| Attributes | Values |
|---|
| rdf:type
| |
| http://linked.open...gbank/description
| - Astemizole is a long-acting, non-sedating second generation antihistamine used in the treatment of allergy symptoms. It was withdrawn from market by the manufacturer in 1999 due to the potential to cause arrhythmias at high doses, especially when when taken with CYP inhibitors or grapefruit juice. (en)
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| http://linked.open...generalReferences
| - # Wang X, Hockerman GH, Green HW 3rd, Babbs CF, Mohammad SI, Gerrard D, Latour MA, London B, Hannon KM, Pond AL: Merg1a K+ channel induces skeletal muscle atrophy by activating the ubiquitin proteasome pathway. FASEB J. 2006 Jul;20(9):1531-3. Epub 2006 May 24. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16723379 # Chong CR, Chen X, Shi L, Liu JO, Sullivan DJ Jr: A clinical drug library screen identifies astemizole as an antimalarial agent. Nat Chem Biol. 2006 Aug;2(8):415-6. Epub 2006 Jul 2. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16816845 (en)
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| http://linked.open...gy/drugbank/group
| - approved (en)
- withdrawn (en)
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| http://linked.open...drugbank/halfLife
| |
| http://linked.open...ugbank/indication
| - Astemizole was indicated for use in the relieving allergy symptoms, particularly rhinitis and conjunctivitis. It has been withdrawn from the market however due to concerns of arrhythmias. (en)
|
| sameAs
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| Title
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| adms:identifier
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| http://linked.open...mechanismOfAction
| - Astemizole competes with histamine for binding at H<sub>1</sub>-receptor sites in the GI tract, uterus, large blood vessels, and bronchial muscle. This reversible binding of astemizole to H<sub>1</sub>-receptors suppresses the formation of edema, flare, and pruritus resulting from histaminic activity. As the drug does not readily cross the blood-brain barrier and preferentially binds at H1 receptors in the peripehery rather than within the brain, CNS depression is minimal. Astemizole may also act on H<sub>3</sub>-receptors, producing adverse effects. (en)
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| http://linked.open.../drugbank/synonym
| - Astemison (en)
- 1-(P-Fluorobenzyl)-2-((1-(2-(P-methoxyphenyl)ethyl)piperid-4-yl)amino)benzimidazole (en)
- Astemizol (en)
- Astemizolum (en)
- Astémizole (en)
- 1-(P-Fluorobenzyl)-2-((1-(P-methoxyphenethyl)-4-piperidyl)amino)benzimidazole (en)
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| http://linked.open...drugbank/toxicity
| - LD<sub>50</sub>=2052mg/kg in mice (en)
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| http://linked.open...k/foodInteraction
| - Take on an empty stomach, food decreases absorption by 60%. (en)
|
| http://linked.open...nk/proteinBinding
| |
| http://linked.open...ynthesisReference
| - Godelieve Irma Christine Maria Heylen, Cornelus Gerardus Maria Janssen, Jurzak Mirek, Henricus Petrus Martinus Maria Van Assouw, "Radiolabeled astemizole and method of making." U.S. Patent US07541476, issued June 02, 2009. (en)
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| foaf:page
| |
| http://linked.open...ugbank/IUPAC-Name
| |
| http://linked.open...gy/drugbank/InChI
| |
| http://linked.open...Molecular-Formula
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| http://linked.open.../Molecular-Weight
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| http://linked.open...noisotopic-Weight
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| http://linked.open...y/drugbank/SMILES
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| http://linked.open.../Water-Solubility
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| http://linked.open...ogy/drugbank/logP
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| http://linked.open...ogy/drugbank/logS
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| http://linked.open...l/drug/hasATCCode
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| http://linked.open...nd-Acceptor-Count
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| http://linked.open...-Bond-Donor-Count
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| http://linked.open...drugbank/InChIKey
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| http://linked.open...urface-Area--PSA-
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| http://linked.open...nk/Polarizability
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| http://linked.open...bank/Refractivity
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| http://linked.open...atable-Bond-Count
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| http://linked.open...ugbank/absorption
| - Rapidly absorbed from the gastrointestinal tract. (en)
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| http://linked.open.../affectedOrganism
| - Humans and other mammals (en)
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| http://linked.open...casRegistryNumber
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| http://linked.open...drugbank/category
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| http://linked.open...k/Bioavailability
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| http://linked.open...bank/Ghose-Filter
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| http://linked.open...nk/MDDR-Like-Rule
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| http://linked.open...ank/Melting-Point
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| http://linked.open...k/Number-of-Rings
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| http://linked.open...siological-Charge
| |
| http://linked.open...bank/Rule-of-Five
| |
| http://linked.open...tional-IUPAC-Name
| |
| http://linked.open...-strongest-basic-
| |
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