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POD > Pharm > Flashcards

Pharm Flashcards

1
Q

What are the properties of drugs that contribute to activity?

A

molecular size
solubility
charge

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2
Q

What is the partition coefficient?

A

determined by overall polarity of drug
[lipid]/[water]
>1 lipophilic, easier to distribute

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3
Q

What is significant about quaternary ammonium salts?

A

permanent cations

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4
Q

What are the factors that govern filtration?

A

size of pore

pressure gradient

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5
Q

How are neutral drugs absorbed?

A

uncharged-pores, passive diffusion

charged-pores, active transport

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6
Q

How are acidic drugs absorbed?

A

HA-pores, passive diffusion

A-pores, active transport

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7
Q

How are basic drugs absorbed?

A

B-pores, passive diffusion

HB-pores, active transport

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8
Q

What is enteral administration?

A

placing the drug into some portion of the GI

oral, sublingual, rectal

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9
Q

What are the advantages of oral administration?

A

passive diffusion
most in small intestine due to time and size
carried to liver via portal

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10
Q

What is first pass elimination?

A

extensive hepatic clearance via biotransformations

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11
Q

What are the advantages of sublingual administration?

A

enter general circulation by passive diffusion

useful for drugs that do not survive oral administration (nitroglycerin)

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12
Q

What are the advantages of rectal administration?

A

dissolves and absorbed by passive diffusion
enters general circulation
good for unconscious, vomiting, or uncooperative patients

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13
Q

What is parenteral administration?

A

drug in some portion of body other than GI (subcutaneous, intramuscular, intravenous, intraarterial, inhalation, intrathecal)

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14
Q

What are the advantages of subcutaneous administration?

A

absorption by passive diffusion
small and large hydrophilic
rate depends on blood flow

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15
Q

What are the advantages of intramuscular administration?

A

can use large volumes and more irritating drugs

good for orally labile, depot preparations

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16
Q

What are the advantages of intravenous administration?

A

no absorption

rapid onset but cannot redraw or retard absorption

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17
Q

What are the advantages of intraarterial administration?

A

no absorption

achieves high localized drug concentration

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18
Q

What are the advantages of inhalation administration?

A

must dissolve in pulmonary fluids before absorption by passive diffusion

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19
Q

What are the advantages of intrathecal?

A

directly into subarachnoid space

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20
Q

What is the first barrier for drug distribution?

A

capillary endothelium

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21
Q

How do drugs enter the CNS?

A

passive at ventricles
active at choroid plexus
movement mainly out of CSF and into blood

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22
Q

What is significant about the prostate?

A

highly acidic

basic drugs are protonated and build up

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23
Q

What is biotransformation and where does it occur?

A

mainly in the liver
Phase I-oxidation, reduction, hydrolysis
Phase II-conjugation

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24
Q

What are microsomal enzymes?

A 
located in smooth ER
cytochrome P450-terminal oxidase
substrates must be lipophilic
activity is inducible
CYP3A4/5 is most important
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25
Q

Where does acetylation occur?

A

omega-1 or para on aromatic ring

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26
Q

What are nonmicrosomal enzymes?

A

in cytosol and mitochondria
also in blood as esterases
not inducible
perform all hydrolysis reactions

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27
Q

What are the conjugation reactions that occur?

A

sulfate is more common but cofactor is limited

gluconuration becomes more important

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28
Q

What are the two primary routes of drug excretion?

A

biliary and renal

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29
Q

How does a drug get excreted in bile?

A

Portal vein from absorption
Hepatic artery from circulation
if greater than 300–>biliary excretion
can undergo enterohepatic recycling (reabsorbed into portal) to increase half life

30
Q

How does a drug get excreted in urine?

A

filtration if less than albumin and not bound to protein
can be secreted by OCT or OAT
back flow can occur in distal convoluted tubule

31
Q

What is the difference between pharmacokinetics and pharmacodynamics?

A

kinetics-system on drug

dynamics-drug on system

32
Q

What is affinity?

A

ability with which the drug binds to the specific receptors

33
Q

What is intrinsic activity?

