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Pharmacology 2 > ADME > Flashcards

ADME Flashcards

1
Q

Range between Minimum Effective Conc. and Minimum Toxic Conc.

A

Therapeutic Window

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2
Q

__ compounds can readily partition into fat tissue, becoming stored there

A

Lipid soluble

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3
Q

__ drugs commonly bind to Albumin

A

Acidic

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4
Q

__ drugs commonly bind to Globulins

A

Basic

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5
Q

Absorption describes

A

Rate at which a drug leaves its site of admin, and extent to which that occurs

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6
Q

Acidification of urine facilitates

A

Removal of Basic Drugs and Metabolites

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7
Q

Active Transport: exhibits saturation?

A

Yes

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8
Q

Alkalinization of urine facilitates

A

Removal of Acidic Drugs and Metabolites

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9
Q

At steady state, acidic drugs will accumulate on more __ side of membrane

A

Basic

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10
Q

At steady state, basic drugs will accumulate on more __ side of membrane

A

Acidic

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11
Q

Cause of drug accumulation in tissues often arises from

A

Active transport or binding

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12
Q

Concentration difference between Minimum Effect Conc. and Peak Plasma Concentration

A

Intensity of Oral Drug

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13
Q

Conjugated byproducts of drugs previously metabolized by liver may undergo hydrolysis back to parent in intestines, and be reabsorbed to liver by portal circulation

A

Enterohepatic Cycling

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14
Q

Diffusion Coefficient (D)

A

Inversely related to the size of the drug

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15
Q

Driving force for drug movement across membrane is

A

Concentration gradient of non-ionized rug

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16
Q

Drug binding to plamsa proteins is a ___ process

A

Saturable and Nonlinear

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17
Q

Drug types good for Percutaneous

A

Lipid soluble

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18
Q

Drugs are absorbed only when

A

Non-ionized

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19
Q

Effect of Enterohepatic Cycling on elimination

A

Decreases elimination rate

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20
Q

Facilitated Diffusion: exhibits saturation?

A

Yes

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21
Q

Falling Phase

A

(Met + Exc) > Abs

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22
Q

Fat soluble vitamins (ADEK) get in via

A

pinocytosis

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23
Q

Fick’s Law

A

*-DAK (dC) / dX

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24
Q

Formula for Vd

A

Amount of drug administered / Plasma drug concentration

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25
Q

Fractional extent to which a given dose of a drug reaches either its site of action or a biological compartment from which the drug has free access to its site of action

A

Bioavailability

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26
Q

Glomerular Filtration Rate is a ___ process

A

Passive and Nonsaturable

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27
Q

How does gastric emptying affect absorption

A

Increasing gastric emptying increases absorption

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28
Q

How is GFR often measured clinically

A

Clearance of Creatinine

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29
Q

How many ATP necessary for CYP

A

none

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30
Q

If dissolution is slow relative to absorption, then we are concerned with

A

dissolution

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31
Q

If drug is filtered, but not secreted or reabsorbed, renal clearance will be

A

120 ml/min

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32
Q

If drug is net reabsorbed, renal clearance will be

A

less than 120 mL/min

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33
Q

If Phase 1 metabolites are sufficiently polar, they

A

may be excreted in urine

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34
Q

If renal clearance is < GFR)

A

Net reabsorption

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35
Q

If renal clearance is >120 mL/min (CLr > GFR)

A

Tubular secretion must be contributing

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36
Q

If renal clearance is 120 mL/min (CLr = GFR)

A

Drug is filtered, but not secreted or reabsorbed

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37
Q

If tubular secretion is contributing to elmination, renal clearance will be

A

greater than 120mL/min

38
Q

Important consequence of Phase 1 metabolic reactions

A

Products are often highly reactive and potentially toxic

39
Q

In non-uniform distribution pattern, the highest concentrations are often present in the

A

kidney, liver, and intestine

40
Q

Increasing gastric emptying time will

A

increase drug absorption

41
Q

Induction vs Inhibition

A

Induction increases metabolism of that and/or other drugs

42
Q

Intensity of Oral Drug

A

Concentration difference between Minimum Effect Conc. and Peak Plasma Concentration

43
Q

Ion trapping

A

Acidic drugs accumulate on more basic side of membrane and vice versa

44
Q

Large and polar drugs need

A

carrier

45
Q

Main conjugation reaction in body

A

Glucoronidation

46
Q

Main way drugs get in

A

Passive Diffusion

47
Q

Major catalyst of Phase 1 biotransformation

A

CYP450 family

48
Q

Major determinant of fraction of drug bound to serum proteins at high conc.

