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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
Carbamazepine Oxcarbazepine Adverse
Hepatotoxicity SJ/ten **Aplastic anemia/agranulocytosis (monthly blood work)** Suicide idealation (especially w/ biopolar CYP3A4 autoinducer
26
Aripiprazole Ziprasidone Risperidone Olanzapine MOA
Atypical antipsychotics block D2 High affinity for 5HT2
27
Morphine MOA
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
28
Morphine adverse
- **M**iosis - **O**rthostatic hypotension - **R**espiratory depression - **P**ain suppression - **H**istamine release (itch) - **I**ncreased ICP - **N**ausea - **E**uphoria - **S**edation/Slowed GI
29
Hydromorphone MOA
- higher potency than morphine - more lipid soluble: faster onset - Class: phenanthrene
30
Hydromorphone use
Less histamine release → better for asthmatics
31
Fentanyl MOA
- More potent than morphine - Class: Phenylpiperddine
32
Metabolism of remifentanil
Metabolized by plasma esterase (not liver)
33
Meperidine MOA
- Block serotonin reuptake - Rapid onset/short duration - less efficacious than morphine
34
Meperidine Adverse
- Complex CYP metabolism: Pro-convulsant - Less antitussive and constipation Interactions with: - Selegiline → seizure - MOAI, TCA, SSRI
35
Methadone MOA
- Pure Mu agonist (effiacy = morphine, different tolerance profile) - very long acting, bioavailability → Less severe withdraw/less abuse
36
Codeine MOA
- Parital Mu agonist - Slow onset, less addictive - Metabolized to morphine in brain (2D6) - differential effiacy
37
Codeine adverse
- Nausea - Histamine: pruritus
38
Oxycodone MOA
- Stronger partial agonist than codeine (activates all mu subtypes)
39
Oxycodone adverse
- Less nausea/less histamine - Aspirin/ibuprofen prep's not recommended with asthmatics
40
Tramadol MOA
- Partial mu opioid agonist/mixed properties - Blocks NET/SERT
41
Tramadol adverse
- opioid related - ↑ seizure - serotonin syndrome with antidepressants
42
Buprenorphine MOA
- Partial mu agonist/kappa antagonist (greater mu affinity than morphine) - Lipophilic → rapid onset, long duration: less withdraw
43
Buprenorphine Adverse
- Sedation - Respiratory depression (not reversed)
44
Nalbuphine MOA
- Kappa agonist/mu antagonist - Less histamine: less pruritus, nausea, hypotension - ceiling effect on respiratory depression
45
Nalbuphine Adverse
- Dysphoric effect (kappa) - precipitate withdrawl in mu opioid addicts
46
Pentazocine MOA
- Kappa agonist, weak mu agonist - Less efficacy, less addictive, less nausea than morphine
47
Pentazocine Adverse
- Dysphoric - hallucination (schizo, dementia) - Seizure risks
48
Benzodiazepam MOA
- Allosterically facilitate Cl- influx when endogenous GABA activates GABA-a • ↑Frequency of Cl- channel opening
49
Phenytoin MOA
- Bind to inactivated state of VGNC → prevent reopening
50
Phenytoin adverse
- Gingaval hyperplasia - Teratogen (fetal hydantoin syndrome) - Hepatotoxicity - CV: Hypotension/Arrhythmia (OD) - Purple glove syndrome (IV)
51
Fosphenytoin MOA
- Same as phenytoin: Bind to inactivated VGSC - Rapid onset (converted to phenytoin in body)
52
Fosphenytoin Adverse
- CV: Hypotension/arrythmias
53
Levetiracetam MOA
- Alter synaptic release of GABA - ↓Glutamate release? - Rapid onset/versatile/well tolerated
54
Levetiracetam Adverse
- Dizziness - Ataxia - Anxiety
55
Ethosuximide MOA
- Inhibit VGCC (T-type)
56
Ethosuximide use
- Absence sizsure
57
Ethosuximide contraindication
- harmful if used with other VGSC
58
Ethosuximide Adverse
- Dizziness - Vomit initially
59
Gabapentin MOA
- VGCC (N-type) blocked by binding to Ca2+a2sigma subunit
60
Gabapentin use
Partial seizures Adjunct
61
Gabapentin adverse
- Dizziness - Ataxia
62
Tiagabine MOA
- Inhibit GAT-1 neuronal GABA uptake site → • ↑synaptic GABA
63
Tiagabin adverse
- Dizziness - depression - psychosis (rare)
64
Topiramate MOA
- Enhance GABA at GABA-a (not BDZ site) - AMPA antagonist
65
Topiramate Adverse
- Dizziness - Paresthesia, ocnfusion - Vision problems/glaucoma (FDA Warning)
66
Vigabatrin MOA
- Inhibit GABA transaminase to increase GABA
67
Vigabatrin adverse
- Somnolence, headache - Teragoten - psychiatric (depression, psychosis)
68
Benzodiazepine Adverse
- Respiratory depression - Anterograde amnesia - Sedation - Delirium (elderly - use half dose) - Behavioral disinhibtion (violence) - Dependence/Withdrawal - Tolerance develops/cross tolerance
69
Midazolam Tiazolam Duration
Short duration
70
Lorazepam Oxazepam Alprazolam Temazepam Duration
Intermediate duration
71
BZD for pregancy? for Alcoholic withdrawal?
Preg: Lorazepam Alcoholic: Orazepam
72
Chlordiazepoxide Diazepam Clonazepam Duration and metabolite
Long duration (few withdrawals) All metabolize to oxazepam
73
Buspirone MOA
- 5HT1a autoreceptor partial agonist (downregulation chronic use)
74
Buspirone Adverse
- Serotonin syndrome - CV: MI/arrhthymias - GI - nonaddictive - No tolerance/withdraw - No rebound anxiety
75
Phenobarbital MOA
- Activate GABA-a → ↑duration Cl- influx - Lipid soluble - Long acting - CYP3A4 inducer
76
Phenobarbitoal Adverse
- Highly sedative - Respiratory depression (Narrow TI - no antidote)
77
Zolpidem MOA Zalepion MOA
- Zolpidem: Bind GABA-a at BZ1 site - Zalepion: Bind GABA-a at Omega1 site
78
Zolpidem Zalepion Adverse
- Tolerance/rebound insomnia - Additive sedative - Dizziness, disinhibition, disoreitnation - Parasomnia/amnesia
79
Eszopiclone MOA
- Bind GABA-a different than BZD site - Short onset, long duration
80
Eszopiclone Adverse
- Dizziness, disinhibition, disorientation - Nocturnal enuresis - Sexual disorder - Amnesia - CV: Prolonged ST and arrythmias
81
Propofol MOA
- Activates GABA-a/others - Rapid onset, short duration
82
Propofol Adverse
- Hypotension - Apnea

S-6 (2 decks)

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