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Psychopharmacology > Chapter 5: Targeting for psychosis > Flashcards

Chapter 5: Targeting for psychosis Flashcards

1
Q

neurolepsis

A

extreme slwoness or absence of motor movements as well as behavioral indifference

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2
Q

what are seconday negative symptoms

A

negative symptoms that are caused by side effects of other drugs for psychosis

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3
Q

which dopamine pathway has a major role in regulating motivation and reward

A

D2 receptors in the mesolimbic pathway that targets the nucleus accumbens

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4
Q

which mesocortical dopamine pathways that are thought to be hypoactive in untreated schizophrenia

A

DLPFC
VMPFC

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5
Q

hypoactivity of which mesocortical dopamine pathway leads to cognitive symptoms of schizophrenia

A

DLPFC

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5
Q

hypoactvity of which mesocortical dopamine pathways lead to negative symptoms of schizophrenia

A

DLPFC and VMPFC

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6
Q

hypoactivity of which mesocortical dopamine pathway is thought to cause affective symptoms of schizophrenia

A

VMPFC

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7
Q

when schizophrenia is untreated are mesocortical dopamine pathways thought to be hypoactive or hyperactive

A

hypoactive

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8
Q

prolactin elevation is a result of targeting which D2 receptors

A

tuberoinfundibular D2 receptors

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9
Q

why do D2 blockers cause increased prolactin

A

they reduce activity in the tuberoinfundibular dopamine pathway by preventing dopamine from binding to D2 receptors, causing prolactin levels to rise

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10
Q

what two neurotransmitters have a reciprocal relationship in the nigrostriatal dopamine pathway

A

dopamine and acetylcholine

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11
Q

what type of drugs are typically used to combat side effects caused by D2 blockers in the nigrostriatal pathway (motor side effects)

A

anticholinergics (often benztropine)

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12
Q

what is a medications that can be used to treat drug induced parkinsonism that lacks anticholinergic effects

A

amantadine

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13
Q

can you treat late-onset drug-induced dystonia from chronic D2 blockade with anticholinergics? why or why not?

A

No. Anticholinergics can make this type of dystonia worse

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14
Q

treatment for drug-induced acute dystonia

A

IM anticholinergic injection usually effective within 20 minutes

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15
Q

how do you treat drug-induced akathisia

A

usually with B-adrenergic blockers or benzodiazepines. Not well treated with anticholinergics

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16
Q

what is neuroleptic malignant syndrome

A

potentially fatal complication of D2 blockade in the nigrostriatal pathway that causes extreme muscle rigidity, high fever, coma, and death

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17
Q

treatment of neuroleptic malignant syndrome

A

-withdraw D2 blocker
-muscle-relaxing agents (dantrolene, dopamine agonists, intensive supportive medical treatments)

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18
Q

3 ways to treat TD

A

-increase D2 blocker dose (helps in short term by blocking super sensitive D2 receptors but can ultimately make TD worse)
-stop D2 blocker and hope effects reverse
-VMAT inhibitors

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19
Q

2 types of VMAT inhibitors

A

reserpine
tetrabenazine-related drugs

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20
Q

mechanism of action for reserpine

A

irreversibley inhibits VMAT1 (central and periphery) and VMAT2 (CNS only)

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21
Q

3 tetrabenazine-related drugs

A

tetrabenazine
deutetrabenazine
valbenazine

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22
Q

what enzyme metabolizes tetrabenazine-related drugs

A

2D6

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23
Q

tetrabenazine

A

inactive prodrug metabolized by carbonyl reductase into 4 active metabolites

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24
Q

deutetrabenazine

A

inactive prodrug metabolized by 2D6 into 4 active metabolites

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25
Q

what is deuteration

A

when a drug that is a good substrate for 2D6 is converted to a poorer substrate

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26
Q

chlorpromazine

A

1st gen antipsychotic
thorazine
low potency

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26
Q

valbenazine

A

amino acid valine linked to an enaniomer of tetrabenazine

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27
Q

fluphenazine

A

1st gen antipsychotic
prolixin
high potency
comes in depot

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28
Q

haloperidol

A

1st gen antipsychotic
haldol
high potency
comes in depot

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29
Q

loxapine

A

1st gen antipsychotic
loxitane

30
Q

perphenazine

A

1st gen antipsychotic
trilafon
high potency

31
Q

pimozide

A

1st gen antipsychotic
orap
high potency
QTC issues
2nd line for tourettes

32
Q

thioridazine

A

1st gen antipsychotic
mellaril
low potency
QTC issues
second line

33
Q

thiothixene

A

1st gen antipsychotic
navane
high potency

34
Q

trifluoperazine

A

1t gen antipsychotic
stelazine
high potency

35
Q

drugs targeting 5HT2A in schizophrenia

A

the more potent the 5HT2A/D2 is for 5HT2A, the lower the D2 antagonism needed so the drug may be better tolerated.

