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Neuro B5 - WLB > Antidepressants/Drugs for Manic Disorders - Slattery > Flashcards

Antidepressants/Drugs for Manic Disorders - Slattery Flashcards

(40 cards)

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1
Q

What is the MOA of Tricyclic Antidepressants?

A
  • Block the reuptake of NE and/or 5-HT by pre-synaptic nerve terminals
    • blocked reuptake increases amount of NT in synaptic space –> downstream effects
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2
Q

What drug class does Desipramine (Norpramin) belong in?

A

NE-selective TCA

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3
Q

What drug class does Imipramine (Tofranil) belong in?

A

NE/5HT mixed action TCA

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4
Q

What are adverse symptoms of TCAs?

A
  • Orthostatic hypotension
  • Weight gain
  • Tachycardia and increased tendency for arrhythmias with high doses
  • Drowsiness
  • Dry mouth
  • Blurred vision
  • Constipation
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5
Q

Why do TCAs cause drowsiness?

A
  • Block histamine receptor
  • Block muscarinic receptor
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6
Q

Why to TCAs cause weight gain?

A

Block histamine receptor (H1)

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7
Q

Why do TCAs cause orthostatic hypotension, light-headedness, and decreased blood pressure?

A

Block alpha-1 receptors

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8
Q

Why do TCAs cause dry mouth, blurred vision, and constipation?

A

block muscarinic receptors

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9
Q

Why do TCAs cause arrhythmias, cardiac arrest, and seizures?

A

Block Na+channels

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10
Q

What is the MOA of Monoamine Oxidase Inhibitors (MAOIs)?

A
  • Irreversibly blocks the oxidative deamination of monoamines
    • Nonselectively inhibit both MAO-A and MAO-B
      • MAO-A = metabolizes NE & 5HT
      • MAO-B = metabolizes DA
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11
Q

What drug class does Phenelzine (Nardil) belong in?

A

MAOIs

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12
Q

Why do you have to wait 14 days to start an SSRI after stopping use of MAOI, and 14 days to start an MAOI after stopping use of an SSRI?

A
  • allow for new synthesis of MAO
  • allow excretion of SSRI’s
  • avoid Serotonin Syndrome
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13
Q

What is Serotonin Syndrome?

A
  • Overactivation of 5HT-2A (also 5HT-1A)
  • Causes:
    • hyperthermia,
    • muscle rigidity,
    • tremors,
    • autonomic instability,
    • confusion,
    • irritability,
    • agitation
    • can progress toward coma & death
  • Also caused by MDMA (Ecstacy)
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14
Q

How do you treat Serotonin Syndrome?

A

Administer nonselective serotonin antagonists (Cyproheptadine, etc.)

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15
Q

What drug interaction is most worriesome when treating with MAOIs?

A

Tyramine

  • Sympathomimetic amine potentiated by MAOIs
  • Metabolized by hepatic MAO
  • If patient has taken MAO inhibitor, tyramine enters systemic circulation
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16
Q

What happens when Tyramine enters systemic circulation?

A
  • Combined effect of tyramine and MAO inhibitor
    • Massive adrenergic stimulation (Epi/NE release)
    • Released catecholamines stimulate postsynaptic receptors in the periphery, increasing blood pressure to dangerous levels
    • May result in a hypertensive crisis
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17
Q

What three foods must people on MOAIs avoid? Why?

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A
  • Foods rich in Tyramine
    • Aged cheese
    • Red wine
    • Beer
18
Q

What is the MOA of Selective Serotonin Reuptake Inhibitors (SSRIs)?

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A

Inhibits pre-synaptic serotonin reuptake pumps

  • inhibits feedback loop, so release continues
  • allows additional release of 5HT
19
Q

What drug class does Fluoxetine (Prozac) belong in?

20
Q

What drug class does Sertraline (Zoloft) belong in?

21
Q

What drug class does Escitalopram (Lexapro) belong in?

22
Q

What are adverse effects of SSRIs?

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A
  • Nausea
  • Diarrhea
  • Weight loss
  • Stimulation:
    • Anxiety
    • Nervousness
    • Insomnia
  • Sexual dysfunction
  • Increased risk for suicidal thoughts & behavior
23
Q

What disorder should SSRIs not be the sole treatment of?

Study These Flashcards
A

Bipolar disorder!

(can switch from depressed right into manic phase)

24
Q

What specific serotonin receptor contributes to the clinical improvement seen in SSRI treatments?

25
What is the MOA of Venlafaxine (Effexor, Effexor XR)?
* Serotonin-Norepinephrine reuptake inhibitor (SNRI) * Blocks 5-HT reuptake like SSRIs * Also blocks NE reuptake
26
What does Venlafaxine (Effexor, Effexor XR) NOT effect?
* Adrenergic receptors * Histaminergic receptors * Cholinergic receptors (TCA effect on these receptors causes its adverse side effects)
27
Why does raising the dose of Venlafaxine improve efficacy?
Secondary mechanisms of action: - low dose only affects 5HT - medium dose affects 5HT/NE - high dose affects DA
28
What is the MOA of Mirtazapine (Remeron)?
* Blocks pre-synaptic alpha-2 receptors on: * adrenergic neurons (autoreceptors) * serotonergic neurons (heteroceptors) * causes increased NE & 5HT levels * (blocks negative feedback loop)
29
What is MOA of Lithium carbonate (Lithobid, Eskalith)?
* Mechanism of action is **unknown** * Most likely involves effect on postsynaptic rather than presynaptic neuron * Interferes with the production and release of IP3 (phosphatdylinositol-4,5-bisphosphate) and DAG (diacyl glycerol) * Can inhibit norepinephrine-sensitive adenylyl cyclase * May uncouple receptor recognition site from GTP-binding protein (G-protein) by competing with Mg2+ * May affect several cell or nuclear regulatory factors * **Working hypothesis**: alters gene expression implicated in long-term neuroplastic events that could underlie long-term mood stabilization
30
What are adverse effects of Lithium carbonate?
* Fatigue * muscular weakness * slurred speech * ataxia * fine tremor of the hands * excessive thirst and urination
31
What are the clinical/therapeutic uses of Lithium carbonate?
* Manic phases of bipolar disorder * Prevention of mood swings in patients prone to bipolar disorder * Antidepressant effect in some patients
32
What happens in Lithium toxicity?
* CNS primarily affected * consciousness is impaired * coma may result * Muscular rigidity * hyperactive deep reflexes * marked tremor and muscle fasciculations
33
Whys is Lithium toxicity easy to acheive?
Therapeutic dose (0.8 - 1.4 mEq/l) is very close to toxic range (\>2 mEq/l).
34
How do you treat Lithium toxicity?
Symptomatic
35
What is Valproic acid (Depakene) used to treat?
Rapid-cycling bipolar disorder (appropriate first-line treatment for some)
36
What drug class does Valproic acid (Depakene) belong in?
Anticonvulsant
37
What is Carbamazepine (Tegretol) used for?
Prophylaxis of bipolar disorder
38
What drug class does Carbamazepine (Tegretol) belong in?
Anticonvulsants
39
Why should SSRIs/SNRIs never be used as monotherapy in patients with bipolar disorder?
* May cause rapid onset of mania * Patients should be receiving prophylactic mood stabilizer therapy to prevent this from occurring
40
What new drug was just approved in 2013 to treat bipolar disorder and presumably works through central dopamine (D2) and serotonin (5-HT2A) receptor antagonism, but the precise mechanism is unknown?
Lurasidone (Latuda) Atypical Antipsychotic

Neuro B5 - WLB (19 decks)

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