The following is a table of 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.
Antiquity
editPrehistory
editArchaeological evidence indicates that the use of medicinal plants dates back to the Paleolithic age.[citation needed]
4th millennium BCE
editIn 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.[1] Medical recipes from 4000 BCE were for liquid preparations rather than solids.[2] In the 4th millennium BCE, Soma (drink) and Haoma are named, but is not clear what ingredients were used to prepare them.[citation needed]
3rd millennium BCE
editDiscovery | Name of drug | Active ingredients |
---|---|---|
2,700 BCE | Cannabis sativa | Cannabinoids, (e.g. tetrahydrocannabinol, a cannabinoid agonist, and cannabidiol, an analgesic and anticonvulsant).[3] |
2,700 BCE | Mandragora officinarum | Atropine and scopolamine (antimuscarinics), scopine, cuscohygrine, apoatropine, Belladonnines and non-alkaloid constituents including sitosterol and scopoletin.[citation needed] |
2,700 BCE | Rhubarb | Anthraquinones, (e.g. emodin)[4] which are cathartic and laxative. Stilbenoids (e.g. rhaponticin), which may lower blood glucose levels.[5] Flavanol glucosides (e.g. (−)-catechin-7-O-glucoside) which may be cytoprotective.[6] |
2nd millennium BCE
editWritten around 1600 BCE, the Edwin Smith Papyrus describes the use of many herbal drugs. The Ebers Papyrus – one of the most important medical papyri of ancient Egypt – was written around 1550 BCE, and covers more than 700 drugs, mainly of plant origin.[7] The first references to pills were found on papyri 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.[2] 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 BCE.[8]
1st millennium BCE
editIn Greece, Theophrastus of Eresos wrote Historia Plantarum in the 4th century BCE.[9] Seeds likely used for herbalism have been found in archaeological sites of Bronze Age China dating from the Shang dynasty[10] (c. 1600 BCE–c. 1046 BCE). Over a hundred of the 224 drugs mentioned in the Huangdi Neijing – an early Chinese medical text – are herbs.[11] Herbs also commonly featured in the medicine of ancient India, where the principal treatment for diseases was diet.[12]
Opioids are among the world's oldest known drugs.[13][14] Use of the opium poppy for medical, recreational, and religious purposes can be traced to the 4th century BCE, when Hippocrates wrote about it for its analgesic properties, stating, "Divinum opus est sedare dolores." ("Divine work is the easing of pain")[15]
Year of discovery | Name of the drug | Active ingredients |
---|---|---|
1st millennium BC | Hyoscyamus niger | Tropane alkaloids (e.g. hyoscyamine and scopolamine).[16] |
600 B.C. | Glycerol, produced | Glycerol[citation needed] |
300 B.C. | Opium | Phenanthrenes (e.g. morphine, codeine, and thebaine).[17] Morphine binds to and activates Mu opioid receptors and is analgesic. Opium also contains isoquinolines (e.g. papaverine and noscapine). |
1st century CE
editIn ancient Greece, pills were known as katapotia ("something to be swallowed"). Pliny the Elder, who lived from 23–79 CE, first gave a name to what we now call pills, calling them pilula.[2] Pliny also wrote Naturalis Historia a collection of 38 books and the first pharmacopoea.
Pedanius Dioscorides wrote De Materia Medica (c. 40 – 90 CE); this book dominated the area of drug knowledge for some 1500 years until the 1600s.[18]
Jojoba was used in the 1st millennium CE.
2nd century CE
editAelius Galenus wrote more than 11 books about drugs, also use terra sigillata with kaolinite and goats blood to produce tablets.
Post-classical to Early modern
editDrugs developed in the post-classical (circa 500 to 1450) or early modern eras (circa 1453 to 1789).
6th–11th century CE
editIn middle age ointments were a common dosage form.
