Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

Pharmacology > ADME > Flashcards

ADME Flashcards

(96 cards)

Start Studying
1
Q

 A:
 D:
 M:
 E:

A

 Absorption
 Distribution
 Metabolism
 Excretion

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

 Absorption

A

How a drug moves from its site of
administration into the bloodstream

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

 Distribution

A

Movement of the drug between blood and
tissues

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

 Metabolism

A

Conversion of drugs into more hydrophilic
metabolites

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

 Excretion

A

Removal of drugs and/or metabolites from
the body

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

Features that predict
movement
(4)

A

 Molecular size
 Degree of ionization
 Lipid solubility
 Protein binding

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

Rule 1
 To pass through lipid membranes, drugs
have to be
 To be water soluble, drugs need to be

A

non-ionized (aka: uncharged)
ionized (aka: charged)

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

**Most drugs are either

A

weak acids or weak bases**

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

Weak acid
Occurs more in a — environment

A

basic

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

Weak base
Occurs more in a — environment

A

acidic

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

Remember: Acids are non-ionized (fat soluble)
when —, ionized (water soluble) when
—

A

protonated, deprotonated

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Bases are non-ionized when —,
ionized when —

A

deprotonated, protonated

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

The pKa is the pH at which

A

there are
equal amounts of protonated and
nonprotonated

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

 pH = pKa
 pH < pKa
 pH > pKa

A

Protonated equals non-
protonated
Protonated form predominates
Non-protonated form predominates

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

Only the — of a drug can
readily cross the lipid membrane

A

non-ionized form

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

Ratio of ionized and non-ionized
influences rate of —

A

absorption

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

Henderson-Hasselbalch equation

A

pH = pKa + log [Ionized]/[Non-ionized]

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

Ion Trapping

A

 Because ionized
molecules (drugs)
can’t cross the
membrane, can
effectively trap them
and enhance
excretion
 Principle is very
useful in toxicology

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

Acidic environments of abscesses will affect ionization state of

A

local anesthetics

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

Acidic environments of abscesses will affect ionization state of local anesthetics
(3)

A

 Local anesthetics = basic, high pKA
 Abscess = low(er) pH
 When a basic drug is in an acidic pH, the protonated and ionized form predominates

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

Absorption
(3)

A

 Movement of a drug from its site of administration into the central compartment
 Process of dissolution and diffusion
 Bioavailability more important

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

Bioavailability (F)
(3)

A

 Fraction of drug that reaches the systemic
circulation intact
 Bioavailability of IV = 100%
 Affected by route of administration

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

First Pass and Hepatic Extraction
(2)

A

 Hepatic extraction ratio
 First pass clearance

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

 Hepatic extraction ratio

A

 Fraction of drug in blood that is irreversibly
removed during one pass through the liver

