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PRITE > Pharmacology PRITE Review (JB PPT) Part 1 > Flashcards

Pharmacology PRITE Review (JB PPT) Part 1 Flashcards

1
Q

What is the first pass effect?

A

Phenomenon in which a drug gets metabolized at a specific location in the body that results in a reduced concentration of the active drug upon reaching its site of action or the systemic circulation

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2
Q

How does Phase 1 metabolism occur? Phase 2?

A

Phase 1 - CYP450 enzymes (i.e., via oxidation)

Phase 2 - Glucuronidation

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3
Q

What is the difference between a pharmacodynamic vs. pharmacokinetic interaction?

A

Dynamic - alteration due to changes in drug binding to a receptor site

Kinetic - alteration due to changes in absorption, distribution, metabolism, or excretion

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4
Q

Important considerations of drug metabolism in the elderly?

A
  • Elderly patients have a decreased GFR
  • Decreased liver Phase 1 oxidation (CYP enzymes)
  • Absorption is UNCHANGED
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5
Q

Important considerations of drug metabolism in newborns?

A
  • Drug absorption and transportation is equivalent to adults at approximately 4 months old
  • GFR and CYP enzymes in children are equivalent to adults at approximately 1 year old
  • Immediately after birth, babies have a lower GFR than adults, but it increases rapidly
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6
Q

Important considerations of drug metabolism in pregnant women?

A
  • Increased GFR and renal blood flow rate

- Increased blood volume and cardiac output (by 30-50%)

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7
Q

List key landmark drug trials in psychiatry.

A
  1. CATIE trial
  2. STAR*D trial
  3. COMBINE trial
  4. 1999 Multimodal Treatment Study of kids of ADHD
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8
Q

Medications involved in CATIE trial + key finding?

A

Olanzapine, perphenazine, quetiapine, risperidone, ziprasidone

Olanzapine was more effective at reducing agitation, hostility, aggression

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9
Q

Key findings of STAR*D trial?

A
  • Depression study
  • Only about 1/3 of patients remit with first antidepressant
  • Typical placebo response is also ~30%
  • Bupropion augmentation is more effective and better tolerated than buspirone
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10
Q

Key findings of COMBINE trial?

A

Any combination of therapies including CBI, naltrexone, or both performed better than any combination that did not include these interventions.

Acamprosate fared poorly compared to various combinations of naltrexone/CBI.

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11
Q

Key finding of 1999 Multimodal Treatment Study of kids with ADHD?

A

Medication alone = medication + psychosocial interventions.

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12
Q

List FDA-approved medications for the treatment of MDD (MAOIs - 4).

A
  1. Isocarboxazid
  2. Phenelzine
  3. Selegiline (MAO-B selective)
  4. Tranylcypromine
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13
Q

List FDA-approved medications for the treatment of MDD (TCAs - 7).

A
  1. Amitriptyline
  2. Clomipramine
  3. Desipramine
  4. Doxepin
  5. Imipramine
  6. Nortriptyline
  7. Trimipramine
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14
Q

List FDA-approved medications for the treatment of MDD (TeCAs - tetracyclic antidepressants - 3).

A
  1. Amoxapine
  2. Maprotiline
  3. Mirtazapine
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15
Q

List FDA-approved medications for the treatment of MDD (NDRI - norepinephrine-dopamine reuptake inhibitors - 1).

A
  1. Bupropion
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16
Q

List FDA-approved medications for the treatment of MDD (SSRIs - 6).

A
  1. Citalopram
  2. Escitalopram
  3. Fluoxetine
  4. Fluvoxamine
  5. Paroxetine
  6. Sertraline
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17
Q

List FDA-approved medications for the treatment of MDD (SNRIs - 4).

A
  1. Desvenlafaxine
  2. Duloxetine
  3. Levomilnacipran
  4. Venlafaxine
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18
Q

List FDA-approved medications for the treatment of MDD (SRI/SRMs - serotonin reuptake inhibitors/modulators).

A
  1. Nefazodone
  2. Trazodone
  3. Vilazodone
  4. Vortioxetine
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19
Q

Augmentation options for the treatment of depression (6)?

A
  1. Bupropion
  2. Atypical antipsychotics (aripiprazole, olanzapine, quetiapine, risperidone)
  3. Buspirone
  4. Lithium
  5. Liothyronine (T3)
  6. Mirtazapine
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20
Q

MDD with atypical features?

