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Pharmacology > Unit 3-CNS 1 and II > Flashcards

Unit 3-CNS 1 and II Flashcards

1
Q

Levodopa

Drug Class

A

Dopamine precursor

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2
Q

Levodopa

Mechanism

A

Crosses BBB and is converted to dopamine->improves nigrostriatal functioning

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3
Q

Levodopa

Uses

A

Given with carbidopa (as Sinemet); first-line treatment for Parkinson’s unless patient is young (want to delay as long as possible)

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4
Q

Levodopa

Side Effects

A
  • Dyskinesias; hypotension, nausea, anxiety, fatigue
  • Psychoses if dosed too high
  • MAO-A inhibitors are contraindicated (except MAO-B, which only hits DA)
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5
Q

Carbidopa

Drug class

A

Aromatic amino acid decarboxylase inhibitor

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6
Q

Carbidopa

Mechanism

A

Inhibits peripheral conversion of L-DOPA to dopamine; does not cross BBB

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7
Q

Carbidopa

Uses

A

Parkinson’s (given with Levadopa to lower side effects)

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8
Q

Carbidopa

Side effects

A

Dyskinesias, on-off phenomenon,

MAO-A inhibitors are contraindicated (except MAO-B, which only hits DA)

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9
Q

Bupropion

Drug class

A

Norepinephrine-dopamine reuptake inhibitor (NDRI)

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10
Q

Bupropion

Mechanism

A

Blocks dopamine transporter (DAT) -> increased dopamine in synapse

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11
Q

Bupropion

Uses

A

Parkinson’s

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12
Q

Bupropion

Side effects

A

Insomnia, anxiety, agitation, nausea, dry mouth, sweating, palpitations

Mild increase in BP

Side effects due to increase in NE (drug acts to block reuptake of both NE and DA)

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13
Q

dextroamphetamine; lisdexamfetamine

Drug class

A

Stimulants

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14
Q

dextroamphetamine; lisdexamfetamine

Mechanism

A
  • Blocks dopamine transporter (DAT) to block reuptake
  • also increases VMAT2 to cause more DA to be ejected from nerve terminal
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15
Q

dextroamphetamine; lisdexamfetamine

Uses

A

ADHD

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16
Q

dextroamphetamine; lisdexamfetamine

Side effects

A

Norepi (sympathetic) and dopamine side effects; weight loss; addictive

Psychosis at high doses

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17
Q

Modafinil; Armodafinil

Drug Class

A

Stimulant

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18
Q

Modafinil; Armodafinil

Mechanism

A
  • Increases histamine activity in the tuberomammilary nucleus–> activates alertness in frontal cortex
  • may increase orexin activity
  • may block DAT
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19
Q

Modafinil; Armodafinil

Uses

A

Fatigue due to narcolepsy, apnea, shiftwork (but not ADHD)

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20
Q

Modafinil; Armodafinil

Side effects

A
  • Similar to, but less severe, than amphetamines (ie NE and DA effects)
  • Addiction (b/c inncreases DA in mesolimbic pathway ie reward center)
  • appetite and weight loss
  • psychosis at very high doses
  • Can lower birth control effectiveness (use same P450-3A4 enzymes)
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21
Q

Selegiline

Drug class

A

MAO-B inhibitor

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22
Q

Selegiline

Mechanism

A

Prevents breakdown of DA

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23
Q

Selegiline

Uses

A
  • Early Parkinson’s (low dose: inhibits MAO-B
  • depression (high dose: inhibits MAO-A and B)
  • For depression it comes in a patch called EMSAM
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24
Q

Selegiline

Side effects

A

Hypotension, dizziness, insomnia, weight gain

Nausea, vomiting

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25
Q

Rasagiline

Drug Class

A

MAO-B inhibitor

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26
Q

Rasagiline

Mechanism

A

Prevents breakdown of DA

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27
Q

Rasagiline

Uses

A

Early Parkinson’s

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28
Q

Rasagiline

Side effects

A

Hypotension, dizziness, insomnia, weight gain

Nausea, vomiting

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29
Q

Tranylcypromine (Parnate); Isocarboxazid (Marplan); Phenelzine (Nardil)

