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Pharmacokinetics Flashcards

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1
Q

pharmacokinetics

A

what happens to a drug when you put it in your body (effect of body on drug)

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2
Q

What does the drugs concentration in the body depend on

A

drug regimen (dose, route, formulation, frequency)
how the drug moves through the body over time (ADME)

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3
Q

What does pharmacokinetics describe

A

ADME

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4
Q

What is on the X axis of a PK curve

A

Time

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5
Q

what is on the Y axis of a PK curve

A

Blood level or “plasma concentration”

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6
Q

Pharmacodynamics = __________ = what the drug does to the body

A

concentration-effect relationship

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7
Q

Pharmacokinetics = ____________ = What the body does to the drug

A

Dose-Time-Concentration relationship

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8
Q

codeine getting metabolized (broken down) by hte body into a few different compounds, including morphine.

A

Pharmacokinetics

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9
Q

Opioids, such as codeine and morphine, work by agonizing (activating) mu-opioid receptors in the central nervous system causing analgesia.

A

pharmacodynamics

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10
Q

a central goal of drug therapy is to _____

A

achieve a desired effect while inflicting the minimum possible adverse effects

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11
Q

Understanding PK allows us to find the drug dosing regimen necessary to achieve the least possible adverse effects. This is achieved by __________

A

getting a drugs blood level in the Theraputic window

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12
Q

what is the theraputic window

A

the window between the minimum theraputic dose and the dose where the drug becomes toxic

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13
Q

what does Enteral mean

A

goes through the intestine (digestive tract)

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14
Q

what does parenteral mean

A

Stays outside digestive tract

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15
Q

why does a 150mcg tablet taken orally and 75mcg given IV have the same effectiveness

A

IV is absorbed better than oral

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16
Q

Bioavailability (F)

A

the Fraction of intact drug that reaches the systemic circulation

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17
Q

F= _____ for IV drugs

A

100%

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18
Q

if you take 100mg of a drug and only 80% of the drug reaches the systemic circulation (bloodstream) what is F? (what is bioavailability)

A

F=80%

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19
Q

What is used to measure bioavailability

A

Area Under the Curve (AUC)

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20
Q

What does AUC represent

A

bioavailability, the total systemic exposure to a drug.

