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Intro to Pharm
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Lecture notes of 20 pages for the course PHAR100 at QU (Intro to Pharm)
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Pharm – module 1SECTION 1
History of drug use and development
- Useful drugs were identified over 2000 years ago, majority of clinically useful drugs were
developed over the past 250 years
Historical influences and modern pharmacology
Several key historical influences have shaped modern pharmacology:
- Many discoveries made by ancient civilizations
- Role of poisons in history
- Influence of religion
Ancient civilizations
Ancient Greece:
- In 80 b.c.e, Theophrastus, a pupil of Aristotle, wrote a textbook on therapeutics that
included opium
o Opium’s from the opium poppy (papaver somniferum)
- Serturner, a pharmacist working in Germany in 1803, isolated crystals of morphine from
opium and tested the pure substances himself and three companions, discovering its
pain-relieving capabilities.
- Opium was found to contain two important substances: morphine and codeine
Morphine: opium was found to contain 10% morphine. Serturner coined the name morphine
from Morpheus, god of dreams.
Codeine: opium contains 0.5%. widely used for pain relief and constitute of T3 presrip drug
Ancient Egypt
- History was recorded on documents called papyri. The Ebers Papyrus from the year
1550 b.c.e was intended to be a textbook of drug use for medical students
- This papyrus contains true information on purgatives – which are drugs used to cause
bowel movements.
o One of the drugs recommended for use was senna – products containing senna
are still available today
Ancient China
- Earliest recorded drug experiments are those from China in the year 2700 b.c.e.
emperor Shen Nung classified all drugs according to taste
- The drug Ma Huang was classified as a “medium drugs” – drug is used in Chinese
medicine for coughs, influenza and fevers
- In modern days, ephedrine has been isolated from Ma Huang. Ephedrine has been used
to treat asthma, and a derivative of ephedrine is used as a decongestant
,The influences of poisons
Curare
- A plant-derived drug, was historically used by Indigenous Peoples in various regions of
the Amazon rainforest in South America
Use as poison
- They dipped their arrows in curare to use as a poison for hunting. Curare acted on the
muscles, paralysis and eventually death by respiratory paralysis.
Use as a drug
- Use by Indigenous Peoples inspired allopathic medicine. By giving patients a small dose
of curare, muscles were relaxed which would facilitate the surgeons work.
- Structure of curare has been modified to make the drug safer, and these newer
derivatives of curare are used by anesthetists today.
Ergot
- Poisonous fungus that grows on the heads of rye, particularly during wet seasons.
- In Middle Ages, ergot was grounded together with the rye, thereby finding its way into
bread. As a result, terrible epidemics occurred and 250 years ago one of these
epidemics killed 20,000 people in one region of Russia.
Effects of poisoning
- Effects the nervous, cardiovascular and reproductive systems
- Nervous: once it enters the body, ergot targets the nervous system. This results in
symptoms such as mental frenzy, hallucinations and convulsions
- Cardiovascular: can cause the constriction of blood vessels leading to fingers, toes and
limbs becoming starved of their blood supply, and a resulting burning sensation
o Over time, limbs become black and gradually die, and in extreme cases fall off
- Reproductive: can cause violent contractions of the uterus
o Early as the 16th century, midwives recognized small amounts of ergot could be
useful in hastening labour
o In 1800s, physicians used ergot to expedite lingering labour. *if not used
properly it could result in death.
As a drug
- Ergotamine: useful in the treatment of migraines. One theory suggests that migraines
are caused by pulsation of the arterial blood vessels that carry blood to the head.
Ergotamine constricts these blood vessels, reducing the amplitude of the pulsation
- Ergonovine: once used to hasten birth but not anymore since the force of uterine
contractions may be too strong and the parents may be injured by too rapid delivery.
Now it can be used to arrest uterine bleeding after childbirth.
The influence of Religion
- In ancient societies, traditional healers acted as both physicians and priests, resulting in
therapy being influenced by both religion and magic
- Plants containing intoxicating substances were used by traditional healers in order to
alter the state of consciousness and facilitate communication with their gods
, Peyote
In Mexico, peyote cactus was widely used to achieve a mystical state, which was linked to
spiritual and ritualistic use
- The peyote cactus contains the potent substance mescaline, which causes
hallucinations, a feeling of well-being and distortion of perception similar to that
experienced with LSD
Drug discovery
A drug is any substance received by a biological system that is not received for nutritive
purposes, and which influences the biological function of the organism. This means chemicals,
biological agents and herbal products are all considered drugs
- About 25% of the drugs used today are derived from plant sources, with the active
substances being purified and then potentially modified to be either more effective or
less toxic
- 19th century heralded the era of chemical synthesis and most drugs discovered or
introduced into therapy were small molecules obtained by chemical synthesis in the lab.
Drugs acting on the brain
- drugs that act on the brain alter the normal chemical signalling in the brain
o LSD is an example and it’s one of the most potent hallucinogenic drugs
- Discovery of LSD: Albert Hofmann, who worked for a Swiss pharmaceutical firm, was
involved in trying to synthesize improved pharmaceutical products based on
components of ergot
- in 1943, he synthesized LSD, which was similar in chemical structure to ergotamine and
ergonovine
- Contribution to pharm: the discovery of the psychedelic effects of LSD supported the
idea that certain mental illnesses might be due to the production of potent substances
in the brain that could produce psychic disturbance
- research into therapeutic effects of LSD stopped in 1970s, since it was classified as a
controlled substance. Some evidence shows LSD might be effective in treating
depression, anxiety and addiction
SECTION 2
Drug development process
Five steps: basic research and drug discovery, preclinical trials, Health Canada review and
manufacturing, post-market surveillance and phase IV clinical trials.
Drug discovery:
- basic research + drug discovery
- preclinical trials
- both 3-6 years
Drug development:
- clinical trials have phase 1, 2 and 3
- patients enrolled in study in 10s, 100s, 1000s
- this all takes 6-7 years
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