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Phase 1 Drugs > Block 3 Drugs > Flashcards

Block 3 Drugs Flashcards

1
Q

Dopaminergics

Pharmacology of Basal Ganglia Disorders

A

Levodopa (L-dopa)

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2
Q

Levodopa (L-dopa) MoA

A

Dopamine precursor

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3
Q

Dopaminergics

Pharmacology of Basal Ganglia Disorders

A

Pramipexole

Ropinirole

Rotigotine

Apomorphine

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4
Q

Dopaminergics (Pramipexole / Ropinirole / Rotigotine / Apomorphine) MoA

A

Dopamine D2 receptor agonist (synthetic)

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5
Q

Dopa-decarboxylase inhibitor

Pharmacology of Basal Ganglia Disorders

A

Benserazide

Carbidopa

(Car - Benz - Dope)

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6
Q

Dopa-decarboxylase inhibitor MoA

A

Stops breakdown of Levadopa in periphery by inhibiting dopa-decarboxylase

(Can be given in combo with L-dopa)

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7
Q

COMT (catechol-O-methyl transferase) Inhibitor

Pharmacology of Basal Ganglia Disorders

A

Entacapone

Tolcapone

(Big guns when nothing else working - Al Capone)

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8
Q

COMT (catechol-O-methyl transferase) Inhibitor MoA

A

Stops breakdown of dopamine in CNS by inhibition of COMT

Used in later stages of disease

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9
Q

MAOB (monoamine oxidase, B form) Inhibitor

Pharmacology of Basal Ganglia Disorders

A

Selegiline

Rasagiline

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10
Q

MAOB (monoamine oxidase, B form) Inhibitor MoA

A

Stops breakdown of dopamine into homovanillic acid in CNS by inhibition of MAOIB

(Better for younger patients in which motor symptoms are not impacting QoL, can be used with as an adjunct with L-dopa in later stages)

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11
Q

Anticholinergics

Pharmacology of Basal Ganglia Disorders

A

Procyclidine

Orphenadrine

Trihexphenidyl

(POT = CRAzy muscles)

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12
Q

Anticholinergics MoA

A

Muscarinic cholinergic receptor antagonist

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13
Q

Anti-Parkinsonism

Pharmacology of Basal Ganglia Disorders

A

Amantadine

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14
Q

Anti-Parkinsonism MoA

A

Antiviral - glutamate (NMDA) receptor antagonist, dopamine agonist

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15
Q

Dopamine-depleting drugs

Pharmacology of Basal Ganglia Disorders

A

Tetrabenazine

Playing Tetris depletes phone battery

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16
Q

Dopamine-depleting drugs MoA

A

Blocks VMAT, preventing uptake of dopamine into vesicles - used for hyperkinetic movement disorders

(Playing Tetris depletes phone battery)

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17
Q

Weak Analgesic/Antipyretic

Analgesic Drugs

A

Paracetamol

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18
Q

Weak Analgesic/Antipyretic MoA

A

Non-selective COX inhibitor (CNS)

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19
Q

Non-steroidal anti-inflammatory drugs (NSAIDs)

Analgesic Drugs

A

Aspirin

Ibuprofen

Diclofenac

Naproxen

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20
Q

Non-steroidal anti-inflammatory drugs (NSAIDs) MoA

Analgesic Drugs

A

Non-selective COX inhibitor

  • Non-selective COX inhibitor blocks enzyme action of platelet COX enzyme.
  • COX is required for synthesis of thromboxane A2 (TXA2).
  • Reduced TXA2 inhibits platelet activation and thrombus formation.
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21
Q

COX2-selective NSAIDs

Analgesic Drugs

A

Celecoxib

Etoricoxib

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22
Q

COX2-selective NSAIDs MoA

Analgesic Drugs

A

Selective COX-2 inhibitor

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23
Q

Weak Opioid Analgesics

Analgesic Drugs

A

Codeine

Dihydrocodeine

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24
Q

Weak Opioid Analgesics MoA

Analgesic Drugs

A

Opioid receptor agonist

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25
Q

Weak Opioid Analgesics: Side Effects

Analgesic Drugs

A

Nausea

Vomiting

Light-headedness

Dizziness

Sweating

Constipation

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26
Q

Strong Opioid Analgesics

Analgesic Drugs

A

Morphine (half life 3/4 hrs)

Diamorphine (half life 3/4 hrs)

Methadone (long half-life over 24 hrs)