A

property of drug to impart a cellular response

34
Q

What is an agonist?

A

stimulates-affinity and intrinsic activity

35
Q

What is an antagonist?

A

affinity but no intrinsic activity

36
Q

What is an inverse agonist?

A

turns off a constitutively activated receptor

37
Q

What is specificity?

A

single receptor type

38
Q

What is selectivity?

A

single effect

39
Q

What are the different mechanisms?

A 
intracellular
membrane spanning enzymes
intracellular tyrosine kinase
membrane ion channels
G proteins
40
Q

What is supersensitization?

A

sustained antagonist increase the number of receptors

41
Q

What is desensitization?

A

sustained agonist decrease number of receptors

42
Q

What is tachyphylaxis?

A

loss of response on repeated administration-slower dissociation

43
Q

What actions are not receptor mediated?

A

neutralization of gastric acid
osmotic diuretics
cholesterol binding resins
antibiotics

44
Q

What is the one compartment model?

A

equilibriates between plasma and tissues relative to elimination
proportional changes
not necessarily distributed to all tissue
semi log plot is linear

45
Q

What is the two compartment model?

A 
drug takes longer time to equilbriate
two slopes (distribtuion and elimination)
46
Q

What is first order elimination?

A

constant rate of elimination
independent of dose
linear on semi log
enzymes are not saturated

47
Q

What is zero order elimination?

A

constant amount of elimination
linear on linear scale
enzymes are saturated

48
Q

What is bioavailability? How is it calculated?

A

amount that reaches circulation
F=1 for iv
compare area under curve for route compared to iv
important in preparation of generic drugs

49
Q

What is half life? What is the formula?

A

time to remove half of drug

0.693/Ke

50
Q

What is the volume of distribution? What is the significance of high/low Vd? What is the formula?

A

apparent volume that a drug is distributed within the body
high=lipophilic, low=bound to protein
Vd=dose/concentration

51
Q

What is clearance? How is it calculated?

A

volume of blood from which a drug is completely removed in a given time
Cl=Ke(Vd)

52
Q

What is the steady state concentration?

A

first order kinetics will eventually reach equilibrium in 4 half lives (balance between intake and elimination)
Css=MD/Cl

53
Q

What is the maintenance dose?

A

drug given at constant interval

MD=[dose(F)]/interval

54
Q

What is a loading dose?

A

iv administration to get to Css quickly

loading dose=[Css(Vd)]/F

55
Q

What is the median effective dose?

A

dose required to produce therapy in 50%

56
Q

What is the median lethal dose?

A

dose required to produce death in 50%

57
Q

What is the therapeutic ratio?

A

LD50/ED50

larger is safer

58
Q

What is the certain safety factor?

A

LD1/ED99

greater than 1 means little overlap

59
Q

What is the standard safety margin?

A

(LD1-ED99)/ED99

60
Q

What is pharmacogenetics?

A

genetic basis for variation in drug response

61
Q

What can polymorphisms do to Km and Vmax?

A

change
increase Km decrease affinity
decrease Vmax decrease rate

62
Q

What happens with Asians flushing?

A

loss of aldehyde dehydrogenase

63
Q

What happens with NAT2 acetylators?

A

isoniazid
Inuit and Japanses are fast
Scandanavians are slow

64
Q

What is the significance of CYP3A5?

A

variation metabolism faster in African population

65
Q

What is significant about vitamin K oxidoreduction?

A

variant requires higher dosing

66
Q

What is significant about CYP2C9?

A

variant requires lower dose because not metabolized as well

67
Q

What is significant about 2B6?

A

cannot make prodrug of cyclophosphamide

68
Q

What is significant about GST?

A

increased toxicity of alkylating agents

decrease response in breast cancer

69
Q

What is signficant about G6PD deficiency?

A

methemoglobinemia when given Dapsone (oxidized)

70
Q

How does the dose response curve shift with an antagonist?

A

shift to the right

71
Q

What does potentiation do to the graph?

A

shift to the left-increases the effect

example-cocaine keeping norepinephrine in synaptic cleft longer due to decrease in reuptake

POD (4 decks)

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