Pharmacokinetics Flashcards

1
Q

What is the diffference between clearance and elimination half-life?

A

Clearance - Body’s Efficiency of drug removal

Elimination Half-life - Rate of Drug Removal

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2
Q

What is the difference between Bioavailability and Volume of Distribution?

A

Bioavailability - Fraction of Drug Absorbed

Volume of Distribution - Apparent Space the Drug Resides in

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3
Q
  • **What is the most important concept to be considered when designing a regimen for long-term drug administration?
  • Define this term.
  • **How can this be calculated?
  • Define the variables
A

Clearance

Clearance - theoretical Volume of Fluid from which the drug is removed per unit of time

CL = Rate of Elimination/Concentration
CL = Q [(Ca-Cv)/Ca] = QE
Q = Blood Flow to the organ 
Ca = Arterial Concentration of Drug
Cv = Venous Concentration of Drug
E = [(Ca-Cv)/Ca] - Extraction ratio
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4
Q

How do you ensure that you maintain steady-state concentrations of a drug within the therapeutic window?

A
  • Administer the Drug at the same rate that it is eliminated
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5
Q

What is the Rate Limiting Variable in Clearance of a drug?

A

Blood Flow to the Organ

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6
Q

What are the two methods by which all drugs are eliminated?

- which is most common?

A

0 order and 1st order kinetics

  • 1st order is by far the most common
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7
Q

Between 0 order and 1st order kinetics, which eliminates a constant fraction of the remaining concentration per unit of time?

A

1st order - specific fraction of the drug is elminated from the remaining concentration per unit time

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8
Q

What is Ke?

- how is it obtained

A

Elimination Rate constant obtained by taking the log of [Drug] and graphing it against time

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9
Q

What is the volume of distribution?

- What is the formula?

A

The fluid volume that would be required to contain all of the dose at the same concentration as exists in the blood plasma

Vd = Dose / Cb

Cb = Blood concentration

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10
Q

How do you find the elimination constant for a drug eliminated by 1st order kinetics?

A

Ke= Q [(Ca-Cv)/Ca] / Vd

also,

Ke = CL/Vd

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11
Q

What is the relationship of half life to dosing interval?

A

A drug is often given at half-life intervals

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12
Q

What are the 4 main factors that make 1/2 life a clinically important thing?

A
  1. Determination of Dosing Interval
  2. A factor in Determining Dose
  3. May Determine Route
  4. Good indicator of the time required to reach steady-state after a dosage regimen is initiated
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13
Q

What is the one compartment pharmacokinetic Model?

  • how accurate is it?
  • Kinetics?
A

*Assumes the Body is One Compartment

***ONLY WORKS FOR DRUGS THAT ARE DISTRIBUTED UNIFORMLY THROUGHOUT THE BODY

  • Not a very adequate model
  • 1st order Elimination
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14
Q

What is the two compartment model?

- how does the graph of the two compartment model differ from that of the one compartment model?

A

Two Compartment Model - assumes drug is injected into the blood then must equilibrate between two compartments

  • Graphically you’ll see in initial large drop in concentration that corresponds to equilibration between the two compartments
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15
Q

How do you find clearance rate for a multicompartment model?

A

Clearance Rate = Dose / AUC

AUC = area under the curve

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16
Q

How do you determine dosing while taking into account bioavailability?

A

F(Dosing Rate) = CL/Css

F Dose/T = CL/Css

Dose = (CssCLT) / F

Where:

  • T = Dosing Interval
  • CL = clearance
  • Css = Steady State Concentration (in plasma)
17
Q

How many half-lives does it typically take to reach steady state?
- what is the time to steady state strictly dependent on?

A

FIVE

***SINCE it takes 5 half lives then time to steady state is DEPENDENT ONLY ON T(1/2)

18
Q

When determining what drug to give a patient, what are the only two factors that the physician can control?

A
  • Dose and Dosing Interval

PHYSICIANS CAN ONLY CONTROL STEADY STATE MAX AND MIN*

19
Q

T or F: for IV administration the time to steady state is still 5 half lives

A

True

20
Q

How do you determine how fast to administer a drug intravenously to get to a given concentration?

A

Css = Infusion Rate / Total Body Clearance

21
Q

When would you administer a loading dose?

A
  • Heart Attacks
  • Serious Heart Failure
  • Overwhelming Bacterial Infections
22
Q

What is the formula for Loading dose?

A

LD = (Css * Vd) / F

where: 
LD - Loading Dose
Css - Steady State Concentration (DESIRED) 
Vd - volume of distribution 
F - Bioavailability
23
Q

What are patients given following a loading dose?

- what is the formula for calculating this?

A

Dosing Rate

Dosing Rate = (Target Css * CL) / F

24
Q

What are some drugs that exibit zero order kinetics?

A

Ethanol
Heparin
Aspirin
Tetracycline

(Phenytoin, Amobarbital)

25
Q

When do drugs display zero order kinetics?

A

When the enzyme is overloaded with drug

26
Q

What is the formula for loading dose in zero order kinetics?

A

LD = (Vd x Css)/F

27
Q

What is the formula for steady state concentration for zero order kinetics?

A

Css = (Km*DR)/(Vm-DR)

Km = CONCENTRATION/dose for 50% max Rate

28
Q

What is the formula for Dosing rate for zero order kinetics?

A

DR = (Css*(Vm-DR))/Km

Km = CONCENTRATION/dose for 50% max rate
Vm = Max Rate