Antipsychotics

Question 1

what is schizophrenia?

Answer 1

chronic psychotic disorder c:

• disturbed behavior
• thinking
• emotions
• perceptions

Question 2

what are some schizo (+) sx’s?

Answer 2

1. hallucinations/delusions
2. thought disorder
3. perceptual disturbances
4. incongruous mood
5. increased motor function

Question 3

what are some schizo (-) sx’s?

Answer 3

1. blunted affect
2. poverty of speech
3. diminished motivation
4. social withdrawal

Question 4

what are some cognitive sx’s of schizo?

Answer 4

deficits in memory and cognitive control of behavior

Question 5

schizo (+) sx’s biological basis?

Answer 5

linked to overactivity of mesolimbic pathway.

Question 6

Schizo (-) and cognitive sx’s biological basis?

Answer 6

hypoactivity of the mesocortical pathway

Question 7

what is the dopamine hypothesis of schizo?

Answer 7

excessive dopaminergic activity plays a role.
rx’s increase activity = increase/produce (+) psychotic sx’s
- ex) amphetamine and cocaine
rx’s decrease activity = decrease/stop (+) sx’s.

Question 8

what are 4 well-defined dopamine pathways in the brain?

Answer 8

1. mesolimbic pathway
2. nigrostriatal pathway
3. mesocortical pathwya
4. tuberoinfundibular pathway

Question 9

describe mesolimbic pathway

Answer 9

midbraine to limbic system.
role: emotional behaviors
hyperactive = (+) psychotic sx’s
block D2 receptors = antipsychotic effects

Question 10

describe nigrostriatal pathway

Answer 10

substantia nigra to basal ganglia
role: controls motor movements
block D2 recpetors = disorders of movement can appear
part of extrapyramidal nervous system.
- blck dopamine recpetors can give motor a.e AKA extrapyramidal rxns.

Question 11

describe mesocortical pathway

Answer 11

midbrain to prefrontal cortex.
reduce activity = (-) and cognitive sx’s.
block D2 recptors = cause/worsen sx’s

Question 12

Describe tuberoinfundibular pathway

Answer 12

hypothalamus to anterior pituitary.
dopamine released from these neurons inhibits prolactin secretion.
when blocked = prolactin level rise, can cause galactorrhea.

Question 13

what are some classical antipsychotic drugs?

Answer 13

1. chlorpromazine
2. fluphenazine
3. haloperidol
4. thioridazine

Question 14

what are some atypical antipsychotic drugs?

Answer 14

1. clozapine
2. risperidone
3. olanzapine
4. quetiapine
5. ziprasidone
6. aripiprazole
7. paliperidone

Question 15

what are HIGH potency classical antipsychotic drugs?

Answer 15

1. fluphenazine

2. haloperidol

Question 16

what are LOW potency classical antipsychotic drugs?

Answer 16

1. chlorpromazine

2. thioridazine

Question 17

1. chlorpromazine
2. fluphenazine
3. haloperidol
4. thioridazine

MOA?

Answer 17

block D2 receptors in the mesolimbic pathway

Question 18

what are atypical antipsychotics drugs?

Answer 18

they have higher affinities for other receptors than D2 receptors

ex)

1. clozapine: high affinity for D1, D4, 5HT2, musc, and a-adrenergic
2. risperidone: 5HT2

Question 19

what are some common properties of atypical antipsychotics?

Answer 19

1. dual antagonism at 5HT2A and D2
2. part of action is d/t 5HT block
3. less likely to cause EPRs than classical agents
4. less likely to cause tardive dyskinesea
5. less likely to cause increases prolactin
6. more effective at treating (-) sx’s
7. effective in refractory populations

Question 20

properties of clozapine?

Answer 20

prototype of the atypical agents

Question 21

properties of risperidone?

Answer 21

causes EPR, rare at therapeutic doses

Question 22

properties of paliperidone?

Answer 22

9-hydroxyrisperidone, active metabolite of risperidone

Question 23

properties of aripiprazole?

Answer 23

partial agonist at D2 and 5HT1A

antagonist at 5HT2A

Question 24

what are two atypical antipsychotics least likely to induce EPR?

Answer 24

1. clozapine

2. quetiapine

Question 25

antipsychotics actions?

Answer 25

- reduce hallucination/agitation - calming effect - don't depress intellectual function - motor incoordination is minimal - onset is

Question 26

antipsychotics antiemetic effects?

