Antidepressants and antianxiety medication Flashcards by Bethan Williams

Most sedating SSRI

Paroxetine

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Reason for paroxetine’s sedating effect

High H1 affinity

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SSRI with the highest rate of discontinuation symptoms

Paroxetine

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SSRIs with the highest rates of drug interactions

Fluoxetine
Fluvoxamine
Paroxetine

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SSRI which causes the most short term anxiety and agitation

Fluoxetine

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SSRI which causes the most short term weight loss

Fluoxetine

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SSRI which has the least drug interactions

Citalopram

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SSRI which is most often used with elderly patients due to its lower risk of interactions

Citalopram

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SSRI which has the most evidence for safe use post-MI

Sertraline

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SSRI which is most often used for children and adolescents

Fluoxetine

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Most common side effect of SSRIs

GI side effects

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SSRI which causes the most GI upset

Fluvoxamine

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SSRIs which cause the least sexual dysfunction

Vortioxetine

Fluvoxamine

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SSRI which is the most anticholinergic

Paroxetine

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Medication which should be co-prescribed if a patient is taking an SSRI and NSAID

Protein pump inhibitor

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Drugs where SSRIs should be avoided where possible

NSAIDs
Warfarin
Aspirin
Triptans

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SSRI which does not need to be gradually reduced when stopping

Fluoxetine

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SSRI discontinuation symptoms

Restlessness
Insomnia, vivid dreams
Unsteadiness/dizziness
Sweating
GI symptoms - pain, cramps, diarrhoea, vomiting
Paraesthesia, shock-like symptoms
Flu-like symptoms
Crying spells

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Half life of citalopram

33 hours

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Half life of escitalopram

30 hours

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Half life of fluoxetine in early use

1-3 days

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Half life of fluoxetine with prolonged use

4-6 days

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Half life of fluvoxamine

17-22 hours

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Half life of paroxetine

22 hours

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Half life of sertraline

26 hours

Mechanism of action of MAOIs

Block the monoamine oxidase enzyme, which breaks down different neurotransmitters

Where MAO A is found

Placenta, gut, liver

Where MAO B is found

Brain, liver, platelets

Neurotransmitters MAO A breaks down

Serotonin, noradrenaline, dopamine, tyramine

Neurotransmitters MAO B breaks down

Phenylethylamine, methylhistamine, tryptamine, dopamine, tyramine

Types of MAOIs

Reversible or irreversible, selective for MOA A or MOA B, or non-selective

Irreversible and selective inhibitors of MAO B

Selegiline (no longer selective at high doses)

Reversible and selective inhibitor of MAO A

Meclobemide

Most common adverse effects

Dry mouth, nausea, diarrhoea, constipation, insomnia, dizziness/light-headedness

Cause of MAOI cheese reaction

Tyramine is a monoamine found in different foods which displaces noradrenaline from neurons, causing hypertension. When MAO doesn't break down tyramine it can build up and cause a hypertensive reaction

Foods to avoid due to risk of cheese reaction

``` Cheese (except cream cheese and cottage cheese) Broad beans Alcohol Banana peels Bean curd Sauerkraut Yeast extracts (e.g. marmite) ```

First generation TCAs (tertiary amines)

``` Amitriptyline Lofepramine Imipramine Dosulepin Doxepin Clomipramine ```

Second generation TCAs (secondary amines)

Nortriptyline Desipramine Amoxapine

Most dangerous TCAs in overdose

Amitriptyline | Dosulepin - possibly the most dangerous

Common side effects of TCAs

``` Drowsiness Dry mouth Blurred vision Constipation Urinary retention ```

Features of overdose of TCAs

``` Sedation/coma Seizures Hypertension (early) then hypotension Tachycardia Broad complex dysrhythmias Increased anticholinergic side effects ```

ECG features of TCA overdose

Increased QRS - >100ms in lead II Terminal R wave >3mm in aVR Sinus tachycardia

Specific treatments for overdose of TCAs

IV sodium bicarbonate Hyperventilation IV lidocaine Avoid 1a (procainamide) and 1c (flecainide) antiarrhythmics, beta-blockers and amiodarone

Drug interactions of TCAs

Cytochrome p450 inhibitors can lead to toxicity as TCAs are highly metabolised by cytochrome p450 Cytochrome p450 inducers can lead to treatment failure MAOIs - contraindicated with some TCAs due to serotonin syndrome like reactions QTc prolonging drugs

Mechanism of action of TCAs

Block the serotonin transporter and the noradrenaline transporter which leads to elevated synaptic concentrations of serotonin and noradrenaline Weak affinity for the dopamine transporter Antagonists of multiple receptors including 5-HT2 Inhibit sodium channels leading to their cardiotoxicity in overdose

Interaction of TCAs with warfarin

TCAs increase warfarin levels - high risk of bleeding

Interaction of TCAs with clonidine

TCAs decrease clonidine levels - risk of hypertension

Interaction of TCAs with MAOIs

Increase serotonin levels via synergistic serotonergic enhancement - increased risk serotonin syndrome like reaction Decrease tyramine entry - reduced risk cheese reaction

