Psychopharmacology - drugs Flashcards
Antipsychotics - both generations
Mechanism of action
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
Antipsychotics - first generation - typical
Side effects (1/2)
from blocking the nigrostriatal pathway
(neurological)
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
Antipsychotics - first generation - typical
Side effects (2/2)
from blocking the nigrostriatal pathway
(others)
Drowsiness
Hypotension
QT prolongation ( => arrhythmias)
Erectile dysfunction
Tuberohypophyseal blockage can cause hyperprolactinaemia
Danger of using Antipsychotics - first generation - typical in a dementia patient?
increased risk of stroke and death
Name some Antipsychotics - first generation - typical
haloperidol
chlorpromazine
prochlorperazine
Haloperidol is what type of drug is it?
Antipsychotics - first generation - typical
Chlorpromazine is what type of drug is it?
Antipsychotics - first generation - typical
Prochlorperazine is what type of drug is it?
Antipsychotics - first generation - typical
Antipsychotics - first generation - typical
Uses
= 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
Atypical antipsychotics - second generation
Mechanisms (how they differ from first generation
Still block D2 receptors
But also affect other receptors too.
‘Looser D2 binding’
Better for treatment resistant forms of schizophrenia
Atypical antipsychotics - second generation
Side effect profile
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)
How is prolactin release usually controlled?
Prolactin is produced in the lactotroph cells of the anterior pituitary gland, under inhibitory control by dopamine (less dopamine = more prolactin)
Hyperprolactinaemia
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.
Name some Atypical antipsychotics - second generation
Risperidone, olanzapine, clozapine, quetiapine
What is Risperidone
Atypical antipsychotics - second generation
First line
What is Olanzapine
Atypical antipsychotics - second generation
First line
What is Clozapine
Atypical antipsychotics - second generation
Second line
What is Quetiapine
Atypical antipsychotics - second generation
What is Modecate
Fluphenazine decanoate
Long acting ‘depot’ injection
Anti psychotic given every 2-5 weeks
What is aripiprazole
Atypical antipsychotic
Best for not affecting the QTc
Doesn’t have loads of side effects relatively
What is Dopamine’s effect on blood pressure
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
Selective serotonin reuptake inhibitors
Mechanism of action
Inhibit neuronal reuptake of serotonin (5-HT) so that there’s more for neurotransmission
Metabolised by the liver
Selective serotonin reuptake inhibitors
Side effects
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