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Pharmacology COPY > EXAM #3: ANTIDEPRESSANTS > Flashcards

EXAM #3: ANTIDEPRESSANTS Flashcards

1
Q

What is the “delay of therapeutic response” in antidepressant therapy?

A

Weeks to months are required for therapeutic benefit

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2
Q

What generally limits the use of antidepressants?

A

Side effects

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3
Q

What is the monoamine/ biogenic amine hypothesis?

A

Depression is caused by a lack of:

  • 5-HT
  • NE
  • DA
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4
Q

What is the neurotrophic hypothesis of depression?

A

Changes in nerve growth factors play a role in depression

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5
Q

What is the mechanism of action of currently available antidepressants?

A

Increase in 5-HT and/or NE in the synapse

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6
Q

What is the general function of neurotrophic factors e.g. BDNF?

A

“Brain fertilizer” for neuronal growth and survival

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7
Q

How do antidepressants alter BDNF?

A

Increase

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8
Q

What is the general mechanism of MAOIs?

A

Monoamine oxidase inhibitors block the degradation of monoamines (5-HT and NE)

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9
Q

What classes of drugs block reuptake of monoamines?

A

SSRIs
TCAs
SNRIs

SNRI= 5-HT and NE reuptake inhibitors*

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10
Q

What is the function of autoreceptors on the pre-synaptic terminal?

A

Agonism of autoreceptors decreases NT release

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11
Q

What class of antidepressant is commonly used to treat PTSD?

A

SSRI

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12
Q

What is the role of antidepressants as anxiolytics?

A

Long-term anti-anxiety effects at LOW doses

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13
Q

What class of antidepressants is used commonly to treat chronic pain?

A

TCAs

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14
Q

What is the mechanism of action of the MAOIs?

A

Antagonism of MAO to increase availability of 5-HT and NE in the synaptic cleft

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15
Q

What is the difference between MAO-A and MAO-B inhibitors?

A

A= Tyramine, NE, 5-HT, and DA

B= DA

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16
Q

What is the clinical use of MAOIs?

A

1) Treatment of resistant depression
2) Atypical depression
3) Anxiety states i.e. social anxiety and panic disorder

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17
Q

What are the most common side effects associated with MAOIs?

A

1) Orthostatic hypotension
2) Weight gain
3) Sexual dysfunction

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18
Q

What causes orthostatic hypotension with MAOI use?

A

Inhibition of alpha-1 receptors in the CNS

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19
Q

What is the important food interaction associated with MAOIs?

A

Tyramine ingestion with MAOIs can cause a hypertensive crisis

(wine and cheese phenomenon)

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20
Q

What is the mechanism of action of the tricyclic antidepressants?

A

Block reuptake of 5-HT and NE by inhibition of SERT and NET

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21
Q

How are TCAs used clinically?

A

1) 2nd line for major depression

2) CHRONIC PAIN (first line)

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22
Q

What TCA is used to treat bedwetting? Why?

A

Imparamine b/c of anticholinergic effects

23
Q

What TCA is used to treat neuropathic pain?

A

Desipramine

24
Q

What TCA has the most sedative effects?

A

Amitriptyline

25
Q

What are the side effects of the TCAs?

A

1) Orthostatic hypotension (elderly = “hip breakers”)
2) Delerium in elderly
3) Sexual dysfunction
4) Cardiac toxicity–> LETHAL CARDIAC ARRHYTHMIA

26
Q

What are the 3 Cs of TCA overdose?

A
  • Convulsions
  • Coma
  • Cardiac arrhythmia
27
Q

What is the mechanism of action of the SSRIs?

A

Selective inhibition of SERT; block 5-HT reuptake into the pre-synaptic terminal

28
Q

What is the clinical use of SSRIs?

A

First line for depression

29
Q

What is important to remember clinically about SSRIs?

A

Much safer than MAOIs or TCAs

30
Q

What are the short term side effects of SSRIs?

A

Nausea
Dyspepsia
Diarrhea

31
Q

What are the long-term side effects of SSRIs?

A

Sexual Dysfunction*

Number 1 reason to switch SSRIs

32
Q

What precipitates Serotonin Syndrome with SSRIs?

A

1) Combination use with other antidepressants

2) Switching SSRIs (allow time for previous drug to clear)

33
Q

What is Serotonin Syndrome?

A

Classically, a triad of:

1) mental status changes
2) autonomic hyperactivity
3) neuromuscular abnormalities

34
Q

What is SSRI Discontinuation Syndrome?

A

Sudden d/c of short half-life SSRIs can can cause adverse effects in some patients in 1-7 days of cessation

35
Q

How do SNRIs differ from TCAs?

A

SNRIs and TCAs both inhibit SERT and NET, but SNRIs have much LESS AFFINITY for other receptors i.e. have less side effects

36
Q

What is the mechanism of Venlafaxine?

A

1) Major: SERT inhibitor

2) Minor: NET inhibitor

37
Q

What is the clinical indication for Venlafaxine?

A

Severe depression

38
Q

What is the mechanism of action of Duloxetine?

A

Balanced 5-HT and NE reuptake blockade

39
Q

What is Duloxetine inidicated for?

A

Increasingly prescribed for chronic pain over TCAs

40
Q

What is the mechanism of action of Trazadone?

A

H1 receptor antagonist

41
Q

What is Trazadone indicated for?

A

Unlabeled hypnotic i.e. treatment for insomnia

42
Q

What is the major side effect associated with Trazodone?

A

Priapism

43
Q

What is the mechanism of action of Buproprion?

A

1) Blocks NE and DA reuptake

2) Increases presynaptic release of catecholamines

44
Q

What is Bupropion indicated for?

A

1) Major depression

2) Smoking cessation

45
Q

What is the mechanism of action of Mirtazapine?

A

1) Alpha-2 blocker
2) Increases release of 5-HT and NE
3) H1 blocker
4) 5-HT2 and 3 blocker

46
Q

What do you need to remember about prescribing MAOIs, TCAs, and SSRIs?

A

DO NOT COMBINE–can be FATAL

47
Q

What antidepressants are potent CYP2D6 inhibitors?

A
  • Paroxetine
  • Fluoxetine
  • Fluvoxamine
48
Q

What is the drug of choice for Bipolar Disorder?

A

Lithium

49
Q

What anticonvulsants are used to treat Bipolar Disorder?

A

Valproic acid

Carbamazepine

50
Q

What is the clinical utility of Lithium?

A

Maintenance treatment

51
Q

What is the clinical utility of Valproic acid and Carbamazepine?

A

Treatment of acute mania

52
Q

What is the mechanism of action of Lithium?

A

Stabilization of the postsynaptic membrane

53
Q

What are the side effects of Lithium?

A

1) Tremor
2) Hypothyroidism
3) Nephrogenic Diabetes Insipidus
4) Skin reactions

54
Q

What is the important drug interaction to remember with Lithium?

A

Thiazide and loop diuretics diminish Li+ clearance; thus, combination therapy can cause Lithium toxicity

Pharmacology COPY (64 decks)

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