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Restrict the search for
histamine
to a specific field?
Status:
US Approved Rx
(1997)
Source:
NDA020786
(1997)
Source URL:
First approved in 1996
Source:
ALLEGRA by CHATTEM SANOFI
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Fexofenadine is a second-generation, long lasting H1-receptor antagonist (antihistamine) which has a selective and peripheral H1-antagonist action. Histamine is a chemical that causes many of the signs that are part of allergic reactions, such as the swelling of tissues. Histamine is released from histamine-storing cells (mast cells) and attaches to other cells that have receptors for histamine. The attachment of the histamine to the receptors causes the cell to be "activated," releasing other chemicals which produce the effects that we associate with allergy. Fexofenadine blocks one type of receptor for histamine (the H1 receptor) and thus prevents activation of cells by histamine. Unlike most other antihistamines, Fexofenadine does not enter the brain from the blood and, therefore, does not cause drowsiness. Fexofenadine lacks the cardiotoxic potential of terfenadine, since it does not block the potassium channel involved in repolarization of cardiac cells. Fexofenadine is sold under the trade name Allegra among others. ALLEGRA is indicated for the relief of symptoms associated with seasonal allergic
rhinitis in adults and children 2 years of age and older.
Status:
US Approved Rx
(2012)
Source:
NDA202236
(2012)
Source URL:
First approved in 1996
Source:
ASTELIN by NORVIUM BIOSCIENCE
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Azelastine, a phthalazine derivative, is an antihistamine and mast cell stabilizer. Azelastine is oxidatively metabolized to the principal active metabolite, desmethylazelastine, by the cytochrome P450 enzyme system. It is indicated for the relief of the symptoms of seasonal allergic rhinitis and perennial allergic rhinitis. The most common adverse reactions are: pyrexia, dysgeusia, nasal discomfort, epistaxis, headache, sneezing, fatigue, somnolence, upper respiratory infection, cough, rhinalgia, vomiting, otitis media, contact dermatitis, and oropharyngeal pain. Concurrent use of Azelastine with alcohol or other central nervous system depressants should be avoided because reductions in alertness and impairment of central nervous system performance may occur.
Status:
US Approved Rx
(2015)
Source:
ANDA204812
(2015)
Source URL:
First approved in 1996
Source:
NDA020688
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Olopatadine is an antihistamine (as well as anticholinergic and mast cell stabilizer) used to treat itching associated with allergic conjunctivitis (eye allergies). Olopatadine is a selective histamine H1 antagonist that binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. Olopatadine is devoid of effects on alpha-adrenergic, dopamine and muscarinic type 1 and 2 receptors. Some known side effects include a headache (7% of occurrence), eye burning and/or stinging (5%), blurred vision, dry eyes, foreign body sensation, hyperemia, keratitis, eyelid edema, pruritus, asthenia, sore throat (pharyngitis), rhinitis, sinusitis, and taste perversion.
Status:
US Approved Rx
(2011)
Source:
ANDA091263
(2011)
Source URL:
First approved in 1995
Source:
NDA022064
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Levocetirizine dihydrochloride is the R enantiomer of cetirizine hydrochloride, a racemic compound with antihistaminic properties. Levocetirizine is a third-generation non-sedative antihistamine indicated for the relief of symptoms associated with seasonal and perennial allergic rhinitis and uncomplicated skin manifestations of chronic idiopathic urticaria. It was developed from the second-generation antihistamine cetirizine. Levocetirizine was approved by the United States Food and Drug Administration on May 25, 2007 and is marketed under the brand XYZAL. Its principal effects are mediated via selective inhibition of H1 receptors. The antihistaminic activity of levocetirizine has been documented in a variety of animal and human models. In vitro binding studies revealed that levocetirizine has an affinity for the human H1-receptor 2-fold higher than that of cetirizine (Ki = 3 nmol/L vs. 6 nmol/L, respectively). The clinical relevance of this finding is unknown.
