Exam 1 Flashcards
1
Q
what immunoglobulin mediates type 1 reaction?
A
IgE
2
Q
immediate-type hypersensitivity characterizes what type of ADR?
A
type 1
3
Q
anaphylaxis characterizes what type of drug reaction?
A
type 1
4
Q
antibody-dependent cytotoxicity, what type of drug reaction?
A
type 2
5
Q
heparin-induced thrombocytopenia is an example of which drug reaction type?
A
type 2
6
Q
graft rejection is an example of which drug reaction type?
A
type 2
7
Q
heparin-induced thrombocytopenia and graft rejection, examples of which drug reaction type?
A
type 2
8
Q
immune complex hypersensitivity- which drug reaction type?
A
type 3
9
Q
arthus reaction to tetanus vaccine- which drug reaction type?
A
type 3
10
Q
lupus is an example of which drug reaction type?
A
type 3
11
Q
cell-mediated or delayed hypersensitivity- which drug reaction type?
A
type 4
12
Q
rash, eosinophilia, PPD test, poison ivy- which drug reaction type?
A
type 4
13
Q
eosinophilia- which drug reaction type?
A
type 4
14
Q
what is the term for drugs that produce receptor site stimulation?
A
agonists
15
Q
agonists, think WHAT?
A
act
16
Q
what do agonists produce?
A
receptor site stimulation
17
Q
antagonists, think WHAT?
A
block
18
Q
what type of drugs block receptor site stimulation?
A
antagonists
19
Q
what do antagonists block?
A
receptor site stimulation
20
Q
what do antagonists do?
A
block receptor site stimulation
21
Q
parasympathetic nervous system is part of what system?
A
autonomic nervous system
22
Q
what NT does parasympathetic nervous system release?
A
acetylcholine
23
Q
acetylcholine is released by what system?
A
parasympathetic nervous system
24
Q
what system counterbalances sympathetic activity?
A
parasympathetic nervous system
25
what two types of receptors does acetylcholine activate?
muscarinic and nicotinic
26
what are the two cholinergic receptors?
muscarinic and nicotinic
27
muscarinic and nicotininc receptors are activated by what?
acetylcholine
28
what effect does parasympathetic nervous system have on pupils?
constriction
29
what effect does PNS have on salivation?
stimulates salivation
30
what effect does PNS have on heart rate?
decreases HR
31
what effect does PNS have on contractility?
decreases contractility
32
what effect does PNS have on bronchi?
bronchial constriction
33
what effect does PNS have on digestion?
stimulates digestion
34
what effect does PNS have on gallbladder?
stimulates gallbladder
35
what effect does PNS have on bladder?
contracts bladder
36
what effect does PNS have on rectum?
relaxes rectum
37
what effect does PNS have on peripheral vascular system?
peripheral vasodilation
38
what do most postganglionic neurons release? (NT)
norepinephrine
39
what do adrenal medullary neurons release? (NT)
mix of epinephrine and norepinephrine
40
sympathetic nervous system is under which nervous system?
autonomic nervous system
41
what are the three types of receptors activated by epinephrine and norepinephrine?
alpha, beta, dopamine
42
what are the three types of adrenergic receptors?
alpha, beta, dopamine
43
alpha, beta, and dopamine are what type of receptors?
adrenergic
44
what effect does SNS have on pupils?
dilates pupils
45
what effect does SNS have on salivation?
inhibits salivation
46
what effect does SNS have on bronchi?
bronchial dilation
47
what effect does SNS have on heart rate?
increased heart rate
48
what effect does SNS have on digestion?
inhibits digestion
49
what effect does SNS have on contractility?
increases contractility
50
what effect does SNS have on glucose release?
stimulates glucose release by liver
51
what effect does SNS have on bladder?
relaxes bladder????
52
what effect does SNS have on rectum?
contracts rectum
53
what effect does SNS have on peripheral vascular system?
peripheral vasoconstriction
54
what type of drug is clonidine?
central acting adrenergic agonists
55
can you stop taking central acting adrenergic agonists abruptly? (e.g. clonidine)
no
56
what type of receptors are found in the eyes, salivary glands, arterioles, GI and GU tract?
alpha 1 receptors
57
where are alpha 1 receptors located?
eyes, salivary glands, arterioles, GI and GU tract
58
what happens when alpha 1 receptors are stimulated?
cause vascular and GI smooth muscle contraction
59
what effect do alpha 1 agonists have on peripheral vascular resistance?
increased peripheral vascular resistance
60
what effect do alpha 1 agnosists have on contractility?
increased contractility
61
what effect do alpha 1 agonists have on blood pressure?
increased blood pressure
62
alpha 1 agonists- vasoconstriction or vasodilation?
vasoconstriction
63
phenylephrine is an example of what type of drug?
alpha 1 agonists
64
methoxamine is an example of what type of drug?
alpha 1 agonists
65
what are two examples of alpha 1 agonists?
phenylephrine and metoxamine
66
what are the side effects of alpha 1 agonists?
headache, bradycardia, excitability, and restlessness
67
headaches, bradycardia, excitability, restlessness- side effects of what drug class?
alpha 1 agonists
68
what type of medication should be avoided with alpha 1 antagonists?
NSAIDS
69
doxazosin/cardura- what drug class?
alpha 1 antagonist
70
prazosin (for PTSD) what drug class?
alpha 1 antagonist
71
terazosin- what drug class?
alpha 1 antagonist
72
alpha 1 antagonists are often given for what condition?
BPH
73
what do alpha 1 antagonists do in the context of BPH?
block contraction of the GU smooth muscle so patients can urinate
74
what do alpha 1 antagonists do in the context of HTN?
help lower blood pressure through vasodilation as it inhibits norepinephrine
75
what NT do alpha 1 antagonists inhibit?
norepinephrine
76
alpha 1 antagonists cause vasoconstriction or vasodilation?
vasodilation
77
reflex tachycardia- SE of what drug class?
alpha 1 antagonist
78
orthostatic hypotension- seen with what drug class?
alpha 1 antagonist
79
fluid retention- seen with what drug class?
alpha 1 antagonist
80
peripheral edema- seen with what drug class?
alpha 1 antagonist
81
nasal congestion- SE what drug class?
alpha 1 antagonist
82
blurred vision- SE what drug class?
alpha 1 antagonist
83
dry mouth- SE what drug class?
alpha 1 antagonist
84
syncope- SE what drug class?
alpha 1 antagonist
85
impotence- SE what drug class?
alpha 1 antagonist
86
what is heart rate trying to compensate for as SE of alpha 1 antagonists?
hypotension (blood vessels become bigger when relaxed)
87
increased HR is compensating for what with alpha 1 antagonists?
hypotension (blood vessels become bigger when relaxed)
88
where are alpha 2 receptors located?
presynaptic nerve terminal of the smooth muscles, platelets, and lipocytes
89
what receptors are located in the presynaptic nerve terminal of the smooth muscles, platelets, and lipocytes?
alpha 2
90
what effect do alpha 2 agonists have on NE?
decreases NE
91
what effect do alpha 2 agonists have on peripheral vascular system?
cause vasodilation
92
what effect do alpha 2 agonists have on peripheral vascular resistance?
decreased PVR
93
what effect do alpha 2 agonists have on renal vascular resistance?
decreased renal vascular resistance
94
what effect do alpha 2 agonists have on HR?
decrease HR
95
what effect do alpha 2 agonists have on sympathetic response?
blocks body's sympathetic response
96
what effect do alpha 2 agonists have on cardiac output/blood flow?
decreased cardiac output/blood flow
97
clonidine is an example of what drug class?
alpha 2 agonist
98
methyldopa is an example of what drug class?
alpha 2 agonist
99
clonidine and methyldopa are examples of what drug class?
alpha 2 agonist
100
what drug class should be avoided with coronary insufficiency, CVD, MI, renal function impairment and reacts with beta blockers?
alpha 2 agonist
101
what are the side effects of alpha 2 agonists?
hypotension, dry mouth/mucous membranes, bradycardia, impotence, nightmares, sedation
102
hypotension, dry mouth/mucous membranes, bradycardia, impotence, nightmares, sedation- SE what drug class?
alpha 2 agonist
103
what drug class increases release of norepinephrine?
