The learning objectives of the pharmacokinetic course are: 1) understand the meaning of the basic pharmacokinetic parameters (distribution and clearance, bioavailability) and secondary ones (elimination constant, half-life, etc.). 2) Know how to determine pharmacokinetic parameters from the concentration-time curve data. 3) Understand the influence of the mode of administration and the various therapeutic regimens on the plasma concentration-time profile and predict the effect on it of clearance changes, distribution volume, and other specific patient characteristics.
Course Prerequisites
Basics of basic mathematics already used in chemistry and physics courses. Knowledge of biochemical chemistry and physiology. The student must have some concepts of chemical kinetics, i.e. zero and first order processes, however taught in the course.
Teaching Methods
Presentations (PowerPoint) front-facing lectures projected on-screen and insights using the blackboard.
Assessment Methods
The exam will be carried out together with the other pharmacology modules 1 in a single test. It will be a written examination consisting of multiple choice and open questions based on didactic material used in the course, carried out in the presence with a PC or other electronic device. The evaluation will be carried out with a weighted average in relation to the number of credits of each part. Graphics is emphasized: students must know how to draw plasma concentration - time curves, etc.
Texts
Laurence Brunton et al., Goodman and Gilman's Le basi farmacologiche della terapia, 13a Edizione, Zanichelli, Bologna, 2019. M. Fuccella, E. Perucca, C. Sirtori - Farmacologia Clinica. UTET 2006. Stephen H. Curry, Robin Whelpton, Introduction to Drug Disposition and Pharmacokinetics 2017 John Wiley & Sons, Ltd
Contents
Introduction to pharmacokinetics: absorption, distribution and elimination (metabolism and excretion). Phases of the action of a drug. Systemic drug absorption. Movement of drugs through cellular barriers: mechanisms, factors influencing absorption. Drug administration routes. Modified Release Forms. Clinical pharmacokinetics, pharmacodynamics, kinetic homogeneity, models. Exponents and logarithms. Meaning of differential calculus, differential equations, integral calculus. AUC determination by trapezoidal rule. Orders of kinetic: zero- and first-order kinetics, Michaelis-Menten kinetic. Pharmacokinetics models: one-compartment and multiple compartments models. Non compartment model. Concentration-vs-time curves, linear plots, semi-log plots. i.v. (bolus) single dose administration. Pharmacokinetic parameters associated with models and their calculation: C0, volume of distribution, clearance, elimination rate constant, half-life. Distribution: definitions, factors affecting drug distribution (characteristics of drug, characteristics of barrier to be crossed, regional blood flow, drug plasma and tissue protein binding, physiological factors and disease states. Blood-brain barrier and placenta transfer of drugs. Clearance: total plasma or blood clearance, organ clearance, extraction ratio. Hepatic clearance, low and high hepatic extraction ratio drugs, renal clearance. Absolute and relative bioavailability. Route and frequency of administration: i.v. continuous constant rate infusion with and without reaching steady state; extra vascular administration and related parameters, single and multiple doses. Generic drugs, biotechnological and biosimilar drugs. Pharmacokinetic interactions.
Course Language
Italian
More information
The lecturer will provide .pdf presentations and other study materials of the topics discussed. It is also available on request for explanations to groups or individual students by appointment.