- Drugs and Lactation Database (LactMed): Azatadine [BOOK]Drugs and Lactation Database (LactMed). National Library of Medicine (US): Bethesda (MD)BOOK
- Small occasional doses of azatadine are probably acceptable during breastfeeding. Larger doses or more prolonged use may cause drowsiness and other effects in the infant or decrease the milk supply, particularly in combination with a sympathomimetic such as pseudoephedrine or before lactation is well established. The nonsedating antihistamines are preferred alternatives.
- Use of Phenotypically Poor Metabolizer Individual Donor Human Liver Microsomes To Identify Selective Substrates of UGT2B10. [Journal Article]
- UDP-glucuronosyltransferase (UGT)1A4 and UGT2B10 are the human UGT isoforms most frequently involved in N-glucuronidation of drugs. UGT2B10 exhibits higher affinity than UGT1A4 for numerous substrates, making it potentially the more important enzyme for metabolism of these compounds in vivo. Clinically relevant UGT2B10 polymorphisms, including a null activity splice site mutation common in Africa…
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- Report: A comparative study of loratidine physiochemical properties from different brands. [Journal Article]Pak J Pharm Sci. 2018 Nov; 31(6):2569-2574.PJ
- Loratidine is a piperidine derivative resemble to azatadine long acting non sedating commonly used for the treatment of allergic condition like watery or itchy eyes, runny nose, chronic urticaria or throat itching. In the present study different brands of loratidine were evaluated for the weight variation, hardness, friability, disintegration time and dissolution. Dissolution release study perfor…
- Determination of azatadine in human plasma by liquid chromatography/tandem mass spectrometry. [Journal Article]
- A sensitive method using liquid chromatography with tandem mass spectrometric detection (LC-MS/MS) was developed and validated for the analysis of antihistamine drug azatadine in human plasma. Loratadine was used as internal standard (IS). Analytes were extracted from human plasma by liquid/liquid extraction using ethyl acetate. The organic phase was reduced to dryness under a stream of nitrogen …
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- Application of dummy molecularly imprinted solid-phase extraction in the analysis of cyproheptadine in bovine urine. [Journal Article]J Sep Sci. 2009 May; 32(10):1740-7.JS
- Due to the difficulty of monitoring trace levels of cyproheptadine (CYP) residues in complicated biological matrices, specific adsorption materials for the preconcentration and clean-up of CYP are indispensable. In this work, CYP was extracted from urine using dummy molecularly imprinted SPE (DMISPE) to avoid leakage of the imprinting molecules during the desorption phase. For synthesis of DMISPE…
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- Syntheses of molecularly imprinted polymers: Molecular recognition of cyproheptadine using original print molecules and azatadine as dummy templates. [Journal Article]
- The use of custom-made polymeric materials with high selectivities as target molecules in solid-phase extraction (SPE), known as molecularly imprinted solid-phase extraction (MISPE), is becoming an increasingly important sample preparation technique. However, the potential risk of leakage of the imprinting molecules during the desorption phase has limited application. The use of a mimicking templ…
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- Antihistamines in the treatment of dermatitis. [Review]
- CONCLUSIONS: Dermatologists require additional evidence regarding the efficacy of antihistamines and their mechanism of action in the treatment of AD to enhance patient care.
- The use of antiserotonin drugs in the nucleoreticular vestibular syndrome: preliminary observations. [Journal Article]Int Tinnitus J. 2004; 10(1):84-6.IT
- Vestibular neuronitis was described in 1949 and 1952 by Dix and Hallpike. Two groups of patients were described, those with sudden seizures and sensations of blackout (since identified as having vestibular neuritis) and a second group with symptoms of disequilibrium and feelings of top-heaviness or imbalance. The pathology was believed to be central to the inner ear. Arslan labeled these groups a…
- Antiallergic anti-inflammatory effects of H1-antihistamines in humans. [Review]
- Data from in vitro, in vivo, and ex vivo studies suggest that second-generation antihistamines have a number of antiallergic, anti-inflammatory properties that appear to be independent of their H1-blockade activity. First-generation antihistamines also have antiallergic, anti-inflammatory properties, as suggested by the studies with azatadine, chlorpheniramine, mepyramine, and promethazine; most …
- Quantitation of antihistamines in pharmaceutical preparations by liquid chromatography with a micellar mobile phase of sodium dodecyl sulfate and pentanol. [Journal Article]J AOAC Int. 2001 Nov-Dec; 84(6):1687-94.JA