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21
Q

What is the blue line, what is he green line

A

blue line = IV
green line = oral

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22
Q

Which of the PK curves below shows the BEST (highest) bioavailability

A

the one with the red

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23
Q

What are two things that reduce bioavailability

A

incomplete amount of absorption
the First pass effect

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24
Q

what is the first pass effect

A

when the concentration of a drug is greatly reduced before reaching circulation

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25
Paracellular transport
it can go around cells (through the junctions between cells)
26
facilitated diffusion
it can get trasnported along a concentration gradient
27
diffusion
it can diffuse through the cells (ie throught the lipid bilayer cell membranes)
28
In general, drugs that are good at diffusing through lipid bilayers are:
small molecules lipophilic uncharged
29
Which molecule would be better at crossing through cell layers
Fentanyl (left) because its smaller than vncomyocin (right)
30
This tissue cares alot about size, charge, and lipophilicity of drugs that pass through it
continuous capillaries such as CNS (blood brain barrier), skin and lungs.
31
This tissue cares a little bit about size, charge, and lipophilicity of drugs that pass through it
fenestrated capillaries such as (kidneys and small intestine)
32
this tissue cares the least about size, charge, and lipophilicity of drugs that pass through.
sinusoidal capillaries (liver, lymph nodes)
33
influx transporters
active transport proteins that move drugs into cells
34
efflux transporters
active transport proteins that move drugs out of cells
35
active transport
transport requiring energy
36
What is a significant active trasnporter in PK and what is its job
efflux transporters job is to keep xenobiotics (drugs) out of certain places. example: p-gp is an important efflux transporter that keeps many drugs in the intestine and out of the brain
37
What is an example of p-gp
benadryl and allegra benadryl is 1st generation antihistamine (drowsy) Allegra is 2nd generation antihistamines (non drowsy) this works because allegra has gp-gp transporters that keep the allergy medicine in the systemic circulation but out of the CNS
38
blocking histamine receptors peripherally helps_______ but blocking histamine receptors in the CNS causes ______
blocking histamine receptors peripherally helps allergies but blocking histamine receptors in the CNS causes drowsiness
39
What are the additional considerations when considering the absoprtion of tablets/capsules
dissolution of the drug from tablet or capsule form stability of drug rate of gastric emptying intestinal motility and drug interactions
40
dissolution of the drug from tablet or capsule form includes
that the drug must be in solution to be absorbed and different formulations dissolve at different rates
41
What does rate of gastric emptying entail
absorption is much faster in the small intestine (more surface area, more permeability, more blood flow) the speed of getting to small iintestine limits the sped of the drug getting absorbed food slows gastric emptying
42
what does inestinal motility and drug interactions entail
pH, surface area, permeability, and efflux transporter density drugs may bind to other contents of the intestine which can prevent absorption
43
What are the 2 possible pathways that drugs given by IM/SQ/ID can enter the systemic circulation
diffusion through capillary membranes getting carried through the lymph system
44
the pathway consisting of diffusion through capillary membrane is forgiving of ____ and not forgiving of ____
very forgiving of polarity and charge less forgiving of size
45
the pathway of getting carried through the lymph system, name 4 facts about this pathway
1. lymph system is the body's "garbage collector" 2. large molecules and proteins tend to go this route 3. lymph system moves very slowly - which makes absorption slow 4. enzymatic breakdown of drugs can occur in lymph nodes
46
Speed of absorption when given IM/SQ/ID is affected by
slow moving systems site of injection local bloodflow temperature rubbing at injection site
47
Vancomyocin ( a large hydrophilic molecule) would be be absorbed which route and why
IV because the large molecule = hard to absorb and hydrophillic = good diffusion through capillary walls
48
Once any drug reaches the systemic circulation, it gets carried through the _____________, a major site of metabolism
liver
49
What is the key difference between enteral and parenteral that has to do with passing through the liver
enteral drugs go through the liver before they reach the systemic circulation via the hepatic portal vein
50
Aside from first pass (getting metabolized by the liver first) what are three other hazards along the way for enteric drugs
1. not getting absorbed into the gut wall (exretion into feces) 2. breakdown (metabolism) by the gut wall 3. excretion into bile by liver
51
Once a drug gets to the systemic circulation, it starts (reversibly)____________________
Once a drug gets to the systemic circulation, it starts (reversibly) distributing itself to different body tissues (extravascular space)
52
Where the drug distributes to in the body depends on:
1. how well it diffuses through different membranes (size lipophilicity, charge) 2. what it likes to bind to (proteins in the plasma or other tissues)
53
protein bound drugs
drugs that bind heavily to plasma proteins and cannot diffuse through membranes
54
unbound or free drugs
the only type of drug that can leave the bloodstream (or be active)
55
some drugs have a particular affinity for certain _________. give an example
tissues bisphosphonates (osteoporosis drugs) have high affinity for bone minerals
56
What is the formula for volume of distribution and what does it represent
represents how the drug gets distributed by finding whether the drug stays mostly in the bloodstream or if it enters other tissues Volume of distribution = total amount of drug in body(mg)/plasma concentration of drug (mg/L)
57
If the drug stays in the bloodstream what will the volume distribution be
close to the volume of the blood
58
If the drug diistributes widely around the body, what will the Volume of distribution (Vd) be
very large.
59
The Vd is an "_________"
imaginary volume go back and listen to slide 33
60
Go back and do checkpoints 7,8,9
61
metabolism is also known as
biotransformation
62
what happens during metabolism/biotransformation
a parent drug is converted to a metabolite, which is a different chemical form that is more readily excreted from the body
63
metabolites can be
active or inactive for example, morphine has both active and inactive metabolites
64
prodrugs
druugs that have inactive parent forms and active metabolites such as plavix (clopidogrel)
65
Metabolism is performed by ________ which are present in tissues all over the body, but the ______ is the most important site of metabolism
enzymes, liver
66
Phase one metabolism includes
oxidation, reduction, or hydrolysis
67
phase two metabolism includes
conjugation, acetylation and methylation
68
some drugs such as hydrophobic drugs go through ________ while others such as hydrophillic drugs _______
some drugs such as hydrophobic drugs go through the phases sequentially (some just do one, or two, some do both) while others such as hydrophillic drugs leave the body before gettting metabolized at all
69
loves lipids---> _________ loves water ----> _________
loves lipids---> liver loves water ----> urine
70
stopped at slide 40
ok

Pharmacology (19 decks)

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