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
What is Citalopram
Selective serotonin reuptake inhibitor (fewer interactions with other drugs) Prolong QTc PO
26
What is Fluoxetine
Selective serotonin reuptake inhibitor | PO
27
What is Sertraline
Selective serotonin reuptake inhibitor | PO
28
What is Escitalopram
Selective serotonin reuptake inhibitor PO (fewer interactions with other drugs)
29
How long should SSRIs be continued after symptoms stop?
6 months
30
First line treatment for moderate to severe depression | - or in mild if psychological treatments fail
SSRIs
31
Tricyclic anti depressants | Mechanism of action
Inhibit neuronal reuptake of serotonin and noradrenaline Also block muscarinic, histamine (H1), a1, a2 and dopamine receptors Work from the first week
32
Tricyclic anti depressants | Side effects
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
Name some tricyclic anti depressants
Amitripyline, lofepramine
34
What is Amitriptyline
Tricyclic anti depressant | Also good for neuropathic pain
35
What is Lofepramine
Tricyclic anti depressant
36
What is Amisulpride
selective dopamine receptor antagonist with high affinity for mesolimbic D2 and D3 receptors. atypical antipsychotic
37
What is Valproate
- 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
What is Lithium
Mood stabliser First line in bipolar disorder monitoring required. aim for 0.5-1mmol/l
39
Serotonin noradrenaline receptor inhibitors (SNRI) | Name 3
venlafaxine desvenlafaxine duloxetine (mirtazapine isnt an SNRI but works on a2 adrenoceptors and 5HT2c's so does increase NAd+5-HT)
40
What is Venlafaxine
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
What is Duloxetine
SNRI | inhibits NA and 5-HT uptake.
42
Bupropion is a
noradrenaline and dopamine uptake inhibitor.
43
What is Mirtazapine
blocks α2 adrenoceptors and 5-HT2C receptors, enhancing noradrenaline and 5-HT release. causes sedation - so take at night
44
Symptoms of lithium toxicity
when above 1.5mmol/l Nausea, vomiting, diarrhoea, confusion, excessive sleeping, seizures, myoclonic jerks and coarse tremor
45
What may happen if you suddenly stop SSRIs?
Sudden withdrawal of SSRIs can cause gastrointestinal upset, neurological and influenza-like symptoms and sleep disturbance.
46
Low mood and peptic ulcer. Prescribe SSRI? Why?
``` SSRIs increase bleeding risk If patient (without peptic ulcers) is taking aspirin/NSAIDs and needs SSRI - gastro-protection should be prescribed too ```
47
Side effects of SNRIs
``` GI upset (dry mouth, nausea, weight changes, diarrhoea/constipation) CNS - (headache, weird dreams, insomnia, confusion, seizures) ```
48
Benzodiazepines - what do they do and how?
Facilitate GABA binding to receptors (main inhibitory neurotransmitter) - depressant effect on synapses - reduced anxiety, sleepiness/sedation, anti-convulsive effect
49
Uses of benzodiazepines
First line for Seizures/status epilepticus (lorazepam) as well as alcohol withdrawal reactions (chlordiazepoxide) Short term treatment of insomnia/anxiety (if distressing)
50
Name some long acting benzodiazepines
Diazepam, lorazepam, chlordiazepoxide Long acting for seizures, alcohol withdrawal etc
51
Name some short/intermediate acting benzodiazepines
Midazolam (sedation for procedure) Short | Temazepam - intermediate
52
Carbamazepine - uses in psych etc
For focal seizures, trigeminal neuralgia, and bipolar prophylaxis if the other drugs arent working teratogenic tho
53
Gabapentin
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
Pregabalin
Binds to calcium channels - stopping neurotransmission Generalised anxiety disorder Focal epilepsy add on neuropathic pain SE: drowsy/dizzy
55
Z drugs - action & effect
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
name 2 Z drugs
zopiclone | zolpidem
57
Define hypnotic
A drug which will sedate when given during the day - provokes drowsiness facilitating sleep
58
Anxiolytics
'sedatives' will induce sleep when given at night but mainly kinda to treat anxiety - reduces anxiety, causing calm and quietness in patient