L52-53 watts schizo Flashcards
T or F: Decreased ventricle size is included in the etiology of schizo
False, increased ventricle size
T or F: migration of neurons is included in the etiology of schizo
True
T or F: COMT-marijuana is included in the etiology of schizo
True
T or F: Negative sxs respond well to drug therapy in comparison with positive sxs
false
T or F: Decrease in cognitive function involves d2 receptors and glutamate receptors
False, d1 and glutamate receptors
what neurotransmitters are involved in the neurotransmitter hypotheses of schizo
dopamine
serotonin
glutamate
dopamine neurotransmitter hypothesis
first to be developed, but incomplete
serotonin neurotransmitter hypothesis
based on mechanism of LSD and mescaline
glutamate neurotransmitter hypothesis
based on phencyclidine and ketamine
which 2 drugs are noncompetitive inhibitors of ndma receptors that exacerbate psychosis and cognition deficits
phencyclidine and ketamine
T or F: LY2140023-mGluR2/3 antagonists are effective in schizo
False, agonists
T or F: Ampakine (AMPA receptors) are effective in animal models
True
T or F: Dopaminergic agents exacerbate sxs of schizo
yes, too much dopamine is the problem
T or F: Increased D1 receptor density in treated and untreated pts of schizo
false, d2
Saturation binding experiments
A. Vary concentration of radio-labeled ligands
B. Constant radioligand (hot) concentration competing with unlabeled ligand (cold)
A. Vary concentration of radio-labeled ligands
Competition binding experiments
A. Vary concentration of radio-labeled ligands
B. Constant radioligand (hot) concentration competing with unlabeled ligand (cold)
B. Constant radioligand (hot) concentration competing with unlabeled ligand (cold)
Which of the following receptors are antagonized by antipsychotic drugs
A. Dopamine
B. Serotonin
C. Norepinephrine
D. ACh
E. Histamine
F. A and B
G. A, B, and E
H. All of the above
H. All of the above
antagonism of which receptor is responsible for weight gain?
A. alpha 1
B. histamine
C. ACh
D. D2
B. histamine
antagonism of which receptor is responsible for hypotension?
A. alpha 1
B. histamine
C. ACh
D. D2
A. alpha 1
T or F: most antipsychotic drugs are receptor antagonists
True
antagonism of which receptor modulates synthesis and release of dopamine
D2
Which of the following is the primary region of the CNS for therapeutic effects of D2 antagonists?
A. Basal ganglia
B. Mesolimbic
C. Mesocortical
D. Medulla
B. Mesolimbic
Which of the following is the primary region for motor effects and extrapyramidal sxs (EPS)
A. Basal ganglia
B. Mesolimbic
C. Mesocortical
D. Medulla
A. Basal ganglia
what 2 systems are responsible for the d2 receptor blockade in the endocrine system
hypothalamus and endocrine system lol
Which of the following regions is the chemoreceptor trigger zone
A. Basal ganglia
B. Mesolimbic
C. Mesocortical
D. Medulla
D. Medulla
know the kd shit on slides 20 and 21
i will go look at that (you too whoever is on this card rn)
D2 Antagonism:
Extrapyramidal Sxs (EPS)
occurs ______
early, days/weeks
Symptoms of EPS: (4)
dystonia - increased muscle tone
pseudoparkinsonism
tremor
akathisia - restlessness
What is an antihistamine that can treat EPS?
Benadryl
what anticholinergic agents can be used to treat EPS? (3)
Benztropine, trihexyphenidyl, akineton
what dopamine releasing agent can be used to treat EPS?
Amantadine
What medication can be used to treat akathisia in pts w/ EPS
propranolol 1st line -> +lorazepam (Ott)
Excitatory neurotransmitter involved in EPS
A. ACh
B. Dopamine
A.ACh
inhibitory neurotransmitter involved in EPS
A. ACh
B. Dopamine
B. Dopamine
what drug induced movement disorder occurs late (months/year)
Tardive Dyskinesia
T or F: Both EPS and Tardive Dyskinesia are irreversible disorders
False, EPS is reversible
4 sxs of tardive dyskinesia
- Mouth-rhythmic involuntary movements
- Choreiform- irregular purposelessness
- Athetoid - worm-like movements
- Axial hyperkinesia- “to-and-fro” movements
what is the MOA of tardive dyskinesia?
its unknown, pussy
what monitoring scale should be used in pts experiencing tardive dyskinesia
AIMS (Abnormal Involuntary Movement Scale)
what is the best treatment option for tardive dyskinesia?
prevention, then to use the least risky agent at lowest dose possible
what drug class is a “newer drug therapy” option for tardive dyskinesia?