A

A. Mood reactivity (mood brightens in response to positive events)
B. 2 or more of the following:
1. Hypersomnia
2. Increased appetite/weight gain
3. Leaden paralysis (heavy feeling in arms and legs)
4. Interpersonal rejection sensitivity (persistent lifelong trait that may be exacerbated during periods of depression; characterized by sensitivity to rejection and/or criticism)

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21
Q

Key treatment of atypical depression?

A

MAOI

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22
Q

MDD with melancholic features?

A

A. One of the following is present during the most severe period of the current episode:

  1. Loss of pleasure in all, or almost all, activities
  2. Lack of reactivity to usually pleasurable stimuli (does not feel much better, even temporarily, when something good happens)

B. 3+ of the following:

  1. Distinct quality of depressed mood characterized by profound despondency, despair, and/or moroseness or by so-called empty mood
  2. Depression worse in the morning
  3. Early-morning awakening (at least 2 hours before usual)
  4. Marked PMA/PMR
  5. Significant anorexia or weight loss
  6. Excessive or inappropriate guilt
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23
Q

List the selective MAOIs.

A

MAO-A: clorgiline and moclobedmie

MAO-B: selegiline (at low doses)

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24
Q

List the non-selective MAOIs.

A

Isocarboxazid, phenelzine, selegiline (at high doses), tranylcypromine

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25
Q

List the reversible MAOIs.

A

Moclobemide

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26
Q

List the irreversible MAOIs.

A

Clorgiline, isocarboxazid, phenelzine, selegiline, tranylcypromine

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27
Q

How do dietary restrictions vary for MAO-A vs. MAO-B?

A

MAO-A - must follow diet; MAO-A is found in the gut and uses tyramine as a substitute

MAO-B - no dietary restrictions needed (unless taking at very high doses)

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28
Q

What is the purpose of the dietary restriction when taking MAOIs?

A

Tyramine-induced hypertensive crisis

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29
Q

Substrates of MAO-As?

A

Serotonin
Norepinephrine
Dopamine
Tyramine

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30
Q

Substrates of MAO-Bs?

A

Dopamine

Phenylethylamine

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31
Q

Tissue localization of MAO-As?

A 
Brain
Gut
Liver
Placenta
Skin
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32
Q

Tissue localization of MAO-Bs?

A

Brain
Platelets
Lymphocytes

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33
Q

Formulations of selegiline?

A

Oral

Transdermal patch

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34
Q

How is moclobemide unique compared to other MAOI-A’s?

A

Fewer tyramine dietary restrictions

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35
Q

Treatment of MAOI hypertensive crisis?

A

Phentolamine
Calcium channel blockers (e.g., nifedipine)
Nitroprusside
Nitroglycerin

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36
Q

MAOIs increase risk of ___ when taken with certain other medications.

A

Serotonin syndrome

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37
Q

Treatment options for anxiety?

A
  1. SSRI
  2. SNRI
  3. Buspirone
  4. Mirtazapine
  5. Propranolol
  6. Gabapentin
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38
Q

MOA - buspirone?

A

5-HT1A agonist

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39
Q

MOA - gabapentin?

A

Indirectly acts as a GABA agonist by modulating voltage-gated calcium channels (VGCC)

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40
Q

FDA-approved medications for anxiety (antihistamine)?

A

Hydroxyzine (non-specific anxiety)

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41
Q

Adverse effects of antihistamines like hydroxyzine?

A

Dizziness
Dry mouth
Headache
Sedation

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42
Q

FDA-approved medications for anxiety (benzodiazepines)?

A
  1. Alprazolam (non-specific; panic disorder)
  2. Chlordiazepoxide (non-specific)
  3. Clonazepam (panic disorder)
  4. Diazepam (non-specific)
  5. Lorazepam (non-specific)
  6. Oxazepam (non-specific)
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43
Q

Adverse effects of benzodiazepines?

A

Appetite change
Cognitive problems
Fatigue
Somnolence

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44
Q

FDA-approved medications for anxiety (SSRIs)?

A
  1. Escitalopram (GAD)
  2. Fluoxetine (panic disorder)
  3. Fluvoxamine (social anxiety disorder)
  4. Paroxetine (GAD, panic disorder, PTSD, social anxiety disorder)
  5. Sertraline (panic disorder, PTSD, social anxiety disorder)
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45
Q

FDA-approved medications for anxiety (SNRIs)?

A
  1. Duloxetine (GAD)

2. Venlafaxine (GAD, panic disorder, social anxiety disorder)

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46
Q

Adverse effects of SSRIs/SNRIs?

