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Pharmacology > Week 2 Pharmacodynamics and Pharmacokinetics > Flashcards

Week 2 Pharmacodynamics and Pharmacokinetics Flashcards

1
Q

What is pharmacokinetics?

A

What the body does to the drug!

  • ADME
  • Absorption, Distribution, Metabolism, Excretion
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2
Q

What are 3 ways that drugs cross the cell membrane?

A
  • Channels and pores (Small compounds)
  • Transport systems (require energy and depends on drug structure)
  • Direct Penetration (MOST COMMON)
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3
Q

T/F Lipid soluble drugs can easily pass through the membrane?

A

True

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4
Q

Ions and polar molecules?

A

Can not pass through cell membrane

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5
Q

Absorption

A

-Movement of drug from it’s site of administration into the blood

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6
Q

What are factors affecting absorption?

A
  • Rate of dissolution (if a drug is liquid it dissolves quicker)
  • Surface Area (larger the area the faster the absorption)
  • Higher the blood flow the faster the absorption
  • lipid solubility (the higher the faster it is absorbed)
  • pH partitioning ( enhances when drug molecules can be ionized. Manipulate the environment to increase absorption)
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7
Q

Routes of Absorption—– What types are Enteral?

A

Absorbed in the GI Tract (ORAL, Rectal)

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8
Q

Routes of Absorption — What type are Parenteral?

A

IV, IM, SQ

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9
Q

What are some local routes of absorption?

A

Topical, Transdermal, vaginal, inhaled, rectal, direct injection, intraosseous

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10
Q

What is an enteric coated drug?

A

A drug that has an extra coating that protects the drug from the acidity of the stomach. Should not be chewed!

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11
Q

What is a sustained release drug?

A

A drug where the formulation has been changed and is made to last longer.

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12
Q

What is Distribution?

A

-Movement of drugs throughout the body

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13
Q

Types of Distribution: Blood Flow to the Tissues

A
  • drugs being carried by blood to the tissues since tissue is site of action.
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14
Q

Types of Distribution: Exiting the Vascular system

A
  • Drugs can normally pass through capillary cells.
    Exceptions are:
    BBB- due to tight junctions (neonates are vulnerable)
    Placenta- drug can cross placenta and can reach fetus
    Protein Binding: If a drug binds with protein it will stay in the drug! Only the amt that is free goes to site of action. Interactions with other protein bound drugs can cause one to be bound and one to be unbound. The unbound one can cause toxicity.
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15
Q

Types of Distribution: Ability of the drug to enter cell

A

How it can cross cell membrane

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16
Q

What is drug metabolism?

A

Enzymatic alteration of a drug

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17
Q

Cytochrome P450 system

A
  • 12 closely realted enzymatic families
  • drug-drug interactions
  • changes the drug
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18
Q

What changes occurs with CYP450 System?

A
  • Accelerated excretion, inactive, activation, decrease/increase toxicity, inducer, inhibitor
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19
Q

What is the First Pass Effect?

A

Rapid hepatic inactivation of drugs!

  • An oral drug goes to GI tract and goes directly to liver. Liver metabolizes drug.
  • Decreases therapeutic response by inactivating a small portion of drug
  • goes to system circulation
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20
Q

Effects of the First Pass?

A
  • Delays drug entry into blood stream
  • lesser amount of drug in body
  • this is why oral drug dose is higher
  • does not apply to sublingual
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21
Q

What organ plays a part in metabolism?

A

THE LIVER

22
Q

What is Excretion?

A

Removal of drugs from the body

23
Q

What organ plays a part in excretion?

A

The kidneys

24
Q

Where is can drugs be excreted?

A

Bile, sweat, saliva, breastmilk, skin, hair, tears, lungs

25
Q

3 mechanisms of the kidneys that are involved with excretion?

A
  • GFR : Protein bound drugs affect this
  • Tubular resorption: lipid drugs move back into blood stream and avoid excretion
  • Active Tubular secretion: pumps drugs from blood back into urine.
26
Q

Drug Plasma Levels

A
  • Used to regulate drug response

- a specific plasma level of drug must be achieved before therapeutic effects happen

27
Q

Minimum drug level

A

-Will not be high enough to elicit a response from patient

28
Q

Therapeutic Range

A

Narrow or broad range of desired response

29
Q

Toxic Drug level

A

too much drug in the body that causes harmful effects

30
Q

Single Dose Time Course

A
  • Drug levels rise during absorption and distribution. Decline during metabolism and elimination.
31
Q

Drug Half Life

A
  • Time for drug in body to decrease by 50%
  • More drug that’s in larger amount is lot during half life
  • Half live can vary from mins- weeks
32
Q

Half life is a determinant of

A
  • duration of action
  • time required to reach steady state
  • dosing frequency
33
Q

How many half lives does it take for a drug to become therapeutic in the body? For it to hit a plateau? For most of the drugs to be eliminated from the body?

A

4 half lives

34
Q

Plateau

A

-The amt of drug eliminated is equal to amt that is administered

35
Q

Loading Doses

A

Helps get a patient to a plateau much faster

36
Q

Repeated doses

A

Doses that are given that are influenced by rate of absorption and elimination

37
Q

What is a Peak Level?

A

Greatest concentration of drug in the blood.

-If level is too high? Hold dose and repeat blood draw

38
Q

What is the through level?

A

The lowest concentration of drug in blood

39
Q

What can you do based off of peak and through levels?

A
  • Helps to change dose of medications

- Frequency of medication

40
Q

Pharmacodynamics

A

What drugs do to the body and how they do it?

41
Q

Dose Response Relationships

A

-As dosage becomes larger, response becomes larger
-Efficacy :the largest effect a drug can produce. (Morphine has no ceiling versus Tylenol)
-Potency: Dosage needed to produce effect
(Dilaudid 0.3mg is more potent than Morphine 2.0mg)

42
Q

Receptors and Drug Selectivity of Drug Action

A
  • The more selective a drug is, the fewer side effects it will produce. Does not equal safety
  • Each type of receptor participates in the regulation of a few processes
  • Drugs bound to receptors only mimic the body’s natural functions
  • Lock and key matches only one receptor
  • Affinity- strength: How attracted is that drug to receptor. Drugs that have high affinity can bind to receptors when concentration is low
  • Intrinsic activity- ability to activate a receptor upon binding (related to max efficacy)
43
Q

Agonists

A
  • Drugs that activate receptors and mimic the body’s response. Results in process that goes faster of slower.
44
Q

Antagonists

A
  • Block receptor activation. There is affinity but no intrinsic activity. No observable effect.
45
Q

Competitive Nonantagonist

A
  • bind irreversibly to receptors

- effect is non reversible even if an agonist is added

46
Q

Competitive Antagonist

A
  • bind reversibly with whatever agent is available in the highest concentration
  • effect is reversible if agonist is added
47
Q

Partial Agonists

A
  • have only moderate intrinsic activity

- has both antagonist and agonist

48
Q

ED50

A

Effective dose required to produce a therapeutic response in 50% of the population.

49
Q

LD50

A

The does that is lethal to 50% of animals

50
Q

Therapeutic Index

A
  • Highest does required to produce a therapeutic effect must be lower than the lowest dose to produce death.
  • The larger and higher the TI the more safe a drug is more distance.
51
Q

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A

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Pharmacology (14 decks)

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