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Pharmacology > Aspiring, NSAIDs, and Acetaminophen > Flashcards

Aspiring, NSAIDs, and Acetaminophen Flashcards

1
Q

function of NSAIDs

A

inhibit COX-1 and COX-2

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2
Q

how does aspirin inhibit function of COX-1 and COX-2

A

it covalently modifies the enzyme

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3
Q

how does NSAIDs inhibit COX-1 and COX-2

A

competes for the active site of cyclooxygenase (competitive inhibitor)

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4
Q

how does Acetaminophen inhibit COX-1 and COX-2

A
  • interfers with the oxidative state of cyclooxygenase site

- inhibition impaired by “peroxide tone”

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5
Q

acetaminophen metabolites can form a conjugation with arachidonate acid in the brain to yield

A

a neuroactive metabolite
-or inhibition of the nitric oxide pathway mediated by a variety of neurotransmitter receptors including N-methyl-D-aspartate and substance P

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6
Q

general properties of NSAIDs

A
  • anti-inflammatory
  • analgesia (inability to feel pain)
  • antipyresis
  • gastric erosion
  • cause renal dysfunction, impair renal function
  • variable effect on platelet aggregation; increase cardiovascular pathologic events due to COX-2 inhibition
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7
Q

side effects of NSAID therapy

A
  • gastric and intestinal ulceration
  • anemia from resultant blood loss
  • local irritation from drugs (organic acids) plus removal of PGE2 and PGI2 cytoprotective effects (less mucous covering GI)
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8
Q

how should patients at risk of GI toxicity be managed

A

-given celecoxib or other NSAID co-administered with a proton pump inhibitor or the PGE1 analong misoprostol

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9
Q

All NSAIDs have what effect on the cardiovascular system

A
  • prothrombotic effects that increase risk of stroke, TIA, symptomatic coronary artery disease
  • symptomatic peripheral vascular disease (COX-2 inhibition)
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10
Q

All NSAIDs can exacerbate

A

hypertension

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11
Q

what is the safest NSAIDs

A

naproxen bc it has the lowest cardiovascular toxicity effects

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12
Q

what are the adverse effects of NSAIDs on the renal system

A
  • decrease renal blood flow and GFR in patients with congestive heart failure, liver disease (ascites); chronic renal disease; or those who are hypovolemic or dehydrated
  • promote salt and water retention by producing PG-induced inhibition of both the reabsorption of chloride and the action of ADH
  • may cause increased intravascular volume/edema
  • analgesic nephropathy
  • idiosyncratic and dose-related hepatic injury
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13
Q

symptoms of aspirin “intolerance”

A

-vasomotor rhinitis, generalized urticaria (hives), and bronchospasm, laryngeal edema and bronchoconstriction, flushing, hypotension and shock

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14
Q

aspirin “intolerance” occurs in pts with

A
  • nasal polyps, asthma, and chronic urticaria

- asthma may be induced or exacerbated in such patients

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15
Q

what is the mechanism of aspirin intolerance

A
  • defect in mast cell histamine storage/shunting or arachidonic acid to lipoxygenase pathway
  • nonimmunologic mechanism
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16
Q

effects of aspirin in pregnancy

A
  • prolong labor

- promote premature closure of ductus arteriosus

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17
Q

common drug interactions of NSAIDs

A
  • prolong bleeding time (warfarin; heparin)
  • increase the ulcerogenic effects of glucocorticoids
  • reduce effects of diuretics and other antihypertensive agents
  • reduce lithium clearance; also methotrexate; cyclosporine; aminoglycosides
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18
Q

therapeutic uses of NSAID

A
  • relief pain and inflammation
  • reduce body temp in febrile states
  • closure of ductus arterioles
  • with antihistamines, in pts with systemic mastocytosis
  • adjunct in cancer-related hypercalcemia
  • Bartter’s syndrome
  • moderate cutaneous rxns in pts receiving niacin
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19
Q

aspirin in a — dependent pharmacokinetics

A

dose

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20
Q

MAO of aspirin

A

acetylates COX

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21
Q

what type of inhibitor is aspirin (salicylic acid)

