Oxetorone is an antimigraine drug used for the disease-modifying treatment of migraines and marketed in several European countries. It works by non-selective inhibition of serotonin receptors and antihistamine agent. The therapeutic effects of oxetorone are primarily linked to antiserotonergic and also antihistamine and anti-adrenergic properties. Antidopaminergic properties are also suspected because hyperprolactinemia and extrapyramidal reactions have been observed. Adverse effects are: hypertonia, drowsiness at the start of treatment, diarrhoea and lymphocytic colitis. Acute intoxications by oxetorone, although uncommon, are potentially severe poisonings.

Melinamide is an antilipidemic agent similar to gemfibrozil. It acts to lower elevated serum lipids by reducing the very low-density lipoprotein fraction rich in triglycerides. Serum cholesterol may be decreased, particularly in those patients whose cholesterol elevation is due to the presence of IDL as a result of Type III hyperlipoproteinemia. Melinamide caused a decrease of the enhanced intestinal ACAT activity in diabetic rats, but did not affect intestinal cholesterol esterase activity. Marked improvement of hypercholesterolaemia in cholesterol-fed diabetic rats occurred concomitantly with the drug treatment. These results suggest that intestinal ACAT activity is closely related to the serum cholesterol level in diabetic rats, and show that melinamide lowers intestinal ACAT activity. Melinamide (Artes®) was the only marketed (in Japan) ACAT inhibitor. 04 Aug 2004 was withdrawn for Hypercholesterolaemia in Japan.

Incadronate (Disodium Cycloheptylaminomethylene diphosphate) is used to treat malignancy-associated hypercalcemia (MAH) in Japan. Experiments on rodents have revealed that this drug could be an effective agent for the treatment of various arthritic conditions, including human rheumatoid arthritis. In addition was shown, that incadronate induced growth inhibition and apoptotic death of pancreatic cancer cells. Incadronate also inhibited migration presumably by preventing the activation of Rho by lysophosphatidic acid. Thus, this drug can be of value in regimens for the treatment of pancreatic cancer.

Ciclonicate is a vasodilator and is used in cerebral and peripheral vascular disorders. Ciclonicate, given orally, markedly reduced basal and stimulated lipolysis. In 24-h-fasted rats its antilipolytic activity was long-lasting. Cyclonicate would influence not only triglyceride hydrolysis, but also free fatty acid utilization by adipose tissue.

Nifurtoinol, a nitrofuran-derivative, is an antibacterial drug. Nifurtoinol (Urfadyn PL) is used for the treatment of urinary tract infections. Nifurtoinol-associated hepatic injury cases were reported in Netherlands.

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.

Ribostamycin sulfate is an aminoglycoside-aminocyclitol antibiotic isolated from a streptomycete. It is an important broad-spectrum antibiotic with important use against human immunodeficiency virus and is considered a critically important antimicrobial by the World Health Organization. Aminoglycosides work by binding to the bacterial 30S ribosomal subunit (some work by binding to the 50S subunit), inhibiting the translocation of the peptidyl-tRNA from the A-site to the P-site and also causing misreading of mRNA, leaving the bacterium unable to synthesize proteins vital to its growth. Ribostamycin is usually used to treat sepsis, superficial skin infection, deep skin infection, lymphangitis/lymphadenitis, chronic pyoderma, osteomyelitis, pharyngitis/laryngitis, tonsillitis, acute bronchitis, pneumonia, pulmonary abscess, pyothorax, secondary infection in chronic respiratory lesions, cystitis, pyelonephritis, gonococcal infection, peritonitis, cholecystitis, dacryocystitis, keratitis (including corneal ulcer), otitis media, sinusitis and gnathitis. The most commonly reported adverse reactions include renal dysfunction, liver disorder and rash.

Rociverine is the antispasmodic agent with balanced neurotropic and myotropic activity. The muscle-relaxant activity of rociverine is achieved by inhibiting the availability of Ca2+ at contraction site and not through an antiphosphodiesterasic mechanism, which might explain the absence of muscle-relaxant effects on the smooth musculature of the blood vessels. Rociverine did not differ statistically from the reference antispasmodic drug hyoscine butylbromide in premedication for endoscopy of the upper gastro-intestinal tract. No adverse effects were noted. Intrapartum administration of rociverine to nulliparous women may help to reduce the duration of the first stage of labor in a context of uniform labor management. Orally administered rociverine produced a dose-related reversal of the reserpine-induced detrusor hyperreflexia in anaesthetized rats. In experimental models rociverine was more effective than flavoxate. These results point to the usefulness of rociverine in the treatment of urinary bladder motility disorders.

Bisbentiamine is an O-benzoyl thiamine disulfide or vitamin B1 disulfide derivative. Thiamine derivatives and thiamine-dependent enzymes are present in all cells of the body, thus a thiamine deficiency would seem to adversely affect all of the organ systems. Lipid-soluble thiamine precursors such as Bisbentiamine have a much higher bioavailability than genuine thiamine and therefore are more suitable for therapeutic purposes. It is also used as a dietary supplement.

Nemonapride, benzamide derivative (YM-09151-2) is essentially a typical antipsychotic drug, similar in structure to sulpiride. This drug was manufactured by Yamanouchi Pharmaceuticals and released in Japan. The mechanism of action of nemonapride is not proven, but its unique antipsychotic effect arises from its selective binding to the dopamine D2 receptor family. Since nemonapride has high affinity for D3 and D4 dopamine receptors, it is conceivable that its effect on negative symptoms might result from blockade of these receptors. Animal studies have suggested that nemonapride has pharmacological features that are different from those of typical neuroleptics. The low extrapyramidal side effect profile of nemonapride treatment appears to coincide with the characteristic features of another benzamide derivative, remoxipride.