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(ăn'tĭhĭs`təmēn), any one of a group of compounds having various chemical structures and characterized by the ability to antagonize the effects of histaminehistamine
, organic compound derived in the body from the amino acid histidine by the removal of a carboxyl group (COOH). Although found in many plant and animal tissues, histamine is specifically important in human physiology because it is one of the chemicals released from
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. Their principal use in medicine is in the control of allergies such as hay fever and hives. Some antihistamines are also useful as sedatives and for the prevention of motion sickness; others, such as fexofenadine (Allegra) and loratadine (Claritin) are nonsedating.
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A type of drug that inhibits the combination of histamine with histamine receptors. These drugs are termed either H-1 or H-2 receptor antagonists depending on which type of histamine receptor is involved. H-1 receptor antagonists are used largely for treating allergies, and H-2 receptor antagonists are used to treat peptic ulcer disease and related conditions. See Histamine

The primary therapeutic use of H-1 receptor antagonists is to antagonize the effects of histamine released from cells by antigen-antibody reactions; they can thus inhibit histamine-induced effects, such as bronchoconstriction, skin reactions, for example, wheals and itching, and nasal inflammation. These drugs, therefore, are quite effective in reducing allergy signs and symptoms, especially if they are administered before contact with the relevant antigen; however they are not effective in treating asthma. Their effects vary widely, both among the drugs and from individual to individual; in young children excitement may be seen. Another common set of effects caused by many of these drugs, including dry mouth, blurred vision, and urinary retention, can be ascribed to their anticholinergic actions. H-1 receptor antagonists have low toxicity. The chief adverse effect is sedation. Overdoses of H-1 receptor antagonists may be associated with excitement or depression, and although there is no pharmacologic antidote for these drugs, good supportive care should be adequate in managing cases of poisoning. See Allergy, Antigen-antibody reaction

H-2 receptor antagonists are much newer. Histamine stimulates gastric acid secretion by combining with H-2 receptors. By preventing this combination, H-2 antagonists can reduce acid secretion in the stomach, an effect that makes these drugs useful in managing various conditions, such as peptic ulcer disease.

Other conditions in which H-2 antagonists are used to lower gastric acidity include reflux esophagitis, stress ulcers, and hypersecretory states such as the Zollinger-Ellison syndrome, in which tumor cells secrete large amounts of the hormone gastrin, which stimulates gastric acid secretion. In these conditions, administration of H-2 antagonists reduces symptoms and promotes healing.

The toxicity of H-2 antagonists is quite low, and adverse effects are reported by only 1-2% of patients. The most common side effects are gastrointestinal upsets, including nausea, vomiting, and diarrhea.

McGraw-Hill Concise Encyclopedia of Bioscience. © 2002 by The McGraw-Hill Companies, Inc.


A drug that prevents or diminishes the effect of histamine; used in treating allergic reactions and common-cold symptoms.
McGraw-Hill Dictionary of Scientific & Technical Terms, 6E, Copyright © 2003 by The McGraw-Hill Companies, Inc.


any drug that neutralizes the effects of histamine, used esp in the treatment of allergies
Collins Discovery Encyclopedia, 1st edition © HarperCollins Publishers 2005
References in periodicals archive ?
The use of levocabastine contributed to the decrease in the serum levels of histamine, IL-6 and IgE by 33.9% (p<0.05); 23.3% (p<0.05) and 91.9% (p<0.05), respectively, while nasal administration of levocabastine did not significantly affect the change in the concentration of IFN-[gamma] and TNF-[alpha] (there were no statistically significant differences with regard to NC group of animals is not established).
At the same time, the content of histamine, IL-6, IgE, and TNF-[alpha] in mice that were injected with the test spray at a dose of 5 [micro]g, was 26.2% (p<0.05); 81.2% (p<0.05); 81.4% (p<0.05) and 52.1% (p<0.05) are lower in relation to mice treated with levocabastine.
This is comparable to the cost of ophthalmic cromolyn, and lower than that of the ophthalmic antihistamine, levocabastine, which costs approximately $2.35 per day, said Dr.
For sufferers of seasonal allergic conjunctivitis, Iolab has received approval to market levocabastine HCl, an antihistamine for topical use.
One study used azelastine nasal spray as comparator, in the second study a nasal spray based on cromoglicic acid served as control medication, the third study investigated ectoine nasal spray versus levocabastine (Livocab) with beclomethasone nasal spray, and the paediatric study was set up as a placebo-controlled trial.