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Pharmacology and Nutrition > Pharmacokinetics: Part II > Flashcards

Pharmacokinetics: Part II Flashcards

1
Q

drug administration =

A

oral
IV
intraperitoneal
subcutaneous
intramuscular
inhalation

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2
Q

absorption and distribution =

A

membranes of oral cavity, GI tract, peritoneum, skin, muscles, lungs

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3
Q

binding =

A

target site = neuron receptor

inactive storage depots = bone and fat

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4
Q

inactivation =

A

liver

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5
Q

excretion =

A

intestines, kidneys, lungs, sweat glands

excretion products
> feces
> urine
> water vapor
> sweat
> saliva

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6
Q

All drugs must be eliminated:

A

terminate effect

prevent excessive accumulation of drug = maintain proper levels

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7
Q

Mechanisms of elimination:

A

Biotransformation = metabolism

Active Form & Metabolites = excretion

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8
Q

Alternative to elimination =

A

accumulation of drugs or metabolite = adverse event and/or tissue damage

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9
Q

Comprehensive Metabolic Panel =

A

> blood test

measures:
> glucose level
> electrolyte and fluid balance
> kidney function
> liver function

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10
Q

Drug Metabolism

A

Chemical changes in drug following administration

Drug (active) -> metabolite (inactive/reduce activity)

Exception: Prodrug = Inactive when administered, metabolisms converts to active form

ex)
L-Dopa = dopamine metabolite, Parkinson’s Disease

Cortisone = corticosteroid metabolite, injection for inflammation

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11
Q

Metabolism: Drug to Metabolite

A

phase I: oxidation, reuction, and/or hydrolysis
> following phase I the drug may be activate or most often, inactivated

phase II: conjugation
> some drugs enter phase II metabolism -> conjugated products = usually inactive

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12
Q

End-product of metabolism:

A

More polar compound (covalent bonds)/ionized compound (ionic bonds): +/- charge

Non-lipid soluble or Water soluble

More easily excreted in urine

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13
Q

Oxidation:

A

Loss of electron or gain in oxidation state

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14
Q

Reduction:

A

Gain of electron or loss in oxidation state

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15
Q

Hydrolysis:

A

Original compound broken into separate parts due to uptake of H and OH

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16
Q

Conjugation:

A

Following oxidation, reduction, or hydrolysis = original drug coupled with endogenous substance

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17
Q

Yields a large polar/ionized metabolite by:

A

adding endogenous hydrophilic groups to form non-lipid/water-soluble inactive compounds that can be excreted by the body

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18
Q

Non-ionized form to Ionized form

A

Compounds transformed to non-lipid/more water-soluble form

NO LONGER PASS READILY THRU CELL MEMBRANES = EXCRETION

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19
Q

Water soluble drugs =

A

ionized
polar
charged

difficult to permeate cell membranes

ex) water soluble vitamins

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20
Q

Lipid soluble drugs =

A

unionized
non-polar
uncharged

easy to permeate cell membranes

ex) anesthesia

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21
Q

Phase I liver detoxification =

A

fat-soluble toxins

oxidation
reduction
hydrolysis
hydration
dehalogenation

nutrients needed:
vitamin B12, folic acid, glutathione

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22
Q

Phase II liver detoxification =

A

water-soluble toxins eliminated via: urine, bile, stool

conjugation pathways

sulfation
glucoronidation
acetylation
amino acid conjugation
methylation

nutrients needed:
methionine, vitamin B12, vitamin C, glutamine, folic acid

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23
Q

Elimination = ___ + ___

A

metabolism
excretion

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24
Q

Metabolism: Enzymes

A

Primarily produced in the Liver

Also produced in lungs, kidneys, GI epithelium, skin

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25
Q

Enzyme Induction:

A

enzyme production triggered due to the presence of a substance/drug

prolonged use of drugs = body adjusts and enzymatically destroys drugs more rapidly = enzyme induced drug tolerance = increased drug dosage

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26
Q

Enzyme Induction results in Drug Tolerance =

A

reduction in drug’s effectiveness

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27
Q

Drug Excretion

A

Primary site: Renal Excretion

Nephron = functional unit of kidney

Polar compounds/water soluble molecules/ionized compounds = excreted in urine

28
Q

Metabolites filtered in glomerulus =

A

PCT -> LH -> DCT -> CD -> urine

1) proximal tubule
2) descending loop of Henle
3) thick segment of ascending limb
4) distal tubule
5) collecting duct

29
Q

Other areas of drug excretion:

A

Lungs: excrete volatile drugs administered by inhalation = anesthetic gases

GI & liver: bile -> bile duct -> duodenum -> feces

Other minor routes: sweat, saliva, breast milk, tears, hair

30
Q

Drug Elimination

A

Drug Metabolism (inactive metabolites) & Drug Excretion (intact medication)

Removal of a drug from the body

mostly through urination

kidneys clear metabolic waste and foreign substances by filtering the blood

31
Q

Drug delivery > Elimination =

A

drug accumulation

32
Q

Elimination > Drug delivery =

A

no therapeutic effect

33
Q

2 Factors that effect the balance of drug accumulation, therapeutic effect & elimination:

A

Clearance and Half-life

34
Q

Clearance =

A

volume of plasma cleared of a drug per unit of time

predicts the rate of elimination

volume/time

35
Q

Half-Life =

A

amount of time it takes for the plasma concentration to drop by 50%

determined by drug chemical structure

36
Q

Relationship of Clearance (CL) and Half-life

A

Increased clearance rate associated with decrease in drug half-life

Decreased clearance rate associated with increase in drug half-life

37
Q

Clearance influenced by:

A

age, co-morbidities, blood flow, and drug concentration

Clearance at age 80 is estimated to be x2 age 30

38
Q

CL= Q x [(Ci -Co)÷Ci]

A

Q= blood flow to the organ/tissue

Ci =entering drug concentration

Co =exiting drug concentration

Volume of plasma from which a substance is completely removed per unit time

Standard Unit: Rate: ml/min

39
Q

A pt is advised to take Aspirin (primarily metabolized in liver). The blood which enters the liver has 200 µg/mL of aspirin and blood that leaves liver contains 134 µg/mL of aspirin. Calculate the hepatic CL of Asprin, when normal hepatic blood flow is 1500 mL/min?

