Nepaprazole is a proton pump inhibitor of substituted 2-(2-pyridinylmethylsulfinyl)-1H-benzimidazole class evaluated as useful drug for the clinical treatment of peptic ulcer diseases. The effects of the TY-11345 (nepaprazole sodium salt) on gastric mucosal proton pump (H+/K(+)-ATPase) activity, gastric acid secretion and gastro-duodenal lesions were investigated in experimental animals. TY-11345 potently inhibited H+/K(+)-ATPase activity in isolated rabbit gastric mucosal microsomes and the inhibitory effect was enhanced under weak acid conditions. In Ghosh & Schild rats, intravenous injection of TY-11345 significantly inhibited gastric acid secretion stimulated by tetragastrin; the effect of TY-11345 was twice as potent as that of omeprazole. In pylorus ligated rats, TY-11345 inhibited basal gastric acid secretion by both the intraduodenal and oral routes with 9 and 5 times more greater potency than those of omeprazole, respectively. The antisecretory effect of TY-11345 persisted for more than 24 h in pylorus ligated rats. In experimental ulcer models, TY-11345 prevented the formation of water-immersion stress, ethanol or indomethacin-induced gastric lesions and mepirizole-induced duodenal lesions in rats. The antiulcer effects of TY-11345 were 3 to 15 times more potent than those of omeprazole. These results suggested that TY-11345 had potent antisecretory and antiulcer effects which are exerted by suppression of H+/K(+)-ATPase activity in gastric parietal cells. Nepaprazole sodium had been studied in phase II clinical trials for treatment of gastric ulser but this research has been discontinued.

TILIDINE is a low to medium potency opioid analgesic. It is metabolized to its active metabolites, nortilidine and bisnortilidine. Its analgesic activity is largely exerted through nortilidine which is a potent agonist at Mu opioid receptors.

Trimebutine [3,4,5-trimethoxybenzoic acid 2-(dimethylamino)-2-phenylbutylester] is a noncompetitive spasmolytic agent. The actions of trimebutine on the gastrointestinal tract are mediated via (i) an agonist effect on peripheral mu, kappa and delta opiate receptors and (ii) release of gastrointestinal peptides such as motilin and modulation of the release of other peptides, including vasoactive intestinal peptide, gastrin and glucagon. Trimebutine attenuated colonic motility mainly through the inhibition of L-type Ca(2+) channels at higher concentrations, whereas, at lower concentrations, it depolarized membrane potentials by reducing BK(ca) currents, resulting in the enhancement of the muscle contractions.Trimebutine accelerates gastric emptying, induces premature phase III of the migrating motor complex in the intestine and modulates the contractile activity of the colon. It is indicated for the treatment and relief of symptoms associated with the irritable bowel syndrome (spastic colon); and in postoperative paralytic ileus in order to accelerate the resumption of the intestinal transit following abdominal surgery.

Proxibarbal is a non-sedative barbiturate with a specific anti-serotonin and anti-histamine effect, due to enzyme induction of serotoninase and histaminase. Its lack of unpleasant side-effects. Proxibarbal exists in ring-chain tautomeric equilibrium with the two diastereomers of valofan. Proxibarbal is metabolized to a five-membered lactone. Its only barbituric property is its ability to induce enzymes that destroy a surplus of neurohormones and rid people of their neurovegetative sufferings, including migraine and other types of vascular headache. Side effects are: dizziness, drowsiness, dyspepsia, allergic reactions. Proxibarbal enhances the effects of other depriving agents, including alcohol.

Oxolamine under brand names Symphocal, Perebron is used in some countries as a cough suppressant for the treatment of pharyngitis, tracheitis, bronchitis, bronchiectasis, pertussis. Oxolamine possesses anti-inflammatory activity, which causes a reduction in the irritation of the nervous receptors of the respiratory tract.

Cimetropium bromide (cimetropium) is a semi-synthetic belladonna alkaliod, a quaternary derivatives of scopolamine. Cimetropium was used in Italy under the name Alginor for the treatment of painful gastrointestinal conditions, such as irritant bowel syndrome or infant colics as well as in preparation for diagnostic procedures. The drug exerts its action by binding to muscarinic receptors and inhibiting their activity.

Benzoxonium is a quaternary ammonium compound with antibacterial, antiviral, and antimycotic activity. It can be used in topical disinfection, disinfection of surgical instruments, inhibition of plaque formation, and in veterinary products.

Enisamium (4-(benzylcarbamoyl)-1-methylpyridinium iodide) is an isonicotinic acid derivative, that used as an antiviral agent in Russia. Enisamium suppresses the effect of influenza viruses and other pathogens of acute respiratory viral infections due to a direct inhibitory effect on the penetration of viruses through the cell membrane. Enisamium has interferonogenic properties, promotes an increase in the concentration of endogenous interferon (interferon alfa and gamma) in blood plasma by 3-4 times.

Cycloguanil is a dihydrofolate reductase inhibitor and is a metabolite of the antimalarial drug proguanil. The parent drug proguanil was suggested to contribute to the antimalarial activity as well, but the mechanism of action is unknown. Proguanil is a prodrug that is metabolized to its main active metabolite, cycloguanil, mostly via CYP2C19. There is significant variation in proguanil pharmacokinetics.12 CYP2C19 is the predominant enzyme catalyzing the bioactivation of proguanil to cycloguanil. Cycloguanil is one of the few antimalarial drugs that act on both the erythrocytic and on the pre-erythrocytic (hepatic) forms of the malaria parasites. Although cycloguanil is not currently in general use as an antimalarial, the continuing development of resistance to current antimalarial drugs has led to renewed interest in studying the use of cycloguanil in combination with other drugs.

Pinaverium, known under the brand name DICETEL, is a spasmolytic agent used for functional gastrointestinal disorders. It is a quaternary ammonium compound that acts as an atypical calcium antagonist to restore normal bowel function. It is shown to relieve GI spasm and pain, transit disturbances and other symptoms related to motility disorders and may be considered as effective first-lline therapy for patients with irritable bowel syndrome (IBS). Pinaverium is also used to help relieve symptoms caused by certain disorders of the gallbladder associated with secretion of bile. Pinaverium bromide is the common ingredient in formulations, mostly as oral tablets. Although it is not a currently approved drug by the FDA, pinaverium is available in over 60 countries including Canada. DICETEL® (pinaverium bromide) is a calcium antagonist which inhibits the calcium influx by blocking the voltage-dependent calcium channel at the smooth muscle cell level. It possesses a high degree of selectivity for the intestinal smooth muscle.