test 7 acetaminophen Flashcards
Acetaminophen (Paracetamol, APAP, Tylenol, Tempra)
o not considered to be an NSAID.
o Its exact mechanism of action is not completely understood.
o It inhibits prostaglandin synthesis in the CNS. This explains its antipyretic (fever) and analgesic properties.
o Acetaminophen does not affect platelet function or bleeding time
Acetaminophen effectiveness on COX activity
o Acetaminophen has less effect of COX activity in peripheral tissues due to inactivation. This accounts for its WEAK anti-inflammatory effects.
Acetaminophen therapeutic uses
o It’s a suitable substitute for analgesic and antipyretic relief for those with GI complaint risk. Acetaminophen is the drug of choice for children with viral infections and chicken pox.
Acetaminophen Pharmacokinetics
o Under normal conditions, acetaminophen is conjugated in the liver to form inactive metabolites.
o A small fraction is hydroxylated to form N-acetyl-p-benzoquinone imine (NAPQI), which is a reactive metabolite that can react with sulfhydryl groups and cause damage.
o At normal doses of acetaminophen, NAPQI reacts with the sulfhydryl groups of glutathione (anti-oxidant), forming a non-toxic metabolite.
- inhibits phospholipases
large doses of acetaminophen
- glutathione levels in the liver become depleted, and NAPQI reacts with the sulfhydryl groups of liver proteins, causing necrosis.
Patients with liver disease, viral hepatitis, or alcoholics and use of acetaminophen
- increased risk of acetaminophen induced
hepatotoxicity.