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Pharmacology > Pharmacology - Block 1 > Flashcards

Pharmacology - Block 1 Flashcards

1
Q

Competitive antagonists - EC50 and Emax

A

Shift EC50 right, Emax no change

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2
Q

Irreversible or non-competitive antagonists - EC50 and Emax

A

EC50 no change, Emax lower

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3
Q

Acidic drugs ion trap on the ___

A

Basic side

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4
Q

pKa - pH =

A

pKa-pH = log(protonated/unprotonated)

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5
Q

Active transport enzyme pumps drugs back out

A

P-glycoprotein (MDR-1, ABC group)

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6
Q

Acidic drugs circulate with

A

Albumin (liver disease-> need lower dose)

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7
Q

Basic drugs circulate with

A

alpha1-glycoprotein (Crohn’s disease-> need larger dose)

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8
Q

Brain efflux transporters

A

P-glycoprotein and OATP

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9
Q

Fetal plasma and breast milk are more acid/base

A

acidic

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10
Q

Dose, concentration, vol of dist, bioavailability eqn

A

Dose = Vd*Co/F

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11
Q

T1/2 =

A 
T1/2 = .69/Kel
T1/2 = .69*Vd/CL
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12
Q

Slope of logC vs Time

A

slope = -Kel/2.3

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13
Q

CL =

A

CL = Vd*Kel

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14
Q

Maintence Dose / Interval =

A

Maintence Dose / Interval = Css*CL/F

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15
Q

Phase I enzymes located in

A

smooth ER

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16
Q

Phase II enzymes located in

A

cytosol

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17
Q

Cytochrome P450s in descending percentage of drugs metabolized

A

CYP3A (50%)
CYP2D6 (25%)
CYP2C9 (15%)
1A2, 2E1, 2C19

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18
Q

Most ubiquitous protein in liver

A

FMO3

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19
Q

Phase I enzymes need

A

NADPH

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20
Q

List Phase II enzymes

A

UGT (Glucuronidation)
SULT (Sulfation)
NAT (Acetylation)
Glutithione S-transferases

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21
Q

Ethanol induces

A

CYP2E1

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22
Q

Grapefruit juice inhibits

A

CYP3A

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23
Q

Can be inhibited near 0

A

CYP2D6

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24
Q

Not induced or inhibited

A

FMOs

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25
Q

When induced leads to APAP toxicity

A

2E1

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26
Q

NAT-2 (metabolizes, effect of dysfunction)

A

isoniazid (TB drug)

increased neuropathy

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27
Q

CYP2D6 (metabolizes, effect of dysfunction)

A

antidepressants
codeine->morphine
also, gene duplication-> ultra-fast

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28
Q

CYP2C19 (metabolizes, effect of dysfunction)

A

phenytoin (anti-convulsant)
omeprazole (PPI)
clopidogrel (activated by 2C19, anti-platelet)

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29
Q

CYP2C9 (metabolizes, effect of dysfunction)

A

Warfarin (anti-coagulant)

*3 has bigger impact than *2

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30
Q

Vit K Receptor (VKORC1) (drug, effect, clades)

A

Warfarin inhibits VKORC1,

A-clade=lower dose, B-clade=higher dose

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31
Q

Pseudocholinesterase (metabolizes, effect of dysfunction)

A

succinylcholine (muscle relaxant)

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32
Q

TPMT (metabolizes, effect of dysfunction)

A

6-mercaptopurine (6MP) (cancer drug)

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33
Q

P-glycoprotein (drug, effect)

A

digoxin (cardiac glycoside) (dysfunction increases net uptake)

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34
Q

Example of Intracellular steroid receptors

A

cortisol (travels with CBG) -> diffuses to cytosol, binds to glucocorticoid receptor (GR) -> conformational change releases inhibitory proteins -> binds to GRE on DNA promoter

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35
Q

GABA receptor agonist drugs

A

Benzodiazepines (valium)

Barbiturates (Phenobarbital)

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36
Q

Inositol-lipid pathway

A

GPCR->Gaq-GTP activates PLC -> PLC cleaves PIP2 to IP3 + DAG -> IP3 releases Ca from ER, DAG activates PKC

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37
Q

cAMP pathway

A

GPCR->Gas->adenylyl cyclase->cAMP->PKA->CREB->gene transcription

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38
Q

Monomeric G proteins are activated by / turned off by

A

ON: GEF
OFF: GAP
receptor linked tyrosine kinases

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39
Q

MAPKKK cascade

A

RAS-GTP->Raf->MKK1->ERK->phosphorylates transcription factors

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40
Q

Tyrosine kinase inhibitors (EGF receptor)

A

gefitinib

erlotinib

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41
Q

dopamine transported into storage vesicles by

A

VMAT2, vesicular monoamine transporter 2

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42
Q

Metabolic degradation of NE by

A 
Monoamine Oxidase (MAO)
catechol-O-methyltransferase (COMT)
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43
Q

