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Fluconazole
drug data and news
Fluconazole 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 | Fluconazole | ||
| Brand Names/Synonyms | Biocanol; Biozolene; Diflucan; Diflucan in Sodium Chloride 0.9%; Elazor; FLUCONAZOLE , 99%; Flucazol; Fluconazole; Fluconazole in Sodium Chloride 0.9%; Flucostat; Flukezol; Flunizol; Flusol; Pritenzol; Triflucan | ||
| Indication | For the treatment of fungal infections. | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Fluconazole, a synthetic antifungal agent of the imidazole class, is used to treat vaginal candidiasis. | ||
| Mechanism Of Action | Fluconazole interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents. Fluconazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis. | ||
| Fluconazole News (When available) |
A Potential HIV Prophylactic? Feb 7, 2006 Drug combination prevents HIV infection in monkeys Feb 6, 2006 Drug Combination Prevents HIV in Monkeys Feb 7, 2006 Drug combination prevents HIV infection in animal study Feb 8, 2006 Medical Report Feb 4, 2006 CytoDyn Gets Greenlight from Its Investigators for China Joint ... Feb 27, 2006 Daily Injection of Common Antiretroviral Drugs Found To Protect ... Feb 8, 2006 CytoDyn Gets Greenlight from Its Investigators for China Joint ... Feb 27, 2006 MSF Calls on Gilead To Increase Access to Reduced-Cost Viread Feb 9, 2006 Biotech Investing for the Long Haul Feb 22, 2006 Merck, Gilead Drugs Offer Hope Against Resistant HIV (Update1) Feb 7, 2006 Full Text Feb 16, 2006 MSF Calls on Gilead To Increase Access to Reduced-Cost Viread 09 Feb 2006 Truvada Boosts Gilead's Revenue Jan 30, 2006 Fat loss associated with Combivir but not Truvada Jan 23, 2006 ICAAC: Switching from Combivir to Truvada has benefits for ... Jan 11, 2006 Gilead and BMS to seek regulatory approval for efavirenz, Truvada ... Jan 10, 2006 Gilead Sciences Announces Fourth Quarter and Full Year 2005 ... Jan 30, 2006 Medical Report Feb 3, 2006 Gilead 4th-qtr profit doubles but stock falls Jan 30, 2006 Data Comparing Viread(R) and Emtriva(R) to Combivir(R) as Part of ... Jan 18, 2006 Gilead 4th-qtr profit doubles but stock falls Jan 30, 2006 Gilead 4th-qtr profit doubles but stock falls Jan 30, 2006 Gilead 4th-qtr profit doubles but stock falls Jan 30, 2006 Cheer or tax record oil-industry profits? We report, you decide Jan 30, 2006 Zoek in het archief Jan 9, 2006 Bristol-Myers Squibb and Gilead Announce Data Supporting ... Jan 9, 2006 Bristol-Myers Squibb and Gilead Announce Data Supporting ... Jan 9, 2006 HIV drug sales lift Gilead profits Jan 31, 2006 Data Comparing Viread(R) and Emtriva(R) to Combivir(R) as Part of ... Jan 18, 2006 GILEAD SCIENCES INC Jan 31, 2006 Gilead 4th-qtr profit doubles but stock falls Jan 30, 2006 Gilead fourth-quarter profit more than doubles Jan 30, 2006 TECH TICKER Jan 31, 2006 Merck, Gilead Drugs Offer New Approach to Tackle HIV Resistance Feb 6, 2006 Gilead Sciences' Profit More Than Doubles Jan 31, 2006 Gilead HIV drug shows promise Jan 19, 2006 Companies announce success in forming single-pill anti-HIV regimen Jan 9, 2006 Study: Gilead's HIV combo beats Glaxo's Jan 18, 2006 Study Rates Generation Of New AIDS Cocktails Jan 19, 2006 Gilead, Bristol Won't Quit on HIV Drug Jan 9, 2006 New HIV Drug Regimen More Effective Than Existing Therapy Jan 18, 2006 New HIV Regimen Outperforms Gold Standard Jan 19, 2006 Gilead Says Combo Drug Moves Forward Jan 9, 2006 Drug Firms To Produce Single Pill AIDS Treatment Jan 20, 2006 Bristol-Meyers Squibb, Gilead advance single-dose HIV drug Jan 12, 2006 Analysts' Stock Picks: Part 1 Jan 23, 2006 Eye On Stocks For Tuesday, Jan. 31 Jan 30, 2006 Gilead 4Q profit rises on AIDS drug sales Jan 30, 2006 Gilead HIV drug combo beats GSK rival in phase III trial Jan 20, 2006 Health Beat Jan 26, 2006 Drug price reduction makes Aids manageable Jan 25, 2006 Study Sets New Gold Standard For Initial Antiretroviral Treatment ... Jan 25, 2006 Gilead income nearly triples Jan 30, 2006 Brisol-Myers, Gilead advance combo AIDS treatment Jan 9, 2006 Researchers find better HIV medication Jan 18, 2006 Merck, Gilead in integrase-inhibitor race Jan 13, 2006 More efficient HIV treatment discovered Jan 24, 2006 Study