NR 565 Advanced
Pharmacology Fundamentals
– Week 1 Study Guide, Key
Concepts, and Practice
Review
Pre-clincial Stage (Animal testing) of R&D Drug Development Process
INDClinical (Safety and effectiveness)
R&DFinal Product Development
Post-marketing
Variations in drug development process
1. Drug discovery Preclinical stage of R&D
2.Biological characterization (drug action/
fate)
3.Pre-formulation studies
4. Initial formulations
5. Manufacturing and controls
6.Package label and design
Phase 1: Biological effects, safe dosage Clinical Stage
Phase 2: New drug treats small amount of
patients
Phase 3: Larger size, must be as good as or
better than others.
, 1. target identification and validation Drug Discovery
2.hit identification and screening
3.lead identification and optimization
4. candidate preclinical and clinical drug
development
Drug response is continuous and Graded dose response
gradual. The concentration increases, the
magnitude of the effect increases
-Graded - responses that can be measured Types of Drug Response
(BP, HR, Diuresis, Bronchodilation, Pain
scale, Coma Score)
-Quantal Effects- may or may not occur
(convulsions, pregnancy, rash, sleep, death)
1) Inactive (R)2) Active (R*)Equilibrium Receptors exist in what two states?
favors inactive state (R)
1) Ligand-gated ion channel Four major receptor families- receptors are proteins that
2)G protein-coupled receptors transduce extracellular signals to intracellular responses
3) Enzyme-linked receptors
4) Intracellular receptors regulating gene
expression
- Rapid onset and short duration Ion Channel Receptors / Gated ion channels
(muscle contraction)
Transmit signals across the cell
membrane by increasing the flow of ions
and altering the electrical potential or
separation of
charged ions across the membrane
Gated Ion Channel Receptors:
Open or close channels to allow certain
ions to pass through cell membrane.
A gated channel for a specific ion. The
opening or closing of such channels may
alter a cell's membrane potential.
-Found in cell membrane G protein-coupled receptors (Guanine nucleotide regulatory
-Made up of 3 major subunits (alpha α, beta proteins)
β, gamma γ) and can have
isotopes (variations)
Generate intracellular second messengers
that trigger a change in cell function
Pharmacology Fundamentals
– Week 1 Study Guide, Key
Concepts, and Practice
Review
Pre-clincial Stage (Animal testing) of R&D Drug Development Process
INDClinical (Safety and effectiveness)
R&DFinal Product Development
Post-marketing
Variations in drug development process
1. Drug discovery Preclinical stage of R&D
2.Biological characterization (drug action/
fate)
3.Pre-formulation studies
4. Initial formulations
5. Manufacturing and controls
6.Package label and design
Phase 1: Biological effects, safe dosage Clinical Stage
Phase 2: New drug treats small amount of
patients
Phase 3: Larger size, must be as good as or
better than others.
, 1. target identification and validation Drug Discovery
2.hit identification and screening
3.lead identification and optimization
4. candidate preclinical and clinical drug
development
Drug response is continuous and Graded dose response
gradual. The concentration increases, the
magnitude of the effect increases
-Graded - responses that can be measured Types of Drug Response
(BP, HR, Diuresis, Bronchodilation, Pain
scale, Coma Score)
-Quantal Effects- may or may not occur
(convulsions, pregnancy, rash, sleep, death)
1) Inactive (R)2) Active (R*)Equilibrium Receptors exist in what two states?
favors inactive state (R)
1) Ligand-gated ion channel Four major receptor families- receptors are proteins that
2)G protein-coupled receptors transduce extracellular signals to intracellular responses
3) Enzyme-linked receptors
4) Intracellular receptors regulating gene
expression
- Rapid onset and short duration Ion Channel Receptors / Gated ion channels
(muscle contraction)
Transmit signals across the cell
membrane by increasing the flow of ions
and altering the electrical potential or
separation of
charged ions across the membrane
Gated Ion Channel Receptors:
Open or close channels to allow certain
ions to pass through cell membrane.
A gated channel for a specific ion. The
opening or closing of such channels may
alter a cell's membrane potential.
-Found in cell membrane G protein-coupled receptors (Guanine nucleotide regulatory
-Made up of 3 major subunits (alpha α, beta proteins)
β, gamma γ) and can have
isotopes (variations)
Generate intracellular second messengers
that trigger a change in cell function
