Pharmacology 2 Antidepressant Agents

Front 1

According to the biogenic amine theory, depression is due to a deficiency of which two neurotransmitters in the brain

Back 1

Serotonin (5-HT)
Norepinephrine (NE)

Hint 1

None

Front 2

Where in the neuron is monamine oxidase (MOA) located

Back 2

Mitochondria

Hint 2

None

Front 3

Where in the body is MAO located

Back 3

Neuron
Liver
GI tract

Hint 3

None

Front 4

MAOa inactivates which neurotransmitters

Back 4

5-HT; NE

Front 5

MAOb inactivates which neurotransmitter

Back 5

Dopamine (DA)

Front 6

What is the mechanism of action of MAOIs

Back 6

Inactivation of MAO thereby increasing levels of 5-HT, NE, and DA in presynaptic neurons with subsequent leakage of neurotransmitter into the synaptic cleft

Front 7

Name three nonselective MAOIs

Back 7

Tranylcypromine
Phenelzine
Isocarboxazid

Hint 7

None

Front 8

Which medication selectively inhibits MAOb at low to normal doses yet loses its selectivity at higher doses

Back 8

Selegiline

Front 9

Selegiline is commonly used in the treatment of which disease

Back 9

Parkinson disease

Front 10

MAOa also inactivates which monamine commonly found in certain cheese (aged), alcoholic beverages, fish, chocolates, red wines, and processed meats

Back 10

Tyramine (inactivated by MAO in the GI tract)

Front 11

MAOIs are the drugs of choice for treating what type of depression

Back 11

Atypical depression

Front 12

How long does it take to see antidepressant effects in patients who are started on an MAOI

Back 12

2-4 weeks

Front 13

How long should a patient wait from the time of discontinuing an MAOI to the time of starting a new antidepressant medication

Back 13

At least 2 weeks

Front 14

What are the adverse effects of MAOIs

Back 14

Orthostatic hypotension
Blurred vision
Drowsiness
Xerostomia
Constipation
Urinary retention

Hint 14

None

Front 15

What life-threatening condition may develop when MAOIs and selective serotonin reuptake inhibitors (SSRIs) are used concomitantly

Back 15

Serotonin syndrome

Hint 15

None

Front 16

What characterizes serotonin syndrome

Back 16

Rigidity
Diaphoresis
Hyperthermia
Seizures
Autonomic instability
Myoclonus

Hint 16

None

Front 17

What life-threatening condition may develop when patients taking MAOIs ingest food containing tyramine

Back 17

Hypertensive crisis

Front 18

What characterizes hypertensive crisis

Back 18

Hypertension
Tachycardia
Cardiac arrhythmias
Headache
Stroke
Nausea
Vomiting

Hint 18

None

Front 19

A serotonin-like syndrome may develop when MAOIs are used concomitantly with what common OTC medication used to suppress cough

Back 19

Dextromethorphan

Front 20

A serotonin-like syndrome may develop when MAOIs are used concomitantly with which opioid analgesic

Back 20

Meperidine

Hint 20

None

Front 21

What is the mechanism of action of tricyclic antidepressants (TCAs)

Back 21

Inhibits reuptake of 5-HT and NE into presynaptic neurons thereby increasing neurotransmitter concentrations in the synaptic cleft

Front 22

What other types of neurotransmitter and hormonal receptors, other than 5-HT and NE, are inhibited by TCAs

Back 22

Muscarinic
α-adrenergic
Histaminergic

Hint 22

None

Front 23

How long does it take to see antidepressant effects in patients who are started on a TCA

Back 23

4-6 weeks

Front 24

Give examples of TCAs

Back 24

Imipramine→Desipramine
Amitriptyline→Nortriptyline
Clomipramine
Doxepin
Protriptyline

Hint 24

None

Front 25

What is the name of the active metabolite of amitriptyline that selectively inhibits NE uptake

Back 25

Nortriptyline

Front 26

What is the name of the active metabolite of imipramine that selectively inhibits NE uptake

Back 26

Desipramine

Front 27

Which TCA is also used for the treatment of certain types of neuropathic pain and for the prevention of migraine headaches

Back 27

Amitriptyline

Front 28

Which TCA is commonly used to treat obsessive-compulsive disorder (OCD)