A

Diarrhea, headache, HTN, insomnia, nausea, sexual dysfunction, somnolence

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47
Q

What is buspirone approved for and what adverse effects can it cause?

A

Non-specific anxiety

Dizziness, headache, nausea

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48
Q

Which LAIs are FDA-approved for bipolar maintenance in addition to schizophrenia?

A
  1. Abilify Maintena

2. Risperdal Consta

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49
Q

List the two first generation LAIs.

A
  1. Prolixin decanoate (fluphenazine)

2. Haldol decanoate

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50
Q

List the 8 second generation LAIs.

A
  1. Abilify Maintena (aripiprazole monohydrate)
  2. Aristada (aripiprazole lauroxil)
  3. Aristada Initio (aripiprazole lauroxil)
  4. Invega Sustenna (paliperidone palmitate)
  5. Invega Trinza (12-week)
  6. Risperdal Consta
  7. Perseris (risperidone subcutaneous)
  8. Zyprexa Relprevv (olanzapine)
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51
Q

List the LAIs that require PO overlap.

A
  1. Prolixin decanoate
  2. Abilify Maintena
  3. Aristada (unless giving Aristada Initio IM + 1 PO dose
  4. Risperdal Consta
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52
Q

List the medications FDA-approved for acute bipolar depression.

A
  1. Olanzapine/fluoxetine (Symbyax)
  2. Quetiapine + quetiapine XR
  3. Lurasidone
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53
Q

List the medications FDA-approved for acute bipolar mania.

A
  1. Lithium
  2. Chlorpromazine
  3. Divalproex + ER
  4. Olanzapine
  5. Risperidone
  6. Quetiapine + XR
  7. Ziprasidone
  8. Aripiprazole
  9. Carbamazepine ER
  10. Asenapine
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54
Q

List the medications FDA-approved for bipolar maintenance.

A
  1. Lithium
  2. Lamotrigine
  3. Olanzapine
  4. Aripiprazole
  5. Quetiapine + XR
  6. Risperidone LAI
  7. Ziprasidone
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55
Q

Which mood stabilizer is NOT FDA-approved for bipolar maintenance?

A

Depakote

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56
Q

Which medication should NOT be used fo treatment of acute mania?

A

Lamotrigine

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57
Q

What is the best treatment for acute mania?

A

(Lithium or Depakote) + antipsychotic

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58
Q

Preferred treatment for rapid cycling?

A

Depakote

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59
Q

Preferred treatment for mixed episodes?

A

Depakote

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60
Q

Lab work-up for patients who develop rapid cycling must include what and why?

A

TSH; new onset rapid cycling bipolar is associated with hypothyroidism

61
Q

Recommended dosing of Depakote?

A

Weigh-based - 15-20 mg/kg/day

62
Q

Treatment options for OCD?

A
  1. Clomipramine (TCA; only FDA-approved TCA for OCD)
  2. Fluvoxamine (SSRI, only approved for OCD)
  3. Other SSRIs
63
Q

Treatment options for PTSD?

A
  1. FDA-approved - paroxetine and sertraline

2. Off-label - prazosin

64
Q

Medications approved for treatment of MDD in pediatrics?

A

Fluoxetine, escitalopram, sertraline, fluvoxamine, clomipramine

65
Q

Medications approved for treatment of OCD in pediatrics?

A

Fluoxetine, escitalopram

66
Q

Medications approved for treatment of GAD in pediatrics?

A

Duloxetine

67
Q

First-line treatments of ADHD?

A

Methylphenidate and amphetamine

68
Q

Alternative treatments for ADHD?

A

Alpha-2-agonists: clonidine (Kapvay), guanfacine (Intuniv)

Atomoxetine (Strattera; SNRI)

Bupropion (Wellbutrin; NDRI)

69
Q

DSM-5 definition of tics?

A

Sudden, rapid, recurrent, non-rhythmic motor movement or vocalization

70
Q

DSM-5 definition of Tourette’s Disorder?

A

A. Both multiple motor and one or more vocal tics present at some time during the illness, although not necessarily concurrently.
B. Tics may wax and wane in frequency but have persisted for >1 year since first tic onset
C. Onset before age 18

71
Q

DDx for Tourette’s

A

Persistent (chronic) motor or vocal tic disorder

72
Q

Commonly used medications for treatment of Tourette Syndrome?

