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Module 4 > Biopharmaceutics > Flashcards

Biopharmaceutics Flashcards

1
Q

Study of pharmacotechnical factors in drug products that can affect pharmacokinetics of drugs

A

Biopharmaceutics

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2
Q

2 layers of phospholipid between two surface layers of proteins

A

Lipid Bilayer/Unit Membrane Theory

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3
Q

Globular proteins embedded in a dynamic fluid, lipid bilayer matrix

A

Fluid Mosaic Model

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4
Q

Proteins are embedded and are used as receptors and for transport

A

Modified Fluid Mosaic Model

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5
Q

Semi-permeable membrane, Selective barrier, Drugs can transport via several mechanisms

A

Cell Membrane

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6
Q

Mechanism of drug movement across the cell membrane

A

Transport

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7
Q

bile acids/salt

A

deoxycholic acid/chenodeoxycholic acid

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8
Q

Dominant transport mechanism but the slowest/No energy required

A

Passive Diffusion

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9
Q

Drug must be small and should be lipid- soluble/Movement along a concentration gradient

A

Diffusion

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10
Q

_____acids exists more in a non-ionized form in a more acidic

A

Weak

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11
Q

High Ka

A

1 x 10^-2

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12
Q

Low Ka

A

1 x 10^-3

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13
Q

Ratio of solubility of a drug in oil to its solubility in water

A

Partition coefficient

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14
Q

K partition

A

lipid solubility/water solubility

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15
Q

greater the solubility of a substance/higher the permeability of the membrane to that particular substance

A

Higher partition coefficient

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16
Q

Cell membrane CHON w/ specific binding sites and can undergo conformational change

A

Carrier-mediated transport

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17
Q

Transport which requires energy, in which can move against the concentration gradient

A

Active Transport

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18
Q

Transport which doesn’t require energy, it move along the concentration gradient and has specific carriers

A

Facilitated diffusion

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19
Q

Fastest transport system

A

Active Transport

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20
Q

Specificity/Selectivity

A

Carrier-mediated transport

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21
Q

Drugs that are Subject to

competition/inhibition/antagonism

A

▸ Isoniazid and Vitamin B6

▸ Digoxin and quinidine

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22
Q

Saturability of Carrier-mediated transport

A

Zero or First Order of Kinetics

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23
Q

Rate of reaction is independent of the concentration of the drug remaining

A

Zero Order

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24
Q

Rate of reaction is dependent of the concentration of the drug remaining

A

First Order

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25
Q

Time it takes for the drug concentration to decrease by 50%

A

Half life

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26
Q

Movement through water-filled pores = channels

A

Convective Transport

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27
Q

Convective Transport: Charge of pore lining

A

allows movement of ions w/ charge opposite of pore lining

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28
Q

Convective Transport: Movement is by solvent drag

A

ions move along the same direction as water

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29
Q

Convective Transport: Movement along an electrochemical gradient

A

Takes into consideration the net charge and the concentration gradient ions with greater concentration gradient will be the one to move

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30
Q

Describes the movement of transport of large ions

A

Ion-Pair Transport

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31
Q

Examples of exogenous large cation

A

▹Quaternary NH4 Compound ▹ Mucin

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32
Q

Invagination of a cell membrane

A

Vesicular Transport

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33
Q

2 Types of Vesicular Transport

A

Endo and Exocytosis

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34
Q

Release of drug from dosage form or drug product

A

Liberation

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35
Q

Factors that are inherent in the drug product as a consequence of formulation and quality that is built in the product

A

Pharmacotechnical

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36
Q

Motion or change in rate

A

Kinesis

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37
Q

Fate of drugs in the body/What the body does to the drug?

A

Pharmacokinetics

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38
Q

Metabolism + Excretion

A

Elimination

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39
Q

Distribution + Eliminitation

A

Disposition

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40
Q

Biochemical & physiological effects of drugs/MOA

A

Pharmacodynamics

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41
Q

What the drug does to the body

A

Pharmacodynamics

42
Q

Rate and extent of disappearance of drug from the site of administration or drug entry into systemic circulation

A

Absorption

43
Q

Rate and extent of drug entry into systemic circulation

A

Bioavailability

44
Q

Methods of determining bioavailability

A

● Drug Plasma Conc. vs. Time

● Cumulative urinary excretion data

45
Q

Measure of the amount of the drug in the body that reflects the total amount of active drug

46
Q

AUC is computed using ______

A

trapezoidal rule

47
Q

Pharmaceutical equivalents that have similar bioavailability when given in the same molar dose and studied under similar experimental conditions

A

Bioequivalent Drug Product

48
Q

Is established when two drug products have similar bioavailabilities/Measure the AUC ratio,Cmax Ratio,Tmax
Ratio

A

Bioequivalence

49
Q

Similarity is established if each of the ratios fall within _

A

80% - 125% at 90%CI

50
Q

Dissolution testing that includes comparison of the dissolution profiles of a generic and a comparator product in three media:

A

pH 1.2, 4.5, and 6.5

51
Q

Process of dispensing a different brand

or unbranded drug product in place of the prescribed drug product

A

Generic Substitution

52
Q

Drug products that contain the same therapeutic moiety but as different
salts, esters or complexes

