Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

Pharmacology > Pharmacology - Block 1 > Flashcards

Pharmacology - Block 1 Flashcards

(130 cards)

Start Studying
1
Q

Competitive antagonists - EC50 and Emax

A

Shift EC50 right, Emax no change

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Irreversible or non-competitive antagonists - EC50 and Emax

A

EC50 no change, Emax lower

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Acidic drugs ion trap on the ___

A

Basic side

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

pKa - pH =

A

pKa-pH = log(protonated/unprotonated)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Active transport enzyme pumps drugs back out

A

P-glycoprotein (MDR-1, ABC group)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Acidic drugs circulate with

A

Albumin (liver disease-> need lower dose)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Basic drugs circulate with

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Brain efflux transporters

A

P-glycoprotein and OATP

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Fetal plasma and breast milk are more acid/base

A

acidic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Dose, concentration, vol of dist, bioavailability eqn

A

Dose = Vd*Co/F

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

T1/2 =

A 
T1/2 = .69/Kel
T1/2 = .69*Vd/CL
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Slope of logC vs Time

A

slope = -Kel/2.3

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

CL =

A

CL = Vd*Kel

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Maintence Dose / Interval =

A

Maintence Dose / Interval = Css*CL/F

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Phase I enzymes located in

A

smooth ER

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Phase II enzymes located in

A

cytosol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Cytochrome P450s in descending percentage of drugs metabolized

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Most ubiquitous protein in liver

