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Pharmacology > Lec. 5: Antidepressants > Flashcards

Lec. 5: Antidepressants Flashcards

1
Q

What are the two main categories of 1st generation drugs for depression?

A
  1. Tricyclic

2. MAO Inhibitors

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2
Q

What are the four main categories for the 2nd and 3rd generation drugs used to treat depression?

A
  1. Tetracyclics and Unicyclics
  2. 5-HT(2) antagonists
  3. SSRI
  4. SNRI
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3
Q

What is the hypothesis of the pathophysiology of depression?

A

The monoamine hypothesis

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4
Q

What is the monoamine hypothesis?

A

Depletion of monoamines in CNS causes symptoms of depression.

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5
Q

What are the main monoamines in the monamine hypothesis?

A

NE and serotonin

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6
Q

What is the main action of most antidepressant drugs?

A

Increase neurotransmission of amines (5-HT and NE)

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7
Q

Antidepressant drugs are categorized based on their effect on the re-uptake of ? or ?.

A
  1. Ne

2. 5-HT

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8
Q

Name two antidepressants that have little effect on re-uptake of either 5-HT or NE.

A
  1. Bupropion

2. Mirtazapine

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9
Q

Name the drug that inhibits NE re-uptake with great potency (about 500-fold more than 5-HT reuptake).

A

Maprotiline

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10
Q

T or F. Drugs that inhibit 5-HT reuptake with greater potency will have greater than 100-fold more than the inhibition on NE reuptake.

A

False. 50-fold

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11
Q

T or F. There are also drugs that inhibit reuptake of NE and 5-HT with similar potencies.

A

True

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12
Q

Tricyclic antidepressants are ? generation antidepressants. List five examples.

A

1st generation

  1. Imipramine
  2. Desipramine
  3. Amitriptyline
  4. Protriptyline
  5. Doxepine
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13
Q

List seven mechanisms of action of tricyclic antidepressants.

A
  1. Blockade of NE uptake
  2. Blockade of serotonin reuptake
  3. Blockade of muscarinic/cholinergic receptors
  4. Blockade of alpha-1 NE receptors
  5. Blockade of alpha-2 NE receptors
  6. Blockade of histamine H1 receptors
  7. Blockade of cardiac Na channels and Na pump
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14
Q

List the five most common areas effected by TCAs.

A
  1. Sympathomimetic
  2. Cardiovascular
  3. Endocrine/metabolic
  4. Anticholinergic
  5. Neurological
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15
Q

What are three sympathomimetic side effects of TCAs?

A
  1. Hypotension
  2. Compensatory tachycardia
  3. Tremors
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16
Q

What are three cardiovascular side effects of TCAs?

A
  1. Orthostatic hypotension
  2. ECG abnormalities
  3. Arrhythmias
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17
Q

What is a endocrine side effect of TCAs?

A

Weight gain

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18
Q

What are five anticholinergic side effects of TCAs?

A
  1. Dry mouth
  2. Blurred vision
  3. Constipation
  4. Urinary hesitancy
  5. Loss of libido and ED
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19
Q

What are three neurological side effects of TCAs?

A
  1. Paresthesias
  2. Seizures
  3. Hallucinations
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20
Q

Sedative effects of TCAs are enhanced by ?. Some examples include (name three).

A

CNS depressants

  1. BZDs
  2. Barbiturates
  3. Alcohol
21
Q

Inhibitors of ? enzyme will increase the concentration of TCAs.

A

Cytochrome P-450

22
Q

Name an example of an induce of cytochrome P-450.

A

Carbamazepine

23
Q

Name two examples of monoamine oxidase inhibitors.

A
  1. Phenelzine

2. Tranylcypromine

24
Q

T or F. Both Phenelzine and Tranylcypromine irreversibly inhibit MAO-A and MAO-B enzymes.

A

True

25
Q

Combination of antidepressants and ? may cause malignant serotonin syndrome?

A

MAOI

26
Q

MAO-A is located in the ? and preferentially oxidizes ?.

A
  1. Gut

2. 5-HT

27
Q

MAO-B is located in ? and preferentially oxidizes ?.

A
  1. Platelets

2. Dopamine

28
Q

Would you consider MAOI a first line drug for depression?

A

No. Phenelzine and Tranylcypromine should not be used as first line drugs for depression due to serious adverse effects.

29
Q

What does SSRI stand for?

A

Selective Serotonin Reuptake Inhibitor

30
Q

Name five examples of SSRI drugs.

A
  1. Fluoxetine
  2. Sertraline
  3. Paroxetine
  4. Citalopram
  5. Escitalopram
31
Q

What serotonin receptor is mainly responsible for adverse effects?

A

5-HT(2) and 5-HT(3)

32
Q

What serotonin receptor is primarily involved in antidepressants and anxiolytic activity?

A

5-HT(1)

33
Q

What is the main mechanism of action of SSRIs?

A

They block the reuptake of 5-HT and enhance postsynaptic activity at all serotonin receptors.

34
Q

T or F. A side effect of SSRI antidepressant drugs is suicidal ideation.

A

True

35
Q

Serotonin syndrome is associated with what antidepressant drug?

A

SSRIs (selective serotonin reuptake inhibitors)

36
Q

Name three second generation antidepressants that are categorized as 5-HT(2) antagonists.

A
  1. Trazodone
  2. Nefazodone
  3. Bupropion
37
Q

Name the three second generation antidepressants that are categorized as TETRAcyclic and UNIcyclic.

A
  1. Amoxapine
  2. Maprotiline
  3. Mirtazepine
38
Q

T or F. The major anti-depressant drugs are equally effective in relieving depression but vary in producing undesirable side effects.

A

True

39
Q

What is the main difference between tricyclic antidepressants and 2nd/3red generation antidepressants?

A

The degree of sedation and their anti-muscarininc effects.

40
Q

What is the main line drug used to treat bipolar disorder?

A

Lithium salts

41
Q

Describe the two mechanisms of action for Lithium salts in treating bipolar disorder.

A
  1. Li+ inhibits inositol monophophatase, which inhibits intracellular signaling.
  2. Li+ inhibits glycogen synthase kinase-3b and cell-cell interaction.
42
Q

T or F. Lithium has a wide therapeutic index.

A

False. The therapeutic range of Li+ is between 1.0-1.2 mEq/liter

43
Q

What is considered a lethal toxicity dose when taking Li+?

A

Anything greater than 5 mEq/liter

44
Q

How does an decrease in Na+ excretion, thiazide diuretics, ACE inhibitors, and NSAIDs all relate to Li+ toxicity?

A

They all lead to an increase in Li+ retention and potential toxicity

45
Q

What two substances promote Li+ excretion?

A
  1. Caffeine

2. Alcohol

46
Q

Bipolar disorder is alternating episodes of ? and ?.

A
  1. Depression

2. Mania

47
Q

What does SNRI (drugs used to treat depression) stand for?

A

Serotonin Norepinephrin reuptake inhibitor

48
Q

Name the two drugs used to treat depression that are serotonin NE reuptake inhibitors.

A
  1. Venlafaxine

2. Desvenlafaxine

Pharmacology (9 decks)

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