- A reversed-phase liquid chromatographic procedure with a micellar mobile phase of sodium dodecyl sulfate (SDS), containing a small amount of pentanol, was developed for the control of 7 antihistamines of diverse action in pharmaceutical preparations (tablets, capsules, powders, solutions, and syrups): azatadine, carbinoxamine, cyclizine, cyproheptadine, diphenhydramine, doxylamine, and tripelenna…
- Chromatographic analysis of phenethylamine-antihistamine combinations using C8, C18 or cyano columns and micellar sodium dodecyl sulfate-pentanol mixtures. [Journal Article]
- The chromatographic behaviour of binary and ternary mixtures of several phenethylamines (phenylephrine, phenylpropanolamine, ephedrine, pseudoephedrine and methoxyphenamine) and antihistamines (pheniramine, carbinoxamine, doxylamine, chlorpheniramine, dexchlorpheniramine, dexbrompheniramine, diphenhydramine, tripolidine, azatadine and phenyltoloxamine), found in cough-cold pharmaceutical preparat…
- Antiallergic effects of H1-receptor antagonists. [Review]
- The primary mechanism of antihistamine action in the treatment of allergic diseases is believed to be competitive antagonism of histamine binding to cellular receptors (specifically, the H1-receptors), which are present on nerve endings, smooth muscles, and glandular cells. This notion is supported by the fact that structurally unrelated drugs antagonize the H1-receptor and provide clinical benef…
- Interaction between chloroquine and diverse pharmacological agents in chloroquine resistant Plasmodium yoelii nigeriensis. [Journal Article]
- The effect of a number of pharmacological agents on the enhancement of antimalarial activity of chloroquine was evaluated against chloroquine resistant line of Plasmodium yoelii nigeriensis (N-67). The response after combination therapy was monitored on the basis of alteration in the course of parasitaemia, the extension of mean survival time and the percent cure rate in different groups. The stu…
- Hydroxyzine inhibits neurogenic bladder mast cell activation. [Journal Article]
- CONCLUSIONS: Hydroxyzine reduced carbachol-induced serotonin release from rat bladder in vitro through a mechanism which was unrelated to its H-1 receptor antagonistic properties. The ability of hydroxyzine to inhibit bladder mast cell activation by neurogenic stimuli along with its anticholinergic, anxiolytic and analgesic properties, may explain the clinical efficacy of this drug in reducing IC symptoms. Other, nonsedating, hydroxyzine analogues able to inhibit bladder mast cell activation may provide potentially new therapeutic approaches for IC.
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- Causal prophylactic activity of antihistaminic agents against Plasmodium yoelii nigeriensis infection in Swiss mice. [Journal Article]
- The causal prophylactic activity of five tricyclic anti-histaminic agents (histamine H1-receptor antagonists) cyproheptadine, ketotifen, loratadine, azatadine and terfenadine was evaluated in an experimental murine malaria model. Sporozoite induced infections with Plasmodium yoelii nigeriensis (N-67), a strain innately resistant to choloroquine, were employed for the efficacy test and pyrimethami…
- Fungal biotransformation of the antihistamine azatadine by Cunninghamella elegans. [Journal Article]
- The metabolism of the antihistamine azatadine by the zygomycete fungus Cunninghamella elegans ATCC 9245 was investigated. Within 72 h from the addition of the drug to 48-h-old cultures grown in Sabouraud dextrose broth, 95% of azatadine was biotransformed. Two major metabolites, 7-hydroxyazatadine (25%) and 8-hydroxyazatadine (50%), and two minor metabolites, N-desmethylazatadine and 9-hydroxyaza…
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- Loratadine. A reappraisal of its pharmacological properties and therapeutic use in allergic disorders. [Review]
- Loratadine is a long-acting antihistamine agent, exhibiting partial selectivity for peripheral histamine H1-receptors. To date, loratadine has been evaluated in allergic rhinitis, urticaria and, to a limited extent, in asthma. In several large controlled comparative clinical studies, loratadine was superior to placebo, faster acting than astemizole and as effective as azatadine, cetirizine, chlor…
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- An algorithmic approach to chronic cough. [Journal Article]
- CONCLUSIONS: A sequential approach to chronic cough that emphasizes initial treatment with an antihistamine-decongestant is effective. Bronchoprovocation challenge is useful in evaluating patients with chronic cough but can be delayed until the initial response to antihistamine-decongestant therapy has been assessed. The 18% incidence of recurrence highlights the fact that cough often is the manifestation of a chronic or recurring process that requires chronic or episodic therapy.
