Podcast
Questions and Answers
Which infectious disease has the highest case fatality rate?
Which infectious disease has the highest case fatality rate?
In 2023, what percentage of global malaria deaths occurred in the WHO African Region?
In 2023, what percentage of global malaria deaths occurred in the WHO African Region?
What is the primary method of transmission for malaria?
What is the primary method of transmission for malaria?
What is the genus of the plant that produces the medicinally active bark containing quinine?
What is the genus of the plant that produces the medicinally active bark containing quinine?
Signup and view all the answers
Besides quinine, what other alkaloid is found in the bark of the Cinchona tree?
Besides quinine, what other alkaloid is found in the bark of the Cinchona tree?
Signup and view all the answers
Which of these diseases is responsible for the most deaths historically across the world?
Which of these diseases is responsible for the most deaths historically across the world?
Signup and view all the answers
According to the information, what was the significance of the countess of Chinchón?
According to the information, what was the significance of the countess of Chinchón?
Signup and view all the answers
What concept was conceived of by Dr. Samuel Hahnemann after experimenting with Cinchona bark?
What concept was conceived of by Dr. Samuel Hahnemann after experimenting with Cinchona bark?
Signup and view all the answers
What is the believed cause of Hahnemann's symptoms?
What is the believed cause of Hahnemann's symptoms?
Signup and view all the answers
Who was awarded the Nobel Prize for discovering the motile parasite associated with malaria?
Who was awarded the Nobel Prize for discovering the motile parasite associated with malaria?
Signup and view all the answers
Which of the following is NOT a known property of quinine?
Which of the following is NOT a known property of quinine?
Signup and view all the answers
Who first isolated quinine from the cinchona tree?
Who first isolated quinine from the cinchona tree?
Signup and view all the answers
What did William Henry Perkin attempt to use to synthesize quinine?
What did William Henry Perkin attempt to use to synthesize quinine?
Signup and view all the answers
In 1918, what did Rabe and Kindler synthesize quinine from?
In 1918, what did Rabe and Kindler synthesize quinine from?
Signup and view all the answers
What is the primary method by which paracetamol reduces fever and pain?
What is the primary method by which paracetamol reduces fever and pain?
Signup and view all the answers
Which of the following is NOT a direct mechanism of paracetamol's action as described in the text?
Which of the following is NOT a direct mechanism of paracetamol's action as described in the text?
Signup and view all the answers
What is the role of acetylcysteine in the treatment of paracetamol overdose?
What is the role of acetylcysteine in the treatment of paracetamol overdose?
Signup and view all the answers
Which of the following enzyme systems is primarily responsible for metabolizing paracetamol?
Which of the following enzyme systems is primarily responsible for metabolizing paracetamol?
Signup and view all the answers
What is the toxic metabolite produced during the metabolism of paracetamol, and how it is normally detoxified?
What is the toxic metabolite produced during the metabolism of paracetamol, and how it is normally detoxified?
Signup and view all the answers
Which of the following regarding paracetamol synthesis is NOT correct?
Which of the following regarding paracetamol synthesis is NOT correct?
Signup and view all the answers
Which of the following is a minor metabolite of paracetamol?
Which of the following is a minor metabolite of paracetamol?
Signup and view all the answers
What is a potential symptom of an untreated paracetamol overdose?
What is a potential symptom of an untreated paracetamol overdose?
Signup and view all the answers
Which research finding prompted further investigation into the synthesis of quinine?
Which research finding prompted further investigation into the synthesis of quinine?
Signup and view all the answers
The synthesis of racemic vinylic gamma-lactones by Kondo and Mori in 1974 was significant because it:
The synthesis of racemic vinylic gamma-lactones by Kondo and Mori in 1974 was significant because it:
Signup and view all the answers
Which of these correctly states the conclusions of Seeman in the 36-page review?
Which of these correctly states the conclusions of Seeman in the 36-page review?
Signup and view all the answers
Which compound was found to cause methaemoglobinemia as a serious side effect?
Which compound was found to cause methaemoglobinemia as a serious side effect?
Signup and view all the answers
Which of the following is NOT a proprietary name for paracetamol?
Which of the following is NOT a proprietary name for paracetamol?
Signup and view all the answers
The different names for paracetamol such as 'N-acetyl-para-aminophenol', 'acetaminophen', and 'paracetamol' are primarily due to:
The different names for paracetamol such as 'N-acetyl-para-aminophenol', 'acetaminophen', and 'paracetamol' are primarily due to:
Signup and view all the answers
What was the primary contribution made by Julius Axelrod and Bernard Brodie in 1948?
What was the primary contribution made by Julius Axelrod and Bernard Brodie in 1948?
Signup and view all the answers
What was the importance of the work of Ishibashi & Taniguchy in 1988?
What was the importance of the work of Ishibashi & Taniguchy in 1988?
Signup and view all the answers
Study Notes
Medicinal Chemistry Introduction
- CH456 Medicinal Chemistry course, 2025, by James H. Gerlach
The Five Deadliest Infectious Diseases
- Rabies: essentially 100% case fatality rate
- Ebola hemorrhagic fever: 83% case fatality rate
- Marburg hemorrhagic fever: 80% case fatality rate
- H5N1 avian influenza: ~60% case fatality rate
- Nipah virus: 40% to 70% case fatality rate
Share of Total Disease Burden by Cause, World 2021
- Measured in Disability-Adjusted Life Years (DALYs)
- DALYs account for both years of life lost and years lived with disability
- One DALY equals one lost year of healthy life
- Cardiovascular diseases account for a significant portion of the total burden
Share of Total Disease Burden by Cause, Canada 2021
- Cardiovascular diseases, cancers, and musculoskeletal disorders are major contributors to the total burden of disease
Disease Burden from Communicable, Maternal, Neonatal and Nutritional Diseases, World
- Estimated disease burden in Disability-Adjusted Life Years (DALYs) per year.
