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55 Cards in this Set
- Front
- Back
Which is most potent |
A |
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What is potency |
how much it will take to achieve max response |
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Which is high affinity which is low |
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What does simple occupancy theory of drug action state |
More R --> More intense response |
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Law of mass action |
Affinity is directly related to potency |
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What does it mean if somehting has Kd of 10^-6 M |
that when [D] = 10^-6 M, 50% of R is occupied |
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Units of k1 and K-1 |
k1 = /s k-1 = /M s |
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For D + R --> DR Kd = |
[D][R] [DR] |
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3 Factors governing Drug Specificity |
Molecules are not spherical Steric Hinderance Electrostatic interactions |
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T/F Dobutamine has only B1 agonist activity |
F; partial alpha antag for + isomer |
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What is the spare R theory and where did it come from |
observation that ED50 < Kd; so you can get 50% response without using 50% of R
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Which Line has high efficacy? which has lowest |
A = High D = Low |
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What color is what type of Agonist |
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Difference between inverse agonist and antag |
Antag will bring 0% change from basal R levels, IA will decrease |
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Allosterism |
When active site becomes available or disappears when reg. molecule binds allosteric site |
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T/F Allosteric modulations are competitive |
F |
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T/F Antagonists have intrinsic activity with high affinity for R |
F; no intrinsic activity |
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T/F Competitive inhibitors bind reversibly |
T |
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Which is competitive antag? What are the net results? |
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What effects agonist potency |
Competitive antag; NOT active site or allosteric site noncompetitive antags |
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What effects agonist efficacy |
Active site or allosteric site noncompetitive antags; NOT Competitive antag; |
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TI is measure of drug ____ |
Safety |
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TI is measured by what 2 methods |
LD50/ED50 and TD50/ED50 |
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CSF is another method of drug safety. what is formula |
LD1/ED99 |
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What are the 4 major R families |
Ion channels G-protein coupled Receptor-linked enzymes Nuclear R |
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Where are G protein coupled R found |
Sensory Secretory Smooth and Cardiac Muscle Metabolosm |
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What do kinases do |
Phosphorylate |
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name 2 R linked enzymes |
Tyrosine Kinases phosphatases |
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Stimulation of Tyrosine K leads to |
Jak/Stat |
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Advantages and Disadvantages of Enteral route |
A: Simple, cost effective, safe, no infection, no pain D: Harsh GI, 1st pass metab, slow |
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Advantages and Disadvantages of Parenteral (IV) |
A: Rapid, high bioavailability, bypasses 1st pass D: irreversible, infection, pain, fear, skill required |
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Advantages and Disadvantages of Mucous membrane (inhalers) |
A: Rapid, no 1st pass, no GI, simple, can give direct to tissue B: Few drugs available |
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Advantages and Disadvantages of Transdermal |
A: simple, excellent for long term use, bypass 1st pass and GI D; Needs lipophilic drug |
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What is absorption |
Movement of drug from site of administration into blood |
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What does Rate and amount tell us about absorption |
Rate: how fast Amount: how intense |
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3 Main ways to cross cell membranes |
Passive diffusion of lipid soluble Passive diffusion of water soluble through water pore Mediated transport |
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5 factors that affect drug absorption |
Rate of dissolution Surface Area Blood Flow Lipid Solubility pH Partitioning |
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Henderson Hasselbalch |
log (protonated/nonprotonated) = pka -pH ph=pka whren prot = nonprot |
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Weak acids go to what body compartments |
alkaline areas like urine (opposite true for weak bases, the go to acidic places like gut) |
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What is Tissue Distribution |
Movement of drug into body compartments from blood |
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Factors influencing tissue distribution |
Tissue blood flow Plasma protein binding BBB Vd |
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What capillaries are porous |
Typical; specialized are not |
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What is Vd = |
Dose/[plasma] |
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Renal clearance = |
Excretion rate/[plasma] |
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Excretion rate = |
[urine] x urine vol/time |
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What most significantly limits the time course of action of drug |
Clearance (Vol/time) |
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T/F Rate of elimation changes as amount changes for 1st order? 0 order? |
T for 1st; F for 0 |
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Slop of [plasma] x time = |
-k; trace back to extrapolate [plasma] at time 0 |
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what is t 1/2 |
(.693 x Vd)/k |
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What 2 factors determine 1/2 life |
Clearance and Vd |
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What time is required to reach steady state with chronic dosing |
1/2 life |
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Loading dose = |
V * target [plasma] |
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Initial [x] = Stead state [x] = Elimination 1/2 life = |
1. Loading dose/Vd 2. Fraction absorbed x maintainance dose/ (Dosing interval x clearance) 3. .693 |
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T/F 1st ordeer kinetics will saturate and taper off in Therapeutic range |
T; 0 will not |