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S-6 > Drugs > Flashcards

Drugs Flashcards

1
Q

Fluoxetine MOA

A

Block 5HT reuptake transporter

  • downregulate 5HT1a inhibitor autoreceptor in weeks
  • ↓ B-adrenergic and 5HT2 receptors
  • Changes in transcription factors CREB/BDNF
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2
Q

Adverse effects of Fluxoetine

A
  • Nausea (5HT gut)
  • Sexual dysfucntion
  • Anxiety (initial)
  • Drug interactions (CYP)
  • 5HT syndrome (poor CYP metabolizers + other drugs that increases 5HT)
  • Suicide ideation - teenagers/children (fluxoetine approved for peds)
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3
Q

Adverse effects of Paroxetine

A

Weight gain

Most potent CYP inhibitor

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4
Q

Citalopram adaverse

A

↑QT

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5
Q

Venlafaxine/Desvenlafexine/
Duloxietine
MOA

A

Block SERT and NET

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6
Q

Venlafaxine/Desvenlafaxine/
Duloxetine
Side effect

A
  • Anxiety (↑ initally)
  • Sexual dysfunction
  • CV: Arrhtymias, HTN
  • Serotonin syndrome
  • Seizure
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7
Q

Amitryptaline/clomiparmine MOA

A
  • Block NET > SERT
    • Dlayed anti-depression asssoc with downreg of B-adrenergic
    • Antagonist of cholinergic muscarinic/hstamine receptors
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8
Q

Amitriptyline/Clomipramine adverse effects

A
  • Antimuscarinic: Dry mouth, blurry vision, constipation, urinary retention
  • Antihistamine: Wt gain, sedation, drowsiness
  • Cardiac: arrhythmias
  • Convulsions
  • Coma/stupor
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9
Q

Bupropion MOA

A
  • Block DAT and NET
  • nicotinic cholinergic antagonist (↓ craving
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10
Q

Bupropion Adverse

A

Seizure
HTN
Weight loss
Major 2D6 inhibitor (increase SSRI dose)

Advantage: no sexual dysfunction, no sedation

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11
Q

Mirtazapine MOA

A
  • Presynaptic a2 antagonist → ↑NE, 5HT
  • 5HT2a and 6HT1a antagonist
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12
Q

Mirtazapine Side effect

A
  • Antihistamine: Sedative, weight gain, vestibular (dizziness/vertigo)
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13
Q

Trazodone MOA

A
  • 5HT2 and 5HT1a autoreceptor antagonist
  • Block SERT (weak)
  • Blocks a1 (side effect)
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14
Q

Trazadone Adverse

A
  • Antihistamine: sedative, weight gain
  • A1 antagonist effect: orthostatic hypotension, priapism, nasal congestion
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15
Q

Phenelzine/selegiline MOA

A
  • Phenelzine: inhibit MOA-A
  • Selegiline: inhibit MOA-B
  • inhbit enzyme metabolizing NE and 5HT
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16
Q

Phenelzine/selegiline Adverse

A
  • HTN crisis with other sympathomimetics (tyramine)
  • Serotonin syndrome
  • CNS agitation
  • Stroke/seizure
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17
Q

Lithium MOA

A

Uncompetitive inhibitor of inositol monophosphate (regenerate inositol)

  • slow neurotransmitter receptors coupled to PLC 2nd msger system
  • ↓ PKC
  • Inhibit glycogen syntase kinase (GSK3)
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18
Q

Lithium adverse

A
  • Weight gain
  • Polydipsia/polyuria (nephrogenic DI - interfere with ADH)
  • Hypothyroidism
  • Tremor
    Neurotox - Delirum, memory loss, encephalopathy
  • CV: Hx of afrrhythmia/CV disease)
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19
Q

Lithium contraindication

A

Renal failure (completely renal excreted)

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20
Q

Valproate MOA

A
  • Blocks neuronal votage-gated Na+ channel
  • Enhance GABA activity
  • inhibit GSK3 and ↓ PKC
  • Alter Ca2+ current NMDA receptor function
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21
Q

Valproate adverse

A
  • Hepatotox
  • Pancreatitis
  • Hair loss
  • Weight gain
  • Teratogen (OCP)
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22
Q

Lamotrigine MOA

A
  • Anticonvulsant block neuronal Na+ channel
  • Weak VGCC
  • ↓glutamate release
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23
Q

