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42 Cards in this Set
- Front
- Back
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Define: pharmacodynamics
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Drugs effect on body - determines the most appropriate drug for a given disease
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What are the steps in drug action?
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1. Drug/receptor modification -> modification of receptor, 2. modified receptor -> activates an effector to produce effects
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Define: drug receptors
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Endogenous initiator of drugs effects
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What are the properties of drug receptors
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1. Selectivity, 2. capable of multiple conformations, 3. dynamism, 4. mediate drug actions
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What drug works on the 5HT1 receptor?
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Sumatriptan - autocoid
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What drug works on NR3C2 receptor?
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Sironolactone - Hormone
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What drug works on NEUROTRANSMITTERS?
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Terazosin - alpha-1 receptor
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What drug works on acetylcholinesterase and inhibits it?
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Edrophonium
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What drug works on vitamin K epoxide reductase?
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Warfarin
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What drug works on reverse transcriptase?
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zalcitabine
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What drug works on the transport protein - Ca2+ channel?
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Verapamil
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What drug works on the structural protein - Tubuline
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colchicine
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What mechanism allows for selectivity of drug-receptor interaction?
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Lock and key - determines selectivity, depends on type of chemical bonding involved
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The stronger the bond between drug and receptor
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Less selectivity
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The weaker the bond between drug and receptor
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More selective
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What is the graph of dose occupancy?
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Non- linear relationship - the receptors fill up quickly but once it gets close to max it slows down filling up
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What is the equation for receptor OCCUPANCY?
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B/ Bmax = C / C+ Kd
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What happens to receptor occupancy as u ↑ dose?
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↑ dose = ↑ receptor occupancy is u easier to bind more drug cuz there's more around (non-linear relationship)
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What is the equation for dose-RESPONSE relationship?
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E = (Emax * C)/ (C + EC50)
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Define: agonist
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Stabilizes receptors in active conformations
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What drug is an agonist @ M?
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Bethanechol
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What drug is a partial agonist @ beta-receptors?
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Carteolol
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Define: partial agonist
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Stabilizes receptors equally in active & inactive conformations
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What has a higher efficacy - full agonist or partial agonist?
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Full agonist has a higher efficacy
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Define: competitive antagonist
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Prevents agonist from interacting w/receptor
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Define: non-competitive antagonist
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Covalent or high affinity binding
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What happens to efficacy of drug in presence of competitive antagonist?
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Competitive antagonist - efficacy stays the same but potency ↓
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What happens to the efficacy of drug in presence of non-competitive antagonist
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Non-competitive antagonist - ↓ both efficacy and potency
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Allosteric antagonist
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No at agonist binding site
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What drug is an example of allosteric antagonist
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Strychnine
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Inverse agonist
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Possible when receptor has intrinsic activity - turns off intrinsic activity
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What drug is an example of inverse agonist
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Fexofenadine - treats allergies (allegra)
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Chemical antagonist
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Neutralizes agonist
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Example of chemical antagonist
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Protamine working on heparin
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Define:physiologic antagonist
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Produces physiologically opposing effects
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Examples of physiologic antagonists
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Insulin(building) and cortisol(destruction)
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Define: spare receptors
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Maximum effect w/o occupancy of all available receptors(ie max cardiac stimulation is possible w/stimulating only 10% of beta-receptors) (non-competitive antagonist)(↑ patient sensitivity to drug)
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What effect does spare receptors do to efficacy and potency?
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Efficacy = stays same, potency = ↑ b/c u need less drug to get same effect
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What is a non-receptor drugs?
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Drugs that works w/o working on a receptor system
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MOA of sucralfate
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Forms a protective coat on ulcers -> ↓ further erosion by stomach acid
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MOA of osmotic diuretics
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↑ osmotic pressure in proximal tubules and descending loop of henle
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MOA of antacids
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Neutralizes stomach acid
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