A

Pharmaceutic Alternatives

53
Q

Different dosage forms and strengths within a product line by a single manufacturer

A

Pharmaceutic Alternatives

54
Q

Drug products with the same API, dosage form, dosage strength, mode of administration, standard quality

A

Pharmaceutic Equivalent

55
Q

Process of dispensing a pharmaceutic alternative for the prescribed drug product

A

Pharmaceutic Substitution

56
Q

Drug products containing different different API that are indicated for the same therapeutic or clinical objectives

A

Therapeutic alternatives

57
Q

Drug products that can be used interchangeably in clinical practices

A

Therapeutic Equivalent

58
Q

Process of dispensing a therapeutic alternative in place of prescribed drug product

A

Therapeutic Substitution

59
Q

Process of drug movement from systemic circulation to different body compartments/Drug reaches the site of action

A

Distribution

60
Q

Factor to be considered with drug distribution

A

▹ Cardiac Output

▹ Regional Blood Flow

61
Q

Volume of blood pumped out by heart in 1 minute

A

Cardiac Output

62
Q

Fraction of Cardiac Output that is delivered to specific tissues or organs

A

Regional Blood Flow

63
Q

Areas with poor blood flow

A

Bones, fats

64
Q

Areas with Highest perfusion

A

Brain, kidney, liver and heart

65
Q

Distribution Parameters

A

Protein Binding

Volume Distribution

66
Q

Large molecule whose distribution is restricted

A

Protein-bound drug

67
Q

Type of drug that can readily cross the cell membrane and exert a pharmacologic effect

68
Q

Blood protein that is dominant and binds with weak acids

A

Albumin: Blood Protein

69
Q

Blood Protein that binds with Weak bases

A

Alpha 1-acid glycoprotein

70
Q

Blood protein that binds with selective hormones

71
Q

Fatty Acids, Vitamin C, Salicylates, Sulphonamides, Barbiturates, Phenylbutazone, penicillins, tetracycline, probenecid; binds with what site ?

72
Q

Adenisine, Streptomycin , Chloramphenicol, Digitoxin, Coumarin binds with what blood protein?

A

Globulins, Alpha (1,2), Beta (1,2), gamma

73
Q

Hypothetical or apparent volume of body fluid that is necessary to dissolve a given amount or dose of a drug to a concentration equal to that of plasma concentration

A

Volume of Distribution

74
Q

Based on hypothesis and simplifying assumptions that describe biological systems in mathematical terms in order to predict drug action

A

Pharmacokinetic Model

75
Q

A hypothetical volume that contains a certain drug concentration

A

Compartment

76
Q

Type of compartment that the body is single compartment where certain volume remains constant; Instantaneous Distribution

A

One Compartment

77
Q

Central/Peripheral

A

Two Compartment

78
Q

Other name of Metabolism

A

Biotransformation

79
Q

Converts drugs into other form

A

Metabolism

80
Q

Drugs that are metabolised are converted into?

A

inactive/non toxic/water soluble compounds

81
Q

Inactive parent drug that needs to be metabolized to active form

82
Q

Initial metabolism of a drug before it reaches the systemic circulation/ decreases oral bioavailability of a drug

A

First Pass Effect/Metabolism

83
Q

Known as the 1st phase of drug metabolism

A

Functionalization Phase

84
Q

Under Phase 1 Metabolism

A

Oxidation
Reduction
Hydrolysis

85
Q

Enzymes under Phase 1: Oxidation

A

CYP Mediated/Independent

86
Q

Substrate under CYP 1A2

A

Acetaminophen, theophylline, Caffeine

87
Q

Substrate under CYPC19

A

Clopidogrel, PPIs

88
Q

Substrate under CYP2C9

A

Warfarin, Phenytoin

89
Q

Substrate under CYP2D6

A

Codeine, Antipsychotics

90
Q

Substrate under CYP3A4,5,7 (superfamily)

A

More than 50% of drugs, CCBs,Macrolides, Azoles, Antifungal, Antihistamines

91
Q

Enzymes under CYP Independent Oxidation

A

monoamine oxidase

Alcohol and aldehyde dehydrogenase

92
Q

Phase 2 Drug Metabolism is also known as?

A

Conjugation reaction/ Synthetic Phase

93
Q

Phase that involves the addition of a polar conjugate

A

Phase 2 Metabolism

94
Q

Glucoronidation Enzyme

A

Glucoronosyl acyltransferase (GluCAT)

95
Q

Acetylation Enzyme

A

N-acetyltransferase

96
Q

Most common endogenous amine for conjugation with organic acids

A

Glycine conjugation

97
Q

Enzymes localised in the liver and kidneys

A

Glutamine Conjugation

98
Q

Reaction that reacts with electrophillic oxygen intermediates

A

Glutathione and mercapturic acid conjugation

99
Q

Stimulate activity or production of enzymes

A

Enzyme induction

100
Q

What happens if the substrate is a prodrug?

A

Increase in activity and risk of toxicity

101
Q

What happens if the substrate has a toxic metabolite?

A

Increase in toxicity

102
Q

What happens if the substrate is active with inactive metabolite?

A

Decrease d

Module 4 (5 decks)

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