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

gamma-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

Question 17

Disulfiram

Answer 17

• metabolites of disulfiram irreversibly inhibit aldehyde dehydrogenase (in alc conversion context)
• increase in acetaldehyde→ unpleasant symptoms, flushing, dizziness, nausea and headaches
• Not used in active drinkers but used in conjunction with behavioural interventions and motivated ppl
• maintain abstinence

Question 18

Acamprosate

Answer 18

• oral administration in the form of a calcium salt (oral bioavailability is ~11%)
• not hepatically metabolised, and excreted unchanged in urine and faeces
• MoA: modulate glutamate transmission and maybe GABA
• dose adjust for renal impairment
• diarrhoea is common; nausea, vomiting, rash, mild abdominal pain
• maintain abstinence

Question 19

Naltrexone

Answer 19

• an opioid receptor antagonist (binding affinity: µ > k>delta
• Heptically metabolised by dihydrodiol DH: 6-β-naltrexol (active)
• Oral tablets
• NOT for opioid used bc induce withdrawal symp
• • nausea, headache, dizziness, fatigue, insomnia, vomiting, and anxiety
• block pleasure and rewards

Question 20

Benzodiazepines

Answer 20

• long-acting benzodiazepines - preferred
• short-acting benzodiazepines for elderly patients or ppl with liver disease
• anticonvulsant and anxiolytic effects
• short-term use; gradual cessation of drugs as withdrawal effects are similar to alcohol
• relieve acute withdrawal symptoms

Question 21

Morphine acts on what receptor

Answer 21

opioid µ-receptor agonist

Question 22

tramadol

Answer 22

• opioid and meta by cyp2D6 to O-desmethyl tramadol
• a synthetic and atypical centrally acting opioid
• μ opioid receptor agonist - O-desmethyl tramadol
• serotonin-noradrenaline reuptake inhibitor - descending path

Question 23

Name 3 µ opioid agonist

Answer 23

Morphine and tramadol and methadone

Question 24

Name serotonin-noradrenaline reuptake inhibitor

Answer 24

Tramadol

Question 25

how is tramadol an analgesic

Answer 25

* opioid agonist part will reduce ascending pathway signals * Inhibiting Sero/NA enhance descending inhibitory pain control

Question 26

2 typical and 1 atypical opioid

Answer 26

Codeine and morphine Tramadol

Question 27

Opioid OD then use

Answer 27

Naxolone

Question 28

Naxolone

Answer 28

µ opioid receptor antagonist

Question 29

Name 2 µ opioid receptor antagonist

Answer 29

Naxolone and Naltrexone

Question 30

Name an NMDA receptor antagonist

Answer 30

Methadone (also µ-agonist) Ketamine

Question 31

Chlorpropamide

Answer 31

* 1st generation sulfonylureas

Question 32

Glipizide

Answer 32

* 2nd gen sulfonylureas * (more common, increased potency, more rapid onset of action, shorter plasma half-lives and longer duration of action)

Question 33

Gliclazide

Answer 33

* 3rd generation sulfonylurea * (modified release, high glucose-lowering efficacy, once-daily oral administration, few side effects (mild hypoglycaemia), cardiovascular safety)

Question 34

Canagliflozin

Answer 34

* sodium-glucose co-transporter 2 inhibitor * prevent reabsorption of glucose and NA and instead removed by urine

Question 35

Glucagonlike-peptide1

Answer 35

* Incretin mimetisc (GLP-1 receptor agonist) * Incretins are pepide hormone groups secreted from the gut in response to food * Short lived * CLeared by kidneys * Injectable and oral

Question 36

Pegvisomant

Answer 36

* mutant GH molecule, with a single amino acid substitution (Gly for Arg at position 120), that disrupts the binding to the 2nd GH receptor & prevents GH receptor dimerization & activation * GH receptor antagonist

Question 37

pasireotide

Answer 37

* pan SST receptor agonist, increase response rate * somatostatin analgue

Question 38

Somatropin

Answer 38

cause growth in dwarfism caused by low GH production (e.g. hypopituitary).

Question 39

octreotide lanreotide

Answer 39

SSTR-2 selective

Question 40

cortisol in replacement therapy

Answer 40

* mimic the physiologic patterns of cortisol action. * Low, physiologic doses used for long periods → minimal side-effects

Question 41

beclomethasone

Answer 41

* To inhibit inflammation associated with asthma * High doses used, but given locally → some localised side-effects * GCC inhibit inflam. reactions, by altering transcription of genes involved in the inflammatory process. * given locally

Question 42

prednisolone

Answer 42

* anti-inflam. * Immunosupressive * allergic reactions treatment * some Na retention * High oral doses used, but for a short period → minimal side-effects

Question 43

3. To suppress the immune system (clincal GCC)

Answer 43

High, oral doses used for long periods → significant side-effects

Question 44

dexamethasone

Answer 44

* As an adjunct therapy in cancer * ↓ chemo-therapy nausea and vom * reduce swelling in brain tumours * High, oral doses used for long periods → significant side-effects