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Pharmacology > Neuropharmacology > Flashcards

Neuropharmacology Flashcards

1
Q

What do the nervous system and endocrine system do?

A

coordinate the regulation and integration of body functions

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2
Q

Endocrine system

A

various levels of blood-borne hormones

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3
Q

nervous system

A

transfer signals via the transmission of electrical impulses over nerve fibers to effector cells, which release neuromodulator substances

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4
Q

Central Nervous System

A

brain and spinal cord

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5
Q

Peripheral Nervous System

A

neurons located outside the brain and spinal cord

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6
Q

efferent nervous system

A

efferent neurons deliver signals away from the CNS to the peripheral tissues

autonomic nervous system and somatic nervous system

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7
Q

Afferent nervous system

A

afferent neurons deliver signals from the peripheral tissues to the CNS
provide sensory info to regulate the function of the efferent division through neural pathways

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8
Q

Somatic Nervous System

A

voluntary functions
contraction of skeletal muscles, essential for locomotion

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9
Q

Autonomic nervous system

A

involuntary functions
vital bodily functions without consciousness
require sensory input from peripheral structures to provide information on the current state of the body
includes the sympathetic nervous system, the parasympathetic nervous system, and the enteric nervous system

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10
Q

ganglion

A

collection of neuron cell bodies in the PNS
functions for communication

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11
Q

Where are preganglionic neurons located

A

in the CNS

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12
Q

Where are postganglionic neurons located?

A

distal/posterior to a ganglion

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13
Q

Functions of the sympathetic nervous system

A

adjust to stressful situations
incr heart rate and blood pressure
incr blood flow to skeletal muscles and the heart
divert flow from the skin and internal organs
dilate pupils and bronchioles

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14
Q

Functions of parasympathetic nervous system

A

maintain homeostasis within the body, essential bodily functions
opposes/balances the actions of the sympathetic division

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15
Q

Sympathetic has wide distribution and parasympathetic has x

A

short distribution

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16
Q

Hormones

A

endocrine cells secrete hormones into the circulation, traveling throughout the body, initiating effects on target cells

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17
Q

Local mediators

A

cells secrete chemicals that act on nearby cells
rapidly destroyed, don’t enter circulation

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18
Q

Neurotransmitters

A

communications between nerve cells occurs via chemical signals released from the nerve terminals
triggered by arrival of action potential at the nerve ending

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19
Q

How are neurotransmitters signals mediated?

A

by binding to receptors on the cell surface of target organs

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20
Q

Types of neurotransmitters in the autonomic nervous systems

A

ACh
NE
Epi

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21
Q

Sympathetic innervation of adrenal medulla

A

preganglionic neuron releases ACh
it binds to nicotinic receptor on adrenal medulla
Epi and NE released into blood
they bind to adrenergic receptor

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22
Q

Sympathetic path

A

preganglionic neuron releases ACh
it binds to the nicotinic receptor
postganglioni neuron releases NE
NE binds to adrenergic receptor

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23
Q

parasympathetic path

A

preganglionic neuron releases ACh
binds to nicotinic receptor
postganglionic neurons release ACh
binds to muscarinic receptor

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24
Q

M1, M3, M5

A

stimulators of muscarinic receptors in parasympathetic nervous system
Gq-PLC-IP3/ DAG- Ca^2+

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25
Q

M2, M4

A

inhibitory muscarinic receptors in parasympathetic nervous system
inhibits adenylyl cyclase and regulates specific ion channels

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26
Q

Synthesis and Release of ACh from cholinergic neuron

A
  1. Ach is made
  2. taken up into storage vesicles
  3. released in to synaptic cleft
  4. binds to nAChR
  5. AChE degrades ACh
  6. Choline is take back up by the neuron
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27
Q

muscarinic receptors

A

cholinoceptors
weak affinity for nicotine
GPCR

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28
Q

nicotinic receptor

A

cholinoceptors
weak affinity for muscadine
iontropic receptor

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29
Q

What does ACh do to the cardiovascular system?

