TLW's Drugscope™ (Drug Historyscope)
By T.L. Winslow (TLW), the Historyscoper™
© Copyright by T.L. Winslow. All Rights Reserved.
Original Pub. Date: Sept. 6, 2016. Last Update: Mar. 4, 2018.
Westerners are not only known as history ignoramuses, but double dumbass history ignoramuses when it comes to Drug history. Since I'm the one-and-only Historyscoper (tm), let me quickly bring you up to speed before you dive into my Master Historyscope.
In 1837 French chemist Charles Frederic (Frédéric) Gerhardt (1816-56) discovers Acetylsalicylic Acid, the active ingredient in willow bark, but sets it aside as impractical after his formulation proves unstable; in 1878 Felix Hoffman rediscovers it. In 1890 the non-addictive topical anesthetic Benzocaine is isolated in Germany, and given the trade name Anesthesin. In 1898 Bayer Pharmaceutical Products (founded Aug. 1, 1863) of Darmstadt, Germany begins marketing a new, rather habit-forming cough suppressant formula (good also for laryngitis and TB), with its trademarked drug heroin (diacetylmorphine) as it main ingredient ("Heroin, the medicine for coughs"); the name is derived from the German word heroisch (large, powerful); German chemist Heinrich Dreser (1860-1924) is dir. of research. In 1899 Bayer Co. of Germany patents and trademarks Aspirin, from the "a" in acetyl, and the "spir" in Spiraea ulmaria, the willowleaf meadowsweet, later calling it the "Wonder Drug"; it is sold in powder form, the first tablets being sold in 1915; as part of the 1919 Versailles Treaty Bayer gives up its patents on aspirin and heroin - WWI was one giant headache?
In 1849 Mrs. Winslow's Soothing Syrup is introduced by Mrs. Charlotte N. Winslow of Bangor, Maine; the active ingredient is morphine; in 1879 English composer Edward Elgar composes a wind quintet in its honor; it is not withdrawn until 1930; in 1940 Woody Guthrie's "Tom Joad" mentions Grandpa Joad being given it before he dies.
In 1881 Valproate is discovered, later being discovered to be useful in preventing migraine headaches and seizures and treating epilepsy and bipolar disorder; it is first used medically in 1962, and is marketed under the brand name Depakote.
In 1897 German pharmacologist-chemist Arthur Carl Wilhelm Heffter (1859-1925) isolates Mescaline, the hallucinatory agent in peyote cactus, and becomes the first "psychonaut", willing to test the stuff on himself.
In 1902 Barbital (Barbitone) is synthesized by German chemists Emil Fischer and Joseph von Mering, becoming the first commercially available barbituate, used as a sleeping aid (hypnotic) until the 1950s; in 1904 Bayer markets it as Veronal, while Schering markets it as Medinal for "insomnia induced by nervous excitability", replacing bromides as a sleeping aid; too bad, tolerance is easily developed, encouraging lethal ODs.
In 1912 German Merck chemist Anton Kollisch (Köllisch) (1888-1916) synthesizes MDMA (Ecstasy) to stop abnormal bleeding; it is patented on May 16, 1914; its potential as a recreational drug is first publicized in 1978 by Russian-Am. chemist Alexander Theodore "Sasha" Shulgin (1925-) of UCB.
In 1917 the semisynthetic opioid Oxycodone, extracted from the opium poppy is developed in Germany; it is 1.5x as potent than morphine.
In 1922 Emil Werner and James Bell first describe the biguanide Metformin (Glucophage), found in French lilac (goat's rue); in 1929 its sugar-lowering action is discovered in rabbits; in 1958 it is introduced in Britain by Aaron subsidiary Rona; it is approved in Canada in 1972, and the U.S. FDA in 1994, with Bristol-Myers Squibb introducing it in the U.S. on Mar. 3, 1995, going on to become the world's most widely prescribed antidiabetic medication.
In 1927 the first commercial amphetamines are synthesized by pharmacologist Gordon Albert Alles (1901-63) in Los Angeles, Calif., who notes the "stimulating effect on the central nervous system"; the Benzedrine (amphetamine sulfate) inhaler is introduced in 1932.
