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Pharmacology > 24 Antidepressant drugs > Flashcards

24 Antidepressant drugs Flashcards

1
Q

24.01 TRICYCLICS

Amitriptyline, imipramine, desipramine, clomipramine, nortriptyline - actions

A

antidepressant

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2
Q

24.01 TRICYCLICS

Amitriptyline, imipramine, desipramine, clomipramine, nortriptyline - MOA

A

inhibits reuptake of noradrenaline into noradrenergic neurons and 5-HT into serotonergic neurons, so potentiating transmitter action
the clinical effects are not seen for a few weeks, meaning that longer-term changes (e.g. down-regulation of receptors) are required

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3
Q

24.01 TRICYCLICS

Amitriptyline, imipramine, desipramine, clomipramine, nortriptyline - abs/distrib/elim

A

given orally
metabolised in liver by cytochrome P450 system with subsequent conjugation reactions
plasma half-life of amitriptyline 12-24h (influenced by P450 inhibitors or inducers)
strong protein binding

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4
Q

24.01 TRICYCLICS

Amitriptyline, imipramine, desipramine, clomipramine, nortriptyline - clinical use

A

depression
panic disorder
neuropathic pain
enuresis

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5
Q

24.01 TRICYCLICS

Amitriptyline, imipramine, desipramine, clomipramine, nortriptyline - adverse effects

A

sedation (antihistamine action, less with nortriptyline and desipramine)
blurred vision, dry mouth, constipation, urinary retention (antimuscarinic action)
postural hypotension (α1-adrenoceptor antagonism)
overdose potentially fatal due to cardiac dysrhythmia, severe hypotension, seizure and CNS depression
not given with MAOIs

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6
Q

24.02 SSRIs

Fluoxetine, paroxetine, citalopram, escitalopram, sertraline, fluvoxamine - actions

A

antidepressant

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7
Q

24.02 SSRIs

Fluoxetine, paroxetine, citalopram, escitalopram, sertraline, fluvoxamine - MOA

A

inhibits the reuptake of 5-HT into serotonergic neurons, so potentiating transmitter action
the clinical effects are not seen for a few weeks, meaning that longer-term changes (e.g. down-regulation of receptors) are required
less marked antimuscarinic and antihistaminergic actions than TCAs

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8
Q

24.02 SSRIs

Fluoxetine, paroxetine, citalopram, escitalopram, sertraline, fluvoxamine - abs/distrib/elim

A

given orally
brain concentration rises over a few days
hepatic P450 metabolism followed by conjugation reactions
half-lives: fluoxetine 1-3 days (has a longer-lasting active metabolite), paroxetine/fluvoxamine 18-24h, escitalopram/sertraline 24-36h
strongly bound

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9
Q

24.02 SSRIs

Fluoxetine, paroxetine, citalopram, escitalopram, sertraline, fluvoxamine - clinical use

A

widely prescribed
depression
obsessive-compulsive disorder
panic disorder
bulimia nervosa

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10
Q

24.02 SSRIs

Fluoxetine, paroxetine, citalopram, escitalopram, sertraline, fluvoxamine - adverse effects

A

anxiety and insomnia
can cause nausea, diarrhoea and headache
sexual dysfunction
increased risk of suicide in young patients
not prescribed with MAOIs due to risk of serotonin syndrome
hypo­natraemia in elderly
overdose toxicity much less than for TCAs

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11
Q

24.02 SSRIs

Fluoxetine, paroxetine, citalopram, escitalopram, sertraline, fluvoxamine - special points

A

escitalopram is the active enantiomer of citalopram
sertraline and escitalopram are the SSRIs that are most selective for 5-HT uptake inhibition

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12
Q

24.03 SNRIs

Venlafaxine, duloxetine, desvenlafaxine - actions

A

antidepressant

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13
Q

24.03 SNRIs

Venlafaxine, duloxetine, desvenlafaxine - MOA

A

inhibits the reuptake of noradrenaline into noradrenergic neurons and 5-HT into serotonergic neurons, so potentiating transmitter action
the clinical effects are not seen for a few weeks
no important effects on histamine, muscarinic or adrenergic receptors

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14
Q

24.03 SNRIs

Venlafaxine, duloxetine, desvenlafaxine - abs/distrib/elim

A

given orally
metabolised in liver by cytochrome P450 system
half-lives: venlafaxine 5h (active metabolite - desmethylvenlafaxine 11h), duloxetine 12-24h