A

FMO3

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Phase I enzymes need

A

NADPH

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

List Phase II enzymes

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Ethanol induces

A

CYP2E1

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Grapefruit juice inhibits

A

CYP3A

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Can be inhibited near 0

A

CYP2D6

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Not induced or inhibited

A

FMOs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
When induced leads to APAP toxicity
2E1
26
NAT-2 (metabolizes, effect of dysfunction)
isoniazid (TB drug) | increased neuropathy
27
CYP2D6 (metabolizes, effect of dysfunction)
antidepressants codeine->morphine also, gene duplication-> ultra-fast
28
CYP2C19 (metabolizes, effect of dysfunction)
phenytoin (anti-convulsant) omeprazole (PPI) clopidogrel (activated by 2C19, anti-platelet)
29
CYP2C9 (metabolizes, effect of dysfunction)
Warfarin (anti-coagulant) | *3 has bigger impact than *2
30
Vit K Receptor (VKORC1) (drug, effect, clades)
Warfarin inhibits VKORC1, | A-clade=lower dose, B-clade=higher dose
31
Pseudocholinesterase (metabolizes, effect of dysfunction)
succinylcholine (muscle relaxant)
32
TPMT (metabolizes, effect of dysfunction)
6-mercaptopurine (6MP) (cancer drug)
33
P-glycoprotein (drug, effect)
digoxin (cardiac glycoside) (dysfunction increases net uptake)
34
Example of Intracellular steroid receptors
cortisol (travels with CBG) -> diffuses to cytosol, binds to glucocorticoid receptor (GR) -> conformational change releases inhibitory proteins -> binds to GRE on DNA promoter
35
GABA receptor agonist drugs
Benzodiazepines (valium) | Barbiturates (Phenobarbital)
36
Inositol-lipid pathway
GPCR->Gaq-GTP activates PLC -> PLC cleaves PIP2 to IP3 + DAG -> IP3 releases Ca from ER, DAG activates PKC
37
cAMP pathway
GPCR->Gas->adenylyl cyclase->cAMP->PKA->CREB->gene transcription
38
Monomeric G proteins are activated by / turned off by
ON: GEF OFF: GAP receptor linked tyrosine kinases
39
MAPKKK cascade
RAS-GTP->Raf->MKK1->ERK->phosphorylates transcription factors
40
Tyrosine kinase inhibitors (EGF receptor)
gefitinib | erlotinib
41
dopamine transported into storage vesicles by
VMAT2, vesicular monoamine transporter 2
42
Metabolic degradation of NE by
``` Monoamine Oxidase (MAO) catechol-O-methyltransferase (COMT) ```
43
Acetylcholine release inhibited by
botulinum toxin
44
alpha1 receptor
Gq - activate PLC eye (iris), vascular, smooth muscle, vas deferens contraction and ejaculation
45
alpha2 receptor
Gi - inhibit AC (cAMP), activate PLC in vascular SM pre-synaptic nerve terminals, CNS decrease NE release, decrease sympathetic outflow
46
beta1 receptor
Gs - activate AC (cAMP) cardiac muscle, kidney increase force, rate, renin release
47
beta2 receptor
Gs - activate AC (cAMP) arteries, skeletal muscle, liver, bronchi dilation, glycogenolysis
48
beta3 receptor
Gs - activate AC (cAMP) adipose tissue lipolysis
49
Norepinephrine uptake (by NET) blocked by
cocaine
50
Dopamine1 receptor
Kidney - dilation of kidney vasculature
51
Norepinephrine
Adrenergic agonist - direct Catecholamine a1, a2, b1 mainly a1 -> cardio effects -> peripheral vasoconstriction, up BP, can cause reflex bradycardia
52
Epinephrine
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
53
Isoproterenol
``` Adrenergic agonist - direct Catecholamine b1, b2 CV -> down peripheral resistance, up HR, up CO, down BP bronchodilation use in emergency to up HR ```
54
Dopamine
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
Dobutamine
``` Adrenergic agonist - direct Catecholamine b1 CV-> up HR, CO, no change in PR use in cardiac decomp, and stress testing ```
56
Methyldopa
``` 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
Phenylephrine
``` Adrenergic agonist - direct a1 up BP, down HR, down blood flow use as nasal decongestant also aphthalmic, w/ local anesthetics, and hypotension ```
58
Clonidine
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
Albuterol
Adrenergic agonist - direct b2 short acting bronchodilator (asthma) side effect = tremor, tachycardia, anxiety
60
Salmeterol
Adrenergic agonist - direct b2 long acting bronchodilator use in COPD, asthma
61
Tyramine
Adrenergic agonist - INdirect (release NE) found in some foods metabolized by MAO
62
Amphetamine
``` Adrenergic agonist - Mixed acting CNS stimulant and weakly peripheral a and b orally available also weakly blocks NET depresses appetite, narcolepsy, ADD ```
63
Ephedrine
Adrenergic agonist - Mixed acting CNS releases NE and direct a and b agonist orally effective used to be in herbals, now FDA banned
64
Pseudoephedrine
Adrenergic agonist - Mixed acting direct a1, with little b2 + release NE orally available, but less CNS use nasal decongestant (a1 effect)
65
Guanethidine | Guanadrel
``` 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
Reserpine
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
Phenoxybenzamine
``` Adrenergic receptor blocker a1, a2 irreversible antagonist orally active, long duration vasodilation use in pheochromocytoma ```
68
Phentolamine
``` Adrenergic receptor blocker a1, a2 competitive antagonist orally active, shorter duration vasodilation use in HTN, pheochromocytoma ```
69
Prazosin
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
Tamsulosin
Adrenergic receptor blocker a1, a1A > a1B effective for BPH (prostate), less side effects
71
Propranolol
Adrenergic receptor blocker B1, B2 competitive use in hypertension, angina, myocardial infarction, pheochromocytoma, migraine side effects= bradycardia, up airway resistance, mask hypoglycemia, sedation
72
Timolol
``` Adrenergic receptor blocker B1, B2 competitive similar to propranolol also used for glaucoma to decrease intraocular pressure ```
73
Metoprolol