In 1944 Methylphenidate is first synthesized by Leandro Panizzon of Ciba, who names it Ritalin after his wife Rita; it is identified as a central nervous stimulant in 1954; medical use begins in 1960.
In May 1950 the tranquilizer Miltown (Meprobamate), AKA Don't-Give-a-Damn Pills is synthesized by Wallace Labs; in 1955 it hits the market bigtime in Madison Ave. and Hollywood, going on to become the #1 selling drug in the U.S.; Milton Berle quips "I'm thinking of changing my name to Miltown Berle."
The 1960s is the Pharamaceutical Decade as blood pressure, tranquilizer, and other drugs hit the market bigtime, starting with the anti-anxiety sedative-hypnotic Benzodiazepines (BZDs) incl. Librium (Chlordiazepoxide) (AKA Librax, Libritabs, Mesural, Multum, Novapam, Sonimen, Tropium, Angirex, Elenium, Klopoxid et al.) of Hoffmann-La Roche Labs, which was discovered accidentally in 1955 by Leo Sternbach and receives FDA approval on Feb. 24; in 1963 it markets the benzodiazepine drug Diazepam AKA Valium; in 1977 the benzodiazepine drug Lorazepam is introduced, becoming known for its ability to induce sleep and amnesia, making it the date rape drug of choice - my mother used to look like this?
In 1961 Beecham Co. of Britain begins marketing the antiobiotic Ampicillin (Penbritin).
In 1963 Croatian-born Jewish-Am. chemist Leo Henryk "Xanman" Sternbach (1908-2005) of Roche Labs in N.J. develops the anti-anxiety drug Valium (Diazepam), the first "blockbuster drug", which in 1969-82 becomes the most prescribed drug in the U.S. (2.3B in 1978); although he makes zillions for Roche, he never becomes wealthy.
In 1964 Romanian psychologist-chemist Corneliu E. Giurgea (1923-95) synthesizes the learning-memory enhancing drug Piracetam; in 1972 he coins the term Nootropic for intelligence enhancing or smart drugs.
In 1976 the opioid pain reliever Oxycodone/Paracetmol (AKA Percocet, Endocet, Ratio-Oxycocet) is approved by the U.S. FDA.
In 1977 the antidepressant drug Sertraline AKA Zoloft is developed by Kenneth Koe and Willard Welch of Pfizer; it is approved by the U.K. in 1990, the U.S. FDA in 1991, and Australia in 1994; the U.S. patent expires in 2006.
In 1977 opioid pain drug Tramadol (Ultram) (originally Tramal) is introduced by Grunenthal GmbH of West Germany, reaching the U.S., U.K., and Australia in 1997.
In 1981 Alprazolam (Xanax) is introduced by Upjohn to treat anxiety disorders, becoming a blockbuster drug in the U.S.
In 1987 AZT (Azidothymidine) (Zidovudine) becomes the first drug to gain FDA approval for use in the treatment of AIDS.
On Sept. 18, 1988 Rogaine (originally Regain) (Minoxidil) becomes the first drug approved by the FDA for hair growth.
In 1993 BASF Bioresearch Corp. and Cambridge Antibody Technology U.K. begin developing monoclonal antibody drugs, coming up with Adalimumab, which is sold under the trade name Humira to treat rheumatoic and psoriatic arthritis, ankylosing spondylitis, Crohn's disease et al., becoming the #1 best-selling pharmaceutical product by the time its U.S. patent expires in 2016, with $16B global sales/year.
In 1995 Otsuka Pharmaceutical develops the anti-psychotic drug Aripiprazole (brand name Abilify), partnering with Bristol-Meyers squibb in 1999 and obtaining U.S. FDA approval for use in treatment of schizophrenia on Nov. 15, 2002, later acute manic and mixed episodes associated with bipolar disorder, and major depressive disorder; in 2013 it has global sales of $7B.
On Mar. 27, 1998 the Viagra (sildenafil citrate) pill for male impotence by Pfizer is approved by the U.S. FDA, and hits the market hard, with 3.6M prescriptions written in its first 4 mo.
On Oct. 17, 2006 the antidiabetic drug Sitagliptin by Merck & Co. (brand name Januvia) is approved by the U.S. FDA; on Apr. 2, 2007 they approve an oral combo with metformin, and on Oct. 7, 2011 an oral combo with simvastatin.