Diethylenetriaminepentaacetate

Diethylenetriaminepentaacetate Uses, Dosage, Side Effects, Food Interaction and all others data.

Diethylenetriaminepentaacetate, also known as diethylenetriaminepentaacetic acid (DTPA), is a synthetic polyamino carboxylic acid with eight coordinate bond forming sites that can sequester metal ions and form highly stable DTPA-metal ion complexes. DTPA, along with its calcium and zinc trisodium salts, are the only FDA approved agents for the treatment of internal contamination by transuranics. It is currently considered, in all the dosage forms, as a member of the list of approved inactive ingredients for drug products by the FDA. DPTA was developed by the pharmaceutical company CIS US and FDA approved on April 14, 2004.

There are reports in vivo of low stability of complexes of DPTA with uranium and neptunium which is being reported to cause deposition of the radionuclides into the tissues. In the case of plutonium, some preclinical studies have shown a very high urine elimination efficacy 1 hour after initial contamination. This efficacy is conserved for approximately 24 hours while the radiocontaminant is circulating. When the radionuclide is inhaled, it has been reported a DPTA-induced reduction of even 98% of the lung deposits. It is important to consider that pentetic acid can bind directly to other trace metals in the body which can cause deficiencies.

Trade Name Diethylenetriaminepentaacetate
Generic Pentetic acid
Pentetic acid Other Names Diethylene triamine pentaacetic acid, Diethylenetriamine pentaacetic acid, Diethylenetriaminepentaacetate, Diethylenetriaminepentaacetic acid, DTP-A, DTPA, Pentetate, Pentetic acid
Type
Formula C14H23N3O10
Weight Average: 393.349
Monoisotopic: 393.138343953
Protein binding

The fast clearance and very short half-life of pentetic acid suggest that this compound is very unlikely to become bound to serum proteins to any significant extent. It is reported that DPTA is negligibly bound to alpha1-antitrypsin.

Groups Approved
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Diethylenetriaminepentaacetate
Diethylenetriaminepentaacetate

Uses

DTPA is widely used in industry and medicine. As a medical agent, it is approved for its use in medical imaging and for the decorporation of internally deposited radionuclides. It is FDA approved for the treatment of individuals with known or suspected internal contamination with plutonium, americium or curium to increase the rates of elimination.

Due to the pharmacokinetic elimination by the kidneys, pentetic acid conjugated with technetium Tc-99m is being used clinically to estimate physiological parameters such as glomerular filtration rat and effective renal plasma flow.

Diethylenetriaminepentaacetate is also used to associated treatment for these conditions: Internal contamination with americium, Internal contamination with curium, Internal contamination with plutonium

How Diethylenetriaminepentaacetate works

The calcium and zinc trisodium salts of DTPA achieve the therapeutical potential by exchanging calcium and zinc cations with transuranic radionuclides to form higher affinity complexes and then promote their elimination by glomerular filtration into the urine. DTPA as an acid acts in a very similar way by sequestering ions with its eight coordinate bond forming sites.

Toxicity

Some toxicity has been reported related to administration of pentetic acid including depletion of trace metals, kidney and liver vacuolization and small bowel hemorrhage lesions.

Food Interaction

No interactions found.

Volume of Distribution

The volume of distribution of DPTA is 17 L.

Elimination Route

DTPA and its trisodium salts present a very poor bioavailability after oral administration. Therefore, the normal administration of DTPA is done by slow intravenous infusion or inhalation with a nebulizer. When inhaled, the absorption is of about 20% of the administered dose.

Half Life

In preclinical studies, DTPA has been shown to present a very short half-life of 18.5-31.8 min after intravenous administration.

Clearance

Diethylenetriaminepentaacetate presents a very rapid blood clearance which explains for the short half-life. The reported clearance rate in patients with normal renal function is 80-120ml/min.

Elimination Route

DTPA metal complexes are quickly excreted in the urine.It is predominantly excreted by the kidney and it is not excreted by non-renal routes to any significant extent.

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