A

competitive inhibitor

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22
Q

dose-dependent therapeutic effects of aspirin

A
  • anti-platelet effects
  • analgesia; reduction in febrile responses
  • anti-inflammatory
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23
Q

aspirin metabolism

A
  • aspirin is metabolized in plasam to yield salicylic acid

- salicylic acid is biotransformed in liver and mitochondria

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24
Q

therapeutic uses of aspirin

A

-antipyretic, analgesic, anti-inflammatory

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25
aspirin can be used as a prophlaxis of disease assocaited with
- platelet hyperaggreability (CAD; unstable angina; post_MI or stent; postoperative deep vein thrombosis; risk of stroke) - pre-eclampsia and hypertension indued by pregnancy
26
adverse effects of aspirin
- gastric irritation, ulceration, erosion, hemorrhage - increased bleeding time (2X for 4-7 days) - decreased renal function in patients at risk - hepatic injury (usually with larger doses associated with treatment of RA)
27
low doses of aspirin inhibits
uric acid excretion
28
large doses of aspirin promotes
uric acid excretion
29
10 mg/dl of aspirin causes
analgesia, antipyretic, anti-platelet; gastric intolerance/bleeding, hypersensitivity
30
10-49 mg/dl of aspirin causes
anti-inflammatory, uricosuric
31
50-80 mg/dl of aspirin causes
mild intoxication; tinnitus, central hyperventilation
32
80-100 mg/dl causes
moderate intoxication; fever, dehydration, metabolic acidosis
33
110-160 mg/dl of aspirin causes
severe intoxication; hypoprothrombinemia, vasomotor instability; coma
34
>160 mg/dl of aspirin causes
lethal blood levels; renal and respiratory failure
35
what is salicylism
aspirin overdose
36
effects of salicylism
-confusion; tinnitus, dizziness
37
how does salicylism affect respiration
- contributes to acid-base disturbances - stimulation via uncoupling of oxidative phosphorylation - direct stimulation of respiratory centre - toxic doses suppress respiration
38
what metabolic effects does salicylism have
- increases uncoupling - inhibit aerobic respiration - release epinephrine - reduces lipogenesis - large doses stimulate glucocorticoid secretion
39
uncoupling of oxidative phosphorylation causes
increase of O2 consumption and CO2 production
40
toxic doses of aspirin inhibit aerobic respiration leading to
accumulation of pyretic, lactic and acetoacetic acids
41
aspirin promotes epinephrine release which promotes
hyperglycemia and depletes muscle and hepatic glycogen
42
aspirin reduces lipogenesis which causes
increase in oxidation of F/A
43
full therapeutic dose of aspirin produces respiratory alkalosis, how does compensation occur
-increase renal excretion of bicarbonate, accompanied by increased Na+ and K+ excretion
44
extreme metabolic acidosis is caused by
- salicylate accumulation - renal dysfunction with accumulation of organic acids - derangement of carbohydrate metabolism
45
what is Acetaminophen (Tylenol)
an effective antipyretic and analgesic
46
does Acetaminophen have anti-inflammatory effects
very little
47
Acetaminophen does not effect the --- and ---
GI tract | platelets
48
main toxicity of Acetaminophen is directed toward
liver
49
mechanism of action of Acetaminophen
-inhibits cyclooxygenase, by altering oxidate state of active site
50
ability of Acetaminophen to inhibit cylooxygengase is impaired in the presence of
peroxides (ie. inflammation)
51
ability of Acetaminophen to inhibit cylooxygenase is enhanced in the presence of
high [ ] of antioxidants (ie. brain)
52
experimental demonstration of novel metabolite of acetaminophen in
CNS which inhibits COX and stimulates TRPV1 receptor or possible interference with nitric oxide pathway and interface with central neurotransmitters
53
Large dose of Acetaminophen (>7.5 g) may cause
hepatotoxicity
54
hepatotoxicity of acetaminophen is mediated by
a metabolite formed by P450, which is normally inactived by glutathione
55
hepatotoxic dose may be substantially smaller in individuals with
preexisting liver disease or who consume alcohol regularly
56
acetaminophen over dose is the most common cause of
-acute liver failure 50% of adults 13% of pediatric cases
57
treatment of acetaminophen toxicity
N-Acetylcysteine
58
administration of N-Acetylcysteine is based on
a nonogram derived from time-dependent acetaminophen [ ] data generated in adults with a single, acute ingestions of drug who presented to medical centres with 24 h of the overdose
59
FDA issued manufactuers of TC pain delivers and fever reducers to revise their labelling to include warnings about potential safety risks. Products covered by the FDA action included
``` -acetaminophen (in a class by itself) NSAIDs -aspirin -ibuprofen -naproxen -ketoprofen ```
60
acetaminophen prescription products limited to
325 mg per dose
61
what were the changes in Aceaminophen dosing regulations and warnings
- require boxed warning highlighting the potential for liver injury, as well as allergic runs - used in many combination products; label abbreviations are currently not standardized

Pharmacology (23 decks)

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