VMAT2 inhibitors
what are the 3 VMAT2 inhibitors
Tetrabenazine
Valbenazine
Deutetrabenazine
what do VMAT2 inhibitors do to dopamine?
Deplete it so it cant activate receptors that affect movement
Used for Huntington’s Chorea
A. Tetrabenazine
B. Valbenazine
C. Deutetrabenazine
A. Tetrabenazine
B. Deutetrabenazine
used for tardive dyskinesia
A. Tetrabenazine
B. Valbenazine
C. Deutetrabenazine
B. Valbenazine
C. Deutetrabenazine
used for tardive dyskinesia and huntington’s chorea
A. Tetrabenazine
B. Valbenazine
C. Deutetrabenazine
C. Deutetrabenazine
Serious and rapid with 10% fatality
A. EPS
B. Tardive dyskinesia
C. Neuroleptic malignant syndrome
C. Neuroleptic malignant syndrome
Occurs early, days/weeks, reversible
A. EPS
B. Tardive dyskinesia
C. Neuroleptic malignant syndrome
A. EPS
Occurs late (months/year), irreversible, 20-40% incidence
A. EPS
B. Tardive dyskinesia
C. Neuroleptic malignant syndrome
B. Tardive dyskinesia
how long do antipsychotic drugs take to show effectiveness in the tx of psychosis?
A. 4-8 weeks
B. 4-7 days
C. 6 weeks-6 months
D. 2-3 weeks
D. 2-3 weeks
How long does it take an antipsychotic drug to reach its maximal efficacy?
6 weeks to 6 months (damn)
Used in Huntington’s chorea
A. Tetrabenazine
B. Chlorpromazine
C. Haloperidol
D. Metoclopramide
E. Droperidol
A. Tetrabenazine
Used for intractable hiccups
A. Tetrabenazine
B. Chlorpromazine
C. Haloperidol
D. Metoclopramide
E. Droperidol
B. Chlorpromazine
Used for alcohol withdrawal
A. Tetrabenazine
B. Chlorpromazine
C. Haloperidol
D. Metoclopramide
E. Droperidol
C. Haloperidol
Used for N/V
A. Tetrabenazine
B. Chlorpromazine
C. Haloperidol
D. Metoclopramide
E. Droperidol
D. Metoclopramide
Used for potentiation of opiates and sedatives
A. Tetrabenazine
B. Chlorpromazine
C. Haloperidol
D. Metoclopramide
E. Droperidol
E. Droperidol
Orthostatic hypotension, impotence, failure to cum
A. Muscarinic cholinoceptor blockade
B. Alpha adrenoceptor blockade
C. Dopamine receptor blockade
D. Histamine receptor blockade
B
Loss of accommodation, dry mouth, cant piss, cant shit
A. Muscarinic cholinoceptor blockade
B. Alpha adrenoceptor blockade
C. Dopamine receptor blockade
D. Histamine receptor blockade
A
Parkinson’s syndrome, akathisia, dystonias
A. Muscarinic cholinoceptor blockade
B. Alpha adrenoceptor blockade
C. Dopamine receptor blockade
D. Histamine receptor blockade
C
Sedation
A. Muscarinic cholinoceptor blockade
B. Alpha adrenoceptor blockade
C. Dopamine receptor blockade
D. Histamine receptor blockade
D
Tardive dyskinesia
A. Supersensitivity of dopamine receptors
B. Muscarinic blockade
C. Dopamine receptor blockade resulting in hyperprolactinemia
D. Possibly combined H1 and 5HT2 blockade
A
Toxic-confusional state
A. Supersensitivity of dopamine receptors
B. Muscarinic blockade
C. Dopamine receptor blockade resulting in hyperprolactinemia
D. Possibly combined H1 and 5HT2 blockade
B
Amenorrhea-galactorrhea, infertility, impotence
A. Supersensitivity of dopamine receptors
B. Muscarinic blockade
C. Dopamine receptor blockade resulting in hyperprolactinemia
D. Possibly combined H1 and 5HT2 blockade
C
Weight Gain
A. Supersensitivity of dopamine receptors
B. Muscarinic blockade
C. Dopamine receptor blockade resulting in hyperprolactinemia
D. Possibly combined H1 and 5HT2 blockade
D
Contraindications for antipsychotics (4)
Cardiovascular
Parkinsons (no shit)
epilepsy (no shit)
Diabetes (in atypicals)
First antipsychotic
A. Chlorpromazine
B. Promezine
C. Triflupromazine
D. Promethazine
A. Chlorpromazine
what does the 3 atom chain allow for in chlorpromazine?