A

vasodilation
decr heart rate, cardiac conduction velocity in AV-node, and force of contraction

effects mediated by M2 receptors:
incr K^+ current
decr L type Ca^2+ current
decr cAMP
inhibition of NE release form sympathetic nerve terminals

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30
Q

What does ACh do to the respiratory tract?

A

bronchoconstriction
increased tracheobronchial secretion
effects mediated by activation of M3 receptors

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31
Q

What does ACh do to the urinary tract?

A

detrusor muscle contraction
incr urinary voiding pressure
ureteral peristalsis
effects mediated by M2 and M3 receptors

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32
Q

What does ACh do to the GI tract?

A

incr tone of GI muscle, muscle contraction, secretory activity of stomach and intestine
effects mediated by M2 and M3 receptors

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33
Q

What secretory and ocular effects is ACh responsible for?

A

glandular secretion
mitosis
effects mediated by M1 and M3 receptors

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34
Q

What effects does ACh have on the CNS?

A

cognition
motor control
appetite regulation
nociception
arousal
effects mediated by all 5 muscarinic receptors

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35
Q

Acetylcholine

A

muscarinic agonist
direct acting
used topically to induce miosis during eye exams or ophthalmic surgery
ganglionic blocker - arousal and cognitive enhancement

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36
Q

Methacholine

A

muscarinic agonist
used as an inhalant to diagnose bronchial airway hypersensitivity in patients with subclinical asthma

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37
Q

Bethanechol

A

muscarinic agonist
directs acting
used for treating urinary retention & inadequate emptying of bladder postoperatively
used to stimulate GI tract peristalsis and increase LES pressure

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38
Q

Pilocarpine

A

muscarinic agonist
direct acting
used to treat xerostomia following head and neck irradiation and Sjogren syndrome
used topically to treat glaucoma and as a miotic agent
reduces intraocular pressure in open and narrow angle glaucomas
uncharged tertiary amine that can penetrate the CNS

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39
Q

Contraindications of Muscarinc Agonists

A

asthma
COPD
urinary/GI obstruction
acid-peptic disease
cardiovascular disease
hypotension
hyperthyroidism

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40
Q

Adverse Effects of Muscarinic Receptor Agonists

A

Diaphoresis
NVD, abdominal cramps
blurry vision
hypotension

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41
Q

Muscarinic Receptor Antagonists

A

Prevents effects of ACh by binding to muscarinic receptors
little effect on nicotinic receptors

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42
Q

Ipatropium [Atrovent]

A

muscarinic receptor antagonist
used in respiratory tract to treat COPD, frequently in combo with inhaled long-acting beta 2 adrenergic receptor agonists

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43
Q

Tiotropium [Spriva]

A

muscarinic receptor antagonist
derivative of atropine, bronchodilator
used in respiratory tract to treat COPD, frequently in combo with inhaled long-acting beta 2 adrenergic receptor agonists

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44
Q

Oxybutynin [Ditropan]

A

muscarinic antagonist
used in the genitourinary tract to treat overactive bladder; relaxes detrusor muscle of the bladder

synthetic atropine-like drug

adverse effects: xerostomia, blurred vision, constipation and dyspepsia, drowsiness and confusion

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45
Q

Atropine

A

muscarinic antagonist
binds competitively and prevents ACh from binding to muscarinic receptors

used in GI tract to treat irritable bowl and increased tone, and to decrease GI motility

used in the cardiovascular system to reduce the degree AV-block that results from overactive parasympathetic tone

used in anesthesia to block vagaries responses to surgical manipulation of visceral organs

used to treat
- AChE poisoning from use of pesticides and nerve gas agents
- Spastic disorders of the GI tract
- organophosphate poisoning
- suppress respiratory secretions prior to surgery
- bradycardia

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46
Q

Homatropine [Ispto Homatropine]