A

Alpha-agonists: clonidine, gunafacine

Antipsychotics: haloperidol, fluphenazine, pimozide, risperidone

Dopamine depleter: tetrabenazine

73
Q

FDA-approved treatment of Tourette’s

A

Haloperidol

Pimozide

74
Q

Medications used to treat anorexia/bulimia?

A

Mirtazapine
Fluoxetine
Olanzapine + fluoxetine
Cyproheptadine (appetite stimulant)

75
Q

Medications used to treat binge-eating?

A

Lisdexamfetamine (Vyvanse)
Topiramate
Sibutramine (appetite suppressant)

76
Q

FDA-approved medications to treat anorexia?

A

None

77
Q

FDA-approved medications to treat bulemia?

A

Fluoxetine

78
Q

FDA-approved medications to treat binge-eating?

A

Lisdexamfetamine (Vyvanse)

79
Q

Treatment for narcolepsy?

A

No single treatment - medications are used to target symptoms

80
Q

List 4 common features of narcolepsy.

A
  1. Excessive daytime sleepiness
  2. Cataplexy
  3. Sleep paralysis
  4. Hyponagogic/hypnopompic hallucinations
81
Q

What is the best diagnostic marker of narcolepsy?

A

Cataplexy (sudden episode of bilateral muscle weakness triggered by the onset of strong emotions) - examples include buckling/unlocking of knees, head or jaw dropping, facial muscle flickering, sagging of jaw/weakness in arms, garbled speech/voice

82
Q

Treatment options for excessive daytime sleepiness in narcolepsy?

A
  1. Modafinil, armodafinil
  2. Methylphenidate, dextroamphetamine, amphetamine-dextroamphetamine
  3. Sodium oxybate
83
Q

Treatment options for cataplexy in narcolepsy?

A

Venlafaxine
Fluoxetine
Clomipramine
Sodium oxybate

84
Q

Which narcolepsy treatment can target both daytime sleepiness and cataplexy?

A

Sodium oxybate (GHB)

85
Q

Medications FDA-approved for treatment of autism or ID?

A

None

86
Q

Medications FDA-approved for pediatric irritability/aggression in autism?

A

Risperidone

Aripiprazole

87
Q

Off-label medication classes used for patients with ASD and/or ID?

A
  1. SGAs (targeting irritability, aggression, self-injury, severe tantrums)
  2. Alpha-2 agonists (inattention, hyperactivity)
  3. Stimulants (inattention, hyperactivity)
  4. SSRIs (anxiety-related symptoms)
  5. Anti-epileptics (irritability, repetitive behaviors)
88
Q

FDA-approved treatment for dementia?

A
  1. Donepezil - MILD TO SEVERE
  2. Galantamine - MILD TO MODERATE
  3. Rivastigmine - MILD TO MODERATE
  4. Memantine - MODERATE TO SEVERE memory impairment
89
Q

MOA of donepezil/galantamine/rivastigmine?

A

Cholinesterase inhibitor

90
Q

MOA of memantine

A

NMDA receptor agonist

91
Q

Medications to treat symptoms of Parkinson’s disease?

A
  1. Dopamine precursors (levodopa)
  2. Dopamine agonists (pramipexole, ropinirole, bromocriptine, pergolide, cabergoline)
  3. COMT inhibitors (entacapone, tolcapone)
  4. MAO-B inhibitors (selegiline, rasagiline)
  5. Anticholinergics (benzotropine, trihexyphenidyl)
  6. Other - amantadine
92
Q

MOA carbidopa/levodopa?

A

Levodopa - converted in the brain to dopamine

Carbidopa - prevents levodopa from being converted into dopamine in the peripheral circulation

93
Q

Compare pros and cons of Carbidopa/levodopa compared to direct dopamine agonists.

A

L-Dopa: significantly improves mobility; does not slow disease progression, increased doses needed to maintain efficacy

Dopamine agonists: less motor fluctuations than L-Dopa; does not slow disease progression, not as effective, causes daytime sleepiness, hallucinations, impulsivity

94
Q

Pros/cons of anticholinergics (benztropine, trihexyphenidyl) in Parkinson’s?

A

+ helpful to relieve tremor and may ease dystonia

  • side effects (blurred vision, dry mouth, constipation, urinary retention, hallucinations)
95
Q

MOA of MAO-B inhibitors and COMT inhibitors in Parkinson’s?

A

Prolongs the effect of L-dopa by blocking its metabolism

96
Q

Pros/cons of MAO-B and COMT inhibitors in Parkinson’s?

