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28 Cards in this Set
- Front
- Back
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516 BASIC CONCEPTS OF PHARMOCOLOGY
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516 BASIC CONCEPTS OF PHARMOCOLOGY
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Pharmacokinetics
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What the body does to the drugs
Ex.: absorption, distribution, metabolism, and excretion of drugs. |
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Pharmodynamics
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What the DRUG does to the body.
Intrinsic sensitivity/responsiveness of the body's receptors to a drug. |
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What type of receptor is GABA-a?
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Ligand gate ion channel.
Meaning that a drug binds to the receptor and the ion flows through. |
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Noncompetitivie antagonism
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Receptor inhibition which CANNOT be overcome by increasing conc. of agonist.
Irrev. blockade |
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Competitive antagonism
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Receptor inhibition
Can be overcome by increasing conc. |
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Prodrug
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Ex is morphine where its metabolite is more potent than morphine.
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Antagonistic effect
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A + B < A or B alone
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Where do the drugs go once they're administered?
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1. compartment model
2. vol of distribution 3. ionization |
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What is the theory behind the Compartment model?
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Body is composed of multiple compartments having calculated volumes.
Depending on which compartments they travel to, pharmacokinetics can then be used. |
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2- Compartment Model
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1. central
2. peripheral |
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Central compartment
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Rapid uptake of drug.
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What is included in the central compartment?
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1. intravascular fluid
2. highly perfused tissues like lungs, heart, brain, kidneys, and liver. |
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Peripheral Compartment
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Slower uptake
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What does the peripheral compartment include?
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Less vascular tissues like fat, bone, and inactive skeletal muscle.
NOTE: drugs equilibrate between compartments, and are eventually eliminated from the central compartment. |
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Which proteins are involved when protein binding of drugs occur?
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1. albumin
2. alpha-1-acid glycoproteins |
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What is the relationship of the degree of protein binding to volume of distribution?
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Inversely proportional
More binding, less volume distribution. |
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What type crosses the membrane? Bound or unbound?
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Unbound
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The effects of protein binding of drugs?
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1. bound drugs do not cross cell membrane
2. free drugs are more available for elimination 3. bound drugs are NOT pharmacologically inert. NOTE: keep in mind the law of mass action |
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Concept behind volume of distribution?
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The total approximation of ALL the compartments to which a drug goes.
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How do you define the distribution phase?
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Immediately after adm of drug
Movement from central to peripheral. |
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Elimination phase?
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It's more gradual as drug is removed from circulation.
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Ionization of drugs
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Drugs' ionization state affects their ability to permeate through membranes.
Ionized form do NOT cross membrane. |
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What determines the degree of ionization of a drug?
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1. pK of substrate
2. pH of surrounding fluid |
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What is ion trapping?
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Where one form of drug (ionized) is separated from the nonionized due to a pH gradient. Nonionized form can travel or diffuse and equilibrate.
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Define clearance
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Removal of drug from plasma
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Define metabolism
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Enzymatic alteration of drug's chemical structure
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What are the four major types of metabolic reactions?
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1. oxidation
2. reduction 3. conjugation 4. hydrolysis |
