Pharmacokinetics Flashcards

1
Q

are xenobiotics

A

Drugs

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2
Q

chemical which is found in an organism but which is not normally produced or expected to be present in it) (Biocompatible)

A

xenobiotic

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3
Q

Disciplines Involved in Drug Development

A

Physiology and Pharmacology required to select appropriate drug candidates.

Physics and Physical Chemistry and Mathematics involved in dosage form design.

Kintics, Analytical Chemistry and Therapeutics required to determine appropriate dose.

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4
Q

the study of the kinetics of drug absorption, distribution, metabolism and excretion of drugs (ADME) (body action)

A

Pharmacokinetics

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5
Q

the study of factors that affect the bioavailability of drugs in animals and man.

A

Biopharmaceutics

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6
Q

the study of the biochemical and physiological effects of drugs on the body or on microorganisms or parasites within or on the body and the mechanisms of drug action and the relationship between drug concentration and effect.

A

Pharmacodynamics

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7
Q

ADME

A

Pharmacokinetics

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8
Q

Transfer of drug from the absorptions site (stomach, intestine) to the blood. Rapid and not reversible.

A

Absorption

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9
Q

Fate of drug after Absorption (Distribution and Elimination).

A

Disposition

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10
Q

Transfer of drug from the blood to extravascular fluid, tissue, plasma proteins or other fluids. Rapid and reversible. Usually occurs much more rapidly than elimination.

A

Distribution

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11
Q

Rate of distribution to tissue/organ is determined by

A

blood flow

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12
Q

Biotransformation of drug, mainly in liver (Also kidney, skin).

A

Metabolism

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13
Q

Removal of drug compound and metabolites from the body.

A

Elimination

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14
Q

Goals of Pharmacokinetics

A

A. To compare the pharmacology and toxicology of drugs and their relationship to Cp of both the drug and its metabolite/s.

B. To determine the accumulation characteristics of drugs for the evaluation of chronic toxicity.

C. To individualize and optimize the therapeutic management of individual patients (dose, time).

D. To determine patient compliance

E. To evaluate the effect of disease states on drug elimination.

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15
Q

used an alternative to treadmill stress and used for elderly patients.

A

Dipyridamole (Persantine)

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16
Q

can increase the blood flow up to four to five times than in normal value.

A

Adenosine (Adenocard)

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17
Q

Used for increase of cerebral blood flow in cerebral perfusion imaging

A

Acetazolamide (diamox)

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18
Q

quantity that is always unchanged

A

Constant

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19
Q

mathematical constants

A

. π and e

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20
Q

physical constants

A

R, k (Boltzmmann constant) and N (Avagadro’s number)

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21
Q

constant that is not universal but does not vary in a particular instance.

A

Parameter

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22
Q

Examples of parameters

A

Rate constants, equilibrium constants, slopes and intercepts of graphs

23
Q

a quantity that is changing during the course of an experiment

A

Variable

24
Q

Examples of variables

A

axes of a graph - In a rate process time and concentration are variable.

25
Q

the half-life of a drug is 2 hrs, and the concentration at 30 minutes were found 20 mg/mL - What is the half-life

A

half-life, t1/2 = 0.693/k

26
Q

Decay Function

A

f(t)=e^-kt=exp(-kt)

27
Q

Growth Function

A

f(t)=1-e^-kt

28
Q

Intravascular routes

A

Intravenous

Intra-arterial

29
Q

Extravascular routes

A
Oral
Buccal 
Rectal
Pilmonary
Intramuscular and subcuteaneous injection
Etc.
30
Q

Intravascular Administration (bolus) characteristics

A

No absorption phase

Immediate onset of action

Entire dose is available

Route used frequently in life threatening situations

Adverse reactions difficult to reverse. Accurate dosing is thus essential.

31
Q

Which function would be used for a bolus

A

Decay Function

32
Q

An absorption phase is present.

Onset of action determined by a number of factors including formulation, route of administration (Oral, pulmonary, etc.), drug physicochemical properties, and physiological properties.

The entire administered dose may not be available.

A

Extravascular Administration

33
Q

Which function would be used for extravascular administration

A

Combined Decay and Growth Function

34
Q

Which function would be used for intravascular infusion

A

Growth Function

35
Q

represent the area under the curve (AUC)

A

Definite integrals

36
Q

In pharmacokinetics the integral is often referred to as

A

AUC

37
Q

How to get AUC

A

Integration or Trapezoid Rule

38
Q

Trapezoid Rule Equation

A

(b-a) ( h(a) – h(b))
Area= —————————
2

39
Q

a technique for approximating the definite integral

A

Trapezoid Rule

40
Q

How does the Trapezoid Rule work

A

The trapezoidal rule works by approximating the region under the graph of the function f(x) as a trapezoid and calculating its area

41
Q

assumes quadratic dependence in this small interval - more accurate than trapazoid rule.

A

Simpson’s Rule

42
Q

assumes function is linear in the small interval h

A

Trapezoid rule

43
Q

AUC provides

A

the pk information such a duration of drug in blood, tmax, cmax, bioavailability etc.

44
Q

Rate Equation

A

Rate depends on concentration

45
Q

Decomposition reactions in the solid phase often show

A

zero order kinetics - not dependent on concentration

46
Q

characterized by exponential decay

A

First order reactions

47
Q

time required for concentration to become half

A

Half-Life

48
Q

half life is 2 hr, how much will be left after 4 hrs?

A

25%

49
Q

Is Half-life of first order reactions constant or variable

A

constant

50
Q

How do Drug diffuse from compartments

A

Drug diffuses from compartments with high concentration to those with low concentration.

51
Q

Pharmacokinetic models recognize that _____is an important mechanism for the absorption, distribution and excretion of drugs and their metabolites.

A

passive diffusion

52
Q

What is the central compartment

A

blood and organs which are perfuse such as heart, kidney have same blood flow as in the blood vessel

53
Q

considered as peripheral compartment.

A

Tight tissues such as muscle, bone where blood flow is more slower