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AI-Generated response:

What are examples of ester local anesthetics and how are they metabolized?

Answer generated on June 4, 2024

The AI-generated responses are for illustration purposes only and should not be used for medical purposes.

Examples of ester local anesthetics include proparacaine, tetracaine, and chloroprocaine.

These anesthetics are metabolized primarily by plasma esterases.

  • Proparacaine is metabolized to para-aminobenzoic acid (PABA), which can cause hypersensitivity reactions in susceptible individuals.[1]

  • Tetracaine is also metabolized by plasma esterases, and caution is advised in patients with pseudocholinesterase deficiency due to the risk of toxic concentrations.[2]

  • Chloroprocaine is rapidly metabolized in plasma by hydrolysis of the ester linkage by pseudocholinesterase, producing ß-diethylaminoethanol and 2-chloro-4-aminobenzoic acid.[3]

Additional info

When prescribing ester local anesthetics, it is crucial to consider the patient's metabolic profile, especially their pseudocholinesterase activity, as deficiencies can lead to prolonged and potentially toxic effects of the anesthetic. Additionally, hypersensitivity to PABA, a common metabolite of ester anesthetics, should be screened for to prevent allergic reactions. These considerations are vital for ensuring patient safety and effective anesthesia management.

References

Reference 1

1.

Elsevier ClinicalKey Drug Monograph

Content last updated: September 5, 2023.

Contraindications And Precautions Ophthetic is contraindicated for use in patients with a known hypersensitivity to any component of the solution. Ophthetic is a local ester anesthetic and should not be used in patients with an ester local anesthetic hypersensitivit y. Also, ester-type local anesthetics, such as ophthetic, are metabolized to para-aminobenzoic acid (PABA) and should not be used in patients with para-aminobenzoic acid, PABA hypersensitivity.

Contraindications And Precautions Alcaine is contraindicated for use in patients with a known hypersensitivity to any component of the solution. Alcaine is a local ester anesthetic and should not be used in patients with an ester local anesthetic hypersensitivit y. Also, ester-type local anesthetics, such as alcaine, are metabolized to para-aminobenzoic acid (PABA) and should not be used in patients with para-aminobenzoic acid, PABA hypersensitivity.

Contraindications And Precautions Proparacaine is contraindicated for use in patients with a known hypersensitivity to any component of the solution. Proparacaine is a local ester anesthetic and should not be used in patients with an ester local anesthetic hypersensitivit y. Also, ester-type local anesthetics, such as proparacaine, are metabolized to para-aminobenzoic acid (PABA) and should not be used in patients with para-aminobenzoic acid, PABA hypersensitivity.

Contraindications And Precautions Parcaine is contraindicated for use in patients with a known hypersensitivity to any component of the solution. Parcaine is a local ester anesthetic and should not be used in patients with an ester local anesthetic hypersensitivit y. Also, ester-type local anesthetics, such as parcaine, are metabolized to para-aminobenzoic acid (PABA) and should not be used in patients with para-aminobenzoic acid, PABA hypersensitivity.

Contraindications And Precautions Ocu-Caine is contraindicated for use in patients with a known hypersensitivity to any component of the solution. Ocu-Caine is a local ester anesthetic and should not be used in patients with an ester local anesthetic hypersensitivit y. Also, ester-type local anesthetics, such as ocu-caine, are metabolized to para-aminobenzoic acid (PABA) and should not be used in patients with para-aminobenzoic acid, PABA hypersensitivity.

Reference 2

2.

Elsevier ClinicalKey Drug Monograph

Content last updated: November 1, 2023.

Contraindications And Precautions Ester-type local anesthetics, like lidocaine; tetracaine, should be used cautiously, if at all, in patients with low plasma concentrations of pseudocholinesterase (e.g., pseudocholinesterase deficiency). Tetracaine, an ester-type local anesthetic, is metabolized by plasma esterases. Patients with pseudocholinesterase deficiency are at a greater risk of developing toxic tetracaine concentrations.

Reference 3

3.

Food and Drug Administration (DailyMed).

Publish date: February 5, 2022.

Clinical Pharmacology The in vitro plasma half-life in neonates is 43 ± 2 seconds. Chloroprocaine is rapidly metabolized in plasma by hydrolysis of the ester linkage by pseudocholinesterase. The hydrolysis of chloroprocaine results in the production of ß-diethylaminoethanol and 2-chloro-4-aminobenzoic acid, which inhibits the action of the sulfonamides (see PRECAUTIONS ). The kidney is the main excretory organ for most local anesthetics and their metabolites. Urinary excretion is affected by urinary perfusion and factors affecting urinary pH.

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