Topic 2: What is a drug? Flashcards
recreation drugs
affect CNS
used for perceived beneficial effects
can cause addiction/habituation
Chemical characterization of drugs
structure, synthesis, purity, pKa
bio characterization
LD50, ED50, receptors
Pharmacology
study of drugs
pharmaco def. of drug
chemical substance used in treatment, cure ,prevention, or diagnosis of disease or used to otherwise enhance mental wellness
Paracelsus
1493-1541
german swiss physician, botanist
gave zinc its name
challenged hippocrates
illness result of outside agents
pioneered use of chemicals in medicine
- sickness and health relied on microcosm and macrocosm
humans must have certain balances of minerals in their bodies
reductive science - compounds need to show efficacy
two main drug targets
GPCR, and protein kinases
use SAR to
increase activity against target
reduce activity to unrelated targets
improve drug-likeness or ADME properties
HTS
commonly used for drug discovery
diffs between natural products and compounds in combinatorial chem libraries
natural compounds have more chiral centres
nat. compounds have higher structural rigidity, and higher non-aromatic unsat.
combinatorial libraries have higher aromatic moieties
O and N enriched in nat. products
S + halogens enriched in synthetic compounds
pre clinical
assessment of major organ toxicity
determine FHD
clinical phase 1
healthy volunteers
determine safety dosing
clinical phase 2
small # sick patients
efficacy
Clinical phase 3
safety and efficacy
confounding factors
placebo re-interpretation (why people use OTC cough syrups) observer bias (affects doctors) selection bias natural course of illness
Food and drug act of 1906
fist of 200 laws
Federal food drug and cometic act (1938)
after elixir killed many people
overhauled Public health system
authorized FDA to demand evidence of safety of new dugs, issue standards for food, and conduct factory inspections
Kefauver Harris Ammendments 1962
inspired by thalidomide
rules, requires proof of drugs effectiveness
medical device amendments (1976)
effectiveness safeguards to new devices
WHO defines traditional medicine
health practices, approaches, knowledge…
how many in Africa use traditional medicine
80%
how many in China use traditional medicine
30-50%
how many in India use traditional medicine
2/3 of pop
how many iwith HIV/AIDS use traditional medicine
75%
