Analgesics Flashcards
NSAID analgesics are given to those with what type of pain for pain relief?
Mild‐moderate pain
Severe or chronic malignant pain is treated with what type of pain relief?
opioids
fentanyl is an NSAID or opioid?
opioid
what type of receptors do Opioids bind to?
GPCRs
Most opioids are full agonists for all receptors, except: Pentazocine and buprenorphine, which are ??? based on receptor type
mixed agonist/antagonist
Opioids have actions at two sites, the
presynaptic nerve terminal and the ???
postsynaptic neuron
Opioids: Activation of presynaptic opioid receptors (GPCR) = decrease Ca2+ flux = decreased neurotransmitter release = Decreased or Increased (?) transmission of the pain signal
decreased
Activation of ??? opioid receptors = increase K+ flux =
hyperpolarisation = inhibition of neurons in the pain pathway
postsynaptic
All opioid receptors couple to adenylate cyclase. Inhibition of adenylate cyclase = inhibition of ???
neurotransmitter release
Naloxone is a ??? antagonist and is useful for treating overdose of this drug
an opioid antagonist
NSAIDs are drugs with analgesic and
antipyretic effects and have, in higher doses, ??? effects
anti‐inflammatory
NSAIDs act upon ???
COX 1 and COX 2
COX‐1 or 2 (?): Constitutively expressed => house keeping function
COX 1
COX‐2 or 1(?): Constitutively expressed in brain/kidney/bone and induced by pro‐ inflammatory factors
COX-2
the inhibition of COX‐1 or COX-2 causes the following?
− impaired gastric protection;
− decrease in platelet aggregation
− decrease glomerular filtration rate and renal blood flow
COX-1
the inhibition of COX‐1 or COX-2 causes the following?
- analgesic, antipyretic, and anti‐inflammatory;
− decrease glomerular filtration rate and renal blood flow;
COX-2
NSAIDs enter hydrophobic channel and form H‐bonds with an arginine residue at position 120 = prevents fatty acid substrates from entering ???
enzyme
Aspirin is an NSAID or Opioid?
NSAID
Aspirin works as an irreversible, non‐selective COX inhibitor (causes acetylation of COX) = anti‐inflammatory & inhibits ???
platelet aggregation
??? is a weak acid so protonated in acidic environment of stomach, facilitating passage across mucosa but most absorbed in ileum.
aspirin
Aspirin can cause hazardous increase in effect of ??? by
displacing it from plasma proteins and because it interferes with the haemostatic mechanisms
warfarin
Aspirin to prevent blood clots, stroke and heart attack is usually ~ 100 mg
Aspirin to have ??? effect is usually ~ 300‐500 mg
analgesic and anti‐inflammatory
??? is an oxicam derivative which has anti‐inflammatory action in rheumatoid arthritis and other connective tissue disorders
piroxicam
paracetamol inhibits the synthesis of ??? in the CNS
prostaglandin
paracetamol has weak anti‐inflammatory activity (e.g. headache), does not affect ??? or bleeding time, overdose can produce fatal hepatotoxicity.
platelet function
Acetylcysteine or oral methionine can prevent damage from toxicity of ??? overdose if given early
paracetamol
