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CAM305 Pharm > Psychotropics > Flashcards

Psychotropics Flashcards

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

A

Short term: Mild GI upset, agitation

Longer-term: Insomnia, sexual dysfunction, discontinuation syndrome

21
Q

Imipramine

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

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

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

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
Q

Doxepine

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

26
Q

Amitriptyline (endep)

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

27
Q

MAOIs =?

A

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
Q

Phenylzine

A

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
Q

Tranylcypromine

A

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
Q

SNRIs = ?

A

Serotonin-norepinephrine reuptake inhibitors

Used in MDE
contrast to SSRIs which comparatively only prevent serotonin reuptake

31
Q

Venlafaxine

A

SNRI - Depression

MDE and Generalised Anxiety Disorder

Most commonly used SNRI

32
Q

Desvenlafaxine

A

SNRI - Depression

MDE

Hepatic issues

33
Q

Duloxetine

A

SNRI - Depression

MDE
Also used for Fibromyalgia

Hepatic issues

34
Q

Mirtazipine

A

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
Q

Lithium

A

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
Q

1st, 2nd and 3rd line treatment for acute manic episodes

A 
1st line:
Lithium
Valporate
Carbamezapine
2nd Gen Antipsychotics

2nd line:
2nd gen antipsychotic + lithium OR valporate
Lithium + Valporate

3rd line:
ECT
Clozapine

37
Q

Lithium + Anticonvulsant + Anti-psychotics

A

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
Q

Sodium Valporate (epilim)

A

Bipolar Disorder

Not as effective as lithium for depressive episodes

Side-effects: Cognitive dulling, weight gain, pregnancy, fertility issues in females

39
Q

First line for anxiety

A

SSRIs

40
Q

First line for depression

A

SSRIs

41
Q

Diazepam

A

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
Q

Lorazepam

A

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
Q

Alprazolam

A

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
Q

Midazolam

A

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
Q

Barbituates

A

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
Q

Buspirone

A

Anxiety

Not readily available

High affinity for 5-HT receptors and CNS D2 receptors -> action not fully understood

47
Q

Zopiclone

A

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
Q

Zolpidem

A

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
Q

Chloral Hydrate

A

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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