Levocabastine (trade name Livo) is a selective second-generation H1-receptor antagonist used for allergic conjunctivitis. Levocabastine binds the G protein-coupled neurotensin receptor 2 (NTR2), but not NTR1, where it behaves as a weak partial inverse agonist. In an environmental study, LIVOSTIN 0.05% (levocabastine hydrochloride ophthalmic suspension) instilled four times daily was shown to be significantly more effective than its vehicle in reducing ocular itching associated with seasonal allergic conjunctivitis. After instillation in the eye, levocabastine is systemically absorbed. However, the amount of systemically absorbed levocabastine after therapeutic ocular doses is low (mean plasma concentrations in the range of 1-2 ng/mL). Brand name Livostin is no longer available in the U.S., but generic versions may still be available. Common side effects include burning, stinging, itching, or watering of the eyes, eye irritation or discomfort, blurred vision, dry or puffy eyes, headache, nosebleed, nausea, or fatigue.

METHITURAL (as sodium salt) is a barbiturate derivative which was used as an ultrashort-acting intravenous anesthetic.

Glucosulfone (Glucosulfone Free Acid, or Promin) is a compound used to treat mycobacterial infections, such as tuberculosis and leprosy. It is converted to dapsone in the body, which also has been shown to have therapeutic effects against dermatitis herpetiformis, actinomycotic mycetoma, asthma, malaria, rheumatoid arthritis, Kaposiís sarcoma, pneumocystis carinii (pneumonia), subcorneal pustular dermatosis and cystic acne. Once converted to dapsone, it has haemotoxic effects (destroying red blood cells, or disrupting blood clotting, potentially causing organ or tissue damage).

Mandelic acid is an aromatic alpha hydroxy acid that is used for the treatment of urinary tract infections. The drug is marketed in Canada under the name Mandelamine (as a complex with methenamine). Mandelic acid exerts its antibacterial effect mainly by increasing urine acidity. Moreover, mandelic acid is used as a serum for the treatment of wrinkles.

Penimepicycline is a salt of beta-lactam antibiotic penicillin V and tetracycline antibiotic pipacycline. Penimepicycline exerts a bactericidal action on the streptococci, and a bacteriostatic action on various gram-positive and gram-negative bacilli, as well as on the penicillin-resistant staphylococci. In the 1960s it was studied in Japan for the treatment of urological, respiratory, gynecological and other infections.

Eseridine (Geneserine) has been known for many years as an anticholinergic agent and used in therapy as a gastrointestinal antispastic. Eseridine salicylate is an inhibitor of cholinesterase activity that has been given by mouth in preparations for dyspepsia and other gastric disorders. It has also been studied for the treatment of Alzheimer’s disease.

Imolamine is a coronary vasodilator, which is used in the treatment of angina pectoris and as a local anesthetic. Imolamine has been shown to produce in animals coronary vasodilation, local anaesthesia, analgesia and a papaverine like action in duodenal preparations. Imolamine increased the tone of uterus and ileum and this was accompanied by a reduction in amplitude of contraction. The response of the stomach tissue to imolamine was similar to that of butalamine and aminophylline, i.e. a relaxant action on smooth muscle. Imolamine has a variable action on tone, producing an increase in ileum and uterus and a decrease in stomach. Imolamine is able to cause severe cytolytic hepatitis.

Cefteram is a semisynthetic cephalosporin formulated for oral administration as the prodrug ester, cefteram pivoxil. The mechanism of action of cefteram is inhibition of bacterial cell wall synthesis. Cefteram exerts its bactericidal activity by strongly binding to penicillin-binding protein (PBP) 3, 1A, and 1Bs. The drug is available in Japan and is used for the treatment of bacterial infections.

Glyconiazide is an antibacterial drug with high antitubercular activity in vitro as well as in vivo. The drug was reported to cause sensitive polyneuritis upon administration.

Xibornol [6-(isoborn-2-yl)-3,4 xylenol] is a highly lipophilic and poorly soluble drug used as spray mouthwash for the local treatment of infection and inflammation of the throat and in the dental care, due to both its bacteriostatic activity, mainly against Gram positive micro-organisms and its antiviral properties. The drug concentration required for the therapeutic activity is 3% (w/v). Its poor water solubility makes difficult to set up drug formulations based on aqueous solvents, so xibornol is at present commercially available only as spray aqueous suspension. The self-microemulsifying approach was found to be effective to formulate stable and pharmaceutically acceptable liquid spray formulations of xibornol. The minimal inhibitory concentrations (MIC) and the minimal bactericidal concentrations (MBC) of xibornol against 100 strains of Staphylococcus aureus, clinically isolated have been evaluated in range between 2 ug/ml and 8 ug/ml. In the patients treated with xibornol (500 mg every 8 h for 7 days) any modification in phagocytosis frequency (PMF), phagocytosis index (PHI), nitroblue tetrazolium (NBT), reduction frequency (NRF), microbicidal activity and neutrophil mobility of PML, before, during and after the end of therapy wasn’t found.