List of drugs by year of discovery
The following is a table with drugs, organized by their year of discovery.
Naturally occurring chemicals in plants, including alkaloids, have been used since pre-history. In the modern era, plant-based drugs have been isolated, purified and synthesised anew. Synthesis of drugs has led to novel drugs, including those that have not existed before in nature, particularly drugs based on known drugs which have been modified by chemical or biological processes.
- 1 Antiquity
- 2 Post-classical to Early modern
- 3 Modern
- 4 21st Century
- 5 See also
- 6 External links
- 7 References
60th millennium BC
Archaeological evidence indicates that the use of medicinal plants[which?] dates back to the Paleolithic age, these traditions was shared and transmitted by shamans since approximately 60,000 years ago.
4th millennium BC
In ancient Egypt, herbs are mentioned in Egyptian medical papyri, depicted in tomb illustrations, or on rare occasions found in medical jars containing trace amounts of herbs. Medical recipes from 4000 BC were for liquid preparations rather than solids. In 4th millennium BC is named Soma (drink) and Haoma but is not clear what were the ingredients to prepare them.
3rd millennium BC
|Discovery||Name of drug||Active ingredients|
|2,700 BC||Cannabis sativa||Tetrahydrocannabinol (cannabinoid agonist) and cannabidiol (analgesic and anticonvulsant).|
|2,700 BC||Mandragora officinarum||Atropine and scopolamine (antimuscarinics), scopine, cuscohygrine, apoatropine, belladonnines and non-alkaloid constituents including sitosterol and scopoletin.|
|2,700 BC||Rhubarb||Anthraquinones, (e.g. emodin) which are cathartic and laxative. Stilbenoids (e.g. rhaponticin), which may lower blood glucose levels. Flavanol glucosides (e.g. (−)-catechin-7-O-glucoside) which may be cytoprotective.|
2nd millennium BC
Around 1600 BC was written Edwin Smith Papyrus, it describes the use of many herbal drugs, around 1550 BC was written the most important medical papyri of ancient Egypt, the Ebers Papyrus, it covers more than 700 drugs, mainly of plant origin. The first references to pills were found on papyruses in ancient Egypt, and contained bread dough, honey or grease. Medicinal ingredients, such as plant powders or spices, were mixed in and formed by hand to make little balls, or pills. The papyri also describe how to prepare herbal teas, poultices, ointments, eye drops, suppositories, enemas, laxatives, etc. Aloe vera was used in the 2nd millennium BC.
1st millennium BC
In Greece Theophrastus of Eresos wrote in the 4th c. B.C. Historia Plantarum Seeds likely used for herbalism have been found in archaeological sites of Bronze Age China dating from the Shang Dynasty (c. 1600 BC–c. 1046 BC). Over a hundred of the 224 drugs mentioned in the Huangdi Neijing, an early Chinese medical text, are herbs. Herbs also commonly featured in the medicine of ancient India, where the principal treatment for diseases was diet.
Opioids are among the world's oldest known drugs. Use of the opium poppy for medical, recreational, and religious purposes can be traced to the 4th century B.C., when Hippocrates wrote about it for its analgesic properties, stating, "Divinum opus est sedare dolores."
|Year of discovery||Name of the drug||Active ingredients|
|1st millennium BC||Hyoscyamus niger||Tropane alkaloids (e.g. hyoscyamine and scopolamine).|
|600 B.C.||Glycerol, produced||Glycerol|
|300 B.C.||Opium||Phenanthrenes (e.g. morphine, codeine, and thebaine).  Morphine binds to and activates mu opioid receptors and is analgesic. Opium also contains isoquinolines (e.g. papaverine and noscapine).|
1st Century AD
In ancient Greece, pills were known as katapotia ("something to be swallowed"). Pliny the Elder, who lived from 23–79 AD, first gave a name to what we now call pills, calling them pilula., he also wrote Naturalis Historia a collecion of 38 books and the first pharmacopea.
