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PHAR222 > Drug --> Receptors > Flashcards

Drug --> Receptors Flashcards

1
Q

Mirtazapine

A

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

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2
Q

imipramine

A

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

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3
Q

Ketamine

A

a non-competitive NMDA receptor antagonist

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4
Q

moclobemide

A

reversible MAO-A inhibitor

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5
Q

phenelzine

A

irreversible MAO-A and MAO-B inhibitor

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6
Q

fluoxetine

A

Selective serotonin reuptake inhibitors

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7
Q

GABA

A

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

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8
Q

benzodiazepines

A
  • positive allosteric modulator (PAM)
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9
Q

flumazenil

A
  • treated with i.v. flumazenil* (compete with benzodiazepines for the binding site)
  • In BZD overdose
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10
Q

diazepam

A

M: CYP2D6 and CYP2C19
GABA-A receptor modulator

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11
Q

oxazepam

A

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

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12
Q

Buspirone

A

5-HT1A receptor partial agonist

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13
Q

diclofenac

A

compete with arachidonic acid for the cyclooxygenase active site

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14
Q

aspirin

A
  • 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
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15
Q

-coxibs

A

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

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16
Q

Antidote to paracetamol overdose

A

N-acetylcysteine* to replenish glutathione

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17
Q

Disulfiram

A
  • 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
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18
Q

Acamprosate

A
  • 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
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19
Q

Naltrexone

A
  • 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
20
Q

Benzodiazepines

A
  • 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
21
Q

Morphine acts on what receptor

A

opioid µ-receptor agonist

22
Q

tramadol

A
  • 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
23
Q

Name 3 µ opioid agonist

A

Morphine and tramadol and methadone

24
Q

Name serotonin-noradrenaline reuptake inhibitor

A

Tramadol

25
Q

how is tramadol an analgesic

A
  • opioid agonist part will reduce ascending pathway signals
  • Inhibiting Sero/NA enhance descending inhibitory pain control
26
Q

2 typical and 1 atypical opioid

A

Codeine and morphine
Tramadol

27
Q

Opioid OD then use

A

Naxolone

28
Q

Naxolone

A

µ opioid receptor antagonist

29
Q

Name 2 µ opioid receptor antagonist

A

Naxolone and Naltrexone

30
Q

Name an NMDA receptor antagonist

A

Methadone (also µ-agonist)
Ketamine

31
Q

Chlorpropamide

A
  • 1st generation sulfonylureas
32
Q

Glipizide

A
  • 2nd gen sulfonylureas
  • (more common, increased potency, more rapid onset of action, shorter plasma half-lives and longer duration of action)
33
Q

Gliclazide

A
  • 3rd generation sulfonylurea
  • (modified release, high glucose-lowering efficacy, once-daily oral administration, few side effects (mild hypoglycaemia), cardiovascular safety)
34
Q

Canagliflozin

A
  • sodium-glucose co-transporter 2 inhibitor
  • prevent reabsorption of glucose and NA and instead removed by urine
35
Q

Glucagonlike-peptide1

A
  • 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
36
Q

Pegvisomant

A
  • 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
37
Q

pasireotide

A
  • pan SST receptor agonist, increase response rate
  • somatostatin analgue
38
Q

Somatropin

A

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

39
Q

octreotide
lanreotide

A

SSTR-2 selective

40
Q

cortisol in replacement therapy

A
  • mimic the physiologic patterns of cortisol action.
  • Low, physiologic doses used for long periods → minimal side-effects
41
Q

beclomethasone

A
  • 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
42
Q

prednisolone

A
  • anti-inflam.
  • Immunosupressive
  • allergic reactions treatment
  • some Na retention
  • High oral doses used, but for a short period → minimal side-effects
43
Q
  1. To suppress the immune system (clincal GCC)
A

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

44
Q

dexamethasone

A
  • 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
45
Q
A

PHAR222 (25 decks)

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