Pharmacokinetics Lecture 2 Flashcards

1
Q

Pharmacokinetics phase

A

The study of the movement of drugs into, within and out of the body that is necessary to achieve drug action

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2
Q

Phases

A

Absorption
Distribution
Metabolism
Excretion

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3
Q

Absorption

A

Movement of drugs into the bloodstream after administration

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4
Q

Pharmaceutic phase

A

When a drug is in solid form and disintegrates into smaller particles and combine with liquid form a solution

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5
Q

Excipients

A

Fillers and inert substances

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6
Q

What environments so drugs disintegrate and absorb faster in?

A

Acidic fluids with a pH of 1 or 2 rather than alkaline fluids

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7
Q

Small intestines form

A

Covered with villi which increase the surface area available for absorption

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8
Q

Enteric coated drugs disintegrate where?

A

Resist disintegration in gastric acid of the stomach

Only occurs until drug reaches alkaline environment in small intestine

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9
Q

Passive absorption

A

Diffusion

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10
Q

Active absorption

A

Requires carrier (enzyme) and energy is required

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11
Q

Pinocytosis

A

Cells carry drag across membrane by engulfing particles

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12
Q

What is the GI membrane composed of

A
Mostly lipid (fat) and protein 
(Drugs that are lipid soluble pass rapidly through)
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13
Q

What needs a carrier to pass through the membrane?

A

Water soluble drugs need an enzyme or protein and can’t cross blood brain barrier

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14
Q

How do large particles pass through cell membrane?

A

Nonionized

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15
Q

What drugs absorb the fastest

A

Drugs that are lipid soluble and nonionized

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16
Q

Where do drugs absorb faster?

A

Drugs given IM= more more blood vessels

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17
Q

Where do drugs absorb slower

A

Subcutaneous tissue because there is fewer blood vessels

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18
Q

First pass effect

A

Some drugs don’t got to systemic circulation but pay to the intestinal lumen to the liver

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19
Q

What happens in the liver?

A

Some drugs me metabolize in inactive form than excreted (reducing amount Of active drug)

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20
Q

Bioavailability

A

% of drug available for use
PO<100%
IV=100%
Desired drug effect= oral does is 3-5x larger than dose for IV

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21
Q

Factors effecting bioavailability

A
Drug form 
Route 
GI mucosa and motility 
Presence of food and other drugs 
Changes in liver metabolism or function
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22
Q

Effect rapid absorption on bioavailability

A

Increased bioavailability and can increase drug concentration which Amy lead to drug toxicity

23
Q

Effect of Slow absorption on bioavailability

A

Limit the bioavailability of drug causing decrease drug concentration

24
Q

Distribution

A

Process by which drug becomes available to the body fluids and tissues

25
Q

What effects distribution

A

Protein binding
Blood flow
Blood tissue affinity

26
Q

Inactive drug vs active drug

A

Inactive= bound to drug not available to interact with tissue receptor

Active: unbound free and can cause pharmacological response

27
Q

What happens if 2 highly protein bound drugs are given concurrently

A

Compete for protein binding sites cause more free drugs to be released

28
Q

What crosses the blood brain barrier

A

Highly lipid soluble and low molecular weight drugs and not water soluble drugs

29
Q

Metabolism

A

Or bio transformation

Process by which body chemicals changes grubs into form that can be excreted

30
Q

Where does metabolism occur

A

GI tract but mostly in liver (most drugs inactive due by enzymes$

31
Q

Half life

A

Time it takes for one half of the drug concentration to be eliminated

32
Q

Steady state

A

Amount of drug administered=drug eliminated

Necessary for optimal therapeutic benefit

33
Q

Loading dose

A

Large initial dose to achieve rapid MEC

34
Q

Excretion

A

Main route is kidneys

35
Q

What can’t be filtered through kidneys

A

Protein bound drugs

36
Q

Creatinine clearance

A

Between 86-135 mal/min

Metabolic Byproduct of kidneys and compares amount of creatine in blood and urine

37
Q

Blood Urea Nitrogen (BUN)

A

Metabolic breakdown products between 7-20

38
Q

Pharmacodynamic phase

A

Study of drug effect and mechanisms of action

39
Q

Primary effect

A

Desired effect

40
Q

Secondary effect

A

Desirable or undesirable

41
Q

Onset of action

A

Time it takes to reach minimum minimum effective concentration after drug is administered

42
Q

Peak action

A

Reach it’s highest blood concentration

43
Q

Duration of action

A

Length of time drug exerts a therapeutic effect

44
Q

Dose response relationship

A

Bodies psychologic response to changes in drug concentration at side of action

45
Q

Potency

A

Amount of drug needed to elicit a specific psychological response to a drug
High=significant therapeutic response
Low= minimal therapeutic response

46
Q

Therapeutic range

A

Between minimum effective concentration and minimum toxic concentration

47
Q

Therapeutic index

A

Difference between therapeutic index and toxic affect

Closer to 1 equals greater toxicity

48
Q

Peak levels

A

Highest concentration and Blood sample drawn at peak time

Indicate rate of absorption

49
Q

Trough levels

A

Lower plasma concentration and drawn
Immediately before the next dose of drug given
Indicate rate of elimination

50
Q

Agonist

A

Drugs that activate receptors and produce desired response

51
Q

Antagonist

A

Drugs that prevent receptor activation and block a response

52
Q

Side effects

A

Physiological effects not related to desired drug affects and all drugs have side effects

53
Q

Adverse reactions

A

More severe side effects unintentional and undesirable

54
Q

Tolerance

A

Decrease responsiveness over the course of therapy requires higher dosage of drug