alpha 2 antagonist
104
what drug class increases NE release and can be used in some cases to treat sexual dysfunction?
alpha 2 antagonist
105
what are two examples of alpha 2 antagonists?
yohimibine and idazoxan
106
yohimbine and idazoxan- what drug class?
alpha 2 antagonist
107
three common side effects of alpha 2 antagonists?
dizziness, headaches, and reflex tachycardia
108
dizziness, headaches, reflex tachycardia- common SE of what drug class?
alpha 2 antagonist
109
beta 1 antagonist- what effect on heart rate?
decrease heart rate
110
beta 1 antagonist- what effect on contractility?
decrease contractility
111
beta 1 antagonist- what effect on conduction velocity?
decrease conduction velocity
112
three examples of beta 1 antagonists?
atenolol, metoprolol, esmolol
113
atenolol, metoprolol, esmolol- what drug class?
beta 1 antagonist
114
mild bronchoconstriction, bradycardia, hypotension, impotence- commone SE what drug class?
beta 1 antagonist
115
common SE of beta 1 antagonists?
mild bronchoconstriction, bradycardia, hypotension, impotence
116
why do you want to avoid beta 1 antagonists in asthmatic patient?
fear of bronchoconstriction
117
what happens if you stop beta 1 antagonists abruptly? (CV)
cardiac spasms that may potentially lead to MI
118
location of beta 2 agonist receptors?
smooth muscle of eye, arterioles, venules, bronchioles, liver, pancrease, GI and GU
119
what receptors are located in the smooth muscle of the eye, arterioles, venules, bronchioles, liver, pancreas, GI and GU tracts?
beta 2 agonist
120
what drug class- acts as a bronchodilator that can treat bronchospasms?
beta 2 agonist
121
what drug class- decreases GI tone and motility?
beta 2 agonist
122
what drug class- relaxes uterine contractions?
beta 2 agonist
123
what drug class- activates gluconeogenesis in the liver to inrease blood sugar?
beta 2 agonist
124
what effect does beta 2 agonist have on bronchi?
bronchodilator
125
what effect does beta 2 agonist have on GI tone and motility?
decreased GI tone and motility
126
what effect does beta 2 agonist have on uterine contractions?
relaxes uterine contractions
127
albuterol and terbutaline- examples what drug class?
beta 2 agonist
128
what are two examples of beta 2 agonists?
albuterol and terbutaline
129
what class SE- trembling, nervous tension, palpitations, muscle cramps?
beta 2 agonist
130
common SE of beta 2 agonists?
trembling, nervous tension, palpitations, muscle cramps
131
what class- cause bronchoconstriction on beta 2 receptors, oppose vasodilation, increase PVR?
beta 2 antagonists
132
what effect do beta 2 antagonists have on bronchi?
bronchoconstriction
133
what effect do beta 2 antagonists have on PVR?
increase PVR
134
what effect do beta 2 antagonists have on vasodilation?
oppose vasodilation
135
what class- used for angina, HTN, post-MI, migraines, glaucoma?
beta 2 antagonists
136
what are uses for beta 2 antagonists?
angina, HTN, post-MI, migraines, glaucoma
137
common SE what class? Tachycardia, tremors, anxiety, depression, hypotension, sexual dysfunction, arrhythmias
beta 2 antagonists
138
what are common SE of beta 2 antagonists?
tachycardia, tremors, anxiety, depression, hypotension, sexual dysfunction, arrhythmias
139
beta 2 antagonists- avoid giving this med to who? (more than B1)
asthmatics
140
beta 2 antagonists should be avoided more than B1 in asthmatic patients why?
bronchoconstriction
141
beta 2 antagonists- use caution in what patient popultion?
diabetic patients
142
why should beta 2 antagonists be used cautiously in diabetic patients?
block symptoms of hypoglycemic episoes
143
what is an example of a beta 2 antagonist?
propranolol
144
propranolol- what drug class?
beta 2 antagonists
145
where is sodium bicarbonate most likely to be absorbed?
intestines
146
what is the most frequent category of drug-WHAT interaction?
food
147
why is drug-food interaction the most common?
food affects the GI absorption of drugs
148
how should oral enteric-coated tablets be taken?
to achieve the best effect take the tablet with at least 8 oz of fluid
149
how much fluid should be taken orally with EC tablets?
8 oz
150
food in the GI tract affects drug absorption by?
altering gastric emptying time
151
food can alter the Ph of the stomach leading to…?
altered drug bioavailability
152
lipid solubility of the drug affects what?
drug absorption
153
a rich blood supply to the area of absorption leads to what?
better drug absorption
154
term- the fraction of a drug that reaches the systemic circulation?
bioavailability
155
what is the definition of bioavailability?
the fraction of drug that reaches the system circulation
156
what factors (5) affect bioavailability?
solubility, chemical structure, size, polarity, pre-systemic biotransformation
157
solubility, chemical structure, size, polarity, pre-systemic biotransformation affect what?
bioavailability
158
what (4) things do drug absorption depend on?
first pass metabolism, food, surface area, drug size
159
first pass metabolism, food, surface area, drug size- affect what?
drug absorption
160
fasting for an extended period of time can do what to absorption?
cause vasoconstriction which leads to decreased drug absorption
161
a low-carb, high-protein diet may what?
increase drug metabolizing enzymes
162
why do you not crush a sustained-release capsule?
if you crush the capsule the coated beads of drug can lead to toxicity
163
why is medroxyprogesterone/depo provera given IM?
to create a storage reservoir
164
what does the storage reservoir create (depo)?
increased length of time the drug is available and can be actively distributed
165
the ability of the body to excrete drugs via the renal system would be increased by…?
unbinding a nonvolatile drug from the plasma protein
166
until drugs are changed or excreted they continue to what?
act in the body
167
what is the difference in drug effects between men and women? (pharmacokinetics)
percentage of fat differs between the genders
168
nurse practitioner prescriptive authority is regulated by what?
state board of nursing
169
three facets of therapeutic goals when prescribing medications?
curative, palliative, and preventative measures
170
patient education regarding prescription medication should include discussion of what?
expected adverse drug reactions
171
assessment to determine diagnosis is what type of factor in prescribing medication?
factor associated with clinical judgement
172
review of potential alternative therapies is what type of factor in prescribing medication?
factor associated with clinical judgement
173
least invasive, least expensive, and least likely to cause an adverse reaction- what type of factor in prescribing medication?
factor associated with clinical judgement
174
assessment of other medications and supplements the patient is taking- what type of factor in prescribing medication?
factor associated with clinical judgement
175
what are the four factors associated with clinical judgement in prescribing medication?
(1) assessment to determine diagnosis (2) review of potential alternative therapies (3) least invasive, least expensive, least likely to cause an adverse reaction, (4) assessment of other medications and supplements that the patient is taking
176
what criteria should be followed for choosing an effective drug?
consulting nationally recognized guidelines for disease management
177
what are three cultural factors that must be considered when prescribing medications?
(1) who is the decision maker in the family for health-care decisions (2) patient's view of health and illness (3) attitudes regarding use of drugs to treat illness
178
pharmacodynamic considerations in prescribing with different ethnicities?
ethnic differences have been found in drugs in regard to hepatic metabolism
179
what are patient benefits to having an APRN prescriber?
nurses care for the patient from a holistic approach and include patient in decision making regarding their care
180
why may NP thrive under healthcare reform?
the demonstrated ability of nurse practitioners to control costs and improve patient outcomes
181
what are the four clinical influences affecting how providers make decisions?
(1) competing demands (2) knowledge of and agreement with clinical guidelines (3) organizational issues- ancillary support; follow-up appointments (4) assessment of patient adherence
182
(1) competing demands (2) knowledge of and agreement with clinical guidelines (3) organizational issues- ancillary support; follow-up appointments (4) assessment of patient adherence are WHAT?
four clinical influences affecting how providers make decisions
183
what are the five medication-related factors affecting how providers make decisions?
