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Cheatography

PHAR1101-2 Cheat Sheet (DRAFT) by

This is a draft cheat sheet. It is a work in progress and is not finished yet.

Defini­tions

Synthetic Drug
A drug of human origin. Made in a lanratory rather than being extracted from a plant or other ecological source
Medicinal Chemistry
Branch of chemistry that is concerned with design, develo­pment and synthesis of pharma­ceu­tical agents or medicines. Medicinal chemists find the relati­onship between the structure of a drug an its pharma­col­ogical or toxico­logical properties
Animal Model
A living, non-human species that is affected by a specific disease. Which is usually of relevance of human pathology. These animal models are used during the testing of new and unproven treatments for the diseases without initially involving actual humans suffering from the disease
Pathogen
An infectious agent that causes disease or illness in a host.
Pathon­genesis
The develo­pment of a disease and the chain of cellular and tissue events leading to the manife­station of the disease in people.

Human Safety Concerns

A drug that is safe for animal isn't always safe for humans
Only 70% of drugs that are toxic on animals are toxic in humans
Some animal organ model are inaccurate (i.e skin brain and liver models)
Some toxic effects are hard to detect in animal models (hearing loss)
Each animal has a different metabo­lising speed

Classic Animal Models

Zucker Diabetic Rat and SHR Rat assisted in the search of drugs for cardio­vas­cular and metabolic diseases

German Pharma­ceu­tical Industry / Coal

The widespread use of coal led to a vast quantity of coal tar. coal tar is rich with small organic molecules which can be used to build more complex ones. Germany dominated in creating synthetic drugs for several reasons

A) Establ­ishment of in house research labs

B) Creation of partne­rships between resear­chers and academic

C) Creation of partne­rships between university depart­ments and research students
 

Examples of Animal Models

Chloral Hydrate (1869)
By: Oscar Liebreich
Use: Sleep Inducing
Tested: Rabbits
Barbitone
(1903)
By: Emily Fischer
Use: Hypnotic Effect
Tested: Dogs
Prontosil
(1935)
By: Gerhard Domagk
Use: Strept­ococcus
Tested: Mice
Phenytoin
(1936)
By: Tracey Putnam
Use: Antico­nvu­lsant
Tested: Cats
Diphen­hyd­ramine (1943)
By: Daniel Bovet
Use: Antihi­stamine
Tested: Guinea Pigs
Librium
(1957)
By: Leo Sternbach
Use: Tranqu­iliser
Tested: Mice, Cats, Dogs, Monkeys
Ibuprofen
(1969)
By: Stewart Adams
Use: Anti-i­nfl­amm­atory
Tested: Rabbits
Omeprazole
(1979)
By: Astra
Use: Heartburn
Tested: Rats, Dogs

Disease Relevance Issues

Animal Models can never be truly precise and indicative of human disease
Drugs that work on Animal Models don't always work on Humans
Some diseases are too complex to reproduce in animals

Paul Ehrlich

Father of Chemot­herapy
Born in Silesia
Worked with synthetic dies
Noted that some dyes entered certain tissues but not others
Led to the theory that chemicals can be designed to select­ively enter certain tissues
"­magic bullet theory­"
 

Stages of Syphilis

Infection
Bacteria T.Pallidum enters host
First stage
Firm and painless skin lesions at site of infection.
Second Stage
Skin rash, Swollen lymph nodes, Sore throat, Pathy hair loss, headaches, Weight loss, Muscle aches
Latent
Symptoms may subside for months or years
Final Stage
Deteri­oration of cardio­vas­cular system. May result in dementia or blindness

Ethical Concerns

Refinement
Minimise suffering to individual animal's experience
Reduction
Only use as many animals as needed
Reduce number of tests
test multiple things at once
Replac­ement
Find alternate testing Methods

Disease Model Testing

Compound Libraries
A large set of struct­urally similar molecules
by testing each one we can identify related molecules with similar properties
Animal Models
A safe way to identify promising drugs
used to screen compound libraries
Trained Invest­igators
Impartial unbiased scient­ifi­cally trained observers
Disease Biomarkers
A measurable indicator of a disease
used for diagnostic purposes
There is no 100% safe way to test a drug

Compound 606

Dr hata tested a compound library on rabbits. The 606th compound was effective. Named arsphe­namine or salvarsan
It was hard to dissolve in water and was unstable. it had to be prepare onsite and injection was painful. 25-30 injections were needed.