pharm part1 Flashcards

1
Q

what is the pKa

A

pH at which the ionized and unionized concentrations are equal

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2
Q

if pH < pKa, what is favored: the protonated or the unprotonated form

A

protonated

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3
Q

if pH > pKa, what is favored: the protonated or the unprotonated form

A

unprotonated

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4
Q

what is the therapeutic index formula

A

TD50/ED50

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5
Q

bond strength is directly proportional to specificity. true/false?

A

false. it is indirectly proportional

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6
Q

flux is directly proportional to specificity. true/false?

A

true

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7
Q

Kd is directly proportional to drug binding
affinity. true/false?

A

false. it is indirectly proportional

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8
Q

drug safety is directly proportional to drug therapeutic index. true/false?

A

true

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9
Q

Volume of Distribution (Vd) is directly
proportional to the concentration of drug
outside of the systemic circulation. true/false?

A

true

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10
Q

what is the definition of volume of distribution

A

apparent volume of a drug

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11
Q

what is clearance

A

predicts rate of elimination in relation to drug concentration

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12
Q

in first order elimination, which value is constant

A

clearance

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13
Q

in zero order elimination, which value is constant

A

rate of elimination

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14
Q

what 3 meds use zero order elimination

A

ethanol
phenytoin
aspirin

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15
Q

what 4 parameters affect passive diffusion

A

molecular weight
pKa
lipid solubility
plasma protein binding

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16
Q

4 basic mechanisms for transmembrane signaling

A

lipid soluble diffusion to intracellular receptor
ligand binding to RTK
ligand gated ion channel
GPCR

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17
Q

how many trans-membrane alpha helixes does a GPCR have

A

7

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18
Q

what are the 3 major drug efflux transporters in the ABC family

A

B, C, G

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19
Q

what is the major site of exclusion in the blood-brain barrier

A

vascular epithelium

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20
Q

what enzyme is majorly implicated in phase 1 of metabolism

A

cytochrome P450

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21
Q

if a drug X enhances synthesis of CYP450, and the enzyme deactivates another drug Z, what happens to the effect of drug Z

A

decreased drug effect

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22
Q

if a drug X enhances synthesis of CYP450, and the enzyme activates another drug Z, what happens to the effect of drug Z

A

increased drug effect

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23
Q

what is pharmacokinetics

A

the effects of the body on a drug

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24
Q

what is pharmacodynamics

A

the effects of the drug on the body

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25
Q

what is pharmacogenomics

A

the primary reason patients respond differently to the same drug

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26
Q

what is pharmacology

A

the study of the effects of drugs on the body

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27
Q

what are the 6 neurotransmitter classes

A

esters - acetylcholine
monoamines - norepinephrine
amino acids- glutamate
purines - adenosine
peptides - substance P
inorganic gases - nitric oxide

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28
Q

where is the location of the ganglia of the sympathetic ANS

A

close to the spinal cord

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29
Q

where is the location of the ganglia of the parasympathetic ANS

A

in the visceral effector organs

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30
Q

what enzymes does alpha-1 receptor activate

A

phospholipase C

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31
Q

what enzymes does beta-1 receptor activate

A

adenylyl cyclase

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32
Q

what enzymes does beta-2 receptor activate

A

adenylyl cyclase

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33
Q

the gut has its own nervous system called the

A

enteric nervous system

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34
Q

alpha1 receptor activation leads to smooth muscle contraction. what are the second messengers produced by agonist binding to alpha-1 receptors

A

DAG
IP3

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35
Q

give an example of indirect acting adrenergic agonist

A

amphetamine

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36
Q

give 2 examples of adrenergic antagonist drugs

A

phentolamine
prazosin
labetalol

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37
Q

what is the important thing to note about phenoxybenzamine (adrenoceptor antagonist drug)

