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Pharmacology > Antidepressants > Flashcards

Antidepressants Flashcards

1
Q

Characteristics of Depression

A

-depressive mood, severe sadness that interferes with function
-loss of interest or pleasure in daily act.(2wk)
-sleep and appetite disturbances
-low energy levels, decr. cognition

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2
Q

Aetiology of depression

A

unknown but involves genetic & env. factors

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3
Q

Factors affected by depression

A

decr. in monoamines, serotonin and NE
Altered neuroendocrine function and physiological factors

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4
Q

Drugs that induce depression

A

B-blockers (atenolol)
Ca-channel blockers (amlodipine)
BDZ (diazepam)
Dopaminergic agents (levodopa, a-methyldopa)
Corticosteroids (methylprednisone)
Anabolic steroids (testosterone)

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5
Q

Pharmacological drugs used to treat depression

A

TCA
SSRIs
SNRI
5HT2 Antagonists
MAOIs
Atypical antidepressants
Lithium

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6
Q

SSRI drugs are

A

FESP-AC
Fluoxetine
Paroxetine
Atomoxetine
Citalopram
Escitalopram
Sertraline

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7
Q

MOA of SSRIs

A

prevent (presynaptic) reuptake of 5HT therefore more 5HT available to stimulate post synaptic 5HT receptors

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8
Q

5HT 1 R function

A

causes antidepressant and anxiolytic effects

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9
Q

5HT2 Receptor Function

A

for anxiety, insomnia and sexual dysfunction

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10
Q

5HT3 Receptor function

A

for nausea and headache

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11
Q

Indications of SSRIs

A

major depression
anxiety disorders (PTSD, Panic Disorder, OCD, PDD)

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12
Q

Dose of Fluoxetine

A

20-40mg; CVS and suicide risk in elderly

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13
Q

SE of SSRIs

A

Nausea
Diarhoea
Restlessness
Insomnia
Sexual dysfunction
Serotonin-Withdrawal Syndrome
Fluoxetine causes weight gain in first few months

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14
Q

DI of SSRIs

A

Do not use with MOAi; fluoxetine can inhibit CYP450= metabolism of B-blockers including propranolol and metoprolol= hypotension, bradycardia

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15
Q

Which are the SNRIs

A

Venlafaxine
Desvenlafaxine
duloxetine

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16
Q

MOA of SNRIs

A

prevent presynaptic reuptake of 5HT, NE and DA (weak)= more 5HT and NE to stimulate postsynaptic 5HT and NE Receptors

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17
Q

Which are the TCAs

A

CIA DTM
Clomipramine
Imipramine
Amitriptyline
Amoxapine
Doxepin
Trimipramine
Mirtazapine (tetra)
Mianterin (tetra)

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18
Q

MOA of TCAs

A

Prevent presynaptic reuptake of 5HT and NE by neuronal membrane; may also downregulate B-adrenergic and 5HT receptors
=basically block muscarinic, B, Histamine Rs

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19
Q

Indications of SNRIs

A

major depression
Anxiety disorders (PTSD, PD, OCD, PDD)

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20
Q

AE of SNRIs

A

nausea
diarrhea
restlessness
insomnia
sexual dysfunction
Incr. BP
Incr. HR
agitation
Serotonin withdrawal syndrome

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21
Q

AEs of TCAs

A

antimuscarinic: dry mouth, constipation, urinary retention
Orthostatic hypotension due to peripheral a1 blockade

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22
Q

Clomipramine is used for

A

OCD

23
Q

Imipramine is used for

A

enuresis

24
Q

Amitriptyline is used for

A

neuropathic pain (neuroglial pain)

25
Q

Which are the MAOIs

A

Tranylcypromine
Moclobemide
Phenelzine

26
Q

MOA of MAOIs

A

inhibit 1 or both forms of MAO and thus oxidative deamination of NA, DA & 5HT=
Incr. cytosolic stores of these neurotransmitters

