Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharmacology Unit 1 > Pharmaco - Dynamic, Kinetics, & Genomics > Flashcards

Pharmaco - Dynamic, Kinetics, & Genomics Flashcards

1
Q

What drugs do to the body

A

Pharmacodynamics

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

What the body does to drugs:
Absorption
Distribution
Metabolism
Excretion

A

Pharmacokinetics

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

Specialized target that binds a drug or endogenous ligand and mediates the pharmacologic action

A

Drug Receptor

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

Nomenclature used when a drug is bound to a receptor.
Initial Phase: drug receptor interaction
Complex phase: biological response

A

Drug Receptor Complex

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

Occurs when all drug receptors are bound. No further complex & no further increase in response

A

Saturation

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

Compound that binds to the receptor and stimulates the biological response.
* Usually mimics the response of an endogenous ligand.
* Magnitude of the response depends on how many drug receptor complexes are formed.

A

Agonist

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

Blocks or reverses the effects of agonists.
- No effect on their own. Can be competitive or non-competitive.

A

Antagonist

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

Produces a biologic response but not 100% (even at high doses).
- Occupies all receptors but doesn’t activate ligand binding site.
- Opens ion channels differently or incompletely
- Can act as an antagonist if given with full antagonist.

A

Partial Agonist

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

Competes with agonists for the receptor site
- increase concentration = increased odds of winning the receptor site

A

Competitive Antagonists

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

Permanently bind with receptor sites and prevent activation by agonists.
- reduces maximal response an agonist can produce.
- cannot be overcome by increase the concentration of the agonist. (the agonist can bind there all it wants; it will still do no good)

A

Noncompetitive Antagonists

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

Substance that binds to a receptor and causes it to do the opposite of what the naturally occurring transmitter does.
- makes receptors tilt towards the inactive state
or
- decreases the amount of time receptors are open

A

Inverse Agonist

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

Maximal amount of response a drug can produce

A

Efficacy

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

Measure of the dose required to produce a response

A

Potency

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

Measure of drug safety

A

Therapeutic Index

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

How do you calculate the Therapeutic Index?

A

Lethal Dose₅₀/Effective Dose₅₀

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

Is a drug safer if the Therapeutic Index is larger or smaller?

A

Larger = Safer

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

Dose that kills half the population

A

Lethal Dose₅₀

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

Dose at which half the population responds

A

Effective Dose₅₀

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

At what number is the Therapeutic Index considered to be narrow?

A

< 2

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

When two drugs with the opposite effects are given together

A

Functional Antagonism

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

When an antagonist is administered with an agonist
- Narcan blocking the effects of Heroin.

A

Competitive Antagonism

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

Diminished response to a drug over time
- receptor desensitization
- receptor down regulation

A

Tolerance

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

Enhanced response to a drug (super-sensitivity)
- receptor up-regulation = increasing the number of receptors on a cell’s surface

A

Hyperactivity

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

When the body quickly develops a reduced response to the drug, requires higher doses for the same effect

A

Tachyphylaxis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Enhancement of one drug by another which has no effect on its own
- clavulanic acids potentiates amoxicillin (Augmentin)

A

Potentiation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

Occurs when the effects of two drugs together is greater than the effect of either drug by itself
- Trimethoprim + Sulfamethoxazole (Bactrim)

A

Synergism

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

Dose related adverse effects of a drug

A

Toxicity

28
Q

Movement of the drug from the site it was administered into the body

A

Absorption

29
Q

Amount of drug that is absorbed after oral administration vs. the amount of drug that is absorbed after IV administration

A

Bioavailability (f)

30
Q

Bioavailability Equation

A

AUCₒᵣₐₗ / AUCᵢᵥ = f

31
Q

Bioavailability of drugs given IV

A

f = 1 (100%) because they do not undergo first pass.

32
Q

Driven by a concentration gradient
- no carrier and non-saturable
- used by most lipid soluble and uncharged drugs

A

Simple Diffusion

33
Q

Are most drugs polar or non-polar?

A

Non-polar

34
Q

Carrier mediated and driven by concentration gradient.
- Competition by similar molecules and therefore saturable.
- NO ATP NEEDED

A

Facilitated Diffusion

35
Q

Do drugs absorb faster if dissolved in aqueous or oily solutions?

A

Aqueous

36
Q

Do drugs absorb faster if they have a smaller or larger molecular size?

