Psychotropics Flashcards
Clozapine
Psychosis - Atypical Agent
Binds dopaminergic, serotonergic, muscarinic and histaminic receptors
*Strice monitoring via specialist clinic required
Risperidone
Psychosis - Atypical Agent
D2 and 6-HT antagonist
EPSE (extra pyramidal side-effects) only at very high dosages
Quetiapine
Psychosis - Atypical Agent
Effective at high dosages
- Sedating
- Weight gain ++
- Best choice in pregnancy
Olanzapine
Psychosis - Atypical Agent
Efective
Sedating
Weight gain +++
Aripiprazole
Psychosis - Atypical Agent
High D2 receptor affinity: partial dopamine agonst
(shows agonist activity in areas of low neurotransmitter activity, and slight antagonistic activity in areas where there is over-expression of neurotransmitter)
Generally well tolerated
Ziprasidone, Asenapine, Amisulpride
Psychosis - Atypical Agents
What are EPSEs?
Extra-pyrimidal side-effects
Movement disorders caused by dopamine antagonists
Includes akasthisia (inability to still movements) and akinesia (inability to initiate movement)
What is a partial dopamine agonist, and why is it an attractive option in schizophrenia?
Aripiprazole (psychosis; atypical agent)
High affinity for D2 receptors
Shows agonist activity in areas low in neurotransmitter, and antagonistic activity in areas of high neurotransmitter levels
Attractive option for schizophrenia because: acts as functional antagonist in MESOLIMBIC PATHWAY where excessive dopamine activity is thought to create POSITIVE SYMPTOMS; acts as a functional agonist in MESOCORTICAL PATHWAY where reduced dopamine activity is thoguht to produce NEGATIVE SYMPTOMS and cognitive impairment
Fluphenazine
Psychosis - Typical Agent - PHENOTHIZINES
D2 antagonist in MESOLIMBIC, NIGROSTRIATAL & TUBERINFUNDIBULAR SYSTEMS,
EPSEs are verry common, thus overall not commonly used
Trifluoperazine
Psychosis - Typical Agent - PHENOTHYZINES
D2 antagonist in MESOLIMBIC, NIGROSTRIATAL & TUBERINFUNDIBULAR SYSTEMS
EPSEs are verry common, thus overall not commonly used
Pericyazine
Psychosis - Typical Agent - PHENOTHYZINES
D2 antagonist in MESOLIMBIC, NIGROSTRIATAL & TUBERINFUNDIBULAR
SYSTEMS
EPSEs very common; thus not commonly used now
Prochloroperazine
Psychosis - Typical Agent - PHENOTHIZINES
D2 antagonist at MESOLIMBIC, NIGROSTRIATAL & TUBERINFUNDIBULAR SYSTEMS
EPSEs very common; thus not commonly used now
Haloperidol & Droperidol
More commonly used for acute delirium
Uncommonly used for psychosis - Atypical Agent - BUTYRPHENONE DERIVATIVES
Increases turnover of dopamine
High affinity, slow dissociation binding to D2 and Alpha 1 receptors a low doses; 5-HT receptors at high dosages
More effective at treating positive symptoms of schizophrenia
High EPSEs
Sertraline
SSRI - Depression
One of most effective (preferred equally to Escitalopram)
First line in MDE
Block reuptake of serotonin by binding and inhibiting serotonin transporters at the synaptic cleft, resulting in increased serotonin levels and 5-HT stimulation
Start low and titrate up
Short term side-effects: GI upset, agitation
Long-term: Insomnia, sexual function impairments, sidcontinuation syndrome where feel awful
Escitalopram
SSRI - Depression
First line for MDE
Preferred equally with sertraline
Binds and inhibits serononin transporters in synaptic cleft, resulting in higher levels of serotinin and consequently increased 5-HT stimulation
Start low and titrate up
Short-term side effects: GI upset, agitation
Longer-term side effects: Insomnia, sexual function impairments, discontinuation syndromes
Citalopram
SSRI - Depression
SSRIs are first-line for MDE
Binds and inhibits serotonin transporters, inhibiting serotonin reuptake. Thus increases serotonin in synaptic cleft and consequently increases 5-HT stimulation
Fluoxetine
SSRI - Depression
SSRIs are first line for MDE
Binds and inhibits serotonin transporters, inhibiting serotonin reuptake from synaptic cleft. Thus, more serotonin is available, resulting in increased 5-HT stumulation
Paroxetine
SSRI - Depression
*Not as well tolerated as many other SSRIs. Older drug.
