pharm part1 Flashcards
(118 cards)
1
Q
what is the pKa
A
pH at which the ionized and unionized concentrations are equal
2
Q
if pH < pKa, what is favored: the protonated or the unprotonated form
A
protonated
3
Q
if pH > pKa, what is favored: the protonated or the unprotonated form
A
unprotonated
4
Q
what is the therapeutic index formula
A
TD50/ED50
5
Q
bond strength is directly proportional to specificity. true/false?
A
false. it is indirectly proportional
6
Q
flux is directly proportional to specificity. true/false?
A
true
7
Q
Kd is directly proportional to drug binding
affinity. true/false?
A
false. it is indirectly proportional
8
Q
drug safety is directly proportional to drug therapeutic index. true/false?
A
true
9
Q
Volume of Distribution (Vd) is directly
proportional to the concentration of drug
outside of the systemic circulation. true/false?
A
true
10
Q
what is the definition of volume of distribution
A
apparent volume of a drug
11
Q
what is clearance
A
predicts rate of elimination in relation to drug concentration
12
Q
in first order elimination, which value is constant
A
clearance
13
Q
in zero order elimination, which value is constant
A
rate of elimination
14
Q
what 3 meds use zero order elimination
A
ethanol
phenytoin
aspirin
15
Q
what 4 parameters affect passive diffusion
A
molecular weight
pKa
lipid solubility
plasma protein binding
16
Q
4 basic mechanisms for transmembrane signaling
A
lipid soluble diffusion to intracellular receptor
ligand binding to RTK
ligand gated ion channel
GPCR
17
Q
how many trans-membrane alpha helixes does a GPCR have
A
7
18
Q
what are the 3 major drug efflux transporters in the ABC family
A
B, C, G
19
Q
what is the major site of exclusion in the blood-brain barrier
A
vascular epithelium
20
Q
what enzyme is majorly implicated in phase 1 of metabolism
A
cytochrome P450
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
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
23
Q
what is pharmacokinetics
A
the effects of the body on a drug
24
Q
what is pharmacodynamics
A
the effects of the drug on the body
25
what is pharmacogenomics
the primary reason patients respond differently to the same drug
26
what is pharmacology
the study of the effects of drugs on the body
27
what are the 6 neurotransmitter classes
esters - acetylcholine
monoamines - norepinephrine
amino acids- glutamate
purines - adenosine
peptides - substance P
inorganic gases - nitric oxide
28
where is the location of the ganglia of the sympathetic ANS
close to the spinal cord
29
where is the location of the ganglia of the parasympathetic ANS
in the visceral effector organs
30
what enzymes does alpha-1 receptor activate
phospholipase C
31
what enzymes does beta-1 receptor activate
adenylyl cyclase
32
what enzymes does beta-2 receptor activate
adenylyl cyclase
33
the gut has its own nervous system called the
enteric nervous system
34
alpha1 receptor activation leads to smooth muscle contraction. what are the second messengers produced by agonist binding to alpha-1 receptors
DAG
IP3
35
give an example of indirect acting adrenergic agonist
amphetamine
36
give 2 examples of adrenergic antagonist drugs
phentolamine
prazosin
labetalol
37
what is the important thing to note about phenoxybenzamine (adrenoceptor antagonist drug)
forms irreversible covalent bonds
38
what effect does beta agonists have on the blood vessels
opposes beta2-mediated vasodilation
39
which beta blocker is ultra short acting
esmolol
40
which betablocker is safer in COPD and diabetic patients
metoprolol
atenolol
41
what is the effect of cholinomimetics on the eye
miosis
increase intraocular drainage
42
what is the effect of cholinomimetics on the CV
vasodilation
reduction in PVR
bradycardia if given in large doses
43
what indirect acting cholinomimetic is a simple alcohol
edrophonium
44
give 2 major uses of indirect acting cholinomimetics
eye disease
GI/Urinary tract
NMJ
atropine overdose
45
what are the s/s of organophosphate exposure
SLUDGE-M
46
what are the s/s of poisonous mushroom exposure
SLUDGE-M
47
what are the s/s of atropine overdose
BRAND
blind, red, absent bowel sounds, nuts, dry
48
what medication are given for organophosphate exposure
atropine, pralidozime
49
what medication is given for poisonous mushroom exposure
atropine
50
what medication is given for atropine overdose
physostigmine
51
what is the difference between unstable and variant angina
unstable is caused by plaque while variant angina is caused by hyperreactive vessels
52
what is the action of nitrates on vascular smooth muscle
activate guanyly cyclase and increase cGMP, causing relaxation
53
what is the action of beta-2 agonists on vascular smooth muscle
act on GPCR to increase cAMP, causing relaxation
54
what is the action of sildenafil on vascular smooth muscle
blocks PDE-5, increase cGMP, causing relaxation
55
what are the 3 bad effects of nitrates
orthostatic hypotension
syncope
headache
reflex tachy
56
what are the 3 good effects of nitrates
reduced preload
reduced heart size
reduced CO
increased venous capacitance
57
what are 3 effects of calcium channel blocker on the heart
reduced contractility
reduced SA pacemaker rate
reduced AV conduction velocity
58
dihydropyrides are calcium channel blockers selective for what
peripheral vasculature
59
verapamil and diltiazem are calcium channel blockers selective for what
cardiac
60
3 s/s of toxicity of calcium channel blockers
bradycardia
AV block
CHF
61
what are the 4 antihypertensive agents
diuretics
sympathoplegics
direct vasodilators
anti-angiotensins
62
what is the hydraulic equation formula
BP = CO X PVR
63
2 examples of sympathoplegics
clonidine
methyldopa
64
what is the mechanism of action of clonidine
has alpha agonist activity in the brainstem, decreasing symphathetic stimulation
binds more to alpha-2 than alpha-1
65
which alpha receptor does clonidine bind more to
alpha-2
66
what substance produced in the kidney does propanolol prevent from being made
renin
67
alpha1 blockers such as prazosin reduce blood pressure more in which position (upright or supine?)
