Rx: Antipsychotics

Question 1

psychosis MOA

Answer 1

inc dopamine activity, as w/amphetamines, metylphenidate, or cocaine

Question 2

antipsychotics blocking D2 receptors have what effect?

Answer 2

relieve positive sx

Question 3

antipsychotics blocking 5HT2 receptors have what effect?

Answer 3

relieve negative sx

Question 4

antipsychotics blocking a1 receptors have what effect?

Answer 4

produce autonomic SEs, like orthostatic hypOTN and tachycardia

Question 5

antipsychotics blocking H1 receptors have what effect?

Answer 5

produce sedation

Question 6

antipsychotics blocking muscarinic receptors have what effect?

Answer 6

produce confusion and memory impairment, provides protection against EPS

Question 7

which antipsychotics show a lower affinity for D2 receptors and higher affinity for 5HT2 receptors?

Answer 7

atypical (2˚) antipsychotics

-lower affinity for D2 receptors reduces the risk of EPS

Question 8

potent antipsychotics

Answer 8

inc risk of EPS

Question 9

weak antipsychotics

Answer 9

additional sedative, hypOTN and autonomic SEs

Question 10

typical antipsychotics

Answer 10

dopamine D2 blockers, produce EPS, elevate PRL levels, equally effective but differ in potency/SEs, largely effective for positive sxs (e.g. delusions, hallucinations, disorganization of thought and behavior)

Question 11

atypical antipsychotics

Answer 11

D2 and 5HT2 antagonism, but addition of 5HT2 blockade may reduce EPS and improve efficacy for negative sx (e.g w/drawal, flat affect, paucity of thought, avolition)

Question 12

chlropromazine: structure

Answer 12

aliphatic side chain, low potency= lower incidence of EPS

Question 13

thiothixene: structure

Answer 13

piperidine ring, low potency= lower incidence of EPS

Question 14

fluphenazine, perphenazine: structure

Answer 14

piperazine, potent= higher incidence of EPS + weak anticholinergic

Question 15

haloperidol: structure

Answer 15

high potency

Question 16

atypicals: clozapine, olanzapine, quetiapine

Answer 16

low potency, have addtnl anti-serotonin effects –> tx neg sx

Question 17

which atypical acts like a typical antipsychotic?

Answer 17

risperidone, greater risk of EPS at high doses

*only approved agent for use in children and teens

Question 18

what its the active metabolite of risperidone?

Answer 18

paliperidone

Question 19

which risperidone has limited EPS?

Answer 19

ziprasidone

Question 20

what is unique about aripiprazole?

Answer 20

PARTIAL AGONIST for dopamine receptors rather than an antagonist, 5HT2A antagonist, 5ht1A partial agonist
-lower incidence of SEs

Question 21

neuroleptic syndrome

Answer 21

suppression of spontaneous movements and complex beh, reduced initiative and interest in environ, dec manifestations of emotion or affect, psychotic sx disappear over time

Question 22

which class of drugs can cause neuroleptic syndrome?

Answer 22

antipsychotics

Question 23

limbic system

Answer 23

thought to be site of antipsychotic effects, dopamine system adapts to long-term therapy, Anticholinergics do not block therapeutic effect

Question 24

basal ganglia

Answer 24

dec dopamine=dec EPS, like limbic system dopamine will adapt (initially inc dopamine metabolism, synthesis, and firing rate); anticholinergics block anti-psychotic induced inc in DA turnover in basal ganglia, and thus block many sx of EPS
*antipsychotic effect not thought to occur here

Question 25

early EPS effects

Answer 25

acute dystonia, aka thesis, parkinsonian syndrome, neuroleptic malignant syndrome

Question 26

later EPS effects

Answer 26

perioral tremor, tardive dyskinesia

Question 27

acute dystonia: sx

Answer 27

muscle spasms: facial grimacing, torticollis (stiff neck), oculogyeric crisis

Question 28

acute dystonia: tx

Answer 28

anticholinergic antiparkinsonian agents (like benztropine)

Question 29

acute dystonia: onset

Answer 29

usually occur w/in the first 5 days

Question 30

akathesia: sx

Answer 30

strong subjective feelings of distress or discomfort ofter referred to the legs, “ants in pants”, need to be in constant motion

Question 31

akathesia: tx

Answer 31

dec dose + add antiparkinsonian agent + anti anxiety agent or propranolol

Question 32

akathesia: onset

Answer 32

within 5-60 days

Question 33

parkinsonian syndrome: sx

Answer 33

akinesia, mask facies, dec arm movement, rigidity, tremor

Question 34

parkinsonian syndrome: tx

Answer 34

anticholinergic antiparkinsonian agent, amantadine

Question 35

parkinsonian syndrome: onset

Answer 35

gradually during the first month

Question 36

parkinsonian syndrome: what is NOT recommended

Answer 36

L-dopa, bromocriptine –> agitation, enhances psychosis