Discovery Of Lead Compounds Drugggs L10 Flashcards
(16 cards)
What is a lead compound?
A chemical compound that has pharmacological or biological activity
It is rarely the actual drug structure that will go to clinical trials or the market, serving instead as a starting point for chemical modifications.
Where do lead compounds come from?
- Natural products*
- Libraries of chemically synthesised compounds*
- High-throughput screening (HTS)*
- Rational drug design*
- Structure-based drug design*
- Modification of endogenous pharmacological agents*
- Me-too drugs*
- Serendipity
These methods represent various approaches to discovering new lead compounds in drug development.
What landmark event occurred in 2700 BC related to lead compounds?
Discovery and documentation of herbal remedies
Shen Nung produced the first known Chinese Pharmacopoeia, which included examples like Ephedra sinica.
Who isolated cocaine from coca leaves and when?
Albert Niemann in 1860
Cocaine became the first local anaesthetic when Karl Köller used it in 1884.
What are the main effects of cocaine?
- Effective anaesthetic*
- Intense vasoconstrictor*
- Narcotic effects*
- Cardiotoxicity*
- Complex structure*
Cocaine has significant pharmacological effects but also poses risks.
What is the origin of morphine?
It is derived from opium, extracted from the opium poppy (P. somniferum)
Morphine has been cultivated since at least 3400 BC.
What are the primary side effects of morphine?
- Respiratory depression*
- Urinary retention*
- Decreased intestinal peristalsis*
- Development of tolerance*
These side effects highlight the risks associated with morphine use.
What is heroin and when was it first synthesized?
A semi-synthetic opioid synthesized by F. Hoffmann in 1897
Heroin is more lipid-soluble than morphine, making it more potent.
What is the mechanism of action for LSD?
Agonist or partial agonist of 5-HT2A receptors
LSD inhibits the screening section of the brain, causing increased sensory input.
What are the effects of psilocybin?
- Altered sensory perception*
- Euphoria*
- Behavioral disturbances*
- Paranoia*
- Visual distortions*
Psilocybin is linked to significant therapeutic effects in mental health treatment.
What are the primary psychoactive constituents of cannabis?
- ∆-9 tetrahydrocannabinol (THC)*
- Cannabinoids*
THC is the main psychoactive component, while other cannabinoids can have varying effects.
What is the difference between THC and CBD?
- THC: psychoactive, CB1R and CB2R partial agonist*
- CBD: non-psychoactive, CB1R negative allosteric modulator*
These differences highlight their distinct pharmacological profiles.
Fill in the blank: The best-known pharmaceutical record from 1550 BC is Eber’s _______.
Papyrus
This document includes 800 prescriptions and mentions 700 drugs.
True or False: Heroin was initially marketed as a non-addictive substitute for morphine.
True
Heroin was widely available for various medical uses before its addictive properties were recognized.
What are the requirements for a cannabis-based product to be considered for medicinal use?
- Contains cannabis or its derivatives*
- Produced for medicinal use in humans*
- Regulated as a medicinal product*
These criteria ensure that only safe and effective products are prescribed.
Who can get a prescription for medical cannabis?
- Adults with chemotherapy-induced vomiting*
- Children and adults with severe epilepsy*
- People with muscle stiffness caused by MS*
Prescriptions are granted on a case-by-case basis following strict guidelines.
