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24 Antidepressant drugs Flashcards

(45 cards)

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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 or fluvoxamine 18-24h, escitalopram or 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

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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

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A

depression
panic disorder

21
Q

24.04 NORADRENALINE REUPTAKE INHIBITOR

Reboxetine, maprotiline - adverse effects

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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

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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

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A

antidepressant

24
Q

24.05 MONOAMINE OXIDASE INHIBITORS

Phenelzine, isocarboxazid, moclobemide - MOA

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A

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

25
24.05 MONOAMINE OXIDASE INHIBITORS Phenelzine, isocarboxazid, moclobemide - abs/distrib/elim
given orally half-lives: phenelzine 1-2h (but action lasts much longer because of irreversible inhibition of MAO), moclobemide 1-2h
26
24.05 MONOAMINE OXIDASE INHIBITORS Phenelzine, isocarboxazid, moclobemide - clinical use
depression, may have particular value for atypical depression social phobia clinical effect takes some days to develop
27
24.05 MONOAMINE OXIDASE INHIBITORS Phenelzine, isocarboxazid, moclobemide - adverse effects
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
24.05 MONOAMINE OXIDASE INHIBITORS Phenelzine, isocarboxazid, moclobemide - special points
adverse effects are more frequent than with TCAs or SSRIs, so MAOIs are less commonly used in depression
29
24.06 α-ADRENOCEPTOR & 5-HT RECEPTOR ANTAGONIST Mirtazapine - actions
antidepressant
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24.06 α-ADRENOCEPTOR & 5-HT RECEPTOR ANTAGONIST Mirtazapine - MOA
antagonist at presynaptic α2 adrenoceptors - prevents the inhibitory effect of noradrenaline on 5-HT and perhaps also on noradrenaline release from CNS neurons, thus enhances MA transmission 5-HT2 and 5-HT3 receptor antagonism may help reduce side effects due to potentiation of serotonergic transmission (e.g. the sexual dysfunction and nausea produced by uptake inhibitors)
31
24.06 α-ADRENOCEPTOR & 5-HT RECEPTOR ANTAGONIST Mirtazapine - abs/distrib/elim
given orally subject to hepatic P450 metabolism half-life 30h longer in the elderly and those with liver/renal impairment
32
24.06 α-ADRENOCEPTOR & 5-HT RECEPTOR ANTAGONIST Mirtazapine - clinical use
major depression post-traumatic stress disorder
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24.06 α-ADRENOCEPTOR & 5-HT RECEPTOR ANTAGONIST Mirtazapine - adverse effects
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
24.07 DOPAMINE REUPTAKE INHIBITOR Bupropion - actions
‘atypical’ antidepressant elevates mood
35
24.07 DOPAMINE REUPTAKE INHIBITOR Bupropion - MOA
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
24.07 DOPAMINE REUPTAKE INHIBITOR Bupropion - abs/distrib/elim
given orally extensive hepatic P450 metabolism yields active metabolites that contribute to antidepressant action half-life 20h
37
24.07 DOPAMINE REUPTAKE INHIBITOR Bupropion - clinical use
alone or in combination with SSRIs for major depression also used to help with smoking cessation clinical effects take some weeks to develop
38
24.07 DOPAMINE REUPTAKE INHIBITOR Bupropion - adverse effects
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
24.08 DRUGS FOR BIPOLAR DISORDER Lithium: group 1 metallic element - actions
mood ‘stabiliser’
40
24.08 DRUGS FOR BIPOLAR DISORDER Lithium: group 1 metallic element - MOA
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
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24.08 DRUGS FOR BIPOLAR DISORDER Lithium: group 1 metallic element - abs/distrib/elim
given orally uptake of lithium into cells leads to accumulation in the body over a period of 2 weeks
42
24.08 DRUGS FOR BIPOLAR DISORDER Lithium: group 1 metallic element - clinical use
bipolar disorder, mania, adjunct to other agents in unipolar depression clinical effect develops over 3-4 weeks
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24.08 DRUGS FOR BIPOLAR DISORDER Lithium: group 1 metallic element - adverse effects
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)
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24.08 DRUGS FOR BIPOLAR DISORDER Lithium: group 1 metallic element - special points
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
24.08 OTHER DRUGS FOR BIPOLAR DISORDER
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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