A

Mao-B: may have mild antidepressant effect; small benefit, multiple interactions

COMT: improves mobility, may lead to increased L-Dopa side effects

97
Q

FDA-approved medication for treatment of Psychosis in Parkinson’s? Typical correct answer for treatment of psychosis in Parkinson’s (not FDA-approved)

A

Pimavanserin

Quetiapine and clozapine

98
Q

Why are quetiapine and clozapine the best options for treatment of psychosis in Parkinson’s?

A

D2 antagonism worsens motor features of Parkinson’s

Quetiapine and clozapine ahve very low affinity for D2

99
Q

MOA - pimavanserin?

A

Atypical antipsychotic

Antagonist/inverse agonist at 5-HT2A and 5-HT2C (to a lesser extent)

100
Q

Classes of medications used to treat insomnia?

A
  1. Antidepressants (mirtazapine, trazodone, doxepin –> FDA-approved)
  2. Anti-histamines (hydroxyzine, diphenhydramine)
  3. Melatonin (OTC melatonin supplements; ramelteon)
  4. Orexin receptor antagonists (suvorexant)
  5. Z drugs (Zaleplon, zolpidem, eszopiclone)
  6. Benzodiazepines (temazepam)
101
Q

Similarities and differences of Z-drugs and benzos?

A

Not structurally related, but similar MOA - both allosterically modulate GABA-A receptors, binding occurs in nearby areas of the alpha subunit

Z-drugs do not significantly alter sleep architecture like benzodiazepines, better safety profile (less respiratory depression)

102
Q

What condition should be ruled out as a potential etiology of RLS?

A

Iron deficiency anemia

103
Q

Treatment of RLS?

A

Dopamine agonists (ropinirole, pramipexole, rotigotine patch are FDA-approved; pergolide, though not FDA-approved)

Gabapentin enacarbil

104
Q

Rx premature ejaculation

A

SSRIs in high doses (paroxetine on PRITE)

105
Q

First-step in treating TD?

A

Switch from FGA to an SGA with lower D2 affinity (clozapine, quetiapine)

106
Q

Medications used to treat TD?

A

FDA-approved: valbenazine, deutetrabenazine

Not FDA-approved: tetrabenazine

107
Q

Indications for tetrabenazine?

A

Huntington’s
Tourette’s
Hemibalism
TD

108
Q

Treatment of ALS + MOA?

A

Riluzole (glutamate antagonist

109
Q

St. John’s wart (aka hypericum perforatum) is sometimes used for depression - it increases risk for what adverse event?

A

Serotonin syndrome

110
Q

What is valerian root used for?

A

Sleep (hypnotic)

111
Q

Risk asociated with ginko biloba?

A

Bleeding

112
Q

Pain indication for the following TCAs:

  1. Amitriptyline
  2. Desipramine
  3. Doxepin
  4. Nortriptyline
A
  1. Amitriptyline - chronic pain
  2. Desipramine - post-herpetic neuralgia
  3. Doxepin - limited data for LBP
  4. Nortriptyline - post-herpetic neuralgia

(All off-label)

113
Q

Contraindications to TCA use

A

Concurrent use/use within 2 weeks of MAOIs, MI (acute recovery period), glaucoma (doxepin), tendency for urinary retention (doxepin); caution in elderly due to risk for postural hypotension; sedating

114
Q

Pain indication for the following SNRIs:

  1. Duloxetine
  2. Milnacipran
  3. Venlafaxine
A
  1. Duloxetine - chronic MSK; neuropathic; fibromyalgia
  2. Milnacipran - fibromyalgia
  3. Venlafaxine - GAD, mDD, panic disorders, SAD
115
Q

___ are generally not the preferred antidepressants for neuropathic pain but may be useful for ___.

A

SSRIs; fibromyalgia

116
Q

Pain indication for the following SSRIs:

  1. Fluoxetine
  2. Paroxetine
A

Neuropathic pain (off-label for both)

117
Q

FDA-approved indication (pain management) for the following anticonvulsants:

  1. Carbamazepine
  2. Gabapentin
  3. Pregabalin
  4. Topiramate
  5. Depakote
A
  1. Carbamazepine - trigeminal neuralgia
  2. Gabapentin - Post-herpetic neuralgia
  3. Pregabalin - Post-herpetic neuralgia, diabetic neuropathy, fibomyalgia, polyneuropathy
  4. Topiramate - migraine prophylaxis
  5. Depakote - migraine prophylaxis
118
Q