nitrogen to bind the receptor (why the fuck do i care about this)
2 aliphatic phenothiazines that had a * next to them
Chlorpromazine
Promethazine
what are promethazine and chlorpromazine used for, mostly
H1 antagonist properties
what is the one drug under piperidine phenothiazine with a * next to it
Thioridazine
whats next to thioridazine in the slide that tells us about it
sedation, hypotension, anticholinergic, many SE
so just dont ever put this as an option
What are the 3 piperazine phenothiazines with a *
Fluphenazine
Prochlorperazine
Perphenazine
Fluphenazine
A. EPS
B. Antiemetic
C. just as effective w/ anticholinergic vs. new agents
A
Prochlorperazine
A. EPS
B. Antiemetic
C. just as effective w/ anticholinergic vs. new agents
B
Perphanzine
A. EPS
B. Antiemetic
C. just as effective w/ anticholinergic vs. new agents
C
Thioxanthine drug
Thiothixene
Butyrophenone drug
haloperidol
Which drug is most appropriate for a pt with tourette’s?
A. Molindone
B. Haloperidol
C. Pimozide
D. Chlorpromazine
C. Pimozide
T or F: Atypical agents were the first generation of antipsychotics
False, second
First atypical antipsychotic
Clozapine
what is the significant side effect that clozapine has
agranulocytosis
T or F: Weight gain is a side effect of olanzapine
true
what does the metabolite of the atypical antipsychotic loxapine do? do you remember what its called?
amoxipine, inhibits NET which leads to antidepressive properties
T or F: Quetiapine’s metabolite has antidepressant properties
True
what receptors does quetiapine antagonize
5HT2A
D2
Alpha 1
histamine (H1)
9-hydroxyrisperidone
A. Risperidone
B. Paliperidone
C. Iloperidone
B. Paliperidone
vert potent at alpha 1 receptors
A. Risperidone
B. Paliperidone
C. Iloperidone
C. Iloperidone
specifically and structurally designed to be both a 5HT and D2 receptor antagonist
A. Risperidone
B. Paliperidone
C. Iloperidone
A. Risperidone
Relatively low EPS at <8mg/day
A. Risperidone
B. Paliperidone
C. Iloperidone
A. Risperidone
5HT, D2, alpha 1 affinity
A. Ziprasidone
B. Asenapine
A. Ziprasidone
prolongs qt interval
A. Ziprasidone
B. Asenapine
A. Ziprasidone
5HT and D2. (nM affinity at most 5HT, alpha, DA, and histamine receptors)
A. Ziprasidone
B. Asenapine
B. Asenapine
Inverse agonist of 5HT *
A. Lurasidone
B. Pimavanserin
B. Pimavanserin
Less weight gain and metabolic effects (vs olanzapine)
A. Lurasidone
B. Pimavanserin
A. Lurasidone
Low doses similar effectiveness to high doses
A. Lurasidone
B. Pimavanserin
A. Lurasidone
Used for parkinson disease psychosis
A. Lurasidone
B. Pimavanserin
B. Pimavanserin
make sure you understand the table on slide 57 because it will definitely be on the exam
okay fuckface
what receptors does aripiprazole have high affinity for
5HT2 and D2
aripiprazole is a partial agonist of what receptor (being used in depression)
5HT1a
T or F: Aripiprazole has moderate affinity for D4, alpha, and histamine receptor s
True
what drug class are these guys?
A. Brexpiprazole
B. Cariprazine
C. Lumateperone
D2/D3 receptor partial agonists.
a D2/D3 partial agonist with greater affinity D3.
A. Brexpiprazole
B. Cariprazine
C. Lumateperone
B. Cariprazine
Partial D2 agonist presynaptic receptors/antagonist at postsynaptic receptors
A. Brexpiprazole
B. Cariprazine
C. Lumateperone
C. Lumateperone
A D2/D3 partial agonist with supposedly less akathisia vs aripiprazole
A. Brexpiprazole
B. Cariprazine
C. Lumateperone
A. Brexpiprazole
Schizophrenia and as an adjunct to antidepressants for major depression
A. Brexpiprazole
B. Cariprazine
C. Lumateperone
A. Brexpiprazole
Schizophrenia, mania, and bipolar disorder
A. Brexpiprazole
B. Cariprazine
C. Lumateperone
B. Cariprazine
what is the one drug class that has a * on it in the drugs in development/under investigation slid e
dual M1/M4 muscarinic agonist combined with peripheral muscarinic antagonist (KarXT*)