36
Q

treating parkinson and dementia related psychosis

A

5HT2A antagonism alone may be enough to treat psychosis

37
Q

all 5HT2A receptors are…

A

postsynaptic and excitatory

38
Q

How does 5HT2A receptors regulate dopamine release in the first downstream pathway and how do you treat it

A

glutaminergic neurons directly innervate mesolimbic/mesostriatal dopamine neurons projecting to the emotional striatum. Decrease dopamne release at D2 receptors at the end of the pathway and reduce excitatory property of 5HT2A receptors at the begining of the pathway

39
Q

How does 5HT2A receptors regulate dopamine release in the second downstream pathway and how do you treat it

A

glutaminergic neurons indirectly innervate nigrostriatal dopamine neurons that project to the motor striatum.
treat by blocking 5HT2A receptors in this pathway to change the polarity of upstream glutamate release from stimulating to inhibiting which stimulates downstream dopamine release in the motor striatum. When there is more dopamine available to compete with blockade, motor side effects are improved

40
Q

How does 5HT2A receptors regulate dopamine release in the third downstream pathway and how do you treat it

A

-glutaminergic neurons indirectly innervate mesocortical dopamine neurons that project to the PFC
-blocking 5HT2A receptors on these neurons will cause increased downstream dopamine release in the PFC to improve negative cognitive and affective symptoms

41
Q

what are the reciprocal roles of dopamine and serotonin in relation to prolactin

A

-dopamine inhibits prolactin release by stimulating D2 receptors (when blocked, prolactin levels rise)
-serotonin promotes prolactin release by stimulating 5HT2A receptors (when blocked, prolactin release decrease and levels drop)

42
Q

location and action of 5HT1A receptors

A

always inhibitory and can be presynaptic (on serotonin neurons) or postsynaptic (on any neuron)

43
Q

how does 5HT1A partial agonism at glutaminergic neurons indirectly innervating nigrostriatal dopamine neurons projecting to the motor striatum improve motor side effects

A

disinhibits dopamine release in these neurons and the increased release competes w/ D2 blockers for receptors in the motor striatum to reverse side effects

44
Q

5HT1A partial agonist action at glutaminergic neurons indirectly innervating mesocortical dopamine neurons projecting to the PFC

A

disinhibits dopamine release in the PFC to improve negative/cognitive/affective/depressive symptoms

45
Q

mania is thought to result from what

A

excessive dopamine release from mesolimbic/mesostriatal neurons

46
Q

how many D2 receptors need to be blocked for therapeutic action

A

80%

47
Q

2 antipsychotics with high metabolic risk

A

olanzapine
clozapine

48
Q

5 antipsychotics with moderate metabolic risk

A

risperidone
paliperidone
quetiapine
asenapine
iloperidone

49
Q

7 antipsychotics with low metabolic risk

A

lurasidone
cariprazine
lumateperone
ziprasidone
pimvanserin
aripiprazole
brexpiprazole

50
Q

5HT2A antagonist and/or 5HT1A partial agonist action

A

-reduced motor side effects
-prolactin elevation
-therapeutic for positive, negative, depressive, and cognitive symptoms

51
Q

antipsychotics with 5HT2A binding

A

-the “pines” all have higher potency for 5HT2A than D2
-the “dones and a rone” bind more potently to 5HT2A than D2
-aripiprazole and cariprazine are more potent for D2 than 5HT2A
-brexpiprazole has similiar potency at both receptors

52
Q

antipsychotics with 5HT1A binding

A

-clozapine/quetiapine more potent for 5HT1A than D2
-asenapine/zotepine are less potent for 5HT1A than D2
-olanzapine/lumateperone do NOT bind to 5HT1A
-all “dones” less potent for 5HT1A than D2
-aripiprazole, brexpiprazole, cariprazine have similar potency at 5HT1A and D2

53
Q

what is the only “pine” with monoamine reuptake inhibition

A

quetiapine
binds to NET similarly as 5HT2A
binds with NET at greater potency than D2

54
Q

monoamine transporter binding of ziprasidone

A

binds to NET and SERT but with less potency than D2

55
Q

monoamine transporter binding of lumateperone

A

binds to SERT with similiar potency as D2

56
Q

alpha 2 binding of “pines”

A

all bind to varying degrees
*clozapine and quetiapine bind to some a2receptors more potently than D2

57
Q

alpha 2 binding of the “dones”

A

all bind to varying degrees
risperidone and paliperidone bind to a2C with similar potency as D2

58
Q

alpha 2 binding of lumateperone

A

does not bind to a2 receptors

59
Q

alpha 2 binding of aripiprazole

A

binds to a2 with less potency than D2

60
Q

alpha 2 binding of brexpiprazole

A

binds to a2C

61
Q

D3 binding of the “pines”

A

all bind to D3 at varying degrees

62
Q

D3 binding of the “dones”

A

all with varying degrees except lumateperone (doesn’t bind at all)

63
Q

D3 binding of cariprazine

A

most potent binding is at D3

64
Q

D3 binding of aripiprazole and brexpiprazole

A

bind less potently to D3 than D2

65
Q

5HT2C binding of the “pines”

A

more potent binding at 5HT2C than D2

66
Q

5HT2C binding of the “dones”

A

all have some affinity

67
Q

only drug that binds to 5HT2C with similar potency as D2

A

ziprasidone

68
Q

5HT2C binding in “2 pips and a rip”

A

weak

69
Q

5HT3 binding of “pines”

A

bind with less affinity than D2

70
Q

5HT3 binding of “dones and a rone”

A

none have any affinity

71
Q

aripiprazole 5HT3 binding

A

weak

72
Q

which drugs have greater or similiar potency at 5HT7 as D2

A

clozapine
quetiapine
asenapine
zotepine

73
Q

drugs with greater or similar potency for 5HT6 as for D2

A

clozapine
olanzapine
asenapine
zotepine

74
Q

which 4 drugs bind potently to 5HT7

A

risperidone
paliperidone
ziprasidone
lurasidone (greater affinity than for D2)

75
Q
A

Psychopharmacology (13 decks)

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