Antidepressants

Question 1

What are depressive episodes characterised by?

Answer 1

depressive mood, sadness severe enough to interfere with function
loss of interest or pleasure in daily activities (up to 2 weeks).
Sleep and appetite disturbances
Low energy levels, Decreased cognition

Question 2

Aetiology of depression?

Answer 2

Unknown but involves genetic and environmental factors.
‣heredity, changes in neurotransmitter levels (decrease in
monoamines, serotonin & norepinephrine), altered
neuroendocrine function and psychosocial factors thought to play a
role

Question 3

Drugs that induce depression?

Answer 3

• Beta-blockers (Atenolol)
• calcium channel blockers (Amlodipine)
• Benzodiazepines (Diazepam)
• Dopaminergic agents (Levodopa, α-methyldopa)
• Corticosteroids (Methylprednisolone)
• Anabolic steroids (Testosterone)

Question 4

Depression treatment?

Answer 4

• Psychotherapy +
• Pharmacotherapy
  tricyclic antidepressants
  selective serotonin reuptake
  inhibitors (SSRIs)
  Serotonin-norepinephrine
  reuptake inhibitors (SNRIs)
  5-HT2antagonists
  monoamine oxidase
  inhibitors (MAOIs)
  atypical antidepressants
  lithium

Question 5

Selective Serotonin Reuptake Inhibitors (SSRIs) drugs?

Answer 5

FESC (FUSEK FEELINGS)

Fluxoxetine
Escitalopram
Sertraline
Paroxetine

Question 6

Selective Serotonin Reuptake Inhibitors (SSRIs) MOA?

Answer 6

prevent the (presynaptic) reuptake of 5-HT→more 5-HT to
stimulate postsynaptic 5-HT1 receptors

Question 7

SSRIs I?

Answer 7

major depression, anxiety disorders (PTSD, PD, OCD, PDD etc.)
Fluoxetine: 20 - 40 mg po od;

Question 8

What is the risk of fluxetine in the elderly?

Answer 8

cardiovascular & suicide risk
in the elderly

Question 9

SSRIs S/E?

Answer 9

BAD SSRI

Body weight increase
Anorexia(first few months)
Dizziness
Suicidal Thoughts
Serotonin Syndrome
Reproductive-Sexual Dysfunction
Insomnia

Question 10

SSRI DI?

Answer 10

DI: do not use with MAOI; fluoxetine can inhibit cytochrome P-450
isoenzymes and thus the metabolism of certain β -blockers including
propranolol and metoprolol → hypotension, bradycardia

Question 11

Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs) drugs?

Answer 11

Very Damned

Venlafaxine, desvenlafaxine, duloxetine

Question 12

Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs) drugs MOA for selective SNRI?

Answer 12

prevent the (presynaptic) reuptake of 5-HT, NE and DA (weak)→more 5-HT and NE to stimulate postsynaptic 5-
HT and NE receptors.

Question 13

Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs) drugs MOA for TCA?

Answer 13

prevents the (presynaptic) reuptake of 5-HT and NE by
neuronal membrane; may also downregulate β–adrenergic and 5-HT
receptors

Question 14

Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs) drugs I?

Answer 14

major depression, anxiety disorders (PTSD, PD, OCD, PDD etc.

Question 15

Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs) drugs A/E?

Answer 15

N, D, anxiety, restlessness, insomnia, sexual dysfunction, ↑BP,
↑HR, agitation, serotonin-withdrawal syndrome; TCAs [additional
antimuscarinic (dry mouth, constipation, urinary retention),
orthostatic hypotension due to peripheral α1-blockade]

Question 16

Monoamine oxidase inhibitors drugs?

Answer 16

Takes Pride In Shanghai

Tranylcypromine, moclobemide, phenelzine

Question 17

Monoamine oxidase inhibitors MOA?

Answer 17

MOA:Inhibit one or both forms of MAO and thus the oxidative
deamination of NA, DA and 5-HT→ ↑ cytosolic stores of the
neurotransmitters

Question 18

Monoamine oxidase inhibitors I?

Answer 18

I:refractory or atypical depression when SSRIs, TCAs and
sometimes even electroconvulsive therapy is ineffective.

Question 19

MAO Tranycypromine?

Answer 19

irreversible, non-selective (inhibit MAO-A
and MAO-B);
↑ dose (20 - 30 mg po bid) for depression refractory to
sequential trials of other antidepressants

Question 20

Tranycypromine A/E?

Answer 20

HAHA

Hypertension(postural) crsis(tyramine)
Anxiety, Agitation, Anorexia
Hypotension
Anticholinergic

Question 21

Tranycypromine DI?

