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BB Test 3 > Antidepressants > Flashcards

Antidepressants Flashcards

1
Q

__-__% of depression patients will improve with placebo treatment.

A

30-40%

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2
Q

Antidepressants of all classes may increase the risk of _____________________ in children.

A

Suicidal thinking and behavior

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3
Q

_________________ are the standard for antidepressant efficacy.

A

Tricyclic antidepressants

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4
Q

What are some common examples of tricyclic antidepressants?

A
  • Tertiary amines
    • Imipramine
    • Amitryptyline
  • Secondary amines
    • Desipramine
    • Nortriptyline
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5
Q

Pharmacological activity of tricyclic antidepressants:

A
  • All are about equally efficacious
  • All have 2-3 week latency
  • Don’t elevate mood in non-depressed patient
  • May be combined with lithium when treating bipolar disorder
  • Used for treatment of chronic neuropathic pain (greatest use today)
  • May cause insomnia
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6
Q

Imipramine and Amitryptyline, tertiary amine tricyclic antidepressants, more effectively inhibit the reuptake of (serotonin/norepinephrine).

A

Serotonin

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7
Q

Desipramine and Nortriptyline, secondary amine tricyclic antidepressants, more effectively inhibit the reuptake of (serotonin/norepinephrine).

A

Norepinephrine

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8
Q

PCKN of tricyclic antidepressants:

A
  • Slowly absorbed
    • Peak plasma levels in 2-8 hours
    • Delay in gastric emptying time
  • Significant “first pass” effect
    • Enterohepatic circulation
  • Significant protein binding
  • Large volume of distribution
  • T1/2 ranges from 12-72 hours
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9
Q

What are the CNS adverse effects of tricyclic antidepressants?

A
  • Delirium, confusion, and manic reactions
  • Sedation and/or weight gain
  • Tremors
  • Reduced seizure threshold
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10
Q

What are the autonomic adverse effects of tricyclic antidepressants?

A
  • Significant antimuscarinic activity
    • Tertiary amines > secondary amines
    • Dry mouth (teeth loss), blurred vision, constipation, urinary retention
  • α-adrenergic antagonist activity
    • secondary amines > tertiary amines
    • Orthostatic hypotension, reflex tachycardia, and arrhythmias
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11
Q

What are the drug interactions of tricyclics?

A

Causes hypertensive crisis when combined with MAO inhibitors

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12
Q

What is the contraindication of tricyclic antidepressants?

A

Do not use in patients with narrow angle glaucoma.

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13
Q

Why should tricyclics only be prescribed in 1 week supplies?

A

Acute overdoses of lethal levels can be achieved with amounts that are readily available to the patient.

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14
Q

What is the treatment course for an acute overdose of tricyclics?

A
  • Maintain respiration
  • Gastric lavage (stomach pump) with activated charcoal
  • Supportive care
  • Antiarrhythmic agents for arrhythmias
  • Benzodiazepines for seizures
  • Bicarbonate to correct acidosis and to increase plasma protein binding
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15
Q

When tricyclics are combined with MAO inhibitors, what crisis results?

A

Hypertensive crisis

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16
Q

When switching to a MAO inhibitor from a tricyclic, allow a __ week washout period.

A

1 week

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17
Q

When switching to a tricyclic from a MAO inhibitor, allow a __ week washout period.

A

2 week

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18
Q

What are the withdrawal signs of tricyclics?

A
  • Sleep disturbances and nightmares
  • GI upset
  • Irritability
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19
Q

What are some common examples of selective serotonin reuptake inhibitors (SSRIs)?

A
  • Fluoxetine
  • Paroxetine
  • Sertraline
  • Citalopram

“Flashbacks Paralyze Senior Citizens”

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20
Q

What is the pharmacological activity of SSRIs?

A
  • Can be combined with lithium in bipolar disorder
  • Do not elevate mood in normal patients
  • Main advantage over tricyclics is safety
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21
Q

What are SSRIs used to treat?

A
  • Bipolar disorders (with lithium)
  • Panic disorders
  • Generalized anxiety disorder
  • Obsessive compulsive disorder
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22
Q

(T/F) Fluoxetine is 10x more potent than sertraline.

A

False. Sertraline is 10x more potent than fluoxetine.

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23
Q

PCKN of SSRIs:

A
  • Well absorbed orally
  • Rate of metabolism is age dependent
    • Children > young adults > over 60
  • Exception: Fluoxetine and sertraline are metabolized to active metabolites by the liver
  • Fluoxetine T1/2: 2-3 days
  • Paroxetine T1/2: 22 hrs
  • Sertraline T1/2: 25 hrs
  • Citalopram T1/2: 33-38 hrs
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24
Q

The active metabolite of fluoxetine is _____________.

A

Norfluoxetine (7-15 day half-life)

