This document provides an introduction to clinical pharmacokinetics. It defines key terms like volume of distribution, half-life, bioavailability, steady state, and elimination rate constant. It discusses one compartment and two compartment models. Factors that influence pharmacokinetics are also covered, including physiological, biological, and formulation factors. The goal of clinical pharmacokinetics is to enhance efficacy and decrease toxicity by ensuring adequate drug doses reach target tissues.
This document provides an introduction to clinical pharmacokinetics. It defines key terms like volume of distribution, half-life, bioavailability, steady state, and elimination rate constant. It discusses one compartment and two compartment models. Factors that influence pharmacokinetics are also covered, including physiological, biological, and formulation factors. The goal of clinical pharmacokinetics is to enhance efficacy and decrease toxicity by ensuring adequate drug doses reach target tissues.
This document provides an introduction to clinical pharmacokinetics. It defines key terms like volume of distribution, half-life, bioavailability, steady state, and elimination rate constant. It discusses one compartment and two compartment models. Factors that influence pharmacokinetics are also covered, including physiological, biological, and formulation factors. The goal of clinical pharmacokinetics is to enhance efficacy and decrease toxicity by ensuring adequate drug doses reach target tissues.
Lecturer Faculty of Pharmacy Hajvery University (HU) Learning outcomes Students will learn in this lecture about; • Introduction to Clinical Pharmacokinetics • Pharmacokinetics terminologies. Clinical pharmacokinetics • Mathematical interpretation and calculation of ADME. or • Study of time course of ADME and their corresponding pharmacological response. • There are some factors to be study are as follow: • Physicochemical factors, Biological and Formulation factors. • Goal is to enhances the efficacy and decreasing toxicity. • To prevent cure or control of disease state. • Adequate drug doses must be deliver to target tissues, directly sample the drug concentration in blood, plasma, saliva, urine and other fluid samples. Pharmacological terminologies Vd: • It is the hypothetical volume of fluid into which drug is disseminated. its expressed in L. • C=A/Vd where A=amount of drug in body C=concentration of drug in plasma • after administration of drug,initially the plasma concentration falls rapidly after distribution and elimination.However when equilibrium reached then changes in plasma concentration is due to elimination and it falls at slower rate then drug follows two compartment model. • however if drug is quickly distribute then alpha phase is not seen then drug follows one compartment model. • beta phase indicates elimination. Half life: • Time required for serum concentration to decrease by one half of original value. • concentration of drug in plasma or in body is reduced to half of original value. • t1/2=0.693/k(cl) Bioavailability: • the fraction of dose administered which is observed and reaches the systemic circulations. Bioavailability of IV route is 100%. Steady state: • at steady state drug administration is equal to drug elimination and mean concentration remains constant. elimination rate constant: • the fraction or amount of drug in body eliminate per unit time. creatinine clearance: • Creatinine is the metabolic by product of muscle and individual muscle mass or lean body wt. Primarily determine its rate of formation. Its is expressed in ml/min. • Crock-Craft and Gault equation; • CrCl (males) = (140-age) IBW / Scr × 72 • CrCl (females) = CrCl (males) × 0.85 • IBW • Males =50kg +2.3kg for each inch over 5ft • Females= 45.5kg+ 2.3kg for each inch over 5ft Half life (zero order) • Half life in zero order kinetic reaction is directly proportional to the initial concentration of reactants. Half life (First order) • Half life in first order kinetics reactions are independent of initial concentration. • t1/2= 0.693/ Kel one compartment model • Immediate and uniform • Complete drug distribution into single compartment followed by elimination. two compartment model • Distribution initially to central compartment followed by a gradual equilibrium with peripheral compartment. Therapeutic index: • Ratio between the effective dose and toxic dose of drugs. It is the comparison of amount of therapeutic agent that causes the therapeutic effect, to the amount the causes the toxicity. T.I= TD50 / ED50 Systemic drug concentration: • Amount or concentration of drug present in systemic circulation both bound to proteins or unbound the latter of which generally response to the therapeutical active function. Dose regimen • Dose of the drug given at regular intervals in repetitive manner.
individualized dosage regimen
• Dosage individualization is an adaptation of dosage regimen in function of clinical characteristics of the individual to achieve the best possible outcomes or therapeutic efficacy at lowest risk of toxicity. First order elimination • Rate of biotransformation is proportional to amount of drug in apparent compartment in which the site of biotransformation is located. • A directly proportionality exist between drug concentration at any specific time and size of dose. Zero order elimination Here the drug concentration and Kel is constant. It is independent of concentration of drug. Summary The student have learnt about the: • Introduction to Clinical Pharmacokinetics • Pharmacokinetics terminologies. THANK YOU!! ANY QUESTIONS!!!! Students you can ask any question regarding this lecture. Google Classroom discussion board.