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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
what receptor interacts with DNA directly to regulate gene expression- ligant activated transcription factors
nuclear receptors
26
are nuclear receptors monomeric or multimeric
monomuric
27
class/ type 1 nuclear receptors ____ upon ligand binding and translocate to ____
dimerize | nucleus
28
how do type 1 nuclear receptors alter gene expression
bind to positive or negative hormone response elements (HREs) to activate or repress gene expression
29
where are class 2 NR found
nucleus
30
what ligands are for type 2 NR
lipids and other metabolites
31
what forms heterodimers with RXR
class 2 NR
32
what is RXR
retinoid X receptor
33
ion channel pores are filled with
H2O
34
cation nonselective channels are permeable to
Na+, Ca2+, and K+
35
cation selective channels are permeable to
either Na+, Ca2+, or K+
36
anion selective ion channels are permeable to
Cl-
37
what are ligand gated ion channel structures
tetrameric or pentameric (subunits)
38
how many types of subunits are used in ion channels
4 types | - alpha, beta, gamma, delta
39
are ligand gated ion channels fast or slow
fast | - CNS and NMJ
40
ionotropic receptors are
ligand gated ion channels
41
4 main types of ligand gated ion channels
1. Cys loop type 2. ionotropic glutamate type 3. P2X type 4. Ca2+ release type
42
what types of ion channels are used in AP generation and membrane excitability
voltage gated ion channels
43
voltage gated ion channels typically exist as (how many subunits)
tetramers
44
ligand gated ion channels typically exist as (how many subunits)
tetramers or pentamers
45
often, drugs are ____ ____ that acts as ____ inhibitor of enzymes
substrate analogue | competitive
46
with enzymes as drug targets, what can the drug act as (5 things)
reversible/ competitive substrate analogue- inhibitor) irreversible and noncompetitive false substrate prodrug- require enzymatic degradation reactive metabolite- enzymatic conversion results in drug toxicity
47
where are transporters as drug targets typically expressed
throughout body in epithelia of major organs, those with barrier function, various subcellular organelles' PMs
48
3 main families of transporters
1. ATP binding cassette (ABC) superfamily 2. solute carrier (SLC) superfamily 3. P type ATPases
49
ABC superfamily gets energy from ____ and function as ____ transporters
ATP | efflux
50
SLC superfamily tend to be involved in
influx of small molecules into cells
51
P type ATPases example
Na/K+ ATPases- helps maintain membrane potential
52
what do P type ATPases pump
ions
53
3 parts of the ANS
sympathetic parasympathetic enteric
54
4 things the ANS controls
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
55
all autonomic nerve fibres leaving CNS release ____ which acts on ___ receptors
ACh | nicotinic
56
most postganglionic sympathetic fibres release ___ which acts on ______ adrenoceptors
noradrenaline | alpha or beta
57
all postganglionic parasympathetic fibers release ____ which act on _____ receptors
acetylcholine | muscarinic
58
cholinergic transmission also occurs at
1. Sympathetic, para, enteric 2. motor endplate of voluntary (skeletal muscle) 3. within the CNS
59
pharmacological actions of ACh can be distinguished based on 2 types of activity
nicotinic and muscarinic
60
nicotinic receptors are ________ ____ _____
ligand gated ion channels | - cation permeable- Na+, K+
61
structure of nicotinic receptors
pentameric
62
3 main types of nAchRs
1. ganglionic 2. muscle 3. CNS type
63
muscarinic receptors are
GPCR
64
how many molecular subtypes of mAchRs are there
5
65
which mAchRs are Gq coupled
3
66
how many mAchRs are Gi coupled
2
67
M1, 3, 5 are ___ coupled
Gq
68
which M are Gi coupled
2 and 4
69
M1 does what
slow excitation of ganglia
70
M2 does what
decrease cardiac rate and contraction force
71
what does M3 do
cause glandular secretion - contract visceral smooth muscle - vascular relaxation by NO
72
what is vareniciline used for
treatment of nicotine addiction | - nAchR agonist
