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General Description:

Pentetic acid, identified by CAS number 67-43-6, is a notable compound with significant therapeutic applications. Pentetic acid, 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.

Indications:

This drug is primarily indicated for: 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. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Pentetic acid undergoes metabolic processing primarily in: Pentetic acid and its derivatives present a very minimal metabolism in the body. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Pentetic acid are crucial for its therapeutic efficacy: 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. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Pentetic acid is an important consideration for its dosing schedule: In preclinical studies, DTPA has been shown to present a very short half-life of 18.5-31.8 min after intravenous administration. This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Pentetic acid exhibits a strong affinity for binding with plasma proteins: 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. This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Pentetic acid from the body primarily occurs through: 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. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Pentetic acid is distributed throughout the body with a volume of distribution of: The volume of distribution of DPTA is 17 L. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Pentetic acid is a critical factor in determining its safe and effective dosage: Pentetic acid 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. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Pentetic acid exerts its therapeutic effects through: 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. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Pentetic acid functions by: 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. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Pentetic acid belongs to the class of organic compounds known as pentacarboxylic acids and derivatives. These are carboxylic acids containing exactly five carboxyl groups, classified under the direct parent group Pentacarboxylic acids and derivatives. This compound is a part of the Organic compounds, falling under the Organic acids and derivatives superclass, and categorized within the Carboxylic acids and derivatives class, specifically within the Pentacarboxylic acids and derivatives subclass.

Categories:

Pentetic acid is categorized under the following therapeutic classes: Acetates, Acids, Acyclic, Amines, Antidotes, Chelating Agents, Compounds used in a research, industrial, or household setting, Drugs that are Mainly Renally Excreted, Iron Chelating Agents, Lead Chelating Activity, Lead Chelator, Polyamines, Protective Agents, Sequestering Agents. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.

Experimental Properties:

Further physical and chemical characteristics of Pentetic acid include:

• Water Solubility: Highly soluble
• Melting Point: 219-220 ºC
• Boiling Point: Decomposes
• logP: -4.90
• pKa: pentabasic (1.5-10.6)