Drug class

A

MAOI

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30
Q

Tranylcypromine (Parnate); Isocarboxazid (Marplan); Phenelzine (Nardil)

Mechanism

A

Irreversibly inhibit both MAO-A and MAO-B

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31
Q

Tranylcypromine (Parnate); Isocarboxazid (Marplan); Phenelzine (Nardil)

Uses

A

Depression

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32
Q

Tranylcypromine (Parnate); Isocarboxazid (Marplan); Phenelzine (Nardil)

Side effects

A

Hypotension, dizziness, insomnia, weight gain

Hypertensive crisis (with tyramine-rich foods–> increased NE);

serotonin syndrome (MAOI + SSRI)

Interactions with drugs that increase NE and serotonin b/c of its action on MAO-A

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33
Q

Entacapone

Drug class

A

COMT inhibitor

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34
Q

Entacapone

Mechanism

A

Prevents breakdown of DA

Short-acting (2 hours)

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35
Q

Entacapone

Uses

A

Parkinson’s

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36
Q

Entacapone

Side effects

A

Nausea, fatigue

DA side effects

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37
Q

Tolcapone

Drug class

A

COMT inhibitor

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38
Q

Tolcapone

Mechanism

A

Prevents breakdown of DA

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39
Q

Tolcapone

Uses

A

Parkinson’s

Use only if Entacapone fails

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40
Q

Tolcapone

Side effects

A

Nausea, fatigue; liver failure

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41
Q

Bromocriptine

Drug class

A

Ergot D2 receptor agonist

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42
Q

Bromocriptine

Mechanism

A

Increases DA activity via D2 receptor agonism

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43
Q

Bromocriptine

Uses

A

Mild Parkinson’s; Restless Legs Syndrome; hyperprolactinemia

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44
Q

Bromocriptine

Side effects

A

Mania, nausea, dizziness, fatigue

Peripheral DA-like effects

Must be titrated slowly due to hypotension

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45
Q

Pramipexole

Drug class

A

Selective D2 receptor agonist

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46
Q

Pramipexole

Mechanism

A

Increases DA activity via D2 receptor agonism

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47
Q

Pramipexole

Uses

A

Mild Parkinson’s; Restless Legs Syndrome

Less effective with motor symptoms of PD

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48
Q

Pramipexole

Side effects

A

Mania, nausea, dizziness, fatigue

Peripheral DA-like effects

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49
Q

Ropinerole

Drug class

A

Selective D2 agonist

50
Q

Ropinerole

Mechanism

A

Increases DA activity via D2 receptor agonism

51
Q

Ropinerole

Uses

A

Mild Parkinson’s; Restless Legs Syndrome

Less effective with motor symptoms of PD

52
Q

Ropinerole

Side effects

A

Mania, nausea, dizziness, fatigue

Peripheral DA-like effects

53
Q

Apomorphine

Drug class

A

D2 receptor agonist

54
Q

Apomorphine

Mechanism

A

Increases DA activity via D2 receptor agonism

55
Q

Apomorphine

Uses

A

Mild Parkinson’s; Restless Legs Syndrome

Injectable only

56
Q

Apomorphine

Side effects

A

Mania, nausea, dizziness, fatigue

Peripheral DA effects

Serotonin receptor antagonists are contraindicated (eg ondansetron)

57
Q

Aripiprazole

Drug class

A

D2 & D3 receptor (partial) agonist

58
Q

Aripiprazole

Mechanism

A

Increases DA activity

59
Q

Aripiprazole

Uses

A

Schizophrenia; depression

60
Q

Aripiprazole

Side effects

A
  • Less side effects than other DA agonists
  • akathisia (restlessness)
61
Q

Amantadine

Drug class

A

anti-viral

62
Q

Amantadine

Mechanism

A

(?) Stimulates D2 receptors, blocks DAT (?)