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15
Q

24.03 SNRIs

Venlafaxine, duloxetine, desvenlafaxine - clinical use

A

depression (reported to be effective in cases resistant to SSRIs)
panic disorder
generalised anxiety disorder
social phobia

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16
Q

24.03 SNRIs

Venlafaxine, duloxetine, desvenlafaxine - adverse effects

A

nausea, headache, sleep problems, sexual dysfunction
increased risk of suicide in young patients
not given with MAOIs due to risk of serotonin syndrome
overdose causes CNS depression, seizures, cardiac dysrhythmias

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17
Q

24.04 NORADRENALINE REUPTAKE INHIBITOR

Reboxetine, maprotiline - actions

A

antidepressant

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18
Q

24.04 NORADRENALINE REUPTAKE INHIBITOR

Reboxetine, maprotiline - MOA

A

selectively inhibits the reuptake of noradrenaline into noradrenergic neurons (no effect on 5-HT and dopamine transmission)
the clinical effects are not seen for a few weeks, meaning that longer-term changes (e.g. down-regulation of receptors) are required

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19
Q

24.04 NORADRENALINE REUPTAKE INHIBITOR

Reboxetine, maprotiline - abs/distrib/elim

A

given orally
metabolised in liver by cytochrome P450 system
plasma half-life of reboxetine 15h (influenced by P450 inhibitors or inducers)

20
Q

24.04 NORADRENALINE REUPTAKE INHIBITOR

Reboxetine, maprotiline - clinical use

A

depression
panic disorder

21
Q

24.04 NORADRENALINE REUPTAKE INHIBITOR

Reboxetine, maprotiline - adverse effects

A

reboxetine: insomnia, headache, effects due to antagonism of muscarinic and histamine receptors (e.g. sweating, dry mouth, constipation)
maprotiline has similar side effects to TCAs, consistent with block of receptors
not given with MAOIs

22
Q

24.04 NORADRENALINE REUPTAKE INHIBITOR

Reboxetine, maprotiline - special notes

A

patients with a history of suicide-related events, or those exhibiting a significant suicidal ideation prior to treatment, are known to be at greater risk of suicidal thoughts or suicide attempts on these drugs, and should receive careful monitoring during treatment

23
Q

24.05 MONOAMINE OXIDASE INHIBITORS

Phenelzine, isocarboxazid, moclobemide - actions

A

antidepressant

24
Q

24.05 MONOAMINE OXIDASE INHIBITORS

Phenelzine, isocarboxazid, moclobemide - MOA

A

phenelzine and isocarboxacid irreversibly inhibit both the A and B forms of monoamine oxidase
MAO is found in nerve endings, MAO-A acting preferentially on noradrenaline and 5-HT and MAO-B acting mainly on dopamine
MAO inhibition increases the amount of transmitter in the nerve ending
antidepressant action is due to MAO-A inhibition
moclobemide is a selective, reversible inhibitor of MAO-A
MAO-B inhibitors are used for Parkinson’s disease

25
Q

24.05 MONOAMINE OXIDASE INHIBITORS

Phenelzine, isocarboxazid, moclobemide - abs/distrib/elim

A

given orally
half-lives: phenelzine 1-2h (but action lasts much longer because of irreversible inhibition of MAO), moclobemide 1-2h

26
Q

24.05 MONOAMINE OXIDASE INHIBITORS

Phenelzine, isocarboxazid, moclobemide - clinical use

A

depression, may have particular value for atypical depression
social phobia
clinical effect takes some days to develop

27
Q

24.05 MONOAMINE OXIDASE INHIBITORS

Phenelzine, isocarboxazid, moclobemide - adverse effects

A

postural hypotension
headache, insomnia, sexual dysfunction
dry mouth, urinary retention
convulsions with overdose
increased risk of suicide in young patients
cheese reaction with dietary tyramine - hypertensive crisis
cheese reaction is less pronounced with moclobemide (since MAO-B is still functional)

28
Q

24.05 MONOAMINE OXIDASE INHIBITORS

Phenelzine, isocarboxazid, moclobemide - special points

A

adverse effects are more frequent than with TCAs or SSRIs, so MAOIs are less commonly used in depression

