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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
Rasagiline Drug Class
MAO-B inhibitor
26
Rasagiline Mechanism
Prevents breakdown of DA
27
Rasagiline Uses
Early Parkinson's
28
Rasagiline Side effects
Hypotension, dizziness, insomnia, weight gain Nausea, vomiting
29
Tranylcypromine (Parnate); Isocarboxazid (Marplan); Phenelzine (Nardil) Drug class
MAOI
30
Tranylcypromine (Parnate); Isocarboxazid (Marplan); Phenelzine (Nardil) Mechanism
Irreversibly inhibit both MAO-A and MAO-B
31
Tranylcypromine (Parnate); Isocarboxazid (Marplan); Phenelzine (Nardil) Uses
Depression
32
Tranylcypromine (Parnate); Isocarboxazid (Marplan); Phenelzine (Nardil) Side effects
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
33
Entacapone Drug class
COMT inhibitor
34
Entacapone Mechanism
Prevents breakdown of DA Short-acting (2 hours)
35
Entacapone Uses
Parkinson's
36
Entacapone Side effects
Nausea, fatigue DA side effects
37
Tolcapone Drug class
COMT inhibitor
38
Tolcapone Mechanism
Prevents breakdown of DA
39
Tolcapone Uses
Parkinson's Use only if Entacapone fails
40
Tolcapone Side effects
Nausea, fatigue; liver failure
41
Bromocriptine Drug class
Ergot D2 receptor agonist
42
Bromocriptine Mechanism
Increases DA activity via D2 receptor agonism
43
Bromocriptine Uses
Mild Parkinson's; Restless Legs Syndrome; hyperprolactinemia
44
Bromocriptine Side effects
Mania, nausea, dizziness, fatigue Peripheral DA-like effects Must be titrated slowly due to hypotension
45
Pramipexole Drug class
Selective D2 receptor agonist
46
Pramipexole Mechanism
Increases DA activity via D2 receptor agonism
47
Pramipexole Uses
Mild Parkinson's; Restless Legs Syndrome Less effective with motor symptoms of PD
48
Pramipexole Side effects
Mania, nausea, dizziness, fatigue Peripheral DA-like effects
49
Ropinerole Drug class
Selective D2 agonist
50
Ropinerole Mechanism
Increases DA activity via D2 receptor agonism
51
Ropinerole Uses
Mild Parkinson's; Restless Legs Syndrome Less effective with motor symptoms of PD
52
Ropinerole Side effects
Mania, nausea, dizziness, fatigue Peripheral DA-like effects
53
Apomorphine Drug class
D2 receptor agonist
54
Apomorphine Mechanism
Increases DA activity via D2 receptor agonism
55
Apomorphine Uses
Mild Parkinson's; Restless Legs Syndrome Injectable only
56
Apomorphine Side effects
Mania, nausea, dizziness, fatigue Peripheral DA effects Serotonin receptor antagonists are contraindicated (eg ondansetron)
57
Aripiprazole Drug class
D2 & D3 receptor (partial) agonist
58
Aripiprazole Mechanism
Increases DA activity
59
Aripiprazole Uses
Schizophrenia; depression
60
Aripiprazole Side effects
* Less side effects than other DA agonists * akathisia (restlessness)
61
Amantadine Drug class
anti-viral
62
Amantadine Mechanism
(?) Stimulates D2 receptors, blocks DAT (?)
63
Amantadine Uses
Mild Parkinson's (2nd-line); influenza
64
Amantadine Side effects
Nausea, dizziness, psychosis, insomnia, seizures Contraindicated in elderly with dementia (anticholinergic effects)
65
Reserpine Drug class
Synapse depleter
66
Reserpine Mechanism
Blocks VMAT (no release of monoamines into synapses)
67
Reserpine Uses
Hypertension
68
Resperine Side effects
Depression (due to less NE and DA)
69
Tetrabenazine Drug class
Synapse depleter
70
Tetrabenazine Mechanism
Blocks VMAT (no release of monoamines into synapses)
71
Tetrabenazine Uses
Huntington's Chorea | (less DA--\> less choreic movements)
72
Tetrabenazine Side effects
Depression
73
Benztropine Drug class
Anticholinergic
74
Benztropine Mechanism
Antagonize the ACh muscarinic receptor
75
Benztropine Uses
Early Parkinson's; reduce EPS parkinsonian side effects of FGA/SGA
76
Benztropine Side effects
* Typical anticholinergic (dry mouth, blurred vision, racing heart, constipation, confusion, delirium, hallucinations) * Contraindicated in demented Parkinson's; abrupt discontinuation exacerbates symptoms
77
Trihexyphenidyl Drug class
Anticholinergic
78
Trihexyphenidyl Mechanism
Antagonize the ACh muscarinic receptor
79
Trihexyphenidyl Uses
Early Parkinson's; reduce EPS parkinsonian side effects of FGA/SGA
80
Trihexyphenidyl Side effects
* Typical anticholinergic (dry mouth, blurred vision, racing heart, constipation, confusion, delirium, hallucinations) * Contraindicated in demented Parkinson's; abrupt discontinuation exacerbates symptoms