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
 First pass clearance
 Extent to which a drug is removed by the liver during its first pass in the portal blood through the liver to systemic circulation
26
First Pass and Hepatic Extraction  Drugs with low hepatic extraction will have -- first pass clearance, and vice versa
low
27
First pass effect occurs due to metabolism by/in (4)
 Gut bacteria  Intestinal brush border enzymes  Portal blood  Liver enzymes
28
Hepatic Extraction  Low extraction (2)
 Low first pass clearance  Change in hepatic enzymes won’t have significant effect on first pass clearance
29
High extraction (2)
 Hight first pass clearance  Changes in enzyme function will have large effect on first pass effect
30
Enteral administration ADVANTAGES (4)
 Most common route  Safest  Easiest  Most economical
31
Enteral administration DISADVANTAGES (5)
 Limited absorption  Emetogenic potential  Subject to first pass  Absorption may be affected by food or other drugs  Irregularities in absorption or propulsion
32
Parenteral Administration ADVANTAGES (4)
 Not subject to first pass  Most rapid onset  Ability to titrate  Doesn’t require cooperation
33
Parenteral Administration DISADVANTAGES (4)
 Greater patient discomfort  Requires additional training to administer  Concern for bacterial contamination  Injection-associated risks
34
Injection-associated risks (3)
 Extravasation  Intra-arterial injection  Limb loss
35
Oral Administration  Absorption governed by: (5)
 Surface area for absorption  Blood flow to site of absorption  Dosage form administered  Ionization status (lipo- vs. hydrophilic)  Concentration at site of absorption
36
Oral Administration  Enteric coating (2)
 Drugs destroyed by gastric secretions, low pH, or that cause gastric irritation  Risk of bezoar formation
37
Oral Administration --- Release
Delayed
38
►Intravenous (IV): F = 100% (2)
● Immediate onset, Bypasses GI absorption ● Best for emergencies
39
Intramuscular (IM): 75-100% (3)
● Irritating drugs given this route ● Not as rapid response as IV ● Depot preparations (sustained release) ie., suspensions, ethylene glycol, peanut oil- all slow down absorption.
40
►Subcutaneous (SQ): 75-100% (3)
● Slower absorption than IV or IM ● Little risk of intravascular injection ● Examples: Insulin, Mechanical pumps, heparin (DVT prophylaxis)
41
► Intradermal (ID): (2)
● Small amounts of drug ● Tuberculosis skin test, Local anesthetics
42
► Inhalation: 5-100% (3)
● Almost as rapid as IV. (Method of abuse) ● Delivered directly to lung (good selectivity)- minimal systemic side-effects. ● Gases, aerosols of solutions & powders -good for respiratory conditions.
43
► Intranasal: 5-100% (2)
● Vasopressin for tx of diabetes insipidus, calcitonin (osteoporosis). ● Method of drug abuse.
44
►Intrathecal/Epidural: (1)
● Subarachnoid space of spinal cord – into CSF (Lumbar puncture- Baclofen in MS, regional anesthetic in delivery, morphine drip)
45
►Topical: Skin, oral mucosa, sublingual, rectal (avoids 50% of 1st pass metab) ((3)
● When local effect is desired-but can provide systemic effects. ● Sublingual (100%), rectal (50%) bypasses liver- good bioavailability. ● Transdermal Controlled Release- Scopolamine, nitroglycerin, nicotine, estrogens (BCP), fentanyl.
46
►Subgingival:
Perio specific uses: doxycycline(Atridox); minocycline(Arestin)
47
Distribution  The administered drug leaves the blood stream and enters other “compartments”  Dependent upon: (3)
 Cardiac output  Capillary permeability  Blood flow
48
Kidney: -- mL/min/100gm Liver: -- mL/min/100gm Heart: -- mL/min/100gm Brain: -- mL/min/100gm
360 95 70 55
49
 Central
 Well perfused organs and tissues (heart, blood, liver, brain, kidney). Drug equilibrates rapidly.
50
 Peripheral
 Less well perfused organs/tissues (adipose, skeletal muscle, etc.)
51
 Special compartments
 CSF, CNS, pericardial fluid, bronchial secretions, middle ear
52
Protein binding  Albumin –  α-glycoprotein –
acidic drugs basic
53
SKIPPED Distribution (5)
 Protein binding  Free vs. bound  Competition  Disease impact  Drug levels
54
Distribution  Accumulation in tissue (4)
 Organs  Muscle  Adipose  Bone
55
Distribution  Redistribution (2)
 From site of action into other tissues or sites  E.g. propofol
56
CNS (3)
 Blood brain barrier  Efflux transporters  Inflammatory processes
57