Status:
US Approved Rx
(2011)
Source:
ANDA091263
(2011)
Source URL:
First approved in 1995
Source:
NDA022064
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Levocetirizine dihydrochloride is the R enantiomer of cetirizine hydrochloride, a racemic compound with antihistaminic properties. Levocetirizine is a third-generation non-sedative antihistamine indicated for the relief of symptoms associated with seasonal and perennial allergic rhinitis and uncomplicated skin manifestations of chronic idiopathic urticaria. It was developed from the second-generation antihistamine cetirizine. Levocetirizine was approved by the United States Food and Drug Administration on May 25, 2007 and is marketed under the brand XYZAL. Its principal effects are mediated via selective inhibition of H1 receptors. The antihistaminic activity of levocetirizine has been documented in a variety of animal and human models. In vitro binding studies revealed that levocetirizine has an affinity for the human H1-receptor 2-fold higher than that of cetirizine (Ki = 3 nmol/L vs. 6 nmol/L, respectively). The clinical relevance of this finding is unknown.
Status:
US Approved Rx
(2018)
Source:
ANDA208477
(2018)
Source URL:
First approved in 1993
Source:
NDA019658
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Loratadine is a derivative of azatadine and a second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (histamine H1 antagonists) it lacks central nervous system depressing effects such as drowsiness. Loratadine competes with free histamine and exhibits specific, selective peripheral H1 antagonistic activity. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms (eg. nasal congestion, watery eyes) brought on by histamine. Loratadine has low affinity for cholinergic receptors and does not exhibit any appreciable alpha-adrenergic blocking activity in-vitro. Loratadine also appears to suppress the release of histamine and leukotrienes from animal mast cells, and the release of leukotrienes from human lung fragments, although the clinical importance of this is unknown.
Status:
US Approved Rx
(1993)
Source:
NDA020191
(1993)
Source URL:
First approved in 1993
Source:
NDA020191
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Lodoxamide is a mast-cell stabilizer for topical administration into the eye. This compound belongs to the class of organic compounds known as alpha amino acids and derivatives. Lodoxamide inhibits the in vivo Type I immediate hypersensitivity reaction. In vitro, Lodoxamide stabilizes mast cells and prevents antigen-stimulated release of histamine. In addition, Lodoxamide prevents the release of other mast cell inflammatory mediators and inhibits eosinophil chemotaxis. Although Lodoxamide's precise mechanism of action is unknown, the drug has been reported to prevent calcium influx into mast cells upon antigen stimulation. Among side effects to Lodoxamide, the most frequently reported ocular adverse experiences were transient burning, stinging, or discomfort upon instillation. Nonocular events reported were headache and heat sensation, dizziness, somnolence, nausea, stomach discomfort, sneezing, dry nose, and rash.
Status:
US Approved Rx
(2008)
Source:
ANDA078412
(2008)
Source URL:
First approved in 1988
Source:
ANDA077170
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Cetirizine, a human metabolite of hydroxyzine, is an antihistamine; its principal effects are mediated via selective inhibition of peripheral H1 receptors. It is indicated for the relief of nasal and non-nasal symptoms associated with seasonal or perennial allergic rhinitis, hay fever and chronic idiopathic urticaria. Commonly reported adverse reactions of cetirizine include headache, dry mouth and drowsiness or fatigue. Pharmacokinetic interaction studies with Cetirizine in adults were conducted with pseudoephedrine, antipyrine, ketoconazole, erythromycin and azithromycin. No interactions were observed.
Status:
US Approved Rx
(2014)
Source:
ANDA201995
(2014)
Source URL:
First approved in 1986
Source:
PEPCID by BAUSCH
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Famotidine, a competitive histamine H2-receptor antagonist, is used to treat gastrointestinal disorders such as gastric or duodenal ulcer, gastroesophageal reflux disease, and pathological hypersecretory conditions. Famotidine inhibits many of the isoenzymes of the hepatic CYP450 enzyme system. Other actions of Famotidine include an increase in gastric bacterial flora such as nitrate-reducing organisms. Famotidine binds competitively to H2-receptors located on the basolateral membrane of the parietal cell, blocking histamine affects. This competitive inhibition results in reduced basal and nocturnal gastric acid secretion and a reduction in gastric volume, acidity, and amount of gastric acid released in response to stimuli including food, caffeine, insulin, betazole, or pentagastrin.
Status:
US Approved Rx
(2000)
Source:
ANDA075294
(2000)
Source URL:
First approved in 1983
Source:
ZANTAC 150 by GLAXO GRP LTD
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Ranitidine, a histamine H2-receptor antagonist, is now well established as a potent inhibitor of gastric acid secretion effective in the treatment and prophylaxis of gastrointestinal lesions aggravated by gastric acid secretion.
