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Pharmacology- Test 2 Material > 13- Antidepressants/Stimulants > Flashcards

13- Antidepressants/Stimulants Flashcards

1
Q

duloxetine (Cymbalta)

A

SNRI

  • inhibit NET and SERT but structurally diff. from TCAs
  • fewer off target s/fx (nausea, anxiety, insomnia; inc. BP, HR)
  • may be used to treat patients refractory to SSRIs
  • orally active but therapeutic effect required >2 weeks
  • readily penetrate CNS (half-life 11-12 hrs)
  • HIGH binding to plasma proteins (90-95%)
  • metabolized by CYPs and eliminated in kidneys
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2
Q

venlafaxine (Effexor)

A

SNRI

  • inhibit NET and SERT but structurally diff. from TCAs
  • fewer off target s/fx (nausea, anxiety, insomnia; inc. BP, HR)
  • may be used to treat patients refractory to SSRIs
  • orally active but therapeutic effect required >2 weeks
  • readily penetrate CNS (half-life 11-12 hrs)
  • LOW binding to plasma proteins (27%)
  • metabolized by CYPs and eliminated in kidneys
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3
Q

bupropion (Wellbutrin)

A

atypical antidepressant

  • inhibits DAT thus preventing dopamine reuptake and inc. its levels in synapse
  • efficacy similar to TCAs and SSRIs
  • often used in combo with TCAs for ppl that don’t respond to single agent
  • s/fx: headache, nausea, tinnitus, insomnia (safer then TCAs)
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4
Q

mirtazapine (Remeron)

A

atypical antidepressant

  • inhibits a2 receptors thus inc. the release of serotonin and NE (eliminates feedback inhibition)
  • efficacy similar to TCAs and SSRIs
  • often used in combo with TCAs for ppl that don’t respond to single agent
  • s/fx: headache, nausea, tinnitus, insomnia (safer then TCAs)
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5
Q

nefazodone (Serzone)

A

atypical antidepressant

  • inhibits SERT thus preventing serotonin reuptake and blocks post-synaptic serotonin receptor sites
  • efficacy similar to TCAs and SSRIs
  • often used in combo with TCAs for ppl that don’t respond to single agent
  • s/fx: headache, nausea, tinnitus, insomnia (safer then TCAs)
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6
Q

phenelzine (Nardil)

A

MAOI
-blocks MAOa on noradrenergic neurons, MAOa/b on dopaminergic neurons, and MAOa on serotonergic neurons
-orally active but therapeutic effect requires >2 weeks
-block MAO irreversibly (takes weeks to replace)
-most dangerous catagory of antidepressants d/t broad effects and severe/unpredictable s/fx
S/Fx: restless, agitation, psychosis, ortho, hypotension, tachycardia, serotonin syndrome, cheese effect (tyramine)

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7
Q

selegiline (Emsam)

A

MAOI
-blocks MAOa/b on dopaminergic neurons, and MAOa on serotonergic neurons
-orally active but therapeutic effect requires >2 weeks
-block MAO irreversibly (takes weeks to replace)
-most dangerous catagory of antidepressants d/t broad effects and severe/unpredictable s/fx
S/Fx: restless, agitation, psychosis, ortho, hypotension, tachycardia, serotonin syndrome, cheese effect (tyramine)

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8
Q

tranylcypromine (Parnate)

A

MAOI
-blocks MAOa on noradrenergic neurons, MAOa/b on dopaminergic neurons, and MAOa on serotonergic neurons
-orally active but therapeutic effect requires >2 weeks
-block MAO irreversibly (takes weeks to replace)
-most dangerous catagory of antidepressants d/t broad effects and severe/unpredictable s/fx
S/Fx: restless, agitation, psychosis, ortho, hypotension, tachycardia, serotonin syndrome, cheese effect (tyramine)

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9
Q

Monoamine Hypothesis

A

Depression caused by a deficiency in monamines, particularly serotonin and norepinephrine

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10
Q

Cheese Effect

A

In the presence of MAOIs elevated tyramine causes release of large amounts of catecholamines
- Patients taking MAOIs have a restricted diet

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11
Q

Brain Derived Neurotrophic Factor (BDNF)

A

-signaling factor that promotes formation of new neurons in the hippocampus

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12
Q

Psychomotor Stimulants

A
  • drugs that increase vesicular and non-vesicular release of NE and DA
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13
Q

amitriptyline

A

TCA: NON-specific blockers of monoamine uptake
-therapeutic effect requires >2 weeks
-highly lipid soluble
-long 1/2 life
-high plasma protein binding
-metabolized by CYPs
side effects: Anti-muscarinic, othrostatic hypotension, SEDATION, weight gain, sexual dysfunction, seizures, and psychiatric

