Analgesics

Question 1

NSAID analgesics are given to those with what type of pain for pain relief?

Answer 1

Mild‐moderate pain

Question 2

Severe or chronic malignant pain is treated with what type of pain relief?

Answer 2

opioids

Question 3

fentanyl is an NSAID or opioid?

Answer 3

opioid

Question 4

what type of receptors do Opioids bind to?

Answer 4

GPCRs

Question 5

Most opioids are full agonists for all receptors, except: Pentazocine and buprenorphine, which are ??? based on receptor type

Answer 5

mixed agonist/antagonist

Question 6

Opioids have actions at two sites, the
presynaptic nerve terminal and the ???

Answer 6

postsynaptic neuron

Question 7

Opioids: Activation of presynaptic opioid receptors (GPCR) = decrease Ca2+ flux = decreased neurotransmitter release = Decreased or Increased (?) transmission of the pain signal

Answer 7

decreased

Question 8

Activation of ??? opioid receptors = increase K+ flux =
hyperpolarisation = inhibition of neurons in the pain pathway

Answer 8

postsynaptic

Question 9

All opioid receptors couple to adenylate cyclase. Inhibition of adenylate cyclase = inhibition of ???

Answer 9

neurotransmitter release

Question 10

Naloxone is a ??? antagonist and is useful for treating overdose of this drug

Answer 10

an opioid antagonist

Question 11

NSAIDs are drugs with analgesic and
antipyretic effects and have, in higher doses, ??? effects

Answer 11

anti‐inflammatory

Question 12

NSAIDs act upon ???

Answer 12

COX 1 and COX 2

Question 13

COX‐1 or 2 (?): Constitutively expressed => house keeping function

Answer 13

COX 1

Question 14

COX‐2 or 1(?): Constitutively expressed in brain/kidney/bone and induced by pro‐ inflammatory factors

Answer 14

COX-2

Question 15

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

Answer 15

COX-1

Question 16

the inhibition of COX‐1 or COX-2 causes the following?
- analgesic, antipyretic, and anti‐inflammatory;
− decrease glomerular filtration rate and renal blood flow;

Answer 16

COX-2

Question 17

NSAIDs enter hydrophobic channel and form H‐bonds with an arginine residue at position 120 = prevents fatty acid substrates from entering ???

Answer 17

enzyme

Question 18

Aspirin is an NSAID or Opioid?

Answer 18

NSAID

Question 19

Aspirin works as an irreversible, non‐selective COX inhibitor (causes acetylation of COX) = anti‐inflammatory & inhibits ???

Answer 19

platelet aggregation

Question 20

??? is a weak acid so protonated in acidic environment of stomach, facilitating passage across mucosa but most absorbed in ileum.

Answer 20

aspirin

Question 21

Aspirin can cause hazardous increase in effect of ??? by
displacing it from plasma proteins and because it interferes with the haemostatic mechanisms

Answer 21

warfarin

Question 22

Aspirin to prevent blood clots, stroke and heart attack is usually ~ 100 mg
Aspirin to have ??? effect is usually ~ 300‐500 mg

Answer 22

analgesic and anti‐inflammatory

Question 23

??? is an oxicam derivative which has anti‐inflammatory action in rheumatoid arthritis and other connective tissue disorders

Answer 23

piroxicam

Question 24

paracetamol inhibits the synthesis of ??? in the CNS

Answer 24

prostaglandin

Question 25

paracetamol has weak anti‐inflammatory activity (e.g. headache), does not affect ??? or bleeding time, overdose can produce fatal hepatotoxicity.

Answer 25

platelet function

Question 26

Acetylcysteine or oral methionine can prevent damage from toxicity of ??? overdose if given early

Answer 26

paracetamol