Antipsychotics.Opioids.Other Flashcards

1
Q

increased DA activity in limbic system

A

positive sxs

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2
Q

decreased DA activity in frontal cortex

A

negative sxs

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3
Q

what do classic vs atypical target?

A

c: positive sxs
a: negative sxs

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4
Q

what other NT may be involved with schizophrenia?

A

5HT

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5
Q

mesolimbic pathway

A

VTA to limbic system

positive sxs

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6
Q

mesocortical pathway

A

VTA to frontal cortex

negative sxs

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7
Q

nigrostriatal pathway

A

SN to caudate/putamen

EPs

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8
Q

tuberoinfundibular pathway

A

hypothalamus to ant pit

prolactin release

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9
Q

what do classic anatipsychotics block?

A

DA D2 receptor

positive sxs

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10
Q

newer antipsychotics block what?

A

5HT2a receptors

negative sxs

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11
Q

what other receptors do antipsychotics normally block?

A

muscarinic
alpha adrenergic
histamine

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12
Q

why are there sometimes EPS?

A

D2 antagonists block DA in nigrostriatal system which have motor control

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13
Q

EPS

A
anxiety
restlessness
pacing
constant rocking (akathisia)
mm spasms
abnormal postures (dystonia)
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14
Q

dystonia nad akathisia

A

EPS

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15
Q

which drugs have a lower tendency to cause EPS?

A

clozapine

risperidone

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16
Q

how might we treat EPS?

A

anticholinergics

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17
Q

uncontrollable movements of mouth, tongue, face, eyelids, trunk, extremities

A

tardive dyskinesia

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18
Q

endocrine SE of antipsychotics

A

weight gain

prolactin release

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19
Q

autonomic SE of antipsychotics

A

anticholinergic
postural hypotension (alpha block)
sedation

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20
Q

seizures and antipsychotics

A

decrease seizure threshold

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21
Q

muscle rigidity
catatonia
hyperthermia
altered BP/HR

A

neuroleptic malignant syndrome

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22
Q

how do we treat NMS?

A

dantrolene

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23
Q

most common drug interactions with antipsychotics

A

antichoinergics

sedative-hypnotics

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24
Q

chlorpromazine uses

A

sxhizophrenia
psychotic episode assoc. w/ mania
psychosis/hallucination due to SA

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25
Q

SE of chlropromazine

A

anticholinergic
postural hypotension
inhibition of ejaculation
retinal deposits

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26
Q

haloperidol use

A

injection-acute

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27
Q

haloperidol SE

A

EPS

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28
Q

atypical antipsychotics MOA

A

block 5HT2a and

DA D2, D4

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29
Q

when do we use clozapine?

A

refractory

EPS/TD

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30
Q

Se of clozapine

A

agranulcocytosis

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31
Q

how is olanzapine different from clozapine?

A

no agranulocytosis

hyperglycemia, T2DM

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32
Q

quetiapine

A

similar to clozapine-no agranulocytosis

very sedating

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33
Q

aripiprazole MOA

A

dopamine system stabilizer

DA receptors activated when low and blocked if high

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34
Q

SE of aripiprazole

A

decreased motility of esophagus

orthostatic hypotension

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35
Q

risperidone use

A

first line drug for psychosis

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36
Q

benefit of risperidone

A

no significant effect on DA receptors in basal ganglia= no EPS

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37
Q

DOC for psychosis

A

risperidone

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38
Q

SE of risperidone

A

increased prolactin

anxiety

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39
Q

ziprasidoneMOA

A

blocks D2 and 5HT 2a

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40
Q

ziprasidone use

A

Tourette’s

acute mania

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41
Q

SE of ziprasidone

A

drug interactions
prolonged QT interval
sedation

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42
Q

relative CI for ziprasidone

A

hx of seizures

with other drugs that decrease threshold

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43
Q

lurasidone

A

no histamine/muscarinic effects

depression assoc. w/ bipolar

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44
Q

DOC for bipolar

A

lithium

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45
Q

kinetics of lithium

A

small therapeutic window

excreted by kidney-competes with sodium for reabsorption

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46
Q

too much lithium given

A

hyponatremia

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47
Q

sodium decreased while on lithium

A

lithium toxicity

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48
Q

renal effects of lithium

A

nephrogenic diabetes insipidous

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49
Q

how do we treat nephrogenic DI?

A

amiloride

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50
Q

how do we treat lithium overdose?

