Antipsychotics Flashcards
1st generation antipsychotics in general
=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)
Early EPS
and management.
Parkinsonian symptoms (hours) - bradykinesia, resting tremor
Dystonia (days) - involuntary movements, sustained muscle contractions
Akathesia (weeks) - cannot sit still
management: anticholinergic drugs; atropine, procyclidine, piperidine
Late EPS
Perioral tremor (management: anticholinergics) Tardive dyskinesia - choreo-attatoid movements (irreversible)
chlorpromazide
(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.
Promethazine
1st gen. AP
Strong H1 ATG effect
I: anti-emetic (peri-op). not used
thioridazine
(color theory) low potency. FGAP
not used anymore
SE: QT prolongation, retinal deposits!
Fluphenazine
(kid trying to FLY). FGAP
high potency, high EPS risk. less alpha and H1 blockade.
I: depot injection in patients with low compliance.
Trifluoperazine
(kid TRYIng to fly). high potency FGAP.
Haloperidol
FGAP. High potency.
receptorial affinity: D2>D1=D4>alpha1>5-HT2.
high risk for EPS
I: Acute psychosis, acute mania
Droperidol
middle potency FGAP.
neurolept analgesia: droperidol+fentanyl(an opioid).
2nd generation antipsychotics, general
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
mixed ATG second generation antipsychotics
Clozapine (closet) Quetiapine (quiet) Olanzapine (only) Risperidone (whispering) sertendine/sertindol Ziprasidone (zipper)
Clozapine
(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.
Olanzapine
(only)
High potency SGAP.
SE: weight gain - metabolic syndrome. DM, hypertension.
Quetiapine
(quiet)
SGAP.
Have less anticholinergic effect.
Risperidone
(Whispering) high potency SGAP. High dose: fall in BP, have highest risk for EPS among the 2nd gen drugs. Metabolite: Paliperidon Intramuscular depot injection.
Sertindone/Sertindol
SGAP
SE: BP fall (alpha 1 blocking effect), QT prolongation (cardiotoxic)
Less sedative
Ziprasidone
(zipper) SGAP.
Partial AG on 5HT1A - anxiolytic. 5HT2>D2
QT prolongation, less weight gain
Second generation antipsychotics - selective D2, D3 antagonists
These compounds have no effect on D1 receptors - effective against negative symptoms. Sulpirid Amisulpirid Tiaprid Cariprazin
Sulpirid, Amisulpirid
SGAP - selective ATGs (D2, D3 blockers)
Sulpirid - withdrawn
Amisulprid - Inidated in chronic tr. of psychosis
Tiaprid
SGAP - selective ATGs (D2 and D3 blockers)
I: treatment of psychosis in alcoholics, psychosis tr.
Cariprazin
SGAP. slective ATG (D2, D3 blockers)
D3>D2. Better effect on negative sy., and cognitive dysfunctions.
Was developed by a guy working in semmelweis
Aripiprazole
(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
Antipsychotics available as intramuscular depot injection
Fluphenazine (1st gen)
Risperidon (2nd gen)