(1) side effects (2) contraindication (3) cost (4) convenience/complexity/dosing (4) patient/provider medication knowledge
184
diabetes-related knowledge is part of what consideration?
patient attitudes and values (how providers make decisions)
185
what factors are considerations involving patient attitudes and values? (3) (how providers make decisions)
(1) perceived risk (2) belief in treatment efficacy (3) health goals/values
186
cognitive skills (memory) affect what?
how providers make decisions- patient influences
187
health literacy affects what?
how providers make decisions- patient influences
188
autonomous motivation affects what?
how providers make decisions- patient influences
189
self-efficacy affects what?
how providers make decisions- patient influences
190
social support- affects what?
how providers make decisions- patient influences
191
environmental barriers- affects what?
how providers make decisions- patient influences
192
general adherence affects what?
how providers make decisions- patient influences
193
symptom burdon affects what?
how providers make decisions- patient influences
194
comorbidities affect what?
how providers make decisions- patient influences
195
diabetes-specific emotional distress affects what?
how providers make decisions- patient influences
196
drugs with a significant WHAT are rapidly metabolized by the liver and may have little, if any, desired action?
first pass effect
197
drugs with a significant first pass effect are what?
rapidly metabolized by the liver
198
drugs with a signifcant first pass effect that are rapidly metabolized by the liver may have what?
little if any desired action
199
what percentage of drugs are eliminated in the liver at first?
0.5
200
50% of drugs are eliminated in the liver at first and then go where?
systemic circulation
201
how many half lives are required to eliminate a drug? (significant FPE)
4-5 half lives
202
drugs are metabolized mainly by the liver in what two reactions?
phase I and phase II
203
phase I and phase II reactions change drug molecules into…?
a form that an excretory organ can excrete
204
WHAT may be more active, less active, or totally deactivated compared to parent drug?
metabolites
205
metabolies may be WHAT (3 things) than parent drug?
more active, less active, or totally deactivated
206
term? The proportion of a drug which enters the circulation when introduced into the body and so is able to have an active effect
bioavailability
207
bioavailability is what?
the proportion of a drug which enters the circulation when introduced into the body so is able to have an active affect
208
when are bioavailability issues especially important?
drugs with narrow therapeutic ranges or sustained-release mechanisms
209
term? The time it takes for the concentration of the drug in the body to fall by halg/50%
half-life
210
what is the half life?
the time it takes for the concentration of the drug in the blood to fall by half/50%
211
term? The amount of drug needed to get the concentration in the plasma to a therapeutic level quicker
loading dose
212
what is the loading dose?
the amount of drug needed to get the concentration in the plasma to a therapeutic level quicker
213
Example of what? Z-pack with 2 pills the first day to achieve a therapeutic range
loading dose
214
term? The time between drug administration and the minimum concentration of a drug to produce an effect
onset of action
215
what is the onset of action?
the time between drug administration and the minimum concentration of a drug to produce an effect
216
how is the onset of action seen on drug concentration curve?
first sign of therapeutic effect
217
term? The time between drug administration and the maximum concentration of a drug in the blood stream
peak of action
218
another term for peak of action
best therapeutic effect
219
what is the definition of peak of action?
the time between drug administration and the maximum concentration of a drug in the blood stream
220
what is the definition of best therapeutic effect?
the time between drug administration and the maximum concentration of a drug in the blood stream
221
term? The time between the onset of action and metabolism of the drug below the minimum needed for an effect
duration of action
222
what is the definition of duration og action?
the time between the onset of action and metabolism of the drug below the minimum needed for an effect
223
the length of time you have the drug in your system reflects what?
duraction of action
224
duration of action reflects what?
the length of time you have the drug in your system
225
term? The ability of a drug to produce a maximum effect at any dosage
efficacy
226
what is the definition of efficacy?
the ability of a drug to produce a maximum effect at any dosage
227
term? The expression of the maximum effect a drug can produce
efficacy
228
efficacy example- asians are known to be fast WHAT- meaning that they require higher doses of drugs to achieve efficacy?
acetylators
229
effects of tylenol versus morphine is an example of what?
efficacy- morphine is much stronger than tylenol as it produces more pain blocking power
230
what levels are used to determine therapeutic level of drugs?
peak/trough
231
peak/trough levels are used to determine what?
therapeutic level of drugs
232
if a lab result indicates the peak level of a drug is above the WHAT, this means that this will produce an adverse response?
minimum toxic concerntration
233
if a lab result indicates the peak level of a drug is above the minimum toxic concentration, this means that this will produce an ….
adverse response
234
examples of meds with peak/trough (2)?
phenytoin; vancomycin
235
term? The amount of drug in the body that remains constant
steady state
236
steady state definition?
the amount of drug in the body that remains constant
237
term? The rate of drug intake that is equal to the rate of drug elimination; attained after approximately four, occasionally five half-lives
steady state
238
when is steady state attained?
after approximately four, sometimes five half-lives
239
what does lipophilic mean?
lipid loving
240
term? Lipid loving
lipophilic
241
lipophilic drugs generally have a high WHAT?
high volume of distribution
242
lipophilic drugs are primarily cleared by what organ?
liver
243
lipophilic drugs have what two properties?
non-ionized, uncharged
244
lipophilic drugs are small or large in size?
small in size?
245
do lipophilic drugs cross the membranes easily?
yes
246
term? Water loving
hydrophilic
247
hydrophilic definition?
water loving
248
hydrophilic drugs generall have a low WHAT?
low volume of distribution
249
lipophilic drugs generally have a LOW or HIGH volume of distribution?
high
250
hydrophilic drugs generally have a LOW or HIGH volume of distribution?
low
251
organ that primarily clears hydrophilic drugs?
kidneys
252
kidneys or liver primarily clear lipophilic drugs?
liver
253
kidneys or liver primarily clear hydrophilic drugs?
kidneys
254
hydrophilic drugs- small or large in size?
large
255
hydrophilic drugs cross membranes easily?
no
256
hydrophilic or lipophilic drugs cross membranes easily?
lipophilic
257
ionized/charged or non-ionized uncharged- lipophilic?
non-ionized, uncharged
258
ionized/charged or non-ionized uncharged- hydrophilic?
ionized/charged
259
term? Moving from an area of high concentration to an area of low concentration
passive diffusion
260
passive diffusion- definition?
moving from an area of high concentration to an area of low concentration
261
what type of drugs can cross the membrane through passive diffusion?
lipid-soluble drugs
262
what type of drugs have to be filtered through the aqueous pore/paracellular space?
non-lipid soluble drugs
263
passive diffusion involves moving from an area of WHAT concentration to an area of WHAT concentration?
high to low
264
hypoalbuminemia affects what?
distribution of drugs to target tissues
265
what condition? If not enough protein available to bind with the drug
hypoalbuminemia
266
what condition causes too much free drug to build up in the system and become toxic?
hypoalbuminemia
267
what happens when drugs are bound to albumin?
they stay in the system longer and are not eliminated
268
what should you do if giving two protein bound drugs?
consider giving them at different times
269
what kind of diseases can affect production of albumin?
liver diseases
270
what are three examples of liver diseases that can affect production of albumin?
AIDS, cancer, cirrhosis
271
AIDS, cancer, cirrhosis can affect what?
production of albumin
272
what term? Protects the brain from substances that may harm the brain,
blood brain barrier
273
term? Protects the brain from hormones and neurotransmitters that are in the rest of the body?
blood brain barrier
274
blood brain barrier protects brain from what two things in the rest of the body?
hormones and neurotransmitters
275
WHAT helps maintain a constant environment for the brain?
blood brain barrier
276
do large molecules pass through BBB easily?
no
277
low lipid (fat) soluble molecules cross BBB fast or slow?
fast
278
molecules with a high or low electrical charge cross BBB fast or slow?
slow
279
typically, only meds that are WHAT cross the BBB?
lipid-soluble
280
WHAT slows the entry of many drugs into and from brain cells?
BBB
281
term? Lipid membrane that allows passage of drugs by simple diffusion
fetal placental barrier
282
smaller molecule or larger molecule drugs pass more easily across fetal placental barrier?
smaller molecule drugs
283
simultaneous use of several different drugs (drug-drug interactions) increase risk for what?
adverse drug reactions
284
age groups (2) at risk for ADRs?
young or old
285
pregant pts are at risk for what?
ADRs
286
breast feeding patients are at risk for what?
ADRs
287
hereditary factors play a role in the risk for what?
ADRs
288
disease states with may affect drug absorption, metabolism, and/or elimination increase risk for what?
