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Advanced Pharmacology > Pharmacokinetics > Flashcards

Pharmacokinetics Flashcards

1
Q

Pharmacodynamics

A

what the drug does to the body

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2
Q

Pharmacokinetics

A

what the body does to the drug- absorption, distribution, metabolism, elimination

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3
Q

Pharmacogenetics

A
  • individual variation in pharmacokinetics usually caused by a single gene
  • genetic tendency
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4
Q

Pharmacogenomics

A
  • variations in pharmacokinetics and dynamics, usually due to multiple genes and environment
  • how predisposition is expressed
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5
Q

Agonist

A

bind to a receptor on or within a cell and produces a response

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6
Q

Antagonist

A

bind to a receptor to block or reverse the action of an agonist

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7
Q

Receptors

A
  • located on cell membranes and within the cell

- enzymes, nucleic acids, membrane-bound proteins

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8
Q

Full agonist vs Partial agonist

A
  • full agonist produces 100% response that completely reverses the condition (ex/ albuterol)
  • partial agonist cannot produce 100% response, even at very high doses (ex/ morphine)
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9
Q

Competitive vs Noncompetitive antagonist

A
  • Competitive- compete for the same binding site

- Noncompetive- binds to different site and decreases the agonist response, partially interferes

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10
Q

Efficacy

A
  • Max response a drug can produce

- How well a drug produces a response/ quality of response

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11
Q

Potency

A
  • amount of drug required to produce effect

- dose required for a response

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12
Q

Bioavailability

A
  • fraction of drug that reaches circulation in a form that is ready to engage in a biological response
  • a drug can have no effect if it is not bioavailable
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13
Q

How does route of administration affect bioavailability?

A

few roadblocks = greater bioavailability

IV => IM => PO

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14
Q

How does GI motility affect bioavailability?

A

unpredictable effect on drug absorption- increased motility can increase or decrease absorption

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15
Q

How do drug-drug interactions in the gut affect bioavailability?

A
  • drugs can increase pH to effect absorption
  • antacids/ bile acid binding drugs can inactivate/impair absorption
  • drugs that alter GI motility can have unpredictable effects on other drugs
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16
Q

How do drug-drug interactions in serum affect bioavailability?

A

protein-binding- when drugs bind to the same protein, the drug that has less affinity for binding will have exaggerated effect, could cause toxicity

17
Q

How does absorption affect bioavailability?

A

Absorption- the ability of the drug to reach circulation and target tissue
-circulation is key factor- poor circulation= poor absorption

18
Q

What factors influence pharmacokinetics?

A

Nongenetic- age, organ function, concomitant therapy, drug interactions, disease state
Genetic- drug-metabolizing agents, drug transporters, drug targets (these remain stable across lifespan)

19
Q

How does drug metabolism affect bioavailability?

A
  • Drug metabolism- mechanism where administered agent is converted to a form that prepares it for elimination- converts it to water soluble form
  • drugs have to have some lipophilia to act in the body and then need to be converted to hydrophilic to be eliminated
20
Q

CYP450 cascade

A

primary mechanism of drug metabolism,

21
Q

CYP450 cascade

A
  • primary mechanism of drug metabolism
  • series of oxidation-reduction reactions that prepare a drug for excretion
  • responsible for significant adverse effects
  • cause issues when CYP450 inhibitor or inducer are given with substrate- cause toxicity or subtherapeutics
22
Q

What is the first pass effect?

A
  • a large portion of an oral drug is metabolized during the first pass through the liver before reaching circulation, decreasing bioavailability when drug is given in active form
  • drugs given as “prodrug” are activated by the liver, therefore more bioavailable
  • decreased hepatic function can cause toxicity for active drugs or subtherapeutic levels for prodrugs
23
Q

Drug elimination

A

Kidney is major route- need good renal blood flow and function

24
Q

Drug dosing steady state

A
  • goal is to maintain steady state within therapeutic window between minimally toxic concentration (MTC) and the minimally effective concentration (MEC)
  • often takes 5 half-lives (doses) to achieve steady state
25
Q

IM administration in pediatrics

A
  • not an efficient mode d/t decreased muscle tissue

- erradic blood flow in illness makes absorption unpredictable

26
Q

Transdermal and topical administration in pediatrics

A
  • greater skin surface area, higher water content, and thinner stratum corneum can all increase absorption
  • occlusive dressings (diapers) can decrease evaporation => increase absorption
27
Q

Gastric pH in pediatrics

A
  • neonate- very low pH in first couple days, then pH is quite high (relative achlorhydria for first month)
  • gastric acidity reaches adult levels by age 3
  • pH affects absorption- drugs that are weak bases are poorly absorbed in acid environment and vice-versa
28
Q

Gastric motility in pediatrics

A
  • GI transit time and peristaltic activity is prolonged during infancy
  • BF infants longer transit time than formula fed
  • infants have greater intestinal surface area => increased absorption
  • more normal transit time @ 6-8 mnths old
29
Q

Total body water in pediatrics

A
  • higher percentage than adults (70-75%), so may need higher doses of hydrophilic drugs to achieve therapeutic blood levels
  • adult levels at age 6-7
30
Q

Protein binding capacity in pediatrics

A
  • neonates- lower serum plasma protein available for binding
  • basic drugs more bioavailable as they bind to glycoprotein and lipoprotein rather than albumin (acidic drugs)
  • competition for binding sites between meds and endogenous substances (bilirubin) => cross BBB to cause kernicterus
31
Q

Drug elimination in pediatrics

A
  • renal blood flow reaches adult levels @ 5-12 mnths
  • GFR @ adult levels at 3-5 mnths
  • tubular secretion and absorption - 7-12 mnths
  • longer half life d/t prolonged metabolism and slower excretion
32
Q

Considerations for drugs during pregnancy

A

-can it cross the placenta?

may be safe to give in pregnancy but is not ok for infants

33
Q

consideration for lactation

A
  • can it cross into breast milk?
  • infant circulation is responsible for metabolism and excretion
  • safe for infant = safe for BFing
34
Q

Drug administration in the elderly

A
  • less water-soluble content = longer half-life
  • less muscle, more fat
  • decreased renal perfusion
  • comorbid diseases impact metabolism and excretion

Advanced Pharmacology (9 decks)

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