Nepinalone is a new alchilaminate derivative of β-tetralone, which possess a non-opioid antitussive activity. Nepinalone racemus exerted a significant antitussive activity and both L- and D-isomers confirmed to possess a significant dose-correlated antitussive effect with better trend of activity for D-isomer, but not statistically significant. It was predicted to act via sigma receptors. Occasionally, episodes of gastric intolerance have been reported and rapidly receded when treatment was stopped. The use of doses higher than those recommended could cause drowsiness.

Piromidic acid, a quinolone antibiotic has an inhibitory effect against hepatic stages of P. falciparum and P. yoelii yoelii, and has a potential for treatment or prevention of malaria through their unique antiparasitic effect against erythrocytic and hepatic stages of Plasmodium.

Ketobemidone (Cliradon, Ketogan, Ketodur, Cymidon) is a strong opioid analgesic, structurally related to pethidine, which has been in clinical use for more than 50 years. In the Scandinavian countries ketobemidone is only available in combination with a spasmolytic substance N,N-dimethyl-3,3-diphenyl-I-methylallylamine (A29). Ketobemidone has been shown to be a non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist. In spite of a relatively low mu-receptor affinity ketobemidone has a higher analgesic potency than morphine by systemic administration. It is probably due to its higher lipophilicity and consequently more easy penetration into the CNS. Ketobemidone is indicated for the treatment of all types of severe pain, such as postoperative, cancer, kidney stones and fractures.

Dibekacin is a semisynthetic aminoglycoside antibiotic useful in the treatment of severe gram-negative bacterial infections. The drug is marketed in Japan.

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.

Norfenefrine or meta-octopamine, also known as 3,β-dihydroxyphenethylamine, is an adrenergic agent used as a sympathomimetic drug which is marketed in Europe, Japan, and Mexico. Along with its structural isomer p-octopamine and the tyramines, norfenefrine is a naturally occurring, endogenous trace amine and plays a role as a minor neurotransmitter in the brain. Norfenefrine controls blood pressure in acute hypotensive states eg pheochromocytomectomy, sympathectomy, poliomyelitis, spinal anesth, MI, septicemia, blood transfusion and drug reactions. Adjunct in treatment of cardiac arrest and hypotension.

Eperisone is an antispasmodic drug approved in Japan for the treatment of of diseases characterized by muscle stiffness and pain. It is believed that eperisone exerts its effect through inhibition of sodium channels. The drug is still being marketed in Asia under the name Myonal (Square Pharmaceuticals).

Tedisamil is an antiarrhythmic with additional anti-ischaemic properties, which acts via potassium channel blockade. This drug can be categorised as a class III antiarrhythmic agent due to its effects of action potential and QT interval prolongation in these patients. Although tedisamil has been shown to be an effective anti-ischaemic agent, with Phase III trials for angina pectoris now completed, the company are now pursuing the use of tedisamil for the treatment of atrial fibrillation, for which tedisamil is still in Phase II/III clinical trials. The FDA’s Cardiovascular and Renal Drugs Advisory Committee voted not to recommend approval for Solvay Pharmaceuticals’ investigational anti-arrhythmic drug Pulzium (Tedisamil) and asked the company to give the FDA more information.

Domiodol is an iodinated organic compound. Domiodol had a marked cilio-excitatory effect, but did not affect experimental asthma in guinea-pigs or the respiratory resistance of anesthetized dogs. In a placebo-controlled crossover study, domiodol significantly increased the volume of secretions in chronic bronchitis subjects. This was deemed beneficial because patients were able to most easily cough up the mucus. Mucolytic treatment may be helpful in the post-operative treatment of laryngectomized patients with permanent tracheostomy. In addition, domiodol proved effective in reducing the symptoms of infection of the lower respiratory tract and in improving the consistency of mucus in children.

Clebopride is a dopamine antagonist drug. It is used to treat functional gastrointestinal disorder such as nausea or vomiting. Unchanged parent drug was the most abundant compound in human urine. Major metabolites included the hydroxylation at benzyl group to yield carbinolamine and its further N-dealkylation product, and the piperidine ring hydroxylation/oxidation metabolite (a lactam).