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PHARMA I > SECTION II DRUGS > Flashcards

SECTION II DRUGS Flashcards

1
Q

CNS

  • First line for major depressive disorder
  • Inhibits 5-HT (serotonin) transporter reuptake
  • Black box warning: You may have suicidal thoughts
A

SSRI

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2
Q

CNS

  • Most active SSRI with a long half-life
  • Strong CYP2D6 inhibitor
  • Pregnancy category C
  • Most unlikely to cause discontinuation syndrome
  • 5-6 week washout period; stays in the system for a
    long time
A

Fluoxetine (SSRI)

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3
Q

CNS

  • Sedating SSRI that is a strong CYP1A2 inhibitor
  • Pregnancy category C
  • Use to treat OCD
A

Fluvoxamine (SSRI)

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4
Q

CNS

  • Causes weight gain, strong CYP2D6 inhibitor
  • Pregnancy category D
  • Can cause sexual dysfunction
  • Treats a lot of symptoms due to high affinity
A

Paroxetine (SSRI)

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5
Q

CNS

  • Causes more GI upset compared to other SSRIs
  • Pregnancy category C
  • Could cause discontinuation syndrome
A

Sertraline (SSRI)

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6
Q

CNS

  • Enantiomer of citalopram with QT prolongation
  • No clinical advantage over citalopram
A

Escitalopram (SSRI)

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7
Q

CNS

  • Inhibits serotonin and NE transporter for reuptake
A

SNRI

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8
Q

CNS

  • Has multiple pain indications and therefore very broad coverage for treatment
  • Any dose can cause serotonin and NE transporters to be inhibited
  • Can cause liver toxicity
A

Duloxetine (SNRI)

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9
Q

CNS

  • Causes serotonin reuptake to be inhibited at low
    doses
  • Causes NE reuptake to be inhibited at high doses
  • Has hypertensive effects at higher doses, and can
    result in cardiotoxicity
A

Venlafaxine (SNRI)

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10
Q

CNS

  • Only used for fibromyalgia
  • Levomilnacipran has higher activity at NE receptor reuptake inhibition
A

Milnacipran (SNRI)

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11
Q

CNS

  • Tranylcypromine, isocarboxazid, phenelzine,
    selegiline
  • Binds to MAO-A and MAO-B irreversibly, which
    increase concentrations of 5-HT, NE, DA
  • Treats atypical depression
  • MAO-A breaks down serotonin, tyramine, NE, DA in
    brain and GI
  • MAO-B break down DA and tyramine in brain
  • May cause serotonin syndrome
  • Discontinue 10 days before surgery
  • Average 14 day washout period
  • Could cause orthostatic hypotension
  • Patient with ADHD should NOT take MAO-I
A

MAO-inhibitors

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12
Q

CNS

-Selectively taken at low doses to reduce depression
- Useful for treatment of Parkinson’s disease, delays
motor complications
- Selective MAO-B inhibitor; for brain
- Use within 10 days prior to Sx is contraindication
- Interacts with SSRI, SNRI, TCA

A

Selegiline
Rasagiline
Safinamide (MAO-B
inhibitor)

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13
Q

CNS

  • First line for major depressive disorder and social anxiety disorders
  • Does not cause sexual dysfunction
  • Physical stimulus first and then cognitive
  • Most widespread effects, related to weight loss,
    smoking cessation
A

Bupropion (Misc. antidepressant)

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14
Q

CNS

  • Central alpha-2 receptor antagonist, increases
    release of NE and 5HT
  • Appetite and weight gain
  • Little to no sexual effects
A

Mirtazapine (Misc.

antidepressant)

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15
Q

CNS

  • inhibits serotonin transport reuptake and
    antagonizes 5HT2A
  • Orthostatic hypotension (α1 antagonist)
  • Sedative at low doses (H1 antagonist))
A

Trazodone (Misc.

Antidepressant)

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16
Q

CNS

  • Black box: hepatotoxicity!
  • CYP3A4 inhibitor
  • Blocks 5HT2A
A

Nefazodone (Misc.

