Introduction to Pharmacology Flashcards

1
Q

[…] is what the BODY does to the drug

A

pharmacokinetics

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

[…] is what the DRUG does to the body

A

pharmacodynamics

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

What are the 4 parts of pharmacokinetics?

A

Absorption, distribution, metabolism, elimination

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

What are the 2 parts of pharmacodynamics?

A

Efficacy and Toxicity

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

[…] is the process by which a drug moves from site of administration to bloodstream

A

absorption

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

Absorption depends on physical characteristics of the drug such as what?

A

solubility, pKA, binders, formulation

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

[…] is the relative amount of drug that reaches systemic circulation

A

bioavailability

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

What is the bioavailability value for IV medications? Why

A

1, bypasses liver upon administration

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

What are examples of ways drugs can be administered?

A

Oral, sublingual, rectal, transdermal, subcutaneous, IM, IV, Intrathecal, Epidural, Inhalational

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

The route a drug is administered affects its […]

A

absorption

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

[…] is a phenomenon of drug metabolism whereby concentration of the drug is greatly reduced before it reaches systemic circulation

A

first-pass metabolism

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

First-pass metabolism can be attributed to the […] and […] clearance

A

liver , gut wall

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

Which route of administration can bypass the LIVER on the first pass?

A

IV

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

Which drug is more readily absorbed: non-ionized or ionized?

A

Non-ionized since they are uncharged

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

What type of drugs will acidic environment favor during absorption? Example?

A

Acidic drugs, Stomach

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

What type of drugs will alkaline environments favor during absorption? Example?

A

Basic drugs, intestines

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

Where are most oral drugs absorbed? Why?

A

Intestine, surface area and prolonged transit duration

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

Why would drugs absorbed from the stomach or intestine be reduced?

A

Venous drainage goes to liver first (first-pass)

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

Why are sublingual and buccal administration unique?

A

Bypass 1st pass metabolism

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

What does parenteral mean? Examples?

A

Outside of intestine (SQ, IM, IV)

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

[…] administration bypasses process of absorption

A

IV

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

[…] occurs after absorption when the circulation moves the drug throughout the body

A

Distribution

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

[…] defines the group of highly perfused organs

A

Vessel Rich Group (VRG)

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

What organs are in the Vessel Rich Group? (5)

