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ACETAMINOPHEN
ACETAMINOPHEN
Acetaminophen is the active metabolite of
phenacetin and is responsible for its analgesic
effect
• Phenacetin, a prodrug that is metabolized to
acetaminophen, is more toxic than its active
metabolite
...
But more active on COX in
CNS
...
• It does not affect PLATELET function or increase
Bleeding Time
...
• In contrast to aspirin, paracetamol does not
stimulate respiration or affect acid-base
balance;
• does not increase cellular metabolism
...
• It does not affect platelet function or clotting
factors
...
• A portion of acetaminophen is hydroxylated to
form N-acetyl-p-benzoquinoeimine /NAPQI
( a highly reactive metabolite that can react with
sulfhydryl groups and cause liver damage)
• At NORMAL doses,
NAPQI reacts with sulfhydryl group of GULTATHIONE
(produced by liver) -----forming a Non-Toxic Substance
...
With toxic doses or liver disease, the half-life may be
increased twofold or more
...
• ROUTE OF ADMINSTRATION :IV & rectal formulation-
ADVERSE EFFECTS:At normal therapeutic doses ---few adverse effect
• At large doses , GULTATHIONE in the liver depleted
NAPQI reacts with the sulfhydryl group of hepatic proteins
...