ADRs
289
dry mouth, dry eyes, decreased urine output, increased stomach acid- examples of what?
anticholinergic effects
290
cannot see, cannot pee, cannot spit, cannot shit---- memory device for what?
anticholinergic effects
291
anticholinergic prototype drug?
atropine
292
atropine- drug prototype?
anticholinergic
293
two types of adverse reactions?
intrinsic and idiosyncratic
294
term? Predictable and dose-related adverse reaction
intrinsic
295
term? Unpredictable and not dose-related advserse reaction
idiosyncratic
296
example of idiosyncratic adverse reaction?
rash
297
rash is an example of what type of ADR? Intrinsic or idiosyncratic
idiosyncratic
298
term? Using an FDA approved drug for an indication not on the label
off label prescribing
299
what is the definition of off label prescribing?
using an FDA approved drug for an indication not on the label
300
example of off label prescribing?
trazodone (antidepressant) used for sleep
301
what medications (think patient population) are often used off label?
pediatric medications
302
term? Types of drug effects- valued response (BP, HR, Pain, coma score)
graded effect
303
valued response? Term
graded effect
304
yes/no response (seizure, pregnancy, rash) term?
quantal effect
305
graded effect definition?
valued response
306
quantal effect definition?
yes/no response
307
examples of quantal effect?
seizure, pregnancy, rash
308
seizure, pregnancy, rash are examples of what drug effect?
quantal effect
309
examples (4) of graded effect?
BP, HR, Pain, coma score
310
which will predominate in combined alpha and beta?
alpha
311
example (two drugs) of combined alpha and beta?
coreg and labetalol
312
3 uses of combined alpha and beta drugs?
(1) hypertension (2) decreased CHF progression (3) left ventricular dysfunction after MI
313
(1) hypertension, (2) decreased CHF progression (3) left ventricular dysfunction after MI- what type of drugs used?
combined alpha and beta
314
hypotension, bradycardia, bronchospasm exacerbation, dizzy, drowsy, mask low blood sugar- SE of what drugs?
combined alpha and beta
315
common SE of combined alpha and beta?
hypotension, bradycardia, bronchospasm exacerbation, dizzy, drowsy, mask low blood sugar
316
another term for cholinergic agonists?
parasympathomimetics
317
another term for parasympathomimetics?
cholinergic agonists
318
where do cholinergic agonists act? (7)
eyes, heart, blood vessels, lungs, GIT, bladder, sweat glands
319
what drugs work on eyes, heart, blood vessels, lungs, GIT, bladder, sweat glands?
cholinergic agonists
320
what are the two types of cholinergic agonists?
muscarinic and nicotinic
321
two drug examples of muscarinic agonists?
carbachol and pilocarpine
322
carbachol and pilocarpine are examples of what drug class?
muscarinic agonists
323
what type of poisoning can occur with poison mushrooms?
muscarinic poisoning
324
what is the antidote for muscarinic poisoning?
atropine
325
what three things are muscarinic agonists used for?
treats glaucoma, improves GI tone, and urinary bladder tone
326
what class? Treats glaucoma, improves GI tone, urinary bladder tone
muscarinic agonists
327
what class? Metabolize acetylcholinesterase to metabolize and break down acetylcholine at synapses
cholinesterase inhibitor
328
what class? Use for myasthenia gravis (against nicotinic receptors)
cholinesterase inhibitor
329
neostigmine and pyridostigmine help what?
swallow, raise eyelids, treat Alzheimers
330
when should cholinesterase inhibitors be avoided?
if GI/GU obstruction present
331
side effects of cholinesterase inhibitors?
excess GI stimulation, increased salivation, miosis
332
excess GI stimulation, increased salivation, miosis- SE of what class?
cholinesterase inhibitor
333
donepezil drug class?
cholinesterase inhibitor
334
pesticides? (some) drug class
cholinesterase inhibitor
335
donepezil side effects reversible?
yes
336
pesticide SE reversible?
cholinesterase inhibitor SE not reversible
337
class? Selective blockage specific to organ being targeted
anticholinergics
338
another name for cholinergic blockers?
anticholinergics
339
another name for anticholinergics?
cholinergic blockers
340
how to anticholinergics work?
blocks acetylcholine at muscarinic receptors
341
where to anticholinergics block acetylcholine?
muscarininc receptors
342
class? Decreases heart rate, bronchodilation, salivary glands, sweat glands, treats urinary spasms, excitation, and dilates eyes
anticholinergices
343
anticholinergics dilate or constrict pupils?
dilates
344
anticholinergics increase or decrease HR?
decrease
345
effect of anticholinergics on bronchi?
bronchodilation
346
treats urinary spasms- what class?
anticholinergics
347
examples (4) of anticholinergics?
atropine, scopolamine, oxybutynin, carbidopa/levodopa
348
atropine, scopolamine, oxybutynin, carbidopa/levodopa- what class?
anticholinergics
349
atropine- drug class?
anticholinergic
350
scopolamine- drug class?
anticholinergic
351
oxybutynin- drug class?
anticholinergic
352
carbidopa/levodopa- drug class?
anticholinergic
353
SE of what drug class- tachycardia, relaxed respiratory muscles, dry mouth, constipation, urinaty retention, dilated eyes, dizziness, confusion?
anticholinergics
354
SE of anticholinergics?
tachycardia, relaxed respiratory muscles, dry mouth, constipation, urinary retention, dilated eyes, dizziness, confusion
355
term? Referred to as biotransformation/how drug is broken down
metabolism
356
drugs with high WHAT will not be given orally?
first pass effect
357
CYP450 is what?
an oxidative reaction that can vary with genetics
358
an oxidative reaction that can vary with genetics
CYP450
359
CYP34A
responsible for metabolism of many drugs
360
responsible for metabolism of many drugs? (enzyme)
CYP34A (enzyme)
361
Zithromax has a long or short half life?
long
362
penicillin has a long or short half life?
short
363
drug that is inactive until metabolized?
prodrug
364
prodrug is what?
inactive until metabolized
365
there is a lack of studies in safety and efficacy for what population?
pediatric
366
distribution in what population? Less protein binding sites due to less albumin, immature BBB, and increased total body water and lower fat content
infants
367
there are less WHAT type or binding sites in infants?
less protein binding sites
368
why are there less protein binding sites in infants?
less albumin
369
BBB is WHAT in infants?
immature
370
lower or higher fat content in infants?
lower
371
increased or decreased TBW in infants?
increased
372
(metabolism) what organ is immature in infants?
liver
373
there are not enough WHAT (in metabolism) in infants?
enzymes
374
older children may require more meds with WHAT metabolism?
higher
375
less stomach acid until what age?
3 years
376
there is less what until 3 years of age?
stomach acid
377
gastric emptying is slowed until what age range?
6-8 months
378
WHAT is slowed until 6-8 months of age?
gastric emptying
379
immature kidney function- what population?
infants
380
immature GFR- what population?
infants
381
decreased kidney perfusion and renal clearance/urine output until what age?
2 years
382
higher risk for toxicity until what age?
2 years
383
first WHO step in prescribing?
define the patient's problem/make a diagnosis
384
define the patient's problem/make a diagnosis (WHO prescribing)- which step?
first step
385
specify the therapeutic objective and approach- (WHO prescribing)- which step?
second step
386
choose a drug class, generic med, dose, and suitability- (WHO prescribing)- which step?
third step
387
start the treatment/write the script- (WHO prescribing)- which step?
fourth step
388
educate the patient- (WHO prescribing)- which step?
fifth step
389
monitor effectiveness and for adverse effects (WHO prescribing)- which step?
sixth step
390
alter the prescription if necessary- (WHO prescibing)- which step?
seventh step
391
what entity- regulates the labeling of all prescriptions, over the counter medications, and medical devices?
FDA
392
what entity- collect information and monitor safety of human drugs, animal drugs, biological products, medical devices, food, cosmetics, and radiation emission?
FDA
393
what entity? Protecting and promoting publich health through regulation
FDA
394
food safety, tobacco products, RX and OTC, vaccines, biopharmeceuticals, blood transfusions, cosmetics, electromagnetic imaging devices, animal food feeds, veterinary products- regulated by what entity?
FDA
395
post-marketing surveillance- what entity?
FDA
396
determines the official labeling for all Rx and OTC medications?
