Week 1- Study Guide Flashcards

1
Q

Stages of pharmacokinetics

A

Absorption, distribution, metabolism, excretion

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2
Q

What is absorption?

A

How drug moves from site of administration to sign of action

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3
Q

Things that impact route of adminstration

A

compliance, bioavailability, onset of action and duration

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4
Q

What is bioavailability?

A

% of administered drug able to produced a pharmacological effect [IV drugs have higher bioavailability]

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5
Q

What is distribution?

A

Describes the journey of the drug throughout the bloodstream to various tissues of the body and passive diffusion

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6
Q

What does distribution depend on?

A

Different transport systems including size, charge, and structure (pH too!)

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7
Q

Ion Trapping

A

build up of higher concentration of unionized and ionized drugs across the membrane based on pH

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8
Q

What is protein binding?

A

drugs bind to plasma proteins to help normalized concentrations throughout the body, to stay in the body longer

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9
Q

what are plasma proteins impacts by?

A

poor nutrition, liver disease, kidney disease

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10
Q

Transport systems (distribution)

A

P glycoproteins and MRP1 (multidrug resistance protein)– both efflux transporters

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11
Q

What is metabolism?

A

Process of how the body breaks down the drug

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12
Q

What are metabolites?

A

products of metabolism

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13
Q

Phase 1 metabolism

A

non-synthetic reactions: oxidation, reduction, hydrolysis

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14
Q

Phase 2 Metabolism

A

Synthetic or conjugation reactions-metabolites are link/conjugated to polar molecules →making metabolites more water soluble

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15
Q

CYP450

A

catalyzes metabolism of highly lipid soluable drugs and chemicals, transfer electrons from oxidation of drugsrod

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16
Q

Prodrugs

A

inactive compound that rely on metabolism to become activated

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17
Q

what is excretion?

A

How drugs are removed from the body

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18
Q

Organs involved in elimination

A

kidneys, lungs, biliary, intestines

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19
Q

renal excretion

A

metabolites need to be water soluable

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20
Q

factors that influence GFR

A
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21
Q

biliary excretion

A

1 L of bile a day, conjugated (binding with proteins) to enhance biliary excretion

22
Q

enterohepatic cycling

A

Drug excreted in bile→ absorbed from intestines →excreted in the bile again==>extends time that a drug remains in the body

23
Q

first pass effect (metabolism)

A

metabolism at specific locationof the body leads to reduction in concentration of active drug before it reaches the site of action or systemic circulation

24
Q

example of first pass effect

A

metabolism of the liver after oral administration

25
Q

first order kinetics

A

half life elimination, medication will reach peak and trough at 4-5 half-life

26
Q

zero order kinetics

A

rate of drug elimination is independent of drug concentration… same amount is eliminated per hour regardless of how much drug is in the body (think of alcohol)

27
Q

what is the CYP 450 system

A

collection of enzymes essential for metabolism of drugs, toxins and endogenous compounds

28
Q

where is the CYP enzymes found

A

in the liver, but also present in intestines, lungs and brain

29
Q

where does the CYP work?

A

mainly in phase 1 metabolism assisting in oxidation, reduction and/or hydrolysis

30
Q

how does genetic variability play a role in CYP450 enzymes?

A

variations like polymorphisms scan impact how people metabolize drugs

31
Q

examples of genetic variability

A
32
Q

drug interactions with CYP450 systems- inducers

A

rifampin and st. john’s wort can INDUCE CYP3A4, leading to decreased levels of drugs metabolized by this enzyme

33
Q

drug interactions with CYP450 systems- inhibitors

A

Drugs like ketoconazole and grapefruit juice can inhibit CYP3A4, leading to increased levels of drugs metabolized by this enzyme

34
Q

importance of CYP3A4

A

*responsible for up to 50% of drug metabolism
*Works on several classes of drugs: -azole antifungals, calcium channel blockers, antihistamines, anticonvulsants, antimicrobials, and corticosteroids.
*Amiodarone has half life, close to 60 days, and inhibits the CYP450 enzyme system.

35
Q

Factors that affect metabolism of drugs

A

single nucleotide polymorphisms, enzymes, half-life, pro-drugs

36
Q

how do single nucleotide polymorphisms impact metabolism of drugs

A

minor mutations that can exist in an individual enzyme or protein, can help explain why certain groups of people are sensitive to certain drugs

37
Q

how do enzymes impact metabolism of drugs

A

two drugs may be metabolized by the same enzyme and may extend half life of competing drug

38
Q

how are prodrugs related to metabolism of drugs

A

inactive compounds that rely on metabolism to become active

39
Q

herbal medication safety

A

encourage patients to disclose all supplements used, supplements rated as “food” not same standards as medication

40
Q

things that impact herbal medication potency

A

growth, harvesting, processing, storing and shipping

41
Q

what is saw palmetto?

A

helps with BPH, decreases symptoms of enlarged prostate

42
Q

what are ADR of Saw Palmetto

A

dizziness, headache, nausea, vomiting, constipation, diarrhea and slow clotting response

43
Q

what is melatonin

A

hormone produced pineal gland, assists in sleep and prevention of jetlag

44
Q

how does melatonin work

A

Produced when serotonin is broken down in the pineal gland with the help of two enzymes; arylalkylamine N-acetyl transferase (AA- NAT) and hydroxyindole-O-methyl transferase

45
Q

ADRs of melatonin

A

altered sleep patterns, confusion, headache, tachycardia, and hypothermia.
Potentiates benzodiazepines and succinylcholine, thereby blocking the action making it dangerous

46
Q

how often should melatonin be used

A

Should not be used more than 3 times a week

47
Q

what is st. john wort?

A

used for depression, mood regulation

48
Q

what are some ADRs of St John’s Wort

A

trouble sleeping, vivid dreams, restlessness, anxiety, irritability, stomach upset, fatigue, dry mouth, dizziness, headache, skin rash, diarrhea, and tingling.

49
Q

Biggest problem with St Johns Wort

A

Numerous Drug Interactions, which include:
SSRIs, cyclosporin, birth control pills, antidepressants, some cancer and HIV medications, warfarin, oxycodone, and digoxin

50
Q

What is glucosamine?

A

It is an amino acid found in mucopolysaccharides and chitin

51
Q

what is glucosamine used for?

A

Treatment of OA, stimulate cartilage production and enhance rebuilding of damaged cartilage

52
Q

what are some ADRs of glucosamine

A

minor- constipation, diarrhea, drowsiness, headache, heartburn, nausea, and rash