73
antagonists of nAchR effects mainly from
block of sympathetic ganglia
74
nAchRs stimulate
both sympathetic and parasympathetic = it's complex
75
general effects of nAchR agonist
increased HR and BP, variable effects on GI motility, increased bronchial, salivary, and sweat gland secretion CNS stimulation
76
nAchR antagonist effects
decrease BP bloc cardiovascular reflexes = postural hypotension GI inhibition + secretions impaired micturition
77
mAchR agonists are
parasympathomimetics
78
mAch agonists cause
decreased HR, CO, BP visceral smooth muscle contraction increased bronchial, salivary, and sweat gland secretion
79
mAch antagonists cause
increased HR (tachycardia), inhibit salivary, lacrimal, bronchial, and sweat gland secretion decreased GI motility relaxes bronchial, urinary, and biliary tract smooth muscle
80
pilocarpine is a
mAchR agonist | treats glaucomes by decreasing IOP
81
pilocarpine/ cevimeline treats
Sjogren's syndrome- increases lacrimal and salivary secretion
82
atropine is a ____ what does it treat
mAchR antagonist that treats snus bradycardia
83
tropicamide is a
mAchR antagonist - dilates pupils
84
cholinergic transmission can also occur at the motor endplate of _____ where Ach binds ____
voluntary muscle | muscle type nAchR
85
anasthesia produces a
neuromuscular block
86
drugs that produce neuromuscular blocks act by
competitively antagonizing nAChR | agonists of nAChR
87
competitive antagonists of nAChR are called
nondepolarizing agents
88
agonists (activators) of nAChR are called
depolarizing agents
89
nondepolarizing agents act by
competitive antagonism at motor endplate = block presynaptic autoreceptors + inhibit release of ACh = muscle paralysis
90
depolarizing agsnts act by
being agonists + causing persistent depolarization (acetylcholinesterase resistant) + prevents repolarizaton = initial muscle contraction followed by paralysis
91
botulium toxin acts
presynaptically to inhibit Ach release
92
what breaks down Ach
cholinesterases
93
2 types of cholinesterases
acetylcholinesterases- at cholinergic synapse | butyrylcholinesterase- plasma
94
anticholinesterase drugs enhance
Ach activity at parasympathetic postganglionic synapses
95
anticholinesterases cause ___ at NMJ
increased muscle tension, then paralysis due to depolarization block at high doses
96
anticholinesterases within the CNS cause
initial generalized excitation (via mAchR) followed by depression
97
uses of anticholinesterase drugs
1. reversal of nondepolarizing neuromuscular block following operation 2. treatment of myasthenia gravis
98
NE neurons are what
postganglionic sympathetic neurons
99
NE are found in parasympathetic or sympathetic ganglia
sympathetic
100
catecholamines are made of
catechol moiety and amine side chain
101
NE is a ____ released by ______
transmitter | sympathetic nerve terminals
102
E is a ____ secreted by _____
hormone | adrenal medulla
103
dopamine is a _____ of NA and A but is also a ____ in CNS
precursor | transmitter
104
what is isoprenaline (isoproterenol)
synthetic derivative of NA
105
2 subtypes of adrenoceptors
alpha and beta
106
all adrenoceptors are
GPCR
107
alpha1 adrenoceptor activates
IP3 signaling
108
alpha2 adrenoceptor does
inhibits AC and decreases cAMP
109
what are alpha 1 and 2 coupled to
Gq and Gi
110
what are the beta subtypes coupled to
Gs
111
what does beta2 do to blood vessels and bronchi
dilate
112
what does alpha 1 do to blood vessels and bronchi
constrict
113
what does alpha2 do to blood vessels
constrict or dilate
114
what relaxes uterus
beta2
115
what relaxes bladder detrusor
beta3
116
effects of beta 2 on skeletal muscle
tremor increased muscle mass and speed of contraction glycogenolysis
117
what inhibits histamine release from mast cells
beta2
118
what decreases adrenergic and cholingergic release
alpha2
119
what increases adrenergc release
beta 2
120
what does adrenaline act on
alpha and beta as an agonist
121
uses of adrenaline
hypotention anaphylactic shock cardiac arrest asthma- in emergencies
122
unwanted effects of adrenaline
