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NSAIDs
N/A
78
Pharmacology
Professional
04/30/2011

Additional Pharmacology Flashcards

 


 

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Term
salicylates
Definition
non-specific COX 1/2 inhibitors
Term
indole acetic acids
Definition
non-specific COX 1/2 inhibitors
Term
propionic acid
Definition
non-specific COX 1/2 inhibitors
Term
anthranilic acid
Definition
non-specific COX 1/2 inhibitors
Term
phenyl acetate
Definition
non-specific COX 1/2 inhibitors
Term
pyrazolone
Definition
non-specific COX 1/2 inhibitors
Term
oxicam
Definition
non-specific COX 1/2 inhibitors
Term
celecoxib (Celebrex)
Definition
specific COX 2 inhibitor
Term
meloxicam (Mobic)
Definition
specific COX 2 inhibitor
Term
possible COX 3 inhibitor
Definition
acetaminophen (Tylenol)
Term
non-NSAID antipyretic/analgesic
Definition
acetaminophen (Tylenol)
Term
major actions of NSAIDs
Definition
analgesia
antipyretic
anti-inflammatory
Term
common mechanism of action for NSAIDs
Definition
inhibit COX

COX is a key enzyme responsible for synthesis of prostaglandins which contribute to a number of inflammatory processes
Term
COX-1 is _________ active.
Definition
constituitively (always)
Term
COX-2 is ________ and is associated with disease states.
Definition
inducible (by cytokines and other inflammatory mediators)
Term
Traditional NSAIDs inhibit...
Definition
both COX-1 and COX-2
Term
Aspirin _______ inhibits COX-1 and COX-2.
Definition
covalently/irreversibly
Term
Recovery of COX in must tissues is by...
Definition
synthesis of new enzyme
Term
Why is platelet inhibition irreversible?
Definition
platelets cannot synthesize new COX
Term
Other NSAIDs (besides aspirin) produce ______ inhibition of COX.
Definition
reversible
Term
What drugs are used for patients who need NSAID-like activity but do not want GI risks/upset?
Definition
selective COX-2 inhibitors
(celecoxib, meloxicam)
Term
Selective COX-2 inhibitors do/do not affect platelets and bleeding time.
Definition
do not
Term
selective COX-2 inhibitor contraindications
Definition
aspirin allergy
3rd trimester pregnancy
Term
selective COX-2 inhibitor indications
Definition
dysmenorrhea
osteoarthritis
RA
acute post-op pain
Term
black box warning on all NSAIDs
Definition
cardiovascular risk
Term
COX-2 possible links to cardiac disease
Definition
1. COX-2 reduced prostacycline (PGI2) production by vascular endothelium with little or no inhibition of potentially prothrombotic platelet thromboxane A2

2. COX inhibition in general is associated with elevations in blood pressure
Term
Why are some other NSAIDs marginally superior to aspirin?
Definition
-more potent
-more efficacious at tolerated doses
-cause less GI irritation and other side effects
-longer duration of action so taken less frequently
Term
disadvantages of newer NSAIDs over aspirin
Definition
-more expensive
-some are more toxic
Term
What enzyme is responsible for sensitizing pain nerve ending to the action of bradykinin, histamine, and substance P?
Definition
PGE2 (prostaglandin E2)
Term
Aspirin blocks...
Definition
PGE2 formation
Term
NSAIDs are _____ analgesics effective against pain of _________________ intensity.
Definition
mild
low-to-moderate
Term
What conditions can NSAIDs be superioor to intermediate efficacy opioids for?
Definition
post-op pain
pain associated with inflammation
Term
What provides greater pain nrelief than intermediate opioids alone?
Definition
NSAID + opioid
Term
Efficacy of pain relief provided by NSAIDs is higher/lower than with high-efficacy opioids.
Definition
lower
Term
What opioid effects do NSAIDs lack?
Definition
-respiratory depression
-development of physical tolerance/dependence
Term
What type of pain is relieved and not relieved by NSAIDs?
Definition
relieved: integumental structures
not relieved: hollow viscera
Term
What causes fever?
Definition
pyrogens (cytokines) from lymphocytes act on hypothalamus to increase body temp
Term
What type of drugs can suppress fever?
Definition
NSAIDs that cross the BBB
Term
Describe the anti-inflammatory effects of NSAIDs.
Definition
inhibit formation of PGE2 and PGI2, which are important mediators of localized erythema and edema

