For many drugs, the gastrointestinal absorption rate, but not the. A study to evaluate the pharmacokinetics and the effect on. Clinical pharmacokinetics and pharmacodynamics larry a. The same concept can be applied to generally assess pharmacodynamic responses and the deviation of a signal from its baseline value. The area under the plasma drug concentrationtime curve auc reflects the actual body exposure to drug after administration of a dose of the drug and is expressed in mghl. Basic pharmacokinetics 21 cate the amount of drug being removed. Whole organ pharmacokinetics are used to estimate the mean residence times of radioactivity and from these, the radiation absorbed doses deposited in various tissues following administration of a radiopharmaceutical 4. Pdf pharmacokinetics, distribution, metabolism, and.
Evaluation of the ratio of the estimated area under the concentration. Noncompartmental pharmacokinetics and bioequivalence analysis. Pharmacokinetics pk is talked about a lot in the hiv community. Area under a curveusing a limit since letting n be a very large number will result in a huge amount of work, the process can be simplified by using sigma notation and summation formulas to create a riemann sum. Mar 14, 20 the area under the concentrationtime curve extrapolated to infinity auc 0. Standard calculation of auc involves using noncompartmental techniques to calculate the auc from. A linear relationship exists between area under the curve and dose when the. The area under the moment curve aumc from the time of dosing to the last measurable concentration. Curve fitting of experimental data using computers. This area is called the area under the curve regardless of whether it is above or below the x axis.
Large number of subjects 100, up to thousands oral dose. Modeling single and repeated dose pharmacokinetics of pfoa. The definite integral can be used to find the area between a graph curve and the x axis, between two given x values. It is of interest to know the area under the curve, i. In practice, the drug concentration is measured at certain discrete points in time and the trapezoidal rule is. Pharmacokinetics basics absorption, distribution, metabolism. Principles of pharmacokinetics learning objectives.
The auc can be calculated as before using by the trapezoidal rule. Effect of extremes of body weight on the pharmacokinetics. Aaps advances in the pharmaceutical sciences series, vol. Apr 09, 2011 pharmacokinetics is the way the body acts on the drug once it is administered. In a drug with nonlinear kinetics, doubling the dose will double the concentration. The aumc is the area under the concentration times time versus. If you would like to participate, please visit the project page, where you can join the discussion and see a list of open tasks. Mathematical expressions of the pharmacokinetic and pharmacodynamic models implemented in the pfim software anne dubois, julie bertrand and france mentr e umr738, inserm, university paris diderot programmer.
Bioavailability f is a measure of the systemic availability of a drug administered by a route other than iv. In the field of pharmacokinetics, the area under the curve auc is the definite integral of a curve that describes the variation of a drug concentration in blood plasma as a function of time. Binding to plasma proteins will increase the rate of passive absorption by maintaining the concentration gradient of free drug. This area under the curve is dependant on the rate of elimination of the drug from the body and the dose administered. Figures 24 and 25 repr esent two ways of thinking about drug clearance. Combining pharmacokinetics pk and pharmacodynamics pd gives an overall picture of the drug response. Overview of pharmacokinetics clinical pharmacology msd. Deals with relationship of drug dose and conc of drug in body over time important relationship between drug dosage, pharmacokinetic processes, and pharmacological response with respect to plasma drug concentration cp.
Students like that each chapter includes sample problems. Meperidine and morphine presumably combine with the same receptors to. Diagnostic and statistical manual of mental disorders, 4th ed. The first moment is calculated as concentration times time cp t. Quizlet flashcards, activities and games help you improve your grades. Use the accompanied applet and worksheet to develop formula for the area under a curve. The percent of the observed area under the first moment curve aumc that is extrapolated to infinity.
Explain the meaning of the terms absorption, distribution, metabolism, and excretion. Auc area under the curve a measure of the exposure to the drug. Auc dr nirav, md pharmacology, jamnagar it is only in the mysterious equations of love that any logical reasons can be found quote from movie a beautiful mind 2. An additional pharmacokinetic metric for bioavailability and bioequivalence assessments. Area under the curve auc analysis used to determine f f auc area under blood concentration. Scribd is the worlds largest social reading and publishing site. Clinical pharmacokinetics deals with relationship of drug dose and conc of drug in body over time important relationship between drug dosage, pharmacokinetic processes, and pharmacological response with respect to plasma drug concentration cp. Pharmacokinetics of free and total mycophenolic acid in adult lupus. You can also import data from other sources, such as databases or sas files, using the matlab workspace as an intermediate. The auc is calculated by computer or by the trapezoidal method, wherein the entire curve is divided. One determines bioavailability by comparing the area under the plasma drug concentration curve versus time auc, area under the curve for the extravascular formulation to the auc for the intravenous formulation. Population pharmacokinetics poppk characterize pk and pd in target patient population using sparse sampling and pharmacostatistical methodologies. The area is conveniently determined by the trapezoidal rule. By integrating over time rather than looking at individual concentration measurements, a more accurate estimate of the overall exposure to the drug.
