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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
Enzyme Induction:
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
26
Enzyme Induction results in Drug Tolerance =
reduction in drug’s effectiveness
27
Drug Excretion
Primary site: Renal Excretion Nephron = functional unit of kidney Polar compounds/water soluble molecules/ionized compounds = excreted in urine
28
Metabolites filtered in glomerulus =
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
Other areas of drug excretion:
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
Drug Elimination
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
Drug delivery > Elimination =
drug accumulation
32
Elimination > Drug delivery =
no therapeutic effect
33
2 Factors that effect the balance of drug accumulation, therapeutic effect & elimination:
Clearance and Half-life
34
Clearance =
volume of plasma cleared of a drug per unit of time predicts the rate of elimination volume/time
35
Half-Life =
amount of time it takes for the plasma concentration to drop by 50% determined by drug chemical structure
36
Relationship of Clearance (CL) and Half-life
Increased clearance rate associated with decrease in drug half-life Decreased clearance rate associated with increase in drug half-life
37
Clearance influenced by:
age, co-morbidities, blood flow, and drug concentration Clearance at age 80 is estimated to be x2 age 30
38
CL= Q x [(Ci -Co)÷Ci]
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
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?
495ml/min
40
if it takes 4 hours for a drugs concentration to fall from 50 units to 25 units its half life is =
4 hours
41
Dosing Schedules & Plasma Concentration
zero-order controlled release sustained release conventional release
42
controlled release =
release of medication (primarily diffusion) in correlation with drug concentration
43
Sustained Release =
release of medication over time
44
Conventional Release =
immediate release of drug
45
Factors responsible for individual drug response:
Genetics = Pharmacogenomics Co-morbidities Age Drug interactions Diet Gender
46
Co-morbidities:
Concurrent diseases affecting the patient can modify drug response
47
Diseases of the organs of elimination =
liver and kidneys
48
Liver Disease:
Drugs that are largely metabolized in the liver are affected by liver diseases such as cirrhosis
49
Kidney Disease:
In patients with a compromised renal function, urinary excretion of drugs is diminished = clearance of many drugs reduced
50
Circulatory disorders:
Diminished vascular perfusion of one or more parts of the body is encountered in conditions such as cardiac failure
51
Drug-Drug Interactions
Majority = insignificant adverse effects
52
Synergistic: beneficial effects
cumulative effect drugs for HIV, cancer
53
Synergistic: adverse effects
barbiturates (anti-anxiety, sedative effect) + alcohol
54
Antagonistic:
reducing beneficial effects phenobarbital (anti-seizure) + warfarin (anti-coagulant)
55
Serious adverse effects:
if one drug delays metabolism of another = drug accumulation = toxic
56
16.5% of population is 65+ = consume ___ of prescribed drugs in US
34%
57
64-69 yo = average __ medications
15
58
80-84 yo = average __ medications
18
59
Older Adults:
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
A study of over 3,000 older adults examined drug-drug and drug-disease interactions
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
Children:
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
Diet:
Foods, and the nutrients they contain, can interact with medications we take This can cause unwanted effects Most are not serious
63
Avoid ___ while taking antidepressants
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
Avoid drinking ___ juice while taking most prescription drugs
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
Gender:
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
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?
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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