Attributes | Values |
---|
rdf:type
| |
http://linked.open...gbank/description
| - Posaconazole is a triazole antifungal drug that is used to treat invasive infections by Candida species and Aspergillus species in severely immunocompromised patients. (en)
|
http://linked.open...y/drugbank/dosage
| |
http://linked.open...generalReferences
| - # Cornely OA, Maertens J, Winston DJ, Perfect J, Ullmann AJ, Walsh TJ, Helfgott D, Holowiecki J, Stockelberg D, Goh YT, Petrini M, Hardalo C, Suresh R, Angulo-Gonzalez D: Posaconazole vs. fluconazole or itraconazole prophylaxis in patients with neutropenia. N Engl J Med. 2007 Jan 25;356(4):348-59. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17251531 # Ullmann AJ, Lipton JH, Vesole DH, Chandrasekar P, Langston A, Tarantolo SR, Greinix H, Morais de Azevedo W, Reddy V, Boparai N, Pedicone L, Patino H, Durrant S: Posaconazole or fluconazole for prophylaxis in severe graft-versus-host disease. N Engl J Med. 2007 Jan 25;356(4):335-47. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17251530 # Bhattacharya M, Rajeshwari K, Dhingra B: Posaconazole. J Postgrad Med. 2010 Apr-Jun;56(2):163-7. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/20622401 # Frampton JE, Scott LJ: Posaconazole : a review of its use in the prophylaxis of invasive fungal infections. Drugs. 2008;68(7):993-1016. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18457464 # Schiller DS, Fung HB: Posaconazole: an extended-spectrum triazole antifungal agent. Clin Ther. 2007 Sep;29(9):1862-86. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18035188 # Kwon DS, Mylonakis E: Posaconazole: a new broad-spectrum antifungal agent. Expert Opin Pharmacother. 2007 Jun;8(8):1167-78. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17516880 # Groll AH, Walsh TJ: Posaconazole: clinical pharmacology and potential for management of fungal infections. Expert Rev Anti Infect Ther. 2005 Aug;3(4):467-87. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16107193 # Rachwalski EJ, Wieczorkiewicz JT, Scheetz MH: Posaconazole: an oral triazole with an extended spectrum of activity. Ann Pharmacother. 2008 Oct;42(10):1429-38. Epub 2008 Aug 19. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18713852 # Li Y, Theuretzbacher U, Clancy CJ, Nguyen MH, Derendorf H: Pharmacokinetic/pharmacodynamic profile of posaconazole. Clin Pharmacokinet. 2010 Jun;49(6):379-96. doi: 10.2165/11319340-000000000-00000. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/20481649 (en)
|
http://linked.open...gy/drugbank/group
| - approved (en)
- investigational (en)
|
http://linked.open...drugbank/halfLife
| - Posaconazole is eliminated with a mean half-life (t½) of 35 hours (range 20 to 66 hours). (en)
|
http://linked.open...ugbank/indication
| - For prophylaxis of invasive <em>Aspergillus</em> and <em>Candida</em> infections in patients, 13 years of age and older, who are at high risk of developing these infections due to being severely immunocompromised as a result of procedures such as hematopoietic stem cell transplant (HSCT) recipients with graft-versus-host disease (GVHD), or due to hematologic malignancies with prolonged neutropenia from chemotherapy. Also for the treatment of oropharyngeal candidiasis, including oropharyngeal candidiasis refractory to itraconazole and/or fluconazole. Posaconazole is used as an alternative treatment for invasive aspergillosis, <em>Fusarium</em> infections, and zygomycosis in patients who are intolerant of, or whose disease is refractory to, other antifungals. (en)
|
sameAs
| |
Title
| |
adms:identifier
| |
http://linked.open...mechanismOfAction
| - As a triazole antifungal agent, posaconazole exerts its antifungal activity through blockage of the cytochrome P-450 dependent enzyme, sterol 14α-demethylase, in fungi by binding to the heme cofactor located on the enzyme. This leads to the inhibition of the synthesis of ergosterol, a key component of the fungal cell membrane, and accumulation of methylated sterol precursors. This results in inhibition of fungal cell growth and ultimately, cell death. (en)
|
http://linked.open...drugbank/packager
| |
http://linked.open...y/drugbank/patent
| |
http://linked.open...outeOfElimination
| - The excreted metabolites in urine and feces account for ~17% of the administered radiolabeled dose. (en)
|
http://linked.open.../drugbank/synonym
| |
http://linked.open...drugbank/toxicity
| - During the clinical trials, some patients received posaconazole up to 1600 mg/day with no adverse events noted that were different from the lower doses. In addition, accidental overdose was noted in one patient who took 1200 mg BID for 3 days. No related adverse events were noted by the investigator. (en)
|
http://linked.open...umeOfDistribution
| |
http://linked.open...nk/proteinBinding
| - Posaconazole is highly protein bound (>98%), predominantly to albumin. (en)
|
http://linked.open...ynthesisReference
| - Dominic De Souza, "PREPARATION OF POSACONAZOLE INTERMEDIATES." U.S. Patent US20130203994, issued August 08, 2013. (en)
|
foaf:page
| |
http://linked.open...ugbank/IUPAC-Name
| |
http://linked.open...gy/drugbank/InChI
| |
http://linked.open...Molecular-Formula
| |
http://linked.open.../Molecular-Weight
| |
http://linked.open...noisotopic-Weight
| |
http://linked.open...y/drugbank/SMILES
| |
http://linked.open.../Water-Solubility
| |
http://linked.open...ogy/drugbank/logP
| |
http://linked.open...ogy/drugbank/logS
| |
http://linked.open...l/drug/hasATCCode
| |
http://linked.open...nd-Acceptor-Count
| |
http://linked.open...-Bond-Donor-Count
| |
http://linked.open...drugbank/InChIKey
| |
http://linked.open...urface-Area--PSA-
| |
http://linked.open...nk/Polarizability
| |
http://linked.open...bank/Refractivity
| |
http://linked.open...atable-Bond-Count
| |
http://linked.open...ugbank/absorption
| - Posaconazole is absorbed with a median Tmax of approximately 3 to 5 hours. (en)
|
http://linked.open.../affectedOrganism
| - Aspergillis, Candida and other fungi (en)
|
http://linked.open...casRegistryNumber
| |
http://linked.open...drugbank/category
| |
http://linked.open...rugbank/clearance
| - * 32 L/hr * 51 L/hr [Single-Dose Suspension Administration of 200 mg, fasted] * 21 L/hr [Single-Dose Suspension Administration of 200 mg, nonfat meal] * 14 L/hr [Single-Dose Suspension Administration of 200 mg, high fat meal] * 91 L/hr [Single-Dose Suspension Administration of 400 mg, fasted] * 43 L/hr [Single-Dose Suspension Administration of 400 mg with liquid nutritional supplement (14 g fat)] (en)
|
http://linked.open...gbank/containedIn
| |
http://linked.open...k/Bioavailability
| |
http://linked.open...bank/Ghose-Filter
| |
http://linked.open...nk/MDDR-Like-Rule
| |
http://linked.open...k/Number-of-Rings
| |
http://linked.open...siological-Charge
| |
http://linked.open...bank/Rule-of-Five
| |
http://linked.open...tional-IUPAC-Name
| |
http://linked.open...strongest-acidic-
| |
http://linked.open...-strongest-basic-
| |