A

forms irreversible covalent bonds

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38
Q

what effect does beta agonists have on the blood vessels

A

opposes beta2-mediated vasodilation

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39
Q

which beta blocker is ultra short acting

A

esmolol

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40
Q

which betablocker is safer in COPD and diabetic patients

A

metoprolol
atenolol

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41
Q

what is the effect of cholinomimetics on the eye

A

miosis
increase intraocular drainage

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42
Q

what is the effect of cholinomimetics on the CV

A

vasodilation
reduction in PVR
bradycardia if given in large doses

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43
Q

what indirect acting cholinomimetic is a simple alcohol

A

edrophonium

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44
Q

give 2 major uses of indirect acting cholinomimetics

A

eye disease
GI/Urinary tract
NMJ
atropine overdose

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45
Q

what are the s/s of organophosphate exposure

A

SLUDGE-M

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46
Q

what are the s/s of poisonous mushroom exposure

A

SLUDGE-M

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47
Q

what are the s/s of atropine overdose

A

BRAND
blind, red, absent bowel sounds, nuts, dry

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48
Q

what medication are given for organophosphate exposure

A

atropine, pralidozime

49
Q

what medication is given for poisonous mushroom exposure

A

atropine

50
Q

what medication is given for atropine overdose

A

physostigmine

51
Q

what is the difference between unstable and variant angina

A

unstable is caused by plaque while variant angina is caused by hyperreactive vessels

52
Q

what is the action of nitrates on vascular smooth muscle

A

activate guanyly cyclase and increase cGMP, causing relaxation

53
Q

what is the action of beta-2 agonists on vascular smooth muscle

A

act on GPCR to increase cAMP, causing relaxation

54
Q

what is the action of sildenafil on vascular smooth muscle

A

blocks PDE-5, increase cGMP, causing relaxation

55
Q

what are the 3 bad effects of nitrates

A

orthostatic hypotension
syncope
headache
reflex tachy

56
Q

what are the 3 good effects of nitrates

A

reduced preload
reduced heart size
reduced CO
increased venous capacitance

57
Q

what are 3 effects of calcium channel blocker on the heart

A

reduced contractility
reduced SA pacemaker rate
reduced AV conduction velocity

58
Q

dihydropyrides are calcium channel blockers selective for what

A

peripheral vasculature

59
Q

verapamil and diltiazem are calcium channel blockers selective for what

A

cardiac

60
Q

3 s/s of toxicity of calcium channel blockers

A

bradycardia
AV block
CHF

61
Q

what are the 4 antihypertensive agents

A

diuretics
sympathoplegics
direct vasodilators
anti-angiotensins

62
Q

what is the hydraulic equation formula

A

BP = CO X PVR

63
Q

2 examples of sympathoplegics

A

clonidine
methyldopa

64
Q

what is the mechanism of action of clonidine

A

has alpha agonist activity in the brainstem, decreasing symphathetic stimulation
binds more to alpha-2 than alpha-1

65
Q

which alpha receptor does clonidine bind more to

A

alpha-2

66
Q

what substance produced in the kidney does propanolol prevent from being made

A

renin

67
Q

alpha1 blockers such as prazosin reduce blood pressure more in which position (upright or supine?)

A

upright

68
Q

what is the mechanism of action of prazosin

A

blocks alpha1 receptors in arterioles and venules

69
Q

what is the mechanism of action of minoxidil

A

opens potassium channels in smooth muscle

70
Q

name 3 toxicities of hydralazine

A

headache
nausea
sweating
flushing

71
Q

what medications are given for hypertensive emergencies

A

fenoldopam
sodium nitroprusside

72
Q

what medication inhibits renin from converting angiotensinogen to angiotensin

A

aliskiren

73
Q

what medication prevents conversion of kinninogen to bradykinin

A

kallikrein

74
Q

difference between systolic and diastolic heart failure

A

systolic is due to reduced cardiac pumping while diastolic is due to reduced cardiac filling

75
Q

which heart failure has normal ejection fraction

A

diastolic

76
Q

which heart failure does not respond well to positive inotropic drugs

A

diastolic

77
Q

what is the mechanism of action of digoxin

A

inhibits Na/K ATPase

78
Q

is digoxin a positive or negative inotrope

A

positive

79
Q

what dose is the EC50 of digoxin?

