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IC 2 > CNS > Flashcards

CNS Flashcards

1
Q

Phenobarbital

A

Barbituate

Long acting

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2
Q

Pentobabital

A

Barbituate

Med acting

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3
Q

Secobarbital

A

Barbituate

Med acting

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4
Q

Methohexital

A

Barbituate

Short acting, iv

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5
Q

Amobarbital

A

Barbituate

Short acting, iv

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6
Q

Thiopental

A

Barbituate

Ultra short acting, iv

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7
Q

Meprobamate

A

Anxiolytics, less sedating than barbs
Toxicity similar to barbiturates
Affects pain perception

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8
Q

Choral hydrate

A

Hypnotic

Mickey finn date rape drug

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9
Q

Midazolam

A

Benzodiazepines
Short acting
Causes amnesia

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10
Q

Triazolam

A

Benzodiazepines
Short acting
Hypnotic

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11
Q

Alprazolam

A

Benzodiazepines
Moderate acting
Used for panic attacks
Rapid onset

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12
Q

Chlordiazepoxide

A

Benzodiazepines
Moderate acting
Anxiolytic, pre-anesthetic

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13
Q

Lorazepam

A

Benzodiazepines
Moderate acting
Anxiolytic, hypnotic, pre-anesthetic

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14
Q

Clonazepam

A

Benzodiazepines
Long acting
Anticonvulsant

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15
Q

Diazepam

A

Benzodiazepines
Very Long acting
Anticonvulsant, anxiolytic, muscle relaxant, antispastic, pre-anesthetic
Half life 43 hrs

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16
Q

Flurazepam

A

Benzodiazepines
Very Long acting
Half life 74 hours

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17
Q

Flunitrazepam

A

Benzodiazepines
Fast acting, very anmestic, date rape drug
No therapeutic uses

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18
Q

Flumazenil

A

Benzodiazepine antagonist
Used to reverse overdose and anesthesia
Short half life

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19
Q

Zolpidem

A

BZ1 agonist

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20
Q

Zaleplon

A

BZ1 agonist

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21
Q

Eszopiclone

A

Non selective non-benzodiazepine agonist

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22
Q

Buspirone

A 
Partial agonist at 5-HT1A site
Slow onset (1-2 weeks)
Dysphoric at high doses
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23
Q

Hydroxyzine

A

H1 blocker
Used pre and post operatively
Antipruitic and antiemetic

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24
Q

Ramelteon

A

MT1 and MT2 melatonin receptor agonist

Indicate for insomnia with prolonged sleep onset

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25
Q

Suvorexant

A

Orexin antagonist

Indicated for difficulties with sleep onset and/or sleep maintenance

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26
Q

Trazodone

A

Blocks 5-HT re-uptake, H1, and alpha1 receptors

Antidepressant used as a hypnotic

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27
Q

Primidone

A

Anticonvulsants
Converted to phenobartital and phenylethylmalonamide (PEMA)
Effective in patients not responding to phenytoin or phenobarbital
Used for Tonic-clonic, partials, and status epilepticus

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28
Q

Phenytoin

A

Hydantoin
Prolongs inactivation of Na channels and decreases glu release
Less sedating than barbs
Numerous drug interactions, potent
Many side-effects: ataxia, N/V, rash, gum hyperplasia, hirsutism
Teratogenic

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29
Q

Valproic Acid

A 
Increases inactivation of Na channels, inhibits T-type Ca channels, enhances GABAergic transmitting
Idiosyncratic hepatotoxicity in children
Sedation is uncommon
P450 inhibitor
Grand mal and petit mal
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30
Q

Carbamazepine

A 
Increases inactivation of Na channels
Partial seizures
Safe and nontoxic, non sedating 
Induces microsomal enzymes
Blood dyscrasias
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31
Q

Oxcarbazepine

A

Increases inactivation of Na channels
Like Carbamazepine but less blood dyscrasias
Shorter half-life, longer duration of action
Fewer drug interactions

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32
Q

Lamotrigine

A

Increases inactivation of Na channels
Used for partial and possibly absence seizures
Side effects: nausea, GI upset, sedation, HA, diplopia, rashes
Valproic acid increases half life
Add-on or mono therapy

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33
Q

Topiramate

A

Increases inactivation of Na channels
Used for partial and generalized tonic-clinic and also absence
S/E: sedation, mental dulling, nausea, abnormal vision, parathesia, decreased serum bicarbonate
Add-on or monotherapy

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34
Q

Levetiracetam

A

Modifies synaptic release of GABA via binding to synaptic vesicular protein SV2A
Minimal drug interactions, no metabolized by P450
Used for partial seizures

