Pharmacology 3620 Lecture Notes - Lecture 1: Concentration, Pharmacokinetics, Membrane Transport

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Lecture 001: Introduction to Pharmacokinetics
Membrane Permeability of Drugs
Objectives
Describe how pharmacokinetics relates to overall drug effects.
Describe the tissue barriers that influence drug disposition (absorption, distribution,
metabolism, elimination) in the body.
Name the pathways for drug movement across a membrane.
Define and understand the chemical characteristics of drugs that influence the rate of
passive membrane diffusion.
Define biochemical features of facilitated membrane transport.
The goal of drug therapy is to prevent, cure or control various diseases.
Elements of the doctor’s prescription
Dose depends on:
Size of person
Strength of symptoms
Route of Administration
Metabolism in liver
Chronic drug intake
Easier than needles
What are drugs?
4 basic types by chemical composition
Small Molecules
Organic
300-900 Da
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Majority of drug prescribed (although their usages is decreasing)
Peptides
Small chains of A. A. (up to tens)
Small peptidic hormones
Proteins
Large chains of A. A.
Enzymes
Hormones
Antibodies
Immunoglobulins that target specific things
Oligonucleotide
Antisense therapeutics
Binds RNA to alter gene
expression in the cell
Only 1 available on the
market
Drug Names
Generic Name is the one we
are using
Definitions
Pharmacokinetics:
What the body does to the drug.
metabolism
Pharmacodynamics:
What the drug does to the body.
Targets
Pharmacokinetics (PK)
Quantitative description of a drug concentration in the body over time
The pharmacokinetics of a drug, administered via a specific route, in parts the optimum
dose
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Relationship between PK and PD
Pharmocokinetics
The relationship between the dosage regimen of the drug and the blood concentration of
the drug
Pharmacodynamics
The relationship between concentration of the drug at the site of the action and the effect
However, blood concentration of the drug are not often monitored
Use effects to judge and change dosage
Importance of Pharmacokinetics
The therapeutic/toxic effects of the drug are related to the dose!
Concerned about the dose and the drug concentration at the site of action
And how it relates to drug effect
Drug concentration gives a better relationship be is hard to measure
Effects of the drug is related to the concentration of the drug and the time that the drug
persists in the blood
The higher the dose/ concentration in blood/tissue, the greater the
therapeutic/toxic effect
If the drug remains in the body, the effects will remain
Thus the longer the drug is in the body the longer the effect
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Document Summary

Describe how pharmacokinetics relates to overall drug effects. Describe the tissue barriers that influence drug disposition (absorption, distribution, metabolism, elimination) in the body. Name the pathways for drug movement across a membrane. Define and understand the chemical characteristics of drugs that influence the rate of passive membrane diffusion. Define biochemical features of facilitated membrane transport. The goal of drug therapy is to prevent, cure or control various diseases. Majority of drug prescribed (although their usages is decreasing) Binds rna to alter gene expression in the cell. Generic name is the one we are using. What the body does to the drug. What the drug does to the body. Quantitative description of a drug concentration in the body over time. The pharmacokinetics of a drug, administered via a specific route, in parts the optimum dose. The relationship between the dosage regimen of the drug and the blood concentration of the drug.

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