Intro to Pharm Flashcards

1
Q

Agonist

A

binds to same site as ligand and makes same signal

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2
Q

Allosteric Agonist

A

binds to diff site than ligand
no signal
greater response than agonist

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3
Q

Partial Agonist

A

binds to same site
same signal
weaker response

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4
Q

Antagonist

A

same site
no signal
weaker response- inhibits agonist

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5
Q

Competitive Antagonist

A

reversibly bind
same site
receptor can reach max effect with enough agonist concentration

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6
Q

Non-competitive Antagonist

A

irreversibly bind
diff site
receptor cannot reach max effect

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7
Q

Therapeutic Index

TI

A

TD/ED

higher numbers = safer drug

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8
Q

Potency

A

concentration to produce 50% of max effect (EC50)

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9
Q

Efficacy

A

Emax

peak of dose-response relationship

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10
Q

Pharmacologic Antagonism

A

one receptor

responds to one drug while is inhibited by another

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11
Q

Chemical Antagonism

A

no receptor

2 drugs bind to each other and antagonize each other

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12
Q

Physiologic Antagonism

A

D1 affects R1, D2 affects R2

receptors oppose each other

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13
Q

Absorption

A

movement of drug from administration site to blood

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14
Q

Distribution

A

drug mvmt through blood throughout the body

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15
Q

Biotransformation

A

metabolism

drug converted to form where it is more easily eliminated

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16
Q

Elimination

A

excretion of drug from body

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17
Q

Oral Route

A

convenient but slow

subject to first pass effect

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18
Q

First Pass Effect

A

most of drug metabolized in liver before it reaches blood stream

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19
Q

Sublingual and Buccal

A

direct absorption into bloodstream

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20
Q

Intramuscular

A

fast absorption

can be given higher dose

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21
Q

Subcutaneous

A

slower absorption

can be given higher doses

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22
Q

Intravenous

A

NO ABSORPTION

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23
Q

Inhalation

A

Fastest absorption

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24
Q

Topical

A

for local effect

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25
Q

Transdermal

A

for systemic effect

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26
Q

Passive Diffusion

A

driven by concentration gradient- no E

no carrier- not saturable

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27
Q

Facilitated Diffusion

A

driven by concentration gradient- no E

carrier- saturable

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28
Q

Active Transport

A

against gradient- E needed

carrier- saturable

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29
Q

Charged or uncharged pass best through membranes?

A

uncharged

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30
Q
  • pKa
A

acidic

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31
Q

+ pKa

A

basic

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32
Q

pKa

A

pH where 50% is ionized and 50% is nonionized

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33
Q

Lipid Soluble

A

nonionized

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34
Q

Water Soluble

A

ionized

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35
Q

Basic pH will do what to weak acids?

A

get rid of it

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36
Q

Basic pH will do what to weak bases?

A

keep it

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37
Q

Acidic pH will do what to weak bases?

A

get rid of it

38
Q

Acidic pH will do what to weak acids?

A

keep it

39
Q

pH of the Stomach

A

1

40
Q

pH of the SI

A

6

41
Q

pH of Blood

A

7.4

42
Q

pH of Urine

A

5-8

43
Q

pKa > pH

A

mainly HA and BH+

44
Q

pKa < pH

A

mainly A- and B

45
Q

pKa = pH

A
HA = A-
BH+ = B
46
Q

Acidic Drugs

A

HA

47
Q

Basic Drugs

A

BH+

48
Q

Treatment for Hepatic Encephalopathy

A

Lactulose

fixes hyperammonemia

49
Q

Lactulose

A
converts ammonia (NH3) to ammonium (NH4+)
turns GI basic
50
Q

Weak acid overdose treated with….

A

bicarbonate

urine pH = 8

51
Q

Weak base overdose treated with….

