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33 Cards in this Set
- Front
- Back
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(amount of drug)/(fluid compartment concentration)
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Vd
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protein bound drugs
liver and kidney disease pharmacodynamic variable altered? |
Vd
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Vd eq
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Vd = drug amount/drug concentration
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Cl eq
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Cl = elimination rate/[drug]
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t1/2 eq
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t1/2 = .7*Vd/Cl
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10% remaining concentration
# half lives? |
3.3
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12.5% remaining concentration
# half lives? |
3
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25% remaining concentration
# half lives? |
2
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Loading dose eq
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Loading dose = Cp*Vd/F
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Maintenance dose eq
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Maintanence Dose = Cp*CL/F
Cp= target [drug] F = bioavailability |
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change in loading dose with renal/hepatic disease
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Unchanged
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change in maintanence dose with renal/hepatic disease
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lower
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zero order elimination
constant __ of drug eliminated per time |
amount
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first order elimination
constant __ of drug eliminated per time |
fraction
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zero order elimitation
Cp decreases linearly/exponentially? |
linearly
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first order elimination
Cp decreases linearly/exponentially? |
exponentially
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Phase I metabolism
resulting metabolite characteritics |
slightly polar
water soluble often still active |
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Phase I metabolism reactions
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oxidation
reduction hydrolysis |
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oxidation
reduction hydrolysis Phase? |
Phase I
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cytochrome P-450
phase? |
Phase I
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Phase II metabolism
resulting metabolite characteristics |
very polar
inactive *renally excreted |
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Phase II metabolism reactions
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acetylation
glucuronidation sulfanation |
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acetylation
glucuronidation sulfanation Phase? |
Phase II
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conjugation
Phase? |
Phase II
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Phase metabolism lost in geriatrics
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Phase I
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competitive antagonist effect on agonist dose curve
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shift to right
**decreased potency |
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noncompetitive antagonist effect on agonist dose curve
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shifts downward
**decreased efficacy |
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EC50 vs Kd in system w/ spare receptors
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EC50 < Kd
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partial agonist vs full agonist
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less efficacy
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phase 1 clinical trial questions
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is it safe?
pharmacokinetics? |
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Phase 2 clinical trial questions?
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does it work in patients?
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Phase 3 clinical trial questions?
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Does it work double blind?
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Phase 4 clinical trial questions?
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Postmarketing is it safe?
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