Pharmacodynamics Flashcards

1
Q

Define pharmacodynamics

A

Study of what drugs do to the body

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2
Q

Pharmacokinetics is

A
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3
Q

Pharmacodynamics is

A
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4
Q

A drug is a xenobiotic that induces an effect typically by interacting with an endogenous target molecule, also called a _____

A

Receptor

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5
Q

The ____ can be an enzyme, nucleic acid, or a special membrane brown protein

A

Receptor

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6
Q

A large class of drug receptors are ______ _____, a molecule produced by the body (endogenous). Examples include ligand gated ion channels, G protein coupled receptors

A

Physiological receptors

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7
Q

The second largest class of drug targets are _____. Example is penicillin, ACE Inhibitors

A

Enzymes

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8
Q

The third major class of drug receptors are _____.

A

Nucleic acids

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9
Q

Drug dose response graph. The drug concentration is on the X axis and a _____ on the Y axis

A

Biological effect

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10
Q

Fischer projection is a ___ and ____ model of thinking about enzyme and substrate interaction. This model has limitations

A

Lock and key

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11
Q

_____ is the equilibrium dissociation constant of a drug-receptor complex. ______ is the reciprocal of kD. If affinity is high, the dissociation constant will be low.

A

kD
Affinity

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12
Q

Low affinity requires a ____ concentration of molecules

A

Higher

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13
Q

The _____ is the free drug concentration at which half of the receptors are drug bound

A

KD (similar to Km)

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14
Q

Different drugs may possess distinct _____ for a common target (receptor)

A

Potencies

Drug A is more potent than drug B. It takes less concentration of drug A to reach the same effect

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15
Q

A lower ED50 of a drug means the _____ the potency.

A

Higher

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16
Q

The _____ opens the lock, the _____ does not open the lock. These two things can compete for each other.

A

Agonist
Antagonist

17
Q
A

Drug A is an agonist, Drug B is an antagonist

18
Q

_____ ____ can be overcome if sufficiently high concentration of agonist is present

A

Competitive antagonist

19
Q

____ _____ cannot be overcome even in the presence of extremely high agonist levels, sometimes considered insurmountable antagonist. Has no effect on the ED50

A

Non competitive antagonist

20
Q

_____ agonist, not able to produce the full effect as a full agonist.

A

Partial

In this picture, both drugs have identical potencies, meaning they reached half-maximal effect observed at identical doses

21
Q

Fentanyl is a ____ agonist, ibuprofen is a _____ agonist. Fentanyl is more _____.

A

Full
Partial
Efficacious

22
Q

Difference in drug efficacy will have different levels of _____ on a graph. Different drug potencies will effectually reach the same effect levels but at different ____ levels

A

Effect
Dose

23
Q
A

Fentanyl and buprenorphine are equally potent. Fentanyl and morphine are more efficacious than buprenorphine

24
Q

____ ____ ____ model replaced the lock and key model

A

Induced fit binding
(Conformational selection binding model)

25
Q

The ___ ____ model is the idea that the drug receptor can switch back and forth between the active and inactive state

A

Two State

26
Q

____ ____ ___ is how much activity does the receptor have in the absence of ligand

A

Constitutive Receptor Activation

27
Q

_____ receptor activity reduces the response in a system (inverse agonist). _____ receptor activity increases the level of response in a system (agonist). _____ receptor activity, the response remains the same (antagonist).

A

Diminished
Enhanced
Constitutive

28
Q

An agonist has a higher ___to bind to the active site in a receptor and shifts towards higher level of activity. An _____ agonist has a higher affinity to the inactive site of a receptor and diminishes the level of activity. A ____ has the same affinity for both the active and inactive sites on the receptor and has no effect of the levels of activity.

A

Affinity
Inverse agonist
Antagonist

29
Q

____ is the degree to which a drug binds to ONE receptor. Dopamine can interact with three different types of receptors.

A

Selectivity

Dopamine is more selective for DA1

30
Q

______ dose response curve, when the dose of the drug is describe in terms of a percentage of the maximal response. _____ dose response is when a drug is described in terms of the cumulative percent of subject who exhibit an effect

A

Graded
Quantal

31
Q

The range between the ED50 and LD50 (lethal dose) is the ____ ____

A

Therapeutic index

32
Q

Activation of cell surface receptor is associated with Intracellular production of ____ ____. This is the concept of signal transduction

A

Second messengers

33
Q

Second messengers can result in massive ____ of signaling

A

Amplification

34
Q

The largest class of receptors are ____ .
They bind endogenous and therapeutic molecules

A

G protein

35
Q

Some important second messenger molecules include:

A

Ca++, cAMP, IP3, DAG, acetylcholine, nicotine, varenicline

36
Q

Receptor protein _____ ____ and _____ receptors are able to initiate a phosphorylation cascade. This is an example of a signal transduction pathway.

A

Tyrosine kinases
Cytokine