Loperamide Oxide is a prodrug of loperamide, an antidiarrheal agent, patented by Belgian pharmaceutical company Janssen Pharmaceutica N. V. as an antidiarrheal agent. Loperamide oxide is reduced to loperamide and has the same antisecretory potency as loperamide in jejunum and colon. In clinical trials, Loperamide oxide provides a safe and effective treatment for chronic diarrhea associated with Crohn's disease. Loperamide Oxide is used in the Netherlands for the treatment of acute diarrhea in adults under brand name Arestal.

Mefenorex or (+/-)N-(3-chloropropyl)-1-methyl-2-phenylethylamine is an N-alkylated analogue of amphetamine. The therapeutic efficacy of mefenorex as an adjunctive support in the treatment of obesity for limited periods of time, as well as its ability to be well tolerated, has been amply demonstrated. Mefenorex is considered to be racemic mixture, no available data regarding enantiospecific pharmacological activity of the compound.

Timepidium bromide is a quaternary ammonium antimuscarinic used for the symptomatic treatment of visceral spasms. It is a muscarinic antagonist.

Oxabolone is a synthetic anabolic steroid. It can be formulated as the cipionate ester prodrug oxabolone cipionate. Oxabolone cypionate is a structural derivative of nandrolone. It differs via the additional 4-hydroxyl group that is attached, therefore making oxabolone cypionate 4-hydroxynandrolone. Oxabolone is on the World Anti-Doping Agency's list of prohibited substances, and is therefore banned from use in most major sports. Oxabolone cypionate is a relatively rare drug that was once produced in Europe for human use. Was used for the treatment of osteoporosis. It is no longer produced by pharmaceutical companies; Upjohn and Pharmacia were the primary producers of it previously.

METHYLMETHIONINE (S-Methionine methyl sulfonium, SMMS) chloride is a derivative of methionine metabolism in some plants. Methylmethionine has therapeutic effects on gastrointestinal ulceration potentially via its ability to promote dermal fibroblast migration and growth. The natural derivative Methylmethionine is biosynthesized from L-methionine which is first converted to S-adenosylmethionine. The subsequent conversion, involving replacement of the adenosyl group by a methyl group is catalyzed by the enzyme methionine S-methyltransferase. Methylmethionine is particularly abundant in plants, being more abundant than methionine. S-Methylmethionine is sometimes referred to as vitamin U, but it is not considered a true vitamin. The term was coined in 1950 by Garnett Cheney for uncharacterized anti-ulcerogenic factors in raw cabbage juice that may help speed healing of peptic ulcers.

Benfluorex under trade name Mediator was launched in 1976 for controlling blood sugar levels in people with type 2 diabetes. In 2009 this drug together with others medicines containing it was withdrawn because of the risk of heart valve disease. The mechanisms by which benfluorex reduces hepatic gluconeogenesis are markedly different from those of metformin, the main antidiabetic compound used in the world. It was suggested that inhibition of gluconeogenesis by benfluorex was, at least in part, due to a decrease in mitochondrial β-oxidation. First, benfluorex decreased acetyl-CoA concentration, which in turn would reduce pyruvate carboxylase activity and release its inhibitory effect on pyruvate dehydrogenase. Second, benfluorex decreased both the ATP-to-ADP and the NAD+-to-NADH ratios, leading to a reduced gluconeogenic flux at the level of 3-phosphoglycerate kinase and GAPDH. Changes in cellular redox state represent probably the main mechanism by which benfluorex reduces glucose production in hepatocytes.

Tiemonium (often used in a form of iodide or methylsulphate salt) is a muscarinic acetylcholine receptor antagonist, which is available in Asia (mainly Bangladesh) for the alleviation of muscle spasms of the intestine, biliary system, uterus and urinary bladder in gastrointestinal, biliary, urinary and gynecological diseases.

Buformin (1-butylbiguanide) is an oral antidiabetic drug of the biguanide class. AMPK activator. AMPK is a potential therapeutic target in the prevention and the treatment of type 2 diabetes and insulin resistance. Major classes of antidiabetic drugs have been reported to activate AMPK. Buformin exerts its anti-tumorigenic activity via activation of AMPK and inhibition of the mTOR signaling pathways in endometrial cancer cells. Toxicity: guinea pig LD50 subcutaneous 18 mg/kg; mouse LD50 intraperitoneal 140 mg/kg and 300 mg/kg oral. Buformin was withdrawn from the market in many countries due to an elevated risk of causing lactic acidosis.