Jojoba was used in the 1st millennium AD.
2nd Century AD
Post-classical to Early modern
6th-11th Century AD
In middle age ointments were a common dosage form.
|Year of discovery||Name of the drug||Active ingredients|
|10th century||Coffee||Caffeine (adenosine receptor antagonist)
Beta carboline (GABAA receptor inverse agonist)
Avicenna separates Medicine and Pharmacy, in 1025 published his book The Canon of Medicine, an encyclopedia of medicine formed by five books. Drugs mentioned by Avicenna include agaric, scammony and euphorbium. The latex of Euphorbia resinifera contains Resiniferatoxin, an ultra potent capsaicin analog. Desensitization to resiniferatoxin is tested in clinical trials to treat neuropathic pain.
|Year of discovery||Name of the drug||Active ingredients|
|Before 1025||Agaric||Muscimol (GABAA receptor agonist), muscarine (muscarinic receptor agonist), ibotenic acid (NMDA receptor agonist)|
|Before 1025||Euphorbium||Resiniferatoxin (capsaicin analog and possible analgesic)|
Paracelsus expounded the concept of dose response in his Third Defense, where he stated that "Solely the dose determines that a thing is not a poison." This was used to defend his use of inorganic substances in medicine as outsiders frequently criticized Paracelsus' chemical agents as too toxic to be used as therapeutic agents. Paracelsus discovered that the alkaloids in opium are far more soluble in alcohol than water. Having experimented with various opium concoctions, Paracelsus came across a specific tincture of opium that was of considerable use in reducing pain. He called this preparation laudanum.
For over a thousand years South American indigenous peoples have chewed Erythroxylon coca leaves, which contain alkaloids such as cocaine. Coca leaf remains have been found with ancient Peruvian mummies. There is also evidence coca leaves were used as an anesthetic. In 1569, Spanish botanist Nicolás Monardes described the indigenous peoples' practice of chewing a mixture of tobacco and coca leaves to induce "great contentment":
|Year of discovery||Name of the drug|
|Before 1569||Erythroxylon coca leaves (containing cocaine)|
In 1778 John Mudge created the first inhaler devices. In 1747, James Lind, surgeon of HMS Salisbury, conducted the first clinical trial ever recorded, on it he study how citrus fruit were capable of cure scurvy.
In 1830's chemist Justus von Liebig begin the synthesis of organic molecules, stating that "The production of all organic substances no longer belongs just to living organisms." In 1832 produced chloral hydrate, the first synthetic sleeping drug. In 1833 French chemist Anselme Payen was the first to discover an enzyme, diastase. In 1834, François Mothes and Joseph Dublanc created a method to produce a single-piece gelatin capsule that was sealed with a drop of gelatin solution. In 1853 Alexander Wood was the first physician that used hypodermic needle to dispense drugs via Injections. In 1858 Dr. M. Sales Giron invented the first pressurized inhaler.
Amphetamine was first synthesized in 1887 in Germany by Romanian chemist Lazăr Edeleanu who named it phenylisopropylamine; its stimulant effects remained unknown until 1927, when it was independently resynthesized by Gordon Alles and reported to have sympathomimetic properties. Shortly after amphetamine, methamphetamine was synthesized from ephedrine in 1893 by Japanese chemist Nagai Nagayoshi. Three decades later, in 1919, methamphetamine hydrochloride was synthesized by pharmacologist Akira Ogata via reduction of ephedrine using red phosphorus and iodine.
|Year of discovery||Name of the drug||Synthesis mechanism||Year that was Patented||Governmental approval||Patented expired|
|1820||Quinine (isolation)||Woodward and Doering||1944|
|1832||Chloral hydrate||Justus von Liebig||1832|
|1875||Phenylhydrazine||Hermann Emil Fischer||1875||1875|
|1877||Paracetamol||Harmon Northrop Morse||1877||1950||2007|
|1880||Phenazone, "the mother of modern Antipyretics"||Ludwig Knorr||1880||1880|
In 1901 Jōkichi Takamine isolated and synthesized the first hormone, Adrenaline. In 1907 Alfred Bertheim synthesized Arsphenamine, the first man-made antibiotic. In 1927 Erik Rotheim patented the first aerosol spray can. In 1933 Robert Pauli Scherer created a method to develop softgels.