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14
Q

amoxapine

A

TCA: NON-specific blockers of monoamine uptake
-therapeutic effect requires >2 weeks
-highly lipid soluble
-long 1/2 life
-high plasma protein binding
-metabolized by CYPs
side effects: Anti-muscarinic, othrostatic hypotension, SEDATION, weight gain, sexual dysfunction, seizures, and psychiatric

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15
Q

imipramine

A

TCA: NON-specific blockers of monoamine uptake
-therapeutic effect requires >2 weeks
-highly lipid soluble
-long 1/2 life
-high plasma protein binding
-metabolized by CYPs
side effects: Anti-muscarinic, othrostatic hypotension, SEDATION, weight gain, sexual dysfunction, seizures, and psychiatric

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16
Q

nortriptyline

A

TCA: NON-specific blockers of monoamine uptake
-therapeutic effect requires >2 weeks
-highly lipid soluble
-long 1/2 life
-high plasma protein binding
-metabolized by CYPs
side effects: Anti-muscarinic, othrostatic hypotension, SEDATION, weight gain, sexual dysfunction, seizures, and psychiatric

17
Q

citalopram

A

SSRI- Selective Serotonin Reuptake Inhibitor
-therapeutic effect requires > 2 weeks
-highly lipid soluble and plasma protein binding
- long 1/2 life
-high 1st pass metabolism (CYP)
-BLOCK several CYPs (drug interactions)
side effects: INSOMNIA, nausea, anxiety
late onset side effects- anorexia, sexual dysfunction, mania-bipolar

18
Q

escitalopram

A

SSRI- Selective Serotonin Reuptake Inhibitor
-therapeutic effect requires > 2 weeks
-highly lipid soluble and plasma protein binding
- long 1/2 life
-high 1st pass metabolism (CYP)
-BLOCK several CYPs (drug interactions)
side effects: INSOMNIA, nausea, anxiety
late onset side effects- anorexia, sexual dysfunction, mania-bipolar

19
Q

fluoxetine

A

SSRI-Selective Serotonin Reuptake Inhibitor
-therapeutic effect requires >2 weeks
-highly lipid soluble and plasma protein binding
-demethylated to active metabolite norfluxetine (1/2 life up to 30 days)
-block several CYPs (drug interactions)
early onset side effects- INSOMNIA, nausea, anxiety
late onset- anorexia, sexual dysfunction, mania-bipolar

20
Q

sertraline

A

SSRI- Selective Serotonin Reuptake Inhibitor
-therapeutic effect requires > 2 weeks
-highly lipid soluble and plasma protein binding
- long 1/2 life
-high 1st pass metabolism (CYP)
-BLOCK several CYPs (drug interactions)
side effects: INSOMNIA, nausea, anxiety
late onset side effects- anorexia, sexual dysfunction, mania-bipolar

21
Q

Lithium

A

Lithium Salt
-Tx ofBP D/O
-MOA unclear
-therapeutic effects take 3-4wks
-soluble ion; does not bind to Plasma proteins
-Ther level 0.6-1.4 mEq/L; toxic= 1.6-2 mEq/L
-S/E:
+CNS: tremors, confusion, convulsion, coma
+CV: arrhythmias; Thyroid: decrease function
+Renal: polydipsia, polyphagia, induced DI
+Drug interactions: NSAID and thiazides

22
Q

amphetamine (Adderall)

A

Amphetamine, Psychostimulant

  • Tx of ADHD and narcolepsy
  • increased vesicular and non-vesicular monoamine release (NE and DA).
  • inhibit NE and DA reuptake and reverse transports them back into synapse.
  • metabolized in liver via de-esterification.
  • S/E: euphoria, insomnia, vertigo, arrhythmias, HTN, NV, habit forming.
23
Q

atomoxetine (Strattera)

A

Non-psychostimulant

  • NE re-uptake inhibitor
  • Tx of ADHD
  • not habit forming
24
Q

dextro-amphetamine (Dexedrine)

A

Amphetamine, Psychostimulant

  • Tx of ADHD and narcolepsy
  • increased vesicular and non-vesicular monoamine release (NE and DA).
  • inhibit NE and DA reuptake and reverse transports them back into synapse.
  • metabolized in liver via de-esterification.
  • S/E: euphoria, insomnia, vertigo, arrhythmias, HTN, NV, habit forming.
25
Q

methylphenidate (Ritalin)

A

Amphetamine, Psychostimulant

  • Tx of ADHD and narcolepsy
  • increased vesicular and non-vesicular monoamine release (NE and DA).
  • inhibit NE and DA reuptake and reverse transports them back into synapse.
  • metabolized in liver via de-esterification.
  • S/E: euphoria, insomnia, vertigo, arrhythmias, HTN, NV, habit forming.
26
Q

modafinil (Provigil)

A
  • used to treat narcolepsy
  • MOA not completely understood (likely involves NE and DA).
  • fewer psychoactive and euphoric effects.
  • fewer effects on mood and thinking.

Pharmacology- Test 2 Material (10 decks)

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