Lamotrigene Adverse

A
  • Dizziness
  • Diplopia
  • SJ/TEN
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24
Q

Carbamazepine
Oxcarbazepine
MOA

A
  • Potent VGSC blocker
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25
Q

Carbamazepine
Oxcarbazepine
Adverse

A

Hepatotoxicity
SJ/ten
Aplastic anemia/agranulocytosis (monthly blood work)
Suicide idealation (especially w/ biopolar
CYP3A4 autoinducer

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26
Q

Aripiprazole
Ziprasidone
Risperidone
Olanzapine
MOA

A

Atypical antipsychotics block D2
High affinity for 5HT2

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27
Q

Morphine MOA

A

Activates MOR → Gi → ↓cAMP → inhibit VGCC and ↑K+ efflux
- Presynpatic and post-synpatic inhibition of excitatory glutamergic neurotransmission

Activates KOR/DOR

  • Hydrophilic: Slow onset/long duration
  • Class: phenanthrene
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28
Q

Morphine adverse

A
  • Miosis
  • Orthostatic hypotension
  • Respiratory depression
  • Pain suppression
  • Histamine release (itch)
  • Increased ICP
  • Nausea
  • Euphoria
  • Sedation/Slowed GI
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29
Q

Hydromorphone MOA

A
  • higher potency than morphine
  • more lipid soluble: faster onset
  • Class: phenanthrene
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30
Q

Hydromorphone use

A

Less histamine release → better for asthmatics

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31
Q

Fentanyl MOA

A
  • More potent than morphine
  • Class: Phenylpiperddine
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32
Q

Metabolism of remifentanil

A

Metabolized by plasma esterase (not liver)

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33
Q

Meperidine MOA

A
  • Block serotonin reuptake
  • Rapid onset/short duration
  • less efficacious than morphine
34
Q

Meperidine Adverse

A
  • Complex CYP metabolism: Pro-convulsant
  • Less antitussive and constipation

Interactions with:

  • Selegiline → seizure
  • MOAI, TCA, SSRI
35
Q

Methadone MOA

A
  • Pure Mu agonist (effiacy = morphine, different tolerance profile)
  • very long acting, bioavailability → Less severe withdraw/less abuse
36
Q

Codeine MOA

A
  • Parital Mu agonist
  • Slow onset, less addictive
  • Metabolized to morphine in brain (2D6) - differential effiacy
37
Q

Codeine adverse

A
  • Nausea
  • Histamine: pruritus
38
Q

Oxycodone MOA

A
  • Stronger partial agonist than codeine (activates all mu subtypes)
39
Q

Oxycodone adverse

A
  • Less nausea/less histamine
  • Aspirin/ibuprofen prep’s not recommended with asthmatics
40
Q

Tramadol MOA

A
  • Partial mu opioid agonist/mixed properties
  • Blocks NET/SERT
41
Q

Tramadol adverse

A
  • opioid related
  • ↑ seizure
  • serotonin syndrome with antidepressants
42
Q

Buprenorphine MOA

A
  • Partial mu agonist/kappa antagonist (greater mu affinity than morphine)
  • Lipophilic → rapid onset, long duration: less withdraw
43
Q

Buprenorphine Adverse

A
  • Sedation
  • Respiratory depression (not reversed)
44
Q

Nalbuphine MOA

A
  • Kappa agonist/mu antagonist
  • Less histamine: less pruritus, nausea, hypotension
  • ceiling effect on respiratory depression
45
Q

Nalbuphine Adverse

A
  • Dysphoric effect (kappa)
  • precipitate withdrawl in mu opioid addicts
46
Q

Pentazocine MOA

A
  • Kappa agonist, weak mu agonist
  • Less efficacy, less addictive, less nausea than morphine
47
Q

Pentazocine Adverse

A
  • Dysphoric
  • hallucination (schizo, dementia)
  • Seizure risks
48
Q

Benzodiazepam MOA

A
  • Allosterically facilitate Cl- influx when endogenous GABA activates GABA-a
    • ↑Frequency of Cl- channel opening
49
Q

Phenytoin MOA

A
  • Bind to inactivated state of VGNC → prevent reopening
50
Q

Phenytoin adverse

A
  • Gingaval hyperplasia
  • Teratogen (fetal hydantoin syndrome)
  • Hepatotoxicity
  • CV: Hypotension/Arrhythmia (OD)
  • Purple glove syndrome (IV)
51
Q

