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Status:
US Previously Marketed
Source:
THEOMINAL RS THEOBROMINE by WINTHROP
(1961)
Source URL:
First marketed in 1921
Source:
Theobromine Sodio-Salicylate U.S.P.
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Theobromine is the primary alkaloid present in the cocoa and chocolate. Theobromine is found in the shells and beans of the cacao plant and it is extracted from the husks of the bean and used for the synthesis of caffeine. Theobromine is an adenosine A1 and A2a receptor antagonist. Thesodate is used as a vasodilator, a diuretic, and heart stimulant. And similar to caffeine, it may be useful in management of fatigue and orthostatic hypotension. The symptomatic adverse reactions produced by theobromine are more or less tolerable and if they become severe, they can be treated symptomatically, these include anxiety, restlessness, tremors, sleeplessness, nausea and vomiting, loss of appetite. Theobromine is currently not in use as a medicinal drug.
Status:
US Previously Marketed
First marketed in 1921
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Melatonin (5-methoxy N-acetyltryptamine) is a hormone synthesized and released from the pineal gland at night, which acts on specific high affinity G-protein coupled receptors to regulate various aspects of physiology and behaviour, including circadian and seasonal responses, and some retinal, cardiovascular and immunological functions. Melatonin is also made synthetically and available without a prescription as an over-the-counter (OTC) dietary supplement in the U.S. Melatonin supplementation has many uses, however, it has been widely studied for treatment of jet lag and sleep disorders. Parents may consider using melatonin to help their child who has a trouble falling asleep. A medical professional should always evaluate insomnia or other sleeping disorders in children. Additionally, melatonin has been shown to protect against oxidative stress in various, highly divergent experimental systems. There are many reasons for its remarkable protective potential. In mammals, melatonin binds to a number of receptor subtypes including high-affinity (MT1 and MT2) and low-affinity (MT3, nuclear orphan receptors) binding sites, which are distributed throughout the central nervous system and periphery.
Status:
US Previously Marketed
Source:
ALLONAL AMINOPHENAZONE by ROCHE
(1961)
Source URL:
First marketed in 1897
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Aminophenazone is a phenyl-pyrazolone derivative with potent analgesic and antipyretic properties. Aminophenazone has been used as salt or complexes, including topically as the salicylate. It was recommended for the treatment of a fever, neuralgia, myositis, acute rheumatism, arthritis, chorea. In 1999 the FDA suspended aminophenazone. The drug caused agranulocytosis. Some of the cases of agranulocytosis were fatal. Another reason for suspending this drug from the market was its ability to react with nitrite-containing food, thus forming carcinogenic nitrosamines. A breath test with 13C-labeled aminopyrine has been used as a non-invasive measure of cytochrome P-450 metabolic activity in liver function tests.
Status:
US Previously Marketed
Source:
Acetphenetidin U.S.P.
(1921)
Source URL:
First marketed in 1887
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Phenacetin was used as an analgesic and fever-reducing drug in both human and veterinary medicine for many years. Since a major portion of a dose of phenacetin is rapidly metabolised to paracetamol, it seems possible that phenacetin owes some of its therapeutic activity to its main metabolite, paracetamol, whereas its most troublesome side effect (methaemoglobinaemia) is due to another metabolite, p-phenetidine.
Phenacetin was shown to inhibit cyclooxygenase (COX)-3, a cyclooxygenase-1 variant while p-phenetidine potently inhibits both COX-1 and COX-2. There is sufficient evidence in humans for the carcinogenicity of analgesic mixtures containing phenacetin. Analgesic mixtures containing phenacetin cause cancer of the renal pelvis, and of the ureter. Phenacetin was withdrawn from many analgesic mixtures long before the legal ban in several countries.
Status:
US Previously Marketed
First marketed in 1885
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Antipyrine is an analgesic and antipyretic that has been given by mouth and as ear drops. It is often used in testing the effects of other drugs or diseases on drug-metabolizing enzymes in the liver. It inhibits cyclooxygenases and shows little anti-inflammatory activity. Like many old and approved substances after almost 100 years of use, antipyrine has been associated with some serious side effects, namely agranulocytosis and shock reactions.
Status:
US Previously Marketed
First marketed in 1847
Class (Stereo):
CHEMICAL (ACHIRAL)
Chloroform is a colorless, sweet-smelling, dense liquid and widely used industrial and laboratory solvent. The total global flux of chloroform through the environment is approximately 660 000 tonnes per year, and about 90% of emissions are natural in origin. Many kinds of seaweed produce chloroform, and fungi are believed to produce chloroform in soil. Chloroform is used as an industrial solvent and as an intermediate in the manufacture of polymeric materials. The major use of chloroformtoday is in the production of the refrigerant R-22, commonly used in the air conditioning business. Inhaled chloroform anesthesia was introduced in 1847 and Chloroform subsequently became the most widely used volatile anaesthetic, and was used in horses before the end of the 19th century. Pure chloroform is known to be decomposed by the air with the formation of hydrochloric acid, phosgene and carbon dioxide. Phosgene is also generated metabolically from chloroform, and liver and kidney damage can ensue from its production.
Status:
US Previously Marketed
First marketed in 1846
Class (Stereo):
CHEMICAL (ACHIRAL)
Diethyl ether (ether) had been widely used for anesthesia until the 1960s despite its explosive properties and toxicity to both humans and animals. Diethyl ether still serves a role today as an effective inhalation agent. Newer inhalation agents have replaced ether completely and open drop delivery systems have been exchanged for complicated vaporizers and monitoring systems. Anesthesia in the developing world, however, still closely resembles primitive anesthetics.
Status:
US Previously Marketed
Source:
21 CFR 310.544(a) smoking deterrent quinine ascorbate
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Quinine ascorbate is a salt of antimalarial drug quinine and ascorbic acid (vitamin C). Ascorbate reduces the potency of quinolone-containing anti-malarial drugs. Quinine ascorbate was marketed as a component of over-the-counter smoking deterrent products but was not recognized as safe by the FDA regulation in 1993.
Status:
Possibly Marketed Outside US
Source:
NCT03198572: Phase 4 Interventional Recruiting Non-alcoholic Steatohepatitis
(2017)
Source URL:
First approved in 2023
Source:
sugar management gummies by XIAN CHIANG COMPANY LIMITED
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Berberine, an alkaloid isolated from Rhizoma Coptidis, is known to have a wide array of therapeutic effects including antimicrobial, antineoplastic, and hepatoprotective effects. It is found in several plants including European barberry, goldenseal, goldthread, Oregon grape, phellodendron, and tree tumeric. Berberine seems to slightly reduce blood sugar levels in people with diabetes. Berberine might lower blood pressure. Berberine is possibly safe for most adults for short-term use when taken by mouth or applied to the skin.
Status:
Possibly Marketed Outside US
Source:
NCT01380015: Phase 4 Interventional Completed Osteoarthritis of the Knee
(2011)
Source URL:
First approved in 2021
Source:
M020
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Rosmarinic acid (α-o-caffeoyl-3,4-dihydroxyphenyllactic acid; RA) is a naturally occurring hydroxylated compound commonly found in species of the subfamily Nepetoideae of the Lamiaceae and Boraginaceae, such as Rosmarinus officinalis, Salvia officinalis, and Perilla frutescens. RA is biosynthesized from the amino acids L-phenylalanine and L-tyrosine by eight enzymes that include phenylalanine ammonia lyase and cinnamic acid 4-hydroxylase. Recently, RA and its derivatives have attracted interest for their biological activities, which include anti-inflammatory, anti-oxidant, anti-angiogenic, anti-tumor, and anti-microbial functions. Clinically, RA attenuates T cell receptor-mediated signaling, attenuates allergic diseases like allergic rhinitis and asthma, and 2,4-dinitrofluorobenzene-induced atopic dermatitis-like symptoms, protects from neurotoxicity, and slows the development of Alzheimer's disease. Rosmarinic Acid seems to be able to suppress 5-lipoxygenase and 5-HETE synthesis (a pro-inflammatory compound in the omega-6 metabolic chain). Rosmarinic acid appeared to be effective in suppressing allergies in a dose-dependent manner, with 30% of the placebo group reporting symptom relief compared to 55.6% of the 50mg group and 70% of the 200mg group.