Clinical Therapeutics > Week 1 > Flashcards

Week 1 Flashcards

Intro (71 cards)

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1
Q

the study of the movement of drugs in the body

A

pharmacokinetics

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2
Q

branch of science that studies the interactions b/w drugs and biological systems

A

pharmacology

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3
Q

subdisciplines

A

pharmacokinetics, pharmacodynamics, toxicology,
clinical pharmacology

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4
Q

any chemical substance that produces biological effect when consumed

A

drug

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5
Q

substance encased in digestible hard or soft shell

A

capsules

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6
Q

compressed substance that can be swallowed, chewed, or dissolved orally

A

tablets

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7
Q

the ideal drug is

A

safe, effective, predictable, selective, reversible, oral, not interactive with other drugs, cheap, stable

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8
Q

how do health disparities alter drug treatment

A

access to pharmacy, drug cost/ insurance, implicit bias of medical providers, patient trust, ability to complete follow up appointments

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9
Q

how to address health disparities

A

screen for social determinates of health, ask and listen, advocate for systemic changes, (build trust, educate patients)

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10
Q

ADME

A

Absorption, drug ingestion, metabolism, excretion

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11
Q

types of transport

A

active and passive

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12
Q

active transport

A

lower concentration to higher concentration (vice versa) using atp (against concentration gradient)

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13
Q

passive transport

A

something just goes across the membrane

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14
Q

facilitate diffusion

A

going along the concentration gradient doesn’t require atp (type of passive transport)

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15
Q

ion trapping

A

molecule trapped on one side of a membrane due to the environments pH

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16
Q

drug absorption

A

process by which a drug moves from its site of administration into systemic circulation

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16
Q

advantages of IV?

A

fast, can administer a larger dose, avoid irritation

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16
Q

what the bioavailability of IV administration

A

1/100%

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16
Q

bioavaiability

A

the amount of administered drug that reaches peripheral circulation

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17
Q

first pass metabolism

A

drug metabolism hits the liver after absorption before systemic circulation

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17
Q

disadvantages of IV?

A

can easily give too much (toxicity), fast (dangerous; always LOW and SLOW), requires clinical adminstation

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18
Q

what other administration goes through first pass metabolism

A

rectal admin.

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19
Q

drug distribution

A

transfer of drug from one body compartment to another

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20
Q

what is the flow of drug distribution

A

highly vascularized organs (heart, brain, liver, etc)> muscle, skin, fat> adipose tissue

