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1
Q

penicillin

A

accidentally discovered by inhibition of bacterial growth around a mild colony
B-lactam ring gave activity

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2
Q

Semi-synthesis

A

modify natural structure. to improve targeting, stability, cell penetration, reduce resistance and side-effects

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3
Q

Synthesis

A

synthesise basic structure in lab (by-products found to be antibiotics)

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4
Q

Antibacterial resistance

A

continual sub-toxic exposure from high prescription, mismanagement and inappropriate agriculture use
use ESKAPE organisms (share resistance)

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5
Q

Genomic era

A

microbial genomes sequenced and identify drug targets
no success from the 160/4000 targets found - functional redundancy, nutrient conditions, cofactors, genetic diversity, pharmacokinetics failure

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6
Q

Drug to target

A

identification (libraries), validation, expression/purification, structura determination, binding + inhibitory assays, MIC/MBC, validation, optimisation, efficacy/potency, ADME-Tox evaluation

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7
Q

Screening assays

A

MIC- min inhibition conc
metabolic and metabolite assay
dyes, microdroplets/fluidics, combinational

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8
Q

First antibiotic screening

A

Waksman - agar overlay

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9
Q

traditional medicine

A

the knowledge, skills and practices of indigenous cultures used to prevent, diagnose, improve/treat physical/mental illness

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10
Q

Rongoā māori

A

mana received through training by tohunga, tikanga for collection, preparation and storage
holistic, well being, physical, spiritual and NZ native plant based therapies

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11
Q

Rongoā rākau

A

plants rongoa Maori use

eg Manuka oil and honey

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12
Q

ethnopharmacology

A

validate traditional preparations, isolate active substances and test quality, safety and efficacy.

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13
Q

phenolics

A

reduce free radicals protecting against oxidative stress

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14
Q

partnership with rongoa

A

sustainable, mutual transfer of skills, fair share

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15
Q

ownership of nature

A

indigenous population owns/gaurdians of resource, scientists invent derivatives`

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16
Q

Pharmacokinetics side effects

A

enzyme induction or inhibition

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17
Q

pharmacodynamics side effects

A

not specific to receptor

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18
Q

pharmacogenetics side effects

A

mutation in a receptor changes efficacy

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19
Q

absorption

A

into body via different routes, bioavailability (F)

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20
Q

distribution

A

moving around the body in the blood, volume of distribution (Vd = A/Cp)

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21
Q

metabolism

A

more hydrophobic -> kidney excretion, depends on GI motility + distribution, half life (t1/2)

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22
Q

excretion

A

removal via urine, faeces, skin, breathing

clearance (Cl)

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23
Q

ADME is influenced by

A

disease, pregnancy, genetics, age, diet, other drugs, food

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24
Q

CYP3A4

A

inhibited by grapefruit juice, induced by St John’s wort

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25
Q

pharmacodynamics

A

directly linked to drug action

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26
Q

pharmacokinetics

A

can be linked to increased plasma concentration

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27
Q

Adverse effects examples

A

Propranolol/metoprolol + aspirin selectivity (pharmacodynamics)
Warfin - narrow therapeutic index, protein bound
+ St Johns wort CYP3A4 induction (pharmacokinetics)

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28
Q

Animal testing

A

Cattle, sheep, mice

84% no impact on welfare

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29
Q

Animal Welfare Act 1999

A

Care for animals and need ethical approval

30
Q

3Rs

A

Replacement, reduction, refinement

31
Q

replacement

A

alternatives - computer models, charts and diagrams, invertebrates, tissue culture, videos

32
Q

reduction

A

as few as possible - compare related work, use statistic, tissues from already killed animals

33
Q

refinement

A

pain/suffering reduced - non-invasive observations of conscious animals, reduce invasiveness, use sedatives, monitor for stress

34
Q

Animal testing cons

A

expensive, not representative, use animal with disease

35
Q

Not representative example

A

Doxil - nanoparticle anticancer drug - effective in mice , humans tumours are low % of body mass - no accumulation

36
Q

FDA

A

manufactring, efficacy, moa, selectivity, ADME, adverse effects

37
Q

Test

A

acute system toxicity, carcinogenicity, gen-toxicity, neurotoxicity, pharmacokinetics, toxicokinetics, immunotoxicity, reproductive toxicity, miscellaneous safety

38
Q

Why rules?

