3/13EXAM 2 Reading 1 (N.Ch5) Flashcards

1
Q

How will the chronic administration of an antagonist affect the number and sensitivity of the receptors it antagonizes?

A

The NUMBER and SENSITIVITY of the receptors INCREASE

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2
Q

When do receptors become UPREGULATED?

A

When chronically exposed to an antagonist, the receptors upregulate, which means that both the number of receptors and their sensitivity both increase.

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3
Q

Therapeutic index describes the

A

average safety margin for the drug for a specific therapeutic effect

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4
Q

What is often used to compare the potency of two different drugs?

A

The ED50

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5
Q

The lower the ED50, the more /Less potent the drug is.

A

More

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6
Q

If you divide the ED50 by the LD50, you get the

A

Therapeutic Index

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7
Q

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

A

Occupancy Theory

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8
Q

What is the occupancy theory

A

Magnitude of drug effect is proportional to the number of receptors it occupies

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9
Q

Which of the following types of chemical bonds is the strongest?

A

Covalent bonds

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10
Q

Which of the following types of chemical bonds is the strongest?

A

Covalent bonds

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11
Q

Which of the following types of chemical bonds is the Weakest>

A

Van der Waals forces are the weakest of these

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12
Q

Which of the following types of chemical bonds is the Weakest?

A

Van der Waals forces are the weakest of these

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13
Q

A chemical that can bind with a protein to form a new complex is a

A

A ligand is any chemical that can bind with a protein to form another complex.

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14
Q

Typically, it is a signal triggering molecule that binds with a target protein.

A

Ligand

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15
Q

Determining the safety margin of a drug requires that you know data about the effective dose of the drug and

A

the lethal dose

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16
Q

Determining the safety margin of a drug

A

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.

17
Q

An antagonist has affinity for a receptor but lacks

A

Efficacy

18
Q

Efficacy refers to the Antagonist

A

ability of a drug to produce the conformational change in the receptor necessary to elicit a tissue response.

19
Q

A drug that has an affinity for a receptor but lacks efficacy is an a

A

Antagonist

20
Q

Drug has both affinity and efficacy.

A

Agonist

21
Q

can bind with the receptor and has some efficacy, but it cannot elicit the maximal tissue response.

A

Partial agonist

22
Q

can bind with the receptor, but results in the opposite reaction of an agonist.

A

An inverse agonist

23
Q

A drug that binds to a receptor and activates it is referred to as

A

Agonist

24
Q

Characteristics of G-protein receptors include: (select four)

A

modulation of ligand channels
activation of adenylyl cyclase
inhibition of adenylyl cyclase
activation of phospholipase C

25
Q

Which of the following molecular binding forces is the weakest?

A

Van de waars

26
Q

Reaction of reversible with this bonding

A

Van de waars

27
Q

The ability of a drug to bind with a receptor to form a stable complex is referred to as the drug’s

A

Affinity

28
Q

Efficacy refers to the

A

dose-response curve produced by the binding of the opioid to an opioid receptor.

29
Q

Potency refers to the

A

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.