63
Q

Amantadine

Uses

A

Mild Parkinson’s (2nd-line); influenza

64
Q

Amantadine

Side effects

A

Nausea, dizziness, psychosis, insomnia, seizures

Contraindicated in elderly with dementia (anticholinergic effects)

65
Q

Reserpine

Drug class

A

Synapse depleter

66
Q

Reserpine

Mechanism

A

Blocks VMAT (no release of monoamines into synapses)

67
Q

Reserpine

Uses

A

Hypertension

68
Q

Resperine

Side effects

A

Depression (due to less NE and DA)

69
Q

Tetrabenazine

Drug class

A

Synapse depleter

70
Q

Tetrabenazine

Mechanism

A

Blocks VMAT (no release of monoamines into synapses)

71
Q

Tetrabenazine

Uses

A

Huntington’s Chorea

(less DA–> less choreic movements)

72
Q

Tetrabenazine

Side effects

A

Depression

73
Q

Benztropine

Drug class

A

Anticholinergic

74
Q

Benztropine

Mechanism

A

Antagonize the ACh muscarinic receptor

75
Q

Benztropine

Uses

A

Early Parkinson’s; reduce EPS parkinsonian side effects of FGA/SGA

76
Q

Benztropine

Side effects

A
  • Typical anticholinergic (dry mouth, blurred vision, racing heart, constipation, confusion, delirium, hallucinations)
  • Contraindicated in demented Parkinson’s; abrupt discontinuation exacerbates symptoms
77
Q

Trihexyphenidyl

Drug class

A

Anticholinergic

78
Q

Trihexyphenidyl

Mechanism

A

Antagonize the ACh muscarinic receptor

79
Q

Trihexyphenidyl

Uses

A

Early Parkinson’s; reduce EPS parkinsonian side effects of FGA/SGA

80
Q

Trihexyphenidyl

Side effects

A
  • Typical anticholinergic (dry mouth, blurred vision, racing heart, constipation, confusion, delirium, hallucinations)
  • Contraindicated in demented Parkinson’s; abrupt discontinuation exacerbates symptoms
81
Q

Diphenhydramine

Drug class

A

Antihistamine

82
Q

Diphenhydramine

Mechanism

A

Anticholinergic properties

83
Q

Diphenhydramine

Uses

A

Reduce EPS Parkinsonian side effects of FGA/SGA

84
Q

Diphenhydramine

Side effects

A

Typical anticholinergic (dry mouth, blurred vision, racing heart, constipation, confusion, delirium, hallucinations)

85
Q

First-generation antipsychotics (Low Potency)

A

Chlorpromazine

Thioridazine

86
Q

Mechanism of action and side effects of First Generation Antipsychotics

A
  • D2 receptor antagonist

non-selective

occurs in all DA pathways

  • extrapyramidal side effects due to blocking of D2 in nigrostriatal pathway (resembles parkinsonism)
87
Q

Chlorpromazine

Drug class

A

First-generation antipsychotics (Low Potency)

88
Q

Chlorpromazine

Mechanism

A

Non-selective D2 receptor antagonism

89
Q

Chlorpromazine

Uses

A

Psychosis (schizophrenia)

90
Q

Chlorpromazine

Side effects

A
  • EPS; fatigue and weight gain (H1 antagonism); anticholinergic effects; orthostasis (alpha1 antagonism)
  • Tardive dyskinesia with chronic use
  • Little effect on negative symptoms
91
Q

Thioridazine

Drug class

A

First-generation antipsychotics (Low Potency)

92
Q

Thioridazine

Mechanism

A

Non-selective D2 receptor antagonism

93
Q

Thioridazine

Uses

A

Psychosis (schizophrenia)

94
Q

Thioridazine

Side effects

A
  • EPS; fatigue and weight gain (H1 antagonism); anticholinergic effects; orthostasis (alpha1 antagonism)
  • Tardive dyskinesia with chronic use
  • Little effect on negative symptoms
95
Q

First-generation antipsychotics (High Potency)

