Neuropharmacology Flashcards
What is the main side effect of clozapine?
Agranulocytosis
Tricyclic antidepressants have many side effects. Give some side effects and the receptors responsible for these side effects.
TCAs antagonise…
M1 - dry mouth, blurred vision, constipation, urinary retention
H1 - sedation, weight gain
a1 - postural hypotension
For which group of people are TCAs contraindicated?
Which patients do get TCAs?
Contraindications:
Young and old people
Cardiac patients - due to increasde risk of conduction abnormalities
Suicidal patients - due to risk of overdose
Drivers and workers - due to sedation
Uses:
Severe and treatment-resistant depression
Which SSRIs have the highest affinity?
Sertraline and paroxetine
Which type(s) of MAO do the newer forms of MAOIs inhibit? Give an example.
MAOa only - this is responsible for the breakdown of 5-HT and noradrenaline
Old-generation MAOIs break down dopamine too, causing EPSE.
Newer forms block MAOa only - an example is moclopemide.
Name a drug which inhibits 5-HT release? Why is it not used clinically?
Ecstasy. It is addictive and neurotoxic.
Why do antidepressants take a while to work?
Initially levels increase, causing more activation of 5-HT1a receptors found on the neuronal cell body. This receptor inhibits 5-HT secretion.
Eventually, the 5-HT1a receptor become desensitised and this is when the inhibition of 5-HT is stopped.
What are some side effects of antipsychotics due to their interaction with the nigrostriatal pathway?
loss of control of fine movement, EPSE, tardive dyskinesia
How are first generation antipsychotics categorised? Give examples.
Group 1 - sedation = chlorpromazine
Group 2 - anticholinergic = thioridazine
Group 3 - EPSE = fluphenazine
Another first generation antipsychotic is haloperidol.
Give examples of second generation (atypical) antipsychotics.
Clozapine Olanzapine Risperidone Amisulpiride Quetiapine
Give some negative and positive symptoms of schizophrenia…
Positive - disorders of thought, hallucinations, paranoia
Negative - blunted emotions/withdrawal, social withdrawal, apathy
Categorise these neurotransmitters into high and low in anxiety…
- Serotonin
- Noradrenaline
- GABA
- Serotonin is increased
- Noradrenaline is increased
- GABA is decreased
Give a very short half life benzodiazepine and suggest uses for it.
Midazolam
Conscious sedative + status epilepticus
Give a long half-life benzodiazepine and suggest a use for it.
Lorazepam
Chlordiazepoxide - acute alcohol withdrawal
Diazepam (Valium)
They are all anxiolytics used in GAD
Why does diazepam have a long half life?
It undergoes oxidative metabolism into active metabolites.
Why is there a risk of overdose associated with barbiturates?
They work on GABAa receptors.
But they do not require GABA to open the channel, hence risk of overdose as their use is not limited by GABA concentration.
How do Z-hypnotics work?
THey are allosteric modulators of GABAa receptors.
They are more selective to a1 receptors, leading to sedation.
Give examples of Z-hypnotics.
Zopiclone
Zolpidem
Zaleplon