Antipsychotics

Front 1

Antipsychotics are prescribed for 3 different psychoses:

Back 1

1. schizophrenia (chemically-induced or organic)
2. mania
3. organic mental disorder (OMD)

Front 2

DA hypothesis of schoizophrenia

Back 2

1. drugs that block DA receptors (DA antagonists) are therapeutically effective in alleviating psychotic symptoms
2. sympathomimetic drugs such as amphetamine, which release DA, can induce psychosis

Front 3

As a class of drugs, the antipsychotics are generally:

Back 3

1. orally administered (IM for certain drugs)
2. 95-98% plasma protein bound
3. subject to extensive "first pass" mechanism
4. drugs with long "half-lives" (chlorpromazine -T1/2=30 hours)
5. 70% of patients respond to conventional drugs

Front 4

Neuroleptic syndrome includes effects such as:

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1. sedation
2. emotional quieting
3. psychomotor slowing
4. affective indifference

Front 5

Positive symptoms of schizophrenia

Back 5

mania
delusion
paranoia

Front 6

Negative symptoms of schizophrenia

Back 6

flattened affect
catatonia
depressive like symptoms

Front 7

3 types of Typical antipsychotics

Back 7

1. Phenothiazines
2. Butryrophenone
3. Thioxanthenes

Front 8

Phenothiazines

Back 8

typical antipsychotics

predominantly DA type 2 antagonists, with varying degrees of selectivity

1. Aliphatics
2. Piperdines
3. Piperazines

Front 9

Aliphatics

Back 9

typical antipsychotics
low affinity D2 angats that pose an increased risk for autonomic side effects
1. chlorpromazine (Thorazine)
2. promazine (Sparine)- least effective of the aliphatics
3. trifluorpromazine (Vesprin)

Front 10

Piperdines

Back 10

typical antipsychotics

have comparitively high affinity for the D2 receptor (intermediate)

mesoridazine (serentil)-rarely given because they have a black box warning against cardiotoxicity
thioridazine (Mellaril)

Front 11

Piperazines

Back 11

typical antipsychotics

high affinitye D2 antags that pose an increased risk for extrapyriamidal side effects; least sedating (parkinson like effects)

1. fluphenazine (Prolixin)- decanoate formulation available
2. perphenazine (Trilafon)
3. trifluoperazine (Stelazine)

Front 12

Butryophenone

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haloperidol (Haldol)

has high to intermediate affinity for the D2 receptor and poses increased risk of extrapyrimidal side effects; decanoate formulation available

widely used; "depot" injection- can put a reservoir of drug in muscle and will last for a month

Front 13

Thioxanthenes

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typical antipsychotic; also have potent D2 antag properties

1. chlorprothixene (Taractan)
2. thiothixene (Navane)

Front 14

Partial DA receptor agoist

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aripiprazole (Abilify)

partial agonist should reduce incidence of neurolepsis, parkinsonism-like effects and potential for tardive dyskinesia that can occur with the D2 receptor antags

Front 15

Atypical antipsychotics

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do not have prominent D2 angat profiles, which reduces the potential for tardive dyskinesia and drug-induced parkinsonism

1. Dibenzodiasepines
2. Benzisoxazole
3. Other herterocyclic antipsychotics

Front 16

Dibenzodiazepines

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atypical antipsychotic; heterocyclic compounds that have extraordinarliy mixed receptor binding profiles

1. clozapine (Clozaril)- helps those with neg. antipsychotic symptoms; risk for agranulocytosis (with chronic tx, myocarditis and cardiomyopathy)
2. loxapine (Loxitane)- less risk for agranulocytosis
3. olanzapine (Zyprexa)- does not pose the same risk of agranulocytos as clozapine; may cause sleepwalking

Front 17

Benzisoxazole

Back 17

atypical antipsychotic; relatively selective 5-HT2A receptor antag, but at higher doese (>10 mg) has haloperidol-like effects

1. risperidone (Risperdal)
2. ziprasidone (Geodon)- IM and used in ER

Front 18

Other heterocyclic antipsychotics

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atypical antipsychotics

1. molindone (Moban)
2. pimozide (Orap)- also indicated for the tx of severe tics and Tourette's
3. quetiapine (Seroquel)

Front 19

Many antipsychotics block these receptors:

Back 19

muscarinic receptors
alpha adrenergic
histamine

increases sedation and weight gain

Front 20

most common side effects of antipsychotic meds

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1. akathisias- "nervous energy" (contribute to noncompliance)
2. parkinsonism
3. dystonias, dysinesias and akinesias- disorders of muscle tonicity and mvmt.
4. tardive dyskinesias- probably most serious of drug induced extrapyrimidal side effects
5. neuroleptic malignant syndrome- can occur at therapeutic dises
6. blood abnormalities- including fatal agranulocytosis
7. endocrine abnormalities- increased serium prolactin (amenorrhea, gynecomastia, false-positive pregnancy tests)
8. cardio effects- orthostatic htn

Front 21

Neuroleptic malignant syndrome

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occurs in 1% of the patients taking antipsychotic drug therapy; 20-30% of these may die from it
1. can occur at therapeutic doses
2. can be seen within hours of starting tx, or after months of tx
3. symptoms include:

muscular rigidity
impaired breathing or ventilation
autonomic hyperactivity
extremely high temps.

Front 22

Drug interactions with antipsychotics

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1. potentiation of other CNS depressants like alcohol
2. interaction with OTC meds like antihistamines

Front 23

contraindications for "typical" antipsychotic therapy

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1. blood dyscrasias
2. parkinsonism
3. chronic alcoholism
4. liver disease