3/13EXAM 2 Reading 1 (N.Ch5) Flashcards
How will the chronic administration of an antagonist affect the number and sensitivity of the receptors it antagonizes?
The NUMBER and SENSITIVITY of the receptors INCREASE
When do receptors become UPREGULATED?
When chronically exposed to an antagonist, the receptors upregulate, which means that both the number of receptors and their sensitivity both increase.
Therapeutic index describes the
average safety margin for the drug for a specific therapeutic effect
What is often used to compare the potency of two different drugs?
The ED50
The lower the ED50, the more /Less potent the drug is.
More
If you divide the ED50 by the LD50, you get the
Therapeutic Index
The pharmacological theory that states that the magnitude of the effect of a drug is proportional to the number of receptors it occupies is known as the
Occupancy Theory
What is the occupancy theory
Magnitude of drug effect is proportional to the number of receptors it occupies
Which of the following types of chemical bonds is the strongest?
Covalent bonds
Which of the following types of chemical bonds is the strongest?
Covalent bonds
Which of the following types of chemical bonds is the Weakest>
Van der Waals forces are the weakest of these
Which of the following types of chemical bonds is the Weakest?
Van der Waals forces are the weakest of these
A chemical that can bind with a protein to form a new complex is a
A ligand is any chemical that can bind with a protein to form another complex.
Typically, it is a signal triggering molecule that binds with a target protein.
Ligand
Determining the safety margin of a drug requires that you know data about the effective dose of the drug and
the lethal dose
Determining the safety margin of a drug
If you take the LD1, which is the dose of the drug that is lethal in 1% of the population and subtract the ED99, which is the effective dose in 99% of the population, and then divide it by the ED99 times 100, you get the safety margin of the drug.
An antagonist has affinity for a receptor but lacks
Efficacy
Efficacy refers to the Antagonist
ability of a drug to produce the conformational change in the receptor necessary to elicit a tissue response.
A drug that has an affinity for a receptor but lacks efficacy is an a
Antagonist
Drug has both affinity and efficacy.
Agonist
can bind with the receptor and has some efficacy, but it cannot elicit the maximal tissue response.
Partial agonist
can bind with the receptor, but results in the opposite reaction of an agonist.
An inverse agonist
A drug that binds to a receptor and activates it is referred to as
Agonist
Characteristics of G-protein receptors include: (select four)
modulation of ligand channels
activation of adenylyl cyclase
inhibition of adenylyl cyclase
activation of phospholipase C
Which of the following molecular binding forces is the weakest?
Van de waars
Reaction of reversible with this bonding
Van de waars
The ability of a drug to bind with a receptor to form a stable complex is referred to as the drug’s
Affinity
Efficacy refers to the
dose-response curve produced by the binding of the opioid to an opioid receptor.
Potency refers to the
relative dose of a drug that is required to produce the effect and is closely associated with the affinity of the drug for the receptor.
