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Anti-psychotics
Dopamine Theory
Blockade Of D2 Receptors?
D2
ANTAGONIST
Nigrostriatal pathway
extrapyramidal side effects
(EPS) and tardive dyskinesia
Mesocortical pathway
enhanced negative and
cognitive psychotic
symptoms
Mesolimbic pathway
dramatic therapeutic action
on positive psychotic
symptoms
Tuberoinfundibular pathway
hyperprolactinemia (lactation,
Dopamine Receptors
Dopamine Receptors
Conventional or typical
Antipsychotics
Dopamine 2
Muscarinic/choliner
gc
Alpha adrenergic
Histamine
Receptor Affinity
Low Affinity (loosely bound)
- Quetiapine, Olanzapine, Amisulpride,
Clozapine
High Affinity (tightly bound)
- Chlorpromazine, Haloperidol,
Flupenthixol, Fluphenazine
Tightly bound drugs lead to increased
sensitivity to dopamine blockade so
more likely to cause EPSE
Atypical Antipsychotics
Pharmacologic
Properties
5HT2A and D2
antagonism (as
opposed to
conventional drugs
which are D2 without
5HT2A antagonism)
Atypicals blockade
of D2 and 5HT2A
Dopamine and
serotonin have a
reciprocal relationship
Serotonin opposes
the release of
dopamine in the
nigrostriatal and
tuberofundibular
pathways
Atypicals
Anti-psychotics
Conventional eg chlorpromazine,
haloperidol, stelazine, depots such as
flupenthixol, zuclopenthixol, fluphenazine
Atypical eg olanzapine, risperidone,
quetiapine, amisulpride, clozapine,
risperdal consta intramuscular injection,
aripiprazole, paliperidone, ziprasidone
Also have effects on acetylcholine,
histamine,serotonin receptors varying
adverse effects
Atypical antipsychotics
Atypical antipsychotics
Therapeutic effects on
symptoms
Adverse Effects
Sedation
Postural hypotension
Anticholinergic effects dry mouth,
blurred vision, constipation, urinary
hesitancy
Weight gain-clozapine, olanzapine
Metabolic effects-increased serum
lipids, impaired glucose toleranceclozapine, olanzapine, quetiapine
Adverse Effects
Hyperprolactinaemia-leads to
galactorrhoea, amenorrhoea, decreased
libido
Sexual dysfunction
QTc prolongation-leads to cardiac
arrhythmias
EPSE-extrapyramidal side effects
Acute dystonias -laryngeal spasm,
oculogyric crises
Akathisia-severe sense of agitation, inner
restlessness in the limbs, especially the
legs
Adverse Effects
Adverse Effects
Depot Anti-psychotics
Trifluperazine, Fluphenazine
Haloperidol, Droperidol,
Thiothixene, Pimozide
Atypical antipsychotics
Amisulpride
Aripiprazole
Clozapine
Atypical antipsychotics
Olanzapine
Quetiapine
Risperidone, Paliperidone
Ziprasidone
Drug Interactions
Cytochrome P450
Examples
Fluvoxamine inhibits olanzapine and
clozapine metabolism
Smoking induces Olanzapine
metabolism
SSRIs inhibit most antipsychotics and
therefore increase serum concentrations
Phenytoin reduces serum concentration
of Quetiapine
Others grapefruit juice, Antibiotics,
Clozapine
Psychological therapies
Conclusion
Resources