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PHARM 203 > 203 final > Flashcards

203 final Flashcards

1
Q

Which general anesthetic has a small therapeutic margin (IV)

A

thiopental

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2
Q

Which IV GA is used for preoperative sedation

A

midazolam

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3
Q

a higher blood gas coefficient means

A

higher solubility = slower equilibrium within alveoli

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4
Q

a higher oil;gas partition means

A

higher potency, slower recovery

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5
Q

where are local anesthetics injected when it’s parenteral

A

peripheral nerve endings
near major nerve trunks
into epidural or subarachnoid spaces

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6
Q

components of a local anesthetic

A

aromatic ring- ester or amide bond - amine base

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7
Q

what kind of drugs are weak bases

A

local anesthetics

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8
Q

GA act on ___ while LA block ___

A

general: GABAa, 2 pore K+ channels, NMDA block
LA: NA (increases excitability threshold + decreases conduction)

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9
Q

what kind of drugs cause severe toxicity if absorbed systemically

A

local anesthetics

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10
Q

all opioid receptors are _____

A

GPCR- Gi/Go

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11
Q

2 analgesics used for neuropathic pain

A

TCAs and antiepileptic drugs

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12
Q

opioids act on which channels

A

neuronal K+ and VG Ca2+

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13
Q

antiepileptics act on which chanels

A

Na+ and Ca2+

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14
Q

what analgesic inhibits amine uptake and blocks sodium channels

A

nefopam

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15
Q

TCAs act within the

A

CNS

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16
Q

what reduces expression of VG Ca2+ channel + blocks Na+

A

antiepileptics (analgesics)

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17
Q

postsynaptic 5HT are highly expressed in parts of the brain implicated in

A

emotional behaviour (limbic)

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18
Q

benzodiazapines structure

A

benzene ring fused to diazepine ring

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19
Q

-lap/pam are

A

BZs

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20
Q

flumazenil

A

BZ antagonist

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21
Q

PD is associated with a loss of DA neurons in the ____ and _____ of the _____

A

substantia nigra
corpus striatum
of the basal ganglia

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22
Q

levodopa is given with

A

carbidopa/benserazide

entacapone/tolcapone

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23
Q

carbidopa/benserazide are

A

peripheral DOPA decarboxylase inhibitors that don’t cross the BBB

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24
Q

entacapone and tolcapone are

A

COMT inhibitors

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25
Q

amantadine actions

A

increases DA release, decreases uptake, acts on DA receptors

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26
Q

5 PD drugs

A 
levodopa
DA receptor agonists
MAO-B inhibitors
amantadine
mAChR antagonists
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27
Q

GABAergic neurons have _______ decarboxylase

A

glutamic acid

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28
Q

Huntingtons drugs

A

tetrabenazine
chloropromazine
baclofen

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29
Q

what in AZ activates NMDA to cause excitotoxicity

A

beta amyloid

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30
Q

AZ drugs

A

anticholinesterases

NMDA blockers- memantine

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31
Q

HT causes neuronal loss in ___ and _____

A

cortex

striatum

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32
Q

AZ sees neuronal loss in ____ and ____

A

hippocampus

frontal cortex

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33
Q

mephedrone action

A

inhibits 5HT and DAT reuptake + stimulates release

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34
Q

methylphenidate action

A

inhibits SERT, DAT, and NET reuptake

used for narcolepsy and ADHD

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35
Q

modafinil action and treats

A

inhibits DAT

treats narcolepsy

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36
Q

do you know that you’re on LSD when you’re on LSD

A

yes, retained insight into the fact that disturbances are drug induced

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37
Q

can LSD cause long lasting psychopathological changes

A

yes

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38
Q

with MDMA, inhibition of DAT and NET = ___, while SERT causes

A

euphoria and rebound dysphoria

psychomimetic effects

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39
Q

what psychometics causes hyponatremia and acute hyperthermia

A

MDMA

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40
Q

list of stimulants

A 
amphetamines
mephedrone
methylphenidate
modafil
cocaine
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41
Q

list of psychomemetics

A 
LSD
psilocybin
MDMA
mescaline
ketamine and phencyclidine
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42
Q

