Glossary of Antipsychotic Agents
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- What types of symptoms do you find in schizophrenia?
- Positive and negative
- What are the positive symptoms in schizophrenia?
- What are the negative symptoms in schizophrenia?
- Flattened affect
don't initiate behaviors
- What is schizophrenia?
- A disorder in which though processes diverge from reality. May manifest d/o of perception, thinking, speech, emotion or physical activity.
- What is the drugs used to treat psychotic (schizophrenia)?
- What are the signs and symptoms of a neurotic disorder?
- Anxiety, dissatisfaction, feelins of inferiority and frustration, apathy or agitation and hostility
- What are the drugs used for treatment of neurotic d/o's?
- Anxiolytics: Benzodiazepines, Buspirone, SSRI
- What are the signs and symptoms of the depressive affective d/o?
- Disturbances of mood (low self-esteem and guilt), loss of feeling, low level of motivation
- What is the treatment for depression?
- SSRI's, TCA
Monoamine oxidase inhibitors: atypical antidepressants
- What are the signs and symptoms of the manic affective d/o?
- Hyperactivity, ease of enjoyment, unrealistic optimism with acting out, aggressiveness
- What is the treatment for mania?
- Lithium, valproate, carbamezepine, antipsychotics
- What are biological theories?
- Theories which postulate neurochemcial defect as the basis of mental d/o.
- What is the biogenic amine hypothesis?
- Innappropriate amounts of amine neurotransmitters (NE, dopamine, serotonin) in CNS leads to inappropriate behavior.
- What is the biogenic amine hypothesis based on?
- Drug effects
- What do antidepressants do to receptors?
- It increases levels of NE, 5HT (serotonin)
- What is depression caused by?
- Too little NE, 5HT
- What happens if dopamine is increased and unregulated?
- Causes pychosis
- What does antipsychotics do to the receptors?
- Blocks dopamine receptors
- What are the "typical" agents used to treat psychoses?
- Chlorpromazine (Thorazine)
Fluphenazine (Permitil, Prolixin)
- What are the "atypical" agents used to treat psychoses?
- Loxapine (Loxitane)
- What does it mean if it is "atypical"?
- Their mechanism of action is not typical (or binding to receptor) and it will produce different side effects from the typical drugs.
- What is the advantages and disadvantages of chlorpromazine?
- Adv.-Generic and inexpensive
Disadv.-many adverse effects, esecially autonomic
- What is the adv/disad of Thioridazine?
- Adv. slight EPS, generic
Disadv.-800 mg/d limit; no parenteral form, cardiotoxic
- What is the adv./diadv. of Fluphenazine?
- Adv.-Depot form also avialable
Disadv.-Increases tardive dyskinesia
- What is the adv/disad of Thiothixen?
- Parenteral form also available; decreased tardive dyskenesia
- What is the adv/disad of Halperidol?
- Adv.-Parental form also available;generic
- What is the adv/disad of Loxapine?
- Adv.-no weight gain
- What is the adv/disad of Clozapine?
- Adv.-May benefit treatment-resistant patients; little EPS toxicity
Disadv.-May cause agranulocytosis; wt gain, hyperglycemia, diabetes, dyslipidemia
- What is the adv/disad of Risperidone?
- Adv.-broad efficacy; little or no EPS dysfunction at low doses
Disadv.-may cause EPS or hypotension with higher doses; wt gain, hyerglycemia, diabetes, dyslipidemaia
- What is the adv/disad of Olanzapine?
- Adv.-effective against neg. as well as pos. symptoms; little or no EPS
Disadv.-wt gain, hyperglycemia, diabetes, dyslipidemai, cataracts (?)
- What is the adv/disad of Queitapine (Seroquel)?
- Adv.-little or no EPS
Disadv.-Wt gain, hyperglycemia, diabetes, dyslipidemia, cataracts?
- What is the adv/disad of Ziprasidone?
- Adv.-less et gain than other atyipicals
Disadv.-Prolongs QT interval, but no arrhythmias reported yet, somnolence, some EPS
- What is the adv/disad of Aripiperazole?
- Adv.-little or no EPS, less wt gain, or QT changes
Disadv-Akathesia, insomnia, anxiety; cautin in patient siwth epilepsy or Alz.
- What are the receptor interactions of antipsychotic drugs?
- All block D2 but the importance of this in relation to other receptor actions varies from drug to drug. Many receptors are involved.
- What is the receptor binding profile of Chlorpromazine?
- A1 = 5HT2 > D2 > D1
- What is the receptor binding profile of haloperidol?
- D2 > D1 = D4 > A1 > 5 HT2
- What is the receptor binding profile of Clozapine?
- D4 = A1 > 5HT2 > D2 = D1
- What is the difference between atypicals and typicals in regards to potency and receptors?