A

keep people and animals safe from harm
detect problems before people are exposed
different protocols depending on potential rule

39
Q

Preclinical testing mRNA vaccines

A

mice for efficacy, rats for toxicity, rhesus monkeys for final animal model (homologous with ACE2 spike protein sequence)
need to kill animal to test organ conc (don’t want in blood or organs other than site, liver, spleen)

40
Q

thalidomide

A

no toxicity shown in animal tests, caused harm to the foetus

41
Q

TOX21

A

high throughput testing and data processing and modelling
toxicology studies that will reduce animal use
-> takes millions and several years to test toxicity

42
Q

QSAR

A

Quantitive Structure Activity Relationship
LogP, pH, molecular weight, surface area, CYP450, etc -> parameter
use standards for machine learning
in silico (computer)

43
Q

Organ on a chip

A

organ cells on plate, circulate drug around
Model key aspects, use human cells, patient specific
cannot model intact organs, doesn’t mimic in vivo, cell sourcing, need different media for different organs

44
Q

Adverse Outcome Pathways (AOP)

A

Determine toxicity via cells - bind to DNA or cell death etc

45
Q

compartment modelling

A

one part or two (organs + blood) use Vd

46
Q

ADMET modelling

A

test ADME properties before in vitro/in vivo

47
Q

good model

A

good input data, training with lots of information

48
Q

privileged structure

A

single molecular framework to create ligands for multiple receptors
(safe to use, pharmacokinetics and bioavailability

49
Q

partition coefficient

A

P- solubility based off polar, charged and neutral functional groups
bioavailability, transport, pharmacodynamics

50
Q

LogP

A

negative = more soluble in water, positive = lipophilic

51
Q

LogP too great

A

decrease solubility in water, decrease dissolution, decrease absorption, increase membrane trapping, decrease bioavailability

52
Q

Lipinski’s rule of five

A 
< 5 H bond donors
< 500 MW
< 5 LogP
< 10 H bond acceptors
> 10 rotatable bonds
53
Q

Pharmocophores

A

areas of molecule hat can be changed to improve efficacy, absorption etc

54
Q

acetylcholine biosynthesis

A

ACh- rapidly hydrolysed in stomach and blood, poor absorption +ly charged, no selectivity
3 pharmacophores - steric hinder hydrolysis and nucleophilic attack

55
Q

Drug development

A

molecular target -> compound screen -> lead compound optimisation -> drug for preclinical evaluation

56
Q

hanges to molecule

A

Shape and size (rings), degree of saturation, functional groups

57
Q

Change shape and size

A

methylene groups, increase hydrophobicity (crossing membranes into bacterial cell)

58
Q

Change ring size and shape

A

non aromatic, changes binding and bond angles

59
Q

Change degrees of unsaturation

A

flexibility, increase metabolism, toxicity, potency

60
Q

functional groups

A

hydroxyl (H bonds, solubility), amine (H bonds, ionisation), ester (drug delivery and prodrugs)

61
Q

hard drug

A

resistant to metabolism (Cl or F = hard handle)

62
Q

soft drug

A

predictable and controlled metabolism

63
Q

Isosteres

A

atoms or groups of atoms with same valency and similar physical properties

64
Q

Change chirality

A

change binding

65
Q

antioxidant

A

compounds that inhibit the chemical reaction that produces reactive oxygen species (ROS).

66
Q

antioxidant testing

A

spectrophotometric assays - Folin assay (FC reagent). phenolic compounds reduce FC reagent, yellow -> blue

67
Q

antimicrobials

A

kill or stop growth of microorganisms (bacteria). MIC and ZOI

68
Q

MIC test

A

minimum concentration to inhibit visible microbial growth

two fold dilutions in wells and inoculated with microbial broth -> incubated

69
Q

skin toxicity

A

crystal violet assay - incubate skin cells with two fold dilution of product -> spectrophotometry -> % viable cells

70
Q

viability assays

A

provide a readout of cell health through measurement of metabolic activity, ATP, content, or cell proliferation

PHAL221 (5 decks)

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