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- The effect of antihistamines on the immediate allergic response: a comparative review. [Randomized Controlled Trial]
- Antihistamines are believed to reduce the sneezing and rhinorrhea associated with allergic rhinitis, primarily by competitive antagonism of histamine for H1 cellular receptors, but additional mechanisms of action may contribute to their clinical efficacy. To improve our understanding of H1 antihistamine action, we studied the effects of pretreatment with terfenadine, cetirizine, ketotifen, azatad…
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- Discovery and preliminary pharmacology of Sch 37370, a dual antagonist of PAF and histamine. [Journal Article]
- From a series of amide analogs of the histamine H1 antagonist, azatadine, a potent, orally active, dual platelet-activating factor (PAF) and histamine antagonist, Sch 37370, namely 1-acetyl-4-(8-chloro-5,6-dihydro-11H-benzo- [5,6]cyclohepta[1,2-b]pyridin-11-ylidine)piperidine, was discovered. Sch 37370 selectively inhibits PAF-induced aggregation of human platelets in vitro (IC50 = 0.6 microM), a…
- Chloroquine-potentiating action of antihistaminics in Plasmodium falciparum in vitro. [Journal Article]
- Tricyclic antihistaminics have relatively few side-effects compared to other agents that enhance the susceptibility to chloroquine of chloroquine-resistant strains of Plasmodium falciparum. Their efficacy was tested in vitro against resistant and sensitive culture-adapted strains of P. falciparum. Isobologram analysis showed that both cyproheptadine and azatadine exert a marked synergistic action…
- Comparative effects of loratadine and azatadine in the treatment of seasonal allergic rhinitis. [Randomized Controlled Trial]
- The efficacy and safety of loratadine 10 mg once daily were compared with azatadine 1 mg twice daily in controlling symptoms of seasonal allergic rhinitis. The study was a randomized, double-blind, parallel-group design involving 34 patients receiving either loratadine or azatadine for 14 days. Both treatments were effective in relieving the histamine-mediated symptoms of seasonal allergic rhinit…
- The chemotherapy of rodent malaria. XLV. Reversal of chloroquine resistance in rodent and human Plasmodium by antihistaminic agents. [Journal Article]
- The inherent blood schizontocidal activities of five antihistaminic compounds, cyproheptadine hydrochloride (CYP), ketotifen hydrogen fumarate (KET), pizotyline hydrogen maleate (PIZ), azatadine maleate (AZAT) and loratadine (LOR) were examined against the following organisms: chloroquine-sensitive (CS) Plasmodium berghei and chloroquine-resistant (CR) P. yoelii ssp. NS in mice; and CS Tak 9 clon…
- The effects of antihistamines beyond H1 antagonism in allergic inflammation. [Randomized Controlled Trial]
- Antigen and cold dry air were used to challenge the upper and lower airways, skin, and conjunctiva. In each of these four systems an immediate and late-phase reaction to antigen is well characterized. Although the pattern of mediator release is different in these four areas, the degree of infiltration of basophils and eosinophils in the late-phase reaction appears to be constant. Of a number of d…
- Effects of azatadine, terfenadine, and astemizole on allergen-induced nasal provocation. [Randomized Controlled Trial]
- Fifty-six patients with ragweed seasonal rhinitis were challenged intranasally with ragweed. A clinical score (0-12)--including measurements of rhinomanometry, secretions, and sneezes--was generated. Each patient then received either azatadine (A), terfenadine (T), astemizole (AS), or nothing (control), for 1 week. Repeat challenges revealed changes in clinical score with A 3.6 (P less than .01),…
- In vivo and in vitro effects of antihistamines on mast cell mediator release: a potentially important property in the treatment of allergic disease. [Controlled Clinical Trial]
- A nasal antigen challenge model of allergic individuals was used to evaluate whether antihistamines could inhibit human mast cell and basophil mediator release in vivo. In placebo-controlled trials, topically applied azatadine base, a tricyclic antihistamine with in vitro antirelease action, effectively reduced symptoms and mediator levels in nasal lavage fluids after antigen challenge, suggestin…
- Arabinogalactan- and dextran-induced ear inflammation in mice: differential inhibition by H1-antihistamines, 5-HT-serotonin antagonists and lipoxygenase blockers. [Journal Article]
- Intravenous injection of arabinogalactan or dextran together with pontamine sky-blue dye into mice increased vascular permeability and led to marked blueing of the ears. Arabinogalactan caused a rapidly progressing ear blueing (maximal coloration 20-30 min after injection). This response was suppressed by pretreating the animals with the histamine H1-antihistamines levocabastine and loratadine. I…
- Nonsedating histamine H1-receptor antagonists. [Review]
- The chemistry, pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosages of the nonsedating histamine H1-receptor antagonists terfenadine, astemizole, loratadine, and acrivastine are reviewed. Terfenadine and astemizole are chemically unrelated to histamine H1-receptor antagonists such as diphenhydramine and chlorpheniramine. Loratadine is structurally related to the antihis…
- "In vivo" and "in vitro" evaluation of four antihistamines (astemizole, azatadine, mequitazine, terfenadine). [Journal Article]
- A group of 32 patients with perennial allergic rhinitis sensitized exclusively to house dust and mites were evaluated for "in vivo" modifications (skin tests for histamine, house dust and mites) and "in vitro" alterations (seric IgE, specific IgE, histamine release curve to different concentrations of Dermatophagoides pteronyssinus and histamine release curve to this pneumoallergen after incubati…
- Loratadine. A preliminary review of its pharmacodynamic properties and therapeutic efficacy. [Review]
- Loratadine is a long acting antihistamine which has a high selectivity for peripheral histamine H1-receptors and lacks the central nervous system depressant effects often associated with some of the older antihistamines. Results from controlled clinical trials have shown that loratadine (usually 10mg once daily) is a well-tolerated and effective antihistamine which will be beneficial in patients …