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35
Q

Lacosamide

A

Enhances slow inactivation of Na channels

Used for partial seizures

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36
Q

Gabapentin

A

Decreases glu release by binding volt-gated Ca channels with a2-delta1 subunit.
Add on in refractory partial seizures
Used for neuropathic pain

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37
Q

Pregabalin

A

Decreases glu release by binding volt-gated Ca channels with a2-delta1 subunit.
Add on in refractory partial seizures
Used for neuropathic pain
More potent than gabapentin

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38
Q

Tiagabine

A

Inhibits GABA re-uptake

Add-on for partial and tonic-clonic seizures

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39
Q

Zonisamide

A

Increases inactivation of Na channels
Add-on for partial seizures
Not metabolized by P450 -> minimal drug interactions
S/E: Drowsiness, anorexia

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40
Q

Ezogabine

A

K channel facilitator

Add-on for partial seizures

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41
Q

Perampenel

A

AMPA glutamate receptor antagonist

Add-on for partial seizures

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42
Q

Eslicarbazepine

A

Pro-drug

Voltage-gated Na channel blocker

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43
Q

Ethosuximide

A

Inhibits T-type Ca channels
Treats Absence seizures
May precipitate tonic-clinic seizures

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44
Q

Methsuximide

A

Inhibits T-type Ca channels
Treats Absence seizures
May precipitate tonic-clinic seizures
Used for absence seizures that are refractory t other drugs

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45
Q

Levadopa

A

Dopamine precursor
Used to treat Parkinsonism
Reverses rigidity, tremor, and bradydinesia
S/E: N/V, orthostatic hypotension, psychosis

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46
Q

Carbidopa

A

Blocks AADC in periphery

Decreases dose of L-DOPA and peripheral S/E

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47
Q

Selegiline

A

MAO-B inhibitor
Increases dopamine catabolism
Treats on-off effect

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48
Q

Rasagiline

A

MAO-B inhibitor
Increases dopamine catabolism
Treats on-off effect

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49
Q

Tolcapone

A

Catecholamines-O-methyl transferase inhibitor
Blocks dopamine and L-DOPA catabolism
Central and peripheral
Hepatotoxic

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50
Q

Entacapone

A

Catecholamines-O-methyl transferase inhibitor
Blocks dopamine and L-DOPA catabolism
Peripheral only
Not hepatotoxic

51
Q

Pramipexole

A

D2/D3 agonist

52
Q

Ropinerole

A

D2/D3 agonist

53
Q

Rotigotine

A

D1/D2/D3 agonist, transdermal

54
Q

Bromocriptine

A

D2 agonist

Used with L-DOPA

55
Q

Apomorphine

A

Non-ergot D1/D2 agonist, sc

Used with L-DOPA

56
Q

Trihexyphenidyl

A

Anticholinergic

Blocks actions of strictly cholinergic interneurons

57
Q

Benztropine

A

Anticholinergic

Blocks actions of strictly cholinergic interneurons

58
Q

Procyclidine

A

Anticholinergic

Blocks actions of strictly cholinergic interneurons

59
Q

Amantadine

A

Anti-viral that may release dopamaine/be anticholinergic

60
Q

Propranolol

A

Beta blocker

Used to treat physiologic and essential tremor

61
Q

Baclofen

A

GABA-b agonist
Anti-spastic at the spinal cord
S/E: drowsiness, insomnia, weakness, dizziness, ataxia, confusion
S/E decreased with intrathecal administration

62
Q

Tizanidine

A

Alpha2 adrenergic agonist
Anti-spastic at the spinal cord
S/E: Drowsiness, dry mouth, asthenia, hypotension, hepatotoxicigty, visual hallucinations
Metabolized by CYP1A2

63
Q

Dantrolene

A

Decreases Ca release from sarcoplasmic reticulum
Anti-spastic at muscle
Causes generalized muscle weakness and hepatotoxicity
Used for paralysis, hemiparalysis, cerebral palsy, and MS

64
Q

Botulinum Toxin

A

Inhibits Ach release from vesicles
Anti-spastic at muscle
Injected into muscle

65
Q

Cyclobenzaprine

A

Acts as a sedative at brain or spinal cord
For acute muscle spasm from trauma or strain
Structurally related to tricyclics antidepressants
Not effective for cerebral palsy or spinal cord injury

66
Q

Carisoprodol

A

Acts as a sedative at brain or spinal cord
For acute muscle spasm from trauma or strain
Metabolized into meprobamate, a barb-like sedative-hypnotic
Abuse potential