A

495ml/min

40
Q

if it takes 4 hours for a drugs concentration to fall from 50 units to 25 units its half life is =

A

4 hours

41
Q

Dosing Schedules & Plasma Concentration

A

zero-order controlled release

sustained release

conventional release

42
Q

controlled release =

A

release of medication (primarily diffusion) in correlation with drug concentration

43
Q

Sustained Release =

A

release of medication over time

44
Q

Conventional Release =

A

immediate release of drug

45
Q

Factors responsible for individual drug response:

A

Genetics = Pharmacogenomics
Co-morbidities
Age
Drug interactions
Diet
Gender

46
Q

Co-morbidities:

A

Concurrent diseases affecting the patient can modify drug response

47
Q

Diseases of the organs of elimination =

A

liver and kidneys

48
Q

Liver Disease:

A

Drugs that are largely metabolized in the liver are affected by liver diseases such as cirrhosis

49
Q

Kidney Disease:

A

In patients with a compromised renal function, urinary excretion of drugs is diminished = clearance of many drugs reduced

50
Q

Circulatory disorders:

A

Diminished vascular perfusion of one or more parts of the body is encountered in conditions such as cardiac failure

51
Q

Drug-Drug Interactions

A

Majority = insignificant adverse effects

52
Q

Synergistic: beneficial effects

A

cumulative effect drugs for HIV, cancer

53
Q

Synergistic: adverse effects

A

barbiturates (anti-anxiety, sedative effect) + alcohol

54
Q

Antagonistic:

A

reducing beneficial effects

phenobarbital (anti-seizure) + warfarin (anti-coagulant)

55
Q

Serious adverse effects:

A

if one drug delays metabolism of another = drug accumulation = toxic

56
Q

16.5% of population is 65+ = consume ___ of prescribed drugs in US

A

34%

57
Q

64-69 yo = average __ medications

A

15

58
Q

80-84 yo = average __ medications

A

18

59
Q

Older Adults:

A

More sensitive to drugs and exhibit variability in response

Altered pharmacokinetics

Multiple and severe illness

Poor drug compliance

Antihypertensive drugs = orthostatic hypotension
> Beta blockers, diuretics, angiotensin converting enzyme inhibitors (ACE inhibitors)

60
Q

A study of over 3,000 older adults examined drug-drug and drug-disease interactions

A

drug interactions are common among community-dwelling older adults and are related to the number of medications and hospitalizations

Main outcomes: potential drug-drug and drug-disease interactions according to established criteria applied to self-reported prescription and non-prescription drug use

Each additional prescribed drug raised the likelihood of having >1 type of drug interaction by 35-40%

61
Q

Children:

A

Pharmacokinetic & pharmacodynamics data rarely available = relatively little clinical research

Liver & kidney immaturity = deficient in specific drug metabolizing enzymes

Paradoxical effect = opposite of expected effect
> Hyperactivity after administration of sedation drugs

Prolonged administration of corticosteroids = potential effects on growth, bone mass, & adrenal

Drug metabolism and pharmacokinetics change rapidly in first few months of life

62
Q

Diet:

A

Foods, and the nutrients they contain, can interact with medications we take

This can cause unwanted effects

Most are not serious

63
Q

Avoid ___ while taking antidepressants

A

red wine, beer on tap, aged cheese and cured meats

> Foods that contain tyramine can slow the metabolism of antidepressants and lead to severely elevated blood pressure = wine, cheese, cured meat

64
Q

Avoid drinking ___ juice while taking most prescription drugs

A

grapefruit

> The molecule bergamottin, which is found in grapefruit, can inactivate drug-metabolizing enzymes in the liver, which allows drug levels to build up in the bloodstream

65
Q

Gender:

A

Males and females may differ in specific drug pharmacokinetics and pharmacodynamics

Gender differences in drug response may affect drug safety and effectiveness

Special attention should be paid to drugs known to behave differently in pregnancy

Pregnancy-induced changes in drug pharmacokinetics

66
Q

You are conducting a physical therapy evaluation for a patient that has experienced an electrical burn. The burn wound appears charred and you see that the epidermis, dermis, subcutaneous tissues, and muscles have been destroyed. How should this patient’s burn wound be classified?

A

Deep partial-thickness burn – 3rd degree

Full thickness-Subdermal burn – 4th degree

Superficial partial-thickness burn – 2nd degree

Epidermal burn – 1st degree

A: Full thickness - Subdermal burn – 4th degree

A subdermal burn is a burn that appears charred and the epidermis, dermis, subcutaneous tissues and muscles have been destroyed. This type of burn can heal with skin grafting and scarring, but it will require extensive surgery and amputation is sometimes required.

Pharmacology and Nutrition (5 decks)

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