What drugs are hydrolyzed by pseudocholinesterase (also known as butyrylcholinesterase)?

From the Guidelines

Pseudocholinesterase breaks down several important medications, including succinylcholine, mivacurium, and certain ester-type local anesthetics, with succinylcholine being the most notable due to its potential for prolonged muscle paralysis and respiratory compromise in patients with pseudocholinesterase deficiency. The primary drugs metabolized by pseudocholinesterase include:

• Succinylcholine (a depolarizing neuromuscular blocking agent used in anesthesia) 1
• Mivacurium (a non-depolarizing neuromuscular blocking agent) 1
• Cocaine
• Procaine
• Chloroprocaine
• Tetracaine
• Certain ester-type local anesthetics Additionally, pseudocholinesterase is involved in the metabolism of some organophosphate compounds. This enzyme works by hydrolyzing ester bonds in these medications, rendering them inactive. Patients with pseudocholinesterase deficiency, either genetic or acquired, may experience prolonged effects from these medications, particularly succinylcholine, which can lead to extended muscle paralysis and respiratory compromise 1. This is clinically significant in anesthesia practice, where patients with known or suspected enzyme deficiency should receive alternative medications when possible, as noted in guidelines for the determination of brain death in infants and children 1 and clinical practice guidelines for sustained neuromuscular blockade in the adult critically ill patient 1. The deficiency can be inherited as an autosomal recessive trait or acquired through liver disease, malnutrition, pregnancy, burns, or certain medications that inhibit the enzyme. It is essential for physicians to be aware of the total amounts of administered medication that can affect drug metabolism and levels, especially in critically ill patients 1. In some instances, this may require waiting several half-lives and rechecking serum levels of the medication before conducting the brain death examination 1.

From the FDA Drug Label

Succinylcholine is rapidly hydrolyzed by plasma cholinesterase to succinylmonocholine (which possesses clinically insignificant depolarizing muscle relaxant properties) and then more slowly to succinic acid and choline Because ester-type local anesthetics such as NOVOCAIN are hydrolyzed by plasma cholinesterase produced by the liver and excreted by the kidneys, these drugs, especially repeat doses, should be used cautiously in patients with hepatic disease NOVOCAIN is readily absorbed following parenteral administration and is rapidly hydrolyzed by plasma cholinesterase to para-aminobenzoic acid and diethylaminoethanol

The drugs that are broken down by pseudocholinesterase (also known as plasma cholinesterase) are:

• Succinylcholine 2
• Procaine (also known as Novocain) 3 3

From the Research

Drugs Broken Down by Pseudocholinesterase

• Succinylcholine: a muscle relaxant drug that is hydrolyzed by pseudocholinesterase 4, 5, 6, 7, 8
• Mivacurium: a neuromuscular blocking drug that is metabolized by pseudocholinesterase 4, 5, 6, 7, 8

Characteristics of Pseudocholinesterase Deficiency

• Pseudocholinesterase deficiency is a rare genetic or acquired disorder that affects the body's ability to metabolize choline esters such as succinylcholine and mivacurium 5, 6, 7
• Deficiency can lead to prolonged apnea and paralysis following administration of succinylcholine and mivacurium 4, 5, 6, 7, 8
• Patients with pseudocholinesterase deficiency may require mechanical ventilation and sedation until they are strong enough to be safely extubated 4, 8