Nonlinear leastsquares regression analyses determined the pkpd index the maximal unbound drug concentration fcmaxmic, the area under the unbound drug concentrationtime curve faucmic, or the percentage of a 24h time period that the unbound drug concentration exceeds the mic ftmic that was most predictive of the effect. This article is within the scope of wikiproject pharmacology, a collaborative effort to improve the coverage of pharmacology on wikipedia. Drug binding many drugs will bind strongly to proteins in the blood or to food substances in the gut. It is the measure of the rate kinetics of absorption, distribution, metabolism and excretion adme. The following pharmacological definition has been taken from the pharmacology and experimental therapeutics department glossary at boston university school of medicine. Evaluate the steadystate auc area under curve and mean trough of serum total igg for subcutaneously administered gamunexc compared to that. Mpa pharmacokinetics is characterized by the considerable inter and. Some patientrelated factors eg, renal function, genetic makeup, sex, age can be used to predict the pharmacokinetic parameters in populations. Pdf pharmacokinetics of total and unbound ertapenem in. Jan 22, 2014 contents of the powerpoint on non compartmental pharmacokinetics include. The equations and a majority of introductory concepts presented in the reading handout may be. Also, you can add more pdfs to combine them and merge them into one single document. Pharmacokinetics calculation free download as powerpoint presentation.
To be able to cross the membranes it is necessary that the drugs should be able dissolve directly. The basic calculations are based on the area under the plasma concentration versus times curve zero moment and the first moment curve aumc. Pharmacokinetics was defined as 12 of pharmacology. Area under the plasma concentrationtime curve zero, first, secondorder kinetics plasma halflife. In addition, the pharmacokinetics of elimination by the kidneys of certain radiopharmaceuticals e. D department of pharmaceutics kle university s college of pharmacy a free powerpoint ppt presentation displayed as a flash slide show on id. Area under the concentration time curve from 0 to 2 h auc02 and free fraction. Patients need to be prescribed appropriate medicines for a clinical condition. An intermediate merged input dataset is created for pk concentrations based on the clinical dm, ex. Perfluorooctanoic acid pfoa and related compounds are used primarily as surfaceactive agents in the production of various fluoropolymers and fluoroelastomers kudo and kawashima, 2003. All the four processes involve drug movement across the membranes. A peak at pk an introduction to pharmacokinetics lex jansen. Because of the strength of the carbonfluorine bond, pfoa is stable to metabolic and environmental degradation butenhoff et al.
It indicates the volume of plasma or blood from which the drug is completely removed, or cleared, in a given time period. Glossary of terms and symbols used in pharmacology. The most current, handson book in the field, applied clinical pharmacokinetics the perfect textbook for pharmacy students learning the clinical application of pharmacokinetics, which is the mathematical tools for modifying doages. Pharmacokinetics of a drug depends on patientrelated factors as well as on the drugs chemical properties. Modeling of pharmacokinetics and pharmacodynamics with. The absorption, distribution, and excretion of drugs objectives after studying this chapter, the reader should be able to. Pharmacokinetic training packet for pharmacists revised 109, 612 original document compiled by. The area under the curve auc is commonly used to assess the extent of exposure of a drug. Tp made substantial contributions to the conception and design of the work, the acquisition of data as well as revising the manuscript. Based on pharmacokineticspharmacodynamics pkpd and the minimum.
Pharm pharmacokinetics definitions flashcards quizlet. Knowing the bioavailability and the dose, the clearance of the drug may be. Phenytoin needs to be given twice or 3 times daily because it has a halflife of about 12 hours. Area under the curve or auc is a pharmacokinetic statistic used to describe the total exposure to a drug.
Area under the plasma concentration time curve auc. In practice, the drug concentration is measured at certain discrete points in time and the trapezoidal rule is used to estimate auc. The estimated area under the concentrationtime curve from 0 to 12 h. The fundamental principles of compartmental pharmacokinetics. Oct 30, 2010 pharmacokinetics auc area under curve 1. Area under the curve and bioavailability sciencedirect. Bioavailability f is a measure of the systemic availability of a drug administered by a route other than intravenous.
