Psychopharmacology - drugs Flashcards

1
Q

Antipsychotics - both generations

Mechanism of action

A

Dopamine (D2) antagonists at post synaptic receptors
There are three main loops affected in the CNS:

1) mesolimbic/mesocortical (midbrain to limbic system/frontal cortex
Blocking this probably causes most antipsychotic effect

2) nigrostriatal pathway (substantia nigra to striatum (basal ganglia))
3) hypothalamus - pituitary gland (tuberohypophyseal) pathway

X) there are also D2 receptors in the chemoreceptor trigger zone

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2
Q

Antipsychotics - first generation - typical
Side effects (1/2)
from blocking the nigrostriatal pathway

(neurological)

A

movement abnormalities:
- acute dystonic reactions - parkinsonian symptoms/muscle spasms
- akathisia (a state of inner restlessness)
- neuroleptic malignant syndrome (rare)
All occur early after treatment

tardive dyskinesia - months/years later
- pointless, involuntary repetitive movements (lip smacking) - may be permanent

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3
Q

Antipsychotics - first generation - typical
Side effects (2/2)
from blocking the nigrostriatal pathway

(others)

A

Drowsiness
Hypotension
QT prolongation ( => arrhythmias)
Erectile dysfunction

Tuberohypophyseal blockage can cause hyperprolactinaemia

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4
Q

Danger of using Antipsychotics - first generation - typical in a dementia patient?

A

increased risk of stroke and death

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5
Q

Name some Antipsychotics - first generation - typical

A

haloperidol
chlorpromazine
prochlorperazine

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6
Q

Haloperidol is what type of drug is it?

A

Antipsychotics - first generation - typical

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7
Q

Chlorpromazine is what type of drug is it?

A

Antipsychotics - first generation - typical

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8
Q

Prochlorperazine is what type of drug is it?

A

Antipsychotics - first generation - typical

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9
Q

Antipsychotics - first generation - typical

Uses

A

= Psychomotor agitation
= Schizophrenia - if metabolic side effects of atypical antipsychotics is going to be a problem
= Bipolar disorder - acute
= nausea and vomiting control - especially in palliative setting

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10
Q

Atypical antipsychotics - second generation

Mechanisms (how they differ from first generation

A

Still block D2 receptors
But also affect other receptors too.
‘Looser D2 binding’

Better for treatment resistant forms of schizophrenia

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11
Q

Atypical antipsychotics - second generation

Side effect profile

A
Degree of sedation
Parkinsonian symptoms can happen but less than with first generation typical antipsychotics
Metabolic disturbances:
Weight gain, diabetes, lipid changes
Long QTc - arrhythmias
Hyperprolactinaemia (risperidone esp)
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12
Q

How is prolactin release usually controlled?

A

Prolactin is produced in the lactotroph cells of the anterior pituitary gland, under inhibitory control by dopamine (less dopamine = more prolactin)

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13
Q

Hyperprolactinaemia

A

In women, hyperprolactinaemia inhibits gonadotrophin secretion (follicle-stimulating hormone (FSH) and luteinising hormone (LH)), leading to menstrual dysfunction. It also may cause galactorrhoea.

In men, hyperprolactinaemia has a direct, reversible effect on the hypothalamus, causing secondary hypogonadism which results in reduced libido and erectile dysfunction.

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14
Q

Name some Atypical antipsychotics - second generation

A

Risperidone, olanzapine, clozapine, quetiapine

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15
Q

What is Risperidone

A

Atypical antipsychotics - second generation

First line

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16
Q

What is Olanzapine

A

Atypical antipsychotics - second generation

First line

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17
Q

What is Clozapine

A

Atypical antipsychotics - second generation

Second line

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18
Q

What is Quetiapine

A

Atypical antipsychotics - second generation

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19
Q

What is Modecate

A

Fluphenazine decanoate
Long acting ‘depot’ injection
Anti psychotic given every 2-5 weeks

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20
Q

What is aripiprazole

A

Atypical antipsychotic
Best for not affecting the QTc
Doesn’t have loads of side effects relatively

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21
Q

What is Dopamine’s effect on blood pressure

A

Dopamine (dopamine hydrochloride) is a catecholamine drug that acts by inotropic effect on the heart muscle (causes more intense contractions) that, in turn, can raise blood pressure

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22
Q

Selective serotonin reuptake inhibitors

Mechanism of action

A

Inhibit neuronal reuptake of serotonin (5-HT) so that there’s more for neurotransmission

Metabolised by the liver

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23
Q

Selective serotonin reuptake inhibitors

Side effects

A
GI upset, appetite and weight can go up/down
Skin rash (hypersensitivity reactions)
Hyponatraemia - confusion
May increase suicidal thoughts
Bleeding

Sudden withdrawal - GI upset, neuro/flu symptoms, sleep disturbance

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24
Q

Name some selective serotonin reuptake inhibitors

A

citalopram
fluoxetine
sertraline
escitalopram

25
Q

What is Citalopram

A

Selective serotonin reuptake inhibitor
(fewer interactions with other drugs)
Prolong QTc
PO

26
Q

What is Fluoxetine

A

Selective serotonin reuptake inhibitor

PO

27
Q

What is Sertraline

A

Selective serotonin reuptake inhibitor

PO

28
Q

What is Escitalopram

A

Selective serotonin reuptake inhibitor
PO
(fewer interactions with other drugs)

29
Q

How long should SSRIs be continued after symptoms stop?

