Week 3 Pharmacodynamic Flashcards
What does pharmacology define a receptor as
A biologic molecule to which drug binds and produces a measurable response
Hydrophobic ligands interact with receptors that are found ?
Cell cerface of families 123
- Ligand gated ion chanels
- G protein coupled receptors
- Enzyme- linked receptors
The hydrophobic ligans can enter into the cells through the lipid bilayer to interact with ?
Intracellular receptors
Family 4
Function of the ligand gated ion channels
They regulate the flow of ions across the cell membranes
Examples of the ligand gated ion channel
Nicotinic receptors and gama aminobutyric acid
The alpha receptor in g protein binds to what
Gtp ( guanosine triphosphate)
A common effector activated by g and inhibited by gi is
Adenylyl cyclase
Adenylyl cyclase produces the second messenger
Camp ( cyclic adenosine monophosphate )
Gq activates?
Phospholipase c
Phospholipase c generates 2 messengers
Inositol 1,4,5 triphosphate ip3 and diacylglycerol (DAG)
The most common enzyme linked receptors is
Rtk ( receptor tyrosine kinase)
The active form of kinase are
Autophosphorylate and phosphorylate
In the intracellular receptors what are the receptors binding to in order to be transported in the body
Plasma proteins such as albumin
What defines the strength of attraction between drugs and its receptors
Affinity
Potency of drugs can be compared using ?
EC50 values
A smaller EC50 value means?
A strong drug
When is a drug a full agonist
If a drug binds to a receptor and produces a maximal biologic response
Example of a partial agonist
Aripiprazole
Function of inverse agonist
They reverse the activity of receptors and exert the opposite pharmacological effects of agonist
A drug that counters the effect of another drug by binding to a different receptor and causing opposing effect is
Physiological antagonism eg
Noradrenaline and nitrate
Glucocorticoid hormones and insulin
Pharmacological antagonist
It binds to the same site as the agonist and prevents the binding of the agonist against the receptors
Divided into competitive antagonism and non competitive antagonism
Which of the agonist binds covalently to the active site of the receptors
Non competitive
Two types of synergysim
Additive = the effect of the drugs sums up
Potantialization
= the effect is greater than the sum of two drugs
Drugs can bind to
Enzymes , nuclieic Acids or membrane receptors
What chemical bonds are formed from
The interaction of receptors with ligands
Electrostatic and hydrogen bond
Steriod hormone exert their action on target cells through
Intracellular receptors
What is efficacy
Ivivo potency: max response achieved from a drug
What is the measure of safety in drugs
Therapeutic index
Example of physiological antagonism
Noradrenaline and nitrate
Glucocorticoids and insulin