- Data shows trends over time, with different diseases contributing more or less over the years
Disease Burden from Communicable, Maternal, Neonatal and Nutritional Diseases, Canada
- Estimated disease burden in Disability-Adjusted Life Years (DALYs) per year.
- Shows trends over time, with different diseases contributing differently over the years
Deaths from Infectious Diseases, 1980 to 2021, World
- Estimated annual death toll from HIV/AIDS, diarrhea, malaria, respiratory, and other infectious diseases.
- Overall trend is downward since 1980
Deaths from Infectious Diseases, 1980 to 2021, Canada
- Estimated annual death toll from HIV/AIDS, diarrhea, malaria, respiratory, and other infectious diseases.
- Overall trend is upward since 1980
Global Trends in Estimated Number of TB Deaths and Mortality Rate, 2000-2020
- Data presented in a graphical format showing trends in TB deaths and mortality rates.
- Includes total TB, HIV-negative, and HIV-positive breakdowns.
The Deadliest and Most Communicable Diseases
- Chart visualising various diseases based on case fatality rate and basic reproduction number (Ro)
- Infectious diseases are categorized based on primary transmission method and their mortality rate
Malaria is the Disease Responsible Historically for the Most Worldwide Deaths
- Malaria is a life-threatening disease caused by parasites.
- Transmission occurs through infected female Anopheles mosquitoes.
- Preventable and curable, with estimated 263 million cases and 597,000 deaths in 2023.
- WHO African Region carries a disproportionate share of the global malaria burden.
- Children under 5 are significantly affected (76% of deaths in the Region in 2023).
Countries with Indigenous Cases of Malaria in 2000 and Their Status by 2023
- Detailed map visualization of malaria cases in different countries
Quinine
- Cinchona bark contains quinine (anti-malarial) and quinidine (anti-arrhythmic) alkaloids.
- The first European cured of malaria fever, possibly, was the wife of the Spanish Viceroy of Peru.
- In 1753, the Peruvian bark was named Cinchona after the countess.
Homeopathy and Cinchona
- Homeopathy's origins are connected to Cinchona bark testing.
- Samuel Hahnemann, founder of homeopathy, felt symptoms from an overdose of Peruvian bark.
Discovery of the Malaria Parasite
- Alphonse Laveran, a French military doctor, discovered a motile parasite in infected patients' blood in Algeria in 1878.
- He was awarded a Nobel Prize in 1907.
Quinine Properties
- Natural white crystalline alkaloid
- Antimalarial, analgesic, antipyretic and anti-inflammatory properties
- Bitter taste, used in gin and tonic
Quinine Total Synthesis
- Hundreds of years of efforts to synthesize quinine.
- Various chemists and researchers discovered methods and processes to isolate and synthesize quinine over time
Woodward-Doering Quinine Synthesis
- Detailed account of different chemist's approaches to achieve quinine total synthesis.
- Discussion on experimental challenges
Stork Stereoselective Quinine Synthesis
- Different steps involved in achieving synthesis
Related Antimalarial Drugs
- Chloroquine (1934) and Amodiaquine (1948) are related antimalarial drugs.
- Chemical structures are presented and years of development are noted
Paracetamol (Acetaminophen)
- IUPAC name: N-(4-hydroxyphenyl)-acetamide
- Other chemical names: N-acetyl-para-aminophenol, APAP, para-acetamidophenol
- International Nonproprietary Name (INN): Paracetamol
What's the origin of these names?
- Different names for paracetamol are presented and details on their origins
Julius Axelrod and Bernard Brodie Demonstrated Acetanilide is Metabolized to Paracetamol in 1948
- Acetanilide, initially used for pain and fever.
- Methaemoglobinemia, formed by this drug was a serious side effect, leading to liver and kidney damage.
- Later research demonstrated that the body metabolized acetanilide to paracetamol.
Paracetamol Total Synthesis
- Detailed description of steps in synthesizing paracetamol
- Starting materials and chemical reactions
Paracetamol Mechanism of Action
- Paracetamol acts via cyclooxygenase (COX) pathways and inhibits COX-3 enzyme.
- Metabolised to AM404 and this may impact pain receptors.
Paracetamol Metabolism
- Metabolised primarily through the liver.
- Major metabolites are inactive and excreted in the urine.
- NAPQI is a toxic metabolite and can damage the liver if not quickly detoxified.
Reactions Involved in Paracetamol Metabolism
- Paracetamol is metabolized through reactions like glucuronidation and sulfation reactions.
NAPQI Toxicity
- The toxic metabolite causing liver injury in paracetamol overdose.
- Involved in covalent binding with proteins and nucleic acids.
- Causes cellular and organism responses, leading to necrosis and liver injury.
Treating Paracetamol Overdoses
- Toxic doses range from 4–15g.
- Treatment includes administering acetylcysteine within 8 hours to replenish liver glutathione.
- Without treatment, liver failure can occur.
Studying That Suits You
Use AI to generate personalized quizzes and flashcards to suit your learning preferences.
Related Documents
Description
Test your knowledge on the critical aspects of malaria, its transmission, and the medicinal history of quinine. This quiz explores historical facts, significant figures, and the properties of quinine related to malaria treatment. Challenge yourself and learn more about infectious diseases and their impact.