acetyltransferase (NAT) enzymes.
Excretion	Renal (primarily, as N-acetyl-5-aminosalicylic acid, about 80%) and fecal (as unchanged mesalamine, about 20%).
Half-life	Terminal elimination half-life of mesalamine is approximately 12 hours (range 8-15 hours) for the sustained-release formulation; clinical steady-state is reached within 3-5 days.
Protein binding	Mesalamine is approximately 43% bound to plasma proteins, primarily albumin.
Volume of Distribution	Apparent volume of distribution for mesalamine is approximately 0.12 L/kg (range 0.06-0.17 L/kg), suggesting distribution mainly into extracellular fluid.
Bioavailability	Oral bioavailability of mesalamine from LIALDA is approximately 28% (due to first-pass metabolism to N-acetyl-5-aminosalicylic acid); rectal formulations have higher local bioavailability.
Onset of Action	Oral administration: clinical improvement in ulcerative colitis symptoms may be observed within 3-21 days; maximum effect may require several weeks.
Duration of Action	Dosing interval (1-2 times daily) maintains therapeutic drug levels for continuous anti-inflammatory effect; duration of clinical effect is sustained with regular dosing.

Classification & Brands

Dosing & administration

2-4 tablets (2.4-4.8 g) orally once daily. Each tablet contains 1.2 g mesalamine.

Dosage form	TABLET, DELAYED RELEASE
Renal impairment	Contraindicated in patients with severe renal impairment (eGFR <30 mL/min/1.73 m²). For moderate impairment (eGFR 30-59 mL/min/1.73 m²), reduce dose by 50% and monitor renal function.
Liver impairment	No specific dose adjustment recommended for hepatic impairment. Use caution in severe hepatic disease (Child-Pugh class C) due to limited data.
Pediatric use	For children ≥5 years: 2.4 g (2 tablets) orally once daily. For children >12 years: same as adult dosing. No established dosing for children <5 years.
Geriatric use	Start at lower end of dosing range (2.4 g daily). Monitor renal function closely due to age-related decline. Adjust dose per renal function.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for LIALDA (LIALDA).

Breastfeeding	Mesalamine excreted in breast milk in low amounts. M/P ratio not established. Milk concentrations typically <10% of maternal weight-adjusted dose. No adverse effects reported in infants. Consider monitoring infant for diarrhea. Compatible with breastfeeding.
Teratogenic Risk	Pregnancy Category B. No evidence of teratogenicity in animal studies. Limited human data; mesalamine is considered low risk during pregnancy. First trimester: risk of congenital anomalies not increased. Second/third trimester: theoretical risk of renal impairment in fetus; use only if clearly needed.

Warnings & precautions

■ FDA Black Box Warning

None.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Known hypersensitivity to salicylates or any component of the formulation","Severe renal impairment (eGFR < 30 mL/min/1.73 m²)"]

Clinical Precautions

Precautions

["Renal impairment, including minimal change nephropathy and acute/chronic interstitial nephritis","Mesalamine-induced acute intolerance syndrome (cramping, abdominal pain, bloody diarrhea, fever, headache, rash)","Hypersensitivity reactions including myocarditis and pericarditis","Hepatic failure in patients with pre-existing liver disease","Photosensitivity"]

Clinical Tips & Counseling

Drug interactions

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LIALDA

Clinical safety rating: caution

Comprehensive clinical and safety monograph for LIALDA (LIALDA).

How it works

Mesalamine, the active ingredient in Lialda, is an anti-inflammatory agent that inhibits prostaglandin production and leukotriene synthesis, and reduces cytokine production in the colonic mucosa.

What the body does with it

Metabolism	Mesalamine is metabolized primarily in the liver and gut mucosa via N-acetylation to N-acetyl-5-aminosalicylic acid by N-acetyltransferase (NAT) enzymes.
Excretion	Renal (primarily, as N-acetyl-5-aminosalicylic acid, about 80%) and fecal (as unchanged mesalamine, about 20%).
Half-life	Terminal elimination half-life of mesalamine is approximately 12 hours (range 8-15 hours) for the sustained-release formulation; clinical steady-state is reached within 3-5 days.
Protein binding	Mesalamine is approximately 43% bound to plasma proteins, primarily albumin.
Volume of Distribution	Apparent volume of distribution for mesalamine is approximately 0.12 L/kg (range 0.06-0.17 L/kg), suggesting distribution mainly into extracellular fluid.
Bioavailability	Oral bioavailability of mesalamine from LIALDA is approximately 28% (due to first-pass metabolism to N-acetyl-5-aminosalicylic acid); rectal formulations have higher local bioavailability.
Onset of Action	Oral administration: clinical improvement in ulcerative colitis symptoms may be observed within 3-21 days; maximum effect may require several weeks.
Duration of Action	Dosing interval (1-2 times daily) maintains therapeutic drug levels for continuous anti-inflammatory effect; duration of clinical effect is sustained with regular dosing.

Classification & Brands

Dosing & administration

2-4 tablets (2.4-4.8 g) orally once daily. Each tablet contains 1.2 g mesalamine.

Dosage form	TABLET, DELAYED RELEASE
Renal impairment	Contraindicated in patients with severe renal impairment (eGFR <30 mL/min/1.73 m²). For moderate impairment (eGFR 30-59 mL/min/1.73 m²), reduce dose by 50% and monitor renal function.
Liver impairment	No specific dose adjustment recommended for hepatic impairment. Use caution in severe hepatic disease (Child-Pugh class C) due to limited data.
Pediatric use	For children ≥5 years: 2.4 g (2 tablets) orally once daily. For children >12 years: same as adult dosing. No established dosing for children <5 years.
Geriatric use	Start at lower end of dosing range (2.4 g daily). Monitor renal function closely due to age-related decline. Adjust dose per renal function.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for LIALDA (LIALDA).

Breastfeeding	Mesalamine excreted in breast milk in low amounts. M/P ratio not established. Milk concentrations typically <10% of maternal weight-adjusted dose. No adverse effects reported in infants. Consider monitoring infant for diarrhea. Compatible with breastfeeding.
Teratogenic Risk	Pregnancy Category B. No evidence of teratogenicity in animal studies. Limited human data; mesalamine is considered low risk during pregnancy. First trimester: risk of congenital anomalies not increased. Second/third trimester: theoretical risk of renal impairment in fetus; use only if clearly needed.

Warnings & precautions

■ FDA Black Box Warning

None.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Known hypersensitivity to salicylates or any component of the formulation","Severe renal impairment (eGFR < 30 mL/min/1.73 m²)"]