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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

23
Q

Imipramine is used for

24
Q

Amitriptyline is used for

A

neuropathic pain (neuroglial pain)

25
Which are the MAOIs
Tranylcypromine Moclobemide Phenelzine
26
MOA of MAOIs
inhibit 1 or both forms of MAO and thus oxidative deamination of NA, DA & 5HT= Incr. cytosolic stores of these neurotransmitters
27
Indications of MAOIs
refractory/atypical depression when SSRIs, TCAs and sometimes even electroconvulsive therapy is ineffective
28
Tranylcypromine inhibits
MAO-a and MAO-b irreversibly (non-selective)
29
Dosage of Tranylcypromine
incr. dose (20-30mg) for depression refractory to sequential trials for other antidepressants
30
AE of MAOIs
sedation postural hypotension (sympathetic block) Insomnia Impotence, sexual dysfunction anxiety restlessness confusion weight gain
31
DI of MAOIs
cause HT crisis if sympathomimetic drug or food containing tyramine is ingested concurrently (cheese rxn) do not use with other classes of antidepressant
32
What happens if MAOIs are taken with other classes of antidepressants
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
WIthdrawal symptoms of MAOIs
delirium psychosis mental confusion
34
Other antidepressant drugs are
Bupropion Mirtazapine Nefazodone Trazodone
35
MOA of Bupropion
inhibit reuptake of NE and Dopamine
36
I of Bupropion
Major depression smoking cessation
37
AE of Bupropion
NV Headaches Activation Agitation Hypertension Insomnia (less sexual dysfunction than other antidepressants)
38
CI of Bupropion
risk of seizures seizure disorder history of anorexia or bulimia using/withdrawing from alcohol or BDZs
39
DI of Bupropion
Bupropion is a substrate for CYP2B6 liver enzymes and is a strong inhibitor of CYP2D6
40
MOA of Mirtazapine
anatgonises adrenergic, 5HT2, 5HT3 Rs= incr. NE and 5HT. Mirtazapine also has activity at Histamine Rs
41
I for Mirtazapine
Major depression
42
AE of Mirtazapine
Sedation Weight gain constipation dry mouth incr. appetite *has decr. risk for causing sexual dysfunction compared to SSRIs
43
AE of low doses of Mirtazapine
Sedation incr appetite weight gain
44
CI of Mirtazapine
pregnancy Lactation <18 yrs Coadministration with MAOIs or within 14 daus of their use
45
DI of Mirtazapine
its a sustrate for CYP34A and CYP2D6 liver enzymes; a weak inhibitor of CYP1A2 and CYP3A4 enzymes
46
MOA of Nefazodone
thought to block 5HT reuptake, incr. 5HT neurotransmission and block 5HT2 postsynaptic Rs
47
I for Nefazodone
1st line for treatment of depression
48
AE of Nefazodone
Dry mouth nausea constipation visual alterations Orthostatic hypotension sedation (most severe AE is hepatic failure)
49
DI of Nefazodone
highly protein bound is an inhibitor of CYP3A4
50
MOA of Trazodone
thought to block 5HT reuptake, incr. 5HT neurotransmission and block 5HT2 postsynaptic Rs
51
I for Trazodone
depression
52
AE of Trazodone
sedation nausea sexual dysfunction oethostatic hypotension
53
what has Trazodone been rarely been associated with (AEs)
Priapism and QT prolongation
54
DI of Trazodone
metabolised mainly by CYP34A, whereas active metabolite m-chlorophenylpiperazine (mCCP) is metabolised by CYP2D6

Pharmacology (50 decks)

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