MOA - SSRI

A

Selectively inhibits the reuptake of 5-HT at the presynaptic neuronal membrane

119
Q

MOA - SNRI

A

Inhibits reuptake of both serotonin and norepinephrine at the pre-synaptic membrane; also weakly inhibits dopamine reuptake

120
Q

MOA - NDRI (example)

A

Norepinephrine and Dopamine Reuptake Inhibitor; Bupropion; inhibits reuptake of both norepinephrine and dopamine at the pre-synaptic membrane

121
Q

MOA - SARI (examples)

A

Serotonin Antagonist and Reuptake Inhibitor; trazodone and nefazodone; antagonist at the serotonin receptor; also inhibits the reuptake of serotonin as well as NE and/or dopamine

122
Q

MOA - NaSSA (example)

A

Noradrenergic and Specific Serotonergic Antidepressant (Mirtazapine); antagonist at the alpha-2-adrenergic receptor fo the presynaptic membrane causes increased release of NE. Also antagonizes certain serotonin receptors.

123
Q

MOA - TCA

A

Inhibits reuptake of both 5HT and NE at the presynaptic membrane

124
Q

MOA - MAOI

A

Inhibits activity of monoamine oxidase, which prevents degradation of serotonin, norepinephrine, and dopamine

125
Q

SSRI with the longest half-life?

A

Fluoxetine

126
Q

SSRI with the shortest half-life?

A

Fluvoxamine (NOT PAXIL)

127
Q

Antidepressant (all categories) with shortest half-life?

A

Trazodone

128
Q

Antidepressants that have active metabolites that extend their duration of action?

A

Sertraline

Fluoxetine

129
Q

Mirtazapine MOA?

A

Antagonist at alpha-2-adrenergic, 5HT2A-2C, H1

130
Q

Which antidepressant is not serotonergic?

A

Bupropion

131
Q

Uses for bupropion?

A 
Smoking cessation
Weight loss
ADHD
"Treat" antidepressant-related sexual dysfunction (switch or add)
Adjunctive depression treatment
132
Q

MOA - buspirone?

A

5HT-1A pre-synaptic (full agonist)
5HT-1A post-synaptic (partial agonist, especially hippocampus and cortex)
D2, D3, D4 (antagonist)
A1-adrenergic (agonist)

133
Q

MOA of vortioxetine?

A

Antagonist: 5HT3A, 5HT7, 5HT1D, beta-1 receptor
Agonist: 5HT1A
Partial agonist: 5HT1B

134
Q

MOA of vilazodone?

A

SSRI and 5HT1A partial agonist

135
Q

MOA of L-minacepran?

A

SNRI in extended-release formulation

136
Q

MOA of mifepristone?

A

Glucocorticoid receptor antagonist
Progesterone antagonist
Studied as an adjunct to antidepressants in psychotic depression

137
Q

Discuss nortriptyline’s curvilinear dose curve.

A

Can sometimes see improvement in depression symptoms by decreasing the dose; can have a plateau or decline effect at higher plasma concentrations

138
Q

Impact of bupropion on REM sleep

A

Increases

139
Q

MOA - gabapentin?

A

Inhibits calcium channels, specifically acting at the alpha-2-delta subunit of voltage-dependent calcium channels; mimics GABA but does not bind GABA receptors

140
Q

MOA - baclofen?

A

GABA-B agonist

141
Q

MOA - benzodiazepines?

A

GABA-A modulator/agonist

142
Q

MOA - barbitureates?

A

GABA-A agonist (can open the GABA-A channel in the absence of GABA)

143
Q

MOA - Z-drugs?

A

GABA- A modulator/agonist

144
Q

MOA - EtOH

A

GABA-A agonist

145
Q

MOA - flumazenil?

A

GABA-A receptor antagonist

146
Q

Compare the MOA of benzos vs. barbiturates.

A

Bind to GABA-A receptor at different allosteric sites
Facilitate GABA action
- Barbiturates increase duration of opening of chloride channel
- Benzodiazepines increase frequency of opening of chloride channel
Membrane hyperpolarization
CNS depression

147
Q

Liver-safe benzodiazepiens + why?

A

Lorazepam, Oxazepam, Temazepam

Metabolized via liver glucuronidation (instead of CYP), don’t generate active metabolites

148
Q

What is the most rapidly orally absorbed benzo?

A

Diazepam

149
Q

Diazepam is metabolized to what three metabolites?

A

Nordiazepam
Temazepam
Oxazepam

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