A

muscarinic antagonist
administered topically to the eye to induce mydriasis and cycloplegia

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47
Q

Scopolamine [Transderm Scop]

A

muscarinic antagonist
used for the CNS
admin as a transdermal patch prophylactically to treat motion sickness

peripheral effects similar to atropine
greater actions in the CNS and longer duration of action compare to atropine

adverse effects: dry mouth, drowsiness, blurred vision i

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48
Q

Benztropine Mesylate [Cogentin]

A

muscarinic antagonist
used for the CNS
used to treat extrapyramidal side effects of antipsychotic drugs

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49
Q

Contraindications of Antimuscarinic agents

A

urinary tract/ GI obstruction

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50
Q

Adverse effects of antimuscarinic agents

A

xerostomia
constipation
blurred vision
dyspepsia
cognitive impairment

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51
Q

AChE inhibitors

A

enhance cholinergic tone by selectively blocking AChE
acts at cholinergic neuroeffector junctions

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52
Q

There are no vascular adverse effects with AChE because there is not x on the muscarinic receptors on the endothelium of blood vessels

A

cholinergic nerve fibers

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53
Q

Categories of AChE inhibitors

A

Reversible inhibitors
carbamylatipm inhibitors
organophosphate inhibitors

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54
Q

What kind of binding do reversible AChE inhibitors have?

A

non-covalent

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55
Q

Donepezil [Aricept]

A

AChE reversible inhibitor
used to treat the symptoms of Alzheimer’s disease
has not been shown to reduce healthcare costs/delay institutionalization
can be used with memantine in moderate to severe disease

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56
Q

What kind of binding do carbamylatipm inhibitors have?

A

Immediate duration covalent binding (15-30 min)

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57
Q

Neostigmine [Prostigmin]

A

indirect acting reversible muscarinic agonist carbamylatipm AChE inhibitor
used to treat myasthenia gravis, urinary retention without blockage and paralytic ileus
prevents postoperative abdominal distention
used as an antidote for competitive neuromuscular blockers
has intermediate duration of action 0.5-2hrs

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58
Q

What kind of binding do organophosphate inhibitors have?

A

long duration covalent binding (hours-permanent)

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59
Q

Malathion, and insecticide, and sarin, a nerve gas, are both examples of?

A

organophosphate AChE inhibitors

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60
Q

What effects do AChE inhibitors have on the body?

A

eye- miosis

GI Tract- enhanced gastric contractions, increased secretion of gastric acid, increased activity of small and large bowel

increased glandular secretion
increased contraction of smooth muscle of bronchioles and ureters decreased cardiac output
bradycardia

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61
Q

What are the symptoms of AChE inhibitor overdose?

A

salivation
lacrimation
urination
defecation

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62
Q

Nicotine

A

nicotinic agonist
acts at the neuromuscular junction
in PNS - transited stimulation followed by depression of autonomic ganglia and neuromuscular junction leading to paralysis
in CNS- stimulation, weak analgesia, tremors leading to seizures at toxic doses, excitation of respiration, nausea and vomiting
used in smoking cessation

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63
Q

Varenicline [Chantex]

A

nicotinic agonist
acts at the neuromuscular junction
partial agonist at nicotinic receptor
used in smoking cessation

adverse effects: mood and behavior changes

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64
Q

Pancuronium [Pavulon]

A

competitive nicotinic receptor antagonist
induces muscle paralysis by blocking nicotinic receptors at the neuromuscular junction
used for muscle relaxation during general anesthesia
used in the lethal injection cocktail

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65
Q

Direct acting muscarinic agonists

A

acetylcholine
bethanechol
carbachol
pilocarpine
nicotine

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66
Q

Indirect acting reversible muscarinic agonist

A

edrophonium
physostigmine
neostigmine
pyridostigmine
ambenonium
donepezil
rivastigmine
galantamine

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67
Q

indirect acting irreversible muscarinic agents

A

ecothiphate

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68
Q

Which muscarinic agonist reactivates AChE?

