Cholinesterase (Pseudocholinesterase) and Dibucaine Inhibition

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Cholinesterase (Pseudocholinesterase) and Dibucaine Inhibition

Definition

  • Cholinesterase is an enzyme that catalyzes the hydrolysis of the neurotransmitter Ach into choline and acetic acid, a reaction necessary to allow a cholinergic neuron to return to its resting state after activation.
  • Serum cholinesterase, often called pseudocholinesterase or PChE, is distinguished from acetylcholinesterase (AChE or "true cholinesterase " пїЅ) by both location and substrate. PChE is found primarily in the liver. AChE, also known as RBC cholinesterase, erythrocyte cholinesterase, or Ach acetylhydrolase, is found primarily in the blood and neural synapses.
  • The difference between the two types of cholinesterase has to do with their respective preferences for substrates: AChE hydrolyzes Ach more quickly, and PChE hydrolyzes butyrylcholine more quickly.
  • Phenotype interpretation is based on the total PChE activity and the percent of inhibition caused by dibucaine. Although there are >25 different phenotypes, most are extremely rare. Patients with unusual phenotypes cannot metabolize succinylcholine or mivacurium in the normal fashion; therefore, these patients can have prolonged paralysis following the use of these drugs.
  • Other names: choline esterase II, SChE, Ach acylhydrolase, butyrylcholinesterase (BChE), dibucaine inhibition, and plasma cholinesterase.
  • Normal range: Pseudocholinesterase, total: 2,900 " пїЅ7,100 U/L Dibucaine inhibition: 70 " пїЅ90% (congenital deficiency 18 " пїЅ20%)
  • PChE is found primarily in the liver.
  • AChE, also known as RBC cholinesterase, erythrocyte cholinesterase, or Ach acetylhydrolase, is found primarily in the blood and neural synapses.
  • Pseudocholinesterase, total: 2,900 " пїЅ7,100 U/L
  • Dibucaine inhibition: 70 " пїЅ90% (congenital deficiency 18 " пїЅ20%)

Use

  • Monitoring exposure to organophosphorus insecticides
  • Monitoring patients with liver disease, particularly those undergoing liver transplantation
  • Identifying patients who are homozygous for the atypical gene and have low levels of PChE that are not inhibited by dibucaine
  • Identifying patients, who are heterozygous for the atypical gene and have lower than normal levels of PChE and varying levels of inhibition with dibucaine

Interpretation

Increased In

  • Type IV hyperlipoproteinemia
  • DM
  • Hyperthyroidism
  • Insecticide exposure (organophosphates)
  • Nephritic syndrome
  • Psychosis
  • Breast cancer

Decreased In

  • Genetic PChE variants
  • Severe pernicious anemia (PA), aplastic anemia
  • Cirrhosis
  • CHF (causing liver disease)
  • Hepatic carcinoma
  • Malnutrition
  • Acute infections and burns
  • AMI, pulmonary embolism
  • Muscular dystrophy
  • After surgery
  • Chronic renal disease

Limitations

  • PChE levels are not to be confused with AChE levels. PChE levels are earlier indicators than AChE levels of organophosphate exposure.
  • Patients with normal PChE activity show 70 " пїЅ90% inhibition by dibucaine, whereas patients homozygous for the abnormal allele show little or no inhibition (0 " пїЅ20%) and usually low levels of enzyme. Heterozygous patients have intermediate PChE levels and response to inhibitors.
  • Dibucaine inhibition is no value over total PChE, for the diagnosis of organophosphorus pesticide exposure.
  • Anabolic steroids, carbamates, cyclophosphamide, estrogens, glucocorticoids, lithium, neuromuscular relaxants, oral contraceptives, organophosphorus insecticides, and radiographic agents decrease the circulating levels.
  • Serum separator tubes, citrate anticoagulants, detergents, and heavy metals also decrease the serum levels.