William Roberts studies about penicillin were continued by Alexander Fleming, who in 1928 concluded that penicillin had an antibiotic effect. In 1944 Howard Florey and Ernst Boris Chain mass-produced penicilin. In 1948 Raymond P. Ahlquist published his seminal work where divided adrenoceptors into α- and β-adrenoceptor subtypes, this allowed a better understanding of drugs mechanisms of action.
In 1987, after Montreal Protocol, CFC inhalers were phased out and HFA inhalers replace them. In 1987 CRISPR technique was discovered by Yoshizumi Ishino that in the next century would be used for genome editing.
|Year of discovery||Name of the drug||Year when the synthesis mechanism was developed||Year that was Patented||Governmental approval||Patented expired|
|1901||Adrenaline||Jōkichi Takamine, 1901||1901||1901||N/A (Natural Hormone)|
|1906||Oxytocin||Discovered by Henry Hallett Dale, synthesized by Vincent du Vigneaud in 1952||1925||1926||N/A (Natural Hormone)|
|1907||Arsphenamine||Alfred Bertheim, 1907||N/A||N/A||N/A|
|1908||Phenytoin||Heinrich Biltz, 1908||N/A||N/A||N/A|
|1912||Vitamin C||Tadeusz Reichstein, 1933||N/A||N/A||N/A|
|1912||Phenobarbital||Fischer and Mering Synthesis, 1912||1912||1912||1932|
|1915||Thyroxine||Isolated by Edward Calvin Kendall, 1915||1915||1915||N/A (Natural Hormone)|
|1918||Ergotamine||Isolated by Arthur Stoll, Sandoz, 1918||1918||1918||1938|
|1921||Insulin||Frederick Grant Banting, 1921||1921||1921||N/A (Natural Hormone)|
|1927||Levothyroxine||Harington and Barger Synthesis, 1927||N/A||1927||(Synthetic hormone)|
|1928||Penicillin||Alexander Fleming, 1928||1928||1928||Never patented|
|1932||Sulfanilamide||Paul Josef Jakob Gelmo, 1908||N/A||N/A||1938|
|1932||Prontosil||Gerhard Domagk, Josef Klarer and Fritz Mietzsch 1932||N/A||N/A||1938|
|1935||Cortisone||Isolted by Philip Showalter Hench and Edward Calvin Kendall, 1935||1935||1935||N/A (Natural Hormone)|
|1940||Dicoumarol (warfarin)||1940, extracted from Melilotus||1940||1940||1960|
|1943||Lidocaine||Nils Löfgren, 1943||1946||1949||1966|
|1938||Lysergic acid diethylamide (LSD)||Albert Hofmann, Sandoz||1938||1938||1958|
|1955||Chlordiazepoxide||Leo Sternbach, Hoffmann-La Roche, 1955||1955||1955||1975|
|1957||Mepivacaine||A. F. Ekenstam, 1957||1957||1957||1977|
|1958||Triamcinolone acetonide (Nasacort)||1958||1958||1958||1978|
|1960||Fentanyl||Paul Janssen, Janssen Pharmaceutica 1960||1960||1969||1980|
|1961||Mefenamic acid||Claude Winde, Parke-Davis 1961||1961||1969||1981|
|1961||Ibuprofen||Boots Group, 1961||1961||1969||1981|
|1961||Flurbiprofen||Boots Group, 1961||1961||1969||1994|
|1962||Furosemide||Calvin L. Stevens, Parke-Davis 1962||1962||1982|
|1962||Ketamine||Calvin L. Stevens, Parke-Davis 1962||1962||1982|
|1962||Meloxicam||Pfizer 1962||1962||Not for use in humans|
|1962||Beclometasone||David Jack, 1962||1962||1982|
|1963||Diazepam||Leo Sternbach, 1963||1963||1963||1983|
|1963||Flufenamic acid||Parke-Davis, 1963||1963||1965||1983|
|1964||Meclofenamic acid||Parke-Davis, 1963||1963||1965||1983|
|1964||Propranolol||James Black, 1964||1964|