A

Smaller Molecular Size

37
Q

Do drugs absorb faster if they have a smaller or larger particle size?

A

Smaller Particle Size

38
Q
  • Most drugs are weak acids or bases
  • only the nonionized (non-polar form) of the drug can cross the membrane.
  • Ratio of ionized vs. nonionized is determined at the site of absorption and by the drug’s pKa.
A

Degree of Ionization

39
Q

Likes Dissolve Likes

A

Acidic drugs = nonionized in acidic medium
Basic drugs = nonionized in basic medium

40
Q

Tablet, liquid, capsule, injection, etc. can affect the rate and extent of absorption
- liquids given orally are absorbed more rapidly than tabs or caps

A

Route & Dosage Form

41
Q

Some drugs cannot be absorbed in the GI tract so they must be given IV due to their chemical nature. What drug is an example of this?

A

Heparin

42
Q

Non-active components of drugs can change absorption
- Metoprolol tartrate (IR) vs Metoprolol succinate (ER)

A

Formulation

43
Q

How does concentration affect absorption?

A

Higher concentration is absorbed faster

44
Q

How does Area of Absorptive Surface affect absorption?

A

Larger surface area = faster absorption
(intestine > stomach)

45
Q

How does vascularity affect absorption?

A

Faster absorption in areas with more blood flow
(muscle > subcutaneous tissue > stomach)

46
Q

How does pH affect drug absorption?

A

acidic pH favors acidic drug absorption
basic pH favors basic drug absorption

47
Q

How might the presence of other substances affect absorption?

A

Foods or drugs may interact to alter the rate of absorption

48
Q

How does GI motility affect absorption?

A

More contact time = more absorption
(diarrhea = poor absorption)

49
Q

How does the integrity of the absorptive surface affect absorption?

A

Edema = decreased absorption
Skin thickness can affect topical absorption

50
Q

Initial metabolism in the liver of a drug absorbed from the GI tract before the drugs reaches systemic circulation through the bloodstream
(this decreases bioavailability of drugs)

A

First Pass Effect

51
Q

Initially inactive drugs that exert no pharmacology effects until they are metabolized

A

Prodrugs

52
Q

Process by which an absorbed drug moves from the site of absorption to other area in the body

A

Drug Distribution

53
Q

Binding to Plasma Proteins

A
  • mostly albumin
  • reversible, saturable, subject to competition
  • SEQUESTERS DRUGS IN THE BLOOD, slows their transfer into tissues, and prolongs their duration of action
    (Warfarin and Diazepam)
54
Q

Binding to Tissue Proteins

A
  • some drugs accumulate in certain tissues
    (Benzodiazepines accumulate in fat)
55
Q

Highly perfused organs reach higher concentrations of drug than poorly perfused

A

Vascularity

56
Q

Other Distribution Factors

A

Age
Gender
Body Fat

57
Q

The process of converting a drug into another chemical called a metabolite (biotransformation)

A

Drug Metabolism

58
Q

What is the major metabolizing organ of the body?

A

Liver

59
Q

What are the minor metabolizing organs of the body?

A

GI Tract
Lungs
Kidneys
Skin

60
Q

How does metabolism affect most drugs?

A

Usually metabolism makes a molecule more water soluble (hydrophilic) to enhance its removal from the body (excretion) as most molecules are lipid soluble and thus normally are hard for the body to excrete

61
Q

These reactions frequently involve the Cytochrome P-450 Enzymes.
- Introduces or unmasks a polar functional group to increase renal elimination

A

Liver Metabolism: Phase I

62
Q

MAKES IT MORE POLAR TO INCREASE RENAL ELIMINATION
- reactions are conjugations (united).
- combine glucuronic acid, sulfuric acid, acetic acid, or an amino acid with the drug

A

Liver Metabolism: Phase II

63
Q

Removal of drugs from the body, either unchanged or as metabolites

A

Drug Elimination

64
Q

What organ eliminates most drugs from the body?

A

Kidneys

65
Q

Drugs secreted into the bile, then reabsorbed in the small intestine. A fraction is then excreted into the bile, some enters systemic circulation once again.
- Prolongs the amount of time the drug is in the body

A

Enterohepatic Recycling

66
Q

Inherited variation in the DNA sequence (mutation)

A

Polymorphism

67
Q

Variation in a single base pair within the DNA

A

Single Nucleotide Polymorphism (SNP)

Pharmacology Unit 1 (5 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions