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DIT Recommended Course Order > Video 7&8 PB Pharmacokinetics&Pharmacodynamics > Flashcards

Video 7&8 PB Pharmacokinetics&Pharmacodynamics Flashcards

1
Q

What is the Km (Michaelis Kinetics) formula?

A

Km = (S) at 1/2 V max

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2
Q

What is inversely related to the affinity of the enzyme for the enzyme for its substrate?

A

Km

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3
Q

What is directly proportional to the enzyme concentration?

A

V max.

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4
Q

How can you explain the Lineweaver -Burk plot?

A

The further to the right the X-intercept (i.e., closer to zero), the greater the Km and the lower the affinity.

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5
Q

In the Lineweaver-Burk plot what is the formula for Slop?

A

Slop = Km/Vmax

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6
Q

Which are the characteristics of Competitive inhibitors (Reversible)?

A 
Resemble Substrate: Yes.
Overcome by increased Substrate concentration: Yes.
Bind active site: Yes.
Effect on Vmax: Unchanged.
Effect on Km: increase.
Pharmacodynamics: decreased potency.
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7
Q

Which are the characteristics of competitive inhibitors (irreversible)?

A 
Resemble Substrate: Yes.
Overcome by increased Substrate concentration: No.
Bind active site: Yes.
Effect on Vmax: Decrease.
Effect on Km: Unchanged
Pharmacodynamics: decreased efficacy.
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8
Q

Which are the characteristics of Noncompetitive inhibitors?

A 
Resemble Substrate: No.
Overcome by increased Substrate concentration: No.
Bind active site: No.
Effect on Vmax: Decrease.
Effect on Km: Unchanged.
Pharmacodynamics: decreased efficacy.
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9
Q

Which are the 4 pharmacokinetics equations?

A

1) Volume of Distribution.
2) Clearance.
3) Loading Dose.
4) Maintenance Dose.

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10
Q

How is Volume of distribution calculated?

A

Vd = amount of drug in the body / Plasma drug concentration

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11
Q

At which compartment works the drug if the Volume of distribution are low, medium or high?

A

Low: Blood.
Medium: ECF.
High: All tissues including fat.

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12
Q

How is Clearance calculated?

A

CL = Rate of elimination / Plasma drug concentration.

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13
Q

Css (Steady state concentration) X Volume of distribution, this formula belong to…

A

Loading dose.

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14
Q

How is Maintenance dose calculated?

A

Css X Clearance.

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15
Q

What does Bioavailability mean?

A

Fraction of administered drug reaching systemic circulation unchanged. IV dose, F=100%.

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16
Q

What does the function of the Half-life in drugs?

A

It is the time required to change the amount of drug in the body by 1/2 during elimination (or constant infusion).
Property of First-order elimination. It will be 94% after 4 half-life.

17
Q

What term describes the maximum effect a drug can produce?

A

Efficacy.

18
Q

What term describes the measure of the amount of drug needed to produce a given result?

A

Potency.

19
Q

What term describes the dose of a drug that produces the desired effect?

A

Effective dose (ED)

20
Q

What term describes the dose of a drug that produce death?

A

Lethal dose (LD).

21
Q

What term describes the measure of the safety of a drug?

A

Therapeutic index.

22
Q

How is therapeutic index calculated?

A

LD50/ED50

23
Q

How does a competitive antagonist affect the dose-response curve?

A

Shifts it to the right (increased ED50)

24
Q

How does a Noncompetitive antagonist affect the dose-response curve?

A

Shifts it downward (decreased maximal response)

25
Q

How does a partial agonist differ from a full agonist?

A

Acts like an agonist when an agonist is not present; acts like an antagonist if an agonist is present.

26
Q

What is a Therapeutic Window?

A

It is a range of doses of a drug that are safe.

27
Q

What effect will a competitive antagonist have on V max and Km?

A

Km will be higher, but V max will be unchanged.

28
Q

Your patient is taking a experimental drug Z to lower his LDL cholesterol. When he is given the antagonist drug X, the potency of drug Z is decreased, but efficacy is unchanged. Doubling the dose of the drug Z is shown to overcome the inhibition by the drug X. Does drug X competitively, or noncompetitively?

A

Competitive antagonist.

29
Q

Drug A has a therapeutic index of 10:1, while drug B has a therapeutic index of 2:1. Which drug would be considered safer?

A

Drug A is safer.

DIT Recommended Course Order (21 decks)

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