A

6 months

30
Q

First line treatment for moderate to severe depression

- or in mild if psychological treatments fail

A

SSRIs

31
Q

Tricyclic anti depressants

Mechanism of action

A

Inhibit neuronal reuptake of serotonin and noradrenaline
Also block muscarinic, histamine (H1), a1, a2 and dopamine receptors

Work from the first week

32
Q

Tricyclic anti depressants

Side effects

A

Anti muscarinic - dry mouth, constipation, urinary retention
H1/a1 blockage - sedation, hypotension
Dopamine block - prolactin up etc, and parkinsonian symptoms

More toxic than SSRIs so dont use if suicide risk

33
Q

Name some tricyclic anti depressants

A

Amitripyline, lofepramine

34
Q

What is Amitriptyline

A

Tricyclic anti depressant

Also good for neuropathic pain

35
Q

What is Lofepramine

A

Tricyclic anti depressant

36
Q

What is Amisulpride

A

selective dopamine receptor antagonist with high affinity for mesolimbic D2 and D3 receptors.

atypical antipsychotic

37
Q

What is Valproate

A
  • First choice for generalised seizures
  • mood stabiliser - for manic episodes and for prophylaxis

Weakly inhibits neuronal Na channels and increases brain GABA

Teratogenic is first 1/3 of pregnancy (but 90% chance baby will be okay)

38
Q

What is Lithium

A

Mood stabliser
First line in bipolar disorder

monitoring required. aim for 0.5-1mmol/l

39
Q

Serotonin noradrenaline receptor inhibitors (SNRI)

Name 3

A

venlafaxine
desvenlafaxine
duloxetine

(mirtazapine isnt an SNRI but works on a2 adrenoceptors and 5HT2c’s so does increase NAd+5-HT)

40
Q

What is Venlafaxine

A

SNRI
5-HT uptake inhibitor, but less selective for 5-HT versus noradrenaline than SSRIs. It is metabolised to desvenlafaxine, which is also antidepressant.

41
Q

What is Duloxetine

A

SNRI

inhibits NA and 5-HT uptake.

42
Q

Bupropion is a

A

noradrenaline and dopamine uptake inhibitor.

43
Q

What is Mirtazapine

A

blocks α2 adrenoceptors and 5-HT2C receptors, enhancing noradrenaline and 5-HT release.

causes sedation - so take at night

44
Q

Symptoms of lithium toxicity

A

when above 1.5mmol/l

Nausea, vomiting, diarrhoea, confusion,
excessive sleeping, seizures, myoclonic jerks and coarse tremor

45
Q

What may happen if you suddenly stop SSRIs?

A

Sudden withdrawal of SSRIs can cause gastrointestinal upset, neurological and influenza-like symptoms and sleep disturbance.

46
Q

Low mood and peptic ulcer. Prescribe SSRI? Why?

A
SSRIs increase bleeding risk
If patient (without peptic ulcers) is taking aspirin/NSAIDs and needs SSRI - gastro-protection should be prescribed too
47
Q

Side effects of SNRIs

A
GI upset (dry mouth, nausea, weight changes, diarrhoea/constipation)
CNS - (headache, weird dreams, insomnia, confusion, seizures)
48
Q

Benzodiazepines - what do they do and how?

A

Facilitate GABA binding to receptors (main inhibitory neurotransmitter)

  • depressant effect on synapses
  • reduced anxiety, sleepiness/sedation, anti-convulsive effect
49
Q

Uses of benzodiazepines

A

First line for Seizures/status epilepticus (lorazepam) as well as alcohol withdrawal reactions (chlordiazepoxide)

Short term treatment of insomnia/anxiety (if distressing)

50
Q

Name some long acting benzodiazepines

A

Diazepam, lorazepam, chlordiazepoxide

Long acting for seizures, alcohol withdrawal etc

51
Q

Name some short/intermediate acting benzodiazepines

A

Midazolam (sedation for procedure) Short

Temazepam - intermediate

52
Q

Carbamazepine - uses in psych etc

A

For focal seizures, trigeminal neuralgia, and bipolar prophylaxis if the other drugs arent working

teratogenic tho

53
Q

Gabapentin

A

Binds to calcium channels - stopping neurotransmission
(Closely related to GABA in structure. This is irrelevant to its action though)

Migrane prophylaxis
Neuropathic pain
Add on for focal seizures

CAn cause drowsiness/dizziness

Can make urine dipsticks look like there is protein in urine #FalsePositive

54
Q

Pregabalin

A

Binds to calcium channels - stopping neurotransmission

Generalised anxiety disorder
Focal epilepsy add on
neuropathic pain

SE: drowsy/dizzy

55
Q

Z drugs - action & effect

A

Like benzo’s - open the GABA channels causing sedation - they are hypnotic drugs, generally with a shorter duration than benzo’s

only use short term - dependence can occur. good for specific, acute situations (night before surgery etc)

56
Q

name 2 Z drugs

A

zopiclone

zolpidem

57
Q

Define hypnotic

A

A drug which will sedate when given during the day - provokes drowsiness facilitating sleep

58
Q

Anxiolytics

A

‘sedatives’ will induce sleep when given at night

but mainly kinda to treat anxiety - reduces anxiety, causing calm and quietness in patient