A

dialysis

saline

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51
Q

antidepressants and lithium

A

increase mania

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52
Q

antipsychotics or benzodiazepines and lithium

A

sage

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53
Q

diuretics and lithium

A

thiazides decrease clearance

loops =little effect

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54
Q

NSAIDs and lithium

A

decrease lithium clearance

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55
Q

anticonvulsants with mood-stabilizing properties

A

valproic acid
carbamazepine
lamotrigine

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56
Q

lamotrigine use as an mood stabilizer

A

prevents depression that follows mania

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57
Q

Parkinson’s pathophys

A

degerneration of DA neurons in pars compacta of SN leading to overactivity in indirect pathway and underactivity in direct pathway=decreased glutamat into cortex

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58
Q

DA synthesis

A

tyrosine–> l-dopa–> DA via dopa decarboxylase

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59
Q

how is DA metabolized?

A

MAO B in nerve terminal

also MAO A and COMT

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60
Q

carbidopa MOA

A

dopa decarboxylase inhibitor

does not cross BBB

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61
Q

why would you give carbidopa with l dopa?

A

inhibits synthesis of DA from l dopa in the periphery so more l dopa gets into the brain (dose can be decreased)

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62
Q

l dopa half life

A

short

multiple doses/ day

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63
Q

GI SE of l dopa

A

N/V (decreases w/ carbidopa)

64
Q

CV SE of l dopa

A

postural hypotension

arrhythmias

65
Q

l dopa and dyskinesias

A

dose-related
occurs w/ long-term therapy
more common with carbidopa combo

66
Q

Parkinson’s patient with psychosis, how do you treat that?

A

must be atypical antipsychotic– clozapine, quetiapine, aripiprazole

67
Q

on-off phenomenom

A

only when treated with l-dopa–>brain adaptation

off=periods of dyskinesia

68
Q

drug holiday for Parkinson’s

A

not recommended anymore

69
Q

l dopa and MAOI

A

hypertensive crisis

70
Q

Vitamin B6 and l dopa

A

increases peripheral metabolism of l-dopa=decreased effectiveness

71
Q

CI for l dopa

A
psychosis
closed-angle glaucoma
active PUD
malignant melanoma
cardiac dz-small risk
72
Q

why MAOI for Parkinson’s?

A

selective for MAOB which is predominant form in SN

73
Q

effect of MAOI on Parkinson’s

A

decreases formation of free radicals- may slow progression

use in early stages

74
Q

SE of MAOI

A

insomnia, anxiety

75
Q

what can not be taken with MAOI?

A

meperidine

76
Q

tacapone vs entacapone

A

tacapone crosses BBB, entacapone does not

entacapone used as adjunct levodopa/carbidopa

77
Q

issue with tolcapone

A

death from liver dz–pt consent

78
Q

dopamine receptor agonist effect on prolactin

A

decreases release

79
Q

dopamine agonist that is a patch

A

rotigotine

80
Q

GI SE of DA agonists

A

anorexia

N/V

81
Q

CV SE of DA agonists

A
postural hypotension (esp at beginning)
cardiac arrhythmias
82
Q

CNS SE of DA agonists

A

dyskinesia

mental disturbances

83
Q

SE of ergot derivatives

A

erythromelalgia– disappears when discontinued

84
Q

erythromelalgia

A

red, tender, swollen feet due to vasospasm

85
Q

bromocriptine

A

ergot derivative

rarely used

86
Q

pramipexole/ropinirole use

A

Parkinson’s

Rop: restless leg syndrome

87
Q

SE of pramipexole/ropinirole

A

nausea
fatigue
sudden sleep during the day

88
Q

apomorphine use

A

Parkinson’s “rescue”

89
Q

apomorphine MOA

A

potent DA receptor agonist

90
Q

apomorphine kinetics

A

injection

quick effect

91
Q

apomorphine SE

A

nausea

92
Q

amantadine MOA

A

influenza antiviral used for Parkinson’s

93
Q

SE of amantadine

A

psychiatric

94
Q

livedo reticularis

A

amantadine

spotting of skin

95
Q

CI caution with amantadine

A

hx of seizures

CHF

96
Q

why anticholinergics for Parkinson’s?

A

decrease the effects of ACh to match loss of DA

start low

97
Q

what sxs do anticholinergics affect with Parkinson’s?

A

not bradykinesia

rigidty, tremor, drooling

98
Q

neuritic plaques

neurofibrillary tangles

A

Alzheimer’s

99
Q

ApoE4

A

Alzheimer’s

100
Q

RF for Alzheimers

A

age
FH
gender
educational level

101
Q

pathophysiology of Alzheimers

A

degeneration of cholinergic neurons from nucleus basalis of Meynert which projects to cerebral cortex and hippocampus

102
Q

SE of antichoinergics

A

N/D/V

103
Q

memantine MOA

A

antagonist at NMDA receptors

104
Q

memantine use

A

more severe Alzheimer’s dz

105
Q

CI caution for memantine

A

severe renal impairment

106
Q

SE of memantine

A
agitaiton
urinary incontinence
UTI
insomnia
diarrhea
107
Q

what drugs can not be given with memantine?