Answer 26

block D2 receptors of the chemoreceptor trigger zone in the medulla. exceptions: aripiprazole and thioridazine (no antiemetic)

Question 27

antipsychotic metabolisM?

Answer 27

CYP2D6, CYP1A2, CYP3A4 don't interfere c the metabolims of other drugs.

Question 28

causes of antipsychotic extrapyramidal rxns?

Answer 28

- assoc c high D2 potency. - - rx: haloperidol and fluphenazine less likely with: 1. low D2 potency: clorpromazine or thioridazine 2. strong anticholinergic: thioridazine and chlorpromazine 3. atypical antipsychotics

Question 29

what are some Extrapyramidal rxns?

Answer 29

1. parkinsonism 2. dystonia 3. akathisia

Question 30

tx for parkinsonism?

Answer 30

antimuscarinics: 1. benztropine 2. trihexyphnidyl 3. diphenhydramine 4. amantadine Levodopa should never be used in these pts.

Question 31

tx for dystonia?

Answer 31

1. benztropine 2. trihexyphenidyl 3. diphenhydramine

Question 32

tx for akathisia?

Answer 32

1. reduction of dosage or change rx 2. clonazepam 3. propranolol.

Question 33

what is tardive dyskinesia?

Answer 33

late-occuring syndrome of abnl chreoathetoid movements. unwanted effect of antipsychotics potentially irreversible may be d/t dopamine receptor up-regulation

Question 34

management of tardive dyskinesia?

Answer 34

1. d/c or reduce rx. 2. eliminate all rx's c central anticholinergic action (antiparkinsonian and TCAs) 3. diazepam clozapine is rec'd for pts c tardive dyskinesia who require antipsychotics.

Question 35

what is neuroleptic malignant syndrome?

Answer 35

rare and life-threatening disorder. - rigidity, tremor, hyperthermia - altered mental status - autonomic instability - elevated WBC and CK - myoglobinemia c potential nephrotoxicity

Question 36

tx of neuroleptic malignant syndrome?

Answer 36

1. dantrolene | 2. bromocriptine

Question 37

what antipsychotics cause sedation?

Answer 37

low-potency and atypical agents d/t block central H1 receptrs.

Question 38

which antipsychotics cause seizures?

Answer 38

1. chlorpromazine | 2. clozapine

Question 39

how can antipsychotics produce autonomic effects?

Answer 39

block musc receptors, producing anticholinergic effects. 1. block alpha1 receptors = orthostatic hypotension, impaired ejaculation.

Question 40

which antipsychotics cause toxic and allergic rxns?

Answer 40

clozapine causes agranulocytosis | regular blood cell counts are mandatory.

Question 41

what are some endocrine and metabolic effects c antipsychotics?

Answer 41

1. prolactin secretion (less c atypical) - block D2 recpetors in pituitary. - women: amenorrhea-galactorrhea, infertility - men: loss libido, infertility and impotence 2. weight gain - majority atypical

Question 42

which antipsychotics cause high incidence of cardiac toxicity?

Answer 42

1. thioridazine (QTc- and T-wave changes) | 2. ziprasidone (prolong QTc)

Question 43

which antipsychotics cause ocular complications?

Answer 43

1. chlorpromazine - deposits in corean and lens. | 2. thioridazine - retinal deposits.

Question 44

what are some psychiatric indications for antipsychotics?

Answer 44

1. schizo 2. bipolar 3. suppression of tics in tourretts 4. control disturbed behavior in alzheimers 5. adjuncts to antidepressants in tx-resistant major depression. 6. combo c antidepressants in psychotic depression 7. irritability assoc c autism (DOC risperidone)

Question 45

what are some non-psychiatric indications for antipsychotics?

Answer 45

1. nausea and vomiting | 2. droperidol is used in combo c fentanyl in neurolept-anesthesia

Question 46

what are DOC for antipsychotics?

Answer 46

1. atypical preferred d/t: - benefit (-) sx's and cognition - diminished risk of EPRs and tardive dyskinesia - lesser increase in prolactin levels. 2. risperidone - most prescribed 3. clozapine - d/t potential for agranulocytosis is reserved for refractory pts.

Question 47

antipsychotic in pregancy?

Answer 47

cat C clozapine is catB risks (greater c atypicals): 1. hyperglycemia 2. weight gain

Question 48

define psychosis?

Answer 48

sustained mental state of impaired contact c reality