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PHARM 203 > Jurasz > Flashcards

Jurasz Flashcards

1
Q

4 types of drug targets

A

receptors
ion channels
enzymes
transporters

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2
Q

3 main families of receptors

A

GPCR
kinase linked and related receptors
nuclear receptors

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3
Q

how many TM helices does GPCR have? what is the structure called?

A

7

heptahelical

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4
Q

how many polypeptide chains do GPCR have

A

1

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5
Q

where is the N terminal and C terminal in GPCR

A 
N = outside
C = inside
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6
Q

are GPCR fast or slow

A

slow

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7
Q

can GPCR oligomerize to form dimers or larger oligomers

A

yes

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8
Q

what is the most common class of targets for therapeutic drugs

A

GPCR

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9
Q

GPCR are normally activated by ______ ______, but some are activated by protease mediated cleavage of the _____

A

agonist binding

N terminal

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10
Q

how many subunits do G proteins have

A

3- alpha, beta, gamma

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11
Q

when agonist binds to receptor, the subunit binds ____ and ____ to activate or inhibit an effector enzyme

A

GTP

dissociates

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12
Q

kinase linked and related receptors are activated by

A

protein mediators

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13
Q

what are protein mediators

A

growth factors, cytokines, hormones

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14
Q

how many membrane spanning helixes/ chains do kinase linked receptors have

A

1

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15
Q

what receptors control cell division, metabolism, growth, differentiation, inflammation, tissue repair, apoptosis, and immune response

A

kinase linked receptors

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16
Q

kinase linked receptor activation generally involves _____ of receptors and ________ of receptors

A

dimerization

cross autophosphorylation

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17
Q

3 main types of kinase linked receptors

A
  1. receptor tyrosine kinases (RTKs)
  2. receptor serine/ threonine kinases
  3. cytokine receptors
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18
Q

what receptors are for growth factors such as epidermal and vascular endothelial growth factor

A

RTKs

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19
Q

what cascade do RTKs activate

A

MAPK cascade

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20
Q

what receptors regulate gene transcription through MAPK cascade

A

RTKs

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21
Q

what do serine/ threonine kinases phosphorylate

A

ser/thr residues

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22
Q

what kind of receptor is transforming growth factor (TGF) receptor

A

receptor serine/ threonine kinases

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23
Q

cytokine receptors have _____ domains that activate _____ with lingand binding

A

intracellular

cytosolic (tyrosine) kinases

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24
Q

where do nuclear receptors reside

A

cytosol or nucleus

those in the cytosol translocate to the nucleus upon ligand binding

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25
Q

what receptor interacts with DNA directly to regulate gene expression- ligant activated transcription factors

A

nuclear receptors

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26
Q

are nuclear receptors monomeric or multimeric

A

monomuric

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27
Q

class/ type 1 nuclear receptors ____ upon ligand binding and translocate to ____

A

dimerize

nucleus

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28
Q

how do type 1 nuclear receptors alter gene expression

A

bind to positive or negative hormone response elements (HREs) to activate or repress gene expression

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29
Q

where are class 2 NR found

A

nucleus

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30
Q

what ligands are for type 2 NR

A

lipids and other metabolites

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31
Q

what forms heterodimers with RXR

A

class 2 NR

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32
Q

what is RXR

A

retinoid X receptor

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33
Q

ion channel pores are filled with

A

H2O

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34
Q

cation nonselective channels are permeable to

A

Na+, Ca2+, and K+

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35
Q

cation selective channels are permeable to

A

either Na+, Ca2+, or K+

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36
Q

anion selective ion channels are permeable to

A

Cl-

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37
Q

what are ligand gated ion channel structures

A

tetrameric or pentameric (subunits)

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38
Q

how many types of subunits are used in ion channels

A

4 types

- alpha, beta, gamma, delta

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39
Q

are ligand gated ion channels fast or slow

A

fast

- CNS and NMJ

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40
Q

ionotropic receptors are

A

ligand gated ion channels

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41
Q

4 main types of ligand gated ion channels

A
  1. Cys loop type
  2. ionotropic glutamate type
  3. P2X type
  4. Ca2+ release type
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42
Q

what types of ion channels are used in AP generation and membrane excitability

A

voltage gated ion channels

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43
Q

voltage gated ion channels typically exist as (how many subunits)

A

tetramers

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44
Q

ligand gated ion channels typically exist as (how many subunits)