FDA
397
does FDA have regulation over herbal supplements?
no
398
definition of off label use?
use of prescription drugs for unapproved indications, age groups, dose, route of administration
399
term? Use of prescription drugs for unapproved indications, age groups, dose, route of admin
off-label
400
what two types of drugs can be used in off label ways?
prescription and OTC
401
off label prescribing is legal unless what?
violates ethical or safety guidelines
402
drug development- phase 1?
drug is tested on healthy volunteers
403
drug development- phase 2?
trials with people who have the disease for which the drug is thought to be effective
404
drug tested on healthy volunteers- what phase?
phase 1
405
trials with people who have the disease for which the drug is thought to be effective- what phase?
phase 2
406
drug development- phase 3?
large number of patients in medical research centers receive the drug in phase 3
407
large numbers of patients in medical research centers receive the drug- which phase?
phase 3
408
larger sampling provides information about infrequent or rare adverse effects- which phase?
phase 3
409
when will the FDA approve a new drug application?
if phase 3 studies are satisfactory
410
what is the minimum number of drug trials?
two
411
which phase- confirms clinical doses, frequency, and timing of administration for approval?
phase 3
412
single maximal tolerated dose/several dose levels are tested on the target population- which phase?
phase 2
413
adverse effects are collected to assess benefit-risk potential- which phase?
phase 3
414
designed to test the hypothesis of efficacy- which phase?
phase 3
415
which phase- voluntary and involves postmarket surveillance of the drug's therapeutic effects?
phase 4
416
what population- less physiologically tolerate medication error d/t developing renal, immune, and hepatic functions?
infants/children
417
age-related differences and medication metabolism and mechanisms of action don't necessarily apply to what population?
pediatric population
418
why are kids at high risk for toxicity and ADRs?
immature liver and renal function
419
what is dosing based on in infants/children?
weight (mg/kg)
420
infants have more or less water?
more
421
infants have more or less fat?
less
422
immature liver makes fewer what?
serum proteins
423
at what age is renal function fully developed?
30 months
424
when does gastric ph reach adult level?
1 year
425
acidic environment needed to absorb medication- so MORE or LESS medication will be absorbed by infant?
less
426
children have a larger or smaller body surface area?
greater
427
greater body surface area in children leads to greater absorption of what type of medication?
topical
428
why do infants have greater absorption of topical medication?
skin more permeable
429
what anatomical/physio features lead to increased absorption of topical medications in infants?
increased hydration; thinner stratum corneum
430
WHAT will prevent the absorption of IM or SQ medications? (infants)
immature peripheral circulation
431
less albumin and fewer plasma proteins- what age group?
0-6 months
432
fewer WHAT in pediatric patients result in higher blood conceptrations of two or more drugs or less affinity for one of the drugs?
fewer BINDING SITES in pediatric patients
433
BBB not fully developed in infants leading to greater risk of what?
CNS toxicity
434
cytochrome P-450 3A enzymes play a major role in what?
drug metabolism
435
what enzyme is low in neonates and doesn't reach adult levels until about 6-12 months?
34A
436
when does CYP 34A reach adult levels in babies?
6-12 months
437
what is the earliest isoenzyme to show activity and present in utero (declines rapidly after birth)?
CYP3A7
438
what enzyme decreases throughout the first 6 months?
CYP3A7
439
what enzymes INCREASE after the decrease of CYP3A7?
CYP3A4 and CYP3A5
440
what enzyme is absent in neonates and does not reach adult levels until 3-5?
2D6
441
2D6 is relevant in what type of medication?
cold medicine
442
what is the pathway that metabolizes Robitussin and some of the other ingredients in OTC medications?
Cytochrome P-450 2D6
443
2d6 reaches adult levels when?
about age 5
444
neonates and preterm infants have reduced WHAT 3 things re: kidneys?
reduced GFR, reduced tubular secretion, reduced reabsorption
445
renal function does not reach adult levels until what age?
at least 6 month
446
decreased renal function in neonates leads to extended WHAT?
half life
447
medication errors in pediatrics- top two?
#1 immunizations; #2 antibiotics
448
two reasons for drug therapy in pregnang women?
(1) treat pre-existing medical condition (2) treat pregnancy related conditions
449
five classes of pregnancy/lactation meds?
A B C D X
450
which class of meds can be used during pregnancy?
B
451
what hormone decreases gastric tone and motility in pregnancy?
progesterone
452
what is the effect of progesterone on stomach emptying?
prolonged stomach emptying time
453
what hormone in pregnancy alters pharmacokinetics of oral medications?
progesterone
454
what hormone in pregnancy promotes respiratory changes?
progesterone
455
what effect does progesterone have on tidal volume?
increased tidal volume
456
what effect does progesterone have on pulmonary vasodilation?
increased pulmonary vasodilation
457
what effect does progesterone have on inhaled drug absorption?
inhaled drug absorption increased
458
how much does HR increase in pregnancy?
10-15 beats per minue
459
how much does blood volume increase in pregnancy?
0.5
460
what does the increase in blood volume during pregnancy cause?
hemodilution of plasma albumin
461
plasma levels of what increase during pregnancy?
lipid
462
what is the result of increased plasma lipid levels in pregnancy?
more unbound and free drug
463
why is there more unbound and free drug during pregnancy?
drugs compete for receptor site occupied by hormones
464
what kind of drugs enter fetal circulation?
drugs that are not lipophilic
465
is drug metabolism altered by pregnancy or lactation?
no
466
what are the two properties of drugs that allows them to pass easily into breast milk?
increased lipid solubility and low protein binding (e.g. CNS agents)
467
drugs with low or high molecular weight pass into breast milk?
low molecular weight
468
drugs during lactation with LOW ph produce low or high concentrations?
high concentrations
469
changes in what in geriatric patients lead to increased reisk for orthostatic hypotension and falls?
baroreceptor responsiveness
470
what happens to renal and hepatic blood flow in geriatric patient?
decreased renal/hepatic blood flow (stiffer vessels/atherosclerosis)
471
term? Gradual deterioration of the immune system
immunosenescence
472
immunosenescence in geriatric patient leads to increased risk for what two things?
infection and malignancy
473
what is the #1 cause of morbidity in the elderly?
pneumonia
474
gastric acid increased or decreased in elderly?
decreased
475
systemic availability of drug increased or decreased in elderly?
decreased
476
why is there decreased drug absorption with IM or SQ route in elderly?
decreased blood flow at injection site
477
decreased GI motility, decreased gastric acidity, reduced blood flow in elderly lead to what?
overall slow drug absorption
478
what are the three most problematic drugs (decreased drug distribution) in the elderly?
warfarin, dilantin, SSRIs
479
body mass is increased or decreased in elderly?
decreased
480
body fat is increased or decreased in elderly?
increased
481
increased body fat leads to what type of meds having greater time to excretion?
lipophilic (e.g. benzodiazepines)
482
albumin is increased or decreased in elderly?
decreased
483
BBB is more or less effective in elderly?
less
484
cardiac output is increased or decreased in elderly?
decreased
485
body water is increased or decreased in elderly?
decreased
486
decreased body water in elderly leads to increased levels of what kind of meds?
hydrophilic
487
decreased blood flow in elderly results in less what? (metabolism)
drug clearance
488
what happens to size of liver in elderly?
declines
489
what happens to hepatocytes in elderly?
decreased
490
what happens to first pass effect in elderly?
reduced
491
aging effects the efficiency of what phase of metabolism?
phase 1
492
phase 1 metabolism involves which enzyme?
cytochrome P450
493
what two enzyme systems are slowed in elderly?
34A and 2D6
494
what happens to oxidation in drug metabolism in elderly?
reduced
495
what is the effect of reduced oxidation on half life in elderly?
extended half life
496
is phase 1 or phase 2 metabolism affected more in elderly?
phase 1
497
what is the effect of aging on renal function?
decreased
498
what is the effect of aging on glomerular filtration?
decreased
499
what is the effect of aging on renal tubule excretion?
decreased
500
caution with GFR less than what?
60
501
patient is asymptomatic until GFR is less than what?
35
502
levels of WHAT may remain normal despite GFR changes?
creatinine
503
what happens to muscle mass in elderly?
decreases
504
there is less or more overall creatinine in elderly?
less
505
five classes of drugs in elderly at risk for ADR?
