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Astemizole
drug data and news
Astemizole drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Astemizole | ||
| Brand Names/Synonyms | Alermizol; Astemisan; Astemisol; Astemison; Astemizole; Hismanal; Histamen; Histaminos; Histazol; Kelp; Laridal; Metodik; Nono-Nastizol A; Paralergin; Retolen; Waruzol | ||
| Indication | For the relief of symptoms associated with seasonal allergic rhinitis and chronic idiopathic urticaria | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Astemizole, an H1-receptor antagonist, is similar in structure to terfenadine and haloperidol, a butyrophenone antipsychotic. It has anticholinergic (atropine-like) and antipruritic effects. | ||
| Mechanism Of Action | Astemizole competes with histamine for binding at H1-receptor sites in the GI tract, uterus, large blood vessels, and bronchial muscle. This reversible binding of astemizole to H1-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 H3-receptors, producing adverse effects. | ||
| Astemizole News (When available) |
Roche to Focus Resources on Availability of Invirase, Now ... Feb 6, 2006 Boehringer Ingelheim Announces 48-week Results from Aptivus(R) ... Feb 9, 2006 Boehringer Ingelheim Announces 48-week Results from Aptivus(R) ... 09 Feb 2006 Roche to Focus Resources on Availability of Invirase, Now ... Feb 6, 2006 FDA Approves EMEND(R) (aprepitant), in Combination with Other ... Jan 11, 2006 Bristol-Myers Squibb and Gilead Announce Data Supporting ... Jan 9, 2006 Companies Anticipate Filing New Drug Application in Second Quarter ... Jan 9, 2006 FDA Approves EMEND® (aprepitant), in Combination with Other ... Jan 11, 2006 New Data Show a Kaletra(R) (Lopinavir/Ritonavir)-Based Regimen ... Nov 18, 2005 Boehringer Ingelheim Announces 48-Week Results from Aptivus(R) ... Nov 21, 2005 Invasive aspergillosis survival, Voriconazole may be better than ... Nov 19, 2005 Former FDA Commissioner’s Ownership of Stock in Regulated ... Oct 30, 2005 New analysis supports starting with VFEND for life-threatening ... Oct 29, 2005 I wish my straight friends could understand and experience how ... Aug 18, 2005 Kaletra ® may provide convenient dosages in HIV treatment regime Jul 31, 2005 New Study Results Find That Patients Treated With Boosted INVIRASE ... Jul 25, 2005 Abbott Submits Application To EMEA For A New, More Convenient ... Jul 30, 2005 New Study Results Find That Patients Treated With Boosted INVIRASE ... Jul 25, 2005 Abbott Statement on Agreement With Brazilian Government for ... 11 Jul 2005 Antifungal Vfend® provides significant cost advantages when used ... Jun 1, 2005 Committee for Medicinal Products for Human Use Post-authorisation ... May 27, 2005 MedWatch - The FDA Safety Information and Adverse Event Reporting ... Jun 10, 2005 News For Your Web Site Apr 19, 2005 EMEND® (aprepitant) Helps Prevent Nausea/Vomiting for Breast ... Apr 19, 2005 FDA List Serve ~ Important Information About Sustiva (efavirenz) ... Mar 31, 2005 Bristol-Myers Squibb Extends Assistance to State AIDS Drug ... Mar 22, 2005 Bristol-Myers Squibb Extends Assistance to State AIDS Drug ... Mar 22, 2005 Fair of face, foul of heart - cardiotoxicity and drug development Mar 6, 2005 | ||
| Dosage Forms | SUSPENSION; TABLET | ||
| Drug_Category | Anti-allergic Agents; Antihistamines; ATC:R06AX11 | ||
| Absorption | rapidly absorbed from the gastrointestinal tract | ||
| Interactions |
Interactions for Astemizole: Ketoconazole/Itraconazole, Macrolides, Including Erythromycin | ||
| Toxicity | LD50=2052mg/kg in mice | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 1-[(4-fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidyl]-benzoimidazol-2-amine | ||
| Chemical Formula | C28H31FN4O | ||
| Molecular Weight | 458.571 g/mol | ||
| Smiles String | COC1=CC=C(C=C1)CCN2CCC(CC2)NC3=NC4=CC=CC=C4N3CC5=CC=C(C=C5)F | ||
| Melting Point | 149.1°C | ||
| Water Solubility | 432 mg/L | ||
| State | White, odorless crystal | ||
| LogP/Hphobicity | 5.572 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Almost completely metabolized in the liver and primarily excreted in the feces | ||
| Half Life | 1 day | ||
| Protein Binding [%] | 96.70% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Astemizole.html http://www.rxlist.com/cgi/generic/astem.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00585 | ||
| CAS Registry Number | 68844-77-9 | ||
| KEGG Compound ID | C06832 | ||
| PubChem ID | SID:188751 | ||
| PharmGKB ID | PA448498 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2182912 |
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