Antipsychotics Flashcards
What are the 5 most prescribed antipsychotic drugs in the U.K.?
Atypical:
1st: Quetiapine
2nd: Olanzapine
3rd: Risperidone
4th: Aripiprazole
Typical:
5th: Chlorpromazine
What are the two pathways behind the theory of schizophrenia?
1) Mesocortical Pathway:
- Dopamine underactive
- D1 receptors predominate
- Negative symptoms
2) Mesolithic Pathway:
- Dopamine overactive
- D2 receptors predominate
- Positive symptoms
Drugs that release ____ or activate associated pathways induce psychosis- like effect. E.g. L-DOPA, amphetamines, bromocriptine.
Dopamine (and schizophrenic patients have increased DA release)
Dopamine (agonists/ antagonists) cause psychosis?
Dopamine (agonists/ antagonists) cause anti-psychotic effects?
Agonist
Antagonist
MOA of anti-psychotic drugs:
Bloakade of dopamine and/ or 5HT(2) receptors
S/E of dopamine blockade.
1) Dyskinesia
- acute EPS: extrapyramidal symptoms e.g. acute dystonia
- chronic EPS e.g. Tardrive dyskinesias
2) Dysphoria
3) Endocrine dysfunction (temp/ increase prolactin, increase eating disorder)
S/E of muscarinic blockade.
Tachycardia and decrease seizure threshold
S/E of alpha blockade.
Hypotension
Antipsychotic drugs not only act as ______, but also modify ________ function.
DA antagonists
Serotonin
Name two drugs that act primarily as D1 receptor antagonists.
Olanzapine and Zuclopenthixol
Name two drugs that act primarily as D2 receptor antagonists (Gi GPCR).
Olanzapine Risperidone Aripiprazole Zuclopenthixol Haloperidol
(Either two)
Name two drugs that act primarily as Alpha-1 (alpha- adreniceptors 1: Gq GPCRs) receptor antagonists.
Quetiapine
Chlorpromazine
Zuclopenthixol
Clozapine
(either two)
Name two drugs that act primarily as H1 (histamine 1- Gq GPCRs) receptor antagonists.
Quetiapine
Chlorpromazine
Clozapine
(either two)
Name two drugs that act primarily as 5-HT (especially 5-HT2A) receptor antagonists.
Olanzapine Risperidone Aripiprazole Chlorpromazine Zuclopenthixol Clozapine
(Either two)
Name two drugs that act primarily as muscarinic AChRs (Gq/GI GPCRs) receptor antagonists.
Olanzapine
Chlorpromazine
Clozapine
(either two)
There are (a lot/ only a few) antipsychotic drugs in the U.K..
A lot
Common sides effects of antipsychotics.
1) EPS (extrapyramidal symptoms) (D2/D1)
- acute EPS: e.g. acute dystonia
- chronic EPS e.g. Tardrive dyskinesias
2) Endocrine dysfunction (temp/ increase prolactin, increase eating disorder/ breast swelling, pain lactation) ( D2/ D1)
3) sedation (H1 histamine receptor)
4) Weight gain (H1, 5-HT, mAChR)
5) Hypotension (alpha-adrenoceptors)
6) Anticholinergic effects e.g. Dry mouth blurred vision. (mAChR)
7) Autonomic S/E: constipation, dry mouth and hypotension.
8) other S/E: drowsiness, tachycardia
Examples of first generation/ typical antipsychotics.
- Chlorpromazine (phenothiazine class)
- Haloperidol (Butyrophenone class)
- Zuvlopenthixol (Thioxabthene class)
First (typical) / second (atypical) generation antipsychotics are less likely to cause EPS. And give some examples.
Among all, ______ is highly recommended with treatment resistance.
Second generation/ atypical.
Examples: clozapine, Quetiapine, Olanzapine, Risperidone, Aripiprazole, Sulpiride.
Clozapine is highly recommended with treatment resistance.
What is the two most prescribed antipsychotics in the UK?
1st: Quetiapine
2nd: Olanzapine
What is atypical antipsychotics?
Antipsychotics that are free or relatively free of EPSs (extrapyramidal S/E). These may reduce negative symptoms of schizophrenia.
D1 stimulate ______ (enzyme).
Adenylyl cyclase
Blockage of D2 in basal ganglia usually results in ___.
EPS
Deep IM antipsychotic injection is act as ___________ injections in community to decrease risk of patients forgetting daily doses.
Long- action depot injections.
Endocrine effect of increasing prolactin production after D2 receptor blockade.
Gynaecomastia, galactlrrhoea, menstrual irregularities, impotence, weight gain.