Acetylcholine release inhibited by

A

botulinum toxin

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44
Q

alpha1 receptor

A

Gq - activate PLC
eye (iris), vascular, smooth muscle, vas deferens
contraction and ejaculation

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45
Q

alpha2 receptor

A

Gi - inhibit AC (cAMP), activate PLC in vascular SM
pre-synaptic nerve terminals, CNS
decrease NE release, decrease sympathetic outflow

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46
Q

beta1 receptor

A

Gs - activate AC (cAMP)
cardiac muscle, kidney
increase force, rate, renin release

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47
Q

beta2 receptor

A

Gs - activate AC (cAMP)
arteries, skeletal muscle, liver, bronchi
dilation, glycogenolysis

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48
Q

beta3 receptor

A

Gs - activate AC (cAMP)
adipose tissue
lipolysis

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49
Q

Norepinephrine uptake (by NET) blocked by

A

cocaine

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50
Q

Dopamine1 receptor

A

Kidney - dilation of kidney vasculature

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51
Q

Norepinephrine

A

Adrenergic agonist - direct
Catecholamine
a1, a2, b1
mainly a1 -> cardio effects -> peripheral vasoconstriction, up BP, can cause reflex bradycardia

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52
Q

Epinephrine

A

Adrenergic agonist - direct
Catecholamine
a1, a2, b1, b2
mainly B2 -> cardio effects -> up HR, up CO, increase systolic, decrease diastolic BP, constrict most vasculature but dilate skeletal muscle vasculature, decrease peripheral resistance
Bronchodilation
Hyperglycemia and lipolysis
rapid hypersensitivity relief, co-admin w/ local anesthetic, ophthalmic uses, bradyarrhythmias

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53
Q

Isoproterenol

A 
Adrenergic agonist - direct
Catecholamine
b1, b2
CV -> down peripheral resistance, up HR, up CO, down BP
bronchodilation
use in emergency to up HR
54
Q

Dopamine

A

Adrenergic agonist - direct
Catecholamine
a1, b1, DA1
CV_> low dose, dilation of renal and mesenteric arteries
med dose = up HR, CO
high dose = vasoconstriction and up peripheral resistance
use in heart failure, shock

55
Q

Dobutamine

A 
Adrenergic agonist - direct
Catecholamine
b1
CV-> up HR, CO, no change in PR
use in cardiac decomp, and stress testing
56
Q

Methyldopa

A 
Adrenergic agonist - direct
Catecholamine
a2
orally bioavailable, prodrug
CNS-> decrease sympathetic outflow
down PR, HR, CO
use as anti-hypertensive in pregnant women, eclampsia
side effect = rebound hypertension, sedation, dry mouth, edema
57
Q

Phenylephrine

A 
Adrenergic agonist - direct
a1
up BP, down HR, down blood flow
use as nasal decongestant
also aphthalmic, w/ local anesthetics, and hypotension
58
Q

Clonidine

A

Adrenergic agonist - direct
a2
orally active
CNS -> reduce sympathetic outflow -> down PR, HR, CO
use as anti-hypertensive
side effects = edema, sedation, dry mouth, rebound hypertension

59
Q

Albuterol

A

Adrenergic agonist - direct
b2
short acting bronchodilator (asthma)
side effect = tremor, tachycardia, anxiety

60
Q

Salmeterol

A

Adrenergic agonist - direct
b2
long acting bronchodilator
use in COPD, asthma

61
Q

Tyramine

A

Adrenergic agonist - INdirect (release NE)
found in some foods
metabolized by MAO

62
Q

Amphetamine

A 
Adrenergic agonist - Mixed acting
CNS stimulant and weakly peripheral a and b
orally available
also weakly blocks NET
depresses appetite, narcolepsy, ADD
63
Q

Ephedrine

A

Adrenergic agonist - Mixed acting
CNS releases NE and direct a and b agonist
orally effective
used to be in herbals, now FDA banned

64
Q

Pseudoephedrine

A

Adrenergic agonist - Mixed acting
direct a1, with little b2 + release NE
orally available, but less CNS
use nasal decongestant (a1 effect)

65
Q

Guanethidine

Guanadrel

A 
Adrenergic neuron blockers
inhibit NE release
Guanethidine does not enter CNS
long acting anti-essential hypertensive
limited use b/c side effects -> orthostatic hypotension, sex function, edema, diarrhea
66
Q

Reserpine

A

Adrenergic neuron blocker
Inhibits VMAT2
long-acting, orally active, use as anti-hypertensive, rarely used
has CNS side-effects, depression, suicide
also orthostatic hypotension, diarrhea

