Pharmacokinetics And Pharmacodynamics Flashcards

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1
Q

What is bioavailability?

A

Fraction of the administered dose that reaches the required body compartment (usually the circulation).

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2
Q

What is the bioavailability of IV drugs?

A

100%

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3
Q

Name 2 factors that can affect bioavailability

A

Absorption (affected by formulation - oral or IV, age, food, vomiting/malabsorption)
First pass metabolism

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4
Q

What is first pass metabolism?

A

When a drug gets metabolised before it reaches the systemic circulation.

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5
Q

What is the difference between pharmacokinetics and pharmacodynamics?

A

Pharmacokinetics is the way that the drug enters, exits and moves through the body.
Pharmacodynamics is how the drug reacts inside the body.

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6
Q

What is a modified release preparation?

A

When a drug is modified so that it can be given at a single dose that has an extended release, rather than multiple doses throughout the day (can help with drug adherence).

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7
Q

How does protein binding affect drug response?

A

Only free drug can produce a response, therefore protein bound drugs don’t elicit a response.

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8
Q

Name 3 physiological or pathological states that affect protein binding.

A

Pregnancy
Renal failure
Malnutrition (hypoalbuminaemia)

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9
Q

What is volume of distribution?

A

Measure of how widely a drug is distributed around the body. The smaller the Vd, the more confined a drug is to plasma and ECF.

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10
Q

What is the equation for volume of distribution (Vd)?

A

Vd = Dose/[drug]plasma

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11
Q

What is the effect of grapefruit juice on the concentration of statins in the plasma?

A

Grapefruit juice inhibits the metabolism of statins, therefore the concentration of statins is higher.

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12
Q

What is the effect of cranberry juice on warfarin?

A

Inhibits CYP 2c0, reducing the clearance of warfarin

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13
Q

What is the half life (t1/2)?

A

The time it takes for the concentration of drug in the plasma to decrease by half.

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14
Q

What is the relationship between t1/2 and clearance?

A

They are inversely proportional - as t1/2 increases, clearance decreases.

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15
Q

What is the difference between zero order and first order kinetics?

A

Zero order - rate of elimination of drug is constant (straight line).
First order - rate of elimination of drug is proportional to drug concentration (curve).

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16
Q

What is drug clearance?

A

The volume of plasma that is cleared of a substance per unit of time.

17
Q

If you plot a curved first order kinetics graph on a log scale, what will happen?

A

It will become a straight line.

18
Q

How many half lives does it take to reach CpSS (steady state plasma concentration)?

A

5 x t1/2

19
Q

What is the equation linking K (elimination constant), clearance and Vd?

A

K = Cl/Vd

20
Q

What is the difference between loading dose and maintenance dose?

A

Loading dose - the initial higher dose of a drug given at the start of treatment allowing you to reach the therapeutic window and reach CpSS
Maintenance dose - dose required to maintain CpSS - dose should match clearance to maintain the desired therapeutic effect.

21
Q

What is EC50?

A

The concentration of ligand needed for half of the maximal effect (Emax), represents drug potency.

22
Q

What is Kd?

A

The concentration of ligand needed to bind half of all receptors (Bmax), represents affinity of the drug.

23
Q

What is the MOA of naloxone?

A

Reversal agent used for opioid overdose - has a higher affinity than opioids therefore displaced them from receptors.

24
Q

What is efficacy?

A

Ability of a drug to produce a response.

25
Q

What is potency?

A

Dose required to produce the desired response.

26
Q

What are the 6 types of adverse drug reactions?

A

A- augmented effects - reactions known but dose-related
B- bizarre - unpredictable effects often with high rate of mortality
C- chronic - occur due to prolonged treatment not with single doses
D- delayed - occur much later on e.g. in children of treated patients or years later
E- end of treatment effects - withdrawal
F- failure of treatment effects