Antipsychotics Flashcards
First Generation Antipsychotics (FGAs)- Available Drugs
Phenothiazines: CHLORPROMAZINE (THORAZINE) thioridazine fluphenazine trifluoperazine pephenazine
Thioxanthines:
THIOTHIXENE
Butyrophenones:
HALOPERIDOL (HALDOL) = least cholinergic, adrenergic, and histaminergic side effects; greatest risk of dopaminergic side effects
FGAs- Absorption, Distribution
- incomplete GI aborption with PO
- first pass metabolism
- 90% protein bound
- unbound can cross BBB
FGAs- Elimination
half life ~20hrs
steady state in 4-7days
FGAs- Clinical Use
Adults:
Schizophrenia
bipolar
agitation associated with schizophrenia or bipolar
Children:
schizophrenia
autism
Everyone:
major depression with psychosis
Medical illnesses- delirium, dementia
substance induced psychosis
FGAs- Side Effects/Contraindications
Side effects due to DOPAMINE on:
NIGROSTRIATAL TRACT-
EPS
TARDIVE DYSKINESIA
TUBEROINFUNDIBULAR- HYPERPROLACTINEMIA SEXUAL & MENSTRUAL DYSFUNCTION GYNECOMASTIA DECREASED BONE DENSITY
RARELY NEUROLEPTIC MALIGNANT
SYNDROME (HYPERTHERMIA, MUSCLE RIGIDITY, HIGH HR, HIGH BP)
MUSCARINIC- BLURRED VISION DRY MOUTH URINARY RETENTION CONSTIPATION CONFUSION
NO ABSOLUTE CONTRAINDICATIONS
-can increase and decrease levels of various antipsychotics
Histamine-
sedation, weight gain
Adrenergic-
orthostatic hypotension, fall risk
Second Generation Antipsychotics (SGAs)- Available Drugs
RISPERIDONE QUETIAPINE ASENAPINE OLANZAPINE ZIPRASIDONE PALIPERIDONE LURASIDONE
CLOZAPINE
ARIPIPRAZOLE (ABILIFY)
SGAs- Mech of Action (EXCEPT ARPIPRAZOLE)
D2 antagonists
some effects on muscarinic M1, Histamine H1, adrenergic alpha1, and serotonin 5-HT1A, 2A, 2C receptors
- each drug has different affinity profile
Aripiprazole- Mech of Action
Partial D2 agonist
dopamine system stabilization
SGAs- Absorption, distribution
incomplete GI absorption with PO
first pass metabolism
90% protein bound
unbound can cross BBB
SGAs- Elimination (EXCEPT ARPIPRAZOLE)
Half life ~20hrs
steady state in 4-7days
Aripiprazole- Elimination
half life ~75hrs
SGAs- Clinical Use
Adults:
Schizophrenia
bipolar
agitation associated with schizophrenia or bipolar
Children:
schizophrenia
autism
Everyone:
major depression with psychosis
Medical illnesses- delirium, dementia
substance induced psychosis
Clozapine- Notes
THIRD LINE AGENT
GREATER EFFICACY WITH PATIENTS NON-RESPONSIVE TO OTHER ANTIPSYCHOTICS
GREATER EFFICACY IN TREATING NEGATIVE SYMPTOMS OF SCHIZOPHRENIA
LOWERS RISK OF SUICIDE
HUGE SEROTONIN:DOPAMINE RATIO
RISPERIDONE- Side Effects/Contraindications QUETIAPINE ASENAPINE OLANZAPINE ZIPRASIDONE PALIPERIDONE LURASIDONE
Side effects due to dopamine on:
nigrostriatal tract-
EPS
tardive dyskinsesia
Tuberoinfundibular- hyperprolactinemia sexual & menstrual dysfunction gynecomastia decreased bone density
RARELY NEUROLEPTIC MALIGNANT SYNDROME (hyperthermia, muscle rigidity, high HR, high BP)
METABOLIC SYNDROME-
WEIGHT GAIN, DIABETES
Muscarinic- blurred vision dry mouth urinary retention constipation confusion
NO ABSOLUTE CONTRAINDICATIONS
-can increase and decrease levels of various antipsychotics
Histamine-
sedation, weight gain
Adrenergic-
orthostatic hypotension, fall risk
Clozapine- Side Effects/Contraindication
AGRANULOCYTOSIS METABOLIC SYNDROME low seizure threshold sedation hypotension
NO ABSOLUTE CONTRAINDICATIONS
- increase and decrease levels of various antipsychotics
- combined with carbamazepine increases risk of agranulocytosis
