Pharm approach to pain Flashcards
what are analgesics?
drugs that relieve pain without causing loss of consciousness
what is secondary hyperalgesia?
pain caused by glutamate stimulation of spinal NMDA receptors
what are the characteristics of COX1?
expressed in all tissue
responds to physiological stimuli
responds to pathological stimuli (inflammation)
what is the COX1 pain pathway?
- inflammation stimulates AA release
- COX1 converts AA to PGE2
- PGE2 causes symptoms
what are the characteristics of COX2?
expressed in some tissue
physiological role in kidney and complements COX1
response to pathological stimuli (inflammation)
what is the COX2 pain pathway?
- inflammation induces COX2 expression
- COX2 also converts AA into PGE2
- COX2 derived PGE2 amplifies symptoms
what are the NSAIDs?
ASA ibuprofen celecoxib diclofenac inomethacin ketorolac (Toradol) naproxin (Aleve)
what is the MOA of most NSAIDs?
inhibits COX1 and COX2
which NSAID only inhibits COX2?
celecoxib
what are the adverse reactions of ASA?
GI bleeding
hemostatic defects
toxicity leading to respiratory failure
what is the toxic dose of ASA?
400-500 mcg/mL
what is the dose of ASA for antiplatelet or analgesia use?
100 mcg/mL
what is the dose of ASA for anti-inflammatory use?
150-300 mcg/mL
what is the dose of ASA for the treatment of rheumatic fever?
250-400 mcg/mL
what is the progression of ASA toxicity?
- salicylates uncouple ox phos in CNS
- resp center sees decreased ATP as hypoxemia
- hyperventilation causes respiratory alkalosis
- organic acids accumulate from Krebs cycle dysfunction
- metabolic acidosis becomes life-threatening
what are the adverse reactions of ibuprofen?
fetal renal dysfunction in pregnancy
increase risk of MI and stroke
increase risk of GI bleed
what are the adverse reactions of celecoxib?
fetal renal dysfunction in pregnancy
increase risk of MI and stroke
increase risk of GI bleed
what are the 4 major actions of ASA?
anti-inflammatory
mild to moderate pain relief
fever reduction
prevention of MI or stroke (anti-platelet)
what are the differences between ASA and other NSAIDs?
other NSAIDs:
reversible
increase the risk of MI and stroke
how is celecoxib different from ASA and other NSAIDs?
less likely to cause gastric ulceration
no risk of bleeding
increases MI and stroke risk
what are the contraindications of using NSAIDs?
CKD gastric/duodenal ulcer heart failure uncontrolled HTN allergy anticoagulant use
what are the possible MOAs of acetaminophen?
TRPV1 activator
central PG synthase inhibitor
cannabinoid receptor activator
what is the major adverse reaction of acetaminophen?
hepatotoxicity due to overdose
what are the effects of acetaminophen?
suppresses pain and fever
NOT anti-inflammatory
how do you treat acetaminophen toxicity?
acetylcysteine
who should not take acetaminophen?
people with liver disease
people who take warfarin (increased risk of bleeding)
what is the MOA of opioids?
act on central and peripheral µ, ∂ and k receptors