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Psychopharmacology > Chapter 5: Targeting for psychosis > Flashcards

Chapter 5: Targeting for psychosis Flashcards

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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
deutetrabenazine
inactive prodrug metabolized by 2D6 into 4 active metabolites
25
what is deuteration
when a drug that is a good substrate for 2D6 is converted to a poorer substrate
26
chlorpromazine
1st gen antipsychotic thorazine low potency
26
valbenazine
amino acid valine linked to an enaniomer of tetrabenazine
27
fluphenazine
1st gen antipsychotic prolixin high potency comes in depot
28
haloperidol
1st gen antipsychotic haldol high potency comes in depot
29
loxapine
1st gen antipsychotic loxitane
30
perphenazine
1st gen antipsychotic trilafon high potency
31
pimozide
1st gen antipsychotic orap high potency QTC issues 2nd line for tourettes
32
thioridazine
1st gen antipsychotic mellaril low potency QTC issues second line
33
thiothixene
1st gen antipsychotic navane high potency
34
trifluoperazine
1t gen antipsychotic stelazine high potency
35
drugs targeting 5HT2A in schizophrenia
the more potent the 5HT2A/D2 is for 5HT2A, the lower the D2 antagonism needed so the drug may be better tolerated.
36
treating parkinson and dementia related psychosis
5HT2A antagonism alone may be enough to treat psychosis
37
all 5HT2A receptors are...
postsynaptic and excitatory
38
How does 5HT2A receptors regulate dopamine release in the first downstream pathway and how do you treat it
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
How does 5HT2A receptors regulate dopamine release in the second downstream pathway and how do you treat it
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
How does 5HT2A receptors regulate dopamine release in the third downstream pathway and how do you treat it
-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
what are the reciprocal roles of dopamine and serotonin in relation to prolactin
-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
location and action of 5HT1A receptors
always inhibitory and can be presynaptic (on serotonin neurons) or postsynaptic (on any neuron)
43
how does 5HT1A partial agonism at glutaminergic neurons indirectly innervating nigrostriatal dopamine neurons projecting to the motor striatum improve motor side effects
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
5HT1A partial agonist action at glutaminergic neurons indirectly innervating mesocortical dopamine neurons projecting to the PFC
disinhibits dopamine release in the PFC to improve negative/cognitive/affective/depressive symptoms
45
mania is thought to result from what
excessive dopamine release from mesolimbic/mesostriatal neurons
46
how many D2 receptors need to be blocked for therapeutic action
80%
47
2 antipsychotics with high metabolic risk
olanzapine clozapine
48
5 antipsychotics with moderate metabolic risk
risperidone paliperidone quetiapine asenapine iloperidone
49
7 antipsychotics with low metabolic risk
lurasidone cariprazine lumateperone ziprasidone pimvanserin aripiprazole brexpiprazole
50
5HT2A antagonist and/or 5HT1A partial agonist action
-reduced motor side effects -prolactin elevation -therapeutic for positive, negative, depressive, and cognitive symptoms
51
antipsychotics with 5HT2A binding
-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
antipsychotics with 5HT1A binding
-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
what is the only "pine" with monoamine reuptake inhibition
quetiapine binds to NET similarly as 5HT2A binds with NET at greater potency than D2
54
monoamine transporter binding of ziprasidone
binds to NET and SERT but with less potency than D2
55
monoamine transporter binding of lumateperone
binds to SERT with similiar potency as D2
56
alpha 2 binding of "pines"
all bind to varying degrees *clozapine and quetiapine bind to some a2receptors more potently than D2
57
alpha 2 binding of the "dones"
all bind to varying degrees risperidone and paliperidone bind to a2C with similar potency as D2
58
alpha 2 binding of lumateperone
does not bind to a2 receptors
59
alpha 2 binding of aripiprazole
binds to a2 with less potency than D2
60
alpha 2 binding of brexpiprazole
binds to a2C
61
D3 binding of the "pines"
all bind to D3 at varying degrees
62
D3 binding of the "dones"
all with varying degrees except lumateperone (doesn't bind at all)
63
D3 binding of cariprazine
most potent binding is at D3
64
D3 binding of aripiprazole and brexpiprazole
bind less potently to D3 than D2
65
5HT2C binding of the "pines"
more potent binding at 5HT2C than D2
66
5HT2C binding of the "dones"
all have some affinity
67
only drug that binds to 5HT2C with similar potency as D2
ziprasidone
68
5HT2C binding in "2 pips and a rip"
weak
69
5HT3 binding of "pines"
bind with less affinity than D2
70
5HT3 binding of "dones and a rone"
none have any affinity
71
aripiprazole 5HT3 binding
weak
72
which drugs have greater or similiar potency at 5HT7 as D2
clozapine quetiapine asenapine zotepine
73
drugs with greater or similar potency for 5HT6 as for D2
clozapine olanzapine asenapine zotepine
74
which 4 drugs bind potently to 5HT7
risperidone paliperidone ziprasidone lurasidone (greater affinity than for D2)
75

Psychopharmacology (13 decks)

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