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NSG 531 Advanced Pharmacology
Exam 1 Questions and Correct
Answers the Latest Update
Acetaminophen (APAP) toxicity is mediated by _________ .
✓ saturated normal liver conjugation pathways followed by insufficient glutathione to
conjugate the metabolite NAPQI, which binds to hepatocellular proteins causing
oxidative damange, mitochondrial dysfunction, and hepatocellular death
What is the first step in acute overdose of acetaminophen?
✓ Metabolism by conjugation becomes saturated, and excess APAP is oxidatively
metabolized by the CYP enzymes (CYP2E1, 1A2, 2A6, and 3A4) to the hepatotoxic
reactive metabolite N-acetyl-p -benzoquinoneimine (NAPQI).
Glutathione's role in acetaminophen biotransformation
✓ Conjugates the hepatotoxic reactive metabolite N-acetyl-p -benzoquinoneimine
(NAPQI), which can then be renally excreted
Lack of glutathione or excessive NAPQI production can lead to _______ .
✓ NAPQI binding to the cysteinyl sulfhydryl groups of hepatocellular proteins, forming
NAPQI-protein adducts. This causes an ensuing cascade of oxidative damage and
mitochondrial dysfunction. The subsequent inflammatory response propagates
hepatocellular injury and death.
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True or false: the ingested amount of APAP at which toxicity may occur may be
less in the setting of chronic ethanol use, malnutrition, fasting, or viral illness.
✓ true
True or false: co-ingestions of substances or medications known to induce the
activity of the APAP-metabolizing cytochrome P (CYP) oxidative enzymes also
increase the risk of hepatotoxicity
✓ true
What is the antidote for acetaminophen poisoning?
✓ NAC, a precursor of glutathione that increases the concentration of glutathione
available for the conjugation of NAPQI. Also enhances sulfate conjugation of
unmetabolized APAP, is an anti-inflammatory and antioxidant, has positive inotropic
effects, and increases local nitric oxide concentrations for better blood flow.
A drug is ________ .
✓ an agent that affects biological processes and is given to prevent or treat diease;
most are weak acids or bases
Pharmacokinetics
✓ The quantitative study of drug absorption, distribution, metabolism, and excretion
(ADME), and their mathematical relationship; what the body does to the drug once
its administered
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