67
Q

Orphenadrine

A

Acts as a sedative at brain or spinal cord

For acute muscle spasm from trauma or strain

68
Q

Chlorpromazine

A

Phenothiazine = Typical antipsychotic
Produces EPS and tardive dyskinesia
D2 antagonist

69
Q

Fluphenazine

A

Phenothiazine = Typical antipsychotic
Produces EPS and tardive dyskinesia
D2 antagonist

70
Q

Thioridazine

A

Phenothiazine = Typical antipsychotic
Produces EPS and tardive dyskinesia
D2 antagonist

71
Q

Haloperidol

A

Typical antipsychotic
Highest incidence of EPS
D2 antagonist, more selective for dopamine receptors

72
Q

Thiothixene

A

Typical antipsychotic
D2 antagonist
Thioxanthine structure

73
Q

Clozapine

A

Atypical antipsychotics = no EPS or tardive dyskinesia
Antagonist at 5HT2 more than D2
Some effect on negative symptoms (and positive)
Causes agranulocytosis in 3% of patients
Only in treatment resistant patients

74
Q

Risperidone

A

5HT2 and D2 antagonist
Antipsychotic
EPS at higher doses
No effect on negative symptoms

75
Q

Lurasidone

A

5HT2, D2 and 5HT7 antagonist
Antipsychotic
Less EPS

76
Q

Olanzapine

A

Antipsychotic
5HT2 antagonist more than D2 antagonist
High incidence of weight gain and metabolic syndrome
May improve negative symptoms

77
Q

Quetiapine

A

Antipsychotic
Equal 5HT2 antagonist and D2 antagonist
High incidence of weight gain and metabolic syndrome
May improve negative symptoms

78
Q

Ziprasidone

A

Antipsychotic
5HT2A, D2, and 5HT1D antagonist
5-HT1a agonist

79
Q

Aripiprazole

A

Newer antipsychotic
D2 and 5-HT1a partial agonist
5-HT2a antagonist

80
Q

Phenelzine

A

Monoamine Oxidase Inhibitor
Irreversibly inhibit MAO-A and MAO-B
S/E: Postural hypotension, weight gain, sexual dysfunction
Many drug and food interactions

81
Q

Tranylcypromine

A

Monoamine Oxidase Inhibitor
Irreversibly inhibit MAO-A and MAO-B
S/E: Postural hypotension, weight gain, sexual dysfunction
Many drug and food interactions

82
Q

Amitrptyline

A

Tricyclics antidepressant
Inhibit re-uptake of NE and/or serotonin
Also antagonist at cholinergic, H and alpha receptors
S/E: anticholinergic, orthostatic hypotension, sexual dysfunction, suicide risk

83
Q

Nortriptyline

A

Tricyclics antidepressant
Inhibit re-uptake of NE and/or serotonin
Also antagonist at cholinergic, H and alpha receptors
S/E: anticholinergic, orthostatic hypotension, sexual dysfunction, suicide risk

84
Q

Clomipramine

A

Newer Tricyclics antidepressant
Inhibit re-uptake of NE and/or serotonin
Also antagonist at cholinergic, H and alpha receptors
S/E: anticholinergic, orthostatic hypotension, sexual dysfunction, suicide risk
Improved side effect profile

85
Q

Fluoxetine

A

Selective Serotonin Reuptake inhibitor (SSRI)
S/E: GI symptoms, decreased libido, sexual dysfunction
Low risk of overdose
CYP2D6 inhibitor
Active metabolite inhibits CYP2D6 and CYP3A4

86
Q

Sertraline

A

Selective Serotonin Reuptake inhibitor (SSRI)
S/E: GI symptoms, decreased libido, sexual dysfunction
Low risk of overdose

87
Q

Paroxetine

A

Selective Serotonin Reuptake inhibitor (SSRI)
S/E: GI symptoms, decreased libido, sexual dysfunction
Low risk of overdose
CYP2D6 inhibitor

88
Q

Citalopram

A

Selective Serotonin Reuptake inhibitor (SSRI)
S/E: GI symptoms, decreased libido, sexual dysfunction
Low risk of overdose

89
Q

Escitalopram

A

Selective Serotonin Reuptake inhibitor (SSRI)
S/E: GI symptoms, decreased libido, sexual dysfunction
Low risk of overdose

90
Q

Duloxetine

A

NE and 5-HT uptake inhibitors

Newer drug with improved overall side effect profile

91
Q

Venlafaxine

A

NE and 5-HT uptake inhibitors
Newer drug with improved overall side effect profile
High incidence of discontinuation syndrome, less with timed release