Answer 21

cause hypertensive crisis if asympathomimetic drugor
food containing tyramine is ingested concurrently (cheese
reaction);do not use with other classes of antidepressants
→prolong and potentiate the effects of CNS depressants such
as alcohol, anaesthetics, sedative hypnotics; interact with
pethidine causing hyperpyrexia and hypotension

Question 22

Tranycypromine withdrawl?

Answer 22

delirium, psychosis, confusion

Question 23

Bupropion MOA?

Answer 23

MOA: inhibit the reuptake of NE and dopamine

Question 24

Bupropion I?

Answer 24

I: Major depression, smoking cessation
AE: nausea, vomiting, headaches, activation, agitation,
hypertension, and insomnia.
(less sexual dysfunction than other antidepressant medications

Question 25

Bupropion CI?

Answer 25

CI: risk for seizures, seizure disorder, history of anorexia or bulimia, or using or withdrawing from alcohol or benzodiazepines

Question 26

Bupropion DI?

Answer 26

DI: Bupropion is a substrate of CYP2B6 liver enzymes and is a strong inhibitor of CYP2D6.

Question 27

Bupropion S/E?

Answer 27

Increased of risk seizure

Question 28

Mirtazapine MOA?

Answer 28

MOA: antagonizes adrenergic, 5-HT2-, 5-HT3-receptors → ↑ NE and 5-HT. In addition, mirtazapine has activity at histamine (H) receptors. * Sedation, increased appetite, and weight gain can be problematic, particularly at lower doses. * has ↓ risk for causing sexual dysfunction compared to SSRIs. CI:pregnancy, lactation, <18 ,yrs of age, coadministration with MAOIs or within 14 days of their use. DI: a substrate of CYP3A4 and CYP2D6 liver enzymes; a weak inhibitor of CYP1A2 and CYP3A4 enzymes.

Question 29

Mirtazapine I?

Answer 29

I: Major depression

Question 30

Mirtazapine A/E?

Answer 30

Weight gain Sedation

Question 31

Mirtazapine CI?

Answer 31

Pregnancy, lactation, coadminstration with MAOI's

Question 32

Mirtazapine DI?

Answer 32

DI: a substrate of CYP3A4 and CYP2D6 liver enzymes; a weak inhibitor of CYP1A2 and CYP3A4 enzymes.

Question 33

Trazodone MOA?

Answer 33

MOA: thought to block 5-HT reuptake, ↑ 5-HT neurotransmission, and block 5-HT2- postsynaptic receptors.

Question 34

Trazodone I?

Answer 34

I: Depression

Question 35

Trazodone A/E?

Answer 35

AE: sedation, nausea, sexual dysfunction, and orthostatic hypotension. (has rarely been associated with priapism and QT prolongation)

Question 36

Trazodone D/I?

Answer 36

DI: metabolized mainly by CYP3A4, whereas active metabolite m- chlorophenylpiperazine (mCCP) is metabolized by CYP2D6.

Question 37

Trazodone CI?

Answer 37

CI:alcohol or hypnotics intoxication, acute MI, children and adolescents <18 yrs.

Question 38

Nefazodone structure similiarity?

Answer 38

Structurally similar to trazodone

Question 39

Nefazodone MOA?

Answer 39

MOA: similar to trazodone

Question 40

Nefazodone I?

Answer 40

I: first line for treatment of depression

Question 40

Nefazodone I?

Answer 40

AE: dry mouth, nausea, constipation, visual alterations, orthostatic hypotension, and sedation. (The most severe adverse effect associated with nefazodone is hepatic failure).

Question 41

Nefazodone DI?

Answer 41

DI: highly protein bound and is an inhibitor of CYP3A4.

Question 42

Bipolar disorder drug?

Answer 42

Lithium

Question 43

Lithium P/K?

Answer 43

-Narrow TI -Nephrogenic diabetes insipidious -Nephritis -Decreased Blood Pressure -Tremor

Question 44

TCA drugs?

Answer 44

CIA Clomipromine Imipramine Amittryilne

Question 45

TCA drugs uses?

Answer 45

Clomipromine-used in OCD Imipramine-Eneursis Amittryilne-neurolgia

Question 46

TCA MAO?

Answer 46

Blocks SERT, NERT, Alpha-1 & Beta-1 and muscuranic receptors

Question 47

TCA S/E?

Answer 47

Muscuranic S/E: Constipation, Blurred Vision Alpha-receptors: Postural Hypertension Histamine: Weight gain

Question 48

TCA overdose?

Answer 48

Coma, Seizure, Cardiac Arrest and Arrthymias