Psychopharmacology Flashcards
Amisulpride - class
- Benzamide
Aripiprazole - class
- Arylpiperidylindole
Asenapine
- Acute mania in bipolar I, sublingual
- High affinity for 5-HT, alpha-adrenoreceptors, D1-4 and H1/H2.
- Less efficacious than risperidone or olanzapine
- Higher EPSEs than most atypicals, unlikely to raise prolactin, less weight gain
Clozapine - class
- Dibenzodiazepine
Lurasidone - mechanism and side effects
- Antagonist at alpha-receptors, D1/2 and 5-HT
- EPSEs likely, less weight gain and QTc
Olanzapine - class and mechanism
- Thienobenzadiazepine
- Broad receptor antagonism
Paliperidone
- Main hepatic metabolite of risperidone, lower bioavailability (twice dose)
- Useful in hepatic failure, renally excreted
- Higher EPSEs and prolactin; mod weight gain, no QTc changes.
Quetiapine - class and mechanism
- Dibenzothiazepine
- Broad receptor antagonism
Risperidone - class
- Benzoxazole
Sertindole - side effects
- Strict ECG monitoring due to QTc prolongation
- Nasal congestion, decreased ejaculatory volume, postural hypotension
- Occasionally raised LFTs
Thioridizine - class
- Piperidine
Trifluoperazine - class
- Piperizine
Haloperidol - class
- Butyrophenone
Flupenthixol - class and use
- Thioxanthene
- Depressed patients
Chlorpromazine - class
- Aliphatic phenothiazine
Bupropion - mechanism
Norepinephrine-dopamine re-uptake inhibitor and nicotinic acetylcholine receptor antagonist
SSRIs - metabolism and side effects
- Hepatically metabolised
- GI upset, sedation, dizziness, sexual dysfunction, SIADH, bleeding (platelets), convulsions, agitation
Venlafaxine - mechanism and side-effects
- 5-HT and NARI
- Hypertension, seizures, dry mouth, urinary retention, sweating
Trazodone - mechanism
- Weak 5-HT reuptake inhibition
- 5-HT2 antagonist, therefore lower sexual dysfunction than SSRIs
Modafinil
Psychostimulant used in narcolepsy, obstructive sleep apnoea, chronic shift work, adjunct in depression
Similar to amphetamines, but without dependence or tendency to precipitate psychosis
Mirtazapine - mechanism
- Alpha adrenergic, 5-HT and H1 antagonist
TCAs - mechanism and metabolism
- 5-HT reuptake inhibition and/or NA reuptake inhibition
- Hepatically metabolised
- alcohol potentiates
Moclobemide
Reversible MAOI with short half-life
Contraindications to MAOIs
Cardiovascular or cerebrovascular disease Phaeochromocytoma Hyperthyroidism Hepatic disease Delirium
Side-effects of MAOIs
peripheral oedema, postural hypotension, nausea, sweating, tremor, insomnia
Causes of hypertensive crisis with MAOIs
Tyramine containing foods and phenylephrine
Treated with phentolamine, phenoxybenzamine or chlorpromazine
Side-effects of TCAs
Anticholinergic - dry mouth, blurred vision, constipation, retention
Antihistaminergic - sedation, weight gain
Alpha-adrenoceptor - postural hypotension
Cardiotoxicity - QTc, arrhythmias, ST-elevation
Neurotoxicity - delirium, movement disorders, seizures, coma
Mirtazapine - side-effcts
sedation, weight gain, abnormal dreams and blood dyscrasia
Trazodone - side-effects
GI upset, sedation, hypotension, priapism
Agomelatine - mechanism and monitoring
- Agonist at melatonin MT receptors
- Antagonist at 5-HT2C receptors
- LFT monitoring required
Symptoms of antidepressant discontinuation syndrome
sleep disturbance, increased dreams, GI disturbance, mood disturbance, EPSE, lethargy, headache
Symptoms of serotonin syndrome
confusion, myoclonic jerks, hyperreflexia, pyrexia, sweating, autonomic instability, GI symptoms, mood changes