A

1 ng/ml

80
Q

what dose is the TC50 of digoxin?

A

2 ng/ml

81
Q

what is the mechanism of action of PDEi

A

inactivate cAMP and cGMP

82
Q

what is the effect of phosphodiesterase inhibitor on cardiac inotropy

A

they are positive inotropes

83
Q

what is the normal contraction rate of the SA node

A

75 beats/min

84
Q

where is the bundle of His located

A

interventricular septum

85
Q

what ions are moving out in phase 1 of the cardiac action potential

A

K
Cl

86
Q

what ions are moving in phase 2 of the cardiac action potential and what is their direction of movement

A

Ca (in)
K (out)

87
Q

example of type A sodium channel blocker, and what does it do to the action potential duration

A

quinidine
lengthens APD

88
Q

example of type B sodium channel blocker, and what does it do to the action potential duration

A

lidocaine
shortens APD

89
Q

example of type C sodium channel blocker, and what does it do to the action potential duration

A

flecainide
no effect

90
Q

what medication can act as all four classes of the antiarrhytmics

A

amiodarone

91
Q

where is the NHE exchanger located

A

PCT

92
Q

does furosemide cause acidosis or alkalosis as a side effect

A

alkalosis

93
Q

what channel is found in the DCT

A

NCC

94
Q

what ion is actively reabsorped in the DCT

A

Ca

95
Q

what influence does thiazide diuretic have on carbonic anhydrase

A

some inhibition

96
Q

priniciple cells in collecting duct are sites for transport of what ions

A

water
Na
K

97
Q

what is the antagonist for ADH in the collecting ducts

A

conivaptan

98
Q

effect of toxicity of mannitol

A

extracellular volume expansion

99
Q

what are the 4 receptors of histamine

A

H1
H2
H3
H4

100
Q

give 2 effects of histamine H1

A

bronchoconstriction
vasodilation

101
Q

relationship of antihistamines to H1 (are they: agonist, antagonist, partial agonist, inverse agonist)

A

inverse agonists

102
Q

diphenhydramine is most useful for what type of hypersensitivity

A

type 1

103
Q

effects of histamine on the nervous system

A

stimulates pain and itching

104
Q

effects of first generation H1 antagonist on parkinson disease

A

suppress extrapyramidal symptoms

105
Q

effect of first generation H1 antagonist on excitable membrane

A

act as anesthestic - block Na channel

106
Q

which substance released in the body during anaphylaxis is slow acting

A

leukotriene

107
Q

where is leukotriene liberated during inflammation

A

lungsw

108
Q

name 3 effects of leukotriene

A

bronchospasm
airway edema
mucous secretion
microvascular permeability

109
Q

what are the 3 bronchodilator classes used to treat asthma

A

beta agonists
methylxanthines
anti-muscarinics

110
Q

what are the 3 anti-inflammatory classes used to treat asthma

A

steroids
antibodies
slow antiinflammatory drugs

111
Q

what are the 2 leukotriene antagonist classes used to treat asthma

A

lipooxygenese inhibitors
receptor inhibitors

112
Q

what is the toxic effect of sympathomimetics

A

skeletal muscle tremors

113
Q

what is the clinical use of muscarinic antagonists in asthma

A

block contraction of airway smooth muscle

114
Q

what do leukotriene pathway inhibitors do

A

interrupt synthesis pathway

115
Q

what enzyme does zileuton inhibit (leukotriene pathway)

A

5-lipoxygenase

116
Q

which medication is a leukotriene pathway inhibitor that inhibits binding to receptor

A

montelukast
zafirlukast

117
Q

what do anti-IgE monoclonal antibodies do

A

target the portion of IgE that binds to mast cell

118
Q

example of anti-IgE monoclonal antibody

A

omalizumab