A

tetramers or pentamers

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45
Q

often, drugs are ____ ____ that acts as ____ inhibitor of enzymes

A

substrate analogue

competitive

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46
Q

with enzymes as drug targets, what can the drug act as (5 things)

A

reversible/ competitive substrate analogue- inhibitor)
irreversible and noncompetitive
false substrate
prodrug- require enzymatic degradation
reactive metabolite- enzymatic conversion results in drug toxicity

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47
Q

where are transporters as drug targets typically expressed

A

throughout body in epithelia of major organs, those with barrier function, various subcellular organelles’ PMs

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48
Q

3 main families of transporters

A
  1. ATP binding cassette (ABC) superfamily
  2. solute carrier (SLC) superfamily
  3. P type ATPases
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49
Q

ABC superfamily gets energy from ____ and function as ____ transporters

A

ATP

efflux

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50
Q

SLC superfamily tend to be involved in

A

influx of small molecules into cells

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51
Q

P type ATPases example

A

Na/K+ ATPases- helps maintain membrane potential

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52
Q

what do P type ATPases pump

A

ions

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53
Q

3 parts of the ANS

A

sympathetic
parasympathetic
enteric

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54
Q

4 things the ANS controls

A
  1. heartbeat
  2. contraction/ relaxation of vascular and visceral smooth muscle
  3. exocrine and some endocrine secretion
  4. energy metabolism- esp in the liver and skeletal muscle
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55
Q

all autonomic nerve fibres leaving CNS release ____ which acts on ___ receptors

A

ACh

nicotinic

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56
Q

most postganglionic sympathetic fibres release ___ which acts on ______ adrenoceptors

A

noradrenaline

alpha or beta

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57
Q

all postganglionic parasympathetic fibers release ____ which act on _____ receptors

A

acetylcholine

muscarinic

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58
Q

cholinergic transmission also occurs at

A
  1. Sympathetic, para, enteric
  2. motor endplate of voluntary (skeletal muscle)
  3. within the CNS
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59
Q

pharmacological actions of ACh can be distinguished based on 2 types of activity

A

nicotinic and muscarinic

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60
Q

nicotinic receptors are ________ ____ _____

A

ligand gated ion channels

- cation permeable- Na+, K+

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61
Q

structure of nicotinic receptors

A

pentameric

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62
Q

3 main types of nAchRs

A
  1. ganglionic
  2. muscle
  3. CNS type
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63
Q

muscarinic receptors are

A

GPCR

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64
Q

how many molecular subtypes of mAchRs are there

A

5

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65
Q

which mAchRs are Gq coupled

A

3

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66
Q

how many mAchRs are Gi coupled

A

2

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67
Q

M1, 3, 5 are ___ coupled

A

Gq

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68
Q

which M are Gi coupled

A

2 and 4

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69
Q

M1 does what

A

slow excitation of ganglia

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70
Q

M2 does what

A

decrease cardiac rate and contraction force

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71
Q

what does M3 do

A

cause glandular secretion

  • contract visceral smooth muscle
  • vascular relaxation by NO
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72
Q

what is vareniciline used for

A

treatment of nicotine addiction

- nAchR agonist

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73
Q

antagonists of nAchR effects mainly from

A

block of sympathetic ganglia

74
Q

nAchRs stimulate

A

both sympathetic and parasympathetic = it’s complex

75
Q

general effects of nAchR agonist

A

increased HR and BP, variable effects on GI motility, increased bronchial, salivary, and sweat gland secretion
CNS stimulation

76
Q

nAchR antagonist effects

A

decrease BP
bloc cardiovascular reflexes = postural hypotension
GI inhibition + secretions
impaired micturition

77
Q

mAchR agonists are

A

parasympathomimetics

78
Q

mAch agonists cause

A

decreased HR, CO, BP
visceral smooth muscle contraction
increased bronchial, salivary, and sweat gland secretion

79
Q

mAch antagonists cause

A

increased HR (tachycardia), inhibit salivary, lacrimal, bronchial, and sweat gland secretion
decreased GI motility
relaxes bronchial, urinary, and biliary tract smooth muscle

80
Q

pilocarpine is a

A

mAchR agonist

treats glaucomes by decreasing IOP

81
Q

pilocarpine/ cevimeline treats

A

Sjogren’s syndrome- increases lacrimal and salivary secretion

82
Q

atropine is a ____ what does it treat

A

mAchR antagonist that treats snus bradycardia

83
Q

tropicamide is a

A

mAchR antagonist - dilates pupils

84
Q

cholinergic transmission can also occur at the motor endplate of _____ where Ach binds ____