Fentanyl (short half-life 1/2 hrs)

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27
Q

Strong Opioid Analgesics MoA

Analgesic Drugs

A

Opioid receptor agonist

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28
Q

Partial/Mixed Agonist-Antagonist Opioid Analgesic

Analgesic Drugs

A

Buprenophine (half-life 12 hours)

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29
Q

Partial/Mixed Agonist-Antagonist Opioid Analgesic MoA

Analgesic Drugs

A

Opioid receptor agonist (μ)/antagonist (κ)

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30
Q

Opioid Receptor Antagonist

Analgesic Drugs

A

Naloxone (short half life - 1/2 hours)

Naltrexone (long half life - 10 hours)

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31
Q

Opioid Receptor Antagonist MoA

Analgesic Drugs

A

Opioid receptor antagonist

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32
Q

Synthetic Opioid

Analgesic Drugs

A

Tramadol

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33
Q

Synthetic Opioid MoA

Analgesic Drugs

A

Opioid receptor agonist + 5HT/NA reuptake inhibitor

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34
Q

Drugs to Manage Opioid Addiction

Analgesic Drugs

A

Methadone

Buprenorphine

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35
Q

Drugs Treat Neuropathic Pain

Analgesic Drugs

A

Tricyclic Antidepressants (TCAs) - see TCA cards

Gabapentin (AED) - MoA: inhibits VDCC, increases GABA transmission

Pregabalin (AED) - MoA: inhibits VDCC,

Carbamazepine (AED) - MoA: sodium channel blocker

36
Q

Tricyclic Antidepressants (TCAs)

Pharmacology of Depression

A

Amitriptyline (also used for neuropathic pain)

Nortriptyline (also used for neuropathic pain)

Clomipramine (also used for neuropathic pain)

37
Q

Tricyclic Antidepressants (TCAs) MoA

Pharmacology of Depression

A

SRI, NRI, H1, M1, noradrenaline a1 Adrenergic antagonist

38
Q

Selective serotonin reuptake inhibitors (SSRIs)

Pharmacology of Depression

A

Sertraline

Citalopram (good for older patients)

Escitalopram

39
Q

Selective serotonin reuptake inhibitors (SSRIs) MoA

Pharmacology of Depression

A

Inhibits serotonin (5HT) reuptake pump

N.B side effect: can have increase in negative symptoms e.g. suicidal intention before mood improves and serotonin syndrome: hyperthermia, CV problems, aggression, tremor and rigidity -> MEDICAL EMERGENCY!

40
Q

Monoamine (A) oxidase inhibitors (MAOIs)

Pharmacology of Depression

A

Moclobemide

41
Q

Monoamine (A) oxidase inhibitors (MAOIs) MoA

Pharmacology of Depression

A

Stops breakdown of monoamines in CNS. Reversible inhibitor of monoamine oxidase A (RIMA)

42
Q

Monoamine (A) oxidase inhibitors (MAOIs): Side Effect

Pharmacology of Depression

A

Tyramine cheese reaction -> vasoconstriction and hypertension = MEDICAL EMERGENCY!

Do not use with SSRIs/TCA’s!

43
Q

Atypical Antidepressant

Pharmacology of Depression

A

Venlafaxine

44
Q

Atypical Antidepressant: Venlafaxine MoA

A

SNRI

45
Q

Atypical Antidepressant

Pharmacology of Depression

A

Reboxetine

46
Q

Atypical Antidepressant: Reboxetine MoA

A

NRI

47
Q

Atypical Antidepressant

Pharmacology of Depression

A

Bupropion

48
Q

Atypical Antidepressant: Bupropion MoA

A

NDRI

49
Q

Atypical Antidepressant

Pharmacology of Depression

A

Mirtazapine

50
Q

Atypical Antidepressant: Mirtazapine MoA

A

α2-Adrenergic antagonist

51
Q

1st Generation Antipsychotic

A

Chlorpromazine

Haloperidol

52
Q

1st Generation Antipsychotic MoA

A

Selective dopamine (D2) receptor antagonist

53
Q

2nd Generation Antipsychotic

A

Risperidone (used in PTSD)

Clozapine

54
Q

2nd Generation Antipsychotic MoA

A

Serotonin (5HT2A) + dopamine (D2) antagonist

can also be used for disorders of the basal ganglia

55
Q

3rd Generation Antipsychotic

A

Aripiprazole

last resort - RIP

56
Q

3rd Generation Antipsychotic MoA

A

Partial agonist at 5HT and DA receptors

57
Q

Anxiolytic - anxiety drug (adjunct in depression)

