Antipsychotic Medications
Treat the negative and/or positive symptoms of psychotic illnesses.
Neuroleptics
Chlorpromazine (Throazine)
Haloperidol (Haldol)
Mellaril (Thioridazine)
Prolixin (Fluphenazine)
Phenothiazines
Chlorpromazine (Throazine)
First antipsychotic - a neuroleptic
Blocks dopamine centrally and increases dopamine synthesis; has a molecular configuration similar to dopamine.
Efficacy correlates with ability to block dopamine in mesocortical and mesolimbic dopaminergic systems
Most
Haloperidol (Haldol)
most commonly used; Similar to chlorpromazine except not as sedating.
Often used as part of emergency treatment.
Alleviates positive symptoms but not negative symptoms.
Mellaril (Thioridazine)
EPS - yes.
May cause retinitis pigmentosa in high doses.
Prolixin (Fluphenazine)
EPS - yes.
Can be given by periodic injection; some side effects have rapid onset.
Phenothiazines
Used for:
Nausea, vomiting; Hiccoughs; Sedation; Relieve severe itching; Manage symptoms of acute mania, alcoholic hallucinosis
Nonneuroleptics
new generation" - novel antipsychotics.
Treat positive and negative symptoms; have fewer side effects. Meaningful research from 1975-1990
Clozaril (Clozapine)
Risperidone (Risperdal)
Zyprexa (Olanzapine)
Quetiapine (Seroquel)
Ziprasidone (geodon)
Aripipr
Clozaril (Clozapine)
Very popular in Europe and then taken off the market after issues in Finland.
Up to 60% of treatment resistant patients benefited from this drug - most effective!
Greater effect on mesocortical/mesolimbic dopamine systems than on basal ganglia; has blocki
Risperidone (Risperdal)
1994. May be used for first episode of schizophrenia.
Treats positive and negative symptoms.
Side effects - orthostatic hypotension; Doesn't cause agranulocytosis, little sedation, few anticholinergic side effects.
Zyprexa (Olanzapine)
Diminishes both positive and negative symptoms.
Side effects similar to resperidal -
Anticholinergic due to effect on muscarinic receptors; Somnolence due to effect on histaminic receptors; Orthostatic hypotension due to alpha adrenergics; Low EPS, some T
Quetiapine (Seroquel)
Low propensity to produce EPS; Low prolactin levels.
Similar to Clozaril in affinity for serotonin; Reasonable efficacy; some side effects.
Ziprasidone (Geodon)
Targets same DA receptors as other novels
May improve thinking and motivation
For mania and schizophrenia; effects on dopamine and serotonin
Rarely causes abnormal movements; Does not cause weight gain; May cause insomnia and fatigue; May have marginal ef
Aripiprazole (Abilify)
Affects both positive and negative symptoms
Many side effects.
Extrapyramidal Side Effects
Extrapyramidal System - descending fivers arising in cortical and subcortical motor centers that reach medulla and spinal cord by non-pyramidal pathways; maintains equilibrium and muscle tone.
Pseudoparkinsonian
Dystonias
Akathesias
Tardive dyskinesia
EPS: Pseudoparkinsonian
Mask-like faces; Tremor at rest; Cogwheel rigidity; Shuffling gait; Stooped posture
Major symptoms=tremor, rigidity, bradykinesia
EPS: Dystonias
Impaired/disordered muscle tone; Broad range of bizarre movements in tongue, face, neck; Buccofacial movements
Sialorrhea, torticollis, oculogyric crisis, opisthotonous.
Laryngospasm***
Occurs in early treatment; hypocalcemia reduces CNS ability to counte
EPS: Akathisia
Characterized by motor restlessness, great urge to move around, difficult to sit still
Most common, most important side effect in psychopharmacologic treatment;
Causes nonadherence and Increased suicide risk. Cogentin not effective.
EPS Tardive Dyskinesia
Characterized by movements of neck, shoulders, dramatic hip jerks, rocking, twisting, squirming, pelvic gyrations and thrusts.
Bizarre facial movements: blinking, smiling, grimacing, frowning, puckering, blowing, protruding tongue, rabbit tremor, chewing
Neuroleptic Malignant Syndrome (NMS)
Side effect of all neuroleptics (in young men) and Zyprexa (in elderly women).
Caused: decreased dopaminergic activity secondary to drug- induced dopamine blockade.
Onset 45 minutes - 65 days after beginning meds.
NMS Symptoms and treatment
Lead pipe rigidity, Elevated temperature , Fluctuating consciousness, Labile vital signs, Diaphoresis, Dysphagia, Tremor, Mutism, Incontinence
Lab evidence of muscle injury - Creatine kinase, leukocytosis
This is medical emergency. Lethal in 18%
Tx: Stop