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PROD131 > Topics Relevant to Pharmaceutical Formulations > Flashcards

Topics Relevant to Pharmaceutical Formulations Flashcards

1
Q

Biological systems

A

molecules > cell > tissue > organ > organism > population > ecosystems > biosphere

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2
Q

Basic macromolecules of life

A

lipids, carbohydrates, proteins, nucleic acids (DNA/RNA)

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3
Q

Human biological systems

A

Chemical level (C, H, O, N, P)
Cellular
Tissue
Organ
System
Organism

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4
Q

Pharmacology

A

science of study of drug

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5
Q

Pharmacokinetics

A

study of medicine movement. absorption, distribution, metabolism, excretion ADME

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6
Q

Systemic circulation

A

within the system

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7
Q

Site of action

A

where the drug goes

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8
Q

Subtherapeutic

A

in the blood, not enough concentration yet

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9
Q

Drug toxicity

A

too much in the system

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10
Q

Absorption

A

site of administration in to plasma

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11
Q

Distribution

A

journey of drug through bloodstream to reach target cells and molecules.

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12
Q

Metabolism

A

breakdown of drug in liver

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13
Q

Excretion

A

transportation of drug metabolites out of the body

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14
Q

Cell membrane physiology

A

control intake and elimination to and from blood. control movement of molecules.

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15
Q

Hepatocyte

A

liver cell

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16
Q

Epithelial cell membranes

A

can flatten and stretch in human body. have different adaptations depending on where they are in the body

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17
Q

Cell transport

A

through biological membrane to move food, water and waste

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18
Q

Passive transport

A

no energy
diffusion (simple)
facilitated diffusion
osmosis
filtration

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19
Q

Diffusion

A

single substance moves from an area of high concentration to low until concentration is equal

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20
Q

Facilitated diffusion

A

material moves across plasma membrane with assistance of proteins down concentration gradient without cellular energy use

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21
Q

Osmosis

A

diffusion of water through semipermeable membrane according to concentration gradient

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22
Q

Filtration

A

movement of water and solute molecules across cell membrane due to hydrostatic pressure from cardiovascular system

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23
Q

Active transport

A

requires energy
primary, secondary, carrier proteins

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24
Q

Primary active transport

A

direct active transport or uniport. Energy (ATP) used to directly pump solute across membrane against electrochemical gradient

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25
Q

Secondary active transport

A

coupled transport or cotransport. energy used to transport molecules across membrane through electrochemical potential difference

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26
Q

Types of carrier proteins

A

Uniporter, symporter, antiporter (diff directions)

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27
Q

Bulk transport

A

movement of macromolecules
exocytosis, endocytosis

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28
Q

Exocytosis

A
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29
Q

Endocytosis

A
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30
Q

Drug absorption

A
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31
Q

Factors affecting drug absorption

A

biological, pharmaceutical and others

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32
Q

Biological factors affecting drug absorption

A

pH of GIT organs, presence of food and other drugs, surface area of GIT organs, disease state, GIT mobility, first pass metabolism

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33
Q

Pharmaceutical factors affecting drug absorption

A

physical state of drug, water or lipid solubility of drug, chemical stability, molecular weight, particle size of drug, disintegration time, dissolution rate, enteric coating of drug

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34
Q

Other pharmaceutical factors affecting drug absorption

A

gastric emptying time, drug formulation, pH and fluid in small intestine, surface area of absorption surfaces, blood flow, membrane penetration rate, food, age, gender and health situation

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35
Q

Chemical nature of drugs (pH affect)

A

pH of drug will dissolve and absorb in similar pH organs and remain unionized

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36
Q

Oral route metabolism

A

esophagus, GIT, liver, pulmonary circulation, systemic circulation, targeted site of action.

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37
Q

Intravenous route metabolism

A

venous network, pulmonary circulation, systemic circulation, targeted site of action. By passes GIT so no chance of first pass metabolism

38
Q

First pass metabolism

A

degree of metabolic breakdown of oral administered drug in liver/intestine before systemic circulation

39
Q

Pharmacokinetic curves

A

blood plasma concentration - time curve. shows rate of absorption and therapeutic window

40
Q

MTC

A

max tolerated concentration of a drug

41
Q

MEC

A

min effective concentration of a drug

42
Q

Theraputic range

A

MTC - MEC

43
Q

Duration of action

A

window of therapeutic range. begins at the onset time at the first MEC

44
Q

AUC

A

area under the curve. concentration over time (bioavailability)

45
Q

Pharmacokinetic curves depending on dosage route (order of efficiency)

A

IV - negative linear (no absorption)
Intramuscular
Subcutaneous (skin layer)
Oral
Rectal

46
Q

Bioavailability

A

amount or % of active drug that is absorbed from given dosage and reach systemic circulation. Is AUC and calculated for non-IV route

47
Q

Bioavailability calculation

A

BA = AUC(per oral) / AUC(IV) (x 100)

