DEFINITION OF TERMS | Pharmacokinetics | Bioavailability

of 3

Please download to get full document.

View again

All materials on our website are shared by users. If you have any questions about copyright issues, please report us to resolve them. We are always happy to assist you.
PDF
3 pages
0 downs
5 views
Share
Description
MY NOTES FOR CHAP 1 IN BIOPHARMACEUTICS
Tags
Transcript
  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
Related Search
We Need Your Support
Thank you for visiting our website and your interest in our free products and services. We are nonprofit website to share and download documents. To the running of this website, we need your help to support us.

Thanks to everyone for your continued support.

No, Thanks