PCP causes ____ and ____

A

psychotic episodes and schizophrenic attacks

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43
Q

what part of amphetamines actions result in their rewarding effect

A

more DA

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44
Q

schizophrenia’s root cause is what receptor

A

NMDA receptor hypofunction

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45
Q

NMDA receptor hypofunction on ____ GABAergic interneurons alter cortical processing = cognitive impairment

A

cortical

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46
Q

what happens if you block D2 in cortex

A

worsening of negative symptoms

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47
Q

what happens if you block D2 in nigrostriatal pathway

A

dystonia (sim to PD) and dyskinesia

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48
Q

what happens if you block D2 in mesolimbic pathway

A

enhanced prolactin secretion + galactorrhea

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49
Q

where would you use a mAchR block for schizophrenia

A

for motor disturbances
on neuron downstream from cholinergic
on dopaminergic neuron = secretes more dopamine

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50
Q

blocking 5HT2a in mesocortical results in

A

improved negative symptoms

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51
Q

in the mesolimbic pathway, combined __ and __ receptor antagonism may counteract the increased dopamine function

A

D2

5HT2a

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52
Q

what receptors do antipsychotics block besides D

A

H1
mAchR
alpha-adrenoceptor

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53
Q

to relieve antipsychotic motor effects, you would block mAChR in the

A

striatum
on post ACh neuron
on DOPA neuron

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54
Q

sodium channel blockers for seizures are use dependent, they preferentially bind to

A

inactivated state of the channel

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55
Q

focal seizure drugs

A

carbamazepine, lamotrigine, levetriacetam, phenytoin

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56
Q

SARI stands for

A

serotonin-2 antagonists/ 5ht reuptake inhibits

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57
Q

NaSSA stands for

A

noradrenergic/ specific serotonergic agent

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58
Q

inhibitors of monoamine uptake

A 
SSRIs
TCA
SNRIs
NDRIs
St. John's wort
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59
Q

2 classes of MAOIs

A

irreversible, noncompetitive, nonselective inhibitors
both MAOA and MAOB

reversible, MAOA selective inhibitors

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60
Q

antidepressant effect
tremors, tachycardia, HT, sweating, insomnia, erectile and ejaculation problems

caused by ____ block

A

NE reuptake blockade

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61
Q

antidepressant, antianxiety, antipanic, antiobsessional, antiaggressive caused by ______ block or agonism

A

5HT reuptake blockade or 5HT receptor agonism

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62
Q

what blockade mitigates against prolactin elevation but aggravates psychosis

A

DA reuptake blockade

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63
Q

5HT2A blockade causes

A

antipsychotic

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64
Q

dry mouth, blurred vision, constipation, urinary retension, sinus tachy, glaucoma are caused by ___ block

A

M1

65
Q

what blockade would potentiate drugs with anticholinergic properties

A

M1

66
Q

alpha 2 blockade effect

A

possible decrease in depressive symptoms

67
Q

order of TCA action

A

H1 block
M1 block
NE reuptake block
5HT reuptake block

68
Q

MAOA prefers

A

5HT and NE degradation

69
Q

MAOB prefers

A

phenylethylamine and dopamine

70
Q

hypertensive crisis occurs when

A

MAOI inhibits the inactivation of tyramine with MAO

71
Q

contractile state is controlled by (3)

A

endothelium
circulating hormones
sympathetic nerves

72
Q

major vasoconstrictors produced by endothelial cells

A

endothelin
TXA2
angiotensin II

73
Q

endothelin acts by

A

acting on ETa receptors to cause Ca2+ release via IP3

74
Q

captopril is a vasodilator. what does it inhibit

A

RAS inhibitor

75
Q

nicorandil action

A

Katp channel open
prevent VGCC
donates NO

76
Q

what acts on V1 receptors

A

ADH

77
Q

MOA of -olol

A

decreased cardiac output
decreased renin
reduce sympathetic activity

78
Q

-dipine are

A

Ca2+ antagonists

dihydropyridines

79
Q

-sartans act on what receptors

A

AT1

80
Q

-pril are

A

ACE inhibitors

81
Q

treatment starts with either a ____ (young white) or a ________ (older or african)

