Pharmacodynamics Flashcards
Study of detailed MECHANISM OF ACTION by which drugs produce their pharmacologic effects
Pharmacodynamics
Pharmacodynamics is the relationship between
Drug concentration
Site of action
Receptors are also known as
Substrates
Specific molecules in a biological system with which DRUGS INTERACT to produce change
Receptors
It is the BIOLOGIC SITE of action
Receptors
Are receptors selective or non-selective
Selective
Ability of the drug molecule to BIND
Affinity
Ability of the drug to GENERATE AN IMPULSE
Intrinsic activity
It is the CAPACITY TO BIND
Have AFFINITY and INTRINSIC activity
Agonist
Capable of FULLY ACTIVATING the effector organ
Produce ALL EXPECTED EFFECTS
Full agonist
Example of full agonist
Opioids-morphine
Produce LESS THAN FULL effect when receptors are saturated
Acts as ANTAGONIST with full agonist
Partial agonist
Have more AFFINITY to the INACTIVE SITE
Inverse agonist
Example of partial agonist
Tramadol
Bucrenorphine
Example of inverse agonist
Benzodiazepine
Roles of receptors
Determine quantitative relationship of drug dose concentration and pharmacologic effects
Responsible for selectivity of drug action
Meditate actions of pharmacologic effect
Has affinity WITHOUT intrinsic activity
Antagonist
2 agonists in DIFFERENT receptors=opposite effects
Physiological antagonism
Physiological antagonism has no
Direct effect
Example of physiological antagonism
Epinephrine during anaphylaxis
2 drugs to SAME receptor
Pharmacologic antagonism
Example of pharmacologic antagonism
Dobutamine and propanolol
INACTIVATION due to chemical interaction
Chemical antagonism
Example of chemical antagonism
Heparin overdose- Protamine sulfate
Dimercaprol- Lead poisoning
A British anti lewisite
Dimercaprol
ALTERATION of pharmacokinetic parameters
Dispositional or pharmacokinetic interaction
Example of dispositional or pharmacokinetic interaction
Activated charcoal and ipecac for poisoning
Antagonist binds in NON-COVALENT LINKS
Reversible-competitive
Example of reversible antagonism
Naloxone
Flumazenil
Antagonist binds in COVALENT LINKS
Irreversible/non-competitive
Aspirin is irreversible inhibitor of
Organophosphate is irreversible inhibitor of
Prasugrel is irreversible inhibitor of
COX
Acetylcholinesterase
P2Y12 receptors
Agonist in high concentrations can DISPLACE
Competitive antagonism
August in high concentrations CANNOT DISPLACE
Non-competitive
Hypothesis of Clark follows what law
Law of mass action
The pharmacological effect friends on the PERCENTAGE OF RECEPTORS
Must have AFFINITY
ALL receptors occupied=MAXIMUM effect
Hypothesis of Clark
Effectiveness last as long as the receptor is OCCUPIED
Occupation theory
Hypothesis of Ariens and Stephenson
Effectiveness does not depend in occupation but on the ATTACHMENT of the drug
Hypothesis of Paton
Rate theory
The most COMMON
FIT into the receptor
Lock and key hypothesis
Drug will BIND to the ACTIVE SITE of protein
Target-protein meditate
Proteins/biomolecules that form CELL FRAMEWORK/CYTOSKELETON
Structural proteins
Example mitotic agents
Ability to REGULATE cellular activity or function
Regulatory proteins
Conduct changes in ELECTRICAL SIGNALS
Movement of IONS
Voltage-gated channels
Cell membrane proteins with SPECIFIC BINDING SITES which undergo conformational changes
Movement of IONS (SPECIFIC)
Carriers
Biological CATALYSTS
Enzymes
What receptors have TRANSPORTERS
Ligand-gated ion channel
Role of ligand-gated ion channel
REGULATE movement of IONS and produce action
Gs
Gi
Gq
Stimulatory to adenylyl cyclase = increase camp
Inhibitory = decrease
Releases phospholipase c = release of calcium in SR
What is the receptor involved
Gs
Gi
Gq
B1 Tachycardia
M2 Bradycardia
A2 Contraction
Role of G-protein coupled or Metabotropic
REGULATE activity of ENZYMES
Role of enzyme linked
Binds with RNA POLYMERASE and REGULATE expression of HORMONES
Regulates movement of calcium
Parathyroid hormone
Example of an ADH
Vasopressin
Role of gene transcription
Cell growth and differentiation
No relationship towards drug and protein mechanism
Non target-protein mediated
What non target-protein is MANNITOL
Colligative mechanism
What non target-protein are ANTACIDS
Direct chemical
Acid-base neutralization
What non target-protein are ANTIDOTES
Direct chemical
Complexation/Chelation