NR565 ADVANCED PHARMACOLOGY
FUNDAMENTALS WEEK EXAMS GRADED
A+
Pre-clincial Stage (Animal testing) of R&D
INDClinical (Safety and effectiveness)
R&DFinal Product Development
Post-marketing
1. Variations in drug development process - -ANS☑️☑️--Drug Development
Process
Drug discovery
Biological characterization (drug action/ fate)
Pre-formulation studies
Initial formulations
Manufacturing and controls
1. Package label and design - -ANS☑️☑️--Preclinical stage of R&D
Phase 1: Biological effects, safe dosage
Phase 2: New drug treats small amount of patients
2. Phase 3: Larger size, must be as good as or better than others. - -ANS☑️☑️--
Clinical Stage
target identification and validation
hit identification and screening
lead identification and optimization
1. candidate preclinical and clinical drug development - -ANS☑️☑️--Drug
Discovery
3. Drug response is continuous and gradual. The concentration increases, the
magnitude of the effect increases - -ANS☑️☑️--Graded dose response
, 4. -Graded - responses that can be measured (BP, HR, Diuresis, Bronchodilation,
Pain scale, Coma Score)
5. -Quantal Effects- may or may not occur (convulsions, pregnancy, rash, sleep,
death) - -ANS☑️☑️--Types of Drug Response
1) Inactive (R)2) Active (R*)Equilibrium favors inactive state (R) - -
ANS☑️☑️--Receptors exist in what two states?
Ligand-gated ion channel
G protein-coupled receptors
Enzyme-linked receptors
1) Intracellular receptors regulating gene expression - -ANS☑️☑️--Four
major receptor families- receptors are proteins that transduce extracellular
signals to intracellular responses
i. Rapid onset and short duration (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. - -ANS☑️☑️--Ion Channel Receptors / Gated
ion channels
-Found in cell membrane
-Made up of 3 major subunits (alpha α, beta β, gamma γ) and can have isotopes
(variations)
6. Generate intracellular second messengers that trigger a change in cell function - -
ANS☑️☑️--G protein-coupled receptors (Guanine nucleotide regulatory proteins)
FUNDAMENTALS WEEK EXAMS GRADED
A+
Pre-clincial Stage (Animal testing) of R&D
INDClinical (Safety and effectiveness)
R&DFinal Product Development
Post-marketing
1. Variations in drug development process - -ANS☑️☑️--Drug Development
Process
Drug discovery
Biological characterization (drug action/ fate)
Pre-formulation studies
Initial formulations
Manufacturing and controls
1. Package label and design - -ANS☑️☑️--Preclinical stage of R&D
Phase 1: Biological effects, safe dosage
Phase 2: New drug treats small amount of patients
2. Phase 3: Larger size, must be as good as or better than others. - -ANS☑️☑️--
Clinical Stage
target identification and validation
hit identification and screening
lead identification and optimization
1. candidate preclinical and clinical drug development - -ANS☑️☑️--Drug
Discovery
3. Drug response is continuous and gradual. The concentration increases, the
magnitude of the effect increases - -ANS☑️☑️--Graded dose response
, 4. -Graded - responses that can be measured (BP, HR, Diuresis, Bronchodilation,
Pain scale, Coma Score)
5. -Quantal Effects- may or may not occur (convulsions, pregnancy, rash, sleep,
death) - -ANS☑️☑️--Types of Drug Response
1) Inactive (R)2) Active (R*)Equilibrium favors inactive state (R) - -
ANS☑️☑️--Receptors exist in what two states?
Ligand-gated ion channel
G protein-coupled receptors
Enzyme-linked receptors
1) Intracellular receptors regulating gene expression - -ANS☑️☑️--Four
major receptor families- receptors are proteins that transduce extracellular
signals to intracellular responses
i. Rapid onset and short duration (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. - -ANS☑️☑️--Ion Channel Receptors / Gated
ion channels
-Found in cell membrane
-Made up of 3 major subunits (alpha α, beta β, gamma γ) and can have isotopes
(variations)
6. Generate intracellular second messengers that trigger a change in cell function - -
ANS☑️☑️--G protein-coupled receptors (Guanine nucleotide regulatory proteins)