A

Fluphenazine

Thiothixine

Haloperidol

96
Q

Fluphenazine

Drug class

A

First-generation antipsychotics (High Potency)

97
Q

Fluphenazine

Mechanism of action

A

Non-selective D2 receptor antagonism

98
Q

Fluphenazine

Uses

A

Psychosis (schizophrenia);

movement disorder in Huntingtons

99
Q

Fluphenazine

Side effects

A

EPS;

NMS

Tardive dyskineasia with chronic use

Little effect on negative symptoms

100
Q

Thiothixine

Drug class

A

First-generation antipsychotics (High Potency)

101
Q

Thiothixine

Mechanism

A

Non-selective D2 receptor antagonism

102
Q

Thiothixine

Uses

A

Psychosis (schizophrenia);

movement disorder in Huntingtons

103
Q

Thiothixine

Side effects

A

EPS;

NMS

Tardive dyskineasia with chronic use

Little effect on negative symptoms

104
Q

Haloperidol

Drug class

A

First-generation antipsychotics (High Potency)

105
Q

Haloperidol

Mechanism

A

Non-selective D2 receptor antagonism

106
Q

Haloperidol

Uses

A

Psychosis (schizophrenia); movement disorder in Huntingtons

107
Q

Haloperidol

Side effects

A

EPS; NMS

Tardive dyskineasia with chronic use

Little effect on negative symptoms

108
Q

Clozapine

Drug class

A

Second-Generation Antipsychotic

109
Q

Clozapine

Mechanism

A

D2 (& D1, D4) receptor antagonist;

5HT2a receptor antagonist

110
Q

Clozapine

Uses

A

Refractory shizophrenia

111
Q

Clozapine

Side effects

A

Side effects similar to other “pines”, but also agranulocytosis (NMDA receptor antagonism?)

Most metabolic risk of all antipsychotics, but little EPS/TD; must monitor WBC

112
Q

Olanzapine (Zyprexa); Quetiapine (Seroquel); Asenapine (Saphris)

Drug class

A

Second-Generation Antipsychotics

113
Q

Olanzapine (Zyprexa); Quetiapine (Seroquel); Asenapine (Saphris)

Mechanism

A

D2 receptor antagonist, 5HT2a receptor antagonist

114
Q

Olanzapine (Zyprexa); Quetiapine (Seroquel); Asenapine (Saphris)

Uses

A

Psychosis, mania, agression

115
Q

Olanzapine (Zyprexa); Quetiapine (Seroquel); Asenapine (Saphris)

Side effects

A

Suicide risk in ages <25; Metabolic Syndrome; TD/EPS; stroke in dementia patients

Sedation (H1 antagonism)

116
Q

Risperidone (Risperdal); Ziprazidone (Geodon); Paliperidone (Invega); Iloperidone (Eanapt); Lurasidone (Latuda)

Drug class

A

Second-Generation Antipsychotics

117
Q

Risperidone (Risperdal); Ziprazidone (Geodon); Paliperidone (Invega); Iloperidone (Eanapt); Lurasidone (Latuda)

Mechanism

A

D2 receptor antagonist; but various other receptor agonism/antagonism

118
Q

Risperidone (Risperdal); Ziprazidone (Geodon); Paliperidone (Invega); Iloperidone (Eanapt); Lurasidone (Latuda)

Uses

A

Psychosis, mania, agression

119
Q

Risperidone (Risperdal); Ziprazidone (Geodon); Paliperidone (Invega); Iloperidone (Eanapt); Lurasidone (Latuda)

Side effects

A

Suicide risk in ages <25; Metabolic Syndrome; TD/EPS; stroke in dementia patients

Fewer metabolic complications than “pines”, but more EPS

120
Q

Extrapyramidal Syndromes

(EPS)

A
  • When dopamine is too low
  • akathisia=restlessness
  • dystonia=muscle spasm
  • parkinsonism=like parkinson disease but reversible
  • neuroleptic malignant syndrome
    • hyperthermia
    • muscle rigidity
    • vital sign instability
    • rhabdomyolysis

Pharmacology (26 decks)

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