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Pharmacology > Pharmacokinetics and Pharmacodynamics > Flashcards

Pharmacokinetics and Pharmacodynamics Flashcards

1
Q

3 ways of membrane crossing

A
  1. Channels and pores
  2. Transport system
  3. Direct penetration (lipid soluble only)
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2
Q

First pass effect

A

The initial metabolism in the liver of a drug absorbed from the GI tract before drug reaches systemic circulation through the bloodstream

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3
Q

Where does metabolism usually take place?

A

Liver

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4
Q

Therapeutic range

A

Between MEC and toxic

Larger range = safe

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5
Q

What factors affect absorption?

A 
Rate of dissolution
Surface area
Blood flow
Lipid solubility
Rate of administration
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6
Q

Enteric coated

A

Special coating on a drug that prevents absorption until drug reaches small intestine
Protects stomach or keeps drug from being destroyed by stomach acids

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7
Q

CYP450

A

Group of enzymes in GI tract and liver that metabolize drugs —> take fat soluble item (drug) and make it water soluble so it can be excreted

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8
Q

3 steps of renal excretion

A
  1. Glomerular filtration - filtration moves drugs from blood to urine
  2. Passive tubular reabsorption - lipid soluble drugs move back into blood while polar and ionized drugs remain in the urine
  3. Active tubular secretion - tubular pumps for organic acids and bases and moves drugs from blood to urine
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9
Q

Can ions be excreted?

A

Yes - they are not lipid soluble

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10
Q

T/F: drugs can only elicit or block normal physiologic responses

A

True

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11
Q

Intrinsic activity (efficacy)

A

Intensity of effect that the drug produces, ability of a drug to active the receptor after binding

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12
Q

Interpatient variability

A

The dose required to produce a therapeutic response can vary substantially among patients

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13
Q

ED50

A

Effective dose in 50% of population

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14
Q

LD50

A

Dose that is lethal in 50% of population

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15
Q

Drug

A

Any chemical that affects living systems

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16
Q

Is there any such thing as an ideal drug?

A

No

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17
Q

Clinical pharm

A

Study of drugs in humans

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18
Q

Therapeutics

A

Medical use of drugs to diagnose, treat and prevent

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19
Q

Ideal drug properties

A

Effectiveness, safety, selectively, reversible, predictability, ease of administration, freedom from drug interactions, low cost, chemical stability, possession of simple generic name

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20
Q

Pharmacokinetics

A

The process by which drugs are absorbed, distributed, metabolized and excreted

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21
Q

Pharmacodynamics

A

What the drug does to the body and how does it illicit a response

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22
Q

P-glycoprotein (P-gp)

A

Transmembrane protein that transports a wide variety of drugs out of cells

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23
Q

Pka

A

Ph at which the drug is 50% ionized

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24
Q

Ion trapping

A

Occurs when a drug molecule changes from ionized to non ionized from as it moves from one body compartment to another 0 drug will accumulate on the side that favors the ionized state and cannot cross back over

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25
Where will acidic drugs accumulate?
Alkaline side
26
Where will basic drugs accumulate?
Acidic side
27
Administration routes
enteral (GI), PO, PR (per rectum)
28
Parenteral route
IV, IM (not GI)
29
Distribution
Movement of drug from blood into the interstitial spaces and cells to the site of action
30
What is distribution determined by?
Blood flow to tissues, ability of drug to exit vascular system, ability of drugs to enter the cells
31
Volume of distribution
Reflection of how much drug is left in vasculature
32
What is a small Vd?
Drug is mostly held in vasculature
33
What is large Vd?
Drug is widely distributed outside of vasculature
34
What affects Vd?
CO, perfusion of tissues, type of capillary system, polarity of drug molecules, protein binding
35
Metabolism (bio transformation)
How bio chemical reactions alter drugs in the body | *does not always inactivate the drug
36
Consequences of metabolism
Accelerated renal excretion, drug inactivation to inactive metabolites, increased therapeutic action (metabolites are more effect), activation of prodrugs (inactive until metabolism), increased or decreased toxicity
37
CYP450 inducers
Drugs that increase synthesis of enzymes —> increased enzyme concentration and increased drug metabolism —> decreased therapeutic response
38
CYP450 inhibitors
Decrease synthesis of enzymes —> decreased drug metabolism —> increase drug effects/risk for toxicity (i.e. grape fruit juice)
39
Most common excretion site
Renal system
40
Other methods of excretion
Feces, sweat, saliva, breast milk, expired air
41
Minimum effective concentration (MEC)
The plasma drug level below which therapeutic effects will not occur
42
Toxic concentration
Level of drug that will result in serious side effects
43
Half life
Time required for amount of drugs in body to decrease by 50%
44
Plateau
- steady level achieved once repeated doses cause build up - amount of drug eliminated b/w doses equals amount administered - when a drug is administered repeatedly in the same dose, plateau will be reached in approx. 4 half lives
45
Peak level
Highest concentration
46
Trough level
Lowest concentration
47
Zero order
Same amount of drug will be metabolized per hour no matter how much drug is present (i.e. alcohol)
48
First order
% of drug metabolized is related to dose size | A larger dose = a larger amount metabolized
49
Types of receptors
1. Cell membrane embedded enzymes 2. Ligand gated ion channels 3. G protein coupled receptors 4. Transcription factors (intracellular)
50
Affinity (potency)
How much drug must be administered to elicit a desired effect Strength of attract b/w drug and receptor
51
Agonists
Mimic action of endogenous ligand and activate receptors
52
Antagonists
Produce their effects by preventing receptor activation by endogenous regulatory molecules and drugs
53
Competitive antagonists
Bind reversibility to receptors
54
Noncompetitive antagonists
Drug that reduces the effect of an agonist but does not compete at the receptor site -irreversible
55
Partial agonist
Drugs that interact with a receptor to stimulate a response but to a lesser intensity
56
Dose response curve
As dose increases, response becomes progressively larger
57
Orthosteric sites
Same site as endogenous ligand
58
Allosteric sites
Alternative site from endogenous ligand
59
Upregulation with continues antagonist usage
Receptors will proliferate
60
Downregulation w/ continuous agonist usage
Receptors decrease and drugs elicit less of a resposne
61
Therapeutic Index (TI)
Measure of drug’s safety ratio (ED50/LD50) | Wider TI = safe
62
Adverse drug effects
Any noxious, unintended, and undesired effect that occurs at normal drug doses —> can be annoying to life threatening
63
Side effect
Nearly unavoidable effect that occurs with therapeutic doses
64
Toxicity
Negative effects due to excessive drug doses
65
Allergic reaction
Immune response
66
Black boxed warning
Strongest safety warning a drug can carry and still remain on the market
67
What are the highest fatal potential medication errors?
Wrong route, wrong drug, overdose
68
T/F: nurses are required to report medication error
TRUE - to institution, to provider, national program exists (MER)

Pharmacology (6 decks)

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