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)
Antipsychotics used in acute cases, IV injection
Haloperidol (1st gen - IM)
Aripiprazone (2nd gen IM)
Tiaprid (2nd gen, IV or IM)
Antipsychotics side effects (both 1st and 2nd generation)
- 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
Antipsychotics more prone to cause weight gain.
Why.
Olanzapine and clozapine (both SGAP)
Due to H1 and 5HT2c receptor blockade.
clozapine specific side effects
Agranulocytosis
Weight gain (clozapine and olanzapine especially)
Myocarditis
Seizures - lowers seizure treshold.
Indications of 1st generation antipsychotics
- Acute psychosis - haloperidol, promethazine
- Antiemetic, peri-op: promethazine
- Neurolept analgesia: droperidol+fentanyl (analgesic)
- Neurolept anesthesia: droperidol+fentanyl+N2O
Indications of 2nd generation, atypical antipsychotics
- chronic treatment of schizo, or other psychotic diseases
- Acute mania - given until lithium effect develops
- Schizoaffective disorders
- Alcoholic agitation, or psychotic reaction
