Pharmacology Principles Flashcards

Exam 1 (66 cards)

1
Q

What are the three phases of drug action?

A

Pharmaceutic phase, pharmacokinetic phase, and pharmacodynamic phase

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2
Q

What is the pharmaceutic phase of drug action?

A

Dissolution (the drug begins to dissolve so it can be used).

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3
Q

What is the pharmacokinetic phase of drug action?

A

Drug is moving through the body and what the body does to the drug (absorption, distribution, metabolism, excretion)

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4
Q

What is the pharmacodynamic phase of drug action?

A

What the drug does to the body. The mechanism of action, intended effect of the drug and therapeutic action.

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5
Q

What route does the pharmaceutical phase of drug action only occur with?

A

Oral

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6
Q

What are the four processes of the pharmacokinetic phase of drug action?

A

Absorption (small intestine)
Distribution (through blood)
Metabolism/biotransformation (liver)
Excretion (kidneys)

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7
Q

Describe drugs crossing cell membranes, specifically the phospholipid layer.

A

Drugs must be lipid soluble to pass membrane. Water soluble drug require passage through channels or pores (transport mechanisms)

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8
Q

What is the first pass effect?

A

Metabolism of drug before systemic circulation. The % of drug broken down in the liver before going into systemic circulation.

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9
Q

What is bioavailability?

A

The amount of drug left after first pass

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10
Q

What is the bioavailability of PO medications?

A

Varies (liver takes some of it)

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11
Q

What is the bioavailability of IV medications?

A

100%

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12
Q

What are the three routes of absorption?

A

Enteral, parenteral, and topical (transdermal)

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13
Q

Describe the enteral route of absorption.

A

By way of GI tract (oral/gastric mucosa, small intestine, rectum)

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14
Q

Describe enteric coated enteral route.

A

EC intended to break down in small intestine NOT stomach- first pass effect

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15
Q

Describe oral enteral route.

A

PO break down starts in stomach, absorbed in small intestine- first pass effect

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16
Q

Descibe sublingual, buccal, and rectal enteral route.

A

All highly vascularized tissue- no first pass effect, by-passes liver

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17
Q

Describe the parenteral route of absorption.

A

SQ, IM, IV, intrathecal (into spinal cord), epidural (the space around spinal cord)
IV is the fastest (no barriers to absorption, often irreversible)
Does not go through first-pass effect

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18
Q

Describe topical (transdermal) route of absorption.

A

Application of meds to body surfaces (eyes, skin, ears, nose, lungs)

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19
Q

What is distribution in the pharmacokinetic phase?

A

Distribution is the movement of the drug through the body
Process by which the drug molecules leave the blood stream and arrive at the site of action
Depends largely on adequacy of blood circulation

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20
Q

What could be some disruptions in distribution?

A

Decreased blood flow = decreased distribution (less effective)
Peripheral vascular disease
Abscesses (< blood flow to site due to inflammation)
Tumors

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21
Q

What is the blood brain barrier?

A

Cells in the capillary wall in the brain with very tight junctions that prevent drugs passages.

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22
Q

What drugs can cross the blood brain barrier (BBB)?

A

Only drugs that have a transport system or are lipid-soluble can cross the BBB
(Alcohol, Glucose)

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23
Q

Describe the protein-binding effect during distribution.

A

Temporary storage of drug molecule that allows the drug to be available for a longer period of time
Goal: maintain a steady free drug concentration aka steady state
Remember, only unbound drug is active and free to exert effects

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24
Q

What is the primary plasma protein during the protein-binding effect?