A

meperidine, dextromethorphan (also block NMDA)

108
Q

how does memantine affect l dopa?

A

enhances adverse effects of l dopa

109
Q

three opioid receptors

A

mu
kappa
delta

110
Q

endogenous opioids

A

met-, leu- enkephalin
beta endorphin
dynorphins

111
Q

opioid receptor activation

A

closes voltage-gated Ca2+ channels–decrease release of NT

opens K+ channels-hyperpolarize–inhibition of postsynaptic neurons

112
Q

which opioid receptor is most associated with dysphoria?

A

kappa

113
Q

what components of pain are affected with opioids?

A

sensory

affective (emotional)

114
Q

neuropathic pain and opioids

A

not great

use TCAs or gabapentin

115
Q

GI effects of opioids

A

nausea
constipation
decreased gastric motility

116
Q

which opioid does not suppress cough?

A

meperidine

117
Q

what receptor does meperidine most affect?

A

mu

118
Q

other general effects of opioids

A
respiratory depression
elevated ICP
miosis
decreased body temp
truncal rigidity
119
Q

what opiod SE does not develop tolerence?

A

miosis

120
Q

CV effects of opioids

A

bradycardia
meperidine-tachycardia
orthostatic hyopotension

121
Q

why can there be orthostatic hypotension with opioids?

A

depression of central vasomotor systems and histamine release

122
Q

GU effects of opioids

A

decrease urine output
increased sphincter tone
increased ureteral tone

123
Q

what makes a histamine flush with opioids more common?

A

injected

124
Q

what drugs might you give for opioid withdrawal?

A

clonidine

another opioid-methadone

125
Q

pin point pupils

A

opioid OD

126
Q

sedative-hypnotics and opioids

A

CNS depression

respiratory depression

127
Q

antipsychotics and opioids

A

sedation

increased CV effects

128
Q

MOAIs and opioids

A

hyperpyrexic coma

129
Q

which opioids are the worst to mix with MAOI?

A

meperidine

dextromethorphan

130
Q

opioids that must be demethylated

A

codeine
hydrocodone
oxycodone

131
Q

opioid CI

A
pure agonist with partial
head injuries
during pregnancy
impaired respiratory function
impaired hepatic or renal function
Addison's
132
Q

morphine unique

A

IV

histamine flush

133
Q

hydromorphone

A

less metabolite accumulation

more potent than morphine

134
Q

methadone

A

long duration
also blocks NMDA
less likely for addiction

135
Q

meperidine

A

no antitussive activity
mydriasis
tachycardia
not for long term use

136
Q

what pts do we have to caution with using meperidine?

A

renal failure–seizures

137
Q

why is meperidine not good for long-term use?

A

short duration
metabolites accumulate
large dose=tremor, mm twtich, convulsions

138
Q

why does meperidine cause mydriasis and tachycardia?

A

antimuscarinic activity

139
Q

what drugs combined with meperidine can cause serotonin syndrome?

A

phenelzine
selegiline
linezolid

140
Q

fentanyl

A

highly potent
short-acting
usually used with anesthesia/surgery
CYPs-drug interactions

141
Q

hydrocodone and oxycodone

A

usually produced with acetaminophen

142
Q

metabolism of hydrocodone and oxycodone

A

CYP2D6 (some of it)

143
Q

opioids that have drug interactions with fluoxetine and paroxetine

A

codeine
hydrocodone
oxycodone
(CYP2D6)

144
Q

pentazocaine/naloxone MOA

A

agonist at kappa

partial agonist at mu

145
Q

use of pentazocaine/naloxone

A

moderate pain

146
Q

SE of pentazocaine/naloxone

A

less SE compared to others

dysphoria

147
Q

withdrawal with pentazocaine/naloxone

A

can precipitate in opioid addicts

148
Q

buprenorphine MOA

A

partial agonist at mu/kappa receptors

149
Q

use for buprenorphine

A

reduce drug cravings

sublingual

150
Q

what if buprenorphine is given with a full agonist?

A

acts as an antagonist

151
Q

MOA of tramadol

A

weak mu agonist

inhibits reuptake of norepi and serotonin

152
Q

what happens with combo of tramadol and antidepressants?

A

seizures

153
Q

what should be avoided with tramadol?

A

TCAs
SSRIs
MAOIs
*serotonin syndrome

154
Q

tapentadol

A

similar to tramadol
N/V
sedation

155
Q

what happens when mixing MAOIs and dextromethorphan?

A

serotonin syndrome

156
Q

DOC for opioid overdose

A

naloxone–short-acting

157
Q

naltrexone

A

oral, long-acting antagonist