SKIPPED  Blood brain barrier (2)
 Lipid solubility  Clinical effects
58
Volume of Distribution (Vd) (2)
 Volume of fluid in which a drug would need to be dissolved to have the same concentration in plasma. Doesn’t represent “real” volume  Relationship between dose and resulting Cp
59
 Lipophilic drugs tend to have a -- Vd  Protein bound drugs have --- Vd
larger lower
60
Drugs with a Vd of:  < 5L:  5-15L:  > 42L:
Confined to plasma Distributed to extracellular fluid (RBCs + plasma) Distributed to all tissues in the body, especially adipose
61
 increase Vd =
increase likelihood that drug is in the tissue
62
increase Vd =
decrease likelihood that drug is confined to the circulatory system
63
Metabolism  Removal (2)
 Either metabolized/biotransformed and eliminated or excreted unchanged  Must be water-soluble to be removed
64
Lipid solubility good for --- and ---, bad for ---
absorption, distribution excretion
65
Metabolism  Process of biotransformation (2)
 Converts drugs into polar metabolites  Lipophilic into hydrophilic
66
Liver does the heavy lifting
 P-450
67
Cytochrome P-450 system (2)
 70+ forms  Liver, kidney, intestines
68
Metabolism – Phase I (4)
 Catabolic  Exposes functional group on parent compound  Usually results in loss of pharmacologic activity  Activation of prodrugs
69
Metabolism and P450 Interaction (3)
 Substrates  Inhibitors  Inducers
70
Genetic Polymorphisms
 Genetic variability in function of CYP isoenzymes
71
Genetic variability in function of CYP isoenzymes May be poor metabolizers (PM) or rapid metabolizers (RM), leading to: (2)
 Subtherapeutic effect: CYP2D6 PM – codeine, tramadol  Toxicity: CYP3A4 – diazepam, alprazolam (insufficient activity in some Asian populations)
72
Phase II (3)
 Occurs after functional groups are exposed  Anabolic: adds water soluble molecules to structure  Much less interpatient variability
73
Phase II  Major reactions (4)
 Glucuronidation  Glutathione conjugation  Sulfate conjugation  Acetylation
74
Excretion (3)
 Removal of unchanged drug  Kidney, lung, feces – primary routes  Polar compounds > lipid soluble compounds
75
Excretion kidney  3 processes (3)
 Glomerular filtration  Active tubular secretion  Passive tubular reabsorption
76
Excretion- kidney  Dependent upon  Only --- drug filtered  Non-ionized weak acids and bases  Alkaline urine “traps”
renal function unbound passively reabsorbed ionized, acidic molecules, increases excretion
77
Excretion- lungs (2)
 Primarily inhaled anesthesia or volatile liquid  Affected by respiratory rate and blood flow
78
Excretion- feces  Unabsorbed  Metabolites excreted in the  Un-reabsorbed metabolites secreted into the
orally administered meds bile intestinal tract
79
 Drugs have to cross
lipid membranes, can do this by passive (with the concentration gradient) or active (against the gradient) transport
80
 --- is main factor that determines rate of passive transport
Lipid solubility
81
 Only --- drugs can diffuse across lipid membrane
uncharged
82
 Partition –
acids get trapped in basic environments, vice versa
83
 --- most prominent re: protein binding; binds acidic drugs (~2 molecules/albumin)
Albumin
84
 Extensive protein binding can slow drug --
elimination
85
 Competition for protein binding can sometimes lead to ---
interactions
86
 Drugs with low --- are not well absorbed from the gut
lipid solubility
87
Gut absorption depends on factors such as: (4)
GI motility, GI pH, particle size, interaction w/ gut contents
88
 --- is fraction of dose that makes it to systemic circulation to elicit an effect
Bioavailability (F)
89
 Phase I reactions are
catabolic; involves oxidation, reduction, and hydrolysis
90
 Phase I prepares the drug for Phase II, can result in more active products; often involves
P450 system
91
 Phase II reactions are
anabolic, conjugated, leaving inactive and polar product for excretion
92
 --- induction and inhibition are hugely important concepts regarding drug interaction
P450
93
 Unless they’re protein bound, most drugs are filtered through the ---
glomerulus
94
 Weak acids and bases are actively secreted into the
renal tubule
95
 Lipid soluble drugs are
passively reabsorbed, not efficiently excreted
96
 Can use pH partition concept to facilitate
excretion of certain drugs

Pharmacology (13 decks)

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