OPTIMARK IN PLASTIC CONTAINER

Clinical safety rating: caution

Comprehensive clinical and safety monograph for OPTIMARK IN PLASTIC CONTAINER (OPTIMARK IN PLASTIC CONTAINER).

How it works

Gadolinium-based paramagnetic contrast agent. The gadolinium ion (Gd3+) has seven unpaired electrons and a high magnetic moment, which enhances the relaxation rates of surrounding water protons in tissues, increasing signal intensity on T1-weighted magnetic resonance imaging (MRI) scans.

What the body does with it

Metabolism	Gadoversetamide is not metabolized; it is eliminated unchanged primarily by glomerular filtration.
Excretion	Primarily renal excretion via glomerular filtration; >90% of administered dose eliminated unchanged in urine within 24 hours. Less than 1% eliminated in feces.
Half-life	Terminal elimination half-life is approximately 2 hours in patients with normal renal function. In patients with severe renal impairment (GFR < 30 mL/min), half-life may be prolonged up to 30 hours.
Protein binding	Negligible (<10%); primarily binds to albumin minimally.
Volume of Distribution	Approximately 0.2 L/kg (12-14 L in adults), indicating distribution primarily in extracellular fluid.
Bioavailability	Not applicable for intravenous administration; when administered orally, bioavailability is less than 1% due to poor absorption and first-pass metabolism.
Onset of Action	Immediately after intravenous administration; contrast enhancement observed within seconds, with peak enhancement occurring within 4 minutes for brain MRI.
Duration of Action	Contrast enhancement persists for approximately 1 hour after injection, sufficient for MRI imaging. Clearance from blood is rapid; elimination half-life determines duration.

Classification & Brands

Dosing & administration

0.2 mL/kg (0.1 mmol/kg) IV bolus; may repeat once within 30 minutes for total dose of 0.4 mL/kg (0.2 mmol/kg) if needed for contrast-enhanced MRI.

Dosage form	INJECTABLE
Renal impairment	Contraindicated in acute kidney injury or chronic severe renal impairment (GFR < 30 mL/min/1.73 m²). In patients with GFR 30-60 mL/min/1.73 m², use lowest possible dose and avoid multiple doses; no specific dose reduction studied.
Liver impairment	No dosage adjustment required for mild to moderate hepatic impairment; not studied in severe hepatic impairment (Child-Pugh C).
Pediatric use	0.2 mL/kg (0.1 mmol/kg) IV bolus; not recommended for children < 2 years due to limited data.
Geriatric use	Use lowest effective dose; assess renal function prior to administration due to age-related decline in GFR; avoid if GFR < 30 mL/min/1.73 m².

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for OPTIMARK IN PLASTIC CONTAINER (OPTIMARK IN PLASTIC CONTAINER).

Breastfeeding	Gadoversetamide is excreted in human milk in low amounts. M/P ratio not established. The American College of Radiology recommends that breastfeeding may be continued without interruption after gadolinium administration, but the infant should be observed for potential allergic-type reactions or gastrointestinal disturbance.
Teratogenic Risk	Gadoversetamide crosses the placenta. Animal studies have shown fetal harm, but no adequate human studies. In first trimester, risk cannot be ruled out (Category C). In second and third trimesters, use only if clearly needed; gadolinium-based contrast agents may accumulate in amniotic fluid and fetal tissues, with unknown long-term effects.

Warnings & precautions

■ FDA Black Box Warning

Nephrogenic systemic fibrosis (NSF) occurs in patients with acute or chronic severe renal insufficiency (GFR <30 mL/min/1.73m2) or acute kidney injury. The risk increases with higher doses and repeated exposure. Do not use in these patients unless diagnostic information is essential and not available by other means.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to gadoversetamide or any component of the formulation","Patients with chronic severe renal insufficiency (GFR <30 mL/min/1.73m2) or acute kidney injury due to risk of NSF"]

Clinical Precautions

Precautions

["Risk of NSF in patients with renal impairment","Acute adverse reactions including anaphylaxis and hypersensitivity reactions may occur","Risk of gadolinium deposition in tissues and brain; clinical significance unknown","Nephrotoxicity may be increased in patients with pre-existing renal dysfunction","Use with caution in patients with history of allergic disorders or drug reactions"]

Clinical Tips & Counseling

Drug interactions

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OPTIMARK IN PLASTIC CONTAINER

Clinical safety rating: caution

Comprehensive clinical and safety monograph for OPTIMARK IN PLASTIC CONTAINER (OPTIMARK IN PLASTIC CONTAINER).

How it works

What the body does with it

Metabolism	Gadoversetamide is not metabolized; it is eliminated unchanged primarily by glomerular filtration.
Excretion	Primarily renal excretion via glomerular filtration; >90% of administered dose eliminated unchanged in urine within 24 hours. Less than 1% eliminated in feces.
Half-life	Terminal elimination half-life is approximately 2 hours in patients with normal renal function. In patients with severe renal impairment (GFR < 30 mL/min), half-life may be prolonged up to 30 hours.
Protein binding	Negligible (<10%); primarily binds to albumin minimally.
Volume of Distribution	Approximately 0.2 L/kg (12-14 L in adults), indicating distribution primarily in extracellular fluid.
Bioavailability	Not applicable for intravenous administration; when administered orally, bioavailability is less than 1% due to poor absorption and first-pass metabolism.
Onset of Action	Immediately after intravenous administration; contrast enhancement observed within seconds, with peak enhancement occurring within 4 minutes for brain MRI.
Duration of Action	Contrast enhancement persists for approximately 1 hour after injection, sufficient for MRI imaging. Clearance from blood is rapid; elimination half-life determines duration.

Classification & Brands

Dosing & administration

0.2 mL/kg (0.1 mmol/kg) IV bolus; may repeat once within 30 minutes for total dose of 0.4 mL/kg (0.2 mmol/kg) if needed for contrast-enhanced MRI.

Dosage form	INJECTABLE
Renal impairment	Contraindicated in acute kidney injury or chronic severe renal impairment (GFR < 30 mL/min/1.73 m²). In patients with GFR 30-60 mL/min/1.73 m², use lowest possible dose and avoid multiple doses; no specific dose reduction studied.
Liver impairment	No dosage adjustment required for mild to moderate hepatic impairment; not studied in severe hepatic impairment (Child-Pugh C).
Pediatric use	0.2 mL/kg (0.1 mmol/kg) IV bolus; not recommended for children < 2 years due to limited data.
Geriatric use	Use lowest effective dose; assess renal function prior to administration due to age-related decline in GFR; avoid if GFR < 30 mL/min/1.73 m².

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for OPTIMARK IN PLASTIC CONTAINER (OPTIMARK IN PLASTIC CONTAINER).

Breastfeeding	Gadoversetamide is excreted in human milk in low amounts. M/P ratio not established. The American College of Radiology recommends that breastfeeding may be continued without interruption after gadolinium administration, but the infant should be observed for potential allergic-type reactions or gastrointestinal disturbance.
Teratogenic Risk	Gadoversetamide crosses the placenta. Animal studies have shown fetal harm, but no adequate human studies. In first trimester, risk cannot be ruled out (Category C). In second and third trimesters, use only if clearly needed; gadolinium-based contrast agents may accumulate in amniotic fluid and fetal tissues, with unknown long-term effects.

Warnings & precautions

■ FDA Black Box Warning

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to gadoversetamide or any component of the formulation","Patients with chronic severe renal insufficiency (GFR <30 mL/min/1.73m2) or acute kidney injury due to risk of NSF"]