HTN, CAD, analgesics/anti-inflammatory, sedatives, GI meds
506
what meds are often the cause of accidental overdose in elderly?
pain meds
507
how much is hepatic blood flow decreased in elderly?
nearly one-half
508
what percentage is hepatic flow decreased by in elderly?
0.4
509
what percentage of elderly have chronic kidney disease?
0.5
510
what percentage of elderly are affected by heart failure? (over age 80)
0.4
511
what effect does aging have on the first pass effect?
decreases
512
what are the four medications that cause 2/3 of hospitalizations in the elderly?
(1) warfarin, (2) insulin, (3) oral antiplatelet, (4) oral hypoglycemic (sulfonylureas)
513
what ratio is decreased in elderly affecting distribution to body compartments?
lean body weight to body fat
514
what happens to level of serum protein in the elderly?
decrease
515
drug metabolism can be affected by what two types of substance abuse in elderly?
alcohol, polypharmacy
516
what are two examples of medication factors- ADRs in elderly?
drug to drug or drug to food
517
what are two examples of physiological aging changes- ADRs in elderly?
cant hear instructions; can't see label
518
what are patient-related errors in ADRs in elderly?
cognitive; sensory
519
polypharmacy is an example of what type of ADR/error in elderly?
system error
520
what age group (elderly) is at high risk for ADR?
>85
521
what BMI (elderly) is at high risk for ADR?
<22
522
what creatinine clearance is at high risk for ADR (elderly)?
<50 ml/min
523
how many comorbid disorders place elderly at risk for ADR?
>6
524
how many meds place elderly at risk for ADR?
>9 meds
525
how many daily doses place elderly at risk for ADR?
>12 daily doses
526
previous adverse drug effect place elderly at risk for what?
ADR
527
what does STOPP stand for?
screening tool of older persons' potentially inappropriate
528
what does START stand for?
screening tool to alert doctors to right reatment
529
what is the BBB a barrier to?
drug distribution
530
what blocks many types of drugs from getting into or getting access to the brain?
BBB
531
what other three things does BBB block?
toxins, pathogens (viruses and bacteria), some inflammatory cells
532
what provides protection for the CNS?
BBB
533
what does the BBB help transport? (two things)
nutrients and oxygen
534
what does the BBB help get rid of? (two things)
metabolites and waste products (from cellular function within the brain)
535
what two types of drugs are able to cross the BBB?
highly lipid soluble and non-ionized
536
what does the fetal placental barrier operate by?
simple diffusion
537
what must drugs be to cross fetal placental barrier?
lipid soluble
538
is the fetal placental barrier a perfect barrier?
no
539
why is the fetal placental barrier not perfect?
many substances a mother takes into her body will reach the fetus
540
what three things does fetal placental barrier help transport to fetus?
nutrients, oxygen, fluids
541
what two things does fetal placental barrier remove?
waste and CO2
542
does fetal placental barrier protect against infection?
yes
543
what does IV med administration take effect?
immediate
544
does IV administration bypass first pass?
yes
545
does IM bypass first pass?
yes
546
does SQ bypass first pass?
yes
547
which is faster- SL or PO?
SL
548
can SL bypass first pass?
yes
549
does topical admin produce systemic absorption?
yes
550
is inhalation systemic?
yes
551
what isoenzyme? Convert a drug that is less lipid soluble to more water soluble to be excreted
CYP450
552
where is CYP450 located?
liver
553
what phase of biotransformation? Oxidation metabolites are still able to act in the body (bioactive)
phase 1
554
what phase of biotransformation? Conjugation of the drug molecule metabolites are not able to act in the body are water soluble
phase 2
555
if two drugs are metabolized by the same metabolic pathway they will what?
compete for the site of metabolism
556
term? Adverse effects that appear unpredictably
idiosyncratic ADRs
557
which hypersensitivity? Results from production of IgE after exposure to an antigen (most severe)
type 1
558
which hypersensitivity? Allergic reaction provoked by re-exposure to a specific type of antigen referred to as allergen
type 1
559
which hypersensitivity? Urticaria, wheezing, rhinitis, anaphylaxis
type 1
560
which hypersensitivity? Occurs when drug binds to cells and is recognized by an antibody
type 2
561
which two antibodies are involved in type 2 hypersensitivity?
IgG and IgM
562
which hypersensitivity? Complement and cytotoxic T cells are activated
type 2
563
which hypersensitivity is rare?
type 2
564
which hypersensitivity? ABO blood incompatibility
type 2
565
which hypersensitivity? Occurs when antibodies (IgG and IgM) are formed against soluble antigens
type 3
566
which hypersensitivity? Antigen-antibody complexes are deposited in tissues like joints and lungs
type 3
567
which hypersensitivity? Reaction takes hours, days, or weeks to develop
type 3
568
which hypersensitivity? Causes serum sickness
type 3
569
which hypersensitivity? Ceclor
type 3
570
what antibodies are involved in type 3 hypersensitivity?
IgG and IgM
571
which hypersensitivity? Cytotoxic t cells are activated, cell mediated
type 4
572
which hypersensitivity? Poison ivy and latex
type 4
573
which hypersensitivity? Contact dermatitis
type 4
574
which hypersensitivity? Repeated exposure to drugs causes a cytokine storm
type 4
575
which hypersensitivity? Delayed-type hypersensitivity
type 4
576
which hypersensitivity? Rash
type 4
577
term? Drugs dissolve and cross the cell membrane following concentration gradient
passive diffusion
578
term? Moving passively with no energy required from a higher to lower concentration area until equilibrium achieved
passive diffusion
579
passive diffusion moves from an area of WHAT to WHAT concentration?
higher to lower
580
what type of molecules move by passive diffusion?
small, mainly lipid soluble, uncharged
581
small or large molecules- passive diffusion?
small
582
charged or uncharged molecules- passive diffusion?
uncharged
583
ionized or unionized- passive diffusion?
unionized
584
stomach- acidic or basic?
acidic
585
intestine- acidic or basic?
basic
586
term? Moves against concentration gradient; requires energy
active transport
587
another term for active transport?
carrier mediated transport
588
carrier mediated transport is another term for what?
active transport
589
term? Involves specific membrane transport proteins that carrier the drug across the membrane
active transport
590
what carries drugs across the membrane in active transport?
specific membrane transport proteins
591
does active transport cross entire cell membrane?
yes
592
does active transport require energy?
yes
593
most drugs are weak WHATs or WHATs?
acids or bases
594
term? Characteristic of a drug- the ph at which half the molecules are ionized and the other half is unionized
pka
595
henderson-hasselbach equation is involved with what?
pka
596
the ionization of drugs may markedly reduce their ability to what?
permeate membranes
597
what two factors determine degree of ionization of drugs?
ph and pka
598
drus that are weak WHAT are uncharged in an acidic environment?
weak acids
599
drugs that are WHAT are uncharged in a basic environment?
basic
600
term? Transfer of a drug from its site of administration to the blood stream
absorption
601
most absorption occurs through what?
passive diffusion
602
what favors charged species?
solubility
603
solubility favors what?
charged species
604
permeability favors what?
neutral species
605
some molecules have what two things to facilitate movement from the lumen into circulation?
exchange proteins and channels
606
what is the fastest route of absorption?
inhalation
607
the GIT is lined with what?
epithelial cells
608
drugs must permeate through what cells to be absorbed into the circulatory system?
GI epithelial cells
609
does IV medication need absorption?
no- direct to circulation
610
which has greater predictability of absorption? IM/SQ or PO
IM/SQ
611
what is drug property is reduced by liver metabolism of drugs?
bioavilability
612
term? Before the drug reaches the systemic circulation significant portion of the drug can be metabolized by the liver
first pass
613
first pass causes what to be decreased?
concentration of drug in systemic circulation
614
what is the pathway of first pass?
portal vein
615
does rectal route bypass FPE?
yes
616
does buccal route bypass FPE?
yes
617
does SL route bypass FPE?
yes
618
term? A measure of an amount of administered dose of a drug that actually reaches the systemic circulation in unchanged form
bioavilability
619
what is the bioavailability of IV administration?