SSRIs are first-line for MDE
Binds and inhibits serotonin transporters, inhibiting serotonin reuptake from synaptic cleft. Thus, more serotonin available, resulting in increased 5-HT stimulation
Fluvoxamine
SSRI - Depression
SSRIs are first-line for MDE
Binds and inhibits serotonin transporters in synaptic cleft, resulting in higher levels of available serotonin for greater 5-HT stimulation
General side effects of SSRIs
Short term: Mild GI upset, agitation
Longer-term: Insomnia, sexual dysfunction, discontinuation syndrome
Imipramine
Tricyclic antidepressant - Depression
TCAs inhibit reuptake of NA and serotonin at synaptic cleft, leaving higher concentrations of both these neurotransmitters
TCAs have high levels of drug interactions, and renal/liver issues
Side effects include: Toxic in overdose, prolonged QT, anti-cholinergic (increases SNS activity) side effects
Trimipramine
Tricyclic Antidepressant - Depression
TCAs inhibit reuptake of NA and serotonin at synaptic cleft, leaving higher concentrations of both these neurotransmitters
TCAs have high levels of drug interactions, and renal/liver issues
Side effects include: Toxic in overdose, prolonged QT, anti-cholinergic (increases SNS activity) side effects
Mortriptyline
Tricyclic Antidepressant - Depression
TCAs inhibit reuptake of NA and serotonin at synaptic cleft, leaving higher concentrations of both these neurotransmitters
TCAs have high levels of drug interactions, and renal/liver issues
Side effects include: Toxic in overdose, prolonged QT, anti-cholinergic (increases SNS activity) side effects
Dothiepin
Tricyclic Antidepressant - Depression
TCAs inhibit reuptake of NA and serotonin at synaptic cleft, leaving higher concentrations of both these neurotransmitters
TCAs have high levels of drug interactions, and renal/liver issues
Side effects include: Toxic in overdose, prolonged QT, anti-cholinergic (increases SNS activity) side effects
Doxepine
Tricyclic Antidepressant - Depression
TCAs inhibit reuptake of NA and serotonin at synaptic cleft, leaving higher concentrations of both these neurotransmitters
TCAs have high levels of drug interactions, and renal/liver issues
Side effects include: Toxic in overdose, prolonged QT, anti-cholinergic (increases SNS activity) side effects
Amitriptyline (endep)
Tricyclic Antidepressant - Depression
TCAs inhibit reuptake of NA and serotonin at synaptic cleft, leaving higher concentrations of both these neurotransmitters
TCAs have high levels of drug interactions, and renal/liver issues
Side effects include: Toxic in overdose, prolonged QT, anti-cholinergic (increases SNS activity) side effects
MAOIs =?
Mono-amine oxidase inhibitors
Inhibit activity of mono-amine oxidase, inhibiting break-down of monoamine neurotransmitters
(serotonin, melatonin, epinephrine, norepinephrine, dopamine)
Increases levels of these monoamines, and improves mood, but many adverse effects -> best left to specialists
Phenylzine
MAOI: Non-selective MAOI-A/MAOI-B inhibitor
Depression
Improves mood and increases monoamines
Best prescribed by specialists due to extreme and many adverse effects
Inhibits monoamine oxidase to prevent break-down of monoamine neurotransmitters: serotonin, dopamine, epinephrine, norepinephrine, melatonin
Tranylcypromine
MAOI: Non-selective MAOI-A/MAOI-B inhibitor
Depression
Improves mood and increases monoamines
Best presribed by specialists due to many and extreme side-effects
Inhibits monoamine oxidase to prevent breakdown of monoamine neurotransmitters: serotonin, dopamine, melatonin, epinephrine, norepinephrine
SNRIs = ?