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25
Acute overdose is more serious in (tricyclics/SSRIs).
Tricyclics
26
What are some adverse effects of SSRIs?
* CNS stimulation * Nausea and vomiting * Headache * Sexual dysfunction * Black Box warning for cardiac birth defects
27
Sexual dysfunction is more common in (tricyclics/SSRIs).
SSRIs
28
What are the contraindication of citalopram?
* **Citalopram** may cause **QT prolongation** * Not to be prescribed to patients with history of congenital long QT syndrome * If QT is \>500msec, citalopram should be discontinued
29
When SSRIs are combined with MAO inhibitors, what condition may result?
Serotonin syndrome
30
What are the drug interactions of SSRIs?
* Causes **serotonin syndrome** when combined with **MAO inhibitors** * SSRIs inhibit mixed function oxidases (CYP2D6) * Reduces metabolism of other drugs * Sertraline and citalopram do not inhibit P450 system * Fluoxetine binds to plasma proteins * Displaces warfarin and digoxin
31
What are the symptoms of serotonin syndrome?
* **SMARTS** * **S**weating * **M**yoclonus * **A**NS instability * **R**igidity * **T**emperature increase (hyperthermia) * **S**eizures
32
What are the symptoms associated with withdrawal from SSRIs?
* Less symptoms with longer T1/2 compounds * Dizziness * Nausea * Paresthesias * Tremors * Anxiety * Palpitations
33
What are some common examples of selective serotonin and norepinephrine reuptake inhibitors (SSNRIs)?
* Venlafaxine * Duloxetine
34
What is the pharmacological activity of SSNRIs?
Block reuptake of both serotonin and norepinephrine (equally) with **minimal antimuscarinic** and **α-adrenergic antagonist effects**
35
Venlafaxine has a 10x (higher/lower) affinity for 5-HT than sertraline, an SSRI.
Lower
36
Venlafaxine has a 11x (higher/lower) affinity for 5-HT than amitriptyline, a tricyclic.
Higher
37
Venlafaxine, an SSNRI, is more selective for (5-HT/NE) transporters.
5-HT
38
What are some common examples of miscellaneous antidepressants?
* Bupropion * Trazodone * Nefazodone * Mirtazapine
39
What is the pharmacological activity of miscellaneous antidepressants?
* Effective in treating **bipolar disorder** in combination **with lithium** * Does not elevate mood in normal patients
40
(T/F) The mechanism of action for bupropion might involve dopamine and norepinephrine transporters, but has little to no effect on 5-HT and MAO.
True.
41
The active metabolite of bupropion is \_\_\_\_\_\_\_\_\_\_\_\_\_\_\_.
Hydroxybupropion
42
What is the mechanism of action for Trazodone?
* Blocks 5-HT 2a receptor * Modest antagonist at H1 receptor (histamine receptor) * Weak but selective inhibitor of SERT with little effect on NET * Weak to moderate antagonism of α-2 adrenergic receptors
43
What is the mechanism of action for Nefazodone?
* Blocks 5-HT 2a receptor * Inhibits SERT and NET
44
What are the adverse effects of Mirtazepine?
* **Sedation** (opposite of Bupropion) * **Increased appetite** and weight gain (opposite of Bupropion) * Can be used to an advantage, such as in anorexic patients * Dry mouth and constipation * **No sexual side effects**
45
What are the drug interactions associated with miscellaneous antidepressants?
**Do not combine any with MAO inhibitors** * Bupropion * Trazodone * Nefazodone * Mirtazapine
46
What are some common examples of monoamine oxidase inhibitors (MAO inhibitors)?
* Phenelzine * Tranylcypromine * Selegiline
47
What is the pharmacological activity of MAO inhibitors?
* Used in depression only when refractory to other drugs * Narcolepsy
48
What is the mechanism of action for MAO inhibitors?
* Inhibition of both MAO-A and MAO-B * Selegiline is specific for MAO-B * Increase norepinephrine, dopamine, and serotonin levels * Takes 2-3 days for optimum inhibition of 70% to be reached
49
What is the pharmacokinets of MAO inhibitors?
* Good oral absorption * Slow elimination * Termination of activity is dependent upon the synthesis of new enzyme
50
What are some adverse effects of MAO inhibitors?
* Insomnia * Agitation * Hyperthermia * Convulsions * Hypo or hypertension * Rare hepatotoxicity
51
What are the drug and food interactions of MAO inhibitors?
* Interacts with: * Sympathomimetics * Tricyclics * SSRIs * Foods (such as wine and cheese - **tyramine**)
52
What are some common examples of atypical antipsychotics?
* Aripiprazole * Quetiapine * Olanzapine * Risperidone
53
\_\_\_\_\_\_\_\_\_\_\_\_\_, taken from the Hypericum perforatum plant, is commonly prescribed for mild to moderate depression in Europe.
St. John's wort
54
(T/F) St. John's wort activates CYP3A4 and CYP2C9. It also activates CYP1A2 only in females.
True.
55
What are the adverse effects of St. John's wort?
* GI symptoms * Dizziness * Confusion * Sedation * Photosensitivity * May aggravate mania in bipolar patients and psychosis in schizophrenics
56
(T/F) Ketamine has a rather slow onset and short-lasting antidepressant effects in otherwise treatment-resistant patients.
False. Ketamine has a **fast onset** and a **sustained** antidepressant effect in otherwise treatment-resistant patients.
57
What are the two first line treatments of major depression?
* SSRIs * SSNRIs
58
\_\_\_\_\_\_\_\_\_\_ is the only SSRI approved for depression in children and adolescents.
Fluoxetine
59
(T/F) 2nd generation antidepressants (the miscellaneous antidepressants) are not effective in the severely depressed. Bupropion is the exception to this rule.
True.
60
\_\_\_\_\_\_\_\_\_\_\_\_\_, a tricyclic, has the cheapest generic form of medication.
Imipramine
61
Which two antidepressants have lowest incidence of sexual side effects?
* Bupropion (decreased appetite and awake) * Mirtazepine (increased appetite and sedation)
62
What are some adverse side effects seen with Trazodone (2nd generation antidepressent)?
* Drowsiness * **Priapism (permanent impotence)**
63
What are some adverse side effects seen with Nefazodone (2nd generation antidepressent)?
* **Hepatotoxicity** * Dry mouth
64
What are some adverse side effects seen with Bupropion (2nd generation antidepressant)?
* **Agitation** (most frequent reson for discontinuation) * **Decreased appetite** (opposite of Mirtazepine) * **Sedation** (opposite of Mirtazepine) * **No sexual side effects**

BB Test 3 (26 decks)

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