|1964||Clonazepam||Leo Sternbach, 1964||1964||1964||1984|
|1966||Salbutamol (Albuterol)||David Jack, Allen & Hanburys, 1966||1966||1986|
|1970||Ciclosporin||B. Vithal Shetty, 1971||1982|
|1971||Metolazone||B. Vithal Shetty, 1971||1971|
|1971||Cimetidine||James Black, 1971||1971|
|1971||Mupirocin||Isolated in 1971||1971|
|1971||Etidocaine||Isolated in 1971||1971|
|1973||Diclofenac||Synthesized by Alfred Sallmann and Rudolf Pfister in 1973||1973||1993|
|1974||Sulfentanil||Janssen Pharmaceutica, 1974||1994|
|1974||Carfentanil||Janssen Pharmaceutica, 1974||1994|
|1977||Ranitidine||John Bradshaw, Allen & Hanburys, 1977||1981|
|1977||Propofol||John Bradshaw, Allen & Hanburys, 1977||1981|
|1977||Tramadol||Grünenthal GmbH, 1977||1977||1997|
|1985||Salmeterol (Serevent)||David Jack, Allen & Hanburys, 1985||1985||2005|
|1984||Sumatriptan||David Jack, 1984||1984||2006|
|1987||Ondansetron||David Jack, 1987||1990||2006|
|1993||Fluticasone propionate||David Jack, 1993||1993||2004|
|1993||Ketoprofen||James W. Young, William J. Wechter and Nancy M. Gray in 1993||1993||2003|
|1997||Mometasone furoate (Nasonex)||1997||1997||2017|
21st century begins with the first complete sequences of individual human genomes by Human Genome Project, on February 12, 2001, this allowed a switch in drug development and research from the traditional way of drug discovery that was isolating molecules from plants or animals or create new molecules and see if they could be useful in treatment of illness in humans, to pharmacogenomics, that is the study and knowledge of how genes respond to drugs. Another field beneficed by Human Genome Project is pharmacogenetics, that is the study of inherited genetic differences in drug metabolic pathways which can affect individual responses to drugs, both in terms of therapeutic effect as well as adverse effects.
Humane genome study also allowed to identify which genes are responsible of illness, and to develop drugs for rare diseases and also treatment of illness through gene therapy. In 2015 a simplified form of CRISPR edition was used in humans with Cas9, and also was used an even more simple method, CRISPR/Cpf1 that prevent genetic damage from viruses. These advances are improving personalized medicine and allowing precision medicine.
|Year of discovery||Name of the drug||Year when the synthesis mechanism was developed||Year that was Patented||Governmental approval||Patented expiry||Drug type *|
|2007||Sofosbuvir||2007, Raymond F. Schinazi.||N/A||N/A||N/A||SM|
|2014||Umeclidinium bromide (Incruese Ellipta)||2014||2034||SM|
* MA = Monoclonal antibody
SM = Small molecule
ACT = Adoptive cell transfer
- List of drugs
- Lists of molecules
- History of medicine
- List of pharmaceutical laboratories by year of foundation
- Lists of diseases by year of discovery
- Discovery and development of beta2 agonists
- Edwin Smith Papyrus
- De Materia Medica
- Shennong Ben Cao Jing
- The Canon of Medicine
- The Book of Healing
- Nunn, John (2002). Ancient Egyptian Medicine. University of Oklahoma Press. p. 151. ISBN 978-0-8061-3504-5.
