Pharm Anti Depressants

Front 1

(Big picture question)
What are the major drug categories that are used as anti depressants?

Back 1

1)TCAs (tricyclic antidepressants)
2)MAO-Inhibitors
3)SSRIs (selective serotonin reuptake inhibitors)
4)SNRIs (serotonin norepinephrine repuptake inhibitors)
5)Atypicals
6)Melatonin agonists

Front 2

What drugs are included in the Tricyclic antidepressants?

Back 2

Imipramine
Amytriptyline
Clomipramine

Front 3

TCAs do what at the neuronal level?

Back 3

They inhibit reuptake of serotonin (5-HT) and Norepinephrine (NE).

Front 4

What are the relative ratios of 5-HT to NE of reuptake inhibition of the three TCAs? (Imipramine, Amytriptyline, Clomipramine)
Also, what can Clomipramine treat in addition to depression that the others can't?

Back 4

Imipramine (5-HT = NE)

Amytriptyline (5-HT > NE, slightly favors 5-HT)

Clomipramine (5-HT>>NE, favors 5-HT)
Clomipramine also used to treat OCD.

Front 5

What is the biochemical/physiological explanation for TCA's Adverse Effects?

Back 5

In addition to inhibiting reuptake of NE and 5-HT, the TCA's all block:
1) Muscarinic sites
2) Histamine sites (H1)
3) Alpha adrenoceptors

Front 6

Which major antidepressant drug category is effective in resistant patients?

Back 6

TCA's

Front 7

Uses of TCA's include? (4)

Back 7

1) Used as third line (or later) treatment of MAJOR DEPRESSION and ANXIETY DISORDERS (including OCD) (Effective even in resistant patients)

2) Neuropathic pain
3) Nocturnal enuresis, urinary incontinence
4) Irritable bowel syndrome

Front 8

This anti-depressant drug category has a limited use because of it's side effects and narrow therapeutic index.

Back 8

TCA's

Front 9

TCA's are often lethal in overdose. Why?

Back 9

Narrow therapeutic index.

Front 10

MAO Inhibitors include what drugs?

Back 10

Phenelzine
Selegiline

Front 11

MOA of Phenelzine?

Back 11

Irreversible, nonselective MAO-A/MAO-B inhibitor.
Results in an increase of 5-HT, Dopamine, NE

Front 12

Adverse effects of Phenelzine?

Back 12

Hypertensive crisis
Sexual dysfunction
Insomnia

Front 13

MOA of Selegiline?

Back 13

Irreversible, selective inhibitor of MAO-B at low doses. High doses inhibits both.

Front 14

Adverse effects of Selegiline include?

Back 14

Skin reactions
Headaches
Insomnia

Front 15

MAO-A deaminates what?

Back 15

Serotonin
Melatonin
Epinephrine
Norepinephrine
Dopamine

Front 16

MAO-B deaminates what?

Back 16

Dopamine
Phenylethylamine
Trace amines

Front 17

Ingestion of MAO-A inhibitor can lead to what?

Back 17

Hypertensive crisis

Front 18

Use of a Selegiline patch will inhibit both MAO-A and MAO-B. Will it lead to hypertensive crisis?

Back 18

No, for some reason hypertensive crisis will only occur if it's ingested.

Front 19

Use of Selegiline patch will lead to an increase in the levels of?

Back 19

Dopamine, NE, 5-HT

(also other stuff, but those three are important for treating depression)
(it'll increase the levels of anything that usually gets deaminated by MAO-A and MAO-B, (this includes melatonin, epinephrine, phenylethylamine, trace amines, in addition to the first three mentioned)

Front 20

Selegiline patches will not inhibit MAO where?

Back 20

In the stomach/GI tract.

Front 21

Increase in what substance, and where, will increase neuroplasticity?

Back 21

Increase in BDNF in the Hippocampus

Front 22

Stress leads to (increased/decreased) BDNF?

Back 22

Decreased

Front 23

1st generation antidepressants include?

Back 23

TCAs
MAO Inhibitors

Front 24

How do SSRI's work?

Back 24

They bind to SERT (serotonin transport(er?) on the presynaptic terminal and prevent it reuptake.

Front 25

If someone is on SSRI's for a couple of weeks, what will happen to the number of autoreceptors on the presynaptic terminal?

Back 25

They are down regulated and desensitized.

Front 26

Name the SSRI's.

Back 26

Sertraline
Escitalopram
Citalopram
Fluoxetine
Paroxetine

Front 27

Which SSRI's inhibit CYP450's?

What else is unique about them?

Back 27

Fluoxetine
Paroxetine

Fluoxetine has a decreased seizure threshold.
Paroxetine has higher rates of sexual dysfunction.