Back 28

Clomipramine

Front 29

Which TCA is also used to treat pediatric nocturnal enuresis

Back 29

Imipramine

Front 30

Why is imipramine used for childhood enuresis

Back 30

Increases contraction of internal sphincter of bladder; Decreases stage 3 and 4 sleep

Front 31

What are the adverse effects of the TCAs

Back 31

Xerostomia
Blurred vision
Urinary retention
Constipation
Precipitation of acute glaucoma attacks
Cardiac arrhythmias
Seizures (lowers seizure threshold)
Orthostatic hypotension with reflex tachycardia
Sedation
Serotonin syndrome when combined with MAOIs and/or SSRIs
Coma

Hint 31

None

Front 32

What are the “3-C’s” of TCA toxicity

Back 32

Coma, convulsions, and cardiotoxicity

Front 33

Can overdosing on a TCA lead to death

Back 33

Yes

Front 34

Can overdosing on a SSRI lead to death

Back 34

No

Front 35

What is the mechanism of action of amoxapine and maprotiline

Back 35

Inhibits reuptake of NE into presynaptic neurons thereby increasing neurotransmitter concentrations in the synaptic cleft

Front 36

What is the mechanism of action of trazodone and nefazodone

Back 36

Inhibits reuptake of 5-HT into presynaptic neurons thereby increasing neurotransmitter concentrations in the synaptic cleft

Front 37

Which antidepressant, trazodone or nefazodone, can inhibit cytochrome P-450 enzymes

Back 37

Nefazodone

Hint 37

None

Front 38

What adverse effect is unique to trazodone

Back 38

Priapism

Front 39

What is the mechanism of action of bupropion

Back 39

Weak inhibitor of DA, 5-HT and NE uptake

Front 40

Bupropion is also used in what setting (other than depression)

Back 40

Smoking cessation; OCD

Front 41

Does bupropion cause sexual dysfunction

Back 41

No

Front 42

Is bupropion safe to use in patients with epilepsy

Back 42

No (lowers seizure threshold)

Front 43

What is the mechanism of action of mirtazapine

Back 43

α2 antagonist (results in increased release of NE and 5-HT)

Front 44

Name an α2 antagonist that is used in the treatment of sexual dysfunction

Back 44

Yohimbine

Front 45

What is the major side effect of mirtazapine

Back 45

Weight gain via appetite stimulation (may be beneficial in depressed patients who become anorexic)

Front 46

What is the mechanism of action of venlafaxine

Back 46

Potent inhibitor of 5-HT and NE reuptake; weak inhibitor of DA reuptake

Front 47

What is the major side effect of venlafaxine

Back 47

Hypertension

Front 48

What is the mechanism of action of duloxetine

Back 48

Selective serotonin and norepinephrine reuptake inhibitor (SSNRI)

Front 49

Give examples of SSRIs

Back 49

Fluoxetine→Norfluoxetine
Fluvoxamine
Paroxetine
Sertraline
Citalopram
Escitalopram

Hint 49

None

Front 50

What is the prototype of the SSRI drug class

Back 50

Fluoxetine

Front 51

What is the longest-acting SSRI

Back 51

Fluoxetine

Front 52

What is the half-life of fluoxetine

Back 52

5 days

Front 53

Fluoxetine is also used in what setting (other than depression)

Back 53

Premenstrual dysphoric disorder (PMDD)
Bulimia nervosa
OCD
Panic disorder
Selective mutism

Hint 53

None

Front 54

Which SSRI has a sole FDA indication for the treatment of OCD

Back 54

Fluvoxamine

Front 55

What is the name of fluoxetine’s active metabolite

Back 55

Norfluoxetine

Front 56

What kind of drug interactions may SSRIs produce

Back 56

Inhibition of cytochrome P-450 enzymes

Front 57

Do SSRIs cause sexual dysfunction

Back 57

Yes (anorgasmia)

Front 58

Do SSRIs cause cardiac arrhythmias

Back 58

No (unlike TCAs)

Front 59

What are the adverse effects of SSRIs

Back 59

Sexual dysfunction
Agitation
Anxiety
Seizures (with overdose)
Nausea
Vomiting
Diarrhea
Sedation

Hint 59

None

Front 60

Which SSRI is also FDA approved for social anxiety disorder, generalized anxiety disorder, and posttraumatic stress disorder

Back 60

Paroxetine

Front 61

Which SSRIs cause the least amount of drug-drug interactions

Back 61

Sertraline
Citalopram
Escitalopram

Hint 61

None