A

pralidoxime

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69
Q

Antimuscarinic agents examples

A

atropine
ipratropium
tiotropium
tropicamide
cyclopentolate
benztropine
trihexyphenidyl
darifenacin
fesoterodine
oxybutynin
solifenacin
tolterodine
trospium chloride

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70
Q

Which muscarinic antagonist is a ganglionic blocker?

A

nicotine

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71
Q

What are the 2 types of neuromuscular blockers?

A

nondepolarizing and depolarizing

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72
Q

Adrenergic agonist direct acting agents

A

epinephrine
norepinephrine
isoproterenol
dopamine
fenoldopam
dobutamine
phenylephrine
clonidine
albuterol
terbutaline
salmeterol
formoterol
mirabegron

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73
Q

indirect acting adrenergic agonists

A

amphetamine
cocaine

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74
Q

mixed action adrenergic agonists

A

ephedrine
pseudoephedrine

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75
Q

adrenergic antagonists: alpha blockers

A

phenoxybenzamine
phentolamine
prazosin
terazosin
doxazosinn
tamsulosin
alfuzosin
Yohimbine

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76
Q

Adrenergic Antagonists: Beta blockers- nonselective

A

propranolol
nadolol
timolol

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77
Q

Adrenergic antagonists: beta 1 blockers- selective

A

acebutolol
atenolol
betaxolol
bisprolol
esmolol
metaprolol
nebivolol

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78
Q

adrenergic antagonists: beta blockers with partial agonist activity

A

acebutolol
pindolol

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79
Q

adrenergic antagonists: beta blockers- antagonists of both alpha and beta adrenoreceptors

A

labetalol
carvedilol

80
Q

Which adrenergic antagonist affects neurotransmitter uptake or release?

A

reserpine

81
Q

physostigmine

A

indirect acting reversible muscarinic agonist
increases intestinal and bladder motility
reverses CNS and cardia effects of tricyclic antidepressants
reverses CNS effects of Atropine
uncharged tertiary amine that can penetrate the CNS

82
Q

Rivastigmine

A

indirect acting reversible muscarinic agonist
first line treatment for Alzheimer’s disease
not been shown to reduce healthcare costs/delay institutionalization
can be used with memantine in moderate to severe disease

83
Q

Galantamine

A

indirect acting reversible muscarinic agonist
first line treatment for alzheimer’s disease
has not been shown to reduce healthcare costs/ delay institutionalization
can be used with memantine

84
Q

What do antimuscarinic agents do?

A

blocks the muscarinic receptor and inhibits muscarinic function

85
Q

What do ganglionic blockers do?

A

blocks the entire output of ANS at the nicotinic receptor

86
Q

What do neuromuscular blockers do?

A

block cholinergic transmission between motor nerve endings and the nicotinic receptors on the skeletal muscles

87
Q

Ipatropium

A

muscarinic antagonist
derivatives of atropine, bronchodilator
used to treat COPD

88
Q

Tropicamide

A

muscarinic blocker
duration of action is shorter than atropine
in ophthalmology used to produce mydriasis and cycloplegia prior to refraction

89
Q

Cyclopentolate

A

muscarinic blocker
duration of action is shorter than atropine
in ophthalmology used to produce mydriasis and cycloplegia prior to refraction

90
Q

Benztropine

A

muscarinic blocker
adjuncts with other antiparkinsonian agents
used to treat Parkinson’s disease

91
Q

Trihexyphenidyl

A

muscarinic blocker
adjuncts with other antiparkinsonian agents
used to treat Parkinson’s disease

92
Q

Darifenacin

A

muscarinic blocker
synthetic atropine-like drug
used to treat overactive urinary bladder

93
Q

Fesoterodine

A

muscarinic blocker
synthetic atropine-like drug
used to treat overactive urinary bladder