hypertension tachycardia or reflex bradycardia ventricular dysrhythmia
123
noradrenaline acts on
alpha and beta as an agonist
124
noradrenaline is used to treat
hypotension
125
phenylephrine is used for
nasal decongestion
126
side effects of phenylephrine
hypertension | reflex bradycardia
127
phenylephrine acts on
alpha 1 as an agonist
128
salbutamol acts on
beta2 as an agonist
129
what relaxes the uterus in premature labour
beta 2 agonists- salbutamol
130
side effects of salbutamol
tachycradia dysrhythmia tremor peripheral vasodlation
131
salmeterol is similar to
salbutamol
132
mirabegron is used for
overactive bladders
133
what does mirabegron act on
beta3 agonist
134
side efffects of mirabegron
tachycardia
135
phenoxybenzamine is an
nonselective alpha antagonist
136
what is phenoxybensamine used for
phaeochromocytoma
137
side effects of phenoxybenzamine
psotural hypotension tachycardia reflex nasal congestion impotence
138
prazosin and doxazosin are
alpha 1 antagonists
139
what are prazosin and doxazosin used to treat
hypertension
140
what do propanolol and alprenolol target
nonselective beta antagonists
141
alprenolol is full or partial agonist
partial
142
what are propanolol and alprenolol used to treat
``` cardiac dysrhythmia hypertension angina anxiety, tremor glaucoma ```
143
propanolol and alprenolol side effects
``` bronchoconstriction cardiac depression cold extremities fatigue and depression hypoglycemia ```
144
metoprolol and atenolol are
beta1 antagonists
145
what do metoprolol and atenolol treat
cardiac dysrhythmia hypertension angina heart failure
146
what is the perk of metoprolol and atenolol over propanolol and alprenolol
less risk of bronchoconstriction
147
nebivolol targets
beta1 antagonist and increases NO
148
nebicolol side effects
fatigue, headache
149
nebivolol is used to treat
hypertension
150
labetalol is an
alpha beta angatonist
151
what is labetalol used to treat
hypertension in pregnancy
152
side effect of labetalol
postureal hypotension | bronchoconstriction
153
what does carvdedilol treat
heart failure
154
what does carvedilol target
beta and alpha 1 antagonist
155
what does alpha methyl tyrosine do
inhibits tyrosine hydroxylase in the synthesis of NA and A
156
uses for alpha methyl tyrosine
phaeochromocytoma
157
side effects of alphamethyl tyrosine
hypotension and sedation
158
mechanism of methyldopa
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
what do you use for hypertension in pregnancy
methyldopa or labetalol
160
methyldopa is used for
hypertension in pregnancy
161
side effects of methyldopa
hypotension, drowsiness, diahhrea, hypersensitive reactions
162
L-DOPS mechanism
a prodrug converted into NA by dopa decarboxylase
163
use for LDOPS
neurogenic orthostatic hypotension
164
side effects of LDOPS
headache, hypertension, nausea
165
drugs that release NA - indirect sympathomimetics
amphetamine and ephedrine
166
mechanism of amphetamine
stimulates NA release and inhibits reuptake
167
uses for amphetamine
CNS stimulant, narcolepsy reduces hyperactivity in children suppress appetite
168
side effects of amphetamines
hypertension, tachycardia, insomnia, acute psychosis with overdose, dependence
169
ephedrine mechanism
NA release and beta agonist
170
uses for ephedrine
Nasal decongestant and CNS stimulant
171
mechanism of imipramine
inhibits NA reuptake by blocking NET | also has anticholinergic effects
172
use for imipramine
depression
173
unwanted effects of imipramine
tachycardia dry mouth constipation postural hypotension
174
cocaine mechanism
inhibits NA reuptake by blocking NET
175
uses for cocaine
CNS stimulant and local anesthetic
176
side effects of cocaine
hypertension excitement convulsions dependence
177
what receptors are cys loop type
nAChR, GABA, 5HT
178
what receptors are ionotropic glutamate type
NMDA - ketamine
179
what receptors are calcium release type
IP3R, RyR
180
what acts at the motor endplate of skeletal muscle
ACh
181
nAchR are found at
synapse )anatomic ganglia or CNS) or neuromuscular junction

PHARM 203 (21 decks)

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