81
Diphenhydramine Drug class
Antihistamine
82
Diphenhydramine Mechanism
Anticholinergic properties
83
Diphenhydramine Uses
Reduce EPS Parkinsonian side effects of FGA/SGA
84
Diphenhydramine Side effects
Typical anticholinergic (dry mouth, blurred vision, racing heart, constipation, confusion, delirium, hallucinations)
85
First-generation antipsychotics (Low Potency)
Chlorpromazine Thioridazine
86
Mechanism of action and side effects of First Generation Antipsychotics
* D2 receptor antagonist non-selective occurs in all DA pathways * extrapyramidal side effects due to blocking of D2 in nigrostriatal pathway (resembles parkinsonism)
87
Chlorpromazine Drug class
First-generation antipsychotics (Low Potency)
88
Chlorpromazine Mechanism
Non-selective D2 receptor antagonism
89
Chlorpromazine Uses
Psychosis (schizophrenia)
90
Chlorpromazine Side effects
* EPS; fatigue and weight gain (H1 antagonism); anticholinergic effects; orthostasis (alpha1 antagonism) * Tardive dyskinesia with chronic use * Little effect on negative symptoms
91
Thioridazine Drug class
First-generation antipsychotics (Low Potency)
92
Thioridazine Mechanism
Non-selective D2 receptor antagonism
93
Thioridazine Uses
Psychosis (schizophrenia)
94
Thioridazine Side effects
* EPS; fatigue and weight gain (H1 antagonism); anticholinergic effects; orthostasis (alpha1 antagonism) * Tardive dyskinesia with chronic use * Little effect on negative symptoms
95
First-generation antipsychotics (High Potency)
Fluphenazine Thiothixine Haloperidol
96
Fluphenazine Drug class
First-generation antipsychotics (High Potency)
97
Fluphenazine Mechanism of action
Non-selective D2 receptor antagonism
98
Fluphenazine Uses
Psychosis (schizophrenia); movement disorder in Huntingtons
99
Fluphenazine Side effects
EPS; NMS Tardive dyskineasia with chronic use Little effect on negative symptoms
100
Thiothixine Drug class
First-generation antipsychotics (High Potency)
101
Thiothixine Mechanism
Non-selective D2 receptor antagonism
102
Thiothixine Uses
Psychosis (schizophrenia); movement disorder in Huntingtons
103
Thiothixine Side effects
EPS; NMS Tardive dyskineasia with chronic use Little effect on negative symptoms
104
Haloperidol Drug class
First-generation antipsychotics (High Potency)
105
Haloperidol Mechanism
Non-selective D2 receptor antagonism
106
Haloperidol Uses
Psychosis (schizophrenia); movement disorder in Huntingtons
107
Haloperidol Side effects
EPS; NMS Tardive dyskineasia with chronic use Little effect on negative symptoms
108
Clozapine Drug class
Second-Generation Antipsychotic
109
Clozapine Mechanism
D2 (& D1, D4) receptor antagonist; 5HT2a receptor antagonist
110
Clozapine Uses
Refractory shizophrenia
111
Clozapine Side effects
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
Olanzapine (Zyprexa); Quetiapine (Seroquel); Asenapine (Saphris) Drug class
Second-Generation Antipsychotics
113
Olanzapine (Zyprexa); Quetiapine (Seroquel); Asenapine (Saphris) Mechanism
D2 receptor antagonist, 5HT2a receptor antagonist
114
Olanzapine (Zyprexa); Quetiapine (Seroquel); Asenapine (Saphris) Uses
Psychosis, mania, agression
115
Olanzapine (Zyprexa); Quetiapine (Seroquel); Asenapine (Saphris) Side effects
Suicide risk in ages \<25; Metabolic Syndrome; TD/EPS; stroke in dementia patients Sedation (H1 antagonism)
116
Risperidone (Risperdal); Ziprazidone (Geodon); Paliperidone (Invega); Iloperidone (Eanapt); Lurasidone (Latuda) Drug class
Second-Generation Antipsychotics
117
Risperidone (Risperdal); Ziprazidone (Geodon); Paliperidone (Invega); Iloperidone (Eanapt); Lurasidone (Latuda) Mechanism
D2 receptor antagonist; but various other receptor agonism/antagonism
118
Risperidone (Risperdal); Ziprazidone (Geodon); Paliperidone (Invega); Iloperidone (Eanapt); Lurasidone (Latuda) Uses
Psychosis, mania, agression
119
Risperidone (Risperdal); Ziprazidone (Geodon); Paliperidone (Invega); Iloperidone (Eanapt); Lurasidone (Latuda) Side effects
Suicide risk in ages \<25; Metabolic Syndrome; TD/EPS; stroke in dementia patients Fewer metabolic complications than "pines", but more EPS
120
Extrapyramidal Syndromes | (EPS)
* 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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