94
Q

Solifenacin

A

muscarinic blocker
synthetic atropine-like drug
used to treat overactive urinary bladder

95
Q

Tolterodine

A

muscarinic blocker
synthetic atropine-like drug
used to treat overactive urinary bladder

96
Q

Trospium Chloride

A

muscarinic blocker
synthetic atropine-like drug
used to treat overactive urinary bladder

97
Q

Adverse effects of muscarinic antagonists

A

blurred vision
confusion
mydriasis
constipation
urinary retention

98
Q

Dopamine

A

ganglionic blocker
pleasure
appetite suppression
catecholamine
alpha 1 and beta 1 receptors
treats shock and congestive heart failure
raises blood pressure
increased cardiac output, increased blood flow

99
Q

Norepinephrine

A

ganglionic blocker
arousal
appetite suppression

100
Q

Glutamate

A

ganglionic blockers
learning + memory enhancement
NMDA receptors- calcium and sodium channels
in the brian
neuronal excitation
synaptic plasticity
excitotoxicity

101
Q

Serotonin

A

ganglionic blocker
mood modulation
appetite suppression
5HT3 receptor
excitatory; gates sodium, potassium, and calcium ions
in the CNS and PNS
nauesea and vomiting, anxiety, seizure propensity, pro-nociception

102
Q

Beta Endorphin

A

ganglionic blocker
anxiety and tension reduction

103
Q

GABA

A

ganglionic blocker
anxiety and tension reduction
receptor is inhibitory and gates Cl^-
major inhibitory transmitter in the CNS
hyperpolarizes cell membranes
decreases neuronal fibrin rate
in the CNS
anxiolytic, anticonvulsant, amnesic, sedative, hypnotic, muscle relaxant

104
Q

Blocking sympathetic ganglion means

A

reduction in norepinephrine release
reduction in heart rate and blood pressure

105
Q

Blocking parasympathetic ganglion means

A

reduction in ACh release
increase in heart rate

106
Q

Nondepolarizing competitive neuromuscular blocking drugs

A

pancuronium, vecuronium, cistracurium, rocuronium
highly polar compounds that are poorly absorbed from the GI tract; preferred parenteral admin

low doses competitively block ACh at the nicotinic receptors

high doses block the ion channels of the motor endplate, leads to weakening of neuromuscular transmission, resulting in decrease of the ability of AChE inhibitors to reverse nondepolarizing blocker’s action

used for muscle relaxation during general anesthesia and in the lethal injection cocktail

safe with minimal side effects

107
Q

Depolarizing neuromuscular blocking agents

A

succinylcholine
binds to the nAChR and acts like ACh to depolarize the junction
rapid onset
used for rapid endotracheal intubation during the induction of anesthesia, electronvulsive shock treatment

adverse effects: hyperthermia, apnea, hyperkalemia

108
Q

Adrenergic drugs affect receptors stimulated by

A

norepinephrine and epinephrine

109
Q

Sympathomimetics

A

adrenergic drugs activating adrenergic receptors

110
Q

Sympathy lyrics

A

drugs blocking the activation of adrenergic receptors

111
Q

What does DOPA stand for?

A

dihydroxyphenyalanine
prodrug

112
Q

What does COMT stand for?

A

catechol-O-methyltransferase

113
Q

What does MOA stand for?

A

monoamine oxidase

114
Q

What does SNRI stand for?

A

serotonin-norepinephrine reuptake inhibitor

115
Q

Steps for the release of norepinephrine from the adrenergic neuron

A
  1. hydroxylation of tyrosine makes dopamine
  2. uptake into storage vesicles and converted to norepinephrine
  3. Norepinephrine is released into the synaptic cleft
  4. Norepinephrine binds to receptors
  5. norepinephrine is taken back up into the neuron
  6. norepinephrine is methylated by COMT and. oxidized by MAO
116
Q

alpha1 adrenoreceptors

A

on postsynaptic membrane of the effector organs
leads to constriction of smooth muscle
GPCR- generates IP3 and DAG which turns on cytosolic proteins and releases calcium ions

117
Q

alpha 2 adrenoreceptors

A

on presynaptic nerve endings
decreases NE release and inhibits cAMP production
inhibits release of ACh

118
Q

What are the effects of alpha1 receptors?