A

voluntary muscle

muscle type nAchR

85
Q

anasthesia produces a

A

neuromuscular block

86
Q

drugs that produce neuromuscular blocks act by

A

competitively antagonizing nAChR

agonists of nAChR

87
Q

competitive antagonists of nAChR are called

A

nondepolarizing agents

88
Q

agonists (activators) of nAChR are called

A

depolarizing agents

89
Q

nondepolarizing agents act by

A

competitive antagonism at motor endplate = block presynaptic autoreceptors + inhibit release of ACh = muscle paralysis

90
Q

depolarizing agsnts act by

A

being agonists + causing persistent depolarization (acetylcholinesterase resistant) + prevents repolarizaton = initial muscle contraction followed by paralysis

91
Q

botulium toxin acts

A

presynaptically to inhibit Ach release

92
Q

what breaks down Ach

A

cholinesterases

93
Q

2 types of cholinesterases

A

acetylcholinesterases- at cholinergic synapse

butyrylcholinesterase- plasma

94
Q

anticholinesterase drugs enhance

A

Ach activity at parasympathetic postganglionic synapses

95
Q

anticholinesterases cause ___ at NMJ

A

increased muscle tension, then paralysis due to depolarization block at high doses

96
Q

anticholinesterases within the CNS cause

A

initial generalized excitation (via mAchR) followed by depression

97
Q

uses of anticholinesterase drugs

A
  1. reversal of nondepolarizing neuromuscular block following operation
  2. treatment of myasthenia gravis
98
Q

NE neurons are what

A

postganglionic sympathetic neurons

99
Q

NE are found in parasympathetic or sympathetic ganglia

A

sympathetic

100
Q

catecholamines are made of

A

catechol moiety and amine side chain

101
Q

NE is a ____ released by ______

A

transmitter

sympathetic nerve terminals

102
Q

E is a ____ secreted by _____

A

hormone

adrenal medulla

103
Q

dopamine is a _____ of NA and A but is also a ____ in CNS

A

precursor

transmitter

104
Q

what is isoprenaline (isoproterenol)