A

RAS inhibitor

thiazide diuretic/ Ca2+ antagonist

82
Q

treatment for a old white man for hypertension usually starts with a

A

thiazide diuretic/ Ca2+ antagonist

83
Q

there is a young african needing a antihypertensive drug, what are your choices

A

thiazide diuretic

Ca2+ antagonist

84
Q

what to use in hypertensive emergencies

A

nitroprusside

85
Q

2 actions of nitroprusside

A

cGMP signaling increase

NO donor

86
Q

what does carvedilol target

A

beta and alpha 1

87
Q

negative inotropics ___

A

weaken contraction force

88
Q

isosorbide mononitrate is an

A

organic nitrate

89
Q

what reduces preload by relaxing veins through NO

A

isosorbide mononitrate

90
Q

hydralazine MOA

A

inhibits IP mediated intracellular Ca2+ increase

results in a fall in BP

91
Q

in heart failure, there is ____ CO

A

insufficient

92
Q

digoxin MOA

A

inhibits Na+/K+ ATPase

93
Q

digoxin ___ contraction force, ___ HR, ____ ventricular filling

A

increases contration forces
decreases HR
increases ventricular filling

94
Q

-one are

A

aldosterone receptor antagonists

95
Q

does spironolactone directly inhibit electrolyte transporter activity?

A

no

inhibits expression of transporters

96
Q

furosemide is a

A

loop diuretic

97
Q

furosemide MOA

A

inhibits Na+/K+/2Cl- transporter at loop of henle

98
Q

isosorbide mononitrate is an

A

organic nitrate

99
Q

-prost-

A

prostacyclin and analogues

100
Q

in PAH, the __ ventricle gets larger

A

right

101
Q

familial PAH is caused by mutations in the

A

Bmpr2 gene

102
Q

riocuguat is a

A

sGC stimulator = increased cGMP

103
Q

inhaled NO is used for

A

acute vasodilator testing of PAH

pulmonary hypertensive crisis in newborns

104
Q

-etan- are

A

endothelin antagonists

105
Q

what drugs cause the largest reductions in pulmonary artery pressure

A

prostacyclin

106
Q

dobutamine is

A

beta1 effects to increase CO during cardiogenic shock

107
Q

competitive inhibitors of HMG CoA reductase

A

statins

108
Q

fibrates bind to

A

PPARalpha

109
Q

ezetimibe inhibits

A

luminal cholesterol uptak eby inhibiting NPC1L1 = reduction of incorp of cholesterole into chylomicron

110
Q

water soluble B3 complex vitamine for increasing HDL-C

A

niacin (nictontinic acid)- nicotinamide

111
Q

disorders of lipoprotein metabolism that reuslt in abnormalities in plasma cholesterol, TGs, LDL-C and/or HDL-C levels

A

hypercholesterolemia and dyslipidemia

112
Q

lipoprotein density ranking

A

chylomicron, VLDL, LDL, IDL, LDL

113
Q

what drug inhibits dietary cholesterol uptake

A

ezetimibe

114
Q

6 cholesterol drugs

A 
statins
fibrates
ezetimibe
bile acid sequestrants
nacin
PCSK9 inhibitors
115
Q

what inhibits the absorption of ezetimibe

A

bile acid sequestrants

116
Q
  • grel are
A

thienopyridines

117
Q

ASA is often combined with ____ for dual antiplatelet therapy

A

P2Y12 inhibitors

118
Q

dipyridamole actions

A

PDE inhibitor
blocks adenosine uptake
inhibits TXA2 and increases PGI2
used with ASA_ not effective alone

