week 2: Ch. 3-4 [Pharmacokinetics/dynamics] Flashcards

1
Q

Pharmaco means:

A

medicine

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2
Q

Kinetics means:

A

movement

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3
Q

Pharmacokinetics means:

A

what the body does to drugs after administration

[study of drug movement throughout body]

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4
Q

What are 2 barriers to drugs attempting to reach target cells?

A

Many membranes must be crossed

Physiological processes

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5
Q

4 processes of Pharmacokinetics

A

absorption
distribution
metabolism
excretion

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6
Q

Drugs use _________ and ______ __________ to cross plasma membranes to reach target cells

A

diffusion, active transport

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7
Q

2 types of diffusion:

A

simple diffusion
passive transport

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8
Q

diffusion is the movement of a chemical from an area of :

A

higher to lower concentration

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9
Q

diffusion assumes a chemical can cross :

A

plasma membranes freely

[not the case for all drugs]

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10
Q

What factors affect movement across plasma membranes?

A

size of drug molecule
ionization of drug molecule
lipid solubility

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11
Q

Facilitated diffusion utilizes ____1____ ________ to cross membranes.

does it require energy? 2:

A

carrier proteins

2- no

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12
Q

Active transport pumps require:

A

cell energy

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13
Q

_________ is the first step toward reaching the target cell for a drug

A

Absorption

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14
Q

Absorption is the movement from site of administration to:

A

bloodstream

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15
Q

The primary factor for determining the onset of drug action:

A

absorption

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16
Q

Enteral route of administration

Drugs delivered to__________________
~orally or through ______________________________________________________________

~common: ______________________

[slow onset bc must absorb as goes through system to be available]
~Oral liquid absorbed much faster

A

Drugs delivered to GI tract
~orally or through NG tube or gastromy tubes

~common: tablets/capsules [slow onset bc must absorb as goes through system to be available]
~Oral liquid absorbed much faster

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17
Q

Explain enteric-coated tablet/capsule

Hard, waxy coating to resist ________________________________contents
~designed to dissolve in _____________ environment of small intestine

A

Hard, waxy coating to resist strongly acidic stomach contents
~designed to dissolve in alkaline environment of small intestine

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18
Q

Explain extended-release tablets/capsule

Designed to dissolve ____________ over longer time = ____________duration of action

A

Designed to dissolve slowly over longer time = longer duration of action

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19
Q

The following should never be chewed/crushed/opened:

A

extended-release formulations
enteric coated drugs
oral cavity drugs

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20
Q

Tablets/capsules go through a first-pass effect: drugs absorbed from the stomach and small intestine travel to liver, where they may be:

A

inactivated before reaching target organs

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20
Q

Recent devlopments of med administration (within enteral route) include

A

orally disintegrating tablets ODT
oral soluble films

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21
Q

Describe sublingual/buccal routine of medication (enteral)

medications kept in mouth

dissolves in_____________________

not subjected to ______________________________________________________________

sublingual- _____________
buccal- ___________________

[in case of multiple meds, oral meds first, then sublingual]

A

medications kept in mouth

dissolves in under 30 seconds

not subjected to stomach acid/ first-pass effect

sublingual- under tongue
buccal- in cheek

[in case of multiple meds, oral meds first, then sublingual]

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22
Q

Explain medications given through nasogastric and gastromy tubes

drugs usually_____________, to prevent _____________________

do not use ________________________ meds

A

drugs usually liquid, to prevent clogging tubes

do not use sustained release meds

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23
Q

Explain absorption of topical route meds

usually_________ absorption

drugs must penetrate ___________________________

ex) ________________ patch- like sticker- rate of delivery varies; can depend on amount of ______

A

usually slower absorption

drugs must penetrate thick skin layer

ex) transdermal patch- like sticker- rate of delivery varies; can depend on amount of hair

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24
Q

3 types of topical routines include

opthalmic route-
otic roue-
intranasal route-
vaginal route-
rectal route-

A

opthalmic route- treating local conditions in eye

otic route- in ear

intranasal route- within nose

vaginal route- local conditions or BC

rectal route- local or systemic; ex) suppository or enema; avoids first-pass effect

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25
Q

Describe parenteral route of drug administration

______________ & ______________ administration
~any medication penetrating through skin

~__________________ adminstration- drug into large muscle (thigh/arm/bottom); rapid onset of action

~_______________ administration: directly to bloodstream; fastest onset but most dangerous [miscalculation or reaction can lead to bad outcome]

A

intradermal & subcutaneous administration
~any medication penetrating through skin

~intra muscular adminstration- drug into large muscle (thigh/arm/bottom); rapid onset of action

~intravenous administration: directly to bloodstream; fastest onset but most dangerous [miscalculation or reaction can lead to bad outcome]

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26
Q

major difference between intradermal & subcutaneous administration

A

depth of injection

[intradermal more superficial]

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27
Q

Examples of subcutaneous administration drugs:

A

insulin
heparin
vitamins
vaccines

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28
Q

for most drugs, higher doses produce:

A

faster and greater drug response

& greater concentration gradient for diffusion

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29
Q

Most absorption of drug occurs in:

A

GI tract (small intestine)

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30
Q

why does digestive motility vary among patients?

A

different amount of acid in stomach, or quicker digestion

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31
Q

Presence of food in stomach _______ absorption

A

slows

[with very few exceptions]

Usually best to take med on empty stomach or between meals

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32
Q

Drugs are absorbed faster from areas of the body where blood flow:

A

is high

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33
Q

How can blood flow be purposefully manipulated to slow absorption?

