Lercanidipine is antihypertensive drugs which acts by blocking L-type calcium channels, allowing relaxation and opening of blood vessels. Lercanidipine exists as a racemate, with anti-hypertensive activity residing primarily in S-enantiomer. NDA for lercanidipine was submitted to FDA in 2002 by Forest Laboratories, but FDA refused to approve the drug, and lercanidipine is not marketed in USA. Lercanidipine is also investigated in preclinical models of epilepsy and ischemic stroke.

Thiobutabarbital is a barbiturate derivative invented in the 1950s. It has sedative, anticonvulsant and hypnotic effects, it is used in veterinary medicine for induction in surgical anaesthesia. Thiobutabarbital was formerly used as anesthetic Inactin. ‘Inactin’ (sodium thiobutabarbital) produces smooth induction of anaesthesia after intravenous administration and has a prolonged duration of action. It has variable analgesic activity.

Casopitant (GW679769) is a novel substituted piperidine derivative that competitively binds with NK1 receptors. The full occupancy of the receptor by their piperidine compound inhibits its binding with tachykinin neurotransmitters, including SP. Casopitant, in a series of in vitro and in vivo experimentations, has exhibited a potent NK1 receptor antagonism. On 29 May 2008, GlaxoSmithKline announced the submission of a new drug application to the FDA for intravenous and oral formulations of casopitant mesylate. This drug was proposed for the prevention of chemotherapy-induced nausea and vomiting as an add-on therapy to the standard dual therapy of 5-HT3 receptor antagonists + dexamethasone. The submission also included a proposed indication for postoperative nausea and vomiting prevention. Rezonic™ is the proposed trade name for casopitant mesylate in the United States; Zunrisa™ is the proposed trade name for casopitant mesylate for GlaxoSmithKline’s global group of companies. In September 2009, GlaxoSmithKline decided to discontinue all regulatory filings for casopitant based on an estimate of the amount of additional safety data.

Dipyrone, also known as Metamizole (INN), is an ampyrone sulfonate analgesic, antispasmodic and antipyretic. It was withdrawn from US market in 1977 on the basis of reports of agranulocytosis. Depyrone is still used to treat severe and diffucult for relieving pains of different origin; headache, tooth-ache, pains in the joints, muscles, following traumas and operations, gall and kidney colics, neurites, neuralgias, traumatic cerebrasthenia; inflammation of upper respiratory ways of microbial or virus origin; chorea; febrile states. Mechanism of action of dipyrone is complex. It is believed that dipyrone exerts its action by inhibiting COX-3, and activates opioid and cannabioid systems either itself, or by products of its metabolic degradation.

Mitiglinide is a drug for the treatment of type 2 diabetes currently marked under tradename Glufast. Glufast® is available as the tablet for oral use, containing 5 mg or 10 mg of Mitiglinide calcium hydrate. The recommended dose is 10 mg three times daily just before each meal (within 5 minutes). Mitiglinide was approved by Pharmaceuticals and Medical Devices Agency of Japan (PMDA) on January 29, 2004, and is currently co-marketed in Japan by Kissei and Takeda. Mitiglinide is a rapid-acting insulin secretion-stimulating agent, its belongs to the meglitinide (glinide) class of blood glucose-lowering drugs. Mitiglinide is thought to stimulate insulin secretion by closing the ATP-sensitive K(+) (K(ATP)) channels in pancreatic beta-cells.

BENFURODIL, a 5-benzofuran derivative, is an arterioleptic drug used in the treatment of different arteriopathies.

Butedronic acid is used for diagnostic purposes. Tetrasodium salt of butedronic acid is bone imaging agent.

Pefloxacin is a fluorinated quinolone that is structurally related to nalidixic acid. It can be administered both orally and intravenously, and has a broad spectrum of in vitro activity against Gram-negative organisms and staphylococci. The bactericidal action of pefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited. It is prescribed for the treatment of uncomplicated gonococcal urethritis in males and for gram-negative bacterial infections in gastrointestinal system and genitourinary tract.

Iocarmic acid is a molecule used in seventies as a contrast media for myelography. Iocarmate meglumine (Dimer-X), a water-soluble salt of iocarmic acid was reported to be safe and best tolerated by central nervous system compared to metrizamide in a double-blind test in patients with symptoms of lumbar and sacral root involvement. In the experimental and clinical studies of Dimer-X used for ventriculography the apparent superiority of Dimer-X over Conray 60 and Angiografin as far as side effects were concerned was demonstrated, but there were no particular differences in the intensities of the ventriculograms obtained. Morphological studies of the ventricles and histological examinations of the ventricular walls 1 month after injections of Dimer-X into the ventricles of dogs showed no abnormalities. In the clinical studies, ventriculography Dimer-X, performed on patients with diseases of the central nervous system, produced ventriculograms of good diagnostic value with no side effects, such as convulsions, apart from mild headache or vomiting in 4 instances. Ventriculography with Dimer-X was carried in 15 infants with myelomeningocele and progressive hydrocephalus. However, as was shown in a number of studies iocarmate produced moderate to severe arachnoiditis from myelography in primates. Early meningitis side effects following lumbar radiculography with iocarmate meglumine were demonstrated.

Flupirtine is a triaminopyridine derivative having a chemical structure - 2-amino-3-ethoxy-carbonylamino-6-4-fluoro-benzylamino-pyridine. The basic molecule used for synthesis of flupirtine was 2, 6-dichoro 3-nitropyridine. It was first synthesized in 1980s in Germany and was marketed by Degussa Pharma. Flupirtine is a centrally acting, non-opioid analgesic that is available in a number of European countries for the treatment of a variety of pain states. The therapeutic benefits seen with flupirtine relate to its unique pharmacological properties. Flupirtine displays indirect NDMA receptor antagonism via activation of potassium channels and is the first representative of a pharmacological class denoted the 'selective neuronal potassium channel openers'. The generation of the M-current is facilitated by flupirtine via the opening of neuronal Kv7 potassium channels. The opening of these channels inhibits exaggerated neuronal action potential generation and controls neuronal excitability. Neuronal hyperexcitability is a physiological component of many pain states such as chronic pain, migraine and neurogenic pain.