29
Q

24.06 α-ADRENOCEPTOR & 5-HT RECEPTOR ANTAGONIST

Mirtazapine - actions

A

antidepressant

30
Q

24.06 α-ADRENOCEPTOR & 5-HT RECEPTOR ANTAGONIST

Mirtazapine - MOA

A

antagonist at presynaptic α2 adrenoceptors, so preventing the inhibitory effect of noradrenaline on 5-HT and perhaps also on noradrenaline release from CNS neurons, thus enhancing monoaminergic transmission
5-HT2 and 5-HT3 receptor antagonism may be beneficial in reducing side effects due to potentiation of serotonergic transmission (e.g. the sexual dysfunction and nausea produced by uptake inhibitors)

31
Q

24.06 α-ADRENOCEPTOR & 5-HT RECEPTOR ANTAGONIST

Mirtazapine - abs/distrib/elim

A

given orally
subject to hepatic P450 metabolism
half-life 30h
longer in the elderly and those with liver/renal impairment

32
Q

24.06 α-ADRENOCEPTOR & 5-HT RECEPTOR ANTAGONIST

Mirtazapine - clinical use

A

major depression
post-traumatic stress disorder

33
Q

24.06 α-ADRENOCEPTOR & 5-HT RECEPTOR ANTAGONIST

Mirtazapine - adverse effects

A

devoid of many side effects associated with muscarinic or adrenoceptor block, but does have antihistamine actions, e.g. sedation (useful if insomnia accompanies depression)
increased appetite and weight gain
agranulocytosis is rare but serious

34
Q

24.07 DOPAMINE REUPTAKE INHIBITOR

Bupropion - actions

A

‘atypical’ antidepressant
elevates mood

35
Q

24.07 DOPAMINE REUPTAKE INHIBITOR

Bupropion - MOA

A

relatively selective inhibitor of neuronal dopamine reuptake, with a lesser effect on noradrenaline and little effect on 5-HT uptake
also antagonist at neuronal nicotinic receptors

36
Q

24.07 DOPAMINE REUPTAKE INHIBITOR

Bupropion - abs/distrib/elim

A

given orally
extensive hepatic metabolism by cytochrome P450 yields active metabolites that contribute to antidepressant action
half-life 20h

37
Q

24.07 DOPAMINE REUPTAKE INHIBITOR

Bupropion - clinical use

A

alone or in combination with SSRIs for major depression
also used to help people give up tobacco smoking
clinical effects take some weeks to develop

38
Q

24.07 DOPAMINE REUPTAKE INHIBITOR

Bupropion - adverse effects

A

agitation, tremor, dry mouth, nausea, insomnia, skin rashes
it does not cause the weight gain or sexual dysfunction common with other antidepressants
seizures may be induced with larger doses

39
Q

24.08 DRUGS FOR BIPOLAR DISORDER

Lithium: group 1 metallic element - actions

A

mood ‘stabiliser’

40
Q

24.08 DRUGS FOR BIPOLAR DISORDER

Lithium: group 1 metallic element - MOA

A

MOA not well established
being a group 1 element like Na+ and K+, one proposal is that Li+ interferes with membrane ion transport, perhaps including neurotransmitter reuptake
actions on phosphatidyl inositol metabolism and on glycogen synthase kinase are other possible mechanisms

41
Q

24.08 DRUGS FOR BIPOLAR DISORDER

Lithium: group 1 metallic element - abs/distrib/elim

A

given orally
uptake of lithium into cells leads to accumulation in the body over a period of 2 weeks

42
Q

24.08 DRUGS FOR BIPOLAR DISORDER

Lithium: group 1 metallic element - clinical use

A

bipolar disorder, mania, adjunct to other agents in unipolar depression
clinical effect develops over 3-4 weeks

43
Q

24.08 DRUGS FOR BIPOLAR DISORDER

Lithium: group 1 metallic element - adverse effects

A

diarrhoea, tremor, confusion
renal toxicity, including nephrogenic diabetes insipidus - dehydration
depresses thyroid function
overdose results in convulsions, coma and death
many drug interactions (e.g. with diuretics)

44
Q

24.08 DRUGS FOR BIPOLAR DISORDER

Lithium: group 1 metallic element - special points

A

because of a low therapeutic index, it is essential to measure the serum Li+ concentration to ensure an effective therapeutic concentration with minimal toxicity

45
Q

24.08 OTHER DRUGS FOR BIPOLAR DISORDER

A

antiepileptic drugs: carbamazepine, valproate, lamotrigine
antipsychotics: olanzapine, risperidone, quetiapine, aripiprazole, brexipiprazole, cariprazine
melatonin receptor agonists: agomelatine
NMDA receptor channel blocker: ketamine

Pharmacology (34 decks)

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