A

Brain, Heart, Kidneys, Liver, Endocrine Glands

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
What percentage of cardiac output do vessel rich groups receive?
75%
26
What type of drugs will quickly equilibrate into CNS tissue?
Lipophilic
27
[...] will reach equilibrium quicker than other less perfused tissues
Vessel Rich Groups (VRG)
28
Fat & Skin can absorb [...] drugs which results in [...] reservoir of drug following long infusions
lipophilic, larger
29
What is the mass action law?
When plasma concentration exceeds tissue concentration, drug moves from plasma into tissue
30
What is redistribution?
Drug moves back due to plasma concentraiton being less than tissue concentration
31
What does drug concentration in an organ depend on?
Blood flow to organ, Solubility in organ vs solubility in blood
32
What can molecules in the blood be bound to when they aren't free?
Plasma proteins and lipids
33
What are 2 examples of plasma binding proteins? What can cause these to be diminished?
Albumin and Alpha Acid Glycoprotein (AAG); Kidney disease, Liver disease, CHF
34
Which induction agent is in lipid emulsion and acts as its own binding molecule?
Propofol
35
What molecules readily cross between blood and organs?
Lipophilic
36
What molecules can pass in SMALL quantities?
Charged
37
Blood Brain Barrier has limited penetration by [...] drugs due to pericapillary glial cells and endothelial cell tight junctions
ionized
38
Drugs that are able to cross BBB are readily taken up by what?
Body fat
39
When a drug is highly bound on tissues and unbound in plasma, where is it more likely to transfer to?
Tissues
40
When a drug is unbound in the tissue, it is more likely to transfer to [...]
plasma
41
What is albumins capacity and affinity like?
High capacity, low affinity
42
What type of drugs does albumin bind?
Weak acids and some bases
43
What is Alpha-1 Acid Glycoprotein capacity and affinity like?
High affinity, low capacity
44
What type of drugs are bound to alpha-1 glycoprotein?
Weak bases
45
What type of drugs are bound to lipoproteins?
Lipophilic drugs
46
When an IV bolus is given what will occur in terms of distribution?
Distribution from plasma to tissues (plasma concentration declines) and equilibrium occurs
47
When tissue concentration exceeds plasma concentration what will occur?
Redistribution
48
When we give prolonged infusions of a drug, what will be affected when the infusion is discontinued?
Redistribution (pro-long drug action)
49
[...] is the time required for a 50% decrease of drug plasma concentration following a steady state infusion
context sensitive half-time (context refers to time of infusion)
50
[...] is the apparent volume into which a drug has distrubted
Volume of distribution (Vd)
51
Volume of Distribution (Vd) equation:
Bolus Dose / [Blood Concentration] at certain time
52
If a drug has a low Vd, what does that mean?
Hydrophilic and largely in intravascular space
53
If a drug has a high Vd, what does that mean?
Lipophilic and easily cross and distribute throughout tissues
54
Metabolism can also be referred as [...]
biotransformation
55
[...] is the chemical process by which a drug molecule is altered in the body
Metabolism/Biotransformation
56
What organ is a major player in the metabolism process?
Liver
57
Where do esters undergo hydrolysis?
Plasma or tissue
58
Most products of metabolism are inactive and [...] making it easy to be excreted by the [...]
water soluble ; kidneys
59
How many phases of metabolism are there?
2
60
[...] of metabolism is the breakdown of the initial parent compound into more polar metabolites via oxidation, reduction, or hydrolysis
Phase 1
61
What enzyme catalyzes most phase 1 metabolism reactions?
Cytochrome P-450 (CYP 450)
62
What can cause CYP activity to increase?
Constant drug exposure
63
What can inhibit CYP activity?
Drugs competing for same CYP subtype
64
[...] metabolism reactions couple or conjugate parent or metabolite with endogenous subtrate to form water soluble product eliminated via stool or urine
Phase II
65
Can phase I products be excreted without undergoing phase II reaction?
Yes
66
Can phase II reactions occur without a phase I reaction?
Yes
67
Give an example of a metabolism polymorphism that exists:
pseudocholinesterase deficiency
68
[...] is the volume of blood or plasma cleared of drug per unit of time
Hepatic clearance
69
What is the fraction of drug removed by the liver called?
Extraction ratio
70
What is the equation for hepatic clearnace?
Hepatic Clearance = Liver Blood Flow x Extraction Ratio
71
What does a high extraction ratio mean?
Depends on CO - "Flow limited"
72
What does a low extraction ratio mean?
Capacity limited - can only handle a set amount at a time
73
What organ removes some drugs and many drug metabolites?
Kidney
74
[...] is the rate of elimination of a drug from the body by kidney excretion
Renal clearance
75
What is the renal clearance equation?
Renal Clearance = Renal Blood Flow x Renal Extraction Ratio
76
[...] portion is reabsorbed in the renal tubules and [...] portion is excreted in the urine. This is dependent upon [...]
Nonionized, Ionized, pH
77
Why do patients with decreased renal function need altered drug dosing?
Avoid accumulation of parent compounds and metabolite
78
Drugs can sometimes be excreted from liver to intestine via [...]
biliary system
79
[...] is the process in which metabolites excreted in bile are subsequently reversed and absorbed back into the parent drug
Enterohepatic recirculation
80
[...] is when a fixed percentage of an existing drug is removed per unit of time
First-order kinetics
81
In first order kinetics, the [...] removed depends on serum levels but the [...] removed is independent of serum levels
amount ; fraction
82
[...] describes a fixed amount of drug removed per unit of time
zero-order kinetics
83
[...] is the time required for serum concetration to decrease by 50%
half-life
84
Half life formula
Half life = ln2/K
85
[...] is the time required for the drug concentration in the body to fall by 50%
elimination half-life
86
What does the 2-compartment model consist of?
Central compartment (plasma + VRG) and peripheral compartment
87
What is the alpha phase of the two-compartment model?
Quick decline - distribution phase
88
What is the beta phase of the two-compartment model?
Slower decline - elimination phase
89
What does pharmodynaics involve concepts of?
Potency, efficacy, therpaeutic window
90
Exposure response relationships shows that as the body is exosed to increasing amount of drug the response to the drug can [...] up to a maximum value
increase
91
[...] dose required to produce a specific effect in 50% of the population
ED50 (effective dose)
92
[...] dose required to cause death or toxicity in 50% of the population
LD50 (lethal dose)
93
[...] is a safety measure or how much wiggle room you have before your desired outcome starts becoming harmful to the patient
Therapeutic index
94
Therapeutic index equation
LD50/ED50
95
[...] is the amount of drug needed to produce a given effect
potency
96
[...] refers to the relative ability of a drug-receptor complex to produce a maximum fuctional response
efficacy
97
[...] bind to a receptor and produce an effect
agonists
98
[...] binds to receptor but produces a lower maximal effect than a full agonist
partial agonist
99
[...] is diminished response to a drug due to chronic exposure
tolerance
100
[...] is an acute tolerance after only a few doses
tachyphylaxis
101
[...] bind to receptor without producing an effect
antagonists
102
[...] bind reversibly to the same binding site as the agonist
competitive antagonists
103
[...] bind irreversibly or at a separate site on the same receptor
noncompetitive antagonists