Fosphenytoin MOA

A
  • Same as phenytoin: Bind to inactivated VGSC
  • Rapid onset (converted to phenytoin in body)
52
Q

Fosphenytoin Adverse

A
  • CV: Hypotension/arrythmias
53
Q

Levetiracetam MOA

A
  • Alter synaptic release of GABA
  • ↓Glutamate release?
  • Rapid onset/versatile/well tolerated
54
Q

Levetiracetam Adverse

A
  • Dizziness
  • Ataxia
  • Anxiety
55
Q

Ethosuximide MOA

A
  • Inhibit VGCC (T-type)
56
Q

Ethosuximide use

A
  • Absence sizsure
57
Q

Ethosuximide contraindication

A
  • harmful if used with other VGSC
58
Q

Ethosuximide Adverse

A
  • Dizziness
  • Vomit initially
59
Q

Gabapentin MOA

A
  • VGCC (N-type) blocked by binding to Ca2+a2sigma subunit
60
Q

Gabapentin use

A

Partial seizures

Adjunct

61
Q

Gabapentin adverse

A
  • Dizziness
  • Ataxia
62
Q

Tiagabine MOA

A
  • Inhibit GAT-1 neuronal GABA uptake site → • ↑synaptic GABA
63
Q

Tiagabin adverse

A
  • Dizziness
  • depression
  • psychosis (rare)
64
Q

Topiramate MOA

A
  • Enhance GABA at GABA-a (not BDZ site)
  • AMPA antagonist
65
Q

Topiramate Adverse

A
  • Dizziness
  • Paresthesia, ocnfusion
  • Vision problems/glaucoma (FDA Warning)
66
Q

Vigabatrin MOA

A
  • Inhibit GABA transaminase to increase GABA
67
Q

Vigabatrin adverse

A
  • Somnolence, headache
  • Teragoten
  • psychiatric (depression, psychosis)
68
Q

Benzodiazepine Adverse

A
  • Respiratory depression
  • Anterograde amnesia
  • Sedation
  • Delirium (elderly - use half dose)
  • Behavioral disinhibtion (violence)
  • Dependence/Withdrawal
  • Tolerance develops/cross tolerance
69
Q

Midazolam
Tiazolam
Duration

A

Short duration

70
Q

Lorazepam
Oxazepam
Alprazolam
Temazepam
Duration

A

Intermediate duration

71
Q

BZD for pregancy? for Alcoholic withdrawal?

A

Preg: Lorazepam
Alcoholic: Orazepam

72
Q

Chlordiazepoxide
Diazepam
Clonazepam
Duration and metabolite

A

Long duration (few withdrawals)

All metabolize to oxazepam

73
Q

Buspirone MOA

A
  • 5HT1a autoreceptor partial agonist (downregulation chronic use)
74
Q

Buspirone Adverse

A
  • Serotonin syndrome
  • CV: MI/arrhthymias
  • GI
  • nonaddictive
  • No tolerance/withdraw
  • No rebound anxiety
75
Q

Phenobarbital MOA

A
  • Activate GABA-a → ↑duration Cl- influx
  • Lipid soluble
  • Long acting
  • CYP3A4 inducer
76
Q

Phenobarbitoal Adverse

A
  • Highly sedative
  • Respiratory depression (Narrow TI - no antidote)
77
Q

Zolpidem MOA
Zalepion MOA

A
  • Zolpidem: Bind GABA-a at BZ1 site
  • Zalepion: Bind GABA-a at Omega1 site
78
Q

Zolpidem
Zalepion
Adverse

A
  • Tolerance/rebound insomnia
  • Additive sedative
  • Dizziness, disinhibition, disoreitnation
  • Parasomnia/amnesia
79
Q

Eszopiclone MOA

A
  • Bind GABA-a different than BZD site
  • Short onset, long duration
80
Q

Eszopiclone Adverse

A
  • Dizziness, disinhibition, disorientation
  • Nocturnal enuresis
  • Sexual disorder
  • Amnesia
  • CV: Prolonged ST and arrythmias
81
Q

Propofol MOA

A
  • Activates GABA-a/others
  • Rapid onset, short duration
82
Q

Propofol Adverse

A
  • Hypotension
  • Apnea

S-6 (2 decks)

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