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CAM305 Pharm > Psychotropics > Flashcards

Psychotropics Flashcards

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1
Q

Clozapine

A

Psychosis - Atypical Agent

Binds dopaminergic, serotonergic, muscarinic and histaminic receptors

*Strice monitoring via specialist clinic required

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2
Q

Risperidone

A

Psychosis - Atypical Agent

D2 and 6-HT antagonist

EPSE (extra pyramidal side-effects) only at very high dosages

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3
Q

Quetiapine

A

Psychosis - Atypical Agent

Effective at high dosages

  • Sedating
  • Weight gain ++
  • Best choice in pregnancy
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4
Q

Olanzapine

A

Psychosis - Atypical Agent

Efective
Sedating
Weight gain +++

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5
Q

Aripiprazole

A

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

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6
Q

Ziprasidone, Asenapine, Amisulpride

A

Psychosis - Atypical Agents

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7
Q

What are EPSEs?

A

Extra-pyrimidal side-effects

Movement disorders caused by dopamine antagonists

Includes akasthisia (inability to still movements) and akinesia (inability to initiate movement)

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8
Q

What is a partial dopamine agonist, and why is it an attractive option in schizophrenia?

A

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

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9
Q

Fluphenazine

A

Psychosis - Typical Agent - PHENOTHIZINES

D2 antagonist in MESOLIMBIC, NIGROSTRIATAL & TUBERINFUNDIBULAR SYSTEMS,

EPSEs are verry common, thus overall not commonly used

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10
Q

Trifluoperazine

A

Psychosis - Typical Agent - PHENOTHYZINES

D2 antagonist in MESOLIMBIC, NIGROSTRIATAL & TUBERINFUNDIBULAR SYSTEMS

EPSEs are verry common, thus overall not commonly used

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11
Q

Pericyazine

A

Psychosis - Typical Agent - PHENOTHYZINES

D2 antagonist in MESOLIMBIC, NIGROSTRIATAL & TUBERINFUNDIBULAR
SYSTEMS

EPSEs very common; thus not commonly used now

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12
Q

Prochloroperazine

A

Psychosis - Typical Agent - PHENOTHIZINES

D2 antagonist at MESOLIMBIC, NIGROSTRIATAL & TUBERINFUNDIBULAR SYSTEMS

EPSEs very common; thus not commonly used now

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13
Q

Haloperidol & Droperidol

A

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

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14
Q

Sertraline

A

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

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15
Q

Escitalopram

A

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

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16
Q

Citalopram

A

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

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17
Q

Fluoxetine

A

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

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18
Q

Paroxetine

A

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

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19
Q

Fluvoxamine

A

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

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20
Q

General side effects of SSRIs

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A

Short term: Mild GI upset, agitation

Longer-term: Insomnia, sexual dysfunction, discontinuation syndrome

21
Q

Imipramine

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A

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

22
Q

Trimipramine

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A

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

23
Q

Mortriptyline

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A

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

24
Q

Dothiepin

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A

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

25
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
26
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
27
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
28
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
29
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
30
SNRIs = ?
Serotonin-norepinephrine reuptake inhibitors | Used in MDE contrast to SSRIs which comparatively only prevent serotonin reuptake
31
Venlafaxine
SNRI - Depression MDE and Generalised Anxiety Disorder Most commonly used SNRI
32
Desvenlafaxine
SNRI - Depression MDE Hepatic issues
33
Duloxetine
SNRI - Depression MDE Also used for Fibromyalgia Hepatic issues
34
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
35
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
36
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
37
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
38
Sodium Valporate (epilim)
Bipolar Disorder Not as effective as lithium for depressive episodes Side-effects: Cognitive dulling, weight gain, pregnancy, fertility issues in females
39
First line for anxiety
SSRIs
40
First line for depression
SSRIs
41
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
42
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
43
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
44
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
45
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
46
Buspirone
Anxiety Not readily available High affinity for 5-HT receptors and CNS D2 receptors -> action not fully understood
47
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
48
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
49
Chloral Hydrate
Short-term insomnia Prodrug (inactive form administered which is activiated via normal metabolic process) Powerful hypnotic )sleep-inducing) Used for paediatric anaesthetic

CAM305 Pharm (1 decks)

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