INDIUM IN-111 PENTETREOTIDE KIT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for INDIUM IN-111 PENTETREOTIDE KIT (INDIUM IN-111 PENTETREOTIDE KIT).
Indium In-111 pentetreotide binds to somatostatin receptors, particularly subtypes 2 and 5, allowing scintigraphic localization of primary and metastatic neuroendocrine tumors bearing these receptors.
| Metabolism | Indium In-111 pentetreotide is not metabolized; it is eliminated primarily by renal excretion. |
| Excretion | Renal: 80-90% unchanged within 24 hours; Fecal: 5-10% |
| Half-life | Terminal half-life approximately 24 hours (range 22-26 hours), allowing imaging up to 24-48 hours post-injection |
| Protein binding | Approximately 80% bound to plasma proteins, primarily albumin and transferrin |
| Volume of Distribution | Vd approximately 10-15 L/kg, indicating extensive distribution into tissues expressing somatostatin receptors, including tumors and normal organs (spleen, liver, kidneys) |
| Bioavailability | Bioavailability: 100% following intravenous administration; not administered via other routes |
| Onset of Action | IV: Uptake at somatostatin receptor-positive sites detectable within 1-2 hours, optimal imaging at 4-24 hours |
| Duration of Action | Clinical imaging window extends to 24-48 hours post-injection, with residual activity detectable up to 72 hours |
111 MBq (3 mCi) indium In-111 pentetreotide administered intravenously over 1 minute; single dose for planar and SPECT imaging.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustments are recommended for renal impairment; however, caution is advised if GFR < 30 mL/min due to potential altered biodistribution. |
| Liver impairment | No specific dose adjustments are recommended for hepatic impairment; use caution in severe hepatic dysfunction (Child-Pugh class C) as safety has not been established. |
| Pediatric use | Weight-based dose: 3 MBq/kg (0.08 mCi/kg) with a minimum of 10 MBq (0.27 mCi) and a maximum of 111 MBq (3 mCi), administered intravenously. |
| Geriatric use | No specific dose adjustments are required; use the same dose as for younger adults, considering age-related decline in renal function and potential comorbidities. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for INDIUM IN-111 PENTETREOTIDE KIT (INDIUM IN-111 PENTETREOTIDE KIT).
| Breastfeeding | No data on excretion in breast milk. The radioactive indium-111 may be present in milk. Interrupt breastfeeding for at least 2-3 days after administration. No M/P ratio available. |
| Teratogenic Risk | Pregnancy Category C. Radiation exposure from indium-111 may cause fetal harm. Risk of teratogenic effects is highest during organogenesis (first trimester) and the second trimester. Use only if benefit outweighs risk. |
| Fetal Monitoring |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to pentetreotide or any component of the kit"]
| Precautions | ["Risk of hypersensitivity reactions including anaphylaxis","Radiation exposure risk","False-negative results may occur in tumors with low somatostatin receptor density"] |
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| Monitor fetal radiation dose; consider cumulative radiation exposure. Assess pregnancy status before administration. For inadvertent exposure, consult radiation safety officer. |
| Fertility Effects | Radiation exposure may impair fertility, especially with repeated doses. Gonadal radiation dose is significant; consider potential for temporary or permanent infertility. |