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21
what does volume of distribution mean
the EXTENT to which a drug is distributed in body tissue rather than the plasma (Being able to locate the drug in the body after administration)
22
what volume implies that a drug is being concentrated in tissues
>42L for a 70kg male
23
if the Vd is below 40L what does that mean?
drug is staying the blood stream
24
what do you call a drug that is restricted from crossing membranes into tissues due to being attached to plasma proteins
highly plasma protein bound
25
what can happen if two drugs are competing for binding sites?
protein binding becomes saturated (liver cannot produce enough protein for drugs to bind)
26
will highly protein bound drugs have a large Vd
no
27
what compounds do protein bound drugs have
Low Vd (stay in the blood) Reduced metabolism (they dont get into the liver) low clearance( not filtered in the kidney)
28
what is drug redistribution
the movement of a drug from an area of high blood flow to an area of low blood flow (can alter or end drug action)
29
how does drug redistribution occur with highly lipophilic drugs
lipophilic drugs distributed to organs with high blood flow> drug moves to low blood flow areas (adipose tissue)> plasma conc. drop
30
drug metabolism
chemical transformation of a drug into compounds that are easier to eliminate from the body
31
what two ways do drug metabolism occur
biotransformation(metabolism=breaking things down)>liver excretion> kidney (biliary)
32
what is the process of biotransformation
foreign molecule (xenobiotic) which are mostly lipophilic drug>(converted)> hydrophilic drug> excreted via (kidney>urine, feces, sweat etc)
33
where does biotransformation occur mainly
LIVER, has the highest conc. of biotransformation enzymes
34
what can alter metabolism in liver
genetics, tobacco and drug use, environmental toxins, drug interactions, diet Foreign: environmental pollutants, food additives, cosmetics, processed foods and agrochemicals
35
what is Phase 1 of metabolism
uses oxidation, reduction and hydrolysis reactions to add function groups to a molecule (involves Cytochrome p450 (CYP)) non-conjugative mostly inactivates...sometimes activates
36
what is phase 2 metabolism
conjugation reactions >modified molecule (from phase 1)> attaches a polar molecule (endogenous subs) >makes the molecule more water-soluble> facilitates excretion
37
how could phase 1 metabolism cause liver toxicity?
drug can transform >highly reactive metabolites aka toxicophores>damage liver cells
38
what is a prodrug
a drug that is pharmacologically inactive>require metabolism>active drug molecule usually use oxidation and CYP enzymes act as catalyst.
39
Where is Vd high
Where blood flow is high such as heart brain liver kidney
40
what CYP is high in metabolism prodrugs
CYP3A4-3A5
41
how can metabolizing enzymes become saturated?
inactive drugs increase above threshold >enzyme becomes saturated> drugs isn't going to work> increase drug serum levels.
42
what happens if drugs change metabolizing enzyme activity?
drugs can INHIBIT function/expression(making of protein) =REDUCED metabolism drugs can INDUCE expression= INCREASED metabolism
43
grapefruit inhibits what CYP?
CYP3A
44
How does Phase II inactivate a drug
It adds carbon group/sulfur to completely inactivate the drug for excretion via urine.
45
what can alter drug metabolism
1. decreased hepatic mass, blood flow, cirrhosis (liver issues) 2. genetic variation in metabolizing enzymes (CYP219 mutations etc) 3. Drug induced changes in hepatic enzymes ( CYP450 interactions, Competition for metabolism) 4. Dietary Intake (grapefruit, ST John worts) 5. Tobacco , alcohol, drug use 6. Exercise
46
Polypharmacy
administration of many drugs at the same time or the administration of an excessive number of drugs
47
how many drugs can a person take at one time and have definite drug interactions
8
48
Drug excretion
process by which a drug and its metabolites are removed from the body (drug cleared)
49
what is the primary site for drug excretion
renal
50
what are two ways drug is eliminated
metabolism and excretion
51
clearance
is the volume of blood or plasma cleared of drug over time
52
what could cause problems with excretions
Renal problems things that reduce renal function: -Age -Hypertension -Kidney stones -Acute renal injury -severe dehydration
53
whats the gold standard test for renal function
Inulin clearance
54
what is commonly used to check renal function
creatinine
55
why is creatinine a good choice to check glomerulus function
its freely filtered by the glomerulus and is not reabsorbed or metabolized on the kidney
56
If the person has renal impairment how do you administer drugs
Variable dose method (change the dose and keep the interval the same) Variable frequency (keep the dose the same and change the dosing interval) Combination method:BOTH
57
First-order kinetics
same fraction of the drug is removed per unit time
58
half life
the time to reduce plasma concentration by 50%
59
Zero order Kinetics
amount the body eliminates is fixed (only can excrete a certain amount over time)
60
how can Zero order kinetics result in overdose
because only a certain amount can be excreted overtime> if dosage is too high it can trigger overdose because its only getting excreted at a certain pace
61
steady state
the concentration in same as concentration out -keep the plasma levels safer(unsafe drugs)
62
loading dose
giving a big dose (serious situation) to reach therapeutic levels quicker
63
when should your measure serum blood concentrations
after the first two hours because absorption and distribution usually takes this long
64
how does obesity alter drug dosing
if the person is obese: -the drug is lipophilic the patients actual body weight is neededd -drug not lipophilic need ideal body weight
65
Volume overload in body (edema, ascites, and pleural effusions)
weight can be calculated by estimating excess fluid from measured weight before volume of distribution
66
how is pharmacokinetics altered in elderly
reduced 1st pass metabolism increased body fat decreased total body fat
67
how is pharmacokinetics altered in infants
absorption: decreased ; frequent feeding, low levels of gastric flora, low peripheral perfusion Distribution increased-low plasma protein conc. greater BBB (super leaky) and skin permeability, high total body water, low body fat Metabolism: decreased=drug metabolizing enzymes are immature Excretion decreased=immature kidneys lead to slow excretion
Clinical Therapeutics
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