Anxiolyics and Related Drugs

A

Buspirone

58
Q

Anxiolytic - anxiety drug (adjunct in depression) MoA

Anxiolyics and Related Drugs

A

5HT1a partial agonist

59
Q

Muscle relaxants / Sedatives / Anxiolytic-hypnotic

Anxiolyics and Related Drugs

A

SSRI/SNRI

60
Q

SSRI/SNRI MoA

A

5HT1a partial agonist

61
Q

Muscle relaxants / Sedatives / Anxiolytic-hypnotic

Anxiolyics and Related Drugs

A

Zolpidem (‘Z-drug’)

uses: short term/crises

62
Q

Zolpidem (‘Z-drug’) MoA

Anxiolyics and Related Drugs

A

GABA PAM (γ-subunit) (mechanistically identical to BDZ)

63
Q

Muscle relaxants / Sedatives / Anxiolytic-hypnotic

Anxiolyics and Related Drugs

A

Temazepam

64
Q

Temazepam MoA

Anxiolyics and Related Drugs

A

GABA PAM (γ-subunit) (mechanistically identical to BDZ)

65
Q

Symptom Reduction (Autonomic)

Anxiolyics and Related Drugs

A

Propranolol

uses: specific phobia to reduce symptoms only

66
Q

Symptom Reduction (Autonomic) MoA

Anxiolyics and Related Drugs

A

β-blocker aka β-adrenegic receptor

67
Q

Anti-epilepsy drugs (AEDs)

A

Sodium valproate
(Side effect: anti-epileptic hypersensitivity syndrome / TERATOGENIC)

Lamotrigine
(First line for epilepsy apart from generalised tonic-clonic)

Ethosuximide
(First line for generalised absence)

Carbemazepine
(Side effect: anti-epileptic hypersensitivity syndrome)

68
Q

Sodium valproate / Lamotrigine / Carbemazepine MoA

A

Sodium channel blocker

69
Q

Ethosuximide MoA

A

Calcium channel blocker (T-type)

70
Q

Benzodiazepine (BDZ)

Epilepsy Drugs

A

Midazolam

Lorazepam
(uses: epilepsy and anxiety - short term/crises)

Diazepam

71
Q

Benzodiazepines (BDZ) MoA

Epilepsy Drugs

A

GABA PAM (γ-subunit)

72
Q

BDZ Antagonist

Epilepsy Drugs

A

Flumazenil

73
Q

BDZ Antagonist MoA

Epilepsy Drugs

A

Competitive antagonist at BDZ site

74
Q

Barbiturates

Epilepsy Drugs

A

Phenobarbitone

Pentobarbitone

Primidone

75
Q

Barbiturates MoA

Epilepsy Drugs

A

GABA PAM (β-subunit)

76
Q

Adjuncts

Epilepsy Drugs

A

Tiagabin

Levetiracetam

77
Q

Adjuncts MoA

Epilepsy Drugs

A

Tiagabin - GABA reuptake inhibitor

Levetiracetam - unclear

78
Q

Anticholinesterases

Drugs used for Dementia

A

Donepezil

Galantamine

Rivastigmine

79
Q

Anticholinesterases MoA

Drugs used for Dementia

A

Inhibitor of acetylcholinesterase (reversible)

80
Q

Glutamate (NMDA) receptor antagonists

Drugs used for Dementia

A

Memantine

81
Q

Glutamate (NMDA) receptor antagonists MoA

Drugs used for Dementia

A

VD blocker of NMDA (N-Methyl-D-aspartate) receptor

82
Q

Antimicrobial drugs

Drugs used for CNS infection

A

Ceftriaxone (antibiotics, B4)

83
Q

Ceftriaxone MoA

Drugs used for CNS infection

A

Inhibits synthesis of cell walls in bacteria

84
Q

Antimicrobial drugs

Drugs used for CNS infection

A

Amoxicillin (antibiotics, B4)

85
Q

Amoxicillin MoA

Drugs used for CNS infection

A

Induces cell lysis by blocking last stages of cell wall synthesis

86
Q

Corticosteroid

A

Dexamethasone

87
Q

Corticosteroid MoA

A

Glucocorticoid receptor agonist

Phase 1 Drugs (5 decks)

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