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pharm sci > test 3 > Flashcards

test 3 Flashcards

1
Q

rate of elimination

A

mass removed per unit time (mg/hr)

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2
Q

which order is the clearance

A

first order drugs

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3
Q

concentration

A

mass per volume (mg/L)

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4
Q

clearance

A

volume per unit time (L/hr) , Q X E, flow rate times extraction ratio, clearance is a consitant and based on pt liver, kidney, and blood flow to different organs.

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5
Q

the resevior represents

A

vd

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6
Q

the extractor represents

A

organ eliminating drug

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7
Q

amount represents

A

mass of drug in the body “dose”

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8
Q

volume represents

A

vd

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9
Q

Q represents

A

blood to/from organ

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10
Q

C and Cout represents

A

drug going in / out of organ (extractor)

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11
Q

E represents

A

Extraction ratio, Rate of Elimination divided by Rate of presentation

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12
Q

high E vs low E

A

high means the liver chews it up, low means there is a slower process in the liver “how effective is the body at removing the drug”

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13
Q

rate of presentation

A

how much drug is being presented/unit time, Q X Cin - flow to the extractor and multiplying by the concentration of the drug that is entering

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14
Q

Rate of elimination

A

flow rate into and out of the extractor, Q, and multiplying by the difference between the concentration coming in and coming out OR Rate of presentation X Q X E. Concentration dependent. ROE x Cl volume cancles. ROE = Conc x CL

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15
Q

extraction ratio

A

rate of elimination divided by the rate of presentation (C in-C out)/ C in

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16
Q

what variables could we manipulate in order to change the rate of drug elimination

A

blood flow to make Q lower than normal - liver is more confined. Q and E can affect the liver to remove the drug

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17
Q

Cl / vd

A

clearance

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18
Q

as k becomes small

A

half life longer, clearance small, vd large

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19
Q

if Cl is big

A

K is big (hr -1)

20
Q

fractional RoE

A

RoE / Ao (dose)

21
Q

can you change the extraction ratio?

A

yes! drug inhibitor of an enzyme, enzyme inducer- cl changes and goes up, give more drug

22
Q

enzyme inducer

A

clearance will change and go up! excreting the drug faster. half life will decrease and give more drug because of eliminating more frequent!

23
Q

why does k stay the same

A

cl and vd are dependent on body weight. as cl increases the vd will also increae. the half life will also stay the same. if a drug is fat soluble then the k may change

24
Q

other ways to say drug metabolism

A

xenobiotic metabolism, drug metabolism, drug biotransformation

25
Q

in general drug metabolism

A

converts a lipophillic substance, chemical to a metabolite (product) that is more hydrophilic than the parent drug in order to facilitate elimination - filtered more easily - the drug is usually catalyzed by enzymes

26
Q

in drug metabolism it is usually catalyzed by enzymes

A
  1. multiple enzymes and paths are possible for a single drug

2. multiple metabolites with varying properties are possible - metabolite can be more active than the parent drug

27
Q

routes of elimination for top 200 drugs by percentage

A

75% metabolism
20% kidneys
15% bile (does not chemically alter the drug or else it would be metabolism - hepatocyte takes from blood and puts it in the bile!)

28
Q

consequences of drug metabolism

A

usually inactivation, the pharmacological activity (therapeutic or toxic) may be changed, resulting metabolites can be classified as active or inactive

29
Q

inactive metabolites

A

devoid of pharmacological activity, metabolic changes result in the termination of drug action, chemical properties of the drug are changed, affecting how a drug interacts with target or changes the distribution of the drug
EX: blocks alpha1 receptors and then blocks Beta1 receptors when metabolized

30
Q

active meatabolites

A

have pharmacological activity, similar to the desired activity, unexpected/new activity not observed with parent drug

31
Q

what effect can a quinone do

A

causes harm in the body - deplete glutathione which can result in no liver activity afterwards

32
Q

nor/des

A

without a methyl group

33
Q

drug bioactivation

A 
parent drug (prodrug) has no pharmacological activity
to attain pharmacological activity the prodrug must undergo metabolism - more lipophilic will cross the membrane and enhance absorption, when it overcomes activation it is now more polar
34
Q

where is the highest concentration of drug metabolizing enzymes

A

liver

35
Q

phase one reactions

A

oxidation, hydrolysis, reduction, add or reveal a polar functional group, inc water solubility and facilitate excretion, does not always terminate drug action, metabolite may undergo phase 2 reactions. can go through several phase one reactions, small functional group

36
Q

phase two reactions

A

conjugation, add biomolecules to a functional group on drug or phase one metabolite. increases water solubility and facilitates elimination, increases molecular weight (sulfate or glutathione) and requires a high energy cofactor, usually terminates drug action, phase 2 conjugates may undergo phase 1 metabolism

37
Q

oxidation

A

most common phase 1 reaction, largely catalyzed by the cytochrome 450 enzymes, responsible for metabolism of 85% of drugs, several isoforms of CYP450, broad substrate specificity, looks for lipophilic and tries to make it more hydrophilic

38
Q

about CYP450

A

contains heme molecules bound to iron (Fe), absorbs light at or near 450 nm when Fe is bound to carbon monoxide, embedded in the endoplasmic reticulum of cells, requires a NADPH and molecular oxygen - something has to be reduced,

39
Q

major CYP reactions

A 
aromatic, aliphatic, acyclic hydroxylation
alkene oxidation
o and n dealkylation
deamination
N oxidation
40
Q

hydroxylation

A

adding a hydroxyl group, at places with little steric hindrance, para and ortho are the most reactive by p450

41
Q

alkene oxidation

A

converts it to an epoxide by a p450, very reactive molecule

42
Q

epoxide hydrolase

A

converts epoxide to two alcohols with addition of H2O, no p450 added, makes the molecule much less reactive

43
Q

O and N dealkylation

A

CYP2D6, remove methyl groups (alkyl groups)

44
Q

deamination vs dealkylation

A

deamination removes entire amine group, dealkylation just removes the methyl and makes the amine group primary

45
Q

N and S oxidation

A

adds an OH group. CYP. also catalyzed by flavin-containing monooxygenases (FMOs), FMOs and CYPs share a substrate

pharm sci (12 decks)

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