67
Q

Phenoxybenzamine

A 
Adrenergic receptor blocker
a1, a2
irreversible antagonist
orally active, long duration
vasodilation
use in pheochromocytoma
68
Q

Phentolamine

A 
Adrenergic receptor blocker
a1, a2
competitive antagonist
orally active, shorter duration
vasodilation
use in HTN, pheochromocytoma
69
Q

Prazosin

A

Adrenergic receptor blocker
a1
orally active, competitive (prototypical)
minimal tachycardia
decrease vascular tone
produces favorable lipid profile
use in hypertension, heart failure, and BPH (prostate)

70
Q

Tamsulosin

A

Adrenergic receptor blocker
a1, a1A > a1B
effective for BPH (prostate), less side effects

71
Q

Propranolol

A

Adrenergic receptor blocker
B1, B2
competitive
use in hypertension, angina, myocardial infarction, pheochromocytoma, migraine
side effects= bradycardia, up airway resistance, mask hypoglycemia, sedation

72
Q

Timolol

A 
Adrenergic receptor blocker
B1, B2
competitive
similar to propranolol
also used for glaucoma to decrease intraocular pressure
73
Q

Metoprolol

A

Adrenergic receptor blocker
B1 (prototypical)
competitive, more B1 selective at low doses
similar to propranolol, also used for heart failure
less bronchoconstriction than propranolol

74
Q

Atenolol

A 
Adrenergic receptor blocker
B1 
similar to Metoprolol
once a day, orally
does not enter CNS
75
Q

Labetalol

A

Adrenergic receptor blocker
a1, b1, b2
use in essential hypertension and hypertensive emergencies

76
Q

Carvedilol

A

Adrenergic receptor blocker
a1, b1, b2
also has anti-oxidant and anti-inflammatory effects
use in chronic heart failure, hypertension, acute MI

77
Q

Muscarinic receptor functions

A

Eye - contract ciliary muscle (lens), contract iris (miosis)
Heart - decrease rate
Lung - contrict bronchi, promote secretion
Bladder / GI - promote voiding/secretion/motility
Sweat glands - sweating
-Blood vessels - vasodilation (via NO)

78
Q

Nicotinic receptor functions

A 
Nm = skeletal muscle depolarization
Nn = autonomic ganglia, adrenals
CNS = control of NT release
79
Q

Bethanechol

A

Muscarinic agonist - direct
choline ester
primarily on GI/GU tract, peripherally restricted
used orally for urinary retention

80
Q

Pilocarpine

A

Muscarinic agonist - direct
CNS available
used orally to treat xerostomia (dry mouth)
miotic agent for glaucoma

81
Q

Edrophonium

A

AChE inhibitor - reversible (non-subtrate)
rapid onset and short duration
IV (not oral)
use in diagnosis of myasthenia gravis
reversal of paralysis by neuromuscular blocking drugs

82
Q

Physostigmine

A

AChE inhibitor - reversible (substrate)
slowly reversible (hours)
CNS available
used for glaucoma and to reverse toxicity of antimuscarinic drugs

83
Q

Neostigmine

A 
AChE inhibitor - reversible (substrate)
slowly reversible (hours)
NOT CNS available
used for treatment of myasthenia gravis (oral)
prevention of post-op gut atony
reversal of paralysis by NMJ blockers
84
Q

Sarin

A

Nerve gas
irreversible AChE inhibitor
SLUDGE, hypotension, bradycardia, visual blurryness,
medullary respiratory center depression, muscle paralysis
Antidotes: atropine, pralidoxime

85
Q

Malathion

A

Insecticide (rapidly detoxed in animals)
irreversible AChE inhibitor
SLUDGE, hypotension, bradycardia, visual blurryness,
medullary respiratory center depression, muscle paralysis
Antidotes: atropine, pralidoxime

86
Q

Atropine

A

Muscarinic receptor antagonist
used to treat bradycardia
opthalmic use for mydriasis (dilation) and cylcoplegia (paralyze accomodation)
long duration
use in anesthesia to block vagal response
and treat anti-AChE toxicity

87
Q

Scopolamine

A

Similar to Atropine (Muscarinic antagonist)
greater CNS penetration
used to treat motion sickness and vestibular disease
transdermal patch

88
Q

Ipratropium

A

Muscarinic antagonist
used to treat COPD (inhalation)
NO CNS penetration
reduce bronchial constriction

89
Q

Tropicamide

A

Muscarinic antagonist
used as opthalmic to mydriasis and cycloplegia
fast onset and short duration

90
Q

Oxybutynin

A

Muscarinic antagonist
used to treat overactive bladder and incontinence
lots of anti-muscarinic side effects (xerostomia)

91
Q

Darifenacin

A

Similar to Oxybutynin (Muscarinic antagonist)
M3 selective
less CNS effects

92
Q

Glycopyrrolate

A

Muscarinic antagonist
used to block parasympatheticomimetic effects during reversal of NM blockade with anti-AChE agents
NO CNS effects