A

vasoconstrictors [constricts blood flow]
ice packs

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34
Q

Depending on the pH of surrounding fluid, most drugs are either :

A

charged or uncharged state

35
Q

__________ of a drug affects its ability to cross plasma membranes and to be excreted by the body

A

Ionization

36
Q

acids are absorbed in acids because they are:

A

nonionized

37
Q

bases are absorbed in bases because they are:

A

nonionized

38
Q

Drug interactions can be-

A

drug-drug
or drug-food

39
Q

drug interactions can potentially affect-

A

absorption of drugs

40
Q

high fat meals can slow:

A

stomach motility

41
Q

Drugs are absorbed faster when applied to:

A

regions with larger surfacer area, like small intestine or lung

42
Q

Distribution describes movement of medication throughout the body after

A

absorption

43
Q

What 4 factors affect drug distribution?

___________ to tissues
drug ___________
tissue __________
drug-protein ___________

A

blood flow to tissues
drug solubility
tissue storage
drug-protein binding

44
Q

drug-protein complexes cannot cross :

A

capillary membranes

45
Q

only ________ drugs reach target cells

A

unbound

46
Q

What does the blood brain barrier do?

special anatomic _________

protects brain from ____________________________

____________________ drugs are able to cross

[not fully developed in neonates]

Inflammation can increase ____________________

A

special anatomic barriers

protects brain from pathogens and toxins

lipid-soluble drugs are able to cross

[not fully developed in neonates]

Inflammation can increase permeability

47
Q

Fetal-placenta barrier prevents harmful substances passing from:

A

mother’s bloodstream to fetus

[not as efficient as blood brain barrier]

Inefficient with- alcohol, cocaine, caffeine, prescriptions can cross

48
Q

metabolism __________ the structure and function of drugs, nutrients, vitamins, and minerals

A

alters

49
Q

where is the primary site of metabolism?

A

liver

50
Q

What are prodrugs?

medications that require ________________ to produce their __________________

~no pharmacological activity until after _______________

A

medications that require metabolism to produce their therapeutic actions

~no pharmacological activity until after metabolized

51
Q

What is a hepatic microsomal enzyme?

enzyme____________ CYP450

an enzyme that _________________ many drugs

A

enzyme complex CYP450

an enzyme that metabolizes many drugs

52
Q

3 important consequences of CYP systems

drugs as substrates
~may lead to _____________________________

drugs as enzyme inhibitors
~can contribute to _________________________in body

drugs as enzyme inducers
~accelerate metabolism; drug level may _________________

A

drugs as substrates
~may lead to drug-drug interactions

drugs as enzyme inhibitors
~can contribute to drug toxicity in body

drugs as enzyme inducers
~accelerate metabolism; drug level may decrease rapidly

52
Q

Metabolism can vary due to genetic variations of _____ enzymes

A

CYP

53
Q

Enzyme activity is often _______ in older adults

A

reduced

54
Q

Liver impairment can lead to _________ metabolism

A

decreased

55
Q

Excretion is the process of:

A

removing drugs from the body

56
Q

Rate of excretion is determined by the

A

drug blood level

57
Q

Renal excretion occurs in

A

the kidney

58
Q

Drug excretion depends on urine:

A

pH

[urine pH can be manipulated to help with drug excretion]

59
Q

Glandular secretion of drugs can happen in

A

saliva, sweat, breast milk

60
Q

Pulmonary excretion (example)

A

gases, volatile liquids

61
Q

Biliary excretion- some drugs are:

A

secreted in the bile

62
Q

drugs excreted into the bile will eventually leave in the

A

feces

63
Q

Enterohepatic recirculation:

drug reabsorbed and goes back into _______________________________may recirculate drugs, metabolites, and prolong action

A

drug reabsorbed and goes back into hepatic system may recirculate drugs, metabolites, and prolong action

64
Q

The therapeutic response of most drugs depends on their concentration in:

A

the plasma

65
Q

What is the minimum effective concentration?

A

amount of drug required to produce a therapeutic effect

66
Q

________ concentration is level of drug that results in serious adverse effects

A

Toxic

67
Q

What is the therapeutic range of a drug?

A

range where the drug produces desired actions

after peaking, drug plasma levels fall due to excretion

68
Q

The drug half-life provides an estimation of:

A

duration of action

69
Q

Plasma half-life is the time required for plasma concentration of drug to:

A

decrease by half

70
Q

If a drug has a short half-life, it is given

A

given more frequently

71
Q

A loading dose is a higher amount of drug given to:

A

“prime” the bloodstream

[increase level at the beginning]

72
Q

a maintenance drug dose will keep concentration within:

A

therapeutic range

73
Q

Pharmacodynamics- how a drug

A

changes the body

[involves drug mechanism of action]

[involves effect of drug concentration on body responses]

74
Q

the median effective dose is the desired drug response in:

A

50% of subjects

75
Q

The median lethal dose is

A

lethal to 50% of animals during testing

76
Q

The median toxicity dose is the dose that produces

A

toxicity in 50% of subjects

[animal data/ clinical trial data]

77
Q

The margin of safety MOS is the amount of drug lethal to

____of animals divided by amount of drug that produces _________________ effect in ______ of animals

A

1% of animals divided by amount of drug that produces therapeutic effect in 99% of animals

78
Q

Three phases of dose-response relationship

A

Phase 1- lowest dose

phase 2- most desirable range

phase 3- plateau reached

79
Q

Potency is the amount of drug needed to produce

A

a specified effect

80
Q

Receptor theory- most drugs produce their actions by activating or inhibiting:

A

specific cellular receptors

81
Q

Medications bind to receptors like a

A

lock and key

82
Q

Agonists ________ the action of endogenous substances

A

mimics

83
Q

Antagonists prevent action of:

A

endogenous substances

84
Q

Pharmacogenetics is the branch of pharmacology that studies:

A

role of genetic variation in drug responses

ex) human genome project