DIATRIZOATE MEGLUMINE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DIATRIZOATE MEGLUMINE (DIATRIZOATE MEGLUMINE).
Diatrizoate meglumine is an ionic, high-osmolar iodinated contrast agent that absorbs X-rays due to its iodine content, thereby enhancing radiographic imaging. It does not exert pharmacological effects via receptor interaction but functions by attenuating X-ray beams, providing contrast between vascular structures and surrounding tissues.
| Metabolism | Diatrizoate meglumine is not metabolized; it is eliminated unchanged by glomerular filtration via the kidneys. |
| Excretion | Primarily renal excretion via glomerular filtration; >95% of the administered dose is excreted unchanged in urine within 24 hours. Less than 5% is excreted in feces via biliary elimination. |
| Half-life | Terminal elimination half-life is approximately 1-2 hours in patients with normal renal function (CLcr >90 mL/min). Half-life is significantly prolonged in renal impairment (up to 20-40 hours in anuria), necessitating dose adjustment and caution. |
| Protein binding | Negligible protein binding (<5%); binding to albumin is minimal. |
| Volume of Distribution | Approximately 0.2-0.3 L/kg; distributes primarily in extracellular fluid. Does not significantly cross the blood-brain barrier in intact brain. |
| Bioavailability | Oral: approximately 0% (not absorbed systemically due to high polarity and low lipophilicity); Intravenous: 100% for direct vascular administration. |
| Onset of Action | Intravenous: immediate (within seconds) for contrast enhancement; Oral: 15-30 minutes for gastrointestinal opacification; Rectal: 30-60 minutes for enema studies. |
| Duration of Action | Intravenous: contrast enhancement lasting 15-30 minutes for CT imaging; Oral: adequate bowel opacification for up to 1-2 hours; Rectal: variable, but typically sufficient for the duration of the enema study (15-30 minutes). |
Intravenous: 1-2 mL/kg (305-610 mg I/kg) of 60% or 76% solution for urography; 40-60 mL of 50% solution for retrograde cystourethrography. Oral: 200-600 mL of 4.8% suspension for GI contrast.
| Dosage form | INJECTABLE |
| Renal impairment | GFR <30 mL/min: Consider alternative; reduce dose or extend interval. GFR 30-60 mL/min: Caution with reduced dose. No specific dose recommendations; risk of nephrotoxicity. |
| Liver impairment | No specific dose adjustments; severe hepatic impairment may increase nephrotoxicity risk; use with caution. |
| Pediatric use | Intravenous urography: 1-2 mL/kg (305-610 mg I/kg) of 60 or 76% solution. Oral GI: <5 years: 60-90 mL of 4.8% suspension; 5-10 years: 150 mL; >10 years: 200-300 mL. |
| Geriatric use | Use lowest effective dose; monitor renal function; increased risk of nephrotoxicity and dehydration; ensure adequate hydration. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for DIATRIZOATE MEGLUMINE (DIATRIZOATE MEGLUMINE).
| Breastfeeding | Diatrizoate meglumine is excreted into breast milk in small amounts. Milk to plasma ratio is approximately 0.5. Absorption from infant gastrointestinal tract is minimal. Clinical guidance: breastfeeding may be continued without interruption after standard diagnostic doses. No adverse effects in nursing infants reported. |
| Teratogenic Risk | Diatrizoate meglumine, an ionic iodinated contrast agent, is not associated with teratogenicity in humans at diagnostic doses. Animal studies have not shown fetal harm. However, theoretical risk of fetal hypothyroidism exists if large doses are administered near term due to free iodide release. Use in pregnancy only if clearly needed. |
■ FDA Black Box Warning
None
| Serious Effects |
Absolute: Known hypersensitivity to diatrizoate meglumine or any component, anuria. Relative: History of severe allergic reactions to iodinated contrast agents, advanced renal disease, severe heart failure, hyperthyroidism.
| Precautions | Risk of serious hypersensitivity/anaphylactoid reactions, including fatal cardiovascular and respiratory events; pre-existing renal impairment can lead to contrast-induced nephropathy; caution in patients with sickle cell disease, multiple myeloma, or pheochromocytoma; ensure adequate hydration before administration. |
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| Fetal Monitoring | Monitor maternal renal function (serum creatinine, BUN) prior to administration due to risk of contrast-induced nephropathy. Assess for allergic reactions (urticaria, dyspnea) during and after injection. Fetal monitoring (heart rate) not routinely required but consider in high-risk pregnancies or if large dose used. |
| Fertility Effects | No significant adverse effects on fertility reported in animal studies. Human data limited; no evidence of impaired male or female fertility with diagnostic use. |