- Atypicals tend to be less potent at D2 receptors and much more potent at 5 HT2 and D4 receptors
- What is Aripiprazole?
- partial agonist at D2 and 5HT1a, claimed to be a new generation of antipsychotics
- What happens if you block the D2 receptors in a schizophrenic patient?
- Allevites positive symptoms (tension, hostility, hyperactivity, combativeness, hallucinations, delusions, insomnia, and anorexia)
- What happens if you block D4 nd 5HT2 receptors in a schizophrenic patient?
- Alleviate the negative symptoms (apathy, withdrawal, unresponsivesness)
- What are the 2 dopamine pathways that are important in relieving psychotic symptoms?
- Which 2 pathways contribute to the side effects of antipsychotics?
- What are the neurological side effects of antipyschotic agents?
- Acute dystonia
- What are some of the important side offects of antipsychotics?
Neurological Malignant Syndrome
Late onset (can't treat)
- What are the features of acute dystonia?
- Spasm of muscles of tongue, face, neck, back; may mimic seizures; not hysteria
- How do you treat acute dystonia?
- Antiparkinsonian agents are diagnostic and curative
- What are the features of akathisia?
- Motor restlessness; not anxiety or agiatation
- What is the treatment of akathisia?
- Antiparkinsonian agents, diphenhydramine, benzodiapines, or propranolol
- What are the features of the side effect Parkinsonism?
- Bradykinesia, rigidity, variable tremor, mask facies, shuffling gait
- What are the features of neurologic malignant syndrome (NMS)?
- Catatonia, stupor, fever, unstable BP, myoglobinemia: can be fatal
- Treatment of NMS?
- Stop antipsychotic immmediately: dantrolene or bromcriptinemay help; antiparkinsonian agents NOT effective
- What is late onset side effects?
- Perioral tremor "rabbit syndrome" and Tardive dyskinesia
- How do you treat perioral tremor?
- Antiparkinsonian agents sometimes help
- What are the features of tardive dyskinesia?
- Oral-facial dyskinesia; widespread choreoathetosis or dystonia
- Treatment of tardive dyskinesia?
- Prevention is crucial; clozapinen or olanzapine may help
- What areas of the CNS are affected with side effects from antipsychotics?
- Basal ganglia
Medullary chemoreceptor trigger zone (CTZ)
- What do you see from the basal ganglia SE?
- Parkinson-like extrapyramidal effects which is caused by blocking D2
- What do you see from hypothalamus?
- Increased prolactin secretion; temperature regulation (usually cold)
- What do you see from the CTZ?
- antiemetic action; DMV-increased eating from vagus nerve stimulation; weight gain
- Do you see weight gain with typicals or atypicals?
- What effects do you see in the autonomic nervous system from antipsychotics?
- Peripheral cholinergic block, alpha adrenergic block
- What changes do you see in endocrine system?
- Alterations in secretion of many hormones
- What effects do you see in the CVS?
- Direct depressant effect on the heart, direct vasodilation plus indirect effects due to ANS effects --> decreased BP
- How are antipsychotics metabolized?
- Liver--oxidation and glucruonide conjugation; some active metabolites formed
- How are antipsychotics eliminated?
- Reneal excretion
T 1/2 is 10-20 hours and biological effects last 24 hours or more
- How is antipsychotics absorbed?
- Absorption after oral administraion tends to be erratic and unpredictable
- What are the most serious adverse reactions to antipsychotic drugs?
- EPS and orthostatic hypotension
- What are the early onset adverse reactions?
- Parkinson syndrome
Acute dystonic reactions
- What are the late onset adverse reactions?
- Tardive dyskinesia
- Why do you see orthostatic hypotension in antipsychotic agents?
- Peripheral alpha blockade
- What blood disorders are adverse reactions?
Agranulocytosis (particualry clozapine)
- What is Neuroleptic Malignant Syndrome (NMS)?
- severe muscular hypertonicity, akinesia, dysarthria, fever and cardiovascular changes
- What are some other adverse effects of antipsychotic agents?
- Cholestatic jaundice
Rashes and photosensitivity
Cataracts?--examine eyes every 6 months
- What are some other autonomic side effects of antipsychotics?
- Sedation, nasal stuffiness, dry mouth, constipation, palpitation, skin reactions, arrhythmias (ziprasidone, thioridazine), weight gain, diabetes (atypicals), a risk of stroke in patients with dementia (risperidone and olanzapine)
- What are the therapeutic uses of antipsychotic drugs?
All agents improve positive symptoms
Atypicals will improve negative symptoms
Other neuropsychiatric diseases (Tourette's-Haloperidol or pimozide) and agitation associated with Alzheimer's Disease
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