ORAGRAFIN SODIUM
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ORAGRAFIN SODIUM (ORAGRAFIN SODIUM).
Oragrafin Sodium is an oral cholecystographic contrast agent containing sodium ipodate. It is absorbed orally, excreted by the liver into bile, and concentrates in the gallbladder, allowing radiographic visualization. The iodine atoms in the molecule absorb X-rays, providing contrast. It also inhibits thyroid hormone synthesis by blocking iodine organification and may be used in amiodarone-induced thyrotoxicosis.
| Metabolism | Metabolized in the liver via conjugation with glucuronic acid; elimination is primarily biliary and fecal, with minimal renal excretion. |
| Excretion | Primarily renal (hepatic/biliary/fecal: minimal). Approximately 80-90% of the absorbed dose is excreted unchanged in urine via glomerular filtration; <10% eliminated in feces via biliary excretion. |
| Half-life | Terminal elimination half-life is approximately 60-90 minutes in patients with normal renal function (creatinine clearance > 90 mL/min), reflecting rapid renal clearance of this water-soluble contrast agent. |
| Protein binding | Negligible (<1%); does not bind significantly to plasma albumin due to high water solubility and low lipophilicity. |
| Volume of Distribution | Approximately 0.2-0.3 L/kg, indicating distribution primarily within extracellular fluid (plasma and interstitial space) with minimal intracellular penetration. |
| Bioavailability | Oral: Not systematically absorbed; bioavailability is negligible (<0.1%) as the drug acts intraluminally, providing contrast without significant systemic exposure. Rectal: Similarly, bioavailability is minimal due to poor mucosal absorption. |
| Onset of Action | Oral: Onset of opacification of small intestine observed within 30-60 minutes; colon opacification begins at 1-3 hours. Rectal: Onset within 5-15 minutes for colonic opacification. Intravenous: Not applicable; IV use is contraindicated due to risk of severe adverse reactions. |
| Duration of Action | Oral: Adequate opacification persists for 1-3 hours after onset. Rectal: Duration of diagnostic opacification typically 30-60 minutes after administration. Clinical use is limited to single diagnostic procedures; no prolonged therapeutic effect. |
Oral: 50-60 mL of a 10% solution (5-6 g sodium iopodate) as a single dose 10-12 hours before cholecystography. Repeat if needed: 50 mL (5 g) the next evening. Intravenous: Not applicable (oral agent).
| Dosage form | CAPSULE |
| Renal impairment | No specific dose adjustment guidelines available; use with caution in severe renal impairment (eGFR <30 mL/min/1.73 m²) due to risk of nephrotoxicity; consider alternative imaging. |
| Liver impairment | No specific adjustment; use with caution in Child-Pugh C cirrhosis due to potential altered metabolism. |
| Pediatric use | Insufficient data; not recommended for routine pediatric use. Dose per weight not established. |
| Geriatric use | Initiate at lower end of dosing range (50 mL) due to age-related renal decline; monitor renal function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ORAGRAFIN SODIUM (ORAGRAFIN SODIUM).
| Breastfeeding | Excreted in breast milk in minimal amounts (M/P ratio not established; estimated <1% of maternal dose). Oral bioavailability negligible. Considered compatible with breastfeeding; however, caution with repeated high doses due to theoretical risk of neonatal iodine overload. Discontinue breastfeeding for 24-48 hours post-administration per some guidelines. |
| Teratogenic Risk | FDA Pregnancy Category C. Iodinated contrast agents cross the placenta. First trimester: theoretical risk of fetal hypothyroidism due to iodine overload; avoid unless essential. Second/third trimester: transient neonatal hypothyroidism reported with high doses or repeated exposure; neonatal thyroid function should be assessed postpartum. No teratogenic effects in animal studies. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to iodine or ipodate","Severe hepatic or renal impairment","Thyrotoxicosis (relative; may be used therapeutically under expert guidance)","Pregnancy (Category D) – contraindicated in pregnancy due to risk of neonatal hypothyroidism"]
| Precautions | [] |
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| Fetal Monitoring | Monitor maternal renal function (serum creatinine, eGFR) prior to administration due to risk of contrast-induced nephropathy. Assess for hypersensitivity reactions. Fetal: post-delivery neonatal thyroid function tests (TSH, free T4) at 3-5 days of age if high-dose or repeated contrast used during pregnancy. |
| Fertility Effects | No known adverse effects on human fertility. Animal studies show no impairment of fertility at clinically relevant doses. |