Aescin, the major active principle from Aesculus hippocastanum (Hippocastanaceae) the horse chestnut tree, has shown satisfactory evidence for a clinically significant activity in chronic venous insufficiency (CVI), haemorrhoids and post-operative oedema. In one controlled trial aescin was shown to be as effective as compression therapy as an alternative to medical treatment for CVI. The therapeutic benefit is well supported by a number of experimental investigations in different animal models, indicative of clearcut anti-oedematous, anti-inflammatory and venotonic properties, mainly related to the molecular mechanism of the agent, allowing improved entry of ions into channels, thus raising venous tension in both in vitro and in vivo conditions. Other mechanisms, i.e. release of PGF2 from veins, antagonism to 5-HT and histamine, reduced catabolism of tissue mucopolysaccharides, further underline the wide ranging mechanisms of the therapeutic activity of aescin. Aescin exists in two forms, α and β. β-aescin (b-escin) appears to be the active component of the mixture and is the molecular form present in major available pharmaceutical products. Beta-aescin has cytotoxic activity toward human colon adenocarcinoma cell lines.

Olprinone (INN) is a cardiotonic agent, is used for treatment acute heart failure. It has been marketed in Japan since 1996. The main mechanism of action of olprinone hydrochloride hydrate is selective inhibition of PDE III specific to cAMP. It is considered that this action causes an increase in intracellular cAMP levels and peak Ca2+ levels, thereby increasing myocardial contractility.

Maduramicin is antibiotic isolated from actinobacteria Actinomadura rubra. Maduramicin is used in veterinary as an aid in the prevention of coccidiosis in broiler chickens and turkeys. The compound is reported to be toxic to animals and humans if improperly used or by accident, resulting in heart failure, skeletal muscle degeneration, and even death. Studies have shown that toxicity is due to activation of protein phosphatase 2A, and the manipulation of the ROS-PTEN-Akt-Erk1/2 pathway may be a potential approach to prevent maduramicin -induced cardiotoxicity.

Pirenoxine is an anti-cataract agent which is used in many asian countries under the name Catalin. Although its efficacy is not proved scientifically, the drug may play an important role in cataract prevention. It is supposed that the anti-cataract effect of pirenoxine results from inhibition of sulfhydryl combination of quinoid substances with lens proteins and the inhibition leads to the maintenance of lens transparency.

Picoperine (Coben) is an antitussive agent.

Noxiptiline (brand names Agedal, Elronon, Nogedal), is a tricyclic antidepressant (TCA) that was introduced in Europe in the 1970s for the treatment of depression. In a double-blind comparison of noxiptiline and amitriptyline in hospitalized patients with primary depressive illness for 3-6 weeks there were no significant differences, but noxiptiline had a faster onset of action. A comparison with imipramine also showed no difference in therapeutic efficacy. As regards adverse effects, noxiptiline seemed to cause more mental symptoms, such as delirium. In one study in 44 patients, 9 developed delirium, there were mild manic symptoms in 6, dry mouth in 21, disturbed micturition in 2. and difficulty in accommodation in 3.

Loprazolam is a hypnotic drug which stimulates GABA-A receptors. Due to its hypnotic activity the drug is used to treat short-term sleep disordes.

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.

Butriptyline is a tricyclic antidepressant used in patients with depression associated with anxiety. The drug is supposed to be withdrawn from the market as the last publication about its clinical use is dated by 1988.

Fazadinium (used as a bromide salt) is a muscle relaxant, which was applied in anesthesia under the name Fazadon. The current marketing status is unknown and the drug is supposed to be discontinued.