also inhibit activation and function of inflammatory cells, may stabilize lysosomal membranes, and inhibit phagocytosis
Term
PGE2 inhibits...
Definition
gastric acid secretion
Term
PGE2, PGF2alpha, and PGI2 stimulate...
Definition
synthesis of bicarbonate and mucous
Term
PGE2 promotes mucosal ____________.
Definition
blood flow
Term
What causes the GI irritation associated with NSAID use?
Definition
inhibition of all of the effects of prostaglandins (PGE2) and prostacyclin (PGI2)
Term
GI side effects of NSAIDs
Definition
epigastric distress
nausea/vomiting
microhemorrhage
ulceration
anemia
Term
aspirin effect on platelets
Definition
low doses irreversibly inhibit COX and platelet aggregation for the life of the platelet (8-11 days)
Term
Low dose aspirin together with diet and exercise is useful for the prophylaxis of...
Definition
-coronary artery disease
-DVT
-unstable angina
-prophylaxis and treatment of MI and stroke
Term
What situations can cause NSAIDs to reduce renal blood flow?
Definition
high levels of circulating vasoconstrictors

-compensated CHF
-chronic renal disease
Term
What type of effect to NSAIDs have on hypertensive regimens?
Definition
reduce effectiveness
(retention of sodium and water)
Term
NSAID and COX-2 cautionary conditions
Definition
reduced renal function
heart failure
liver dysfunction
ACE inhibitors
diuretics (esp. in elderly)
Term
What can the use of aspirin and salicylates during infection with chicken pox, varicella, and influeza viruses cause?
Definition
Reye's syndrome
Term
major salicylate contraindication
Definition
children or adolescents with chicken pox or varicella (Reye's syndrome)
Term
What does Reye's syndrome cause?
Definition
liver damage
encephalopathy
Term
therapeutic uses for analgesic-antipyretics
Definition
pain and fever of low-to-moderate intensity
Term
NSAIDs other than aspirin are typically used for....
Definition
chronic treatment

(ibuprofen or naproxen)
Term
NSAIDs suppress the clinical signs in __________, but subsequent tissue damage is not halted.
Definition
rheumatic disease
Term
NSAIDs do not induce _________.
Definition
remission
Term
What NSAID is often used to stimulate closure of a patent ductus arteriosus?
Definition
indomethacin
Term
indomethacin mechanism of action in PDA
Definition
inhibition of PGE2 which keeps the ductus arteriosus open
Term
What condition is currently under research for the use of COX-2 inhibitors?
Definition
familial adenomatous polyposis (FAP)

studies show reduction in number of polyps with COX-2 inhibitors
Term
NSAID adverse effects
Definition
GI irritation
prolonged bleeding time
hypersensitivity reactions
Reye's syndrome
salicylism
Term
How long should a patient be off of aspirin products before having surgery?
Definition
one week
Term
conditions that predispose you to having hypersensitivity reaction
Definition
asthma
nasal polyps
chronic urticaria
Term
NSAID drug interactions
Definition
actacids
phenytoin, thyroxine, thiopental
anticoagulants (risk of bleeding)
uricosuric effect in gout pts
Term
salicylism
Definition
mild NSAID toxicity
Term
symptoms of salicylism
Definition
nausea/vomiting
tinnitus
hyperventilation
headache
confusion
dizziness
Term
symptoms of NSAID overdose
Definition
*acute medical emergency*

fever, dehydration, delerium, hallucination, convulsions, coma, respiratory/metabolic acidosis, death

children especially vulnerable
Term
NSAID adverse effects during pregnancy
Definition
low birth weight
increased perinatal mortality
anemia
antepartum and postpartum hemorrhage
prolonged gestation
premature closure of ductus arteriosus
Term
What drug is more efficacious than aspirin, but its toxicity limits its usefulness?
Definition
indomethacin
Term
What drug can be used in resistant RA, gout, suppression of uterine contraction in preterm labor, and PDA?
Definition
indomethacin
Term
What drug is a potent analgesic but has weak anti-inflammatory effect?
Definition
ketorolac (Toradol)
Term
What selective COX-2 inhibitor was withdrawn from the market first?
Definition
refocoxib (Vioxx)
Term
What drug needs to be used with caution in patients taking warfarin even though it does not have effect on platelets and bleeding time?
Definition
celecoxib (Celebrex)
Term
What is acetaminophen (Tylenol) NOT used for?
Definition
inflammation
Term
mechanism of acetaminophen toxicity
Definition
depletion of glutathione
Term
adverse effects of acetaminophen
Definition
rare in therapeutic usage

occasional skin rash or allergy

OD can result in fulminant hepatic necrosis and liver failure
Term
fatal dose of acetaminophen
Definition
>10g

may be lower in chronic alcoholics of those with underlying liver disease
Term
clinical features of acetaminophen overdose
Definition
up to 24 hours: none or nausea/vomiting

>24 hours: nausea, vomiting, RUQ pain, jaundice, encephalopathy
Term
What should you consider giving for acetaminophen overdose?
Definition
n-acetylcysteine infusion
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