Properties of Organisms & Substances Flashcards

1
Q

Match the following terms to their definition:

  1. Pharmacokinetics
  2. Bioavailability
  3. ADME
  4. Pharmacodynamics

A. Absorption, Distribution, Metabolism, and Elimination. Fundamental principles applicable to all organisms and all xenobiotics.
B. How the organism affects the fate and time course of the substrate. Determines bioavailability.
C. How substrate affects organism. Determined by bioavailability.
D. Rate and extent to which a substance becomes available at the site of action or reaches the systemic circulation. Influenced by ADME.

A
  1. Pharmacokinetics: How the organism affects the fate and time course of the substrate. Determines bioavailability.
  2. Bioavailability: Rate and extent to which a substance becomes available at the site of action or reaches the systemic circulation. Influenced by ADME.
  3. ADME: Absorption, Distribution, Metabolism, and Elimination. Fundamental principles applicable to all organisms and all xenobiotics.
  4. Pharmacodynamics: How substrate affects organism. Determined by bioavailability.
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2
Q

What is the science and study of factors that determine the amount of substance at sites of biological effect at various times after exposure?

A

Pharmacokinetics

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3
Q

The response of pharmacokinetics is __________, which relates to the concentration at ______, commonly measured by blood and urine.

A

Pharmacodynamics, SOA

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4
Q

T/F. The therapeutic range is between the Minimum Effective Concentration (MEC) and Minimum Toxic Concentration (MTC).

A

True!

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5
Q

What are the four different types of mechanisms of pharmacokinetics that takes a dose of drug and turns it into a drug concentration in target organ over time?

A

ADME

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6
Q

What are the three different types of mechanisms of pharmacodynamics that takes a drug concentration in target organ over time and turns it into mechanism and magnitude of drug effect?

A
  1. Receptor binding
  2. Signal transduction
  3. Physiological effect
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7
Q

What is toxicology? Why is toxicodynamics and toxicokinetics often unknown?

A

Toxicology is in reference to toxins. Often unknown because it is unethical to have human data, only relies on animal research. Adverse effects of therapeutics is generally known as pharmacology.

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8
Q

Cells are organized into ______, which have specialized tasks and are compartmentalized to form ______, which work together to form a ______.

A

Tissues, Organs, System

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9
Q

Choose the correct statement:

a) The same substances work the same in humans and animals
b) A substance can affect one or more systems
c) The major tissues in mammals are epithelial, connective, muscle and nervous.

A

c!

a - no can work differently
b - always affects more than one system! never only one system!

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10
Q

What are the three functions/properties of fluids in organisms?

A
  1. water is essential to life
  2. carriers nutrients into cell/body and wastes out
  3. can be manipulated and compartmentalized
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11
Q

What are the two types of fluids?

A
  1. Extracellular fluid
  2. Intracellular fluid
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12
Q

Match the following terms to their definitions:

  1. Extracellular fluid
  2. Intracellular fluid
  3. Plasma
  4. Lymph
  5. Blood
  6. Other fluids

A. Medium in which all cell reactions take place. Pressure helps cell hold shape. Drawn from extracellular fluid.
B. Composed of water, red + white bc, nutrients, platelets, proteins and xenobiotics. Travels within arteries, veins, capillaries, heart chambers.
C. Interstitial fluid collected, transported, then emptied into the blood
D. Compartmentalized fluids (cerebrospinal) & human secretion
E. Flows around cells for exchange of materials. Composed of interstitial fluid (lymph), intravascular fluid (plasma) and cerebrospinal fluid.
F. Liquid part of blood

A

Extracellular fluid - Flows around cells for exchange of materials. Composed of interstitial fluid (lymph), intravascular fluid (plasma) and cerebrospinal fluid.

Intracellular fluid - Medium in which all cell reactions take place. Pressure helps cell hold shape. Drawn from extracellular fluid.

Plasma - Liquid part of blood

Lymph - Interstitial fluid collected, transported, then emptied into the blood

Blood - Composed of water, red + white bc, nutrients, platelets, proteins and xenobiotics. Travels within arteries, veins, capillaries, heart chambers.

Other fluids - Compartmentalized fluids (cerebrospinal) & human secretion

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13
Q

T/F. Humans are primarily composed of interstitial fluid.