1
620
why is oral drug bioavailability lower?
incomplete absorption; first pass metabolism
621
term? Passage of a drug from the circulation to the tissue and its site of action
distribution
622
what are the six factors that affect drug distribution?
(1) lipid solubility (2) drug ph (pka) (3) blood flow to tissues (4) plasma protein binding (5) specialized barriers (6) disease state
623
what are these? (1) lipid solubility (2) drug ph (pka) (3) blood flow to tissues (4) plasma protein binding (5) specialized barriers (6) disease state
factors that affect distribution
624
term? Hypothetical volume of fluid into which the drug is distributed
volume of distribution
625
what are the functional water compartments in the body?
intracellular fluid, extracellular fluid, plasma, interstitial volume ?
626
what is the only form of a drug that is pharmacologically active?
free/unbound drug
627
what is the only form of a drug able to cross membranes?
free/unbound drug
628
what happens when a drug travels through the body and comes in contaact with a protein?
can remain free or bind to the protein
629
the portion of a drug that is bound to a protein is what?
inactive
630
the portion of a drug that is not bound to a protein is what?
active (free)
631
a drug is said to be highly protein-bound if more than what percent of the drug is bound to protein?
0.8
632
what is the primary serum protein responsible for drug binding?
albumin
633
albumin has a strong affininty for what?
weak acids
634
drugs that are minimally bound to protein penetrate the tissue BETTER/WORSE than drugs who are highly bound?
better
635
drugs that are minimally bound to protein are excreted FASTER/SLOWER?
faster
636
if drugs are bound to protein they stay in the plasma to get where they need to go but cannot bind to receptor until WHAT?
unbound
637
low albumin= more WHAT?
free drug
638
low albumin = more/less free drug?
more
639
low albumin= more free drug= more what?
adverse effects
640
two drugs that are highly protein bound do what?
compete
641
when two highly protein bound drugs compete what happens?
can cause increase concentration of the free drug
642
example of highly protein bound competing and increasing free drug concentration?
aspirin and sulfa
643
to penetrate the CNS, drugs need to penetrate what?
BBB
644
what kind of drugs penetrate the BBB?
only highly lipid-soluble ionized drugs are going to penetrate
645
term? Highly selectively permeable barrier that separates the circulating blood from the brain and extracellular fluid on the CNS
BBB
646
what kind of cells form the BBB?
brain endothelial cells
647
what connects brain endothelial cells in BBB?
tight junctions
648
in BBB- brain endothelial cells are connected by tight junctions with extremely high what?
electrical resistivity
649
water, some gases, lipid soluble molecules move across BBB by what process?
passive diffusion
650
BBB allows passage of what three things by passive diffusion?
water, some gases, lipid soluble molecules
651
glucose and amino acids, crucial to neuro function, move across BBB by what?
selective transport molecules
652
is the placental membrane a complete barrier?
no (incomplete barrier)
653
how do molecules move across placental membrane?
simple diffusion
654
what type of molecules move across placental membrane?
lipid soluble
655
term? Impedes certain molecules although allows most fat soluble chemicals to cross
placental membrane
656
what are the two properties of drugs that tend to make it unlikely to cross placental membrane?
drugs that are more water soluble and have a higher molecular weight
657
drugs that are more water soluble and have a higher molecular weight DO/DO NOT as readily cross placental membrane?
do not
658
if a drug binds to a large molecule like blood protein/albumin it is MORE/LESS likely to contact fetus?
less likely
659
term? Lipid bilayer, semipermeable
cell membrane
660
pure lipid bilayers are generally permeable only to what?
small and uncharged solutes
661
ionic molecules are charged/uncharged?
charged
662
whether or not a molecule is ionized will affect its what?
absorption
663
term? Irreversible biochemical transformation of drug into metabolites to increase excretion from body via kidney
metabolism
664
where does metabolism mainly occur?
liver
665
metabolites are usually more or less ionized?
more ionized
666
metabolites are usually more or less lipid soluble?
less lipid soluble
667
why are metabolites not absorbed by renal tubule?
less lipid soluble
668
non-synthetic reactions, which phase of metabolism?
phase 1
669
oxidation- which phase of metabolism?
phase 1
670
what is the most important metabolizing reaction?
oxidation
671
term? Adds oxygen or a charged radical/involves cytochrome P450 isoenzymes
oxidation
672
reduction- which phase of metabolism?
phase 1
673
hydrolysis- which phase of metabolism?
phase 1
674
metabolite may be active or inactive- which phase of metabolism?
phase 1
675
metabolies are only inactive- which phase of metabolism?
phase 2
676
synthetic reactions- which phase of metabolism?
phase 2
677
glucuronidation- which phase of metabolism?
phase 2
678
what enzyme- convert drugs to more water soluble forms?
CYP450
679
what enzyme? The major enzymes involved in drug metabolism
CYP450
680
what percentage of total metabolism does CYP450 account for?
0.75
681
grapefruit is an inducer or inhibitor of CYP450?
inhibitor
682
grapefruit will increase/decrease metabolism of drugs?
decrease
683
where is CYP450 primarily located within liver cells?
endoplasmic reticulum
684
aside from liver, what other organs house CYP450?
kidney and intestine
685
what are the 3 CYP enzymes that carry out largest number (50%) of biotransformation?
3A, 4, and 5
686
term? Some drugs can induce or stimulate the production of one or more isoforms of the enzymes to increase drug metabolism or decrease amount of one of the drugs
enzyme induction
687
what is the result of enzyme induction?
decrease the therapeutic effect of one of the other drugs because the enzymes have been induced
688
term? Drugs will inhibit the production of CYP enzymes and decrease drug metabolism to the effect is increased plasma concentration of concurrently used drugs
enzyme inhibition
689
enzyme inhibition- what kind of interaction?
drug to drug interaction
690
interacting CYP enzymes equates to what?
enzyme inhibition
691
five factors that affect metabolism?
age (small kids, elderly), genetics, gender, diet and environmental factors, disease state
692
acetylation is involving what metabolism factor?
genetics
693
term? Elimination of drugs from the body unchanged or as a metabolite
excretion
694
what is the most common organ of elimination?
kidney
695
via what route does elimination occur?
urine
696
what is the primary organ of excretion?
kidney
697
term? To produce drug metabolites that are more water soluble and more easily removed by the kidneys
excretion
698
what lab used to monitor renal function in the clinical setting?
serum creatinine
699
variability of excretion lies in the WHAT of the patient?
renal function
700
patients with poor renal function have LOWER/HIGHER levels of drugs secondary to decreased excretion of metabolites?
higher
701
what is the hepatic route of excretion?
bile
702
what is the mechanism of lung excretion?
exhalation
703
does excretion occur via breast milk?
yes
704
does excretion occur via skin?
yes
705
what type of compounds can be easily excreted?
hydrophilic compounds
706
why are hydrophilic compounds easily excreted?
body keeps from being reabsorbed
707
what is the most common method of excretion?
renal excretion
708
are protein bound drugs filtered in excretion?
no
709
what is normal GFR?
120
710
what two things does GFR depend on?
plasma protein binding and renal blood flow
711
process? Transported by liver cells from blood to bile then enter GIT and excreted through feces
biliary excretion
712
enterohepatic reabsorption is part of what type of excretion?
biliary excretion
713
term? Action of a drug on the body
pharmacodynamics
714
what receptors do ligand-gated ion channels act on?
cholinergic nicotinic
715
cholinergic nicotinic receptors interact with what channels?
ligand gated ion channels
716
what receptors do g-protein-coupled receptors act on?
alpha and beta adrenoreceptors
717
alpha and beta adrenoreceptors act on what receptor?
g protein coupled receptor
718
what receptors interact with enzyme-linked receptors?
insulin receptors
719
insulin receptors interact with what receptors?
enzyme-linked receptors
720
intracellular receptors interact with what receptors?
steroid receptors
721
steroid receptors interact with what receptors?
intracellular receptors
722
term? The ability of the drug to bind to the receptor
affinity
723
term? How well a drug binds to its receptor
affinity
724
definition of affinity?
the ability of a drug to bind to the receptor (how well)
725
term? The ability of a drug to produce a pharmacological response once the drug attaches to the receptor
efficacy
726
another term for efficacy?
intrinsic activity
727
definition of efficacy?
