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Human Pharmacy > Antidepressants > Flashcards

Antidepressants Flashcards

1
Q

List the relevant classes of antidepressants?

A

TCA = tricyclic antidepressants

MAOi = monoamine oxidase inhibitor

RIMA = reversible inhibitor monoamine oxidase A (RIMA)

SSRIs

SNRIs (less selective)

NARI = noradrenaline reuptake inhibitor

Other = mianserin, mirtazapine (NS-recept antagonist), agomelatine, vortioxetine, hypericin

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2
Q

List the relevant TCAs

A

amitriptyline
imipramine
nortriptyline
clomiparmine
dothiepin
doxepin

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3
Q

List the relevant MOAi

A

phenelzine

tranylcypromine

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4
Q

List the relevant RIMAs

A

moclobemide

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5
Q

List the relevant SSRIs

A

fluoxetine
citalopram
escitalopram
fluvoxamine (can cause sedation)
paroxetine
sertraline (preferred in elderly)

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6
Q

List the relevant SNRIs

A

venlafaxine
desvenlafaxine
duloxetine

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7
Q

List the relevant NARIs

A

Reboxetine

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8
Q

Is there an antidepressant that is more effective than the rest?

A

all are approximately equal in efficacy

Individual patient response may vary markedly (consideration for switch)

Dont want to excessive 5HT (seizures)

SSRIs = regarded as 1st line, favourable risk-benefit ratio

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9
Q

Which antidepressants cause the most sedation and anticholinergic effects?

A

TCAs = amitriptyline, clomipramine, imipramine (but not as much as first two)

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10
Q

Discuss important considerations for antidepressant treatment

A

Treatment = start low dose, inc gradually over 2-4 wks as tolerated
Symptom improvement = 1-3 wks
Full effect = 6-8 wks

Cont Tx = 4-12 months after single episode of major depression (usually cont 4-9 months to prevent relapse)

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11
Q

What should be considered for treatment resistant depression?

A

Inadequate dosing
Inadequate durations
Patient non-compliance

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12
Q

List the indications for SNRIs

A

Depression, anxiety, panic attacks

OCD, PMDD, bulimia nervosa, PTSD

chronic pain syndrome = 5HT in spine > inhibit body brain signal transduction of pain

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13
Q

Discuss MOA of SSRIs

A

Selectively block neuronal reuptake of 5HT, lesser effect on reuptake of noradrenaline

Affects both central and peripheral 5HT receptors, requires adaptation to work

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14
Q

Discuss ADRs of SSRIs

A

Nausea, diarrhoea = dose dependent, activation of 5HT4 receptor > inc Ach > inc motility

Agitation = CNS excitation, Insomnia = H1-R stimulation, sedation = H1-R antagonism

drowsiness, tremor, dry mouth, dizziness, headache, sweating

Extrapyramidal reactions (tardive dyskinesia, dystonia)

Hyponatraemia (part of SIADH) = 5HT > inc ADH > vasopressin -R response > inc aquaporin > H20 from urine back in to blood

hyperprolactinaemia

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15
Q

Why is SSRI efficacy variable between people?

A

It is metabolised by CYP2D6 and CYP2C9 CYTp450 enzymes = very polymorphic

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16
Q

Discuss the MOA of TCAs

A

compete for binding site of amine transporters (NET and SERT) > block uptake of amines

Inhibit 5HT and NA reuptake (equally), lesser effect on DA

Also block = H1, M, alpha-1

17
Q

Discuss the ADRs of TCAs

A

H1 block = sedation, weight gain,
M1-R block = dry mouth, blurred vision, mydriasis, dec lacrimation, constipation, reduced GI motility, anticholinergic delirium, prolonged QT

Alpha-1 block = orthostatic hypotension, sinus tachycardia (M-block too), urinary hesitancy/retention

hyponatraemia, seizures, inc IOP = 5HT

gynaecomastia in males, galactorrhoea (inc prolactin?), breast enlargement

18
Q

Highlight important information about TCA toxicity

A

70-80% who overdose dont make it to hospital

Main effects = CNS (confusion, mania), heart (cardiac arrhythmia)

Initial effect = excitement, delirium, convulsions (sometimes), coma, resp depression (days)

Pronounced atropine-like effects = flushing, dry mouth/skin, mydriasis (pupil dilation), inhibition of gut and bladder

19
Q

Discuss the MOA of SNRIs

A

Inhibit NA, and 5HT reuptake

Does not block M, adrenergic, histamine receptors

20
Q

Common ADRs of SNRIs

A

M block = dry mouth, constipation, sweating, blurred vision, mydriasis

Alpha1 block = orthostatic hypotension

5HT = sexual dysfunction (impotence), dec libido, seizures, akathisia, hyperprolactinaemia

SIADH = hyponatraemia

21
Q

Discuss the MOA of mirtazepine

A

Tetracylic antidepress

Postsyn block of 5HT2-R and 5HT3-R, presynaptic blocker of central alpha2-adrenergic

Inhibition of alpha2 –> prevents alpha 2 mediated inhibition of NA release

potent H1 antagonist = sedative effect

22
Q

Discuss ADRs of mirtazepine

A

Common = inc appetite (H1), weight gain (H1), sedation (H1), peripheral oedema (alpha1B)

Rare = ortho hypotension (alpha1), seizure, mania, nightmares,

23
Q

What are you non-selective MOAi?

A

phenelzine

tranylcypromine

24
Q

What are your irreversible, long acting, non-selective MOAi?

A

phenelzine, tranylcypromine, isocarboxazid

25
Q

What are your short acting, reversible MOA-A selective; a RIMA

A

Moclobemide

It is a better option

26
Q

What do MAOi do?

A

Cause rapid, sustained inc in 5HT (most), noreadrenaline and dopamine (least)

27
Q

Discuss some ADRs of MOAI

A

A1 block = ortho hypotension
5HT = sleep dist (insomnia, hypersomnia), tremor, twitching, myoclonus, hyperreflexia, weight gain, mania, SIADH

Muscarinic block = dry mouth, constipation, blurred vision

NA/5HT = loss of libido, hypersomnia

28
Q

Discuss the cheese reaction

A

Commonly seen with MAOi = severe hypertensive response due to tyramine containing foods

Foods e.g. = cheeses, aged/cured/ pickled meats, overripe vegetables/bananas/raisins/figs

Reaction occurs up to 2 weeks after treatment is discontinued, also due to interactions with other amines

Due to MAOi, MAO is unable to breakdown amine tyromine > inc symp, inc serotinergic, inc dopaminergic

29
Q

Discuss serotonin toxicity and why it occurs

A

Occurs due to synaptic [serotonin] inc in CNS due to hyperstimulation of 5HT2A serotonin-R

Occurs with high dose of single drug, when >1 serotonergic agent used, or changing antidepressant with inadequate washout period

30
Q

What are the symptoms of serotonin toxicity?

A

Clonus, tremor, incoordination, hyperreflexia

mental state changes (confusion, hypomania, agitation)

shivering, sweating, fever

diarrhoea

Human Pharmacy (11 decks)

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