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AP 770 Pharm Exam 1 Lecture 1 Pharmacokinetics Drug Movement Kukanich


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Describe each curve and what they represent.

Zero order example of carrier mediated transport.
First order example of diffusion.
Pharmocokinetics defn:
Use of mathematical models to quantitate the time course of drug disposition.
Pharmacokinetics is essentially
overall description:
4 examples
What the animal does to the drug
Pharmacodynamics definition:
The biological effect a drug elicits.
Pharmacodynamics are essentially:
What the drug does to the animal.
Pharmacokinetics purpose:
Takes into account three things:
Rational dosage design taking into account efficacy, lack of residues and lack of toxicity.
Lipophilic defn:
"fat loving" Non-polar, affinitity for lipids.
aka "water fearing"
Hydrophilic defn:
"water loving." Polar, affinity for water
What are the six areas into which a drug may pass by passing through a lipid membrane?
1) Environment
2) Interstitial fluid
3) Plasma
4) Interstitial fluid
5) Intra-organelle fluid
Where do drugs enter PO?
Into the environment?.
Where do drugs enter IM/SC first?
Interstitial fluid (before plasma)
Where do drugs enter IV first?
Directly into plasma.
Drugs move by what three main mechanisms?
Diffusion, Carrier Mediated, and Endocytosis/exocytosis
Drug Movement
What two types of diffusion are there, and what are examples of these?
Lipid: Across biologic membranes
Aqueous: through pores, within body cavity
Drug Movement
What are the two types of Carrier mediated transport and what are two important characteristics of each?
Active transport
-energy expended
-saturable and specific
Facilitated Diffusion
-no energy required
-saturable and specific
Drug Movement
Endocytosis and Exocytosis
What are minor and major effects (1 of each)?
minor PK effects
Major effects toxicity and residue
What is the primary means of drug movement in the body?
Is Diffusion passive or active?
passive durg movement
How is diffusion affected by the concentration gradient?
Drug moves from higher concentration to lower until equilibrium
What physiochemical properties of the drug affect diffusion?
Molecular weight
Molecular conformation
What is the physiochemical properties of the membrane which affect diffusion?
Lipid composition
What order process is diffusion and what does this mean?
First-order: fixed proporiton of drug moves per time
What are the 6 important factors of diffusion?
1) Primary means of drug movement in the body?
2) Passive
3) Concentration gradient
4) Physiochemical properties of the drug
5) Physiochemical properties of the membrane
6) First-order: fixed proportion of drug moves per time
Diffusion is dependent on what 5 factors?
1) Concentration gradient
2) surface area
3) lipophilicity
4) Soution in membrane
5) Membrane thickness (inversely)
Drug Movement First Order means:
What is constant, what is not?
A fixed proportion of drug moves per time.
Constant rate, not constant amount of drug.
Carrier mediated transport
Which law?
1 very important component:
What order, and what does this mean?
Michaelis-Menton Rate Law
Zero-order: A fixed amount of drug moves per time (not fixed rate)

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