Antihistamine agent

Niperotidine is an H2 antagonist structurally related to ranitidine. H2 antagonists inhibit gastric acid secretion by selectively blocking histamine receptor type 2. Niperotidine was proposed for the treatment of peptic ulcer. Bedtime dose of niperotidine inhibits nocturnal gastric acid secretion in healthy subjects. The duration of niperotidine action was 5 to 7 hours. Twenty-five cases of acute hepatitis (including one death from fulminant hepatitis) associated with niperotidine use were reported in Italy between March and August 1995 and drug was withdrawn from the market. The methylenedioxy group of niperotidine is known to undergo metabolism to catechol and quinone metabolites.

Balofloxacin (Q-35), is an orally active fluoroquinolone antibiotic. It has been developed for the treatment of urinary tract infection. The bactericidal action of Balofloxacin results from interference with the enqyme DNA gyrase which is needed for the synthesis of bacterial DNA. Balofloxacin is efficacious against Gram-negative bacteria. It also has enhanced activity against Gram positive bacteria, including MRSA and Streptococcus pneumoniae. Side effects of Balofloxacin are: sensitivity to light, abdominal pain, nausea, heartburn, urticarial, irritation when applied locally. Balofloxacin may interact with the following medicines and salts: antacids, non-steroidal anti-inflammatory drug, quinolones, theophylline.

Acotiamide (Acofide(®)), an oral first-in-class prokinetic drug, is under global development by Zeria Pharmaceutical Co. Ltd and Astellas Pharma Inc. for the treatment of patients with functional dyspepsia. The drug modulates upper gastrointestinal motility to alleviate abdominal symptoms resulting from hypomotility and delayed gastric emptying. It exerts its activity in the stomach via muscarinic receptor inhibition, resulting in enhanced acetylcholine release and inhibition of acetylcholinesterase activity. Acofide® is launched in Japan for treating functional dyspepsia.

Prenoxdiazine under the brand name Libexin is used as an antitussive agent. It was shown, that the use of this drug for pregnant women with an unproductive cough could be beneficial.

Cinchonidine is an alkaloid found in Cinchona officinalis and Gongronema latifolium. Cinchonidine is an antimalarial drug which has been used clinically in malaria caused by Plasmodium falciparum. Cinchonidine is reported as an ingredient of Quinimax in a number of countries. Quinimax is a combination of four alkaloids (quinine, quinidine, cinchoine and cinchonidine).

Cinchonidine is an alkaloid found in Cinchona officinalis and Gongronema latifolium. Cinchonidine is an antimalarial drug which has been used clinically in malaria caused by Plasmodium falciparum. Cinchonidine is reported as an ingredient of Quinimax in a number of countries. Quinimax is a combination of four alkaloids (quinine, quinidine, cinchoine and cinchonidine).

Kainic acid (kainate) is a natural marine acid present in some seaweed. Kainic acid is a potent neuroexcitatory amino acid that acts by activating receptors for glutamate, the principal excitatory neurotransmitter in the central nervous system. Kainic acid is commonly injected into laboratory animal models to study the effects of experimental ablation. Kainic acid is a direct agonist of the glutamic kainate receptors and large doses of concentrated solutions produce immediate neuronal death by overstimulating neurons to death. Such damage and death of neurons is referred to as an excitotoxic lesion. Thus, in large, concentrated doses kainic acid can be considered a neurotoxin, and in small doses of dilute solution kainic acid will chemically stimulate neurons. Kainic acid is utilised in primary neuronal cell cultures and acute brain slice preparations [5] to study of the physiological effect of excitotoxicity and assess the neuroprotective capabilities of potential therapeutics. Kainic acid is a potent central nervous system excitant that is used in epilepsy research to induce seizures in experimental animals, at a typical dose of 10–30 mg/kg in mice. In addition to inducing seizures, kainic acid is excitotoxic and epileptogenic. Kainic acid induces seizures via activation of kainate receptors containing the GluK2 subunit and also through activation of AMPA receptors, for which it serves as a partial agonist.

Ipidacrine (Neiromidin) is a drug first synthesized by the National Research Center for Biologically Active Compounds in the Russian Federation. Neuromidin has a direct stimulating effect on the conduct of the pulse along the nerve fibers, interneuronal and neuromuscular synapses of the CNS and peripheral nervous system. Pharmacological action neuromidin is based on a combination of two mechanisms of action: blockade of potassium channels of the membrane of neurons and muscle cells; reversible inhibition of cholinesterase in synapses. Neuromidin enhances the effect on smooth muscle acetylcholine not only, but epinephrine, serotonin, histamine and oxytocin. It has the following pharmacological effects: - Improve and stimulate impulse conduction in the nervous system and neuromuscular transmission; - Enhances contractility of smooth muscle organs under the influence of acetylcholine agonists, adrenaline, serotonin, histamine and oxytocin receptors, with the exception of potassium chloride; - Improves memory, slows progressive course of dementia. In preclinical studies Neuromidin is not teratogenic, embryotoxic, mutagenic, carcinogenic and immunotoxic action, had no effect on the endocrine system

Ipidacrine (Neiromidin) is a drug first synthesized by the National Research Center for Biologically Active Compounds in the Russian Federation. Neuromidin has a direct stimulating effect on the conduct of the pulse along the nerve fibers, interneuronal and neuromuscular synapses of the CNS and peripheral nervous system. Pharmacological action neuromidin is based on a combination of two mechanisms of action: blockade of potassium channels of the membrane of neurons and muscle cells; reversible inhibition of cholinesterase in synapses. Neuromidin enhances the effect on smooth muscle acetylcholine not only, but epinephrine, serotonin, histamine and oxytocin. It has the following pharmacological effects: - Improve and stimulate impulse conduction in the nervous system and neuromuscular transmission; - Enhances contractility of smooth muscle organs under the influence of acetylcholine agonists, adrenaline, serotonin, histamine and oxytocin receptors, with the exception of potassium chloride; - Improves memory, slows progressive course of dementia. In preclinical studies Neuromidin is not teratogenic, embryotoxic, mutagenic, carcinogenic and immunotoxic action, had no effect on the endocrine system