A

Albumin

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25
What happens when the patient has hypoalbuminemia (due to malnutrition or liver disease) during the protein-binding effect?
More free drug is available for distribution to tissue site Possibility of overdose and toxicity
26
Describe metabolism (biotransformation) during the pharmacokinetic phase.
Method by which drugs are inactivated or biotransformed (called a metabolite)
27
What organ is the major site for drug metabolism?
The liver
28
Describe drug metabolism in the liver.
Converts lipid-soluble (active) drugs into water-soluble (inactive) metabolites Kidney can excrete these metabolites Uses Cytochrome P-450 enzymes to break drugs down
29
Describe metabolism using Cytochrome P-450 enzymes (CYP450).
Cytochrome P-450 = a group of isoenzymes that metabolize drugs in the liver About 1/2 of all drugs metabolized by this system Drug-drug interactions can occur when drugs metabolized by the same isoenzyme are taken concurrently
30
What is the clinical significance of CYP450?
Substrate- if drug uses CYP450 system for metabolism to convert to an active form Inducer- Speeds up metabolism of CYP450 system. Reduces the amount of drug in body and reduces therapeutic effect Inhibitor- slows down metabolism of the CYP450 system (> amount of drug in body, > risk of toxicity)
31
What is a known CYP450 inhibitor?
Taking grapefruit juice with another drug that uses this system increases the amount of drug in the body Can lead to toxicity
32
Describe excretion during the pharmacokinetic phase.
Elimination of drug from the body- generally, only hydrophilic drugs can be excreted effectively Kidney is the major site of excretion Some of the drug is secreted and some is reabsorbed Important in maintaining a steady state
33
What are the three ways that drugs can be excreted through the kidneys?
Glomerular filtration Tubular secretion Tubular reabsorption
34
How does kidney disease or dysfunction effect excretion?
Decreased excretion = drugs build up and cause toxicity
35
What is the glomerular filtration rate (GFR)?
Best measure of kidney function Calculated from the creatinine level, age, body size, and gender GFR of drugs is related to free drug concentration in plasma
36
Describe half-life during excretion.
Serum half-life (T 1/2) is time required for the serum concentration of a drug to decrease by 50% Takes 5 half-lives for 97% of drug to be eliminated T 1/2 varies from drug to drug
37
How many half-lives would it take for "steady state" to occur?
4-5
38
When does steady state occur?
When intake of drug equals amount metabolized/excreted
39
What does the half-life determine?
Dosing interval
40
What is the goal of around the clock dosing (ATC)?
Maintain 50% concentration in body
41
What is onset?
The time it takes for the drug to elicit therapeutic response (latent period)
42
What is peak?
The time it takes for the drug to reach its maximum therapeutic effect
43
What is duration?
The time the drug concentration is sufficient to elicit a therapeutic response
44
What is phase 3 of the drug action?
Pharmacodynamic phase
45
Describe the pharmacodynamic phase.
What the drug does to the body Drugs may increase, decrease, replace, inhibit, destroy, protect, or irritate to CREATE A RESPONSE Drugs exert MULTIPLE rather than single effects on the body
46
Describe the role of receptors during the pharmacodynamic phase.
Receptors are proteins located on cell surfaces Chemicals in the body interact with drugs to produce effects These chemicals BIND with the drug = drug-receptor complex
47
What does an agonist do?
Stimulates/activates A drug that has the ability to INITIATE a desired therapeutic effect by BINDING to a receptor
48
What does an antagonist do?
Inhibits/blocks A drug that produces its action NOT by stimulating receptors but PREVENTING/BLOCKING/INHIBITING other natural substances from binding and causing a response
49
Describe receptor-less activation.
Not all drug responses involve receptors Some drugs act through simple physical or chemical interactions with small molecules
50
What is a therapeutic index?
The measure of reltive safety of drug
51
What is a narrow therapeutic index (NTI)?
Has a ratio of lowest concentration at which clinical toxicity occurs
52
What is a black box warning?
Required by the FDA for drugs that are especially DANGEROUS Is the strongest safety warning a drug can carry and still remain on the market Must appear prominently (on package insert, product label, and any advertising)
53
What are medication errors a major cause of?
Morbidity and mortality (3rd leading cause of death)
54
Describe the processes to prevent medication errors.
1. Restrict high-alert drugs and medication routes 2. Practice drug differentiation. Use of "tall-man" lettering for look-alike drug names 3. Use computerized systems for administering medications 4. Make patient information readily accessible 5. Standardize and simplify 6. Apply reminders 7. Include the patient in therapy 8. Don't use trailing zeros 9. Use leading zeros
55
What are high alert medications?
Institute for Safe Medication Practices (ISMP) identified these drugs to most likely cause serious harm or death (Insulin, heparin, opioids, injectable potassium chloride, neuromuscular blocking agents, chemotherapy drugs)
56
How do drug interactions occur?
1. Drug- drug. May be intended or unintended. Increased risk with polypharmacy and narrow therapeutic index drugs 2. Drug- food 3. Drug- herb 4. Drug- disease (kidney/liver disease)
57
How can the nurse minimize drug interactions?
Minimize the number of drugs the patient receives Take a thorough drug history- reconcile medications Be extra vigilant in monitoring when a patient is taking drugs with a narrow therapeutic index
58
Describe how a drug interaction increases therapeutic effects using additive effects.
2 drugs taken with similar MOA
59
Describe how a drug interaction increases therapeutic effects using synergism/potentiation.
2 drugs with DIFFERENT MOA but result in a combined drug effect greater than that of either drug alone
60
Describe how a drug interaction increases therapeutic effects using activation of drug-metabolizing enzymes in the liver.
Decreases metabolism rate of the drug (CYP450 system)
61
Describe how a drug interaction increases therapeutic effects using displacement.
Displacement of one drug from plasma protein-binding sites by a second drug increases the effect of displaced drug
62
Describe how a drug decreases therapeutic effects using an antidote.
Drug given to ANTAGONIZE (stop) the toxic effects of another drug
63
Describe how a drug decreases therapeutic effects using decreased intestinal absorption.
Applies to PO medications
64
Describe how a drug decreases therapeutic effects using activation of drug-metabolizing enzymes in the liver (enzyme inducers).
Increased metabolism rate of the drug [quicker out of the system] CYP450 system
65
Describe older adults and pharmacokinetic consequences.
Decreased production of CYO450 enzymes increased risk for drug interactions (can < up to 30%) Hepatic changes- drugs metabolized more slowly Cardiac/Circulatory changes- impaired circulation = decrease distribution of drugs Gastrointestinal changes- decreased absorption of oral drugs Renal changes- drugs excreted less completely
66