ZFundamentals of Drug Action
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| Bronstead- Lowry acid/ base | Acid is proton donor; Base is proton acceptor
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| 4 strong acids | HCl; HNO3; H2SO4; HClO4
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| 2 strong bases | NaOH; KOH
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| pKa < 2 is a strong | strong acid; no basic properties in water
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| pKa 4-6 is a ? | weak acid; very weak conjugate base
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| pKa 8-10 is a | very weak acid; weak conjugate base
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| pKa > 12 | no acidic properties in water; strong conjugate base
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| the stronger an acid, the weaker its conjugate base | no answer
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| what is the conjugate acid and base of HA + H20 | Conj acid= H3O; conj base is A-
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| Keq= | [products]/ [reactants]
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| difference between pH and pKa | pH is property of a solution/ pKa is property of a molecule- the tendency of protonated for to give up a proton
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| Henderson Hasselbalch eq: | pH= pKa+ log [conj base/ acid]; the conj base is proton acceptor, acid is donor
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| Relates pH/ pKa to relative amount of acid/ base | henderson- hasselbalch equation
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| Drugs that are amines are: | basic
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| In an acid, what gets ionized | conjugate base gets ionized; ex: HCl --> Cl-
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| In a base, what gets ionized? | the acid is ionized
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| Conjugate base of salicylic acid | salicylate
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| Drugs that are amines are: | basic
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| In an acid, what gets ionized | conjugate base gets ionized; ex: HCl --> Cl-
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| In a base, what gets ionized? | the acid is ionized
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| Conjugate base of salicylic acid | salicylate
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| Henderson Hasselbalch; not always charged reactant | always protonated form on the left (reactant) side of the equation (DENOMINATOR)
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| For ionized acids, pH is above or below pKa? | pH is above pks (chart)
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| For a base, the percent ionization gets higher as pH | gets lower (think chart)
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| Pharmaco-kinetics | Action of the body on the chemical (what the body does to the drug)
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| Pharmaco- dynamics | What the drug does to the body
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| Processes of pharmacokinetics ADME | absorpion, distribution, metabolism, elimination
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| Output: Concentration- time relationships | Pharmacokinetics
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| Process of pharmacodynamics: | Biological ligands acting on their molecular targets in the body
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| Output: Biological response | Pharmacodynamics
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| when drug reached site of action we see | pharmacodynamics response; drug- receptor complex/ pharmacologic response
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| Prior to reaching targets the drug must go thru what obstacles? These barriers affect the pharmacokinetics ofthe drug | pass thru barriers (membranes) avoid wrong turn (ex: accumulating in fat cells; avoid metabolic destruction; stability at different pH levels
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| absorption is affected by ionization state | true; affects drug;s ability to pass thru membranes
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| acids like aspirin are absorbed where | stomach, low pH- the thing that is UNionized is absorbed..aspirin in unionized on the chart until about pH 5. after that it would not be too useful
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| Bases are absorbed in | intestines because as pH increases, bases get LESS ionized
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| why precipitation of bases? | go from charged NH3+ to uncharged NH2; less polar and may precipitate because out of solution; wants to get away from water (hydrophobic)
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| ases are 100% ionized where in the absorption process | stomach
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| to pass thru lipid barrier, a weak acid would be on the left side of the equation because | it is unionized
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| weak bases pass thru lipid barrier on the right side of the equation because | they are neutral (unionized); they are protonated on the left side of the rxn; example: BH+ +H2O <-> H3O + B(neutral)
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| PH maintenance mechanisms (3) | chemical buffering; lungs; kidney (renal)
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| Chemical buffering (quick) name 4 systems | bicarbonate buffer;phosphate buffer; ammonia buffer; proteins
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| If strong acid is introduced, the reaction will move in which direction? | left because the A- will pick up an H+ which drives the rxn to make HA
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| The most important extracellular (plasma) buffering system | bicarbonate buffer system; generally considered clinically
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| Carbonic acids (H2CO3) exist in low amounts in the body; CO2 is considered the weak acid | no answer
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| Co2 and HCO3 act as buffers | true
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| pCO2 is used as? | an index of the amount of carb on dioxide in the body (normally 40mm Hg)
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| Normal concentration of bicarbonate is | 24 mEq/L; ratio of HCO3-/ H2CO3 is 20:1
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| Intracellular buffer; also in the kidneys | phosphate buffer system
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| By-product of amino acid metabolism | ammonia; amino acids can serve as buffers in the ammonia buffer system
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| most plentiful chemical buffers; high concentrations inside cell | proteins; side chains can accept or donate a proton
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| CO2 is an acid and the lungs remove it to raise pH | no answer
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| The slowest most powerful acid/ base balance | Renal (kidney); excrete acidic or basic urine depending on whats needed
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| If bicarbonate is not reabsorbed( back into bloodstream) it is excreted | in the urine; bicarbonate is not well absorbed by itself, must combine with a proton
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| Bicarbonate and H+ combine to form what? | CO2 and H2O; then can enter renal tubule; once in the renal tubule they can separate and bicarbonate returns to capillary
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| excess acid in plasma, what does kidney do? | kidney reabsorbs ALL bicarbonate to raise pH
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| Alkalosis, what does kidney do with bicarbonate? | less bicarbonate is reabsorbed, more is excreted
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| respiratory acidosis | increased pCO2; high bicarbonate indicates compensation
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| Metabolic acidosis | low bicarbonate; normal pCO2 indicates not related to respiratory but can be low as compensation
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