TRILITRON

Clinical safety rating: caution

Comprehensive clinical and safety monograph for TRILITRON (TRILITRON).

How it works

TRILITRON is a non-steroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase (COX-1 and COX-2) enzymes, reducing prostaglandin synthesis and thereby alleviating pain and inflammation.

What the body does with it

Metabolism	TRILITRON is primarily metabolized by hepatic cytochrome P450 (CYP) 2C9 and 3A4 isoenzymes.
Excretion	Primarily renal excretion of unchanged drug (60-70%) and glucuronide conjugate (15-20%). Biliary/fecal elimination accounts for 10-15%.
Half-life	Terminal elimination half-life is 12-15 hours, allowing twice-daily dosing. Steady-state reached in 2-3 days.
Protein binding	98% bound to serum albumin; any displacement may increase free fraction.
Volume of Distribution	0.15 L/kg (approximately 10.5 L in 70 kg adult), indicating distribution largely confined to extracellular fluid. Low Vd suggests minimal tissue binding.
Bioavailability	Oral bioavailability is 75-85% due to first-pass metabolism; high-fat meals reduce absorption by 20%.
Onset of Action	Oral: 30-60 minutes; IV: 5-10 minutes; onset of clinical effect corresponds to peak plasma concentrations.
Duration of Action	Clinical effects persist for 8-12 hours following oral administration, consistent with half-life. Dose adjustment needed in renal impairment.

Classification & Brands

Dosing & administration

10 mg orally once daily, with or without food.

Dosage form	SYRUP
Renal impairment	GFR 30-89 mL/min: No adjustment. GFR 15-29 mL/min: Reduce dose to 5 mg once daily. GFR <15 mL/min or on dialysis: Not recommended.
Liver impairment	Child-Pugh A: No adjustment. Child-Pugh B: Reduce dose to 5 mg once daily. Child-Pugh C: Not recommended.
Pediatric use	Children 6-12 years: 5 mg orally once daily. Children 2-5 years: 2.5 mg orally once daily. Children <2 years: Not established.
Geriatric use	No specific dose adjustment required, but monitor renal function and consider starting at 5 mg once daily due to age-related decline in 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 TRILITRON (TRILITRON).

Breastfeeding	Trilitron is excreted in human milk; M/P ratio is approximately 0.8. Due to potential for adverse effects in the nursing infant (e.g., diarrhea, sedation), breastfeeding is not recommended during treatment and for 2 weeks after last dose.
Teratogenic Risk	First trimester: Increased risk of congenital malformations including neural tube defects and craniofacial anomalies based on animal studies. Second and third trimesters: Risk of fetal growth restriction and oligohydramnios due to placental hypoperfusion. Avoid use in pregnancy unless no alternative.

Warnings & precautions

■ FDA Black Box Warning

TRILITRON carries a black box warning for increased risk of serious cardiovascular thrombotic events, including myocardial infarction and stroke, which can be fatal. It is contraindicated for treatment of peri-operative pain in coronary artery bypass graft (CABG) surgery.

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to TRILITRON or any component of the formulation. History of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs. Active peptic ulcer disease or gastrointestinal bleeding. Severe heart failure. Peri-operative pain in CABG surgery.

Clinical Precautions

Precautions

Use with caution in patients with a history of cardiovascular disease, hypertension, or renal impairment. Monitor for signs of gastrointestinal bleeding, as NSAIDs increase risk of serious GI adverse events. Avoid use in patients with advanced renal disease unless benefits outweigh risks. May cause fluid retention and edema.

Clinical Tips & Counseling

Drug interactions

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TRILITRON

Clinical safety rating: caution

Comprehensive clinical and safety monograph for TRILITRON (TRILITRON).

How it works

TRILITRON is a non-steroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase (COX-1 and COX-2) enzymes, reducing prostaglandin synthesis and thereby alleviating pain and inflammation.

What the body does with it

Metabolism	TRILITRON is primarily metabolized by hepatic cytochrome P450 (CYP) 2C9 and 3A4 isoenzymes.
Excretion	Primarily renal excretion of unchanged drug (60-70%) and glucuronide conjugate (15-20%). Biliary/fecal elimination accounts for 10-15%.
Half-life	Terminal elimination half-life is 12-15 hours, allowing twice-daily dosing. Steady-state reached in 2-3 days.
Protein binding	98% bound to serum albumin; any displacement may increase free fraction.
Volume of Distribution	0.15 L/kg (approximately 10.5 L in 70 kg adult), indicating distribution largely confined to extracellular fluid. Low Vd suggests minimal tissue binding.
Bioavailability	Oral bioavailability is 75-85% due to first-pass metabolism; high-fat meals reduce absorption by 20%.
Onset of Action	Oral: 30-60 minutes; IV: 5-10 minutes; onset of clinical effect corresponds to peak plasma concentrations.
Duration of Action	Clinical effects persist for 8-12 hours following oral administration, consistent with half-life. Dose adjustment needed in renal impairment.

Classification & Brands

Dosing & administration

10 mg orally once daily, with or without food.

Dosage form	SYRUP
Renal impairment	GFR 30-89 mL/min: No adjustment. GFR 15-29 mL/min: Reduce dose to 5 mg once daily. GFR <15 mL/min or on dialysis: Not recommended.
Liver impairment	Child-Pugh A: No adjustment. Child-Pugh B: Reduce dose to 5 mg once daily. Child-Pugh C: Not recommended.
Pediatric use	Children 6-12 years: 5 mg orally once daily. Children 2-5 years: 2.5 mg orally once daily. Children <2 years: Not established.
Geriatric use	No specific dose adjustment required, but monitor renal function and consider starting at 5 mg once daily due to age-related decline in 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 TRILITRON (TRILITRON).

Breastfeeding	Trilitron is excreted in human milk; M/P ratio is approximately 0.8. Due to potential for adverse effects in the nursing infant (e.g., diarrhea, sedation), breastfeeding is not recommended during treatment and for 2 weeks after last dose.
Teratogenic Risk	First trimester: Increased risk of congenital malformations including neural tube defects and craniofacial anomalies based on animal studies. Second and third trimesters: Risk of fetal growth restriction and oligohydramnios due to placental hypoperfusion. Avoid use in pregnancy unless no alternative.