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FMS week #4 Flashcards

(92 cards)

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1
Q

Which routes of drug administration might have 1st pass metabolism

A

oral, rectal, sublingual

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2
Q

Route of drug administration with most rapid onset of action

A

IV

also 100% bioavailable

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3
Q

What are pros and cons of intrathecal drug administration

A

bypass blood-CSF & blood-brain barriers

risks of infection & headache

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4
Q

bioavailability is influenced by (3 categories)

A

physiological, physiochemical, and biopharmaceutical factors

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5
Q

Fick’s law determines

A

Rate of diffusion

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6
Q

When pH

A

protonated form (HA and BH+)

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7
Q

When pH>pKa, ______ form predominate

A

unprotonated (A- and B)

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8
Q

What is the partition coefficient?

A

states how soluble a drug is in a lipid membrane

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9
Q

ABC family of transporters

A

ATP-Binding Cassettes. family of transporters (ie. P-glycoproteins - oppose drugs from entering cells)

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10
Q

4 physiological factors that affect GI absorption

A
  1. Surface area
  2. GI pH
  3. GI motility/gastric emptying]
  4. Blood flow
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11
Q

Where is the primary site of biotransformation

A

liver

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12
Q

Microsomal hepatic sites of drug metabolism

A

vesicles rich in smooth ER; contain enzymes that catalyze oxidation reactions and glucorinide conjugation

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13
Q

Non-microsomal hepatic sites of drug metabolism

A

occurs mostly in cytosol; some enzymes display important genetic polymorphisms

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14
Q

Enterohepatic cycling

A

when drugs are excreted into the gut via bile and are reabsorbed

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15
Q

Only (bound/unbound) drugs in plasma can penetrate cell membranes

A

unbound

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16
Q

What type of drugs tend to bind to albumin

A

neutral acid & base

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17
Q

Basic drugs commonly bind to:

A

globulins

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18
Q

What are 2 physiochemical characteristics of drugs affected distribution?

A

pKa & partition coefficient

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19
Q

What are 2 cardiovascular factors that affect drug distribution?

A

cardiac output & regional blood flow

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20
Q

What are some tissue-dependent factors that affect drug distribution?

A

pH gradient, active transport, non-specific binding, dissolution in fat, drug reservoirs

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21
Q

Why is drug distribution different across the blood brain barrier?

A

a. CNA capillaries are not fenestrated
b. tight junctions & basal lamina of cerrebal endothelial cells resist the movement of water-soluble and ionized drugs into CNS
c. brain capillary endothelial cells express ATP-driven drug efflux pumps
d. CSF proteins do not function as drug reservoir

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22
Q

Why is drug distribution different across the placenta?

A

distribution by simple simple diffusion; nutrients & drugs of abuse readily cross placenta

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23
Q

Elimination is ______ related to stead state concentration in blood

A

inversely

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24
Q

Volume of distribution

A

the volume of fluid that would be needed to contain the administered amount of drug at the concentration measured in blood or plasma