Antidepressant)

17
Q

CNS

  • 5HT1A agonist, 5HT2A antagonist
A

Vilazodone (Misc.

Antidepressant)

18
Q

CNS

  • 5HT2A and 5HT3 antagonist, 5HT1A agonist
A

Vortioxetine (Misc.

Antidepressant)

19
Q

CNS

  • Anxiolytic, for GAD, generally as effective as BZD
  • No dependence issues, CNS depression
  • Pregnancy category B
20
Q

CNS

  • Enhances activity of GABA resulting in hypnosedative and amnesic effects
  • Zolipdem, zaleplon, eszopiclone
  • Less potential for rebound insomnia, tolerance and
    dependence than BZD
  • Blackbox: complex sleep behavior
  • Avoid for patients with hepatic disease and sleep
    apnea
A

Nonbenzodiazepine benzodiazepine

21
Q

Melatonin receptor agonist

  • No activity on GABA
  • Lasts 2-5 hours, no dependence, can treat chronic insomnia
A

Ramelteon (Misc. insomnia)

22
Q
  • Orexin receptor antagonist, Schedule IV drug
  • Contraindicated in narcolepsy
  • Affects REM sleep, sleep paralysis
A

Suvorexant (Misc.

insomnia)

23
Q

D2 Receptor CNS

  • Low potency: chlorpromazine, thioridazine
  • Mild potency: loxapine, perphenazine
  • High potency: trifluoperazine, thiothixene,
    fluphenazine, haloperidol
  • Decreases central dopamine neurotransmission
    primarily through D2 blockade
  • Agents block muscarinic, α1 and H1 receptors
  • Severe D2 blockade causes neuroleptic malignant syndrome, but could be treated with dantrolene
  • Dopamine blockade causes hyperprolactinemia and extrapyramidal symptoms
  • Abnormal involvement movement scale is used to
    detect and monitor EPS
A

First generation Antipsychotic medication

24
Q

Blocks 5HT2A and D2
receptors CNS

  • Olanzapine: most cardiometabolic side effects, causing weight gain, hyperlipidemia,
    hyperglycemia
  • Ziprasidone: low cardiometabolic side effects, prolonged QT risk
  • Risperidone: high EPS potential and moderate cardiometabolic side effects
  • Paliperidone is the metabolite of risperidone
  • Quetiapine: more sedation, low EPS potential, moderate cardiometabolic side effects
  • Airpiprazole: low EPS potential and low cardiometabolic side effects
  • Lurasidone: must be taken with food, metabolized by CYP3A4, preferred for
  • Cariprazine: D2 and D3 agonist, more EPS than other second generation
A

Second generation

antipsychotic medication

25
Q

D1 and 5HT2A receptors

  • Treatment for resistant schizophrenia, should only
    be considered after failure of 2 other drugs
  • Lowest affinity for D2 receptors in the class, and has antagonism for D1 receptors and serotonin instead
  • Patients, prescribers, pharmacy must be enrolled in Risk evaluation and Mitigation Strategy (REMS)
  • Absolute neutrophil count needs to be monitored
    regularly
A

Clozapine (2nd gen

antipsychotic)

26
Q

NE and dopamine receptors in presynaptic

  • Structurally related to amphetamine
  • Blocks reuptake of NE and dopamine into
    presynaptic neurons
  • Metabolized by liver via carboxylesterase
  • 1st line of treatment for ADHD
A

Methylphenidate

27
Q

Selective NE reuptake
inhibitor

  • May be preferred if patient has active substance
    abuse problem, comorbid anxiety, tics or has
    intolerable effects to stimulants
  • Used as a non-stimulant to treat ADHD
A

Atomoxetineq

28
Q

Postsynaptic α2 adrenergic
agonist

  • Same as clonidine but longer acting
  • More sedation than stimulants and atomoxetine
A

Guanfacine

PHARMA I (138 decks)

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