Pharmacokinetics is the science describing drug absorption from. By dragging your pages in the editor area you can rearrange them or delete single pages. Pharmacokinetic modeling and optimal sampling strategies for. Ppt pharmacokinetics calculations powerpoint presentation. Importance of auc pharmacokinetics measurement of bioavaibility absolute, relative biopharmaceutics comparison of drug products in babe studies calculation of pk parameters 5. A pkpd experiment consists of pharmacokinetic and pharmacodynamic measurements performed in a population of individuals. The auc is a measure of total systemic exposure to the drug. Pharmacokinetics getting to the target pharmacodynamics action at the target. In pharmacology, the area under the plot of plasma concentration of a drug versus time after dosage called area under the curve or auc gives insight into the extent of exposure to a drug and its clearance rate from the body. In pkpd it is assumed that the drug concentration is the driving force of the pharmacological e. Graphpad prism 7 statistics guide area under the curve. Introduction to noncompartmental pharmacokinetic approach differences between compartment and noncompartment models concepts of noncompartmental model statistical moments theorymean residence time different pharmacokinetic parameters in noncompartment model noncompartment pharmacokinetics is a new approach devised to. Pharmacokinetics basic calculation authorstream presentation.
The area under the plot of plasma concentration of drug not logarithm of the concentration against time after drug administration. Drugs with a higher clearance persist for a shorter time in the body. C1 time profile is regarded as expressions of exponents c1 time profile is regarded as statistical distribution. Pharmacokinetics describes how the body affects a specific xenobioticchemical after administration through the mechanisms of absorption and distribution, as well as the metabolic changes of the substance in the body e. Mathematical expressions of the pharmacokinetic and. Area under the curve from 0 to infinity aucifo when using clast. The total amount of drug eliminated by the body may. Pharm pharmacokinetics definitions study guide by broadband109 includes 30 questions covering vocabulary, terms and more.
Pharmacokinetics pk what the body does to the drug pharmacodynamics pd what the drug does to the body an outstanding overview. Overview of pharmacokinetics clinical pharmacology. Area under the plasma concentrationtime curve zero. Pk is the study of what the human body does to drugs to get the drug out of the body.
You can import into simbiology pharmacokinetics software pk and pd data of various sorts, including text files, microsoft excel files, and matlab files. The area under the curve auc from dose time to tau divided by dose time plus tau. Areas under the concentrationtime curve from 0 h to infinity auc0. Professor of clinical pharmacology, flinders university of south australia, adelaide. A single oral dose of 300 mg bioequivalent to 100 mg iv of omadacycline administered to fasted subjects achieved a maximum plasma concentration cmax of 0. The area under the curve is an integrated measurement of a measurable effect or phenomenon.
The medicine is chosen on the basis of an evidencebased approach to clinical practice and assured to be compatible with. To merge pdfs or just to add a page to a pdf you usually have to buy expensive software. The library of pharmacokinetic pk and pharmacodynamic pd models described in this. Area under the curve dr ashwin r linkedin slideshare. The equations and a majority of introductory concepts presented in. Assessment of pharmacologic area under the curve when. More specifically, it is the timeaveraged concentration of drug circulating in the body fluid analyzed normally plasma, blood or serum. It represents the area under the plasma concentration curve, also called the plasma concentrationtime profile. Stub this article has been rated as stubclass on the projects quality scale. The auc 0infinity is the area under the plasma concentrationtime curve from time zero to infinite time, calculated as the sum of auc0last and clastlambdaz. Giltinan, in encyclopedia of biostatistics, 2nd edition 6.
Clearance is the most important pharmacokinetic parameter because it determines the steadystate concentration for a given dosage rate. The area under the plasma drug concentrationtime curve auc reflects the actual. No curve fitting and no computers applicable to linear and nonlinear pharmacokinetics applicable to linear pharmacokinetics. List two physiologic factors that can alter each of the processes of absorption, distribution, and excretion. It is used as a cumulative measurement of drug effect in pharmacokinetics and as a means to compare peaks in chromatography. Davidsonx d001x medicinal chemistry chapter 7 pharmacokinetics part 3 clearance ii video clip area under curve drugs with a lower clearance persist for a longer time in the body. The area under the curve auc is proportional to the fraction absorbed only if the clearance is constant and the concentration uniform. Jul 18, 2014 shargel l, yu a 1999 applied biopharmaceutics and pharmacokinetics, 4th edn. Clinical pharmacokinetics is the discipline that describes the absorption, distribution, metabolism, and elimination of drugs in patients requiring drug therapy. Describe the physicochemical and physiological factors that influence the absorption of drugs from enteral and parenteral routes of administration, their distribution within the body, and their routes and mechanisms of elimination.
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