Serotonin-norepinephrine reuptake inhibitors
Used in MDE
contrast to SSRIs which comparatively only prevent serotonin reuptake
Venlafaxine
SNRI - Depression
MDE and Generalised Anxiety Disorder
Most commonly used SNRI
Desvenlafaxine
SNRI - Depression
MDE
Hepatic issues
Duloxetine
SNRI - Depression
MDE
Also used for Fibromyalgia
Hepatic issues
Mirtazipine
Depresion - Tetracyclic Antidepressant
Good efficacy
Sedative effect (often given nocte to aid sleep)
Increases apetite - often given to elderly to increase apetite; not generally indicated in younger patients for this reason
Lithium
Mania (narrow therapeutic window)
Primarily used in bi-polar
Schizophrenia, major depressive disorder
As a mood stabilizer, lithium more effective at preventing mania than depression
Specific action unknown
Slows down G-protein coupling, adenylate cyclase activity and inhibits neurotransmitter release by impairing actions of Na+
Increases NA and 5-HT turnover
1st, 2nd and 3rd line treatment for acute manic episodes
1st line: Lithium Valporate Carbamezapine 2nd Gen Antipsychotics
2nd line:
2nd gen antipsychotic + lithium OR valporate
Lithium + Valporate
3rd line:
ECT
Clozapine
Lithium + Anticonvulsant + Anti-psychotics
Bipolar Disorder
Prevents mood elevations and controls/prevents depressive episodes
*Note: use of antidepressants is contraversial in bipolar
Very effective, reduced suicides
Risk of toxicity
Sodium Valporate (epilim)
Bipolar Disorder
Not as effective as lithium for depressive episodes
Side-effects: Cognitive dulling, weight gain, pregnancy, fertility issues in females
First line for anxiety
SSRIs
First line for depression
SSRIs
Diazepam
Benzodiazepine - Anxiety
Longer acting
GABA modulator/agonist: bind to specific part on GABA receptor to facilitate GABA (inhibitory) neurotransmitter binding - decreased cell excitability
Induces sedating, sleep-inducing, anti-anxiety, muscle-relaxant, anti-convulsant actions
Also used for alcohol withdrawal
Lorazepam
Benzodiazepine - Anxiety
Shorter acting (safer than diazepam)
Binds to specific location on GABA receptors to enhance GABA (inhibitory) neurotransmitter binding -> decreased cell excitability
Has anti-anxiety, muscle relaxant, anti-convulsant, sleep-inducing actions
Alprazolam
Benzodiazepine - Anxiety
Shorter acting (safer than diazepam)
Binds to specific location on GABA receptors to enhance GABA (inhibitory) neurotransmitter binding -> decreased cell excitability
Has anti-anxiety, muscle relaxant, anti-convulsant, sleep-inducing actions
Midazolam
Benzodiazepine - Anxiety
Shorter acting (safer than diazepam)
Binds to specific location on GABA receptors to enhance GABA (inhibitory) neurotransmitter binding -> decreased cell excitability
Has anti-anxiety, muscle relaxant, anti-convulsant, sleep-inducing actions
Barbituates
Anxiety
Modulate GABA receptor at site different to benzodiazepines: non-specific inhibition of excitory neurotransmission
Compared to benzos: lower selectivity (thus more interactions), less safe (risk of fatality with overdose, higher abuse potential)
Side effects: confusion, disorientation and depression
Buspirone
Anxiety
Not readily available
High affinity for 5-HT receptors and CNS D2 receptors -> action not fully understood
Zopiclone
Short-term insomnia
Increase inhibitory effects of GABA on neurons
Sleep-inducing with less morning sedation
Does not impact normal sleep paterns
Less dependency
Does not reduce anxiety
Zolpidem
Short-term insomnia
Increases GABA inhibitory effects on CNS neurons
Sleep-inducing with less morning sedation
Does not alter normal sleeping patters
Less dependence
Does not reduce anxiety
Chloral Hydrate
Short-term insomnia
Prodrug (inactive form administered which is activiated via normal metabolic process)
Powerful hypnotic )sleep-inducing)
Used for paediatric anaesthetic
