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Pharmacology > Antidepressants > Flashcards

Antidepressants Flashcards

1
Q

What are depressive episodes characterised by?

A

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

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2
Q

Aetiology of depression?

A

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

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3
Q

Drugs that induce depression?

A
  • Beta-blockers (Atenolol)
  • calcium channel blockers (Amlodipine)
  • Benzodiazepines (Diazepam)
  • Dopaminergic agents (Levodopa, α-methyldopa)
  • Corticosteroids (Methylprednisolone)
  • Anabolic steroids (Testosterone)
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4
Q

Depression treatment?

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

Selective Serotonin Reuptake Inhibitors (SSRIs) drugs?

A

FESC (FUSEK FEELINGS)

Fluxoxetine
Escitalopram
Sertraline
Paroxetine

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6
Q

Selective Serotonin Reuptake Inhibitors (SSRIs) MOA?

A

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

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7
Q

SSRIs I?

A

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

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8
Q

What is the risk of fluxetine in the elderly?

A

cardiovascular & suicide risk
in the elderly

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9
Q

SSRIs S/E?

A

BAD SSRI

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

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10
Q

SSRI DI?

A

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

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11
Q

Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs) drugs?

A

Very Damned

Venlafaxine, desvenlafaxine, duloxetine

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12
Q

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

A

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

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13
Q

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

A

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

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14
Q

Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs) drugs I?

A

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

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15
Q

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

A

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]

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16
Q

Monoamine oxidase inhibitors drugs?

A

Takes Pride In Shanghai

Tranylcypromine, moclobemide, phenelzine

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17
Q

Monoamine oxidase inhibitors MOA?

A

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

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18
Q

Monoamine oxidase inhibitors I?

A

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

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19
Q

MAO Tranycypromine?

A

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

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20
Q

Tranycypromine A/E?

A

HAHA

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

21
Q

Tranycypromine DI?

A

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

22
Q

Tranycypromine withdrawl?

A

delirium, psychosis, confusion

23
Q

Bupropion MOA?

A

MOA: inhibit the reuptake of NE and dopamine

24
Q

Bupropion I?

A

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

25
Q

Bupropion CI?

A

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

26
Q

Bupropion DI?

A

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

27
Q

Bupropion S/E?

A

Increased of risk seizure

28
Q

Mirtazapine MOA?

A

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.

29
Q

Mirtazapine I?

A

I: Major depression

30
Q

Mirtazapine A/E?

A

Weight gain
Sedation

31
Q

Mirtazapine CI?

A

Pregnancy, lactation, coadminstration with MAOI’s

32
Q

Mirtazapine DI?

A

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

33
Q

Trazodone MOA?

A

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

34
Q

Trazodone I?

A

I: Depression

35
Q

Trazodone A/E?

A

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

36
Q

Trazodone D/I?

A

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

37
Q

Trazodone CI?

A

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

38
Q

Nefazodone structure similiarity?

A

Structurally similar to trazodone

39
Q

Nefazodone MOA?

A

MOA: similar to trazodone

40
Q

Nefazodone I?

A

I: first line for treatment of depression

40
Q

Nefazodone I?

A

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

41
Q

Nefazodone DI?

A

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

42
Q

Bipolar disorder drug?

43
Q

Lithium P/K?

A

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

44
Q

TCA drugs?

A

CIA

Clomipromine
Imipramine
Amittryilne

45
Q

TCA drugs uses?

A

Clomipromine-used in OCD
Imipramine-Eneursis
Amittryilne-neurolgia

46
Q

TCA MAO?

A

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

47
Q

TCA S/E?

A

Muscuranic S/E: Constipation, Blurred Vision

Alpha-receptors: Postural Hypertension

Histamine: Weight gain

48
Q

TCA overdose?

A

Coma, Seizure, Cardiac Arrest and Arrthymias

Pharmacology (44 decks)

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