A

vasoconstriction
increased peripheral resistance
increased blood pressure
mydriasis
increased closure of internal sphincter of the bladder

119
Q

What are the effects of alpha2 receptors?

A

inhibition of norepinephrine release
inhibition of ACh release
inhibition of insulin release

120
Q

What are the effects of beta1 receptors?

A

tachycardia
increased myocardial contractility
increased release of renin

121
Q

What are the effects of beta 2 receptors?

A

vasodilation
decreased peripheral resistance
bronchodilation
increased muscle and liver glycogenolysis
increased release of glucagon
relaxed uterine smooth muscle
increase plasma glucose concentration

122
Q

What are the effects of beta 3 receptors?

A

increased lipolysis
relaxation of detrusor muscles

123
Q

Catecholamines

A

compounds containing a 3,4-dihydroxybenzene group
high potency to activate receptors
rapid inactivation due to metabolism by COMT and MOA
polar -> poor penetration into the CNS
brief duration of action
not admin orally
epinephrine
norepinephrine
isoproterenol
dopamine

124
Q

Noncatecholamines

A

compounds w/o catechol hydroxyl groups
longer half lives since they are not inactivated by COMT
poorly metabolized by MOA
increased lipid solubility -> greater access to CNS
phenylephirine
ephedrine
amphetamine

125
Q

Epinephrine

A

alpha 1 and alpha 2, beta 1 and beta 2 receptors
catecholamine
treats acute asthma and anaphylactic shock
used to treat cardiac arrest, bronchodilation, bronchospasm
used in local anesthetics to increase duration of action
increases heart rate and blood pressure

126
Q

Norepinephrine

A

catecholamine
alpha 1, alpha 2, and beta 1 receptors
used in the treatment of shock
increases heart rate, blood pressure, and vascular resistance

127
Q

Isoproterenol

A

catecholamine
beta 1 and beta 2 receptors
cardiac stimulant
increase cardiac output
peripheral vasodilation, bronchodilation

128
Q

Dobutamine

A

catecholamine
beta 1 receptor
treats acute heart failure

129
Q

Oxymetazoline

A

Noncatecholamine
alpha 1 receptor
nasal decongestant

130
Q

Phenylephrine

A

noncatecholamine
alpha 1 receptor
nasal decongestant
raise blood pressure
treats paroxysmal suprventricular tachycardia

131
Q

Clonidine

A

noncatecholamine
alpha 2 receptor
treatment of hypertension

132
Q

Albuterol

A

noncatecholamine
beta 2 receptor
treatment of short acting bronchospasm

133
Q

Terbutaline

A

noncatecholamine
beta 2 receptor
treatment of short acting bronchospasms

134
Q

Salmeterol

A

noncatecholamines
beta 2 receptor
treatment of long acting bronchospasms

135
Q

Formoterol

A

noncatecholamine
beta 2 receptor
treatment of long acting of bronchospasm

136
Q

Amphetamine

A

noncatecholamines
alpha and beta receptors, CNS
treats kids with ADD and narcolepsy
helps with appetite control

137
Q

Ephedrine

A

Noncatecholamine
alpha and beta receptors, CNS
nasal decongestant
raises blood pressure

138
Q

Pseudoephedrine

A

Noncatecholamine
alpha and beta receptors, CNS
nasal decongestant
raises blood pressure

139
Q

Adverse effects of adrenergic agonists

A

arrhythmias
headache
hyperactivity
insomnia
nausea
tremors

140
Q

Adrenergic antagonists

A

adrenergic blockers
sympatholytics
reversible/irreversibly bind to adrenergic receptor
prevent receptor activation by endogenous catecholamines
primarily used to relieve complications of cardiovascular disease