93
Q

Muscarinic antagonist side-effects

A

Hot, dry, red, blurry, drowsy
high []-> ataxia, excitement, delerium
can use physotigmine for toxicity reversal

94
Q

AChE inhibitor side effects

A

SLUDGE, hypotension, bradycardia, blurred vision

SLUDGE = salivation, lacrimation, urination, defecation, GI upset, emesis

95
Q

Rocuronium

A 
Neuromuscular blocker (non-depolarizing, competitive)
intermediate duration, rapid onset
used for intubation
metabolized by liver
96
Q

Atracurium

A

Neuromuscular blocker (non-depolarizing, competitive)
intermediate duration
spontaneously degrades
minimal CV effect, slight histamine release

97
Q

Vecuronium

A

Neuromuscular blocker (non-depolarizing, competitive)
intermediate duration
liver metabolism
no CV or histamine effects

98
Q

Pancuronium

A

Neuromuscular blocker (non-depolarizing, competitive)
long duration
renal excretion
slight up BP, slight histamine release

99
Q

Succinylcholine

A 
Neuromuscular blocker (deploarizing)
NAChR agonist
NO CNS action
ultra short duration, rapid onset
used for intubation
can be problem if liver problem
side-effects = prolonged apnea, malignant hyperthermia (genetic), muscle pain, hyperkalemia
100
Q

Non-depolarizing neuromuscular blocker side-effects

A

Prolonged apnea, cardiovascular collapse (from histamine)
toxicity can be reversed with neostigmine or edrophonium (co administer glycopyrrolate to reduce non-CNS muscarinic actions)

101
Q

To dilate pupils

A

muscarinic antagonists
a1 agonists
epinephrine, phenylephrine, atropine, tropicamide

102
Q

Treat glaucoma

A

muscarinic agonist
B antagonist
AChE inhibitors
timolol, pilocarpine, physostigmine

103
Q

Restrict local drug washout

A

a1 agonist

epinephrine, phenylephrine

104
Q

Treat nasal congestion

A

a1 agonist

phenylephrine, pseudoephedrine

105
Q

Treat BPH (Prostate)

A

a1 antagonist

prazosin, tamsulosin

106
Q

Treat bradycardia

A

muscarinic antagonist
B1 agonist
epinephrine, isproterenol, dobutamine, atropine

107
Q

Treat tachycardia

A

muscarinic agonist

B1 antagonist

108
Q

Treat shock, anaphylaxis

A

catecholamine agonist

109
Q

Treat hypertension

A

B antagonists

isoproterenol, methyldopa, clonidine, phentolamine, prazosin, propranolol, timolol, metoprolol, atenolol, carvedilol

110
Q

Cardiac stress test

A

B1 agonist

dobutamine

111
Q

Treat Pheochromocytoma

A

a agonist

phenoxybenzamine, phentolamine, propranolol, timolol

112
Q

Treat asthma

A

B2 agonist
muscarinic antagonist
epinephrine, albuterol, salmeterol, ipratropium

113
Q

Treat GI hypermotility

A

muscarinic antagonist

oxybutynin, darifenacin

114
Q

Treat urinary retention

A

muscarinic agonist
AChE inhibitor
bethanechol, neostigmine

115
Q

a1 drugs

A

phenylephrine

blockers: prazosin, tamsulosin

116
Q

a2 drugs

A

clonidine, methyldopa

117
Q

a1,2 drugs

A

blockers: phenoxybenzamine, phentolamine

118
Q

b1 drugs

A

dobutamine

blockers: metoprolol, atenolol

119
Q

b2 drugs

A

albuterol, salmeterol

120
Q

b1,2 drugs

A

isoproterenol

blockers: propranolol, timolol

121
Q

a,b drugs

A

norepinephrine, epinephrine

122
Q

a1,b1,b2 drugs

A

blockers: labetalol, carvedilol

123
Q

DA1,a1,a2 drugs

A

dopamine

124
Q

NE drugs

A

tyramine

blockers: guanethidine, guanadrel, reserpine

125
Q

NE+a,b drugs

A

amphetamine, ephedrine, pseudoephedrine

126
Q

M drugs

A

bethanechol, pilocarpine

blockers: atropine, scopolamine, ipratropium, tropicamide, oxybutynin, glycopyrrolate

127
Q

M3 drugs

A

blockers: darifenacin

128
Q

AChE drugs

A

blockers: edrophonium, physostigmine, neostigmine, sarin, malathion

129
Q

nAChR drugs

A

blockers: rocuronium, atracurium, vecuronium, pancuronium, succylcholine

130
Q

[LR]/RT =

A

[LR]/RT = [L] / (Kd + [L])

Pharmacology (8 decks)

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