gives high marks to new drugs Jan 19, 2006 Science & Medicine | Gilead, Bristol-Myers Squibb Develop Once-a ... Jan 19, 2006 Gilead's Truvada Seen Superior To GSK's Combivir Nov 18, 2005 Gilead posts positive Truvada results Nov 17, 2005 Switching from twice-daily Combivir to once-daily Truvada in ... Nov 23, 2005 Gilead's Truvada Better at Suppressing HIV Than GSK's Combivir ... Nov 21, 2005 Gilead Posts Positive Truvada Results Nov 17, 2005 *vwd/BUSINESS WIRE: 24-Wochen-Daten zur Wirkung von HIV-Patienten ... Nov 17, 2005 Zoek in het archief Nov 17, 2005 Preliminary 24-Week Data Evaluating the Impact of Switching from ... Nov 17, 2005 Preliminary 24-Week Data Evaluating the Impact of Switching from ... Nov 17, 2005 Gilead Gains a Bit Too Much Respect Dec 2, 2005 Merck & Co. HIV Drug Lowers Virus Level and Gilead Posts Positive ... Nov 21, 2005 Gilead Sciences "buy," target price raised Nov 14, 2005 Gilead Shares Face Limited Upside Nov 15, 2005 Stock Scorecard Nov 13, 2005 Aviva, Elan, Glaxo, Reuters, WPP: UK and Irish Equity Preview Nov 17, 2005 Montgomery & Co. LLC Announces Investment Opinion: Initiates ... Dec 1, 2005 AIDS drugs take financial toll on patients Dec 1, 2005 Biotech Earnings Jump In Quarter Nov 21, 2005 Accord on Sharing Flu Vaccine Production Nov 16, 2005 Gilead's Half-Empty Pipeline Nov 21, 2005 | ||
| Dosage Forms | CAPSULE; LIQUID; POWDER FOR SOLUTION; SOLUTION; TABLET | ||
| Drug_Category | Antifungals; Antifungals; ATC:D01AC15; ATC:J02AC01 | ||
| Absorption | 90% | ||
| Interactions |
Interactions for Fluconazole: Clinically or potentially significant drug interactions between DIFLUCAN and the following agents/classes have been observed. These are described in greater detail below: DIFLUCAN and the following agents/classes have been observed. These are described in greater detail below: Oral hypoglycemics Oral hypoglycemics: Clinically significant hypoglycemia may be precipitated by the use of DIFLUCAN with oral hypoglycemic agents; one fatality has been reported from hypoglycemia in association with combined DIFLUCAN and glyburide use. DIFLUCAN reduces the metabolism of tolbutamide, glyburide, and glipizide and increases the plasma concentration of these agents. When DIFLUCAN is used concomitantly with these or other sulfonylurea oral hypoglycemic agents, blood glucose concentrations should be carefully monitored and the dose of the sulfonylurea should be adjusted as necessary. Coumarin-type anticoagulants: Prothrombin time may be increased in patients receiving concomitant DIFLUCAN and coumarin-type anticoagulants. In post-marketing experience, as with other azole antifungals, bleeding events (bruising, epistaxis, gastrointestinal bleeding, hematuria, and melena) have been reported in association with increases in prothrombin time in patients receiving fluconazole concurrently with warfarin. Careful monitoring of prothrombin time in patients receiving DIFLUCAN and coumarin-type anticoagulants is recommended. (See CLINICAL PHARMACOLOGY: Drug Interaction Studies.) Phenytoin: DIFLUCAN increases the plasma concentrations of phenytoin. Careful monitoring of phenytoin concentrations in patients receiving DIFLUCAN and phenytoin is recommended. (See CLINICAL PHARMACOLOGY: Drug Interaction Studies.) Cyclosporine: DIFLUCAN may significantly increase cyclosporine levels in renal transplant patients with or without renal impairment. Careful monitoring of cyclosporine concentrations and serum creatinine is recommended in patients receiving DIFLUCAN and cyclosporine. (See CLINICAL PHARMACOLOGY: Drug Interaction Studies.) Rifampin: Rifampin enhances the metabolism of concurrently administered DIFLUCAN. Depending on clinical circumstances, consideration should be given to increasing the dose of DIFLUCAN when it is administered with rifampin. Theophylline: DIFLUCAN increases the serum concentrations of theophylline. Careful monitoring of serum theophylline concentrations in patients receiving DIFLUCAN and theophylline is recommended. Terfenadine: Because of the occurrence of serious cardiac dysrhythmias secondary to prolongation of the QTc interval in patients receiving azole antifungals in conjunction with terfenadine, interaction studies have been performed. One