Antipsychotics (quetinapine, olanzapine, aripiprazole)

Question 1

symptoms of schizophrenia

Answer 1

1) positive(affective) syndrome:
- hallucination
- delusions
- conceptual disorganisation
- bizzare behaviour

2) negative syndrome:
- anhedonia;apathia
- social withdrawal
- emotional withdrawal

3)congnitive deficit: difficulty in abstract thinking & concentration

Question 2

Dopamine hypothesis

Answer 2

• all antipsychotic drugs block postsynaptic D2 receptor
• drugs that increase dopaminergic activity ( amphetamine, cocaine) aggravate schizophrenia
• density of dopamine receptors has been found to be increased in the brain of schizophrenic pts
• successful treatment of schizophrenic pts has been reported to change the amount of homovanilic acid (HVA, a DA metabolite)

Question 3

disturbance in regulation

Answer 3

• 5HT system
• glutamate system (enhanced DA release)
• GABA system

Question 4

classification of antipsychotics

Answer 4

• 1st generation antipsy ( typical/traditional)

- 2nd generation (atypical, new)

Question 5

side effects of 1st generation antipsychotics

Answer 5

• EPS: parkinsonian sy & tardiv dyskinesia
• increased prolactine secretion
• lack of effect on -ve symptoms
• high number of non-responders

Question 6

side effects of 2nd generation antipsychotics

Answer 6

• smaller risk or lack of EPS
• smaller effect on prolactine level
• better action against the -ve sy
• action in the non-responders

Question 7

1st generation antipsychotics

Answer 7

Phenotiazins

• dimethilamine derivatives:
  
  • chlorpromazin
  • levomepromazin
  • promethazine
• pipridine derivatives
  
  • thioridazine
• piperazin derivatives
  
  • fluphenazin
  • trifluoperazine

Thioxantenes

• chlorpoxiten
• thiotixen
• flupentixol

Butyrophenons

• haloperidol
• droperidol

Question 8

2nd generation antipsychotics

-mixed D2/5HT2 ATG

Answer 8

A) tricyclic comp

• Clozapin (weak D2 stronger D4 affinity)
• Olanzapin (strong D2 binding)
• Quetiapin

B) heterocyclic compounds
-Risperidon (strong binding to 5HT2 &D2 R)

• Paliperidon (Risperidon’s metabolite)
• Ziprazidon (higher affinity for 5HT2 then to D2 R + PA at 5HT1A receptors)
• Sertindol (cardiotoxic)

Question 9

2nd generation antipsychotics

-selective D2/D3 ATG

Answer 9

Benzamides

• sulpirid
• tiaprid
• amisulprid

Question 10

2nd generation antipsychotics

-partial AG

Answer 10

Aripiprazole

• in animal experiments it works as a :
• -D2 ATG in models of dopaminergic hyperactivities
• -D2 AG in models of dopaminergic hypoactivities
• -5HT2 ATG
• -5HT1A PA

dopamine serotonin system stabilizer

Question 11

adverse effects

Answer 11

1. hyperprolactinemia
   2.neuroleptic malignant syndrome
   3.agranulocytopenia
   4.weight gain
   5.cardiovascular side effects
   (myocarditis, QT prolongation, arrythmia)