DEFINITION OF TERMS | Pharmacokinetics | Bioavailability

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  1.Absolute bioavailability – fraction of drug absorbed upon extravascular administration vs dose size administered2.Absorption – process of uptake of the compound from the site of administration into the systemic circulation.Prereq aqueous solution. !are exception pinocytosis .Accumulation – increase of drug concentration in blood and tissue until steady state is reached#.Apparent partition coe$cient – ratio of the concentrations %lipid phase &usual n'octanol(  aqueous phase &usually bu)er p*+.#(,' uncorrected for dissociation or association in either phase-.Area under the curve – drug blood level over time from zero to innity' measure of quantity of drug absorbed/.Area under rst statistical moment curve – area underthe curve observed for the product of time and concentration vs time+.0iliary recycling %enterohepatic recirculation, drugs emptied via bile into the small intestine %can be reabsorbed from the intestinal lumen into systemic circulation.0ioavailability ' relative amt of drug that enters the systemic circulation and the rate ar hich the drug appears in the blood stream3.0ioequivalence' achieved if the extent and rate of absorption are not statistically signicantly di)erent from those of the standard hen administered at the same molar dose14.0ioequivalence requirement – for in vitro and5 or in vivo testing of specied drug products 11.0iological half life12.0iopharmaceutics – physical and chemical properties of the drug substance1 .0iophase – actual site of action of drugs1#.0lood 6o rate' speed of blood perfusion in an organ %m75144 g organ eight5min, 1-.0lood'8 plasma' or serum' levels – demonstrate the concentration in blood8 plasma or serum upon administration of a dosage form9 samples by venipuncture1/.:entral compartment – sum of all body regions in hich the drug concentration is in instantaneous equilibrium1+.:hronopharmacokinetics – study of pharmacokinetic drug parameters as a)ected by circadian rhythm or diurnal variation1.:ircadian rhythm – biological clock %during a 2# hr cycle,13.:learance – hypothetical volume of distribution %m7, of the unmetabolized drug hich is cleared per unit of time by any pathay of drug removal24.:linical pharmacokinetics – application of pharmacokinetic principles for the treatment of individual patients and the optimization of drug therapy21.A compartment – entity described by a denite colume and a concentration of drug contained in that volume22.:oncentration gradient – di)erence in the concentration in to phases usually separated by a membrane2 .:reatinine clearance – ratio of creatinine in urine  conc. ;f creatinine in plasma' creatinine clearance decreases ith renal impairment and ith age2#.:umulative urinary excretion curves – plots of the actual cumulative amounts of drug excreted into the urine vs time upon administration of a drug2-.<epot phase – portion of a prolonged release dosage ' liberates the drug from the dosage form at a sloer rate than its unrestricted absorption rate2/.<i)usion layer – viscous layer of concentrated drug solution2+.<isposition – loss of drug from the central compartment due to transfer %distribution,2.<iurnal variation – biological clock controlling rhythmsof processes during a 2# hour cycle23.<osage regimen5 dose rate – systematized dosage schedule for therapy 4.<ose dependency – change of one of more of the pharmacokinetic processes of absorption8 distribution8metabolism and excretion ith increasing dose size 1.<ose dumping – the achievement of sustained drug concentration by simply increasing the dose size or byaccidental fast release of drug from a sustained release dosage form 2.<ose'response curve – graphical presentation of the pharmacological or clinical e)ectiveness or toxicity vs dose. ' log dose'response curve is sigmoid ith a straight line' log dose'probability curve results in an entirely straight line .<ose size – amount of drug in microgram #.<osing interval – time period beteen administration of maintenance doses -.A drug – chemical compound of synthetic8 semisynthetic8 natural or biological srcin hich interacts ith human or animal cells /.A drug specialty5 brand product – labeled ith a registered trade mark of a single company +.<rug release5 liberation – delivery of the active ingredient from a dosage form into solution' dissolution medium biological 6uid 5 articial test 6uid' drug release is characterized by the speed %liberation rate constant, and the amount of drug appearing in solution. .A drug product5 dosage form – gross pharmaceutical form containing the active ingredient%s, and vehicle substances 3.<rug receptor interaction – combining of a drug molecule ith the receptor for hich it has a$nity8 initiation of a pharmacologic response by its intrinsic activity#4.=limination half life – time %hrs, necessary to reduce the drug concentration in the blood8 plasma or serum to one half.' in6uenced by dose size8 variation in urinary excretion %p*,8 intersub>ect variation8 age8 protein binding8 other drugs8 and diseases' elimination of the administered parent drug molecule by urinary excretion 8 metabolism or other pathays of elimination#1.=nterohepatic recirculation %biliary recycling, – drugs emptied via bile into the small intestine'reabsorbed from the intestinal lumen into systemic circulation#2.=nzyme induction – increase in enzyme content or rate of enzymatic processes ? faster metabolismauto induction – stimulates its on metabolismforeign induction – caused by other compounds# .=nzyme inhibition – decreased in rate of metabolism##.=xcretion – nal elimination from the body@s systemic circulation#-.=xtravascular administration – refers to all routes of administration %except for those drugs introduced intothe blood stream,#/.eathering – graphical method for the separation of exponents' residual method is synonymous ith feathering#+.irst pass e)ect – phenomenon hereby drugs may bemetabolized folloing absorption but before reaching systemic circulation.' hepatic rst pass e)ect may occur folloing P.;. anddeep rectal administration ' avoided by using sublingual and buccal routes' pulmonary rst pass e)ect cannot be avoided by BC8 buccal or sublingual routes#.lip 6op model – rate of absorption is sloer than the rate of elimination  #3.Dhe gastrointestinal tract – part of the alimentary canal comprising stomach 8 small and large intestine -4.Eeneric product non propriety or common name of the drug-1.