119
Q

is dipyridamole effective alone

A

no- use with ASA

120
Q

what is responsible for heparin’s MOA

A

pentasaccharide sequence

121
Q

are aldosterone antagonists competitive or noncompetitive

A

competitive

122
Q

in HF, you want to ___ ventricular filling

A

increase

123
Q

flurosemide is a diuretic at ____, while thazides are ____ (and ions involved)

A

loop- Na/K/Cl

DCT- Na/Cl-

124
Q

what is the danger with K+ blockers (class 3)

A

extends ventricular ERP = higher changes of TDP arrhythmias

125
Q

what gene encodes pore forming subunit of rapidly activating delayed rectifier cardiac K+ channel

A

hERG

126
Q

what class blocks VGCC (L type) and slows conduction at SA and AV nodes = slow HR

A

4 (CC blockers)

127
Q

L type calcium channels are found at

A

pacemaker cells, myocytes, and vasculature

128
Q

T type calcium channels are found at

A

pacemaker cells

129
Q

calcium channel blockers prevent Ca2+ entry via _____ channels

A

L type calcium

130
Q

NDHP are used on the ___ while ___ are used on vasculature

A 
heart = NDHP
vasculature = DHP
131
Q

electrical activity in pacemaker cells

A

funny sodium channels
T type Ca2+ channels
L type Ca2+ channels
K+ channels

132
Q

sympathetic activity at pacemaker cells on what channels? what receptors

A

funny sodium and calcium

beta1

133
Q

parasympathetic activity at pacemaker cells on what channels? what receptors

A

K+ channels increase open, close calcium

mAChR

134
Q

contractile cell AP process

A

0: rapid depolarization Na
1: small repolarization Na close
2. plateau L type Ca open
3. repolarization K+ open, Ca2+ close
4: resting K+ open-

135
Q

if stimulus occurs during phase ___ of AP (repolarization K+), what happens

A

premature AP is slower and smmaller

136
Q

QT segment

A

ventricular systole

137
Q

what causes torsades de points

A

blocking of K+ channels (hERG) = prolonged ventricular repolarization = tachycardia and ventricular fibrillation

138
Q

general classification of arrhythmias

A

site of origin

rate increase or decrease

139
Q

classes of antiarrhythmic drugs and their actions

A 
1 = Na+
2 = beta blockers
3 = K+
4 = Ca2+
140
Q

class 1A drug

A

procainamide

141
Q

class 1c drugs

A

flecainide, propafenone

142
Q

what class has a weak effect on prolonging phase 0 and shortens the ERP

A

class 1B

143
Q

class 1 Na+ blockers work on phase ___

A 
0 
and 3 (a and b)
144
Q

class 1 antiarrhytmics are ___ dependent block

A

use

145
Q

beta 1 is ___ coupled, beta 2 __ beta 3 ___

A

Gs
Gs/Gi
Gs/Gi

146
Q

what beta receptor is on the heart

A

beta1

147
Q

first generation beta blockers

A

noncardioselective 1 and 2

148
Q

second generation beta blockers

A

cardioselective- only beta1

149
Q

third generation beta blockers

A

vasodilatory properties-NO or alpha adrenergic blockade

150
Q

beta blockers affect what channels

A

Ca+ L type

funny sodium

151
Q

class 3 antiarrhythmics increase

A

ERP

152
Q

amiodarone, dronedarone, sotalol, dofetilide/ ibutilide are

A

class 3 K+ channel blockers

153
Q

class 4 are ___ inotropy, dromotropy, and chronotropy

A

negative

154
Q

what is used for treating torsades de points and digoxin induced arrhythmias

A

magnesium sulphate

155
Q

organic nitrates action besides donating NO is

A

activate sGC = increases cGMP = increases MLCP = muscle relaxation

156
Q

3 types of organic nitrates

A

eNOS by sheer force
those that release NO spontaneously- nitroprusside
those that require enzymes to release NO- organic nitrates

157
Q

do you use nitrates or dipyridamols to dilate collaterals

A

nitrates

158
Q

nicorandil is contraindicated with

A

PDE51

159
Q

ranolazine inhibits

A

cardiac ion fluxes

preferentially late sodium current

PHARM 203 (21 decks)

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