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
Suvorexant
Orexin antagonist | Indicated for difficulties with sleep onset and/or sleep maintenance
26
Trazodone
Blocks 5-HT re-uptake, H1, and alpha1 receptors | Antidepressant used as a hypnotic
27
Primidone
Anticonvulsants Converted to phenobartital and phenylethylmalonamide (PEMA) Effective in patients not responding to phenytoin or phenobarbital Used for Tonic-clonic, partials, and status epilepticus
28
Phenytoin
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
29
Valproic Acid
``` 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 ```
30
Carbamazepine
``` Increases inactivation of Na channels Partial seizures Safe and nontoxic, non sedating Induces microsomal enzymes Blood dyscrasias ```
31
Oxcarbazepine
Increases inactivation of Na channels Like Carbamazepine but less blood dyscrasias Shorter half-life, longer duration of action Fewer drug interactions
32
Lamotrigine
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
33
Topiramate
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
34
Levetiracetam
Modifies synaptic release of GABA via binding to synaptic vesicular protein SV2A Minimal drug interactions, no metabolized by P450 Used for partial seizures
35
Lacosamide
Enhances slow inactivation of Na channels | Used for partial seizures
36
Gabapentin
Decreases glu release by binding volt-gated Ca channels with a2-delta1 subunit. Add on in refractory partial seizures Used for neuropathic pain
37
Pregabalin
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
38
Tiagabine
Inhibits GABA re-uptake | Add-on for partial and tonic-clonic seizures
39
Zonisamide
Increases inactivation of Na channels Add-on for partial seizures Not metabolized by P450 -> minimal drug interactions S/E: Drowsiness, anorexia
40
Ezogabine
K channel facilitator | Add-on for partial seizures
41
Perampenel
AMPA glutamate receptor antagonist | Add-on for partial seizures
42
Eslicarbazepine
Pro-drug | Voltage-gated Na channel blocker
43
Ethosuximide
Inhibits T-type Ca channels Treats Absence seizures May precipitate tonic-clinic seizures
44
Methsuximide
Inhibits T-type Ca channels Treats Absence seizures May precipitate tonic-clinic seizures Used for absence seizures that are refractory t other drugs
45
Levadopa
Dopamine precursor Used to treat Parkinsonism Reverses rigidity, tremor, and bradydinesia S/E: N/V, orthostatic hypotension, psychosis
46
Carbidopa
Blocks AADC in periphery | Decreases dose of L-DOPA and peripheral S/E
47
Selegiline
MAO-B inhibitor Increases dopamine catabolism Treats on-off effect
48
Rasagiline
MAO-B inhibitor Increases dopamine catabolism Treats on-off effect
49
Tolcapone
Catecholamines-O-methyl transferase inhibitor Blocks dopamine and L-DOPA catabolism Central and peripheral Hepatotoxic
50
Entacapone
Catecholamines-O-methyl transferase inhibitor Blocks dopamine and L-DOPA catabolism Peripheral only Not hepatotoxic
51
Pramipexole
D2/D3 agonist
52
Ropinerole
D2/D3 agonist
53
Rotigotine
D1/D2/D3 agonist, transdermal
54
Bromocriptine
D2 agonist | Used with L-DOPA
55
Apomorphine
Non-ergot D1/D2 agonist, sc | Used with L-DOPA
56
Trihexyphenidyl
Anticholinergic | Blocks actions of strictly cholinergic interneurons
57
Benztropine
Anticholinergic | Blocks actions of strictly cholinergic interneurons
58
Procyclidine
Anticholinergic | Blocks actions of strictly cholinergic interneurons
59
Amantadine
Anti-viral that may release dopamaine/be anticholinergic
60
Propranolol
Beta blocker | Used to treat physiologic and essential tremor
61
Baclofen
GABA-b agonist Anti-spastic at the spinal cord S/E: drowsiness, insomnia, weakness, dizziness, ataxia, confusion S/E decreased with intrathecal administration
62
Tizanidine
Alpha2 adrenergic agonist Anti-spastic at the spinal cord S/E: Drowsiness, dry mouth, asthenia, hypotension, hepatotoxicigty, visual hallucinations Metabolized by CYP1A2
63
Dantrolene
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
Botulinum Toxin
Inhibits Ach release from vesicles Anti-spastic at muscle Injected into muscle
65
Cyclobenzaprine
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
Carisoprodol
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
Orphenadrine
Acts as a sedative at brain or spinal cord | For acute muscle spasm from trauma or strain
68
Chlorpromazine
Phenothiazine = Typical antipsychotic Produces EPS and tardive dyskinesia D2 antagonist
69
Fluphenazine
Phenothiazine = Typical antipsychotic Produces EPS and tardive dyskinesia D2 antagonist
70
Thioridazine
Phenothiazine = Typical antipsychotic Produces EPS and tardive dyskinesia D2 antagonist
71
Haloperidol
Typical antipsychotic Highest incidence of EPS D2 antagonist, more selective for dopamine receptors
72
Thiothixene
Typical antipsychotic D2 antagonist Thioxanthine structure
73
Clozapine
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
Risperidone
5HT2 and D2 antagonist Antipsychotic EPS at higher doses No effect on negative symptoms
75
Lurasidone
5HT2, D2 and 5HT7 antagonist Antipsychotic Less EPS
76
Olanzapine
Antipsychotic 5HT2 antagonist more than D2 antagonist High incidence of weight gain and metabolic syndrome May improve negative symptoms