141
Q

Alpha adrenergic antagonists

A

blockade of alpha adrenergic receptors
inhibit vasoconstriction of blood vessels
decrease peripheral vascular resistance
decrease blood pressure

142
Q

Phenoxybenzamine

A

nonselective alpha adrenergic agonist
non competitive

143
Q

Phentolamine

A

nonselective alpha adrenergic antagonist
competitive

144
Q

Adverse effects of alpha adrenergic antagonists

A

provoke reflex tachycardia
syncope
orthostatic hypotension
tachycardia
dizziness and headache
sexual dysfunction

145
Q

Prazosin

A

alpha adrenergic antagonist
selective alpha 1 blocker
competitive
treats hypertension
adverse reactions: tachycardia, dizziness, headache, sexual dysfunction

146
Q

Terazosin

A

alpha adrenergic antagonist
selective alpha 1 blocker
competitive
treats hypertension
adverse reactions: tachycardia, dizziness, headache, sexual dysfunction

147
Q

Doxazosin

A

alpha adrenergic antagonist
selective alpha 1 blocker
competitive
treats hypertension
adverse reactions: tachycardia, dizziness, headache, sexual dysfunction

148
Q

Alfuzosin

A

alpha adrenergic antagonist
selective alpha 1 blocker
competitive
treats hypertension
adverse reactions: tachycardia, dizziness, headache, sexual dysfunction

149
Q

Tamsulosin

A

alpha adrenergic antagonist
selective alpha 1 blocker
competitive
treats hypertension
adverse reactions: tachycardia, dizziness, headache, sexual dysfunction

150
Q

Yohimbe

A

alpha adrenergic antagonist
selective alpha 2 blocker, competitive
treats erectile dysfunction
increases sympathetic outflow from the CNS to the periphery

151
Q

Blockade of beta adrenergic receptors

A

inhibit NE release
decreased heart rate, heart contractility, cardiac output, renin activity

152
Q

Which receptors do nonselective Beta adrenergic antagonists act on?

A

both beta 1 and beta 2

153
Q

Propranolol

A

adrenergic antagonists
Beta 1 and Beta 2 receptor
used to treat hypertension, migraine, hyperthyroidism, angina pectoris, myocardial infarction

154
Q

Nadolol

A

adrenergic antagonist
Beta 1 and beta 2 receptors
treats hypertension

155
Q

Pindolol

A

adrenergic antagonist
Beta 1 and beta 2 receptors
treats hypertension

156
Q

Timolol

A

beta adrenergic antagonists
beta 1 and beta 2 receptors
used to treat hypertension and glaucoma

157
Q

Atenolol

A

beta adrenergic antagonists
beta 1 receptor
used to treat hypertension, angina, myocardial infarction

158
Q

Bisoprolol

A

beta adrenergic antagonists
beta 1 receptor
used to treat hypertension, angina, myocardial infarction

159
Q

Esmolol

A

beta adrenergic antagonists
beta 1 receptor
used to treat hypertension, angina, myocardial infarction

160
Q

Metoprolol

A

beta adrenergic antagonists
beta 1 receptor
used to treat hypertension, angina, myocardial infarction

161
Q

Acebutolol

A

beta adrenergic antagonists
beta 1 receptor
used to treat hypertension

162
Q

Nebivolol

A

beta adrenergic antagonist
beta 1 receptor, increased nitric oxide
treats hypertension

163
Q

Carvedilol

A

beta adrenergic antagonist
alpha 1, beta 1, and beta 2 receptors
treats hypertension

164
Q

Labetalol

A

beta adrenergic antagonist
alpha 1, beta 1, and beta 2 receptors
treats hypertension

165
Q

Adverse effects of Beta adrenergic antagonists

A

fatigue
bronchoconstriction
sexual dysfunction
arrhythmias

166
Q

How many distinct ion channels do humans express?

