Flashcards in Exam 1: PharmacoDynamics Deck (65):
_________ is the study of the biochemical and physiologic actions of drugs, and their mechanisms of drug action at the cell level and sub-cell level...AKA-What the drug does to the body
Drugs do not impart NEW functions: they either: Produce the ____ action as the body’s own chemicals OR _____ the action of the body’s own chemicals
Action at _____ level is an interaction and binding of the drug to receptor macromolecules.
Receptors may be: metabolic or regulatory _______; proteins or ________ associated with transport mechanism; or structural and functional components of the cell membrane or _______.
A single cell may have _______ of receptor sites.
______ binding and _____ binding are the most common methods for a drug to bind to a receptor.
The AFFINITY of a drug for a particular receptor and the type of binding is intimately related to the drug’s _______.
In a typical drug interaction with a protein/glycoprotein receptor, Drug binding occurs at ______ (amino acid residues) on protein structure. (INTERESTING!)
In a typical drug interaction with a protein/glycoprotein receptor, binding to one or more amino acid residues causes a ________ change in the protein molecule.
In a typical drug interaction with a protein/glycoprotein receptor, this results in a modification of the _______ structure to bring other amino acid residues closer to the drug = called an “______ fit”.
Induced fit is also known as the "________" mechanism of binding.
"lock and key"
For drugs that bind within the cell: Receptor protein may be a structural or enzymatic component of the cell membrane = _____ of the cell membrane.
Proteins that ______ the cell membrane act as drug receptors.
The term “______” refers to the molecules that bind to the receptor protein or receptor glycoprotein.
What are the 4 possible types of ligands?
1. hormones 2. neurotransmitters 3.growth factors 4.drug molecules
When a ligand binds to a SPECIFIC area of the receptor protein on the outer surface of the cell, or within the cell membrane, a ________ occurs in the receptor-protein molecule which is transmitted to the inner surface of the cell membrane.
What are the 4 well known mechanisms by which receptors induce a response? you got this dawg
1.Ligand-Gated Ion Channels 2.G-Proteins 3.Intracellular Receptors 4.tyrosine kinase receptors
Ligand-gated ion channels are found in ______ tissues like nerves in the CNS, neuromuscular junctions, and autonomic ganglia.
For Ion Channel Receptors: The ligand binding occurs directly to ______ at channel site.
For Ion Channel Receptors: the receptors are located on ______-gated channels and ______-gated channels.
For Ion Channel Receptors: Binding causes the channel to ______, allowing for the influx of ions.
For Ion Channel Receptors: KEY POINT--->Binding increases cell membrane permeability to ______ and _______ = determines ________ or hyperpolarization of nerve = affects nerve _____.
sodium & potassium..depolarization...firing
In signal transduction: ligand binding causes a series of events which generate a ______ messenger.
Second messengers pass the message from the inside of the cell to the effector ______ (target site of action)
Some _______ receptors and _________ receptors (e.g. in the autonomic nervous system) depend on G proteins to mediate their actions on cells
What are 2 examples of receptors that generate second messengers?
1.Muscarinic Cholinergic Receptors (ACh) 2.Adrenergic Receptors (epi/norepi)
What are the 3 effectors activated in a G-Protein pathway?
1.Adenylyl Cyclase 2.Phospholipase C 3.A membrane channel
If the effector is adenylyl cyclase: the cell’s response is the generation of ______ (____).
cyclic AMP (cAMP)
If the effector is phospholipase C: the cell's response is _______ of proteins.
phosphorylation of proteins
If the effector is a membrane channel: the cell's response is a change in ______ conductance.
Where are tyrosine kinase receptors are located?
on the plasma membrane
_______ receptors are CRITICAL to cell growth and differentiation.
Tyrosine Kinase: A variety of ______ factors and certain _____ (regulate cancer growth) interact with these receptors.
Intracellular receptors are proteins associated with the nuclear matrix that are activated by _______ hormones.
The steroid-receptor complex ultimately increases binding of _____ ________ and the expression of regulated genes.
KEY FREGGIN POINT: steroid hormones interact in the cell nucleus to alter ________!!!
Receptor Specificity!! A drug will have a higher _____ for a
particular type of receptor.
An _______ drug is a drug that is able to bind to a receptor and produce an effect.
_______ drugs produce similar effects as endogenous chemicals.
For agonists drugs, Neurotransmitters, hormones, etc. (think "_______”)
An _______ drug is a drug that binds to same receptor as an agonist, but is unable to activate the receptor.
An _______ drug produces NO EFFECT!
Antagonist drugs oppose the actions of an agonist by reducing or _______ the effect.
_______ drugs are also known as “blocker” drugs e.g. beta blockers, calcium channel blockers
When BOTH agonist AND antagonist compete for the same receptor site the ________ BINDS FIRST! (in either a competitive or noncompetitive manner)
Is binding of the antagonist in competitive inhibition reversible or irreversible?
DONT WORRY! In our battle of agonist vs antagonist-- Administering additional ______ will displace the _______ from the receptor, allowing _____ to produce its effect.
A good example of a noncompetitive antagonist is ______!
Does a noncompetitive antagonist bind reversibly or irrecversibly? Where does a noncompetitive antagonist bind?
irreversibly (CANNOT BE DISPLACED)...binds to either active site or allosteric site
Our dental anesthetic is a great example of a chemical _______ because it blocks ____ channels which promote depolarization of nerves. (so depolarization does not occur=no pain)
A _______ antagonist activates pathways that oppose the action of the agonist.
hmm interesting: In Physiologic antagonism: the agonist and antagonist act ________ on ___ different receptors!
independently on 2 (less desirable in medicine)
When a drug exerts an effect on a biologic system, the effect can be ______ according to the dose given.
The ______ and effect: The dose (how much) of the drug is compared against the intensity (magnitude) of the effect.
Drug Dose and Effect
_______ refers to the amount of drug necessary to produce the effect. (think "_____")...its related to the ______ of the drug to its receptor.
_______ is the degree of maximum intensity of the effect. (think "_____" of the drug"...its related to receptor _______ by drug molecules.
In drug efficacy: Additional doses produce no additional benefit: “______ dose” occurs when all receptors are occupied (intrinsic drug activity once a drug-receptor complex is formed).
An example of _______ and ______: 300+ mg of aspirin for moderate pain, while 25mg of meperidine is used for moderate pain.
potency and efficacy
Example of Meperidine and Morphine: 100mg meperidine for severe pain, 10mg morphine for severe pain. They are SIMILAR in ______, but DIFFER in ______.
________: The range of the doses (concentrations) of a drug that elicits a therapeutic response, without unacceptable side effects (toxicity) in a population of people.
Blood plasma levels of a drug with a ______ therapeutic window must be monitored closely to maintain effective dosing without exceeding the level that could produce toxicity.
TD50: dose that causes _____ response in 50% of the population....ED50: does that is ______ in 50% of the population.... Theraputic Index= _____ / _____
Toxic..effective...TD50 / ED50
The ________ provides a single number that quantifies the relative margin of safety of a drug in a population of people (this is similar to the margin of safety which is done in animals)
A large _______ represents a large (or “wide”) therapeutic window.