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44 Cards in this Set
- Front
- Back
Concentration of drug at site of action is dependent on several variables
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Pharmacodynamics
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Relationships between concentrations of drug and effect (what Drug does to Body)
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Pharmacokinetics
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Drug absorption, distribution, metabolism, and elimination (what the Body does to the Drug)... A.D.M.E.
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Enteral Modes of Administration (Entering Intestine)
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Oral, Sublingual, Rectal
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Oral Admin (PO) Advantages
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convenient, safe, economical
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PO disadvantages
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GI irritation, destruction of drugs by digestive NZMs, irregular absorption due to food or pH, compliance necessity, 1st pass effect
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First Pass Effect
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due to liver metabolism of drug that occurs with oral or rectal admin. prior to drug entering circulation
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Sublingual advantages
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avoids 1st pass via superior vena cava
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Rectal advantages
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can be used avoid vomiting and some of 1st pass effect
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Rectal Disadvantages
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irregular absorption
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Parenteral Injection modes
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IV, SQ, IM- outside intestine
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IV advantages
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instant and accurate admin, can titrate drug efx, can give otherwise irritating solutions
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IV disadvantages
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Danger of toxicity from instant delivery, loss of patent veins
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SQ advantages
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slow and constant absorption provides sustained effect, can manipulate for slow absoprtion and/or release (i.e. via co- vasoconstrictor or inserting pellet form)
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SQ disadvantages
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cannot use irritating drugs because causes necrotic tissue
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IM advantages
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rapid absorption of drugs in aqueous solution, slow but constant absorption of drugs in oil solutions... but can be painful
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Bioavailable dose
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how much of a drug will be absorbed and reach circulation. Expressed as % and takes A.D.M.E into account.
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Factors affecting bioavailability
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Route of Admin., charge, lipid solubility and size of drug, and patient physiology
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Properties of Diffusion
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Not saturable dependent on lipid solubility, only small charged molecules can cross, pH can have a major effect
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Henderson-Hasselbalch equation describes
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the proportion of the drug that is charged a certain pH
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Because many drugs are charged, pH can have a
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major influence on where, along the intestinal tract, a drug is absorbed
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Where should weak acids be best absorbed?
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Stomach because more uncharged drug within the low pH environment
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a Weak Acid can be accumulated or concentrated where?
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in a basic compartment
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a Weak Base can be accumulated or concentrated where?
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in an acidic compartment
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Factors controlling absorption
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pKa of a drug, solubility in aqueous solution, dissolution rate if a solid, Surface area, circulation at site of absorption
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Volume of Distribution
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hypothetical volume of plasma a drug would distribute into if it were only distributed in plasma; this volume is different for each drug
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Volume of Dist. Equation
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Vd = bioavailable dose/ Conc. of drug in plasma
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Volume of Dist. Usages (3)
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1) tells about the behavior of a drug; very high Vd tells drug is accumulated in non-plasma compartments; low Vd implies within plasma (binded to proteins). 2) tells how big a volume is need in order to reach Tx conc. 3) used for other PK parameters, i.e. clearance
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Why can weak bases have a larger Vd in Ruminants?
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b/c weak bases accumulate in acidic compartments, and the Rumen is a large acidic compartment
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How are drugs eliminated
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either by direct excretion of by conversion to metabolites which are then excreted
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If a drug follows first order kinetics, then
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the metabolizing NZM for that drug is not saturated, thus rate of elimination is directly proportional to the drug conc.
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First order kinetics equation
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lnCt = -Ket + lnC0
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Relationship between rate of elimination and the time required to metabolized 50% of the drug (half life)
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0.693/Ke = t 1/2
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Clearance (CL)
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ability of the body to eliminate a drug by all routes; Metabolism and excretion
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CL formula
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CL = 0.693/t 1/2 x Vd units in ml/min Kg
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Effects of altering Ka, Ke, and dosage on concentration in plasma
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Bioavailability
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Amount of drug that enters circulation after first pass effect (fraction or %)
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Drug distribution will frequently be separated into
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phases
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A drug will equilibrate with ____ tissues rapidly, then ___ redistributes into less perfused tissues. This is called __C__
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A) Rapidly, B) Slowly, C) 2 compartment PK model
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If interval of administration is equal to half-life, then
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it will take about 4 doses to get to plateau concentration
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Repeated admin of a drug via any route other than continuous infusion, will cause concentration of drug to do what?
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to rise to a peak level, then fall to trough level
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The average of peak and trough concentrations is called
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plateau concentration
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Generally a drug is given at an interval
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that is less than or equal to 1/2 time for elimination
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0 order kinetics
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same AMOUNT (not %) of drug will be eliminated at each time interval rather than same fraction. i.e. alcohol- NZMS (systems) of inactivation become saturated
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