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
What effects distribution
Protein binding Blood flow Blood tissue affinity
26
Inactive drug vs active drug
Inactive= bound to drug not available to interact with tissue receptor Active: unbound free and can cause pharmacological response
27
What happens if 2 highly protein bound drugs are given concurrently
Compete for protein binding sites cause more free drugs to be released
28
What crosses the blood brain barrier
Highly lipid soluble and low molecular weight drugs and not water soluble drugs
29
Metabolism
Or bio transformation | Process by which body chemicals changes grubs into form that can be excreted
30
Where does metabolism occur
GI tract but mostly in liver (most drugs inactive due by enzymes$
31
Half life
Time it takes for one half of the drug concentration to be eliminated
32
Steady state
Amount of drug administered=drug eliminated | Necessary for optimal therapeutic benefit
33
Loading dose
Large initial dose to achieve rapid MEC
34
Excretion
Main route is kidneys
35
What can’t be filtered through kidneys
Protein bound drugs
36
Creatinine clearance
Between 86-135 mal/min | Metabolic Byproduct of kidneys and compares amount of creatine in blood and urine
37
Blood Urea Nitrogen (BUN)
Metabolic breakdown products between 7-20
38
Pharmacodynamic phase
Study of drug effect and mechanisms of action
39
Primary effect
Desired effect
40
Secondary effect
Desirable or undesirable
41
Onset of action
Time it takes to reach minimum minimum effective concentration after drug is administered
42
Peak action
Reach it’s highest blood concentration
43
Duration of action
Length of time drug exerts a therapeutic effect
44
Dose response relationship
Bodies psychologic response to changes in drug concentration at side of action
45
Potency
Amount of drug needed to elicit a specific psychological response to a drug High=significant therapeutic response Low= minimal therapeutic response
46
Therapeutic range
Between minimum effective concentration and minimum toxic concentration
47
Therapeutic index
Difference between therapeutic index and toxic affect Closer to 1 equals greater toxicity
48
Peak levels
Highest concentration and Blood sample drawn at peak time | Indicate rate of absorption
49
Trough levels
Lower plasma concentration and drawn Immediately before the next dose of drug given Indicate rate of elimination
50
Agonist
Drugs that activate receptors and produce desired response
51
Antagonist
Drugs that prevent receptor activation and block a response
52
Side effects
Physiological effects not related to desired drug affects and all drugs have side effects
53
Adverse reactions
More severe side effects unintentional and undesirable
54
Tolerance
Decrease responsiveness over the course of therapy requires higher dosage of drug