48
Q

Bioequivalence

A

comparison between bioavailabilities of drugs

49
Q

IV BA

A

100% most rapid onset

50
Q

Intramuscular BA

A

75-100% large volumes, feasible, painful

51
Q

Subcutaneous BA

A

75-100% smaller volumes, painful

52
Q

Oral BA

A

0-100% most convenient

53
Q

Rectal BA

A

30-100% less first pass effect

54
Q

Inhalation BA

A

5-100% often rapid onset

55
Q

Transdermal BA

A

80-100% slow absorption and onset of action, no first pass effect, long duration of action

56
Q

ADME

A

absorption, distribution, metabolism, excretion

57
Q

Drugs and proteins in bloodstream

A

sometimes drugs bound to proteins (albumin) and delay entry to site of action. some drugs are highly bound and some aren’t

58
Q

Drug and plasma protein complex

A

drugs bound to proteins. doesn’t show pharmacological action, can’t cross cell membrane and delays excretion

59
Q

High protein bound drug examples

A

doxycycline, warfarin, indomethacin, propranolol, chlorpropamide, imipramine and phenytoin

60
Q

Degree of drug binding

A

bound concentration over total concentration.
alpha = C(b)/(C(u)+C(b)

61
Q

Volume of distribution

A

how extensively the drug is distributed to the rest of the body compared to plasma

62
Q

Volume of distribution equation

A

V(d) (L) = Drug total in body (mg)/concentration in blood (mg/L)

63
Q

Volume of distribution relativity

A

Large V(d) = long duration of action

64
Q

Compartments

A

4 major and many minor which drugs can be found in. Free and bound drugs have equilibrium in each

65
Q

Factors affecting drug distribution

A

protein binding, presence of other drug, solubility in lipids, anatomical barriers, pH of compartments, regional blood flow, route of administration, physiochemical

66
Q

Drug metabolism

A

AKA biotransformation. chemical changes as drug is metabolised by biochemical mechanisms

67
Q

Result of biotransformation

A

conversion to 1 or more compounds that are more water soluble, ionised and don’t bind to proteins - readily excreted

68
Q

Where drug metabolism happens

A

mainly in the liver, chemical reactions take place in 2 phases

69
Q

Phase 1 of metabolism

A

reduction, hydrolysis or oxidation of drug. often still chemically active after this

70
Q

Phase 2 of metabolism

A

conjugation - attachment of iniosed group to the drug make it more water soluble

71
Q

Where does conjugation usually occur

A

in hepatocyte cytoplasm

72
Q

Groups that groups that attach to drug during conjugation

A

glutathione, methyl, sulphur, glucoronide, acetyl

73
Q

Factors affecting metabolism

A

reduced hepatocytes and enzyme activity, disease, genetic defect, alcohol and drugs, nutrition, environment, aging

74
Q

Major processes of excretion

A

renal, biliary, pulmonary

75
Q

Minor routes of excretion

A

saliva, sweat, breast milk, vaginal fluid

76
Q

Clearance of a substance

A

how much of drug is cleared from the blood at a given time. inversely proportional to half life of a drug

77
Q

Clearance of substance equation

A

urine concentration x urine flow over plasma concentration
Clearance = C(u)xV(u)/C(p)

78
Q

Renal clearance

A

how much of drug volume is being cleared by kidney at any given time

79
Q

Biliary excretion

A

drugs excreted by liver into bile then excreted to intestine where may be reabsorbed. prolongs drug action - enterohepatic circulation

80
Q

Pulmonary exretion

A

enter and exit body through lungs. volatile lipophilic substances (gas) and volatile liquids.

81
Q

Drug toxicity

A

sometimes deadly effects of drug. result of excessive pharmacological action

82
Q

Factors affecting drug toxicity

A

age, genetic, pathological conditions, dosage, drug interaction

83
Q

Pharmacodynamics

A

study of magnitude of drug response.

84
Q

Pharmacodynamics involves

A

onset, intensity, duration of drug response and how these are related to concentration of drug at site of action

85
Q

Drugs can act by

A

stimulating, depressing, irritating, replacing, chemical action or cytotoxic action

86
Q

Drug mechanisms

A

receptors, enzymes, ion channels, physical absorption, chemical reactions, metabolic altering

87
Q

Drugs with receptors

A

Receptor proteins. molecules present either on cell surface or in cell that drug interacts with

88
Q

Drugs with enzymes

A

drugs act by inhibition of enzymes and alter their reactions.

89
Q

Types of drug receptors

A

ligand-gated, enzyme-linked, G-protein coupled, intracellular

90
Q

Drug receptor interactions, basic concepts

A

lock and key relationship. Drug fits into specific receptor. Agonist, antagonist or partial agonist.

91
Q

Agonist

A

activate receptor

92
Q

Antagonist

A

block agonist from entering site, no activation

PROD131 (12 decks)

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