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Flashcards in Topic 1 Deck (17):

Timeline of drug sourcing

1) Morphine was isolated in 1805 = first drug to be purified from a natural product, still derived from opium poppies
2) Chloral hydrate discovered in 1832 = not used as a drug until 1869, first synthetic drug
3) Aspirin discovered in 1897 = semisynthetic (modified version of natural product), first blockbuster drug
4) Recombinant human insulin produced in 1978 = first drug produces from genetically engineered bacteria, diabetics had been using insulin from pigs and cows


When was the fact that herbal extracts contain active compounds considered

18th century (this coincided with the development of chemical methods that allowed the purification and identification of the constituents of plant extracts).


What lead to the rise of experimental pharmacology

During the 1800s there was a growing trend in the West of deliberate testing of the individual compounds purified from plant and animal extracts


What did the development of experimental methods allow

The development of experimental methods made it possible to evaluate these compounds by studying and measuring their effects on living organisms


Chemical synthesis of drugs

purification and identification of the constituents of the plants and animal extracts


he active compounds in plants and other natural sources are categorised how

on the basis of their chemical properties


The two types of chemicals that are commonly encountered in natural sources are

alkaloids and glycosides



nitrogen containing alkaline compounds, usually bitter tasting and include drugs such as morphine, cocaine, nicotine and caffeine


Alkaline compounds

compounds that react with acids to form salts



a type of carbohydrate that is metabolised to sugar and various active substances and include the drug digoxin, obtained from Foxglove and used to treat heart failure.


Other types of chemicals in natural sources

hydrocarbons (e.g. castor oil), steroids (such as oestrogen compounds) and oils (such as menthol)



organic compounds containing carbon and hydrogen



natural oils


When purified from a natural source do the active constituents generally retain their pharmacological activity?

yes, when purified from a natural source the active constituents generally retain their pharmacological activity.


Why is it possible to manufacture drugs directly without having to rely on the natural source

With the identification of the chemical structures of many drugs


What does chemical modifications of the original natural compound do

yields drugs with increased potency, specificity and selectivity making it possible to improve the beneficial effects and reducing side effects.


Example of natural source of drug modified

Aspirin - derivative of salicin, a glycoside found in the bark of a hollo tree. Usually causes known to cause severe irritation of the stomach but now slight modification of its chemical structure yielded acetylsalicylic acid, otherwise known as aspirin that was slightly less irritating to the stomach. Adding the acetyl group to the salicylic acid to create aspirin makes the molecule less acidic and thus easier on the lining of the digestive tract but still effective at relieving pain