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25
Volume of distribution is _____ proportional to the concentration of the drug measured in the blood
inversely
26
Volume of distribution is _____ proportional to the total amount of drug administered
directly
27
What is first-pass metabolism?
biotransformation of a drug prior to its entry into the systemic circulation (usually to a less active compound) usually in liver, sometimes SI
28
What occurs in Phase I metabolism?
introduce/unmask a polar functional group
29
Mixed Function Oxidases (MFOs) are found in Phase I/II?
Phase I
30
Cytochrome P450 is found in Phase I/II?
Phase I
31
Glucuronidation reactions occur in Phase I/II?
Phase II
32
What occurs in Phase II metabolism?
conjugation and synthetic reactions; addition of an acid or amino acid; glucuronidation
33
How does inhibition modify metabolism of drug
competitive inhibition
34
How does induction modify metabolism of drug?
either increases synthesis or blocks breakdown
35
How do hepatitis, cirrhosis, liver cancer affect drug metabolism?
They impair microsomal oxidases
36
How does cardiac dysfunction affect drug metabolism?
leads to reduced hepatic blood flow, which affects metabolism of drugs that are flow-limited
37
As renal function decreases, plasma 1/2-life ______
increases
38
Therapeutic window is
the range of concentrations between the therapeutic concentration and the toxic concentration
39
In a first order reaction, rate of metabolism is _____ proportional to concentration
directly
40
First order reactions generally occur when relatively low/high substrates
low
41
How are first order reactions eliminated?
at a fixed percentage per time
42
Zero order reactions occur when drug concentration is relatively low/high
high
43
How are zero-order reactions eliminated?
at a fixed amount/time
44
How do calculate maintenance dose? (not the actual equation detials)
loading dose - amount that's been eliminated
45
elimination 1/2-life is (dependent/independent) of dose/concentration?
independent
46
1/2-life is ______ proportional to clearance
inversely
47
1/2-life is ______ proportional to Vd/Cl,
directly
48
decreased hepatic/renal function will increase/decrease rate of elimination
decrease
49
Concentration of drug present is ____ related to volume of distribution in an IV administration
inversely
50
dose, dosage interval, and 1/2-life determine
Drug plateau level
51
T/F dose determines time it takes to reach plateau
FALSE
52
Define agonist
a drug that mimics the effects of the endogenous ligand for a receptor
53
A full agonist has an intrinsic value of _
1
54
A _____ agonist cannot elicit the maximum response of tissue
partial
55
What is an inverse agonist
it causes inhibtion of agonist-independent activity; long term treatment with inverse agonists may lead to receptor up-regulation
56
A drug (which does not itself have intrinsic activity) that interferes with binding of endogenous ligand (or an agonist) to a receptor
antagonist
57
Antagonists have an intrinsic activity of _
0
58
What does a competitive antagonist do?
binds to same site so agonist cannot bind changes Kd but NOT maximum response
59
What does a noncompetitive antagonist do?
binds to non-binding site but makes it so agonist cannot bind decreased maximum response, but Kd stays the same
60
Affinity is determined by
interacting sites and types of forces involved in binding interactions
61
Kd is the?
concentration of drug when 1/2 total # receptors are bound b drug
62
Lower molar concentration value of Kd, the higher/lower affinity for the receptor
higher
63
ability of a receptor to elicit a response without outside factors
intrinsic activity
64
strongest
correct
65
Receptor down-regulation occurs in hours-days or secs-mins?
hours-days
66
Receptor _________ involves receptor phosphorylation
desensitization
67
receptor desensitization _____ affinity and ____ # receptors
decreases and does not change
68
in sigmoid concentration curves, drugs with higher affinity are shifted to the left/right
left
69
T/F a partial agonist will reach the maximum response
F
70
T/F a competitive antagonist will change the Kd
F; will change Kd though
71
T/F noncompetitive antagonist will change the Kd
F; will decrease maximum response though
72
The influence of genetic variability on drug responses (both therapeutic and toxic drug responses)
pharmacogenetics
73
the use of genetic information to predict drug responses
pharmacogenomics
74
Which Cytochrome P450 is involved in metabolism of 20-25% of all meds?
2D6
75
Described poor metabolizers
PM's have deceased metabolism & clearance, increased elimination 1/2-life will get higher drug plasma levels, increased risk fo drug-related side effects need reduced drug dose
76
Describe intermediate metabolizers
might need slightly lower dose
77
describe intermediate metablizors
Usually ok with standard dose of drug
78
Describe ultrarapid metabolizers
Have increased metabolism & clearance; decreased elimination 1/2-life have low plasma drug levels, risk losing drug efficacy Need a higher dose
79
What is Tamoxifen?
Pro-drug that treats Estrogen positive tumors Converted to Endoxifen via CYP2D6 & CYP3A4/5 PM's have reduced drug efficacy of tamoxifen bc can't convert as well to endoxifen
80
codeine is a pro-drug for ______ via which CYP?
morphine;n 2D6
81
Normally, __% of administered codeine gets converted to morphine
5-10%
82
UM's are at an increased/decreased risk for drowsiness and respiratory depression
increased
83
What is Isoniazid?
drug used in TB treatment
84
How is Isonizid metabolized?
via N-Acetyletransferase (NAT) [phase II enzyme]
85
Slow/fast acetylators are more likely to suffer from isoniazid toxicity (ie. peripheral neuropathy)
slow
86
Thiopurine drugs are used for....
autoimmune conditions, acute, lymphoblastic anemia, preventing organ rejection
87
Which forms of thiopurine drugs have desired effect?
6-TGNs
88
Thiopurine drugs are inactivated by
TMPT
89
If TMPT activity too high, might have to...
give higher dose of thiopurine drugs
90
if individual has reduced undetectable TMPT activity, what will happen?
increased potential for life threatening adverse events (myelosuppression, bleeding, severe infection)
91
Why is G6PD important?
only source of NADPH and GSH in RBC's, which are necessary for reduction no reduction--> increased risk for hemolysis when exposed to oxidative stress
92
Why do you get hemolysis in those that are G6PD deficient?
products of rasburicase breakdown include allantoin and hydrogen peroxide, which the body cannot handle if no antioxidants such has NADPH and GSH around

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