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
Atenolol
``` Adrenergic receptor blocker B1 similar to Metoprolol once a day, orally does not enter CNS ```
75
Labetalol
Adrenergic receptor blocker a1, b1, b2 use in essential hypertension and hypertensive emergencies
76
Carvedilol
Adrenergic receptor blocker a1, b1, b2 also has anti-oxidant and anti-inflammatory effects use in chronic heart failure, hypertension, acute MI
77
Muscarinic receptor functions
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
Nicotinic receptor functions
``` Nm = skeletal muscle depolarization Nn = autonomic ganglia, adrenals CNS = control of NT release ```
79
Bethanechol
Muscarinic agonist - direct choline ester primarily on GI/GU tract, peripherally restricted used orally for urinary retention
80
Pilocarpine
Muscarinic agonist - direct CNS available used orally to treat xerostomia (dry mouth) miotic agent for glaucoma
81
Edrophonium
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
Physostigmine
AChE inhibitor - reversible (substrate) slowly reversible (hours) CNS available used for glaucoma and to reverse toxicity of antimuscarinic drugs
83
Neostigmine
``` 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
Sarin
Nerve gas irreversible AChE inhibitor SLUDGE, hypotension, bradycardia, visual blurryness, medullary respiratory center depression, muscle paralysis Antidotes: atropine, pralidoxime
85
Malathion
Insecticide (rapidly detoxed in animals) irreversible AChE inhibitor SLUDGE, hypotension, bradycardia, visual blurryness, medullary respiratory center depression, muscle paralysis Antidotes: atropine, pralidoxime
86
Atropine
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
Scopolamine
Similar to Atropine (Muscarinic antagonist) greater CNS penetration used to treat motion sickness and vestibular disease transdermal patch
88
Ipratropium
Muscarinic antagonist used to treat COPD (inhalation) NO CNS penetration reduce bronchial constriction
89
Tropicamide
Muscarinic antagonist used as opthalmic to mydriasis and cycloplegia fast onset and short duration
90
Oxybutynin
Muscarinic antagonist used to treat overactive bladder and incontinence lots of anti-muscarinic side effects (xerostomia)
91
Darifenacin
Similar to Oxybutynin (Muscarinic antagonist) M3 selective less CNS effects
92
Glycopyrrolate
Muscarinic antagonist used to block parasympatheticomimetic effects during reversal of NM blockade with anti-AChE agents NO CNS effects
93
Muscarinic antagonist side-effects
Hot, dry, red, blurry, drowsy high []-> ataxia, excitement, delerium can use physotigmine for toxicity reversal
94
AChE inhibitor side effects
SLUDGE, hypotension, bradycardia, blurred vision | SLUDGE = salivation, lacrimation, urination, defecation, GI upset, emesis
95
Rocuronium
``` Neuromuscular blocker (non-depolarizing, competitive) intermediate duration, rapid onset used for intubation metabolized by liver ```
96
Atracurium
Neuromuscular blocker (non-depolarizing, competitive) intermediate duration spontaneously degrades minimal CV effect, slight histamine release
97
Vecuronium
Neuromuscular blocker (non-depolarizing, competitive) intermediate duration liver metabolism no CV or histamine effects
98
Pancuronium
Neuromuscular blocker (non-depolarizing, competitive) long duration renal excretion slight up BP, slight histamine release
99
Succinylcholine
``` 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
Non-depolarizing neuromuscular blocker side-effects
Prolonged apnea, cardiovascular collapse (from histamine) toxicity can be reversed with neostigmine or edrophonium (co administer glycopyrrolate to reduce non-CNS muscarinic actions)
101
To dilate pupils
muscarinic antagonists a1 agonists epinephrine, phenylephrine, atropine, tropicamide
102
Treat glaucoma
muscarinic agonist B antagonist AChE inhibitors timolol, pilocarpine, physostigmine
103
Restrict local drug washout
a1 agonist | epinephrine, phenylephrine
104
Treat nasal congestion
a1 agonist | phenylephrine, pseudoephedrine
105
Treat BPH (Prostate)
a1 antagonist | prazosin, tamsulosin
106
Treat bradycardia
muscarinic antagonist B1 agonist epinephrine, isproterenol, dobutamine, atropine
107
Treat tachycardia
muscarinic agonist | B1 antagonist
108
Treat shock, anaphylaxis
catecholamine agonist
109
Treat hypertension
B antagonists | isoproterenol, methyldopa, clonidine, phentolamine, prazosin, propranolol, timolol, metoprolol, atenolol, carvedilol
110
Cardiac stress test
B1 agonist | dobutamine
111
Treat Pheochromocytoma
a agonist | phenoxybenzamine, phentolamine, propranolol, timolol
112
Treat asthma
B2 agonist muscarinic antagonist epinephrine, albuterol, salmeterol, ipratropium
113
Treat GI hypermotility
muscarinic antagonist | oxybutynin, darifenacin
114
Treat urinary retention
muscarinic agonist AChE inhibitor bethanechol, neostigmine
115
a1 drugs
phenylephrine | blockers: prazosin, tamsulosin
116
a2 drugs
clonidine, methyldopa
117
a1,2 drugs
blockers: phenoxybenzamine, phentolamine
118
b1 drugs
dobutamine | blockers: metoprolol, atenolol
119
b2 drugs
albuterol, salmeterol
120
b1,2 drugs
isoproterenol | blockers: propranolol, timolol
121
a,b drugs
norepinephrine, epinephrine
122
a1,b1,b2 drugs
blockers: labetalol, carvedilol
123
DA1,a1,a2 drugs
dopamine
124
NE drugs
tyramine | blockers: guanethidine, guanadrel, reserpine
125
NE+a,b drugs
amphetamine, ephedrine, pseudoephedrine
126
M drugs
bethanechol, pilocarpine | blockers: atropine, scopolamine, ipratropium, tropicamide, oxybutynin, glycopyrrolate
127
M3 drugs
blockers: darifenacin
128
AChE drugs
blockers: edrophonium, physostigmine, neostigmine, sarin, malathion
129
nAChR drugs
blockers: rocuronium, atracurium, vecuronium, pancuronium, succylcholine
130
[LR]/RT =
[LR]/RT = [L] / (Kd + [L])

Pharmacology (8 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions