Charles Frédéric Gerhardt (1816-56) Heinrich Dreser (1860-1924) Bayer Aspirin Anton Kollisch (1888-1916) Alexander Shulgin (1925-) Gordon Albert Alles (1901-63) Leo Henryk Sternbach (1908-2005) Corneliu E. Giurgea (1923-95)

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: Sept. 5, 2018.



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What Is A Historyscope?


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 the 2nd cent. B.C.E. Illyrian king Gentius allegedly discovers the medicinal (anti-dyspeptic) properties of the gentian (genius Gentiana) plants, found only in high mountain meadows and pastures, with blue or yellow flowers - Ricola?

Charles Frédéric Gerhardt (1816-56) Heinrich Dreser (1860-1924)

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?

Mrs. Winslow's Soothing Syrup, 1849

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active ingredient is morphine; in 1879 English composer Edward Elgar composes a wind quintet in its honor; it is not withdrawn until 1930; in 1940 Woody Guthrie's "Tom Joad" mentions Grandpa Joad being given it before he dies.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 1884 the analgesic Aminopyrine is discovered and used a synthetic substitute for quinine.

Arthur Heffter (1859-1925)

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.

Anton Kollisch (1888-1916) Alexander Shulgin (1925-)

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.

Gordon Albert Alles (1901-63)

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."

In 1951 the sedative-hypnotic drug Methaqualone is first synthesized in India by Indra Kishore Kacker and Syed Husain Zaheer for use as an antimalarial drug; by 1965 it becomes the most commonly prescribed sedative in Britain, sold under the names Mandrax, Malsed, Malsedin, and Renoval; in 1975 it becomes the 6th best-selling sedative in the U.S., marketed under the brand name Quaalude ("quiet interlude") by William H. Rorer Inc.; too bad in the 1960s and 1970s it becomes a popular date rape drug, called ludes and sopers (soaps) in the U.S., and mandrakes in the British Commonwealth.

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?

Paul Janssen (1926-2003)

In 1960 the opioid drug Fentanyl (Fentanil) is discovered by Belgian physician Paul Janssen (Paul Adriaan Jan, Baron Janssen) (1926-2003) (founder of Janssen Pharmaceutica in 1953) , and approved by the U.S. FDA in 1968, going on to cause 20K deaths/year in the U.S. incl. celebs like rock star Prince.

In 1961 Beecham Co. of Britain begins marketing the antiobiotic Ampicillin (Penbritin).

In 1962 the loop diuretic Furosemide (AKA Lasix) is discovered, becoming the drug of choice for fluid buildup due to heart failure et al.

Leo Henryk Sternbach (1908-2005)

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.

Corneliu E. Giurgea (1923-95)

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.

Mansukhy C. Wani (1935-) and Monroe E. Wall (1916-2002)

In 1967 Monroe E. Wall (1916-2002) and Mansukh C. Wani (1935-) of the Research Triangle Inst. in N.C. isolate the anticancer chemical Taxol (Paclitaxel) from the bark of the Pacific yew tree Taxus brevifolia, which is later marketed by Bristol-Myers Squibb for breast and ovarian cancer patients.

Gaylord Anton Nelson of the U.S. (1916-2005) John McConnell (1915-2012) Denis Hayes (1944-)

On Apr. 22, 1970 (Lenin's birthday) the U.S. environmental movement is born with the first Earth Day, founded by U.S. Sen. (D-Wisc.) (1963-81) and former Wisc. gov. #35 (1959-63) Gaylord Anton Nelson (1916-2005), organized by the Earth Week Committee of Philadelphia, Penn., and celebrated in the U.S. by 22M people with demonstrations against pollution of Spaceship Earth (coined by Adlai E. Stevenson) amid herds of massive leaded-gas-slurping V8 sedans, a nation filled with smoky industrial smokestacks, and a coverup of a fuel rod meltdown at the Savannah River Nuclear Plant near Aiken, S.C. (acknowleged in 1988); the idea was first proposed in 1969 by Davis City, Iowa-born John McConnell (1915-2012) (designer of the Earth Flag) to the San Francisco Board of Supervisors, then coordinated by environmental activist Denis Allen Hayes (1944-), and supported by U Thant, Margaret Mead et al.; meanwhile on Jan. 14-23 Nelson goes for a double and holds the Nelson Hearings on the safety of combined oral contraceptive pills, resulting in the first side-effect disclosure for a pharmaceutical drug in the U.S.

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 1984 the synthetic drug Sumatriptan (an analog of psychedelic mushroom drug psilocybin) is developed by Glaxo Research for relieving the intensity of migraine and cluster headaches; in 1991 it is approved by the U.S. FDA, going on to be marketed under the trade names Sumatran, Sumax, Aumatriptanum, Imitrex, and Imigran; on Apr. 15, 2008 the FDA approves Treximet, a combo of sumatriptan and naproxen, followed in July 2009 by a single-use jet injector formulation.

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.

On Oct. 26, 1988 French pharmaceutical co. Roussel Uclaf announces that it will halt worldwide distribution of "abortion pill" RU-486 because of "an outcry of opinion at home and abroad", but two days later the French govt. orders the co. to reverse (abort?) itself.

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 1993 the U.S. FDA approves the sale of the atypical antipsychotic drug Risperidone (brand name Risperdale), which becomes the drug of choice to treat schizophrenia, bipolar disorder, and irritability in autism sufferers.

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. 12, 1996 the FDA approves the AIDS protease inhibitor drug Indinavir, invented by Kate Halloway and Chen Zhiao.

In 1996 the phenethylamine class CNS stimulant Adderall, a mixture of four amphetamine salts is introduced by Richwood Pharmaceuticals, becoming popular as an athletic performance and cognitive performance enhancer as well as a treatment for narcolepsy and ADHD.

In 1996 the USDA approves the marketing of the acetylcholinesterase inhibitor Donepezil for Alzheimer's patients, marketed by Esai Co. of Japan under the name Aricept.

In 1997 after being introduced for the treatment of prostate enlargement in 1992, the FDA approves Finasteride (brand names Propecia, Proscar) for preventing male scalp hair loss.

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 Dec. 31, 1998 the FDA approves Pfizer's Celebrex for arthritis sufferers, becoming the first approved COX-2 inhibitor - since the padded bra?

On Oct. 27, 2000 the U.S. Drug Addiction Treatment Act, sponsored by Sen. Orrin G. Hatch (R-Utah) and Sen. Carl M. Levin (D-Mich.) is signed by Pres. Clinton, treating heroin addiction as a disease, and backing use of methadone alternatives buprenorphine (a partial opiate producing minimum mood alteration) and buprenorphine-naloxone (ditto with an opiate blocker), which go on to win FDA approval in Sept. 2002; now the longtime horrible sin is in the same category as diabetes and hypertension?

On Nov. 6, 2000 the U.S. Needlestick Safety and Prevention Act is signed by Pres. Clinton after clearing Congress in record time, the Centers for Disease Control (CDC) estimating in Mar. that more than 380K subcutaneous injuries from contaminated sharps occur each year among U.S. health profs., and up to 800K worldwide, subjecting them to the risk of contracting HIV and hepatitis-C; the real reason is lobbying by Becton Dickinson & Co. of N.J., which has spent $500M developing "safety-engineered needles" that cost over twice as much as ordinary hypos?

In 2002 the U.S. FDA approves the atypical antipsychotic drug Aripiprazole (brand name Ability), developed by Otsuka of Japan for the treatment of schizophrenia and bipolar disorder; sales reach $6.9B in 2013.

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.

In May 2007 the U.S. FDA approves the birth control pill Lybrel, which completely ends monthly periods except for occasional bleeding.

On July 13, 2015 after Otsuka's patent on aripiprazole (Abilify) expires on Oct. 20, 2014 the U.S. FDA approves the atypical antipsychotic drug Brexpiprazole (brand name Rexulti), developed by Otsuka and Lundbeck for the treatment of schizophrenia and depression.

On Apr. 19, 2018 a U.S. FDA advisory panel unanimously recommends the approval of an epilepsy medication caled Epidiolex by GW Pharmaceutics of Britain made with an ingredient found in marijuana, becoming the first cannabis-derived prescription medicine in the U.S.




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