Analgesic Drugs Flashcards
Acetaminophen chemical name
N-acetyl-para-aminophenol
Acetaminophen INN
Paracetamol
Paracetamol USAN
Acetaminophen
Phenacetin can cause various toxic effects:
▪ Hemolytic anemia
▪ Cancer
▪ Kidney failure
▪ Methemoglobinemia
One of the most common drugs that is involved in suicide attempts and accidental poisoning.
Acetaminophen
Uses of acetaminophen
Analgesic & Antipyretic
T/F: Acetaminophen is an NSAID
FALSE
It is a weak COX-1 and COX-2 inhibitor
Acetaminophen
Active toxic metabolite of acetaminophen
N-acetyl-p-benzoquinone imine (NAPQI) or NAPBQI
Major metabolism pathway of acetaminophen
Glucuronidation
Fatal dose of acetaminophen
15 g (30 tablets)
Acetaminophen overdose during pregnancy has been associated with
fetal death and spontaneous abortion
Acetaminophen acute ingestion of __________ in children is potentially hepatotoxic.
more than 140 mg/kg
Acetaminophen acute ingestion of __________ in adults is potentially hepatotoxic.
6 g
Children < 10-12 yrs. old are ______ susceptible due to smaller contribution of cytochromeP-450 to acetaminophen metabolism.
LESS
Ingestion of 15 g of acetaminophen may be fatal, death being caused by
severe hepatotoxicity with centrilobular necrosis
Ingestion of 15 g of acetaminophen may be fatal, death being caused by severe hepatotoxicity with centrilobular necrosis, sometimes associated with ____________________.
acute renal tubular necrosis
Early after acute acetaminophen overdose
Anorexia, Nausea/Vomiting
After 24-28 hours of acetaminophen overdose
• Prothrombin time and transaminase levels rise
• Hepatic necrosis is evident
acute hepatic failure, encephalopathy, and death is collectively known as
Fulminant hepatic failure
Falsely elevated acetaminophen levels may occur in the presence of _______________
high levels of salicylate
Spontaneous vomiting due to acetaminophen overdose may delay the administration of antidote and charcoal and should be treated with ___________
Metoclopramide
may be necessary for massive hepatic failure
Liver transplant
Antidote for acetaminophen overdose
N-acetylcysteine, 140 mg/kg orally
Brand names of NAC available as IV
Acetadote
Brand names of NAC available as oral
Mucomyst
Acetaminophen will be metabolized by the enzyme CYP450, specifically ______
2E1
removes acetaminophen from blood effectively
Hemoperfusion
uses cartridge containing activated charcoal
Hemoperfusion
These are chemically diverse group of agents that share similar pharmacologic properties and are widely used for control of pain and inflammation.
NSAIDs
Overdose by most of the agents (NSAIDs) in this group usually produces only ________
mild gastrointestinal upset
Pepto-Bismol (bismuth subsalicylate) is used for
Ulcer
Before the introduction of child-resistant containers, _____________ was one of the leading causes of accidental death in children
salicylate overdose
Dose of aspirin used as analgesic and antipyretic
650 mg - 4 g
Dose of aspirin used as anti-inflammatory
4-8 g
Dose of aspirin used as antiplatelet
75-81 mg
________________ leading to respiratory alkalosis, metabolic acidosis contributing to dehydration
Hyperventilation
Characterized by low level of carbon dioxide in the blood. Happens only during hyperventilation
Respiratory alkalosis
Blood test that measures how long it takes for a person’s blood to clot.
Prothrombin time (PTT)
Average therapeutic single dose of aspirin
10 mg/kg
Usual daily therapeutic dose of aspirin
40-60 mg/kg/d
Aspirin acute ingestion of ________ will produce mild intoxication
150-200 mg/kg
Aspirin acute ingestion of ________ will produce severe intoxication
300-500 mg/kg
Chronic intoxication of aspirin may occur with ingestion of
more than 100 mg/kg/d for 2 or more days
Plasma concentration of aspirin that may cause tinnitus
50 mg/dL
Plasma concentration of aspirin that may cause anti-inflammatory uricosuric
20 mg/dL
Severe intoxication of salicylates causes
Coma, seizures, hypoglycemia, hyperthermia, and pulmonary edema
Salicylate overdose caused death by
CNS failure and cardiovascular collapse
Salicylism effects
vomiting, tinnitus, decreased hearing, and vertigo
more common with acute intoxication of salicylates
Cerebral and pulmonary edema
increases brain salicylate concentration and worsening toxicity
Systemic acidemia
Chronic therapeutic concentrations in arthritis patients range from
100 to 300 mg/L (10-30 mg/dL)
A level greater than 600 mg/L (60 mg/dL) accompanied by ________
acidosis and altered mental status
Treat metabolic acidosis with
intravenous sodium bicarbonate
Replace fluid and electrolyte deficits caused by vomiting and hyperventilation with
intravenous crystalloid solutions
Monitor asymptomatic patients for a minimum of ______
6 hours