77
Quetiapine
Antipsychotic Equal 5HT2 antagonist and D2 antagonist High incidence of weight gain and metabolic syndrome May improve negative symptoms
78
Ziprasidone
Antipsychotic 5HT2A, D2, and 5HT1D antagonist 5-HT1a agonist
79
Aripiprazole
Newer antipsychotic D2 and 5-HT1a partial agonist 5-HT2a antagonist
80
Phenelzine
Monoamine Oxidase Inhibitor Irreversibly inhibit MAO-A and MAO-B S/E: Postural hypotension, weight gain, sexual dysfunction Many drug and food interactions
81
Tranylcypromine
Monoamine Oxidase Inhibitor Irreversibly inhibit MAO-A and MAO-B S/E: Postural hypotension, weight gain, sexual dysfunction Many drug and food interactions
82
Amitrptyline
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
Nortriptyline
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
Clomipramine
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
Fluoxetine
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
Sertraline
Selective Serotonin Reuptake inhibitor (SSRI) S/E: GI symptoms, decreased libido, sexual dysfunction Low risk of overdose
87
Paroxetine
Selective Serotonin Reuptake inhibitor (SSRI) S/E: GI symptoms, decreased libido, sexual dysfunction Low risk of overdose CYP2D6 inhibitor
88
Citalopram
Selective Serotonin Reuptake inhibitor (SSRI) S/E: GI symptoms, decreased libido, sexual dysfunction Low risk of overdose
89
Escitalopram
Selective Serotonin Reuptake inhibitor (SSRI) S/E: GI symptoms, decreased libido, sexual dysfunction Low risk of overdose
90
Duloxetine
NE and 5-HT uptake inhibitors | Newer drug with improved overall side effect profile
91
Venlafaxine
NE and 5-HT uptake inhibitors Newer drug with improved overall side effect profile High incidence of discontinuation syndrome, less with timed release
92
Desvenlafaxine
NE and 5-HT uptake inhibitors | Newer drug with improved overall side effect profile
93
Levomilnacpran
NE and 5-HT uptake inhibitors | Newer drug with improved overall side effect profile
94
Maprotiline
NE uptake inhibitor | Used for depression
95
Vilazodone
Serotonin uptake inhibitor 5-HT1a partial agonist S/E: N/V, constipation, and insomnia
96
Vortioxetine
Serotonin uptake inhibitor 5-HT3 antagonist and 5-HT1A agonist S/E: N/V and constipation
97
Mirtazepine
Increases 5-HT and NE release by blocking a2 receptors on nerve terminals Antidepressant Sedating
98
Bupropion
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
Amoxapine
Inhibits reuptake of 5HT and NE, but NE more Dopamine antagonist = antipsychotic activity S/E similar to TCA plus EPS and tardive dyskinesia
100
Trazodone
5-HT2a antagonist Sedating at low doses Used as hypnotic and pre-anesthetic Can cause priapism
101
Lithium
May effect ion transport, serotonin system, PI casacade, or arachidonic acid signaling Narrow therapeutic window Excreted in urine, diabetes insipidus Tremor, acne, teratogenic
102
Morphine
High efficacy opioid Poor oral bioavailability Duration 4-5 hrs
103
Methadone
High Efficacy Opioid Acts for 6hrs, half life 24 hrs Good oral bioavailability Used as maintenance in opiate addicts
104
Meperidine
High efficacy opioid Med. acting 2-4 hrs. Antimuscarinic = tachycardia Active metabolite normeperidine is psychoactive, can cause seizures
105
Hydromorphone
High efficacy opioid | Oral and parenteral
106
Oxymorphone
High efficacy opioid Oral and parenteral New non-crushable formula
107
Fentanyl
``` 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
Alfentanil
``` High efficacy opioid Very short acting (15-45 minutes) Very potent Parenteral only Used for brief painful procedures ```
109
Codeine
Low efficacy opioid Oral Metabolized into morphine by CYP2D6
110
Hydrocodone
Moderate efficacy | Oral
111
Oxycodone
Full agonist | Moderate-high efficacy opioid
112
Propoxyphene
Very low efficacy opioid Oral Withdrawn from US due to cardiac toxicity
113
Tramadol
Opioid Inhibits NE and 5-HT re-uptake Little analgesic effect May have efficacy for neuropathic pain
114
Buprenorphine
Mu partial agonist | Less addictive potential and risk of respiratory depression
115
Butorphanol
Kappa agonist, mu partial agonist or antagonist | Less addictive potential and risk of respiratory depression
116
Nalbuphine
Kappa agonist, mu antagonist | Less addictive potential and risk of respiratory depression
117
Pentazocine
Kappa agonist, mu partial agonist or antagonist | Less addictive potential and risk of respiratory depression
118
Diphenoxylate
Antidiarrheal opioid | Doesn't cross BBB
119
Loperamide
Antidiarrheal opioid | Doesn't cross BBB
120
Dextromethorphan
Antitussive opioid | Poor permeation of BBB
121
Naloxone
Opioid antagonist Used for acute overdose Iv admin can precipitate withdrawal
122
Naltrexone
Opioid antagonist To prevent relapse in recovering addicts Oral, half life 10 hrs. Combined with bupropion for weight loss
123
Methylnaltrexone
``` Opioid antagonist For Opioid induced constipation Poor BBB penetration Increase risk of bowel perforation SubCu ```
124
Naloxegol
``` Opioid antagonist For Opioid induced constipation Poor BBB penetration Increase risk of bowel perforation Oral ```