安徽医科大学国际教育学院教案与讲稿 [Drug Distribution] 6min Factors influencing distribution: 1.Binding of drugs to plasma proteins: ·Reversible A bound drug has no effect ·Nonspecific Competitive displacement Renal failure,fasting,malnutrition can have effect on plasma protein binding 2.Physiological barriers to drug distribution:Blood-Brain Barrier,Placental Barrier 3.Blood flow 4.Selective accumulation of drugs [Drug Metabolism(Biotransformation)] 8min 1.Consequences of drug metabolism:inactive,active drug form,Toxic metabolite 2.General Metabolic Pathways:Phase I Reactions,Phase II Reactions 3.Enzymes Involved in Drug Metabolism:Cytochrome P450 Enzymes(CYP450) Characteristics of CYPs:Low Specificity Genetic variability Enzyme induction or inhibition 4.Factors Influencing Drug Metabolism ·Genetic variability ·Age Clinical or physiological condition Other drug administration (induction or inhibition) ·Food [Drug Excretion] 8min 1.Types of Excretion:Renal excretion,Non-renal excretion 2.Renal excretion of drugs: Glomerular filtration Active tubular secretion Active or passive tubular reabsorption 3.Factors Affecting Renal Excretion/Clearance Physicochemical properties of drug ·Urine pH Blood flow to the kidney Biological factors(Age,sex,species etc.) ·Disease state Review of Basic Pharmacokinetic Parameters 15min 1.Drug concentration-time profiles and AUC AUC can be used to assess the person's overall exposure to a drug. 2.Half-life 3安徽医科大学国际教育学院教案与讲稿 3 [Drug Distribution] 6min Factors influencing distribution: 1. Binding of drugs to plasma proteins:
Reversible
A bound drug has no effect
Nonspecific
Competitive displacement
Renal failure, fasting, malnutrition can have effect on plasma protein binding 2. Physiological barriers to drug distribution: Blood-Brain Barrier, Placental Barrier 3. Blood flow 4. Selective accumulation of drugs [Drug Metabolism (Biotransformation) ] 8min 1. Consequences of drug metabolism: inactive, active drug form, Toxic metabolite 2. General Metabolic Pathways: Phase I Reactions, Phase II Reactions 3. Enzymes Involved in Drug Metabolism: Cytochrome P450 Enzymes (CYP450) Characteristics of CYPs: Low Specificity Genetic variability Enzyme induction or inhibition 4. Factors Influencing Drug Metabolism
Genetic variability
Age
Clinical or physiological condition
Other drug administration (induction or inhibition)
Food [Drug Excretion] 8min 1. Types of Excretion: Renal excretion, Non-renal excretion 2. Renal excretion of drugs:
Glomerular filtration
Active tubular secretion
Active or passive tubular reabsorption 3. Factors Affecting Renal Excretion/Clearance
Physicochemical properties of drug
Urine pH
Blood flow to the kidney
Biological factors (Age, sex, species etc.)
Disease state [Review of Basic Pharmacokinetic Parameters] 15min 1. Drug concentration-time profiles and AUC AUC can be used to assess the person’s overall exposure to a drug. 2. Half-life