- "The Colorful History of Pills Can Fill Many a Tablet". latimes. Archived from the original on 2015-09-19.
- "Cannabidiol". www.drugbank.ca. Retrieved 2019-06-11.
- Cite error: The named reference
mehtawas invoked but never defined (see the help page).
- Chen J, et al. (April 2009). "Rhaponticin from rhubarb rhizomes alleviates liver steatosis and improves blood glucose and lipid profiles in KK/Ay diabetic mice". Planta Med. 75 (5): 472–7. doi:10.1055/s-0029-1185304. PMID 19235684.
- Flavanol glucosides from rhubarb and Rhaphiolepis umbellata. Gen-Ichiro Nonaka, Emiko Ezakia, Katsuya Hayashia and Itsuo Nishioka, Phytochemistry, Volume 22, Issue 7, 1983, Pages 1659–1661, doi:10.1016/0031-9422(83)80105-8
- Atanasov AG, Waltenberger B, Pferschy-Wenzig EM, Linder T, Wawrosch C, Uhrin P, Temml V, Wang L, Schwaiger S, Heiss EH, Rollinger JM, Schuster D, Breuss JM, Bochkov V, Mihovilovic MD, Kopp B, Bauer R, Dirsch VM, Stuppner H (2015). "Discovery and resupply of pharmacologically active plant-derived natural products: A review". Biotechnol. Adv. 33 (8): 1582–614. doi:10.1016/j.biotechadv.2015.08.001. PMC 4748402. PMID 26281720.
- Quattrocchi, Umberto (2012) CRC World Dictionary of Medicinal and Poisonous Plants: Common Names, Scientific Names, Eponyms, Synonyms, and Etymology (5 Volume Set) CRC Press. ISBN 978-1420080445
- Robson, Barry & Baek, O.K. (2009). The Engines of Hippocrates: From the Dawn of Medicine to Medical and Pharmaceutical Informatics. John Wiley & Sons. p. 50. ISBN 9780470289532.
- Hong, Francis (2004). "History of Medicine in China" (PDF). McGill Journal of Medicine. 8 (1): 7984. Archived from the original (PDF) on 2013-12-01.
- Unschuld, Pual (2003). Huang Di Nei Jing: Nature, Knowledge, Imagery in an Ancient Chinese Medical Text. University of California Press. p. 286. ISBN 978-0-520-92849-7.
- Ackerknecht, Erwin (1982). A Short History of Medicine. JHU Press. p. 39. ISBN 978-0-8018-2726-6.
- Manglik, Aashish; Kruse, Andrew C.; Kobilka, Tong Sun; Thian, Foon Sun; Mathiesen, Jesper M.; Sunahara, Roger K.; Pardo, Leonardo; Weis, William I.; Kobilka, Brian K. (2012-03-21). "Crystal structure of the μ-opioid receptor bound to a morphinan antagonist". Nature. 485 (7398): 321–326. Bibcode:2012Natur.485..321M. doi:10.1038/nature10954. ISSN 0028-0836. PMC 3523197. PMID 22437502.
Opium is one of the world’s oldest drugs, and its derivatives morphine and codeine are among the most used clinical drugs to relieve severe pain.
- Kritikos, P. G.; Papadaki, S. P. (1967). "The history of the poppy and of opium and their expansion in antiquity in the eastern Mediterranean area". Bulletin on Narcotics. United Nations Office on Drug Control (3–003): 17–38. Retrieved 2016-06-26.
- Brownstein, M J (1993). "A brief history of opiates, opioid peptides, and opioid receptors". Proceedings of the National Academy of Sciences of the United States of America. 90 (12): 5391–5392. Bibcode:1993PNAS...90.5391B. doi:10.1073/pnas.90.12.5391. ISSN 0027-8424. PMC 46725. PMID 8390660.
