CAINDEXNAME:GUANIDINE,[(3-IODOPHENYL)METHYL]

Absorption

Iobenguane rapidly clears from the blood and is highly retained in adrenergic tissues.

Toxicity

Oral mouse: LD50 = 300 mg/kg; Oral, rabbit: LD50 = 3200 mg/kg; Oral, rat: LD50=980 mg/kg. The most common adverse reactions, dizziness, rash, pruritis, flushing, headache, and injection site hemorrhage occurred in < 1.3% of patients.

Toxicity

As a radiopharmaceutical, iobenguane I-123 carries the risk of radiation toxicity if administered in innappropriately large doses or in patients with renal insufficency [FDA Label]. Fequent voiding of the bladder is encouraged to minimize the radiation dose to the bladder.

Chemical properties

Colourless to off-white solid

The Uses of CAINDEXNAME:GUANIDINE,[(3-IODOPHENYL)METHYL]

m-Iodobenzylguanidine Hemisulfate?can be used to demethylate and oxidize membrane-associated DNA. It has also been employed to develop a cell-based high-throughput screening assay to identify anti-hepatitis C virus compounds.

Indications

Detection of primary and metastatic pheochromocytoma or neuroblastoma

Indications

For use in the diagnostic imaging of adrenergically inervated tissues for the purposes of detecting metastatic pheochromocytoma or neuroblastoma [FDA Label]. Also used to assess the sympathetic inervation of the myocardium via determination of the heart to mediastinum ratio of radioactivity in patients with New York Heart Association class II or III heart failure.

Background

Synthetic guanethidine derivative that locates phaeochromocytomas and neuroblastomas. The radioisotope used can either be iodine-123 for imaging or iodine-131 for destruction of tissues that metabolize noradrenaline. Iodine 123 is a cyclotron-produced radionuclide that decays to Te 123 by electron capture. Images are produced by a I123 MIBG scintigraphy. FDA approved on September 19, 2008.

Background

Iobenguane sulfate I-123 is a radiopharmaceutical used in gamma-scintigraphy of adrenergically inervated tissues [FDA Label].

What are the applications of Application

m-Iodobenzylguanidine hemisulfate salt is an inhibitor of arginine specific mono-ADP-ribosyltransferase

Definition

ChEBI: 2-[(3-iodophenyl)methyl]guanidine is an organoiodine compound.

Pharmacokinetics

AdreView is a diagnostic radiopharmaceutical which contains a small quantity of iobenguane that is not expected to produce a pharmacodynamic effect. Patients with renal insufficiency may experience increased radiation exposure and impaired imaging results.

Pharmacokinetics

Iobenguane I-123 is taken up by and stored in adrenergic nerve terminals allowing for the radiographic imaging of adrenergically inervated organs and tissues [FDA Label].

Metabolism

Less than 10% of the dose is metabolized into m-iodohippuric acid (MIHA). However the mechanism in which this metabolite is produced is unknown.

Metabolism

Metabolized to m-iodohippuric acid and free radioiodide [FDA Label]. The metabolism of iobenguane I-123 and the enzymes involved has not been well studied.