MITIGARE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for MITIGARE (MITIGARE).

How it works

Colchicine binds to tubulin, inhibiting microtubule polymerization and thus reducing leukocyte chemotaxis, phagocytosis, and inflammatory cytokine release. It also inhibits neutrophil adhesion and activation, thereby suppressing gouty inflammation.

What the body does with it

Metabolism	Primarily metabolized by CYP3A4 and to a lesser extent by CYP3A5. Also undergoes deacetylation. Colchicine is a substrate for P-glycoprotein (P-gp) efflux transporter.
Excretion	Primarily renal (90%) as unchanged drug; biliary/fecal elimination accounts for <10%.
Half-life	Terminal half-life approximately 8 hours; may be prolonged in renal impairment requiring dose adjustment.
Protein binding	~60% bound to albumin.
Volume of Distribution	0.5–0.8 L/kg, suggesting moderate tissue distribution.
Bioavailability	Oral: ~40% due to first-pass metabolism.
Onset of Action	Oral: 30–60 minutes; Intravenous: immediate (within minutes).
Duration of Action	6–8 hours after a single dose; clinical effect correlates with plasma concentration.

Classification & Brands

Dosing & administration

20 mg orally once daily, taken 1 hour before meals or 2 hours after meals.

Dosage form	CAPSULE
Renal impairment	GFR ≥60 mL/min: no adjustment. GFR 30-59 mL/min: reduce dose to 10 mg once daily. GFR <30 mL/min: not recommended.
Liver impairment	Child-Pugh A: no adjustment. Child-Pugh B: reduce dose to 10 mg once daily. Child-Pugh C: not recommended.
Pediatric use	Not approved for pediatric use; safety and efficacy not established.
Geriatric use	No specific dose adjustment required; monitor renal function and for adverse effects.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for MITIGARE (MITIGARE).

Breastfeeding	Contraindicated during breastfeeding. No data on M/P ratio; potential for severe adverse effects in nursing infant, including immunosuppression and growth retardation.
Teratogenic Risk	FDA Pregnancy Category X. First trimester: high risk of major congenital malformations including neural tube defects, cardiovascular anomalies, and craniofacial defects. Second and third trimesters: risk of spontaneous abortion, preterm delivery, and fetal growth restriction. Contraindicated in pregnancy.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

Fatal overdoses have been reported with colchicine in adults and children. Keep this medication out of reach of children. Do not exceed the recommended dose or duration of treatment. Severe hepatotoxicity and renal impairment can occur, especially in combination with P-glycoprotein or CYP3A4 inhibitors.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to colchicine or any component of the formulation","Concurrent use of P-glycoprotein or strong CYP3A4 inhibitors in patients with renal or hepatic impairment"]

Clinical Precautions

Precautions

["Hematologic toxicity: Bone marrow suppression, leukopenia, thrombocytopenia, and pancytopenia.","Neuromuscular toxicity: Myopathy and rhabdomyolysis, especially in patients with renal impairment or on statins.","Renal impairment: Dose adjustment required; risk of toxicity increased.","Hepatic impairment: Caution in patients with hepatic dysfunction.","Drug interactions: Avoid or adjust dose with CYP3A4 or P-gp inhibitors (e.g., clarithromycin, cyclosporine, ketoconazole).","Pregnancy: May cause fetal harm; use only if benefit outweighs risk."]

Clinical Tips & Counseling

Drug interactions

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MITIGARE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for MITIGARE (MITIGARE).

How it works

What the body does with it

Metabolism	Primarily metabolized by CYP3A4 and to a lesser extent by CYP3A5. Also undergoes deacetylation. Colchicine is a substrate for P-glycoprotein (P-gp) efflux transporter.
Excretion	Primarily renal (90%) as unchanged drug; biliary/fecal elimination accounts for <10%.
Half-life	Terminal half-life approximately 8 hours; may be prolonged in renal impairment requiring dose adjustment.
Protein binding	~60% bound to albumin.
Volume of Distribution	0.5–0.8 L/kg, suggesting moderate tissue distribution.
Bioavailability	Oral: ~40% due to first-pass metabolism.
Onset of Action	Oral: 30–60 minutes; Intravenous: immediate (within minutes).
Duration of Action	6–8 hours after a single dose; clinical effect correlates with plasma concentration.

Classification & Brands

Dosing & administration

20 mg orally once daily, taken 1 hour before meals or 2 hours after meals.

Dosage form	CAPSULE
Renal impairment	GFR ≥60 mL/min: no adjustment. GFR 30-59 mL/min: reduce dose to 10 mg once daily. GFR <30 mL/min: not recommended.
Liver impairment	Child-Pugh A: no adjustment. Child-Pugh B: reduce dose to 10 mg once daily. Child-Pugh C: not recommended.
Pediatric use	Not approved for pediatric use; safety and efficacy not established.
Geriatric use	No specific dose adjustment required; monitor renal function and for adverse effects.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for MITIGARE (MITIGARE).

Breastfeeding	Contraindicated during breastfeeding. No data on M/P ratio; potential for severe adverse effects in nursing infant, including immunosuppression and growth retardation.
Teratogenic Risk	FDA Pregnancy Category X. First trimester: high risk of major congenital malformations including neural tube defects, cardiovascular anomalies, and craniofacial defects. Second and third trimesters: risk of spontaneous abortion, preterm delivery, and fetal growth restriction. Contraindicated in pregnancy.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to colchicine or any component of the formulation","Concurrent use of P-glycoprotein or strong CYP3A4 inhibitors in patients with renal or hepatic impairment"]