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
Secondary active transport
coupled transport or cotransport. energy used to transport molecules across membrane through electrochemical potential difference
26
Types of carrier proteins
Uniporter, symporter, antiporter (diff directions)
27
Bulk transport
movement of macromolecules exocytosis, endocytosis
28
Exocytosis
29
Endocytosis
30
Drug absorption
31
Factors affecting drug absorption
biological, pharmaceutical and others
32
Biological factors affecting drug absorption
pH of GIT organs, presence of food and other drugs, surface area of GIT organs, disease state, GIT mobility, first pass metabolism
33
Pharmaceutical factors affecting drug absorption
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
34
Other pharmaceutical factors affecting drug absorption
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
35
Chemical nature of drugs (pH affect)
pH of drug will dissolve and absorb in similar pH organs and remain unionized
36
Oral route metabolism
esophagus, GIT, liver, pulmonary circulation, systemic circulation, targeted site of action.
37
Intravenous route metabolism
venous network, pulmonary circulation, systemic circulation, targeted site of action. By passes GIT so no chance of first pass metabolism
38
First pass metabolism
degree of metabolic breakdown of oral administered drug in liver/intestine before systemic circulation
39
Pharmacokinetic curves
blood plasma concentration - time curve. shows rate of absorption and therapeutic window
40
MTC
max tolerated concentration of a drug
41
MEC
min effective concentration of a drug
42
Theraputic range
MTC - MEC
43
Duration of action
window of therapeutic range. begins at the onset time at the first MEC
44
AUC
area under the curve. concentration over time (bioavailability)
45
Pharmacokinetic curves depending on dosage route (order of efficiency)
IV - negative linear (no absorption) Intramuscular Subcutaneous (skin layer) Oral Rectal
46
Bioavailability
amount or % of active drug that is absorbed from given dosage and reach systemic circulation. Is AUC and calculated for non-IV route
47
Bioavailability calculation
BA = AUC(per oral) / AUC(IV) (x 100)
48
Bioequivalence
comparison between bioavailabilities of drugs
49
IV BA
100% most rapid onset
50
Intramuscular BA
75-100% large volumes, feasible, painful
51
Subcutaneous BA
75-100% smaller volumes, painful
52
Oral BA
0-100% most convenient
53
Rectal BA
30-100% less first pass effect
54
Inhalation BA
5-100% often rapid onset
55
Transdermal BA
80-100% slow absorption and onset of action, no first pass effect, long duration of action
56
ADME
absorption, distribution, metabolism, excretion
57
Drugs and proteins in bloodstream
sometimes drugs bound to proteins (albumin) and delay entry to site of action. some drugs are highly bound and some aren't
58
Drug and plasma protein complex
drugs bound to proteins. doesn't show pharmacological action, can't cross cell membrane and delays excretion
59
High protein bound drug examples
doxycycline, warfarin, indomethacin, propranolol, chlorpropamide, imipramine and phenytoin
60
Degree of drug binding
bound concentration over total concentration. alpha = C(b)/(C(u)+C(b)
61
Volume of distribution
how extensively the drug is distributed to the rest of the body compared to plasma
62
Volume of distribution equation
V(d) (L) = Drug total in body (mg)/concentration in blood (mg/L)
63
Volume of distribution relativity
Large V(d) = long duration of action
64
Compartments
4 major and many minor which drugs can be found in. Free and bound drugs have equilibrium in each
65
Factors affecting drug distribution
protein binding, presence of other drug, solubility in lipids, anatomical barriers, pH of compartments, regional blood flow, route of administration, physiochemical
66
Drug metabolism
AKA biotransformation. chemical changes as drug is metabolised by biochemical mechanisms
67
Result of biotransformation
conversion to 1 or more compounds that are more water soluble, ionised and don't bind to proteins - readily excreted
68
Where drug metabolism happens
mainly in the liver, chemical reactions take place in 2 phases
69
Phase 1 of metabolism
reduction, hydrolysis or oxidation of drug. often still chemically active after this
70
Phase 2 of metabolism
conjugation - attachment of iniosed group to the drug make it more water soluble
71
Where does conjugation usually occur
in hepatocyte cytoplasm
72
Groups that groups that attach to drug during conjugation
glutathione, methyl, sulphur, glucoronide, acetyl
73
Factors affecting metabolism
reduced hepatocytes and enzyme activity, disease, genetic defect, alcohol and drugs, nutrition, environment, aging
74
Major processes of excretion
renal, biliary, pulmonary
75
Minor routes of excretion
saliva, sweat, breast milk, vaginal fluid
76
Clearance of a substance
how much of drug is cleared from the blood at a given time. inversely proportional to half life of a drug
77
Clearance of substance equation
urine concentration x urine flow over plasma concentration Clearance = C(u)xV(u)/C(p)
78
Renal clearance
how much of drug volume is being cleared by kidney at any given time
79
Biliary excretion
drugs excreted by liver into bile then excreted to intestine where may be reabsorbed. prolongs drug action - enterohepatic circulation
80
Pulmonary exretion
enter and exit body through lungs. volatile lipophilic substances (gas) and volatile liquids.
81
Drug toxicity
sometimes deadly effects of drug. result of excessive pharmacological action
82
Factors affecting drug toxicity
age, genetic, pathological conditions, dosage, drug interaction
83
Pharmacodynamics
study of magnitude of drug response.
84
Pharmacodynamics involves
onset, intensity, duration of drug response and how these are related to concentration of drug at site of action
85
Drugs can act by
stimulating, depressing, irritating, replacing, chemical action or cytotoxic action
86
Drug mechanisms
receptors, enzymes, ion channels, physical absorption, chemical reactions, metabolic altering
87
Drugs with receptors
Receptor proteins. molecules present either on cell surface or in cell that drug interacts with
88
Drugs with enzymes
drugs act by inhibition of enzymes and alter their reactions.
89
Types of drug receptors
ligand-gated, enzyme-linked, G-protein coupled, intracellular
90
Drug receptor interactions, basic concepts
lock and key relationship. Drug fits into specific receptor. Agonist, antagonist or partial agonist.
91
Agonist
activate receptor
92
Antagonist
block agonist from entering site, no activation