EXAM 4 antipsychotics Flashcards

1
Q

etiology schizophrenia

A

Neurodevelopment/anatomical: increased ventricle size and changes in gray and white matter
Genetics- neuronal growth, migration of neurons
Environmental: birth complications + infections
Gene-environment interations: COMT-marijuana
Neurodevelopmental-environmental interactions

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2
Q

positive symptoms schizophrenia

A

responds well to drug therapy: older agents
hallucinations, delusions, bizarre behavior, thought disorders

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3
Q

negative symptoms schizophrenia

A

little response drug therapy
newer agents are better
blunted emotion

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4
Q

cognitive symptoms

A

decrease cognitive function
involves D1 receptors and glutamate receptors

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5
Q

dopamine hypothesis

A

dopaminergic agents exacerbate symptoms of schizophrenia
increased D2 receptor density in patients with schizophrenia

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6
Q

serotonin hypothesis

A

LSD, mesacline are 5HT agonists
5HT2a receptor is a mediator of hallucinations
5HT2a receptor modulate DA release in cortex, limbic, striatum

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7
Q

glutamate hypothesis

A

major excitatory neuron
phencyclidine and ketamine are noncompetitive inhibitors of NMDA receptors that exacerbate psychosis and cognition deficit

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8
Q

binding affinity

A

intermolecular force between ligand and receptor
lower the number is better
Kd/Ki: estimated concentrations at which 1/2 receptors are occupied

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9
Q

what receptors antagonized by antipsyschotics

A

major: DA
newer: 5HT
minor NE, ACh, Histamine

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10
Q

what is binding affinity vs clinical dose

A

binding to D2 receptors is directly correlated to clinical dose

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11
Q

what are anatgonist actions at the synapse

A

presynaptic terminal acts like safety switch of an autoreceptor
D2 receptors modulate synthesis of DA
DA transporters reduce DA at the synapse

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12
Q

what are dopamine’s effect on parts of the brain?

A

basal ganglia is responsible for EPS motor effects
mesolimbic is where primary therapeutic effects take place
mesocortical is responsible for hypofunction in schizophrenia

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13
Q

what is receptor occupancy for DA

A

for DA, about 60% for efficacy
for DA, at 90% occupancy, there is 50% H1 occupancy

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14
Q

what is EPS

A

extrapyramidal symptoms
occurs early and is reversible
symptoms: dystonia, pseudoparkinsonism, tremor, akathisia

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14
Q

what are the three drug induced movement disorders?

A
  1. EPS
  2. tardive dyskinesia
  3. neuroleptic malignant syndrome
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15
Q

what is drug therapy for EPS?

A

anticholinergics due to excess cholinergic side effects
benztropine, trihyphenidyl, akineton
diphenhydramine
amatadine
propranolol

16
Q

what is tardive dyskinisea

A

occurs late and is irreversible
unknown MOA
symptoms: involuntary mouth movements, choreiform (irregular purposelessness), athetoid (worm-like movements), axial hyperkinesias (to-fro movements)
monitor AIMS every 6 months

17
Q

treatment for tardive dyskinesias?

A

prevention is best
but reduce dose, change to different drug, eliminate anticholinergics, VMAT inhibitors
tetrabenazine, valbenazine, deuterabenazine

18
Q

what is neuroleptic malignant syndrome NMS?

A

rapid block of DA receptor
symptoms: EPS with fever, impaired cognition, muscle rigidity

19
Q

treatment of NMS

A

discontinue drug
DA agonist, diazepam, dantrolene

20
Q

what are the therapeutic uses of antipsychotics?

A

treatment of psychosis: 2-3 weeks for effectiveness, 6 weeks to 6 months for maximal efficacy
mood disorders
tourettes

21
Q

what are adverse effects on autonomic system for antipsychotics?

A

muscarinic blockade: constipation, dry mouth, trouble urinating
alpha blockade: orthostatic hypotension, impotence

22
Q

what are antipsychotic adverse effects on CNS

A

DA block: parkinsons, akathisia, dystonia
supersensitivity to DA receptors: tardive dyskinesias
muscarinic block: toxic confused state
H1: sedation

23
Q

what are adverse effects of antipsychotics related to the endocrine system?

A

DA block so hyperprolactemia: amenorhea galactorrhea, infertility

24
what are first generation antipsychotics?
phenothiazines thioxanthines butrophenones (haloperidol) molindone pimozide
25
which ones are phenothiazines?
aliphatic phenothiazines: chlorpromazine promethazine Piperidine: thioridazine piperazine: fluphenazine, prochlorperazine, perphenazine
26
which ones are other antipsychotics:
thioxanthines haloperidol
27
what are atypical antipyschotics
reduced EPS more metabolic problems like olanzapine and clozapine
28
what is smoking in relation to antipsychotics
1A2 inducer due to the hydrocarbons
29
how do you treat EPS acute dystonia
IM anticholinergics now benztropine 2mg diphenhydramine 50mg
30
how do you treat EPS drug induced parkinsons
oral anticholinergics benztropine trihexyhendyl diphenhydramine
31
how do you treat akathisia
BB - propranolol first line BZD - normally lorazepam
32
how do you treat tardive dyskinesias?
VMAT2 inhbitors
33
what is neuroleptic malignant syndrome
life threatening medical emergency hyperpyrexia(high fever), tachycardia, labile BP muscle rigidity, elevated CK
34
how to treat NMS?
discontinue antipsychotic consider dopamine agonists future antipsychotic use is not CI