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MM Pharmacology > Pharmacology Synopses 1 > Flashcards

Pharmacology Synopses 1 Flashcards

1
Q

ideal for lipid soluble drugs that would otherwise be metabolized in the gut or liver

A

sublingual route

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2
Q

route reserved for nitrates or certain hormones

A

sublingual route

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3
Q

rate and completeness of absorption

A

factors comprising bioavailability

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4
Q

bioavailability of drug types, most to least

A

solution> suspension >capsule >tablet >coated tablet

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5
Q

route commonly used in children, slow absorption

A

rectal (no villi in rectum)

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6
Q

route for rapid clinical response, precise plasma concentrations, no issues of bioavailability

A

intravenous injection

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7
Q

route to deliver high concentrations of drugs to a particular tissue

A

intraarterial injection

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8
Q

route to bypass blood-brain barrier

A

intrathecal, via lumbar puncture to subarachnoid space

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9
Q

intramuscular absorption rates, high to low

A

arm> thigh> buttocks

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10
Q

subcutaneous injections absorb ____ than intramuscular

A

slower than

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11
Q

heat, massage, vasodilators

A

increase rate of subcutaneous absorption

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12
Q

coadministration of vasoconstrictors, as with local anesthetics

A

slows rate of subcutaneous absorption

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13
Q

route for volatile anesthetics or drugs for pulmonary function, not subject to first-pass liver metabolism

A

inhalation

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14
Q

drug patches enter system via

A

zero order kinetics (amount constant per unit time)

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15
Q

occurs only for molecules less than 150-200 MW

A

passive aqueous diffusion

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16
Q

allows molecules of 20-30,000 MW to pass through via aqueous diffusion

A

endothelial capillary lining (but not in brain)

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17
Q

occurs for drugs that are analogs of endogenous compounds

A

carrier mediated facilitated transport

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18
Q

may reduce the amount of drug reaching target tissue, or metabolically activate an inert pro-drug

A

first pass effect (via liver)

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19
Q

will increase rate of passive absorption by maintaining concentration gradient of free drug

A

drug binding to plasma protein

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20
Q

gastrointenstinal absorption rate, but not extent of absorption

A

reduced by the presence of food in the gut

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21
Q

equation for Ka

A

[H+][A-]/[HA]

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22
Q

equation for pH of acids

A

pKa + log [A-]/[HA]

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23
Q

equation for pH of bases

A

pKa + long [B]/[BH+]

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24
Q

more rapid than elimination, accomplished via circulation, influenced by regional blood flow

A

distribution

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25
Q

peripheral compartments

A

adipose and skeletal, less well perfused, drug equilibrates more slowly

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26
Q

special compartments

A

CNS, CSF, pericardial fluid, bronchial secretions, middle ear fluid (difficult to treat infections)

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27
Q

weak acids and neutral drugs bind particularly to

A

albumin

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28
Q

basic drugs tend to bind

A

alpha-1-acid glycoprotein (orosomucoid)

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29
Q

protein binding ____ the net transfer of drugs across membrane

A

decreases

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30
Q

at equilibrium, the total drug concentration in plasma is usually ____ than in extravascular fluid

A

higher (due to protein-drug in plasma)

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31
Q

for drugs secreted renally, protein binding

A

decreases the rate of elimination

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32
Q

for drugs eliminated hepatically, protein binding

A

may promote drug elimination

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33
Q

apparent blood volume

A

amount of drug injected/blood concentration at time zero

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34
Q

if plasma binding is marker, apparent volume will be

A

small

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35
Q

if there is extracellular binding, storage in fat or other tissues, apparent volume will be

A

large

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36
Q

generally bind plasma proteins and have small Vd

A

acidic drugs

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37
Q

generally bind extravascular sites and have large Vd

A

basic drugs

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38
Q

capable of eliminating drugs with low molecular weight or polar and fully ionized at body pH

A

the kidneys

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39
Q

most important extrahepatic site of drug metabolism

A

GI tract

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40
Q

sites of drug metabolizing action

A

Liver, Gi tract, intestines, skin, placenta, lungs

41
Q

most enzymes involved in drug metabolism are located within

A

the lipophilic membranes of the smooth endoplasmic reticulum

42
Q

the enzymes that carry out metabolism on the SER are called

A

the MFO system (microsomal mixed-function oxidase system)

43
Q

phase I reactions convert a drug to a more polar compound by adding or unmasking

A

polar functional groups: OH, NH2, SH

44
Q

phase II reactions conjugate the compound with wndogenous compounds such as

A

glucuronic acid, sulfuric acid, acetic acid, or amino acids (glycine!)