Steady state of Lithium
5-7 days
Consider bipolar maintenance treatment after…
2 illnesses in 2 years or
3 illnesses in 5 years or
1 severe illness
Lithium drug interactions
NSAIDs
Diuretics
ACE inhibitors
Serotonin receptor that is ligand gated
5-HT3
Serotonin receptors associated with nausea
5-HT3
Serotonin receptors associated with circadian rhythms
5-HT7
Serotonin receptor associated with insomnia, agitation and sexual dysfunction
5-HT2
Pregabalin
GABA analogue
High affinity for calcium channels
Eliminated unchanged by kidneys
Buspirone
5-HT1A Partial agonist
Short half life
Nausea, headache, dizziness, akithisia
Disulfiram
Bonds irreversibly to acetaldehyde dehydrogenase
Clozapine - efficacy
- Reduces positive SCZ Sx in 60% of resistant SCZ
Clozapine - side effects
- Sedation, postural hypotension, agranulocytosis, seizures, myocarditis, cardiomyopathy, hypersalivation
Clozapine - interactions
- Avoid carbamazepine, chloramphenicol,cytotoxics, benzodiazepines, depot antipsychotics
- SSRIs and valproate may increase levels
Amisulpride - mechanism
- Selective D2/D3 antagonism
- 5-HT7 antagonism
Amisulpride - side effects
- Low EPSE and weight gain
- prolactinaemia at higher doses
Aripiprazole - mechanism
- High affinity D2 partial agonist
- High affinity 5-HT2A
Aripiprazole - side effects
- Low EPSE at all doses
- may decrease prolactin
- less weight gain than other antipsychotics
- no QTc changes
Olanzapine - pharmacokinetics and adverse effects
- Levels reduced by smoking
- Higher plasma levels in women for same dose
- Low EPSEs and prolactin; high sedation, weight gain, antimuscarinc SEs, glucose dysregulation.
Quetiapine - metabolite and side effects
- Key metabolite (norquetiapine) is NARI
- Low EPSEs and prolactin; high dizziness, sedation, constipation
Risperidone - mechanism
- 5-HT2A/D2 antagonism
Risperidone - side effects
- Less DI Parkinsonism than typicals
- Tachycardia, weight gain, hyperprolactinaemia
SSRI with lowest risk of interactions
Citalopram
SSRIs (2) with highest risk of interactions
Fluoxetine and paroxetine
Causes of tachycardia
Clozapine TCAs MAOIs Antiparkinsonian Antipsychotics (generally the older ones)
Causes of Torsades
Haloperidol
Thioridazine
Mesoridazine
Chlorpromazine
Causes of bradycardia
SSRIs
Lithium
Cholinesterase inhibitors
Causes of heart block
TCAs
Causes of ST segment changes
Thioridazine
Chlorpromazine
Secondary amines
Desipramine
Nortriptyline
Protriptyline
Amoxapine
Zopiclone - class
cyclopyrrolone
Zopiclone - contraindications
unstable myasthenia gravis, respiratory failure, severe sleep apnoea syndrome, breastfeeding
Least likely to cause hyponatraemia
MAOIs, agomelatine
Antidepressants licensed in nocturnal enuresis (children)
Amitriptyline, Imipramine, Nortriptyline
Antidepressant licensed for phobias
Clomipramine
Antidepressant licensed for cataplexy
Clomipramine
Antidepressants licensed for panic disorder and agoraphobia
Citalopram, Escitalopram, Sertraline, Paroxetine, Venlafaxine
Antidepressants licensed for social anxiety
Escitalopram, Paroxetine, Sertraline, Moclobemide, Venlafaxine
Antidepressants licensed for general anxiety
Escitalopram, Paroxetine, Duloxetine, Venlafaxine
Antidepressants licensed for OCD
Escitalopram, Fluoxetine, Fluvoxamine, Paroxetine, Sertraline
Antidepressant licensed for bulimia
Fluoxetine
Antidepressant licensed for PTSD
Paroxetine, Sertraline
Antipsychotics least likely to cause hyperprolactinaemia
Clozapine Aripiprazole Quetiapine Olanzapine Ziprasidone