A

synthetic derivative of NA

105
Q

2 subtypes of adrenoceptors

A

alpha and beta

106
Q

all adrenoceptors are

A

GPCR

107
Q

alpha1 adrenoceptor activates

A

IP3 signaling

108
Q

alpha2 adrenoceptor does

A

inhibits AC and decreases cAMP

109
Q

what are alpha 1 and 2 coupled to

A

Gq and Gi

110
Q

what are the beta subtypes coupled to

A

Gs

111
Q

what does beta2 do to blood vessels and bronchi

A

dilate

112
Q

what does alpha 1 do to blood vessels and bronchi

A

constrict

113
Q

what does alpha2 do to blood vessels

A

constrict or dilate

114
Q

what relaxes uterus

A

beta2

115
Q

what relaxes bladder detrusor

A

beta3

116
Q

effects of beta 2 on skeletal muscle

A

tremor
increased muscle mass and speed of contraction
glycogenolysis

117
Q

what inhibits histamine release from mast cells

A

beta2

118
Q

what decreases adrenergic and cholingergic release

A

alpha2

119
Q

what increases adrenergc release

A

beta 2

120
Q

what does adrenaline act on

A

alpha and beta as an agonist

121
Q

uses of adrenaline

A

hypotention
anaphylactic shock
cardiac arrest
asthma- in emergencies

122
Q

unwanted effects of adrenaline

A

hypertension
tachycardia or reflex bradycardia
ventricular dysrhythmia

123
Q

noradrenaline acts on

A

alpha and beta as an agonist

124
Q

noradrenaline is used to treat

A

hypotension

125
Q

phenylephrine is used for

A

nasal decongestion

126
Q

side effects of phenylephrine

A

hypertension

reflex bradycardia

127
Q

phenylephrine acts on

A

alpha 1 as an agonist

128
Q

salbutamol acts on

A

beta2 as an agonist

129
Q

what relaxes the uterus in premature labour

A

beta 2 agonists- salbutamol

130
Q

side effects of salbutamol

A

tachycradia
dysrhythmia
tremor
peripheral vasodlation

131
Q

salmeterol is similar to

A

salbutamol

132
Q

mirabegron is used for

A

overactive bladders

133
Q

what does mirabegron act on

A

beta3 agonist

134
Q

side efffects of mirabegron

A

tachycardia

135
Q

phenoxybenzamine is an

A

nonselective alpha antagonist

136
Q

what is phenoxybensamine used for

A

phaeochromocytoma

137
Q

side effects of phenoxybenzamine

A

psotural hypotension
tachycardia reflex
nasal congestion
impotence

138
Q

prazosin and doxazosin are

A

alpha 1 antagonists

139
Q

what are prazosin and doxazosin used to treat

A

hypertension

140
Q

what do propanolol and alprenolol target

A

nonselective beta antagonists

141
Q

alprenolol is full or partial agonist

A

partial

142
Q

what are propanolol and alprenolol used to treat

A 
cardiac dysrhythmia
hypertension
angina
anxiety, tremor
glaucoma
143
Q

propanolol and alprenolol side effects

A 
bronchoconstriction
cardiac depression
cold extremities 
fatigue and depression
hypoglycemia
144
Q

metoprolol and atenolol are

A

beta1 antagonists

145
Q

what do metoprolol and atenolol treat

A

cardiac dysrhythmia
hypertension
angina
heart failure

146
Q

what is the perk of metoprolol and atenolol over propanolol and alprenolol

A

less risk of bronchoconstriction

147
Q

nebivolol targets

A

beta1 antagonist and increases NO

148
Q

nebicolol side effects

A

fatigue, headache

149
Q

nebivolol is used to treat

A

hypertension

150
Q

labetalol is an

A

alpha beta angatonist

151
Q

what is labetalol used to treat

A

hypertension in pregnancy

152
Q

side effect of labetalol

A

postureal hypotension

bronchoconstriction

153
Q

what does carvdedilol treat

A

heart failure

154
Q

what does carvedilol target

A

beta and alpha 1 antagonist

155
Q

what does alpha methyl tyrosine do

A

inhibits tyrosine hydroxylase in the synthesis of NA and A

156
Q

uses for alpha methyl tyrosine

A

phaeochromocytoma

157
Q

side effects of alphamethyl tyrosine

A

hypotension and sedation

158
Q

mechanism of methyldopa

A

converted to methylnoradrenaline which can not be broken down by MAO
accumulates and displaces NA in synaptic vesicles = no conversion into A and blocks effects

159
Q

what do you use for hypertension in pregnancy

A

methyldopa or labetalol

160
Q

methyldopa is used for

A

hypertension in pregnancy

161
Q

side effects of methyldopa

A

hypotension, drowsiness, diahhrea, hypersensitive reactions

162
Q

L-DOPS mechanism

A

a prodrug converted into NA by dopa decarboxylase

163
Q

use for LDOPS

A

neurogenic orthostatic hypotension

164
Q

side effects of LDOPS

A

headache, hypertension, nausea

165
Q

drugs that release NA - indirect sympathomimetics

A

amphetamine and ephedrine

166
Q

mechanism of amphetamine

A

stimulates NA release and inhibits reuptake

167
Q

uses for amphetamine

A

CNS stimulant, narcolepsy
reduces hyperactivity in children
suppress appetite

168
Q

side effects of amphetamines

A

hypertension, tachycardia, insomnia, acute psychosis with overdose, dependence

169
Q

ephedrine mechanism

A

NA release and beta agonist

170
Q

uses for ephedrine

A

Nasal decongestant and CNS stimulant

171
Q

mechanism of imipramine

A

inhibits NA reuptake by blocking NET

also has anticholinergic effects

172
Q

use for imipramine

A

depression

173
Q

unwanted effects of imipramine

A

tachycardia
dry mouth
constipation
postural hypotension

174
Q

cocaine mechanism

A

inhibits NA reuptake by blocking NET

175
Q

uses for cocaine

A

CNS stimulant and local anesthetic

176
Q

side effects of cocaine

A

hypertension
excitement
convulsions
dependence

177
Q

what receptors are cys loop type

A

nAChR, GABA, 5HT

178
Q

what receptors are ionotropic glutamate type

A

NMDA - ketamine

179
Q

what receptors are calcium release type

A

IP3R, RyR

180
Q

what acts at the motor endplate of skeletal muscle

A

ACh

181
Q

nAchR are found at

A

synapse )anatomic ganglia or CNS) or neuromuscular junction

PHARM 203 (21 decks)

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