Intro to PK Flashcards

1
Q

What makes something a poison?

A

The dose

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2
Q

What is drug therapy?

A

Planned action that involves risk of unwanted adverse effects

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3
Q

How is a drug dose chosen?

A

Based on its ability to achieve and maintain therapeutic (target) concentrations producing minimal adverse effects in the body

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4
Q

Define appropriate dosage regimen

A
  1. Therapeutic window between MTC and MEC
  2. To achieve and maintain safe and effective therapy
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5
Q

What are components of appropriate dosage regimen?

A

A: Right drug
B: Dose of a drug
C: Dosage form
D: Route of admin
E: Dosing interval/frequency
F: Duration of therapy

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6
Q

What information do we need to design appropriate dosage regimen?

A
  1. Therapeutic range of the drug
  2. PK parameters of the drug
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7
Q

What is a therapeutic range of a drug?

A
  1. Minimum (Cmin) and maximum (Cmax) plasma drug concentration values
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8
Q

Where are therapeutic range values found?

A
  1. Between MEC and MTC
  2. Estimated average plasma concentration (Cavg)/Css
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9
Q

What are the PK parameter of a drug?

A

Vd, CL, Half-life

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10
Q

How does Vd effect loading dose?

A

It relates plasma concentration to the amount of drug in the body

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11
Q

What is LD?

A

A large initial dose given to achieve therapeutic drug levels from the beginning

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12
Q

How is Cl used to determine maintenance dose (dosing rate)?

A

It measures the rate of drug elimination that needs to be replaced to maintain therapeutic concentration

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13
Q

What is another name for Cmax

A

MTC

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14
Q

What is another name for Cmin?

A

MEC

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15
Q

What is MD?

A

Given at fixed intervals to keep drug concentrations within the therapeutic concentration range

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16
Q

Why is half-life used for dosage regimen design?

A

It affects the time to reach Css and determines the shape of the plasma concentration-time courses

17
Q

What are all the PK parameters used to estimate plasma concentration-time profiles?

A
  1. Vd
  2. Cl
  3. T1/2
  4. Cmax
  5. Cmin
  6. Cavg/Css (therapeutic range)
  7. Tmax
  8. AUC
  9. F
18
Q

What are parameters?

A

Observable quantities that remain constant for every state of a system

19
Q

What is the purpose for PK?

A

To study ADME processes of drugs in the body to examine the time course of drug concentrations in mainly plasma, and also in urine and bile

20
Q

What are the methods used to analyze plasma drug concentration-time profiles?

A
  1. Non-compartmental analysis techniques (NCA)
  2. Compartmental model fitting methods
21
Q

What is another name for NCA?

A

Model-independent approaches

22
Q

What is are the approaches of NCAs?

A
  1. Applies the trapezoidal rule for measuring AUC
  2. Estimates Cmax using tmax directly from the data and Cl, k, t1/2, and Vd driven equations
23
Q

How does the compartmental model fitting methods help determine PK parameters?

A
  1. Provide a continuous description of drug concentration
  2. Consider the body as a finite number of interconnected, well-mixed, homogenous compartments
  3. Mathematical PK models are developed using nonlinear regression methods to estimate PK parameters
  4. drug concentrations over a time range are predicted using the developed PK model to estimate Cmax , tmax , Cavg / Css , AUC, F
24
Q

What are the PK approaches of designing dosage regimens?

A
  1. Individualized dosage regimen (Patient-specific values)
  2. Dosage regimen based on population values
  3. Dosage regimen based on partial PK parameters (Bayesian approach)
25
Q

What is individualized dosage regimen?

A

The dose is calculated based on the PK parameters of the drug derived from individual patient drug concentrations measurement in plasma

26
Q

How is a dosage regimen designed based on population values?

A

Regimen is calculated based on population average PK parameters obtained either from package insert or from clinical studies published in the drug literature

27
Q

How is a dosage regimen designed based on partial PK parameters (Bayesian approach)?

A

The use of population PK uses average patient population characteristics and only a few plasma concentration from the patient

28
Q

What is PK used for?

A
  1. Calculate LD and MD
  2. Determine drug dosage regimen
  3. Perform dosage adjustments in patients with renal and hepatic diseases
  4. Perform BA/BE studies
  5. Predict drug-drug and drug-food interactions