Year of discovery | Name of the drug | Active ingredients |
---|---|---|
10th century | Coffee | Caffeine (adenosine receptor antagonist)[citation needed]
Beta carboline (GABAA receptor inverse agonist)[citation needed] |
11th century CE
editAvicenna 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.[19] The latex of Euphorbia resinifera contains resiniferatoxin, an ultra potent capsaicin analog. Desensitization to resiniferatoxin is tested in clinical trials to treat neuropathic pain.[20]
Year of discovery | Name of the drug | Active ingredients |
---|---|---|
Before 1025 | Agaric | Muscimol (GABAA receptor agonist), muscarine (muscarinic receptor agonist), and ibotenic acid (NMDA receptor agonist)[citation needed] |
Before 1025 | Scammony | Scammonin
(In general, a powerful purgative and anthelmintic)[citation needed] |
Before 1025 | Euphorbium | Resiniferatoxin (capsaicin analog and possible analgesic)[citation needed] |
16th century CE
editParacelsus 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.[citation needed]
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.[21] There is also evidence coca leaves were used as an anesthetic.[22] In 1569, Spanish botanist Nicolás Monardes described the indigenous peoples' practice of chewing a mixture of tobacco and coca leaves to induce "great contentment".[citation needed]
1400s Nicotine (Tobacco)[citation needed]
Year of discovery | Name of the drug |
---|---|
Before 1569 | Erythroxylon coca leaves (containing cocaine)[citation needed] |
16th century | Laudanum[citation needed] |
18th century CE
editIn 1778 John Mudge created the first inhaler devices.[citation needed] In 1747, James Lind, surgeon of HMS Salisbury, conducted the first clinical trial ever recorded, on it he studied how citrus fruit were capable of curing scurvy.[citation needed]
Modern
edit19th century CE
editIn the 1830s chemist Justus von Liebig began 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;[23][24][25] its stimulant effects remained unknown until 1927, when it was independently resynthesized by Gordon Alles and reported to have sympathomimetic properties.[25] Shortly after amphetamine, methamphetamine was synthesized from ephedrine in 1893 by Japanese chemist Nagai Nagayoshi.[26] Three decades later, in 1919, methamphetamine hydrochloride was synthesized by pharmacologist Akira Ogata via reduction of ephedrine using red phosphorus and iodine.[27]
Year of discovery | Name of the drug | Synthesis mechanism | Year that was Patented | Governmental approval | Patented expired | |
---|---|---|---|---|---|---|
Synthesis discoverer | Year | |||||
1803–1805[28] | Morphine | Gates synthesis[29] | 1952 | |||
1820 | Quinine (isolation) | Woodward and Doering | 1944 | |||
1830s | Santonin | |||||
1832 | Chloral hydrate | Justus von Liebig | 1832 | |||
1833 | Diastase | |||||
1853 | Acetylsalicylic acid (Aspirin) | 1899 | ||||
1875 | Phenylhydrazine | Hermann Emil Fischer | 1875 | 1875 | ||
1877 | Paracetamol | Harmon Northrop Morse | 1877 | 1950 | 2007 | |
1877 | Mannitol | Julije Domac | 1877 | 1950 | ||
1880 | Phenazone, "the mother of modern Antipyretics" | Ludwig Knorr | 1880 | 1880 | ||
1885 | Ephedrine | Nagai Nagayoshi | 1885 | 1885 | ||
1890 | Benzocaine | August Bischler | 1895 | 1895 | ||
1895 | Quinazoline | August Bischler | 1895 | 1895 | ||
1887 | Amphetamine | Lazăr Edeleanu | 1887 | |||
1893 | Methamphetamine | Nagai Nagayoshi | 1893 |
20th century CE
editIn 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 penicillin. 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 |
1920 | Metamizole | 1920 | N/A | N/A | N/A |
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 | Isolated by Philip Showalter Hench and Edward Calvin Kendall, 1935 | 1935 | 1935 | N/A (Natural Hormone) |
1935 | Tetracaine | 1935 | 1935 | 1935 | 1955 |
1935 | Methylphenobarbital | 1935 | 1935 | 1935 | 1955 |
1935 | Dapsone | 1935 | 1935 | 1935 | 1955 |
1940 | Dicoumarol (warfarin) | 1940, extracted from Melilotus | 1940 | 1940 | 1960 |
1946 | Isosorbide | 1946 | 1946 | 1946 | 1966 |
1943 | Lidocaine | Nils Löfgren, 1943 | 1946 | 1949 | 1966 |
1938 | Lysergic acid diethylamide (LSD) | Albert Hofmann, Sandoz | 1938 | 1938 | 1958 |
1951 | Hydrocortisone | 1951 | 1951 | 1951 | 1971 |
1951 | Imipramine | 1951 | 1951 | 1957 | 1971 |
1952 | Acetazolamide | 1952 | 1952 | 1952 | 1972 |
1954 | Fludrocortisone acetate | 1954 | 1954 | 1954 | 1974 |