study at a 200-mg daily dose of fluconazole failed to demonstrate a prolongation in QTc interval. Another study at a 400-mg and 800-mg daily dose of fluconazole demonstrated that DIFLUCAN taken in doses of 400 mg per day or greater significantly increases plasma levels of terfenadine when taken concomitantly. The combined use of fluconazole at doses of 400 mg or greater with terfenadine is contraindicated. The coadministration of fluconazole at doses lower than 400 mg/day with terfenadine should be carefully monitored. Cisapride: There have been reports of cardiac events, including torsade de pointes in patients to whom fluconazole and cisapride were coadministered. A controlled study found that concomitant fluconazole 200 mg once daily and cisapride 20 mg four times a day yielded a significant increase in cisapride plasma levels and prolongation of QTc interval.The combined use of fluconazole with cisapride is contraindicated. Astemizole: The use of fluconazole in patients concurrently taking astemizole or other drugs metabolized by the cytochrome P450 system may be associated with elevations in serum levels of these drugs. In the absence of definitive information, caution should be used when coadministering fluconazole. Patients should be carefully monitored. Rifabutin: There have been reports of uveitis in patients to whom fluconazole and rifabutin were coadministered. Patients receiving rifabutin and fluconazole concomitantly should be carefully monitored. Tacrolimus: There have been reports of nephrotoxicity in patients to whom fluconazole and tacrolimus were coadministered. Patients receiving tacrolimus and fluconazole concomitantly should be carefully monitored. Short-acting Benzodiazepines: Following oral administration of midazolam, fluconazole resulted in substantial increases in midazolam concentrations and psychomotor effects. This effect on midazolam appears to be more pronounced following oral administration of fluconazole than with fluconazole administered intravenously. If short-acting benzodiazepines, which are metabolized by the cytochrome P450 system, are concomitantly administered with fluconazole, consideration should be given to decreasing the benzodiazepine dosage, and the patients should be appropriately monitored. Fluconazole tablets coadministered with ethinyl estradiol- and levonorgestrel-containing oral contraceptives produced an overall mean increase in ethinyl estradiol and levonorgestrel levels; however, in some patients there were decreases up to 47% and 33% of ethinyl estradiol and levonorgestrel levels. The data presently available indicate that the decreases in some individual ethinyl estradiol and levonorgestrel AUC values with fluconazole treatment are likely the result of random variation. While there is evidence that fluconazole can inhibit the metabolism of ethinyl estradiol and levonorgestrel, there is no evidence that fluconazole is a net inducer of ethinyl estradiol or levonorgestrel metabolism. The clinical significance of these effects is presently unknown. Physicians should be aware that interaction studies with medications other than those listed in the CLINICAL PHARMACOLOGY section have not been conducted, but such interactions may occur. | ||
| Toxicity | hallucinations and paranoid behavior | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 2-(2,4-difluorophenyl)-1,3-bis(1H-1,2,4-triazol-1-yl)propan-2-ol | ||
| Chemical Formula | C13H12F2N6O | ||
| Molecular Weight | 306.271 g/mol | ||
| Smiles String | C1=CC(=C(C=C1F)F)C(CN2C=NC=N2)(CN3C=NC=N3)O | ||
| Melting Point | 138 - 140 °C | ||
| Water Solubility | 1 mg/L | ||
| State | Solid | ||
| LogP/Hphobicity | 2.174 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Hepatic | ||
| Half Life | 30 hours (range 20-50 hours) | ||
| Protein Binding [%] | 11 to 12% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Fluconazole.html http://www.rxlist.com/cgi/generic/flucon.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00327 | ||
| CAS Registry Number | 86386-73-4 | ||
| KEGG Compound ID | C07002 | ||
| PubChem ID | SID:192927 | ||
| PharmGKB ID | PA449653 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2245697 |
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