pharm - analgesics Flashcards
The currently accepted action of paracetamol as an antipyretic is that it:
A. Acts at GABA(B) receptors
B. Acts at mu (μ) receptors
C. Acts on the peripheral nervous system
D. Inhibits prostaglandins in the hypothalamus
E. Reduces histamine release
D. Inhibits prostaglandins in the hypothalamus
how are amides local anaesthesia metabolised?
CYP450 enzymes in liver
how are ester local anaesthesia metabolised?
tissue-associated esterases
does amide or ester LA have longer duration of action?
amides
name 2 amide drugs for LA
bupivacaine
lidocaine
name one ester drug for LA
tetracaine
overdose of which drug is associated with salicylism?
aspirin
irreversible inhibitor of COX-1 and COX-2
aspirin
what is MOA of meloxicam?
selective COX-2 inhibitor
what is the MOA of diclofenac and ibuprofen?
non-selective COX inhibitor
Binds to nuclear glucocorticoid receptor to inhibit phospholipase A2
what type of drug?
steroidal anti-inflammatory drug
name two examples of SAIDs
Dexamethasone
Prednisolone
what SAID can cause dysphonia (croaky voice)?
fluticasone
what is Azathioprine indicated in and what is its MOA?
Rheumatoid Arthritis
MOA: purine analogue –> impair lymphocyte proliferation
what drug competitively inhibits dihydrofolate reductase?
methotrexate
what is the MOA of Sulfasalazine?
reduce cytokine production
what is allopurinol indicated in?
gout
what is the MOA of allopurinol?
converted to alloxanthine by xanthine oxidase
alloxanthine is a non-competitive inhibitor of xanthine oxidase –> prevent production of uric acid from hypoxanthine and xanthine
what is the MOA of probenecid?
increase uric acid excretion by blocking reabsorption
what drug binds to tubulin and prevent polymerisation and is indicated in gout?
Colchicine
what is Naloxone and what is it indicated in?
competitive mu-receptor antagonist
treat life-threatening side effects of opioid overdose (eg. respiratory depression)
what is the pro-drug of morphine called?
codeine (weak opioid)
does loperamide have analgesic effect?
no
what is the MOA of tramadol?
Inhibits NA and 5-HT (serotonin) reuptake and weak mu-receptor agonist
