A chemical (which might be a drug, hormone, neurotransmitter, or other signalling molecule) that binds to its target to increase its activity. Efficacy is 1
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Antagonist
A chemical that opposes the action of another chemical. This means that they should have no action on their targets in the absence of an agonist
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Competitive antagonist
The binding of the antagonist prevents the binding of the agonist by competing for the same binding site. The competitive antagonist will increase the EC50 for the agonist
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Non-competitive antagonist
Binds at a different binding site from the agonist, and prevents the effect of the agonist without preventing its binding. The effect cannot be overcome by adding more agonist and the EC50 for the agonist does not change
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Partial agonist
Drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist (0
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Allosteric potentiating ligand
This occurs when the binding of one ligand enhances the attraction between substrate molecules and other binding sites
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Inverse agonist
Causes an action opposite to that of the agonist yet binds to the same receptor as the agonist. It has an efficacy of less than zero
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Hill-Langmuir
An equation that displays the proportion of receptors occupied by a drug. Kd = [D] when half the receptors are bound, i.e. when p=0.5
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EC50
The molar concentration of an agonist that produces 50% of the maximum possible effect of that agonist
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Pharmacokinetics
The study of the change in drug and metabolite concentrations in tissues and body fluids (ADME)
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Therapeutic ratio
Maximum non-toxic dose (TD50) / Minimum therapeutic dose (ED50)
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TD50
The toxic dose of a drug for 50% of the population
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ED50
The minimum effective drug for 50% of the population
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Bioavailability
The fraction of unchanged drug that reaches the systemic circulation. The value decreases by poor absorption and first pass metabolism
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Absorption
The movement of the drug from point of administration to the circulating body fluids
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Distribution
How drugs equilibrate within the body after reaching systemic circulation
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Volume of distribution
The volume of fluid needed to contain the total amount of drug in the body at the same concentrations as that present in the plasma
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Metabolism
The break down or detoxification of chemicals by CYP450 enzymes (usually in the liver). 2 stages - modification using CYP450 through oxidation, and conjugation of the phase 1 metabolite to mark it for removal
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Pharmacometabolomics
The study of how certain drugs are metabolised in the body in order to predict how the body will metabolise a different drug
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Half-life
The time taken for the concentration of a drug to halve
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Other cards in this set
Card 2
Front
A chemical (which might be a drug, hormone, neurotransmitter, or other signalling molecule) that binds to its target to increase its activity. Efficacy is 1
Back
Agonist
Card 3
Front
A chemical that opposes the action of another chemical. This means that they should have no action on their targets in the absence of an agonist
Back
Card 4
Front
The binding of the antagonist prevents the binding of the agonist by competing for the same binding site. The competitive antagonist will increase the EC50 for the agonist
Back
Card 5
Front
Binds at a different binding site from the agonist, and prevents the effect of the agonist without preventing its binding. The effect cannot be overcome by adding more agonist and the EC50 for the agonist does not change
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