45
Q

the most common phase II reaction is

A

glucuronide formation

46
Q

terminal oxidizing enzyme in most MFO reactions

A

cytochrome P450

47
Q

receptors for exogenous ligands

A

ion channels, enzymes, ion transporters, carriers and pumps, structural proteins

48
Q

glomeruli permit the passage of most drug molecules, except

A

protein bound drugs

49
Q

can kidney actively transport some protein bound drugs?

A

yes, though associated protein dissassociates

50
Q

renal tubules reabsorb

A

nonionized, lipid-soluble drugs

51
Q

alkalinized urine promotes excretion of

A

drugs that are weak acids

52
Q

acidified urine promotes excretion of

A

weak bases

53
Q

drugs and metabolites passed into the small intestine via bile may undergo

A

enterohepatic cycling

54
Q

receptor types for endogenous ligands

A

Ligand-gated ion channels, G-protein receptors, tyrosine kinase receptors

55
Q

See 7 transmembrane passes, think

A

G-protein coupled receptor

56
Q

Adrenergic and muscarinic Ach receptors are in this family

A

single subunit receptor protein

57
Q

receptors for insulin and growth factors are in this class

A

tyrosine kinase

58
Q

steroid hormone receptors are of this class

A

intracellular, hormone-receptor complex binds to DNA

59
Q

for a congerneric series of agonists, lower ED50 means

A

lower dissociation constant (tighter receptor binding)

60
Q

the effect of a competitive agonist is

A

to reduce apparent affinity of D for R

61
Q

competitive antagonist bind

A

reversibly with same site on receptor as the agonist

62
Q

with competitive inhibitor, curve shifts

A

right

63
Q

with competitive inhibitor, slope and maximum response

A

do not change

64
Q

the effect of the inhibitor may reversible or irreversible, but the agonist has no influence on the extent of antagonism

A

noncompetitive inhibition

65
Q

with noncompetitive inhibitor, curve shifts

A

generally not (kd isn’t changing)

66
Q

with noncompetitive inhibitor, maximum response

A

is decreased

67
Q

no drug effect seen until minimum occupancy is achieved

A

fractional occupancy threshold

68
Q

effect of fractional occupancy threshold on slope

A

increases

69
Q

effect of fractional occupany threshold on curve shift

A

shifts to the right

70
Q

with fractional occupancy threshold, the ED50

A

overestimates the dissociation constant (ED50>Kd)

71
Q

drug maximal effect achieved without occupying all receptors

A

spare receptors

72
Q

in the presence of spare receptors, curve shifts

A

to the left

73
Q

in the presence of spare receptors, ED50

A

is less than (underestimates) Kd

74
Q

incapable of causing a maximal response at any concentration

A

partial agonist

75
Q

describes the binding forces between drug and receptor

A

affinity

76
Q

describes the physiological effectiveness of the drug receptor complex

A

efficacy

77
Q

partial agonists act as antagonists by

A

binding receptors but having low intrinsic activity

78
Q

slope of an LDR curve indicates

A

how steeply the drug effect varies with dose = one indication of the margin of safety

79
Q

curve that shows a normal distribution around the average dose patients first respond to

A

Non-cumulative dose-response frequency curve

80
Q

dose at which 50% of patients show a toxic response

A

TD50

81
Q

equation for therapeutic index

A

TD50/ED50

82
Q

rapid decrease in the magnitude of response due to the action of a drug

A

tachyphylaxis

83
Q

decrease in response to a given does resulting from prolonged administration

A

tolerance

84
Q

what follows zero order kinetics?

A

constant IV infusion

85
Q

more rapid absorption will ____ peak plasma concentration, ____latency, and ____duration

A

increase, decrease, decrease

86
Q

increase in dose will ____ latency, ____ peak plasma concentration, and ____ duration of effect

A

decrease, increase, increase

87
Q

more rapid elimination will ____ peak plasma concentration and duration of effect

A

decrease

88
Q

when repeated doses of a drug are given at short intervals and elimination is a first order process, plasma concentration will

A

plateau

89
Q

when a drug is administered at a constant rate IV, and eliminated first order, plasma concentration will

A

plateau

90
Q

approximate total body storage equals

A

1.44 times the amount administered per half life

91
Q

avoiding toxicity and maintaining steady state is easier when drugs have

A

a long half life

92
Q

in zero order elimination, k=

A

Er

93
Q

in first order elimination, k=

A

.693/halflife

94
Q

typically, absorption follows

A

first order kinetics

95
Q

equation for bioavailability

A

F=AUCoral/AUCiv

96
Q

equation for relative bioavialability

A

AUCgeneric/AUCtradename

97
Q

triphasic curve, rapid peak and decline, slow decline

A

Single-dose IV, long decline=Ke

98
Q

level of drug in blood rises slowly until elimination = absorption. Bioavailability=1

A

subcutaneous or intramuscular single dose

99
Q

blood level rises until equal to elimination, Cmax is slower, tmax is later

A

oral, single dose

MM Pharmacology (5 decks)

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