Front 28

Which SSRI's have superior efficacy and tolerability?

What else they do?

Back 28

Sertraline
Escitalopram

They can each treat depression and anxiety.
Sertraline can also treat OCD and panic disorder.

Front 29

Which SSRI shows superior tolerability (without superior efficacy)?

Back 29

Citalopram

Front 30

Adverse effect(s) of SSRI's include?

Back 30

Serotonin Syndrome (***when given with other drug that increases 5-HT)

Nausea and Vomitting
Insomnia/Fatigue
Sexual side effects

Front 31

SSRI's have a (large/small) therapeutic index?

Back 31

Large therapeutic index.

Front 32

List complications of Serotonin syndrome. (note, lists vary, but may include the following)

Back 32

Hyperkinetic
Tremor (which can lead to coma and death)
Myoclonus (muscle twitching)
Hyperreflexia
Agitation
Tachycardia
Hallucinations

Front 33

When switching anti depressants (from say SSRI to MAOI), you should wait AT LEAST how long?

Why?

Back 33

5 half lives of whatever drug they are on.

To avoid drug-drug interactions.

Front 34

SSRI’s are primarily broken down where?

Back 34

Liver

Front 35

Name the SNRI's.

Back 35

Duloxetine
Venlafaxine
Desvenlafaxine

Front 36

Which anti depressants should you taper off slowly when discontinuing?

Back 36

SNRI's

(this may not be the only one, but I saw this writin in her lecture notes)

Front 37

SNRI's are used to treat?

Back 37

Depression
Anxiety
Fibromyalgia
Neuropathic pain
**Approved for BACK PAIN and OSTEOARTHRITIS PAIN

(Venlafaxine and Desvenlafaxine tx hot flashes in menopause too)

Front 38

Adverse effect of Duloxetine?

Back 38

Hepatotoxicity

Front 39

What drugs are first line treatments for anxiety and depression? (give category AND specific drugs within it)

Back 39

(SNRI's)
Duloxetine
Venlafaxine
(desvenlafaxine too?)

Front 40

Adverse effects of SNRI's as a whole are similar to what other anti depressants?

Back 40

SSRI's

(but maybe more severe versions of them)

Include: Nausea and vomiting,
insomnia, sexual dysfunction, etc.

Front 41

What are the atypical anti depressants?

Back 41

Bupropion
Mirtazapine
Trazodone

Front 42

MOA of Bupropion?

Back 42

NE and Dopamine reuptake inhibitor.

Front 43

Bupropion can be used for?

Back 43

Depression (NOT anxiety)
Quit smoking

(Seasonal affective disorder, bipolar disorder)

Front 44

What Atypical antidepressant is safe to use in patients with cardiac problems?

Back 44

Bupropion

Front 45

What are the adverse effects of bupropion?

Back 45

Decreased appetite/weight
Insomnia

(NO sexual dysfunction though)

Front 46

Mirtazapine's MOA?

Back 46

1) Increases 5-HT + NE (via being an Alpha 2 antagonist (Presynaptic))

2) Indirectl augmenter of 5-HT (via Blockade of 5-HT2A and 2C-autoreceptor).

3) Indirect agonist of 5-HT 1A sites (via increases in 5-HT actions)

Front 47

Which anti depressant drugs can be used in mono-therapy (by themselves) or as an adjunct?

Back 47

Bupropion
Mirtazapine

(atypicals)

Front 48

Use(s) of Mirtazapine?

Back 48

2nd line tx or as Adjunct.
Increases efficasy of other drugs
Decreases side effects
*Used especially in patients who show tolerance to traditional drugs.

Front 49

Benefits of using Mirtazapine? (3)

Back 49

Decreased sexual dysfunction.
Few drug-drug interactions
Can be used as anti-nausea

Front 50

Adverse effect(s) of Mirtazapine?

Back 50

Dizziness
Increased appetite/Weight gain
Sedating effect (can be used as sedative for depressed pt)

Front 51

Trazodone's MOA?

Back 51

Serotonin Antagonist and Reuptake Inhibitor (SARI)

5-HT 2A + 2C Antagonist

Partial agonist at 5HT 1A
Antagonist at others

Front 52

True/False: Trazodone is typically used as an adjunct.

Back 52

True

Front 53

Adverse effect(s) of Trazodone?

Back 53

Drowsiness/Sedation
Postural hypotension
(etc)

Front 54

Agomelatine MOA?

Back 54

5-HT 2C antagonist (of autoreceptor).
(Increases release of NE+5-HT from nerve terminals, which decreases depression)

MT1 + MT2 agonist.

Front 55

Use(s) of Agomelatine?

Back 55

Treat Depression
Restores Circadian rhythm
(improve sleep quality)

(Not approved in the US yet)