upright
68
what is the mechanism of action of prazosin
blocks alpha1 receptors in arterioles and venules
69
what is the mechanism of action of minoxidil
opens potassium channels in smooth muscle
70
name 3 toxicities of hydralazine
headache
nausea
sweating
flushing
71
what medications are given for hypertensive emergencies
fenoldopam
sodium nitroprusside
72
what medication inhibits renin from converting angiotensinogen to angiotensin
aliskiren
73
what medication prevents conversion of kinninogen to bradykinin
kallikrein
74
difference between systolic and diastolic heart failure
systolic is due to reduced cardiac pumping while diastolic is due to reduced cardiac filling
75
which heart failure has normal ejection fraction
diastolic
76
which heart failure does not respond well to positive inotropic drugs
diastolic
77
what is the mechanism of action of digoxin
inhibits Na/K ATPase
78
is digoxin a positive or negative inotrope
positive
79
what dose is the EC50 of digoxin?
1 ng/ml
80
what dose is the TC50 of digoxin?
2 ng/ml
81
what is the mechanism of action of PDEi
inactivate cAMP and cGMP
82
what is the effect of phosphodiesterase inhibitor on cardiac inotropy
they are positive inotropes
83
what is the normal contraction rate of the SA node
75 beats/min
84
where is the bundle of His located
interventricular septum
85
what ions are moving out in phase 1 of the cardiac action potential
K
Cl
86
what ions are moving in phase 2 of the cardiac action potential and what is their direction of movement
Ca (in)
K (out)
87
example of type A sodium channel blocker, and what does it do to the action potential duration
quinidine
lengthens APD
88
example of type B sodium channel blocker, and what does it do to the action potential duration
lidocaine
shortens APD
89
example of type C sodium channel blocker, and what does it do to the action potential duration
flecainide
no effect
90
what medication can act as all four classes of the antiarrhytmics
amiodarone
91
where is the NHE exchanger located
PCT
92
does furosemide cause acidosis or alkalosis as a side effect
alkalosis
93
what channel is found in the DCT
NCC
94
what ion is actively reabsorped in the DCT
Ca
95
what influence does thiazide diuretic have on carbonic anhydrase
some inhibition
96
priniciple cells in collecting duct are sites for transport of what ions
water
Na
K
97
what is the antagonist for ADH in the collecting ducts
conivaptan
98
effect of toxicity of mannitol
extracellular volume expansion
99
what are the 4 receptors of histamine
H1
H2
H3
H4
100
give 2 effects of histamine H1
bronchoconstriction
vasodilation
101
relationship of antihistamines to H1 (are they: agonist, antagonist, partial agonist, inverse agonist)
inverse agonists
102
diphenhydramine is most useful for what type of hypersensitivity
type 1
103
effects of histamine on the nervous system
stimulates pain and itching
104
effects of first generation H1 antagonist on parkinson disease
suppress extrapyramidal symptoms
105
effect of first generation H1 antagonist on excitable membrane
act as anesthestic - block Na channel
106
which substance released in the body during anaphylaxis is slow acting
leukotriene
107
where is leukotriene liberated during inflammation
lungsw
108
name 3 effects of leukotriene
bronchospasm
airway edema
mucous secretion
microvascular permeability
109
what are the 3 bronchodilator classes used to treat asthma
beta agonists
methylxanthines
anti-muscarinics
110
what are the 3 anti-inflammatory classes used to treat asthma
steroids
antibodies
slow antiinflammatory drugs
111
what are the 2 leukotriene antagonist classes used to treat asthma
lipooxygenese inhibitors
receptor inhibitors
112
what is the toxic effect of sympathomimetics
skeletal muscle tremors
113
what is the clinical use of muscarinic antagonists in asthma
block contraction of airway smooth muscle
114
what do leukotriene pathway inhibitors do
interrupt synthesis pathway
115
what enzyme does zileuton inhibit (leukotriene pathway)
5-lipoxygenase
116
which medication is a leukotriene pathway inhibitor that inhibits binding to receptor
montelukast
zafirlukast
117
what do anti-IgE monoclonal antibodies do
target the portion of IgE that binds to mast cell
118
example of anti-IgE monoclonal antibody
omalizumab
