Drugs and Their Historical Significance

What is a Drug?

• A drug is a substance with medicinal, intoxicating, performance-enhancing, or other effects when taken into a human body.
• It is not considered food.
• In pharmacology, a drug is a chemical substance used for treatment, cure, prevention, or diagnosis of disease.
• It can also be used to promote physical or mental well-being.
• Recreational drugs affect the central nervous system (CNS), such as opioids and hallucinogens.
• They may be used for perceived benefits on perception, consciousness, personality, and behavior.
• Some drugs can cause addiction and/or habituation.

Selected Drugs from Early Recorded History

• China had documented drug treatment as early as 3000 BCE.
• Ma Huang (Ephedra vulgaris) was used to treat coughs.
• The active component is ephedrine.
• Pseudoephedrine (Sudafed) is a diastereomer of ephedrine used as a decongestant.

Chemical Structures of MDMA and Related Compounds

• Structures of amphetamine, methamphetamine, 3,4-methylenedioxyamphetamine (MDA), and 3,4-methylenedioxymethamphetamine (MDMA) are shown with chemical formulas. This slide provides the chemical structure for these important compounds.

Thalidomide Enantiomers

• The various chemical structures for the isomers, R, and S, of thalidomide is presented.

Physical Harm and Dependence of Various Drugs

• The graph displays the active/lethal dose ratio and dependence potential of various psychoactive drugs.
• Drugs are categorized by their dependence potential (low, moderate, or high) and active/lethal dose ratio (very high, high, medium, moderate/low, or very low).

Middle Ages to Modern Times (6 of 6)

• Thalidomide was developed in 1957 to treat morning sickness in the first trimester of pregnancy.
• Thalidomide caused birth defects in approximately 10,000 children worldwide from 1960-1961, including 115 in Canada.
• Thalidomide wasn't tested on pregnant animals.
• It's a racemic mixture, with the (R) enantiomer being effective against morning sickness, but the (S) isomer being teratogenic.

Middle Ages to Modern Times (1 of 6)

• Caffeine is found in coffee (Coffea arabica) and is a stimulant and a diuretic.
• Introduced to Europe through Constantinople (modern Istanbul) in the 1500s.
• Theobromine is found in cacao seeds (Theobroma cacao).

Middle Ages to Modern Times (2 of 6)

• Arsenic anti-infectives are organic compounds with at least one arsenic atom.
• Arsenic trioxide (As2O3) was used to treat trypanosomes in the 1800s.
• Examples include sleeping sickness (Trypanosoma brucei), Chagas disease (Trypanosoma cruzi), and leishmaniasis (various species of Leishmania) have been treated with arsenicals such as arsanilate, or atoxyl and arsphenamine (“606”).

Middle Ages to Modern Times (3 of 6)

• Sulfonamides (Sulfa drugs) were the first antimicrobial drugs.
• They are synthetic agents containing a sulfonamide group.
• They are competitive inhibitors of dihydropteroate synthetase (DHPS), an enzyme important in folate synthesis.
• They are bacteriostatic (inhibit bacterial growth) but do not directly kill bacteria.

Middle Ages to Modern Times (4 of 6)

• Sulfa drug history began at Bayer AG, a German chemical trust.
• The belief was that coal-tar dyes bound preferentially to bacteria and parasites.
• In 1932, researcher Gerhard Domagk identified a red dye that stopped some bacterial infections in mice.
• Prontosil, named by Bayer, became the first effective compound to treat bacterial infections in the body.

Middle Ages to Modern Times (5 of 6)

• Prontosil is a prodrug (inert until metabolised).
• It becomes active against bacteria in the body.
• The "Elixir Sulfanilamide" disaster involved a formulation that led to widespread deaths.

Thalidomide Update (2012)

• Thalidomide maker apologized 50 years after the drug was pulled from the market.
• The company paid roughly 500 million Euros to victims.
• Canadian Thalidomide survivor Paul Murphy called the apology a joke.

Thalidomide Update (Jan 2015)

• Canadian thalidomide survivors expect an offer this month.
• The Conservative government backed an NDP motion to support victims of thalidomide.
• Victims battle the lingering effects of the drug.
• Survivors hope for $250,000 lump sum compensation and $75,000-$150,000 annual payments contingent on disability levels.

Thalidomide Update (May 2015)

• Survivors cheered a new annual pension program.
• Federal government will provide aid from $75,000-$100,000 per year.

Thalidomide Update (August 2015)

• Frances Oldham Kelsey averted a thalidomide tragedy by refusing to rush approval of the drug.
• She worked as a drug reviewer for the FDA.
• She received an award for her work.
• She passed away at the age of 101.

Thalidomide in Modern Medicine (1 of 2)

• Thalidomide was used to treat leprosy in 1964 (Jacob Sheskin).
• Brazilian doctors prescribe this drug, since 1965, for severe ENL (Erythema nodosum leprosum).
• Women using thalidomide are required to use two forms of birth control and undergo regular pregnancy tests.
• The FDA approved thalidomide's use in ENL (1998).
• The WHO doesn't recommend thalidomide due to control and use difficulty.

Thalidomide in Modern Medicine (2 of 2)

• Judah Folkman's research on angiogenesis plays a key role in cancer research.
• Angiogenesis is essential for tumor growth.
• Thalidomide has shown efficacy in treating multiple myeloma, often in combination with other medications.
• In 2006, the FDA approved a combination of thalidomide and dexamethasone for newly diagnosed multiple myeloma patients.

Cocaine Toothache Drops

• A vintage advertisement for cocaine toothache drops is displayed.
• The LLOYD MANUFACTURING CO. produced these drops.

Bayer Heroin Hydrochloride

• A vintage advertisement for a Bayer heroin product (heroin/hydrochloride) is shown.

Mrs. Winslow's Soothing Syrup

• A vintage advertisement for a Mrs. Winslow's Soothing Syrup is shown..

Cigarettes (Nicotine)

• Vintage cigarette advertisements from the past are demonstrated.

Cocarettes (Coca and Nicotine)

• Vintage cocarette advertisements are displayed.

Middle Ages and Modern Times

• Historical usage and development of various drugs and formulations.

This quiz explores the definition of drugs, their medicinal and recreational uses, and historical applications of selected drugs. It delves into pharmacological substances, their effects on the human body, and notable compounds like ephedrine and MDMA.