*epatic clearance – hypothetical volume of distribution in m7 of the unmetabolized drug hich is cleared in one minute via the liver-2.*omeostasis – maintenance of a steady state' important function regulation of the 6uid medium and volume of the cell- .*ybrid rate constants – composite rate constants consisting of to or more micro constants8 F and G arehybrid rate constants.-#.Bnitial phase' immediately available for absorption--.Bntravascular administration – drug is directly introduced into the blood stream-/.Bntrinsic clearance – theoretical unrestricted maximumclearance od unbound drug by an eliminating organ-+.B.C. bolus ' physiologic nonsense and poor use of language' bolus %greek,  bite8 something solid hich is salloed and is then absorbed from the intestines ' correct term  BC push-.Dhe 7A<H=! system – complex dynamic processes of liberation of an active ingredient' absorption into systemic circulation' distribution and metabolism in the bodyexcretion of the drug' achievement of response-3.7ag time – period of time hich elapses beteen the time of administration' time a measurable drug concentration is found in blood. ' often found upon P.;. administration cause slo integration and dissolution of tablets or capsules/4.7ean body eight – patient@s body eight minus the fat mass.'drugs of lo lipid solubility should be dosed in obese patients according to the lean body eight./1.7oading dose8 priming dose8 or initial dose – used in initiating therapy/2.7ocal e)ect – administered at the site here the pharmacological response is desired' doesn@t enter the systemic blood circulation or lymphatic stream/ .Haintenance dose – required to maintain the clinical e)ectiveness/#.Hean transit5 residence time – time hen / .2 percentof an BC dose has been eliminated /-.Hetabolism – sum of all chemical reactions for biotransformation of endogenous and exogenous substances//.Hichaelis'menten kinetics – equations to characterize certain phenomena % protein binding8 adsorption8 andnon linear or saturation processes often observed ithincreasing dose sizes,/+.Hicro constants – constant that are part of the hybrid constants %ex. I  128 k 21 , /.Honitoring' determination and recording of drug concentrations during the course of therapy/3.Hultiple dose administration – given repeatedly at intervals shorter than those required+4.Jonlinear kinetics5 saturation kinetics – change of one or more of the pharmacokinetic parameters during absorption8 distribution8 metabolism and excretion by saturation or overloading of processes due to increased dose sizes+1.;ral administration – buccal8 sublingual8 and perlingual administration+2.Peripheral compartment – sum of all body regions to hich a drug eventually distributes' not in instantaneous equilibrium ' further subdivided into K*A77;L and <==P :;HPA!DH=JD+ .Peroral administration – salloed' drug is absorbed from the EB tract+#.Pharmaceutical alternatives – contain the identical therapeutic moiety8 or its precursor+-.Pharmaceutical equivalents – contain identical amounts of the identical active drug ingredient' not necessarily containing the same inactive ingredients+/.Pharmacokinetics – changes of drug concentration in the drug product and changes of concentration of a drug and5or its metabolite%s, in the human or animal body'7iberation8 absorption8 distribution8 body storage8 binding8 metabolism and excretion++.Protein binding' occurs hen a drug combines ith plasma protein or tissue protein to form a reversible complex' non specic %depends on drug@s a$nity8 number of protein binding sites8 protein and drug concentration,+.!ate limiting step – sloest rate constant+3.!eceptor – drug molecules can be bound.' usually a protein or proteinaceous material4.!elative bioavailability – extent of drug absorbed uponextravascular administration vs dose size of a standard administered1.!enal clearance – hypothetical plasma volume in m7 of unmetabolized drug hich is cleared in one min via the kidney2.Kingle dose administration – next dose of the same drug is administered only after the previous dose is completely eliminated .Korption promoters or permeation enhancers – substances that have no pharmacological properties' can improve the penetration of drugs into the skin ortheir permeation through skin or mucosa by reducing the barrier resistance. #.Kteady state – level of drug accumulation in blood andtissue upon multiple dosing hen input and output areat equilibrium-.Ktructural nonspecic drugs – pharmacological is not directly dependent on chemical structure. 'highly lipophilic'don@t react easily' act by physic'chemical processes' examples ether8 nitrous oxide8 halothane8 phenol8 ethyl alcohol8 octyl alcohol8 acetone/.Ktructural specic drugs – pharmacological action results primarily from their chemical structure' examples antibiotics8 sulfonamides8 glycosides8 alkaloids8 etc. +.Kustained release – property of prolonged release dosage forms' liberation rate constant is smaller than the unrestricted absorption rate constant..Kystemic e)ect ' drug enters the blood and5or lymphatic streams' distributed ithin the body3.Dotal clearance – clearance of the hypothetical plasmavolume %m7,' drug per unit time due to excretion via kidney8 liver8 lung8 skin8 etc. and metabolism34.Mnit membrane – physical barrier to transport in the body. ' lipoidal' double ro of phospholipids sandiched beteen one layer eAch or protein31.Mrinary recycling – drugs ltered through the glomeruli are reabsorbed from the tubuli into systemiccirculation32.Cehicle – carrier of the drug3 .Cehicle substances – additives necessary in formulating a dosage form' chemically inert'should not have any pharmacological e)ect in the dose used 3#. Colume of distribution – not a real volume' required to dissolve the total amount of drug at the  same concentration as that found in the blood.'proportionally constant
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