A

Number of binding sites

49
Q

Major determinant of fraction of drug bound to serum proteins at low conc.

A

Affinity of binding sites

50
Q

Metabolism tends to convert

A

Active to less active and/or more polar and less lipophilic for excretion

51
Q

Method of termination other than metabolism, excretion

A

Redistribution

52
Q

Michaelis Menten eq.

A

V = Vmax(S) / (Km + [S])

53
Q

Most acidic drugs will be __ in the stomach

A

Non-ionized –> Absorbed

54
Q

Most drug metabolizing enzymes are found in

A

ER and Cytosol

55
Q

Most phase 1 reactions take place in

A

ER

56
Q

Most phase 2 reactions take place in

A

Cytosol

57
Q

MTC / MEC

A

Therapeutic Index

58
Q

Only energy source for CYP

A

NADPH

59
Q

Overall renal excretion is controlled by

A

what happens in tubules

60
Q

Partition Coefficient (K)

A

Reflects the lipid solubility of the drug (oil:H2O)

61
Q

pH Partition Theory

A

Drugs absorbed when non-ionized –> Higher lipid solubility

62
Q

Phase 1 reactions usually convert

A

parent drug to inactive metabolite

63
Q

Phase 2 reactions lead to

A

covalent addition of a functional group to parent compound, or to reactive product of phase 1 rxn

64
Q

Rate at which a drug leaves its site of admin, and extent to which that occurs

A

Absorption

65
Q

Reabsorption of weak electrolytes is ___ and therefore dependent on ___

A

Passive, pH ov urine

66
Q

Renal capillaries have ___ permeability

A

greater –> more filtration

67
Q

Resultant metabolite from phase 2 is usually

A

more water soluble and less lipid soluble –> less drug reabsorbed from kidney

68
Q

Rising Phase

A

Abs > (Met + Exc)

69
Q

Secretion of electrolytes in proximal tubule is

A

Active (requires transporter MDR2)

70
Q

Size cut off for pinocytosis

A

> 25 kD

71
Q

Stomach traps __ drugs

A

basic

72
Q

Substrates for P-Glycoprotein (MDR1)

A

Chemotherapeutic Agents

73
Q

Therapeutic Index

A

MTC / MEC

74
Q

Tissue binding usually arises thru

A

interactions with proteins and/or phospholipids

75
Q

Total blood flow is greatest to

A

Brain, Kidneys, Liver, Muscle

76
Q

Transporter in Proximal Tubule

A

MDR2

77
Q

Type of drugs that would absorbed in stomach

A

Acid drugs (wouldn’t be ionized)

78
Q

Type of solution that absorbs quickly subQ

A

aqueous

79
Q

Vd greater than 40 means

A

Concentrated in organ

80
Q

Vd less than 4 means

A

Plasma

81
Q

Vd of 40 means

A

Uniform

82
Q

What body position decreases gastric emptying

A

Lying on left

83
Q

What drugs decrease gastric emptying

A

Anticholinergics, Narcotics, Analgesics

84
Q

What is excreted in Proximal tubule

A

Weak electrolytes

85
Q

What is passively transferred in Distal Tubule

A

Lipid Soluble drugs

86
Q

What size is considered low MW

A

100-200 Da

87
Q

What type of meal decreases gastric emptying

A

Fatty

88
Q

What type of molecules can be reabsorbed in distal tubules

A

Nonionized (lipid soluble) forms of weak acids/bases

89
Q

Where does Glucoronidation occur

A

Liver

90
Q

Which variable of Fick’s law does ionization affect?

A

K

Pharmacology 2 (8 decks)

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