Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C27H30N4O.H2O |
| Molecular Weight | 444.5686 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
O.O=C1NC2=CC=CC=C2N1CCCN3CCN(CC3)C(C4=CC=CC=C4)C5=CC=CC=C5
InChI
InChIKey=WUVRHFANMRXNRX-UHFFFAOYSA-N
InChI=1S/C27H30N4O.H2O/c32-27-28-24-14-7-8-15-25(24)31(27)17-9-16-29-18-20-30(21-19-29)26(22-10-3-1-4-11-22)23-12-5-2-6-13-23;/h1-8,10-15,26H,9,16-21H2,(H,28,32);1H2
DescriptionCurator's Comment: description was created based on several sources, including, http://www.hindawi.com/journals/jphar/2013/629593/
Curator's Comment: description was created based on several sources, including, http://www.hindawi.com/journals/jphar/2013/629593/
Oxatomide is a H1-histamine receptor antagonist developed for the treatment of broad spectrum of allergic and other hypersensitivity reactions. The drug is currently marketed in Japan, Taiwan, Italy, Portugal, Indonesia, Argentina, South Africa.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: P35367 Gene ID: 3269.0 Gene Symbol: HRH1 Target Organism: Homo sapiens (Human) |
6.23 null [pIC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | TINSET Approved UsePrevention and treatment of allergic diseases: rhinitis, extrinsic asthma (excluding asthma attacks), follicular conjunctivitis, chronic urticaria, atopic dermatitis, food allergies. Launch Date2014 |
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| Primary | TINSET Approved UsePrevention and treatment of allergic diseases: rhinitis, extrinsic asthma (excluding asthma attacks), follicular conjunctivitis, chronic urticaria, atopic dermatitis, food allergies. Launch Date2014 |
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| Palliative | TINSET Approved UsePrevention and treatment of allergic diseases: rhinitis, extrinsic asthma (excluding asthma attacks), follicular conjunctivitis, chronic urticaria, atopic dermatitis, food allergies. Launch Date2014 |
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| Primary | TINSET Approved UsePrevention and treatment of allergic diseases: rhinitis, extrinsic asthma (excluding asthma attacks), follicular conjunctivitis, chronic urticaria, atopic dermatitis, food allergies. Launch Date2014 |
|||
| Primary | TINSET Approved UsePrevention and treatment of allergic diseases: rhinitis, extrinsic asthma (excluding asthma attacks), follicular conjunctivitis, chronic urticaria, atopic dermatitis, food allergies. Launch Date2014 |
|||
| Primary | TINSET Approved UsePrevention and treatment of allergic diseases: rhinitis, extrinsic asthma (excluding asthma attacks), follicular conjunctivitis, chronic urticaria, atopic dermatitis, food allergies. Launch Date2014 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Inhibition of mediator release in RBL-2H3 cells by some H1-antagonist derived anti-allergic drugs: relation to lipophilicity and membrane effects. | 1995 Feb |
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| Effect of oxatomide, an antiallergic agent, on QT interval in dogs. | 2001 |
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| Oxatomide in the treatment of atopic dermatitis in breast-fed and very young infants. | 2001 Aug |
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| Double-blind multicenter study on the efficacy and tolerability of cetirizine compared with oxatomide in chronic idiopathic urticaria in preschool children. | 2001 Jul |
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| Change in tissue kallikrein level in nasal wash after the administration of oxatomide in patients with nasal allergy. | 2001 Mar-Apr |
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| The role of central histaminergic neuron system as an anticonvulsive mechanism in developing brain. | 2001 Nov |
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| Preclinical comparison of ebastine and other second generation H1-antihistamines. | 2001 Oct |
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| Circumvention of acquired resistance to doxorubicin in K562 human leukemia cells by oxatomide. | 2001 Oct |
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| Pharmacokinetics of oxatomide in preterm infants. | 2002 |
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| High-performance liquid chromatographic determination of oxatomide and its metabolite and its application to pharmacokinetic study in rat plasma. | 2002 |
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| The comparison of the efficacy and safety of cetirizine, oxatomide, ketotifen, and a placebo for the treatment of childhood perennial allergic rhinitis. | 2002 Dec |
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| Gateways to clinical trials. | 2002 Jan-Feb |
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| Drug eruption and liver injury caused by terfenadine and oxatomide. | 2002 Jul-Aug |
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| Enhancement of allergic skin wheal responses in patients with atopic eczema/dermatitis syndrome by playing video games or by a frequently ringing mobile phone. | 2003 Jun |
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| Dietary intake of the flower extracts of German chamomile (Matricaria recutita L.) inhibited compound 48/80-induced itch-scratch responses in mice. | 2003 Nov |
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| West syndrome associated with administration of a histamine H1 antagonist, oxatomide. | 2004 |
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| Cetirizine: a review of its use in allergic disorders. | 2004 |
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| Hydroxyzine and metabolites as a source of interference in carbamazepine particle-enhanced turbidimetric inhibition immunoassay (PETINIA). | 2005 Aug |
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| Identification of human P450 isoforms involved in the metabolism of the antiallergic drug, oxatomide, and its kinetic parameters and inhibition constants. | 2005 Feb |
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| Nimesulide-induced fixed drug eruption. | 2005 Sep-Oct |
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| [Comparison of clinical efficacy and cost-quality of antihistamines in early treatment for Japanese cedar pollinosis]. | 2006 May |
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| Effect of inhibitor of tumor necrosis factor-alpha and oxatomide on immune mediated otitis media. | 2006 Sep |
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| Inhibition of angiogenic factor production from murine mast cells by an antiallergic agent (epinastine hydrochloride) in vitro. | 2008 |
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| Intact cell binding for in vitro prediction of sedative and non-sedative histamine H1-receptor antagonists based on receptor internalization. | 2008 May |
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| Development of a list of potentially inappropriate drugs for the korean elderly using the delphi method. | 2010 Dec |
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| An integrative review of systematic reviews related to the management of breathlessness in respiratory illnesses. | 2010 Dec 9 |
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| Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2. | 2011 Jul 14 |
Sample Use Guides
Oxatomide should be taken twice daily, after breakfast and after dinner: 30 mg for adults and 0.5 mg/kg for children older tan 1 year.
Route of Administration:
Oral
The effect of oxatomide on the immunologic release of preformed (histamine and tryptase) and de novo synthesized mediators (leukotriene C4:LTC4 and prostaglandin D2:PGD2) from human basophils and mast cells purified (from 10 to 82%) from human lung parenchyma (HLMC) and skin tissue (HSMC) was studied in vitro. Preincubation (15 min, 37 degrees C) of basophils with oxatomide (10(-7)-10(-5) M) before Der p I antigen or anti-IgE challenge concentration-dependently (10-40%) inhibited the immunologic release of histamine and LTC4. Oxatomide (10(-7)-10(-5) M) also inhibited (10-40%) histamine, tryptase and LTC4 release from HLMC activated by anti-IgE. In addition, oxatomide caused a concentration-dependent inhibition of histamine, tryptase and PGD2 release from HSMC immunologically challenged with a monoclonal antibody against the alpha chain of the high affinity receptor for IgE (anti-Fc epsilon RI) or anti-IgE.
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ACTIVE MOIETY
SUBSTANCE RECORD
