Week 1- Study Guide Flashcards

(52 cards)

1
Q

Stages of pharmacokinetics

A

Absorption, distribution, metabolism, excretion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What is absorption?

A

How drug moves from site of administration to sign of action

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Things that impact route of adminstration

A

compliance, bioavailability, onset of action and duration

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What is bioavailability?

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What is distribution?

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What does distribution depend on?

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Ion Trapping

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

what are plasma proteins impacts by?

A

poor nutrition, liver disease, kidney disease

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Transport systems (distribution)

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What is metabolism?

A

Process of how the body breaks down the drug

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What are metabolites?

A

products of metabolism

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Phase 1 metabolism

A

non-synthetic reactions: oxidation, reduction, hydrolysis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Phase 2 Metabolism

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

CYP450

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Prodrugs

A

inactive compound that rely on metabolism to become activated

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

what is excretion?

A

How drugs are removed from the body

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Organs involved in elimination

A

kidneys, lungs, biliary, intestines

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

renal excretion

A

metabolites need to be water soluable

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

factors that influence GFR

A
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
first order kinetics
half life elimination, medication will reach peak and trough at 4-5 half-life
26
zero order kinetics
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
what is the CYP 450 system
collection of enzymes essential for metabolism of drugs, toxins and endogenous compounds
28
where is the CYP enzymes found
in the liver, but also present in intestines, lungs and brain
29
where does the CYP work?
mainly in phase 1 metabolism assisting in oxidation, reduction and/or hydrolysis
30
how does genetic variability play a role in CYP450 enzymes?
variations like polymorphisms scan impact how people metabolize drugs
31
examples of genetic variability
32
drug interactions with CYP450 systems- inducers
rifampin and st. john's wort can INDUCE CYP3A4, leading to decreased levels of drugs metabolized by this enzyme
33
drug interactions with CYP450 systems- inhibitors
Drugs like ketoconazole and grapefruit juice can inhibit CYP3A4, leading to increased levels of drugs metabolized by this enzyme
34
importance of CYP3A4
*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
Factors that affect metabolism of drugs
single nucleotide polymorphisms, enzymes, half-life, pro-drugs
36
how do single nucleotide polymorphisms impact metabolism of drugs
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
how do enzymes impact metabolism of drugs
two drugs may be metabolized by the same enzyme and may extend half life of competing drug
38
how are prodrugs related to metabolism of drugs
inactive compounds that rely on metabolism to become active
39
herbal medication safety
encourage patients to disclose all supplements used, supplements rated as "food" not same standards as medication
40
things that impact herbal medication potency
growth, harvesting, processing, storing and shipping
41
what is saw palmetto?
helps with BPH, decreases symptoms of enlarged prostate
42
what are ADR of Saw Palmetto
dizziness, headache, nausea, vomiting, constipation, diarrhea and slow clotting response
43
what is melatonin
hormone produced pineal gland, assists in sleep and prevention of jetlag
44
how does melatonin work
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
ADRs of melatonin
altered sleep patterns, confusion, headache, tachycardia, and hypothermia. Potentiates benzodiazepines and succinylcholine, thereby blocking the action making it dangerous
46
how often should melatonin be used
Should not be used more than 3 times a week
47
what is st. john wort?
used for depression, mood regulation
48
what are some ADRs of St John's Wort
trouble sleeping, vivid dreams, restlessness, anxiety, irritability, stomach upset, fatigue, dry mouth, dizziness, headache, skin rash, diarrhea, and tingling.
49
Biggest problem with St Johns Wort
Numerous Drug Interactions, which include: SSRIs, cyclosporin, birth control pills, antidepressants, some cancer and HIV medications, warfarin, oxycodone, and digoxin
50
What is glucosamine?
It is an amino acid found in mucopolysaccharides and chitin
51
what is glucosamine used for?
Treatment of OA, stimulate cartilage production and enhance rebuilding of damaged cartilage
52
what are some ADRs of glucosamine
minor- constipation, diarrhea, drowsiness, headache, heartburn, nausea, and rash