27
Q

Indications of MAOIs

A

refractory/atypical depression when SSRIs, TCAs and sometimes even electroconvulsive therapy is ineffective

28
Q

Tranylcypromine inhibits

A

MAO-a and MAO-b irreversibly (non-selective)

29
Q

Dosage of Tranylcypromine

A

incr. dose (20-30mg) for depression refractory to sequential trials for other antidepressants

30
Q

AE of MAOIs

A

sedation
postural hypotension (sympathetic block)
Insomnia
Impotence, sexual dysfunction
anxiety
restlessness
confusion
weight gain

31
Q

DI of MAOIs

A

cause HT crisis if sympathomimetic drug or food containing tyramine is ingested concurrently (cheese rxn)
do not use with other classes of antidepressant

32
Q

What happens if MAOIs are taken with other classes of antidepressants

A

prolong and potentiate effects of CNS depressants such as alcohol, anesthetics, sedative hypnotics; interact with Pethidine causing hyperpyrexia and hypotension
–> drastic inr. in BP= stroke. MI

33
Q

WIthdrawal symptoms of MAOIs

A

delirium
psychosis
mental confusion

34
Q

Other antidepressant drugs are

A

Bupropion
Mirtazapine
Nefazodone
Trazodone

35
Q

MOA of Bupropion

A

inhibit reuptake of NE and Dopamine

36
Q

I of Bupropion

A

Major depression
smoking cessation

37
Q

AE of Bupropion

A

NV
Headaches
Activation
Agitation
Hypertension
Insomnia
(less sexual dysfunction than other antidepressants)

38
Q

CI of Bupropion

A

risk of seizures
seizure disorder
history of anorexia or bulimia
using/withdrawing from alcohol or BDZs

39
Q

DI of Bupropion

A

Bupropion is a substrate for CYP2B6 liver enzymes and is a strong inhibitor of CYP2D6

40
Q

MOA of Mirtazapine

A

anatgonises adrenergic, 5HT2, 5HT3 Rs=
incr. NE and 5HT.
Mirtazapine also has activity at Histamine Rs

41
Q

I for Mirtazapine

A

Major depression

42
Q

AE of Mirtazapine

A

Sedation
Weight gain
constipation
dry mouth
incr. appetite
*has decr. risk for causing sexual dysfunction compared to SSRIs

43
Q

AE of low doses of Mirtazapine

A

Sedation
incr appetite
weight gain

44
Q

CI of Mirtazapine

A

pregnancy
Lactation
<18 yrs
Coadministration with MAOIs or within 14 daus of their use

45
Q

DI of Mirtazapine

A

its a sustrate for CYP34A and CYP2D6 liver enzymes; a weak inhibitor of CYP1A2 and CYP3A4 enzymes

46
Q

MOA of Nefazodone

A

thought to block 5HT reuptake, incr. 5HT neurotransmission and block 5HT2 postsynaptic Rs

47
Q

I for Nefazodone

A

1st line for treatment of depression

48
Q

AE of Nefazodone

A

Dry mouth
nausea
constipation
visual alterations
Orthostatic hypotension
sedation
(most severe AE is hepatic failure)

49
Q

DI of Nefazodone

A

highly protein bound
is an inhibitor of CYP3A4

50
Q

MOA of Trazodone

A

thought to block 5HT reuptake, incr. 5HT neurotransmission and block 5HT2 postsynaptic Rs

51
Q

I for Trazodone

A

depression

52
Q

AE of Trazodone

A

sedation
nausea
sexual dysfunction
oethostatic hypotension

53
Q

what has Trazodone been rarely been associated with (AEs)

A

Priapism and QT prolongation

54
Q

DI of Trazodone

A

metabolised mainly by CYP34A, whereas active metabolite m-chlorophenylpiperazine (mCCP) is metabolised by CYP2D6

Pharmacology (50 decks)

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