Drug --> Receptors

Question 1

Mirtazapine

Answer 1

antagonist at:
alpha-2-adrenoceptors
5-HT2A/C
5-HT3
Histamine 1 (cause sedation)

Question 2

imipramine

Answer 2

M: CYP2C19 and later CYP2D6
Antagonist:
–Muscarinic acetylcholine receptor antagonist - dry mouth, blurred vision
– Histamine H1 receptor antagonist - sedation

Question 3

Ketamine

Answer 3

a non-competitive NMDA receptor antagonist

Question 4

moclobemide

Answer 4

reversible MAO-A inhibitor

Question 5

phenelzine

Answer 5

irreversible MAO-A and MAO-B inhibitor

Question 6

fluoxetine

Answer 6

Selective serotonin reuptake inhibitors

Question 7

GABA

Answer 7

-aminobutyric acid) - the primary inhibitory neurotransmitter in the brain

Question 8

benzodiazepines

Answer 8

• positive allosteric modulator (PAM)

Question 9

flumazenil

Answer 9

• treated with i.v. flumazenil* (compete with benzodiazepines for the binding site)
• In BZD overdose

Question 10

diazepam

Answer 10

M: CYP2D6 and CYP2C19
GABA-A receptor modulator

Question 11

oxazepam

Answer 11

M: by diazepam through CYP2D6, CYP2C19 and CYP3A4
GABA-A receptor modulator

Question 12

Buspirone

Answer 12

5-HT1A receptor partial agonist

Question 13

diclofenac

Answer 13

compete with arachidonic acid for the cyclooxygenase active site

Question 14

aspirin

Answer 14

• unique mechanism of action
• acetylates the hydroxyl group of serine → irreversible COX inhibition
• anti-platelet effects - platelet COX-1 inhibition →
  inhibition of thromboxane A2 formation

Question 15

-coxibs

Answer 15

COX-2 selective inhibitors - side chain fits the side pocket

Question 16

Antidote to paracetamol overdose

Answer 16

N-acetylcysteine* to replenish glutathione