92
Q

Desvenlafaxine

A

NE and 5-HT uptake inhibitors

Newer drug with improved overall side effect profile

93
Q

Levomilnacpran

A

NE and 5-HT uptake inhibitors

Newer drug with improved overall side effect profile

94
Q

Maprotiline

A

NE uptake inhibitor

Used for depression

95
Q

Vilazodone

A

Serotonin uptake inhibitor
5-HT1a partial agonist
S/E: N/V, constipation, and insomnia

96
Q

Vortioxetine

A

Serotonin uptake inhibitor
5-HT3 antagonist and 5-HT1A agonist
S/E: N/V and constipation

97
Q

Mirtazepine

A

Increases 5-HT and NE release by blocking a2 receptors on nerve terminals
Antidepressant
Sedating

98
Q

Bupropion

A

Inhibits dopamine reuptake (effect on 5HT and NE, too)
S/E: CNS stimulation (anxiety, agitation, insomnia, seizures)
Lower incidence of sexual dysfunction than SSRIs

99
Q

Amoxapine

A

Inhibits reuptake of 5HT and NE, but NE more
Dopamine antagonist = antipsychotic activity
S/E similar to TCA plus EPS and tardive dyskinesia

100
Q

Trazodone

A

5-HT2a antagonist
Sedating at low doses
Used as hypnotic and pre-anesthetic
Can cause priapism

101
Q

Lithium

A

May effect ion transport, serotonin system, PI casacade, or arachidonic acid signaling
Narrow therapeutic window
Excreted in urine, diabetes insipidus
Tremor, acne, teratogenic

102
Q

Morphine

A

High efficacy opioid
Poor oral bioavailability
Duration 4-5 hrs

103
Q

Methadone

A

High Efficacy Opioid
Acts for 6hrs, half life 24 hrs
Good oral bioavailability
Used as maintenance in opiate addicts

104
Q

Meperidine

A

High efficacy opioid
Med. acting 2-4 hrs.
Antimuscarinic = tachycardia
Active metabolite normeperidine is psychoactive, can cause seizures

105
Q

Hydromorphone

A

High efficacy opioid

Oral and parenteral

106
Q

Oxymorphone

A

High efficacy opioid
Oral and parenteral
New non-crushable formula

107
Q

Fentanyl

A 
High efficacy opioid 
Short acting 1-1.5 hours 
100x more potent than morphine
Act act mu receptors
Poor oral bioavailability, transdermal forms available
108
Q

Alfentanil

A 
High efficacy opioid 
Very short acting (15-45 minutes)
Very potent
Parenteral only
Used for brief painful procedures
109
Q

Codeine

A

Low efficacy opioid
Oral
Metabolized into morphine by CYP2D6

110
Q

Hydrocodone

A

Moderate efficacy

Oral

111
Q

Oxycodone

A

Full agonist

Moderate-high efficacy opioid

112
Q

Propoxyphene

A

Very low efficacy opioid
Oral
Withdrawn from US due to cardiac toxicity

113
Q

Tramadol

A

Opioid
Inhibits NE and 5-HT re-uptake
Little analgesic effect
May have efficacy for neuropathic pain

114
Q

Buprenorphine

A

Mu partial agonist

Less addictive potential and risk of respiratory depression

115
Q

Butorphanol

A

Kappa agonist, mu partial agonist or antagonist

Less addictive potential and risk of respiratory depression

116
Q

Nalbuphine

A

Kappa agonist, mu antagonist

Less addictive potential and risk of respiratory depression

117
Q

Pentazocine

A

Kappa agonist, mu partial agonist or antagonist

Less addictive potential and risk of respiratory depression

118
Q

Diphenoxylate

A

Antidiarrheal opioid

Doesn’t cross BBB

119
Q

Loperamide

A

Antidiarrheal opioid

Doesn’t cross BBB

120
Q

Dextromethorphan

A

Antitussive opioid

Poor permeation of BBB

121
Q

Naloxone

A

Opioid antagonist
Used for acute overdose
Iv admin can precipitate withdrawal

122
Q

Naltrexone

A

Opioid antagonist
To prevent relapse in recovering addicts
Oral, half life 10 hrs.
Combined with bupropion for weight loss

123
Q

Methylnaltrexone

A 
Opioid antagonist 
For Opioid induced constipation
Poor BBB penetration
Increase risk of bowel perforation
SubCu
124
Q

Naloxegol

A 
Opioid antagonist 
For Opioid induced constipation
Poor BBB penetration
Increase risk of bowel perforation
Oral

IC 2 (1 decks)

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