Interaction between TCAs and levodopa

Reduces absorption of levodopa and so lowers efficacy

Active metabolite of amitriptyline

Nortriptyline

Active metabolite of clomiprimine

Desmethyl-clomipramine

Active metabolite of dosulepin

Desmethyldosulepin

Active metabolite of doxepin

Desmethyldoxepin

Active metabolite of imipramine

Desipramine

Active metabolite of lofepramine

Desipramine

Active metabolite of fluoxetine

Norfluoxetine

Active metabolite of mirtazapine

Demethyl-mirtazapine

Active metabolite of trazadone and nefazodone

mCPP

Active metabolite of venlafaxine

O-desmethyl-venlafaxine

Start dose of citalopram for depression

10-20mg/day

Maximum citalopram dose for depression

40mg/day

Start dose of escitalopram for depression

5-10mg/day

Maximum escitalopram dose for depression

20mg/day

Start dose of sertraline for depression

50mg/day

Maximum sertraline dose for depression

200mg/day

Start dose of fluoxetine for depression

20mg/day

Maximum fluoxetine dose for depression

60mg/day

Start dose of paroxetine for depression

20mg/day

Maximum dose of paroxetine for depression

50mg/day

Start dose of vortioxetine for depression

5-10mg/day

Maximum vortioxetine dose for depression

20mg/day

Start dose of venlafaxine for depression

75mg/day in divided doses

Maximum venlafaxine dose for depression

375mg/day

Start dose of mirtazapine for depression

15mg/day

Maximum mirtazapine dose for depression

45mg/day

Start dose of moclobemide for depression

300mg/day in divided doses

Usual dose of moclobemide for depression

Up to 600mg/day

TCA discontinuation symptoms

Flu-like symptoms Insomnia Excessive dreaming

MAOI discontinuation symptoms

Agitation Ataxia and movement disorders Insomnia Vivid dreams

Discontinuation symptoms associated with agomelatine

Nil

Minimum effective dose of citalopram

20mg/day

Minimum effective dose of fluoxetine

20mg/day

Minimum effective dose of fluvoxamine

50mg/day

Minimum effective dose of paroxetine

20mg/day

Minimum effective dose of sertraline

50mg/day

Minimum effective dose of mirtazapine

30mg/day

Minimum effective dose of venlafaxine

75mg/day

Minimum effective dose of duloxetine

40-60mg/day

Minimum effective dose of agomelatine

25mg/day

Minimum effective dose of moclobemide

300mg/day

Minimum effective dose of trazadone

150mg/day

Starting dose of fluvoxamine

50-100mg/day

Maximum dose of fluvoxamine

300mg/day

Starting dose of agomelatine

25mg/day

Maximum dose of agomelatine

50mg/day

Starting dose of trazodone

150mg/day in divided doses

Maximum dose of trazodone

300mg/day generally | 600mg/day in hospital inpatients

Non selective MAO A and MAO B inhibitors (all irreversible)

Hydrazine Phenelzine Tranylcypromine Hydracarbazine

Antidepressant that can be given sublingually

Fluoxetine liquid

Antidepressants that can be given buccally

Selegiline | Amitriptyline

Antidepressants that can be given IV

``` Citalopram Escitalopram Mirtazapine Amitriptyline Clomipramine Ketamine ```

IM antipsychotic which has been shown to have antidepressant effects

Flupentixol

Antidepressant that can be given transdermally

Selegiline

Antidepressants that exist as suppositaries

Amitriptyline Clomipramine Imipramine Trazodone

TCA side effects

``` Antimuscarinic - dry mouth, urinary retention Weight gain Sedation Sexual dysfunction Cognitive impairment Arrhythmias Black hairy tongue Tremor Altered LFTs Paralytic ileus NMS ```

Active metabolite of sertraline

Desmethylsertraline

Dose at which antianxiety effects of trazadone appear compared to antidepressant effects

Antianxiety effects occur at lower doses

Number of times a day buspirone is given

Active metabolite of buspirone

1-pyrimidinylpiperazine

Impact of bupropion on seizures

Dose related risk of seizures | Worse with instant release preparations

Treatment combinations with good evidence for treatment resistant depression

SSRI or venlafaxine PLUS mirtazapine or mianserin

Treatment combination for treatment resistant depression known as 'California rocket fuel'

SNRI and mirtazapine

Enantiomers present in citalopram

R and S

Enantiomer present in escitalopram

Pure S enantiomer

Benefit to using escitalopram rather than citalopram

R enantiomer of citalopram has antihistaminic properties - using escitalopram removes these Citalopram has inconsistent therapeutic action due to the R enantiomer and dose often needs to be increased, but can't due to QTc prolongation - using escitalopram lower doses can often be used and there are no higher dose restrictions to avoid prolonging the QTc

