浙江大学：《药理学》课程教学资源（PPT课件）药代动力学 Pharmacokinetics

Chapter 3 Pharmacokinetics 口 PK process in the body S,D Kinetic processes

Chapter 3 Pharmacokinetics PK process in the body Kinetic processes

Parta Pharmacokinetic processes D 1 Overview D 2 Transport of Drug in the Body 0 3 Pharmacokinetic Processes of the Drug 口 in the Body

Part A Pharmacokinetic Processes 1 Overview 2 Transport of Drug in the Body 3 Pharmacokinetic Processes of the Drug in the Body

1. Overview LOCUS OF ACTION TISSUE " RECEPTORS" RESERVOIRS bound free free- bound SYSTEMIC CIRCULATION ABSORPTION free drug EXCRETION bound drug metabolites BIOTRANSFORMATION

1. Overview

Drug at site of administration 1 Absorption (input) ADME Drug in plasma of the drug in 2 Distribution human body Drug in tissues + Metabollsm Metabolite(s) in tissues 4 Elimination Drug and/or metabolite(s) t in urine, feces, bile

ADME of the drug in human body

Part a Pharmacokinetic processes I 2. Transport of Drug in the Body u 2.1 Transmembrane Transport of D rus I (1)Passive Transport 口 Simple diffusion(简单扩散) 口 Filtration(滤过)

2. Transport of Drug in the Body 2.1 Transmembrane Transport of Drugs (1) Passive Transport Simple diffusion（简单扩散） Filtration（滤过） Part A Pharmacokinetic Processes

Part a Pharmacokinetic processes u Characteristics of Passive Transport 口口口口口口 not involving specific carriers Energy-independent no saturability no competition with other drugs Concentration gradient(down-hill)

Characteristics of Passive Transport not involving specific carriers Energy-independent no saturability no competition with other drugs Concentration gradient (down-hill) Part A Pharmacokinetic Processes

Part a Pharmacokinetic processes 口(2) Active Transport o Characteristics of active transport o Involving specific carrier aEnergy-dependent 口 Saturability o Competition at same carrier o Moving against concentration gradient(up-hill)

(2) Active Transport Characteristics of active transport Involving specific carrier Energy-dependent Saturability Competition at same carrier Moving against concentration gradient (up-hill) Part A Pharmacokinetic Processes

Part a Pharmacokinetic processes 口(3) Others 口 Filtration through pores(膜孔滤过) 口 Facilitated diffusion(易化扩散) 口 Endocytosis(内吞) 囗 Pinocytosis(胞饮) 口Ion- pair transport(离子对转运)

(3) Others Filtration through pores（膜孔滤过） Facilitated diffusion（易化扩散） Endocytosis（内吞） Pinocytosis（胞饮） Ion-pair transport（离子对转运） Part A Pharmacokinetic Processes

Transporter Receptor Channel Three types offunctional membrane proteinS

Three types of functional membrane proteins

ATP choroid plexus (BCSFB) B rain aln brain capillary (BBB) hepatocyte OAT OAT proximal tubular cell Transporters OCTOCT 之 ept of drugs in PK ATr' 数式 processes Mrn tp MI ver kidney ATP Per Pgp intestine

Transporters of drugs in PK processes