A
Ammonium chloride (NH4Cl)
urine pH = 5
52
Q

Physical factors affecting absorption

A

blood flow to absorption site
surface area
contact time

53
Q

Bioavailability

A

fraction of dose that reaches bloodstream

= Route/ Injected X 100

54
Q

Factors affecting bioavailability

A

First pass hepatic metabolism (decreases)
solubility of drug (hyrophilic decreases)
chemical instability

55
Q

Lag Time

A

time from administration to entrance into bloodstream

0 in IV

56
Q

Onset of Activity

A

how long it takes for the drug to start working

57
Q

Duration of Action

A

How long the drug works

58
Q

Volume of Distribution

Vd

A

hypothetical volume of fluid in which a drug is disseminated

= amount of drug in body/ concentration in blood

59
Q

High Vd

A

high volume of distribution

does not stay in blood

60
Q

Low Vd

A

Low volume of distribution

drug stays in blood

61
Q

Increasing Vd has what affect on half life?

A

increases it

62
Q

Placenta and Drug Transfer

A

drugs cross by simple diffusion
lipid sol/ nonionized enter easily
NOT a barrier to drugs

63
Q

Drug Metabolism

A

converting drug to an inactive form

64
Q

Metabolism- Prodrugs

A

convert drugs to an active from

65
Q

Benzodiazepine Metabolism

A

administered in an active for and its metabolites are active as well

66
Q

Phase 1 Metabolism

A

uses cytochrome P450
in smooth ER
oxidation, reduction, hydrolysis

67
Q

Phase 2 Metabolism

A

conjugation reactions
in cytoplasm
needs transferase enzymes
young kids can’t do- drug accumulates

68
Q

Conjugation Reaction

A

uses a transferase enzyme to attach a molecule from the body to the drug
makes the drug bigger and more likely to be eliminated (except in kids)

69
Q

Liver

A

most important organ for drug metabolism

70
Q

Cytochrome P450s that metabolize most drugs

A

CYP2C
CYP2D
CYP3A- 50% of all drugs

71
Q

CYP Inducers

A

increase expression of p450s
speeds up metabolic process
reduce plasma lvls and effectiveness of drugs

72
Q

Drugs that are CYP Inducers

A

benzopyrenes (cig smoke), chronic ethanol, carbamazepine, rifampin, phenytoin

73
Q

CYP Inhibitors

A

decrease expression of P450s
slows metabolic process
increases plasma lvl and toxicity risk
bad when mixed with drugs w/ low TI

74
Q

Drugs that are CYP Inhibitors

A

cimetidine, erythromycin, grapefruit juice

75
Q

Glucuronidation

A

most common Phase 2

uses glucuronosyl transferase

76
Q

Sulfation

A

Phase 2

uses sulfotransferase

77
Q

Acetylation

A

Phase 2

uses acetyltransferase

78
Q

Glomerular Filtration

A

only free, unbound drug filtered (too big)

lipid solubility and pH do not affect

79
Q

Proximal Tubular Secretion

A

requires an OAT and OBT for drug secretion

undeveloped in young kids

80
Q

Distal Tubular Reabsorption

A

drugs diffuse out into systemic circulation if they are uncharged
pH changes will increase ionized form/ decrease reabsorption/ increase elimination

81
Q

First Order Kinetics

A

constant fraction is eliminated per unit time
half life constant
nonsaturating kinetics

82
Q

Zero Order Kinetics

A

constant amount of drug is eliminated per unit time
half life not constant
saturating kinetics

83
Q

Drugs that have zero order kinetics

A

aspirin
ethanol
phenytoin

84
Q

Half Life Formula

A

0.693 x Vd / CL

85
Q

Maintenance Dose

A

maintain plasma concentration of long period of time

chronic

86
Q

Loading Dose

A

quickly increase blood plasma concentration

acute

87
Q

Maintenance Dose Formula

A

= Css x CL / F

conc at steady state x clearance / bioavailabilty

88
Q

Loading Dose Formula

A

= Css x Vd / F

89
Q

When do you give a loading dose?

A

when a long time period is needed to reach steady state via continuous IV

90
Q

Steady State

A

maintenance dose needed to reach and stay at

91
Q

Clinical Steady State

A

4-5 half lives

92
Q

Dosage Adjustment for Renal Failure

A

Correct Dose = ave dose x creatinine clearance / 100 mL/min