A

200

167
Q

Ion channels regulate the passive diffusion of these through cell membranes:

A

sodium, potassium, calcium, and chloride

168
Q

What are the types of ion channels?

A

voltage activated
ligand activated
store activated
stretch activated
temperature activated

169
Q

Where are ion channels that generate action potential?

A

excitable tissues

170
Q

Where are ion channels that trigger cellular biochemical and secretory events?

A

non-excitable tissues

171
Q

Sodium

A

binds to voltage gated ion channels
inhibits peripheral neurotransmission- local anesthetics
involved in transmission of myocardial action potential- class 1 antiarrhythmic drugs

172
Q

Potassium

A

expressed in nerve, cardiac and smooth muscle tissues
regulates resting membrane potential
class 3 antiarrhythmic drugs prolong repolarization of cardiac action potentials

173
Q

Where is calcium widely distributed in?

A

nerves- stimulates release of neurotransmitters
myocardium- class 4 antiarrhythmic drugs, depolarization of pacemaker, modification of shape and duration of myocardial action potential
smooth muscle- calcium channels regulate vascular tone, calcium channel blockers dilate blood vessels

174
Q

Acetylcholine ligand-gated ion channels: somatic neuromuscular transmission

A

agonist- carbachol
antagonist- pancuronium, alpha bungarotoxin

175
Q

Acetylcholine ligand-gated ion channels: sympathetic and parasympathetic autonomic ganglia

A

agonist- nicotine
antagonist- trimetaphan

176
Q

Acetylcholine ligand-gated ion channels: CNS

A

3 subtypes involved in attention, addiction, and cognition
agonist- nicotine
antagonist- bupropion

177
Q

Bicuculline

A

antagonist at GABA binding sites

178
Q

Allosteric agonist modulators of GABA

A

barbiturates
ethanol
benzodiazepines
propofol

179
Q

What are the agonists of glutamate?

A

glutamic acid and glycine

180
Q

What are the antagonists of glutamate?

A

ketamine, Mg^2+, memantine

181
Q

What are the agonists of serotonin ?

A

ethanol
ibogaine

182
Q

What are the antagonists of serotonin?

A

ondansetron, clozapine

183
Q

Glycine receptor

A

involved in sensory and motor function
binds the inhibitory neutrotransmitter glycine; gates chloride channels
in the CNS

184
Q

What are the glycine receptor agonists?

A

glycine and taurine

185
Q

What are the glycine receptor antagonists?

A

picrotoxin
strychnine

186
Q

If the G protein heterotrimer forms a complex with GDP there is no?

A

ligand present

187
Q

What binds to and regulates effectors?

A

GTP bound G alpha subunit and beta gamma dimer

188
Q

GTP is inactivated by

A

hydrolysis

189
Q

Prolonged stimulation of GPCR can lead to

A

downregulation of the receptor

190
Q

G protein receptor kinases

A

phosphorylate the C terminal tail on the receptor and recruit proteins known as arrestins

191
Q

Arrestins

A

binds to the receptor on the internal surface, displace g proteins and inhibit signaling

192
Q

GPCR Gi

A

inhibition of adenyly cyclase and decrease in cAMP

193
Q

Adenosine, melatonin, opioids, and acetylcholine all bind to which type of GPCR receptor?

A

Gi

194
Q

GPCR Gq

A

second messengers
IP3- binds to and releases Calcium ions from the endoplasmic/ sarcoplasmic reticulum
DAG- activates kinase PKC
Ca^2+ -binds to and activates intracellular proteins and enzymes
PKC- phosphorylates and activates/deactivates intracellular enzymes
pharmacological response to receptor activation by the agonist

195
Q

Agonists that activate Gq GPCRs

A

NE- alpha 1- vascular smooth muscle contraction
Thromboxane A2 - platelet aggregation
ACh- M3- smooth muscle contraction and glandular secretion

Pharmacology (16 decks)

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