It is hard to decide when and where the opium poppy was first cultivated. ... Despite difficulties in interpreting ancient writings and archeological data, a picture of opium use in antiquity does emerge from them. There is general agreement that the Sumerians, who inhabited what is today Iraq, cultivated poppies and isolated opium from their seed capsules at the end of the third millennium B.C.
- Roberts 1998, p. 31
- "Opiates". Homehealth-uk.com. Archived from the original on October 31, 2011. Retrieved October 7, 2011.
- The Classical Tradition. Harvard University Press. 2010. p. 146. ISBN 978-0-674-03572-0.
- Nasser, Mona; Tibi, Aida; Savage-Smith, Emilie (2009-02-01). "Ibn Sina's Canon of Medicine: 11th century rules for assessing the effects of drugs". Journal of the Royal Society of Medicine. 102 (2): 78–80. doi:10.1258/jrsm.2008.08k040. ISSN 0141-0768. PMC 2642865. PMID 19208873.
- Appendino, Giovanni; Szallasi, Arpad (31 January 1997). "Euphorbium: modern research on its active principle, resiniferatoxin, revives an ancient medicine". Life Sciences. 60 (10): 681–696. doi:10.1016/S0024-3205(96)00567-X. PMID 9064473.
- Altman AJ, Albert DM, Fournier GA (1985). "Cocaine's use in ophthalmology: our 100-year heritage". Survey of Ophthalmology. 29 (4): 300–6. doi:10.1016/0039-6257(85)90153-5. PMID 3885453.
- Gay GR, Inaba DS, Sheppard CW, Newmeyer JA (1975). "Cocaine: history, epidemiology, human pharmacology, and treatment. a perspective on a new debut for an old girl". Clinical Toxicology. 8 (2): 149–78. doi:10.3109/15563657508988061. PMID 1097168.
- "Historical overview of methamphetamine". Vermont Department of Health. Government of Vermont. Archived from the original on 5 October 2012. Retrieved 29 January 2012.
- Rassool GH (2009). Alcohol and Drug Misuse: A Handbook for Students and Health Professionals. London, England: Routledge. p. 113. ISBN 9780203871171.
- Sulzer D, Sonders MS, Poulsen NW, Galli A (April 2005). "Mechanisms of neurotransmitter release by amphetamines: a review". Prog. Neurobiol. 75 (6): 406–433. doi:10.1016/j.pneurobio.2005.04.003. PMID 15955613.
- Grobler SR, Chikte U, Westraat J (2011). "The pH Levels of Different Methamphetamine Drug Samples on the Street Market in Cape Town". ISRN Dentistry. 2011: 1–4. doi:10.5402/2011/974768. PMC 3189445. PMID 21991491.
- "Historical overview of methamphetamine". Vermont Department of Health. Retrieved 15 January 2012.
- Courtwright, David T. (2009). Forces of habit drugs and the making of the modern world (1 ed.). Cambridge, Mass.: Harvard University Press. pp. 36–37. ISBN 978-0-674-02990-3. Archived from the original on 8 September 2017.
- Gates M, Tschudi G (April 1956). "The Synthesis of Morphine". Journal of the American Chemical Society. 78 (7): 1380–1393. doi:10.1021/ja01588a033.
- Klotz, U. (2007). "The role of pharmacogenetics in the metabolism of antiepileptic drugs: pharmacokinetic and therapeutic implications". Clin Pharmacokinet. 46 (4): 271–9. doi:10.2165/00003088-200746040-00001. PMID 17375979.
- "Sofosbuvir (Sovaldi) – Treatment – Hepatitis C Online". www.hepatitisc.uw.edu. Archived from the original on 23 December 2016. Retrieved 8 January 2017.
- Gounder, Celine (9 December 2013). "A Better Treatment for Hepatitis C". The New Yorker. Archived from the original on 20 September 2016.