Antipsychotics

Question 1

1st generation antipsychotics in general

Answer 1

=typical antipsychotics.
only work on + symptoms (no effect on - sympt)
more pronounced EPS
high number of non-responders.
mostly used acutely
have antiemetic effect (can be given perioperatively)

Question 2

Early EPS

and management.

Answer 2

Parkinsonian symptoms (hours) - bradykinesia, resting tremor
Dystonia (days) - involuntary movements, sustained muscle contractions
Akathesia (weeks) - cannot sit still

management: anticholinergic drugs; atropine, procyclidine, piperidine

Question 3

Late EPS

Answer 3

Perioral tremor (management: anticholinergics)
Tardive dyskinesia - choreo-attatoid movements (irreversible)

Question 4

chlorpromazide

Answer 4

(Color-pro), 1st generation AP. low potency. EPS risk++
indication: acute use. maintain hypothermia, hickups.
high affinity for M and alpha 1 receptors and H1 Rs.

Question 5

Promethazine

Answer 5

1st gen. AP
Strong H1 ATG effect
I: anti-emetic (peri-op). not used

Question 6

thioridazine

Answer 6

(color theory) low potency. FGAP
not used anymore
SE: QT prolongation, retinal deposits!

Question 7

Fluphenazine

Answer 7

(kid trying to FLY). FGAP
high potency, high EPS risk. less alpha and H1 blockade.
I: depot injection in patients with low compliance.

Question 8

Trifluoperazine

Answer 8

(kid TRYIng to fly). high potency FGAP.

Question 9

Haloperidol

Answer 9

FGAP. High potency.
receptorial affinity: D2>D1=D4>alpha1>5-HT2.
high risk for EPS
I: Acute psychosis, acute mania

Question 10

Droperidol

Answer 10

middle potency FGAP.

neurolept analgesia: droperidol+fentanyl(an opioid).

Question 11

2nd generation antipsychotics, general

Answer 11

less risk for EPS, act on both positive and negative symptoms. 
3 categories:
1)mixed ATG: dopamine and 5HT blockers
2) selective ATG: D2 and D3 blockers
3) partial AGs

other preceptorial effects, blocking effects:
- M-receptors
-Alpha1 Rs
- H1 receptors 
and D2 and 5HT2A

Question 12

mixed ATG second generation antipsychotics

Answer 12

Clozapine (closet)
Quetiapine (quiet)
Olanzapine (only)
Risperidone (whispering)
sertendine/sertindol
Ziprasidone (zipper)

Question 13

Clozapine

Answer 13

(closet). second gen. AP.
lowest risk of EPS.
I: resistant cases of psychological diseases, PD treatment induced psychosis, seizures
SE: agranulocytosis (blood count needed)
weight gain (especially), seizures, myocarditis, cardiomyopathy.
high muscarinic blocking effect.

Question 14

Olanzapine

Answer 14

(only)
High potency SGAP.
SE: weight gain - metabolic syndrome. DM, hypertension.

Question 15

Quetiapine

Answer 15

(quiet)
SGAP.
Have less anticholinergic effect.

Question 16

Risperidone

Answer 16

(Whispering)
high potency SGAP. 
High dose: fall in BP, have highest risk for EPS among the 2nd gen drugs.
Metabolite: Paliperidon
Intramuscular depot injection.

Question 17

Sertindone/Sertindol

Answer 17

SGAP
SE: BP fall (alpha 1 blocking effect), QT prolongation (cardiotoxic)
Less sedative

Question 18

Ziprasidone

Answer 18

(zipper) SGAP.
Partial AG on 5HT1A - anxiolytic. 5HT2>D2
QT prolongation, less weight gain

Question 19

Second generation antipsychotics - selective D2, D3 antagonists

Answer 19

These compounds have no effect on D1 receptors - effective against negative symptoms. 
Sulpirid
Amisulpirid
Tiaprid
Cariprazin

Question 20

Sulpirid, Amisulpirid

Answer 20

SGAP - selective ATGs (D2, D3 blockers)
Sulpirid - withdrawn
Amisulprid - Inidated in chronic tr. of psychosis

Question 21

Tiaprid

Answer 21

SGAP - selective ATGs (D2 and D3 blockers)

I: treatment of psychosis in alcoholics, psychosis tr.

Question 22

Cariprazin

Answer 22

SGAP. slective ATG (D2, D3 blockers)
D3>D2. Better effect on negative sy., and cognitive dysfunctions.
Was developed by a guy working in semmelweis

Question 23

Aripiprazole

Answer 23

(appropiate)
SGAP
Partial AG on D2 and 5-HT1A receptor, 5-HT2 R ATG. Schizophrenia (good effect on negative sy. due to 5-HT2 ATG), Anxiolytic effect (5-HT1A partial AG effect)
I: Schizophrenia, Mania (BP disorder), Dementia

Question 24

Antipsychotics available as intramuscular depot injection

Answer 24

Fluphenazine (1st gen)

Risperidon (2nd gen)

Question 25

Antipsychotics used in acute cases, IV injection

Answer 25

Haloperidol (1st gen - IM)
Aripiprazone (2nd gen IM)
Tiaprid (2nd gen, IV or IM)

Question 26

Antipsychotics side effects (both 1st and 2nd generation)

Answer 26

• EPS - mostly 1st gen.
• Neuroleptic malignant syndrome (haloperidol, risperidon (in case of depot injection))
• Hyperprolactinemia (FGAP>SGAP)
• Weight gain (olanzapine, clozapine)
• seizures (clozapine)
• heart: QT prolongation, decreased BP
• Atropine-like SE (dry mouth, constipation etc
• Retinal deposits (thioridazine)
• Agranulocytosis - cloazpine

Question 27

Antipsychotics more prone to cause weight gain.

Why.

Answer 27

Olanzapine and clozapine (both SGAP)

Due to H1 and 5HT2c receptor blockade.

Question 28

clozapine specific side effects

Answer 28

Agranulocytosis
Weight gain (clozapine and olanzapine especially)
Myocarditis
Seizures - lowers seizure treshold.

Question 29

Indications of 1st generation antipsychotics

Answer 29

• Acute psychosis - haloperidol, promethazine
• Antiemetic, peri-op: promethazine
• Neurolept analgesia: droperidol+fentanyl (analgesic)
• Neurolept anesthesia: droperidol+fentanyl+N2O

Question 30

Indications of 2nd generation, atypical antipsychotics

Answer 30

• chronic treatment of schizo, or other psychotic diseases
• Acute mania - given until lithium effect develops
• Schizoaffective disorders
• Alcoholic agitation, or psychotic reaction