ability of the drug to produce a pharmacological response once the drug attaches to the receptor
728
alternative definition of efficacy?
how well the drug works to exert its therapeutic effect
729
term? How well a drug exerts its therapeutic effect
efficacy
730
term? Drug that has affinity plus intrinsic activity
agonist
731
term? Binds to a receptor and produces a pharmacological response
agonist
732
term? Binds to receptor and will do something
agonist
733
term? Possess some intrinsic activity, but less than a full agonist
partial agonist
734
term? Measure of drug activity expressed in terms of the amount required to produce an effect
potency
735
term? Amount of drug required to produce an effect of given intensity
potency
736
term? The point in time on the drug concentration curve that indicates the first sign of therapeutic effect
onset of action
737
onset of action, definition?
the point in time on the drug concentration curve that indicates the first sign of therapeutic effect
738
first sign of therapeutic effect? Term?
onset of action
739
term? The point in time on the drug concentration curve that indicates the max therapeutic effect
peak action
740
peak action- definition?
maximal effect in the body
741
term? The length of time the drug shows any effect in the body
duration of action
742
term? Time between onset of action and metabolism of the drug
duration of action
743
term? Amount of drug needed in the body remains constant (five half lives)
steady state
744
how long is the steady state?
five half lives
745
term? The amount of drug going into the body is the amount of drug being eliminated
steady state
746
what is used to determine if a drug is in therapeuti range?
peak and trough
747
what is used to decide dosing schedule?
half life
748
term? The length of time for the concentration of the drug to decrease to half its starting concentration
half life
749
What is the term? What the drug does/action on the body
pharmacodynamics
750
What is the term? What the body does to the drug
pharmacokinetics
751
What is the term? Factors that affect prescribing- include bioavailability
pharmacokinetics
752
Term? Think Absorption, Distribution, Metabolism, Excretion
pharmacokinetics
753
ADME
Absorption, distribution, metabolism, excretion (pharmacokinetics)
754
Description of which route of absorption? Convenient, takes longer to reach blood stream, may be destroyed by stomach acid
oral
755
which route of absorption? May be destroyed by stomach acid
oral
756
Another term for IV administration route?
parenteral
757
which route of absorption? Faster than oral, more readily absorbed, avoids 1st pass effect
sublingual
758
route of absorption that avoids 1st pass effect?
sublingual
759
which route (absorption) faster than oral, absorbs directly through mucous membranes into blood stream?
rectal
760
which route (absorption) can be fast, like IV, but also unreliable?
inhalation
761
which route (absorption) must undergo absorption through injection site?
IM/SQ
762
which route (absorption), drugs cannot create action if they are not distributed in adequate concentrations?
IM/SQ
763
term? Creates equal amounts of un-iodized drug on both sides of the membrane, works best for small unbound, uncharged drugs?
passive diffusion
764
term? Creates equal amounts of un-iodized drug on both sides of the membrane
passive diffusion
765
passive diffusion works best on what drugs?
small, unbound, uncharged drugs
766
what works best on small, unbound, uncharged drugs?
passive diffusion
767
define plasma protein binding
drugs may compete for protein binring sites
768
two examples od drugs re: plasma protein binding?
coumadin, bactrim
769
hypoalbuminemia leads to what?
more free (unbound drug) in the blood stream
770
hypoalbuminemia leads to increased risk of what?
toxic effect
771
why does hypoalbuminemia have increased risk for toxic effect?
drug hanging in the bloodstream and not doing anything productive, less drug available to work in target tissues
772
term? Process in which drugs are transferred from inside the body to outside the body
excretion
773
what age group has less ability to excrete?
older adults
774
why do older adults have less ability to excrete?
decreased kidney function
775
slower excretion increases potential for what?
toxicity
776
what is the likely route of excretion of a volatile drug?
likely the lungs
777
where does excretion primarily take place?
kidneys
778
aside from kidneys, where are the three organs excretion also occurs?
liver, lungs, skin
779
what type of reaction is CYP 450?
oxidative
780
what can cause variation in CYP 450?
genetics
781
what drug? A nonspecific CYP 450 inducer that can induce the metabolism of drugs, like oral contraceptives, leading to therapeutic failure
rifampin
782
what type of drug is rifampin?
nonspecific CYP 450 inducer
783
what does rifampin induce?
metabolism of drugs
784
what enzyme? Drugs may compete for this enzyme, meaning one will not be metabolized?
CYP34A
785
term? Drug cannot be metabolized by enzymes properly; block or slow the enzyme
inhibitor
786
what does an inhibitor do?
block or slow the enzyme
787
what does an inducer do?
stimulate the enzyme
788
ter? Drug is metabolized too fast- make enzymes work better
inducer
789
what hormone? Decreases gastric tone and prolongs stomach emptying
progesterone
790
what are two effects of progesterone in pregnancy?
decreases gastric tone and prolongs stomach emptying
791
what special population? Hormones may occupy protein binding sites leading to more free drug in circulation
pregnancy
792
what kind of drugs pass through breast milk?
highly lipid soluble, low protein binding drugs
793
is drug metabolism changed in pregnancy?
no
794
what special population? Peak serum concentrations lower and delayed
elderly
795
what happens to peak serum concentrations in elderly?
lower and delayed
796
gastric acid increased or decreased in elderly?
decreased
797
drug absorption increased or decreased in elderly?
decreased
798
body water increased or decreased in elderly?
decreased
799
distribution of hydrophilic drugs increased or decreased in elderly?
decreased
800
why is there reduced distribution in elderly?
less albumin, less body mass, less plasma protein
801
why is there increased unbound active drug in elderly?
802
why is there slow metabolism in elderly?
803
what two changes to liver happen in the elderly?
804
what changes to the kidney happen in the elderly?
805
renal tubular secretion increased or decreased in elderly?
806
kidney size increased or decreased in elderly?
807
number of functioning nephrons increased or decreased in elderly?
808
increased fat stores in elderly lead to what?
809
what effect do increased fat stores have on volume distribution in elderly?
810
what increases volume distribution of lipophilic drugs in elderly?
811
first pass effect is increased or decreased in elderly?
812
why is 1st pass effect increased in elderly?
813
role of DEA?
814
schedule of drugs with no medical use?
815
two examples of schedule 1 drugs?
816
heroin and LSD are examples of which drug schedule?
817
what drugs have high potential for abuse and dependence?
818
refills and telephone orders permitted with schedule 2?
819
vicodin, oxycontin, adderall- what schedule?
820
what schedule- moderate potential for abuse and dependence?
821
scripts rewritten after 6 months for 5 refills- what schedule?
822
tylenol with codeine- what schedule?
823
ketamine- what schedule?
824
steroids- what schedule?
825
testosterone- what schedule?
826
tylenol with codeine, ketamine, steroids, testosterone? What schedule
827
what schedule- drugs with low potential for abuse and dependence?
828
xanax, clonazepam, valium, ativan- what schedule?
829
what schedule- xanax?
830
what schedule- valium?
831
what schedule, tramadol?
832
what schedule clonazepam?
833
what schedule- ativan?
834
what schedule- same as all prescrtipion drugs over the counter?
835
robitussin AC- what schedule?
836
lomotil- what schedule?
837
Lyrica- what schedule?
838
robitussin AC, lomotil, lyrica- what schedule?
839
type 1 reaction is mediated by what?
840
immediate type hypersensitivity, which type?
841
anaphylaxis- which type?
842
antibody-dependent cytotoxicity- which type?
843
heparin-induced thrombocytopenia- which type?
844
graft rejection- which type?
845
immune complex hypersensitivity- which type?
846
arthus reaction to tetanus vaccine- which type?
847
lupus- which type?
848
describe type 3 reaction?
849
describe type 2 reaction?
850
what do agonists do?
851
term? Receptor site stimulation?
852
term? Block receptor site stimulation?
853
what do antagonists do?
854
what do antagonists block?
855
which system? Releases acetylcholine and counterbalances sympathetic activity
856
which system? ACH activates muscarinic and nicotinic receptors
857
what are the two cholinergic receptors?
858
what two receptors does ACH activate?
859
parasympathetic nervous system is part of which system?
860
constricts pupils- which system?
861
stimulates salivation- which system?
862
decreases heart rate- which system?
863
decreases contractility- which system?
864
left off on page 3
