gadoversetamide (OptiMARK)
Classes: Gadolinium-Containing Contrast Agents; Contrast Media, Nonionic/ High Osmolality
Dosing and uses of OptiMARK (gadoversetamide)
Adult dosage forms and strengths
injectable solution
- 330.9 mg/mL (0.5mmol/mL)
CNS or Liver MRI
Indicated for use with MRI in abnormal blood brain barrier or abnormal vascularity of the brain, spine, and associated tissues; also indicated to enhance visualization of lesions with abnormal vascularity in the liver
0.2 mL/kg (0.1 mmol/kg) IV; infuse peripherally at rate of 1-2 mL/sec
Pediatric dosage forms and strengths
Safety and efficacy not established
OptiMARK (gadoversetamide) adverse (side) effects
1-10%
Headache (9.4%)
Vasodilation (6.4%)
Dizziness (3.7%)
Nausea (3.2%)
Paresthesia (2.2%)
Diarrhea (1.9%)
Abdominal pain (1.8%)
Rhinitis (2%)
Injection site reaction (2%)
Back pain (1%)
Dyspepsia (1%)
<1%
Seizures
Amblyopia
Anorexia
Cough
Diplopia
Dry skin
Dystonia
Flatulence
Hyponatremia
Neck pain
Pallor
Parosmia
Rash
Seizure
Postmarketing Reports
Seizures
Nephrogenic systemic fibrosis
Hypersensitivity reactions including bronchospasm and laryngeal/pharyngeal edema
Warnings
Black box warnings
Risk for nephrogenic systemic fibrosis (NSF) with acute or chronic renal insufficiency (GFR <30 mL/min/1.73m²), hepatorenal syndrome, or acute renal insufficiency resulting from perioperative liver transplant
NSF affects internal organs, skin, and muscle and can be fataL
Only use if essential and MRI cannot not provide appropriate diagnostic image
Screen for renal dysfunction, do not exceed recommended dosage, and allow for drug elimination before giving subsequent doses
Contraindications
Severe hypersensitivity reactions including anaphylaxis reported
Acute kidney disease or chronic, severe kidney disease (ie, GFR<30 mL/min/1.73m²); use associated with increased risk for nephrogenic systemic fibrosis (NSF)
Cautions
Screen all patients for renal dysfunction
Acute renal failure has occurred in patients with pre-existing renal insufficiency; use the lowest necessary dose and evaluate renal function
Nephrogenic systemic fibrosis (NSF) reported in patients with impaired elimination; higher than recommended dosing or repeat dosing appears to increase the risk
Anaphylactoid and other serious hypersensitivity reactions including fatal reactions reported, particularly in patients with history of allergy or drug reactions; monitor patients closely for need of emergency cardiorespiratory support
Thrombotic syndromes, anemia, hepatic/renal impairment, hemoglobinopathies (sickle cell anemia)
Risk of hypotension
Caution with hepatic impairment
History of grand mal seizure
Brain deposits
- 7/28/2015: FDA is investigating the risk of brain deposits following repeated use of gadolinium-based contrast agents (GBCAs) for MRI
- Recent publications in the medical literature have reported that deposits of GBCAs remain in the brains of some patients who undergo ≥4 contrast MRI scans, long after the last administration
- It is unknown whether these gadolinium deposits are harmful or can lead to adverse health effects
- Early data in rat studies show that linear GBCAs are more prone to dissociation into free gadolinium and demonstrate greater brain deposition than macrocyclic GBCAs, which are less prone to dissociation
Pregnancy and lactation
Pregnancy category: C
Lactation: Excreted in milk of lactating rats; official prescribing information advises women to discontinue breastfeeding and discard milk for 72 hr after receiving gadoversetamide
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of OptiMARK (gadoversetamide)
Mechanism of action
Nonionic gadolinium contrast agent; paramagnetic ion that develops a magnetic moment when placed in magnetic field that can disrupt water protons in the vicinity leading to an increase in signal intensity (brightness) of tissues
Pharmacokinetics
Half-Life: 103.6 minutes (elimination)
Vd: 162 mL/kg
Excretion: Urine (96%)
Hemodialysis: 98% removed by hemodialysis over 3 sessions within 120 hr