A

False, Intracellular fluid is 67% of human weight, while interstitial fluid is 26%.

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14
Q

T/F. Lymphatic vessel allows for larger proteins and nutrients compared to blood vessel.

A

True!

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15
Q

How can xenobiotics cross the cell membrane?

A
  1. Diffusion - passive or facilitated
  2. Active transport
  3. Exocytosis
  4. Endocytosis
  5. Pinocytosis
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16
Q

Match the following terms to their definitions regarding PASSIVE TRANSPORT:

  1. Simple diffusion with channels
  2. Facilitated diffusion with channels
  3. Facilitated diffusion with carrier proteins

A. usually for things that body uses a lot. Selective, Regulated + SATURABLE (can be stopped with competition). Reversible: changes structure.
B. Selective + Regulated & Non-saturable (increasing conc in one side = increases rate).
C. Mostly ions based on size and charge. Never changes structures.

A
  1. Simple diffusion with channels - Selective + Regulated & Non-saturable (increasing conc in one side = increases rate).
  2. Facilitated diffusion with channels - Mostly ions based on size and charge. Never changes structures.
  3. Facilitated diffusion with carrier proteins - usually for things that body uses a lot. Selective, Regulated + SATURABLE (can be stopped with competition). Reversible: changes structure.
17
Q

Carrier proteins for facilitated diffusion are widely distributed in _____ tissues and expressed in adults mostly in ______ and ______ cells of barrier tissues such as the blood-brain barrier.

A

Fetal

Erythrocytes
Endothelial

18
Q

Unlike passive transport, active transport requires _______. Similarly to carrier proteins of passive transport, active transporters are also ________, and ________; can be inhibited by competition.

A

Energy

Reversible (changes stucture)
Saturable

19
Q

Match the following terms to their definitions regarding active transport:

  1. Primary active transporters
  2. Secondary active transporters
  3. Phagocytosis
  4. Pinocytosis
  5. Receptor-mediated endocytosis

A. Utilize energy (stored in voltage/ion gradient) generated by primary transporters.
B. Generate stored energy for subsequent use (create gradient).
C. For larger molecules and is more selective.
D. Kind of like eating.
E. Kind of like drinking, non-selective - everything in the solution gets into cell.

A
  1. Primary active transporters - Generate stored energy for subsequent use (create gradient).
  2. Secondary active transporters - Utilize energy (stored in voltage/ion gradient) generated by primary transporters.
  3. Phagocytosis - Kind of like eating.
  4. Pinocytosis - Kind of like drinking, non-selective - everything in the solution gets into cell.
  5. Receptor-mediated endocytosis - For larger molecules and is more selective.
20
Q

(T/F) Protein carriers recognize xenobiotics because they resemble structural properties/motifs with carrier’s endogenous transport molecule.

A

True!

21
Q

Which molecule in the pair is easier to get into membrane?

  1. Lipid vs water soluble
  2. Non-ionized vs ionized
  3. Small vs bigger molecules
  4. Gases vs small lipid molecules
  5. Large + highly lipophilic molecule vs water
A
  1. Lipid soluble
  2. Non-ionized
  3. Small molecules
  4. Gases (100% permeable)
  5. Large + highly lipophilic molecule
22
Q

How is lipophilicity commonly measured?

A

It is measured by its distribution behaviour in a biphasic system (1-octanol/water).

23
Q

What is the partition coefficient (P)?

A

Concentration dissolved in partition solvent/concentration dissolved in water

24
Q

What is the disadvantage of a too non-polar drug? of a too polar drug?

A

Too non-polar: can stay in membrane

Too polar: can’t come out of lipid bilayer

25
Q

Values smaller than 0 of Log P represent _________ molecules, while values greater than 0 of Log p represent _________ molecules. Most drugs have a log P of ______.

A

Hydrophilic

Hydrophobic

0-4

26
Q
  1. pH < pKa =
  2. pH > pKa =
A

pH < pKa = protonated

pH > pKa = deprotonated

27
Q

(T/F) The higher the pKa, the more acidic the substance.

A

False, the higher the pKa, the more basic. The lower the pKA, the more acidic.

28
Q

Do the last two questions on Lecture 2 slides!

A

:)