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26 Cards in this Set
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Km
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reflects the affinity of the enzyme for its substrate -- the lower the Km, the higher the affinity
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Vmax
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directly proportional to the enzyme concentration
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Competitive vs. Noncompetitive Inhibitors -- Resemble Substrate
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Competitive = Yes; Noncompetitive = No
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Competitive vs. Noncompetitive Inhibitors -- Overcome by increase [S]
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Competitive = Yes; Noncompetitive = No
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Competitive vs. Noncompetitive Inhibitors -- Bind Active Site
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Competitive = Yes; Noncompetitive = No
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Competitive vs. Noncompetitive Inhibitors -- Effect on Vmax
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Competitive = Unchanged; Noncompetitive = decrease
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Competitive vs. Noncompetitive Inhibitors -- Effect on Km
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Competitive = Increased; Noncompetitive = Unchanged
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Volume of Distrution (Vd) Def
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Relates the amount of drug in the the body to the plasma concentration, Vd of plasma protein-bound drugs can be altered by liver and kidney disease
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Vd equation
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(amount of drug in the body)/(plasma drug concentration)
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Drugs with low Vd distribute in
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plasma
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Drugs with medium Vd distribute in
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extracellular space
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Drugs with high Vd distribute in
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tissues
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Clearance (CL) Def
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relates the rate of elimination to the plasma concentration
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Clearance (CL) equation
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(rate of elimination of drug)/(plasma drug concentration) = Vd x Ke
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Half-life (t 1/2) Def
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The time required to change the amount of drug in the body by 1/2 during elimination
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Loading Dose equation
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Cp x Vd/F
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Maintenance Dose equation
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Cp x CL/F
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Zero-order Elimination
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Rate of elimination is constant regardless of C
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First-order Elimination
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Rate of elimination is proportional to the drug concentration. Cp decrease exponentially with time
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Phase I metabolism
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reduction, oxidation, hyrdolysis --> yields slightly polar, water-soluble metabolites (often still active) --> cytochrome P450
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Phase II metabolism
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acetylation, glucuronidation, sulfation --> yields very polar, inactive metabolites (renally excreted)
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Competitive antagonist effects of Agonist Dose (log scale) vs % of maximum effect
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shifts curve to the right, decreasing potency, and increase EC50
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Noncompetitive antagonist effects of Agonist Dose (log scale) vs % of maximum effect
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shifts curve downward, decreasing efficacy
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System with Spare Receptors -- What is effect on relationship btw EC50 and Kd?
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EC50 < Kd, indicating that to achieve 50% of maximum effect, <50% of the receptors must be activated
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Partial agonist effect on efficacy and potency
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acts on the same receptor system as the full agonist but has a lower maximal efficacy no matter the dose and potency is an independent factor
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Therapeutic Index Equation
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TD50/ED50 = median toxic dose/median effective dose
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