1955 | Prednisolone | 1955 | 1955 | 1955 | 1975 |
1955 | Prednisone | 1955 | 1955 | 1955 | 1975 |
1955 | Chlordiazepoxide | Leo Sternbach, Hoffmann-La Roche, 1955 | 1955 | 1955 | 1975 |
1956 | Methylprednisolone | 1956 | 1956 | 1956 | 1976 |
1956 | Triamcinolone | 1956 | 1956 | 1956 | 1976 |
1957 | Spironolactone | 1957 | 1957 | 1957 | 1977 |
1957 | Mepivacaine | A. F. Ekenstam, 1957 | 1957 | 1957 | 1977 |
1957 | Bupivacaine | 1957 | 1957 | 1957 | 1977 |
1957 | Chlorothiazide | 1957 | 1957 | 1957 | 1977 |
1958 | Dexamethasone | 1958 | 1958 | 1958 | 1978 |
1958 | Betamethasone | 1958 | 1958 | 1958 | 1978 |
1958 | Clozapine | 1958 | 1958 | 1958 | 1978 |
1958 | Triamcinolone acetonide (Nasacort) | 1958 | 1958 | 1958 | 1978 |
1959 | Hydrochlorothiazide | 1959 | 1959 | 1959 | 1979 |
1959 | Chlortalidone | 1959 | 1959 | 1959 | 1979 |
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 | Trimethoprim | 1962 | 1982 | ||
1962 | Furosemide | Calvin L. Stevens, Parke-Davis 1962 | 1962 | 1982 | |
1962 | Ketamine | Calvin L. Stevens, Parke-Davis 1962 | 1962 | 1982 | |
1962 | Piroxicam | Pfizer 1962 | 1962 | 1992 | |
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 | Indometacin | 1963 | 1963 | 1965 | 1983 |
1963 | Flufenamic acid | Parke-Davis, 1963 | 1963 | 1965 | 1983 |
1963 | Ropivacaine | 1963 | 1963 | 1963 | 1983 |
1964 | Meclofenamic acid | Parke-Davis, 1963 | 1963 | 1965 | 1983 |
1964 | Propranolol | James Black, 1964 | 1964 | ||
1964 | Clonazepam | Leo Sternbach, 1964 | 1964 | 1964 | 1984 |
1964 | Triamterene | 1964 | 1964 | 1964 | 1984 |
1964 | Tetrahydrocannabinol (dronabinol) | 1964 | 1964 | 1964 | N/A |
1966 | Salbutamol (Albuterol) | David Jack, Allen & Hanburys, 1966 | 1966 | 1986 | |
1967 | Amiloride | 1964 | 1964 | 1964 | 1984 |
1968 | Prilocaine | 1968 | 1968 | 1968 | N/A |
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 | |
1973 | Budesonide | 1973 | 1973 | 1993 | |
1974 | Sufentanil | Janssen Pharmaceutica, 1974 | 1994 | ||
1974 | Carfentanil | Janssen Pharmaceutica, 1974 | 1994 | ||
1976 | Ipratropium bromide | 1976 | 1976 | 1996 | |
1976 | Naproxen | 1976 | 1976 | 1996 | |
1977 | Ranitidine | John Bradshaw, Allen & Hanburys, 1977 | 1981 | ||
1977 | Propofol | John Bradshaw, Allen & Hanburys, 1977 | 1981 | ||
1977 | Tramadol | Grünenthal GmbH, 1977 | 1977 | 1997 | |
1981 | Verapamil | 1981 | 1981 | 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 | |
1989 | Ketorolac | 1989 | 1989 | 2009 | |
1993 | Fluticasone propionate | David Jack, 1993 | 1993 | 2004 | |
1993 | Ketoprofen | James W. Young, William J. Wechter and Nancy M. Gray in 1993 | 1993 | 2003 | |
1993 | Celecoxib | 1993 | 1993 | 2003 | |
1993 | Rofecoxib | 1993 | 1993 | 2003 | |
1995 | Parecoxib | 1995 | Not approved | 2015 | |
1996 | Lopinavir | 2000 | - | ||
1997 | Mometasone furoate (Nasonex) | 1997 | 1997 | 2017 | |
1997 | Eletriptan | 1997 | 2002 | 2017 | |
1998 | Ropivacaine | 1998 | 1998 | 1998 | 2008 |
1998 | Leflunomide | 1998 | 1998 | 2008 |
21st century CE
edit21st century begins with the first complete sequences of individual human genomes by Human Genome Project, on 12 February 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.[30]
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, Cas12a 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 * |
---|---|---|---|---|---|---|
2000 | Bevacizumab | 2004 | 2024 | MA | ||
2001 | Valdecoxib | 2016 | N/A | SM | ||
2001 | Etoricoxib | 2016 | N/A | SM | ||
2003 | Alirocumab | 2015 | 2035 | MA | ||
2006 | Linagliptin | 2011[31] | 2031 | SM | ||
2007 | Apixaban | 2012 | 2032 | SM | ||
2007 | Alectinib | 2014 | 2014 | SM | ||
2007 | Sofosbuvir | 2007, Raymond F. Schinazi.[32][33] | N/A | N/A | N/A | SM |
2007 | Bevirimat | SM | ||||
2012 | Ivacaftor | 2012 | 2032 | SM | ||
2013 | Vilanterol | 2013 | 2033 | SM | ||
2014 | Evolocumab | 2015 | 2035 | MA | ||
2014 | Umeclidinium bromide (Incruese Ellipta) | 2014 | 2034 | SM | ||
2014 | Tisagenlecleucel | 2017 | 2037 | ACT |
* MA = Monoclonal antibody
SM = Small molecule
ACT = Adoptive cell transfer
See also
edit- 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
- Pharmacopoeia
- Edwin Smith Papyrus
- De Materia Medica
- Shennong Ben Cao Jing
- The Canon of Medicine
- The Book of Healing
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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.
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