PENTETATE CALCIUM TRISODIUM
Clinical safety rating
cautionComprehensive clinical and safety monograph for PENTETATE CALCIUM TRISODIUM (PENTETATE CALCIUM TRISODIUM).
Pentetate calcium trisodium is a chelating agent that forms stable complexes with divalent and trivalent heavy metal ions, such as plutonium, americium, and curium. It enhances the urinary elimination of these metals by increasing the rate of dissociation from tissues and promoting renal excretion.
| Metabolism | Pentetate calcium trisodium is not metabolized; it is excreted unchanged in the urine via glomerular filtration and tubular secretion within 24 hours. |
| Excretion | Primarily renal elimination via glomerular filtration; >90% of absorbed dose excreted unchanged in urine within 24 hours. |
| Half-life | Terminal elimination half-life is approximately 0.6-0.8 hours in patients with normal renal function. |
| Protein binding | Negligible (<5%); primarily binds to plasma metal ions rather than proteins. |
| Volume of Distribution | Approximately 0.2-0.3 L/kg, indicating mainly extracellular distribution with minimal intracellular penetration. |
| Bioavailability | Not applicable; administered exclusively intravenously; oral bioavailability is negligible (<1%) due to poor absorption and gastrointestinal degradation. |
| Onset of Action | Intravenous administration: chelation of metal ions occurs immediately upon distribution; clinical effect on decorporation begins within minutes. |
| Duration of Action | Duration of chelation effect persists for approximately 24 hours; repeat dosing required to maintain decorporation due to rapid renal elimination. |
| Molecular Weight | 497.44 |
1 g (one vial) intravenously over 1 hour once daily for up to 5 days.
| Dosage form | SOLUTION |
| Renal impairment | No dose adjustment recommended; use with caution in severe renal impairment (GFR <30 mL/min) due to potential for accumulation. |
| Liver impairment | No specific dose adjustment provided in labeling; use with caution in severe hepatic impairment. |
| Pediatric use | Children: 14 mg/kg intravenously over 1 hour once daily; maximum 1 g/dose. |
| Geriatric use | No specific dose adjustment; start at lower end of dosing range due to potential for decreased renal function. |
| 1st trimester | Pentetate calcium trisodium is a chelating agent used for internal contamination with radioactive actinides. Animal studies have shown teratogenic effects at high doses, but there are no adequate human studies. Use only if clearly needed and potential benefit justifies risk to the fetus. |
| 2nd trimester | Same as first trimester: limited human data; animal studies suggest risk; weigh benefit vs risk. |
| 3rd trimester | Same as first and second trimesters: avoid unless necessary due to potential for fetal harm based on animal data. |
Clinical note
Comprehensive clinical and safety monograph for PENTETATE CALCIUM TRISODIUM (PENTETATE CALCIUM TRISODIUM).
| Placental transfer | In animal studies, pentetate calcium trisodium crosses the placenta and can be detected in fetal tissues. Human data are lacking, but based on molecular weight and animal evidence, placental transfer is expected. |
| Breastfeeding | No human data on excretion in breast milk. Calcium trisodium pentetate is a large, water-soluble chelate; likely minimal transfer into milk. However, caution is advised. Use only if clearly needed and monitor infant for any adverse effects. |
| Lactation Rating | L3: Limited Data - Probably Compatible |
| Teratogenic Risk | Pentetate calcium trisodium is a chelating agent used for specific heavy metal poisonings. No controlled human studies exist. Animal studies indicate no directly observed teratogenicity, but caution is warranted. Fetal risk cannot be excluded in any trimester due to potential maternal toxicity and chelation of essential minerals. |
| Fetal Monitoring | Monitor maternal renal function, serum electrolytes, and complete blood counts. Assure adequate maternal hydration. Assess fetal growth and well-being via ultrasound if ongoing therapy is required. Monitor for signs of trace element deficiency. |
| Fertility Effects | No human studies on fertility. Animal studies have not reported adverse effects on fertility or reproductive performance. Potential disruption of trace element homeostasis may theoretically affect fertility. |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to pentetate calcium trisodium or any component of the formulationSevere renal impairment (unless benefit outweighs risk, as drug is renally eliminated)
| Precautions | May cause depletion of essential trace metals (e.g., zinc, manganese) with prolonged use; monitor serum zinc levels during therapy. Use with caution in patients with impaired renal function, as drug accumulation may occur. Inhalation of pentetate calcium trisodium aerosol (for pulmonary contamination) may cause bronchospasm. |
| Food/Dietary | No specific food interactions are known. Patients should maintain adequate hydration and follow a balanced diet. Avoid excessive intake of calcium-containing foods or supplements unless directed by a healthcare provider, as calcium may interfere with chelation. |
| Clinical Pearls | Administer IV slowly (over at least 1 hour) to minimize local irritation. Monitor renal function and serum electrolytes (especially calcium, magnesium, potassium) before and during therapy. Do not use in patients with significant renal impairment (CrCl <30 mL/min) unless benefit outweighs risk. May cause transient hypotension; ensure adequate hydration. Contraindicated in patients with known hypersensitivity to EDTA. Prolonged use can lead to trace element deficiencies. |
| Patient Advice | This medication is used to treat poisoning from radioactive substances or heavy metals. · Tell your doctor if you have kidney problems, heart disease, or are pregnant or breastfeeding. · You will need regular blood tests to check kidney function and mineral levels. · Report symptoms like fever, chills, muscle cramps, or pain at the injection site. · Do not take any other medications or supplements without consulting your doctor. |
Loading safety data…