NOTES MEDICAL PHARMACOLOGY
Lecture 1: Introduction Medicine
● Pharmacodynamics: what the drug does with the body
● Pharmacokinetics: what the body does with the drug
● Effects of drugs:
○ primary effect: reason and effect for what the compound is given
○ side effect: adverse/unwanted effect
■ DIFFERENCE: determined by AIM of the drug
○ Placebo: no pharmacologically active substance
■ placebo effect: therapeutic effect = strength depends on
expectation
○ Nocebo: placebo with unwanted effects (Side effects)
● Drug approval = 9-14 years
○ drug discovery (2-5 years)
○ drug development (5-9 years)
○ post approval regulation
Lecture 2: Receptor Theory
● 4 Levels of Drug Action and Classification:
○ 1. System: effect on system function
■ NS, cardiovascular system
○ 2. Tissue: effect on tissue function
■ contractions, electrical pulses, metabolic activity
○ 3. Cellular: transduction (transfer of viral DNA from one bacteria to
another and later to host cells)
■ ex: affects ion channels, enzymes, G-protein
○ 4. Molecular: interaction with drug molecular target
■ ex: receptor, ion channel, enzymes
● Drug Targets:
○ RECEPTORS:
, ○ ION CHANNELS:
○ ENZYMES: / pro-drug = reduces side effects due to high selectivity
○ TRANSPORTERS: / ex of false substrate = Cocaine
● 4 Receptor Families:
○ Type I: Ligand-gated Ion Channels (ionotropic
receptor)
■ in membrane
○ Type II: G-protein Coupled Receptor
(metabotropic receptor)
■ in membrane
■ activates second messengers
○ Type III: Kinase-Linked Receptors
■ in membrane
■ alters kinase activity
○ Type IV: Nuclear Receptors (Transcription
factors)
■ located in cytosol and after binding move
to nucleus
, ● Example of Receptors:
○ 1. Ionotropic: ex: Nicotinic Receptors (for ACh)
■ ACTIVATION = milliseconds
○ 2. Metabotropic: ex: Muscarinic Receptors (for ACh)
■ ACTIVATION = seconds
○ 3. Kinase-Linked: ex: Cytokine Receptors (for insulin)
■ ACTIVATION = hours
○ 4. Nuclear Receptors: ex: Oestrogen Receptor (transcription factor)
■ ACTIVATION = Hours
● TERMS:
○ affinity: tendency to bind to receptor (dose-effect relationship)
○ efficacy: relation between receptor occupancy and ability to start a
response at system, tissue, cellular, or molecular level
○ intrinsic activity: capacity of one drug-receptor complex to cause a
response
■ Occupation depends on AFFINITY
■ Activation depends on EFFICACY
● Agonist affects BOTH
● Antagonist affects OCCUPATION = there is no activation
● Dose-Response Relations:
○ RECEPTOR THEORY CRITERIA
■ agonist binds in reversible manner
■ agonist has high affinity for receptor
■ agonist concentration is not altered as binding to receptor
(constant concentration)
■ agonist efficacy is proportionate to occupancy of receptor at
increasing drug concentration
Lecture 1: Introduction Medicine
● Pharmacodynamics: what the drug does with the body
● Pharmacokinetics: what the body does with the drug
● Effects of drugs:
○ primary effect: reason and effect for what the compound is given
○ side effect: adverse/unwanted effect
■ DIFFERENCE: determined by AIM of the drug
○ Placebo: no pharmacologically active substance
■ placebo effect: therapeutic effect = strength depends on
expectation
○ Nocebo: placebo with unwanted effects (Side effects)
● Drug approval = 9-14 years
○ drug discovery (2-5 years)
○ drug development (5-9 years)
○ post approval regulation
Lecture 2: Receptor Theory
● 4 Levels of Drug Action and Classification:
○ 1. System: effect on system function
■ NS, cardiovascular system
○ 2. Tissue: effect on tissue function
■ contractions, electrical pulses, metabolic activity
○ 3. Cellular: transduction (transfer of viral DNA from one bacteria to
another and later to host cells)
■ ex: affects ion channels, enzymes, G-protein
○ 4. Molecular: interaction with drug molecular target
■ ex: receptor, ion channel, enzymes
● Drug Targets:
○ RECEPTORS:
, ○ ION CHANNELS:
○ ENZYMES: / pro-drug = reduces side effects due to high selectivity
○ TRANSPORTERS: / ex of false substrate = Cocaine
● 4 Receptor Families:
○ Type I: Ligand-gated Ion Channels (ionotropic
receptor)
■ in membrane
○ Type II: G-protein Coupled Receptor
(metabotropic receptor)
■ in membrane
■ activates second messengers
○ Type III: Kinase-Linked Receptors
■ in membrane
■ alters kinase activity
○ Type IV: Nuclear Receptors (Transcription
factors)
■ located in cytosol and after binding move
to nucleus
, ● Example of Receptors:
○ 1. Ionotropic: ex: Nicotinic Receptors (for ACh)
■ ACTIVATION = milliseconds
○ 2. Metabotropic: ex: Muscarinic Receptors (for ACh)
■ ACTIVATION = seconds
○ 3. Kinase-Linked: ex: Cytokine Receptors (for insulin)
■ ACTIVATION = hours
○ 4. Nuclear Receptors: ex: Oestrogen Receptor (transcription factor)
■ ACTIVATION = Hours
● TERMS:
○ affinity: tendency to bind to receptor (dose-effect relationship)
○ efficacy: relation between receptor occupancy and ability to start a
response at system, tissue, cellular, or molecular level
○ intrinsic activity: capacity of one drug-receptor complex to cause a
response
■ Occupation depends on AFFINITY
■ Activation depends on EFFICACY
● Agonist affects BOTH
● Antagonist affects OCCUPATION = there is no activation
● Dose-Response Relations:
○ RECEPTOR THEORY CRITERIA
■ agonist binds in reversible manner
■ agonist has high affinity for receptor
■ agonist concentration is not altered as binding to receptor
(constant concentration)
■ agonist efficacy is proportionate to occupancy of receptor at
increasing drug concentration