Main clinical use for buspirone

Generalised anxiety disorder

Hormone given to treat depression

Thyroid hormone

TCA which is most preferable with elderly patients

Lofepramine

Age group who clear TCAs fastest

Children/adolescents

SSRI most selective for serotonin reuptake

Citalopram

SSRI with the longest half life

Fluoxetine

SSRI active metabolite with the longest half life

Norfluoxetine

Antidepressant which shows autoinduction

Paroxetine

Mechanism by which TCAs delay their own absorption

Anticholinergic effects

Time after stopping SSRI when discontinuation symptoms have usually started

By day 5

Discontinuation symptom specific to paroxetine

Suicidal ideation

SSRI which causes the most sexual dysfunction

Paroxetine

SSRI which causes the most weight gain

Paroxetine

First line antidepressant for patients with diabetes

Fluoxetine

Drugs to avoid with MAOIs

``` SSRIs SNRIs TCAs - clomipramine and imipramine only Opioids St John's Wort Triptans OTC cold medication - dextromethorphan and chlorpheniramine ```

SSRI which can be used to help prevent discontinuation symptoms from venlafaxine and clomipramine

Fluoxetine

TCA which shows the highest rates of anticholinergic side effects

Imipramine

Time frame to develop antidepressant related hyponatraemia

Usually within the first 30 days

Antidepressant which most improves sleep wake cycles in major depression

Agomelatine

Alternative name for dosulepin

Dothiepin

Most sedating tricyclics

Amitriptyline | Dothiepin

Effect on receptors of chronic administration of tricyclics

Causes down-regulation of beta-adrenergic receptors

TCA with the most stimulant effect

Desipramine

Medication of choice to treat a hypertensive crisis caused by combination of MAOI and tyramine containing food

Alpha adrenergic antagonist e.g. phentolamine, chlorpromazine

Antidepressants known for causing weight gain

TCAs | Mirtazapine

TCA with the highest antihistaminergic activity

Doxepin

SSRI which should be used with the most caution post-MI

Citalopram

Effect of bupropion on weight

Moderate sustained weight loss

Specific side effect of mianserin that requires regular monitoring

Bone marrow suppression

Side effect associated with venlafaxine and bupropion which can be helped by alpha and beta blockers

Sweating

Common side effects of MAOIs

``` Postural hypotension Insomnia Peripheral oedema Restlessness Nausea Dizziness Sexual dysfunction Sweating Tremor ```

Antidepressant associated with closed angle glaucoma

Paroxetine

Principle cause of death in TCA overdose

Cardiac arrhythmia

SSRI which is present to high concentrations in breast milk

Fluoxetine

Risk factors for antidepressant induced hyponatraemia

Old age Female sex Low BMI Concomitant use of diuretics

Antidepressant which can cause dependence

Tranylcypromine

Antidepressant which can directly influence gene transcription through nuclear receptors

Tri-iodothyronine

Medical condition where the use of MAOIs is contraindicated

Phaeochromocytoma

Antidepressant with good efficacy in patients with atypical depression

Phenelzine

Antidepressants least likely to precipitate mania in a patient with bipolar disorder

Bupropion | Sertraline

Blood test required before starting agomelatine

LFTs

Timing of LFTs required in patients taking agomelatine

Baseline | 3, 6, 12, and 24 weeks after starting treatment

Antidepressants to consider in patients who have developed antidepressant related hyponatraemia

Nortriptyline Lofepramine MAOIs

Likely mechanism of action of SSRI discontinuation syndrome

Temporary deficiency in the brain of one or more essential neurotransmitters associated with mood

Antidepressants known as dual action antidepressants

Venlafaxine | Duloxetine

Impact of smoking on duloxetine plasma levels

Reduced by up to 50%

Mechanism behind the increased risk of bleeding with SSRIs

SSRIs inhibit the serotonin transporter which is responsible for the uptake of serotonin into platelets Depleted platelet serotonin leads to inability to form clots SSRIs increase gastric acid secretion which acts as an irritant to the gastric mucosa, increasing the risk of GI bleeding

Antidepressant most associated with waves of withdrawal symptoms

Venlafaxine

SSRI with the shortest half life

Fluvoxamine

Most serotonergic TCA

Clomipramine

Reversible inhibitor of MAO that does not react with tyramine

Moclobemide

Antidepressant treatment combination known as California rocket fuel for its effects in treatment resistant depression

Mirtazapine and venlafaxine

Antidepressant suggested for patients with hyponatraemia

Agomelatine

Mechanism of action of the delayed onset part of antidepressant medication action

Down regulation of HT1A autoreceptors in the post-synaptic neurons

Antidepressant classes which cause an increased risk of postpartum haemorrhage

All classes

Antidepressant causing the least sexual dysfunction

Agomelatine

Time to wait after stopping a MAOI before starting another antidepressant (particularly an SSRI)

2 weeks

Least sedating TCAs

Imipramine Lofepramine Nortriptyline

Main side effects of buspirone

``` Dizziness Headache Excitement Nausea Dry mouth ```

Most notable side effect of ketamine

Dissociation

TCA which causes the most weight gain

Doxepin

Antidepressant associated with raised cholesterol levels

Mirtazapine

Antidepressant discontinued due to risk of severe liver damage

Nefazodone

Antidepressants least influenced by pharmacokinetic factors

MAOIs

Antidepressants and antianxiety medication Flashcards

(179 cards)