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Ketoconazole: profile and news
Sudden Akathisia After a Ziprasidone Dose Reduction Mar 2, 2006 Stephan Heres, MD , John Davis, MD , Katja Maino, MD , Elisabeth ... Feb 9, 2006 Myocarditis During Clozapine Treatment Feb 14, 2006 Personal Accounts: Scaling Mount Rushmore: Cartography of a Manic ... Feb 14, 2006 Sudden cardiac death and antipsychotics. Part 1: Risk factors and ... Feb 9, 2006 Stephan Heres, MD , John Davis, MD , Katja Maino, MD , Elisabeth ... 09 Feb 2006 Sudden cardiac death and antipsychotics. Part 1: Risk factors and ... 09 Feb 2006 Patient- and Facility-Level Factors Associated With Diffusion of a ... Jan 25, 2006 CATIE Phase I Helps Clinicians Tailor Schizophrenia Treatment Jan 12, 2006 High-Cost Use of Second-Generation Antipsychotics Under ... Jan 25, 2006 People Can Suffer from Bipolar Disorder for Years until It is ... Jan 30, 2006 Brief Reports: Patterns of Psychotropic Medication Use by Race ... Jan 25, 2006 We need more studies like CATIE - says Principal Investigator Jan 11, 2006 Lundbeck gets first nod for revived schizophrenia drug Jan 18, 2006 Prevalence of the Night Eating Syndrome in a Psychiatric ... Jan 24, 2006 Interpreting the Results of the CATIE Study Jan 7, 2006 Ziprasidone Effective in Children and Adolescents with Bipolar ... Nov 11, 2005 International Approvals: Zeldox, Alfimeprase, Bronchitol Nov 15, 2005 Generic Forms of Janssen's Risperdal and Pfizer's Geodon Not ... Nov 22, 2005 Shire/Noven Daytrana Second-Line? Physicians Should Consider Oral ... Dec 2, 2005 Secondary Mania in Older Adults Nov 13, 2005 Olanzapine Versus Ziprasidone: Results of a 28-Week Double-Blind ... Oct 2, 2005 Behavioral and Pharmacologic Treatment of Aggression in Children ... Oct 3, 2005 Effectiveness of Antipsychotic Drugs in Patients with Chronic ... Sep 24, 2005 NIMH study to guide treatment choices for schizophrenia Sep 19, 2005 According to non-industry study, Zyprexa(R) is more effective in ... Sep 21, 2005 Schizophrenia Drugs Still Fall Short Sep 19, 2005 Old antipsychotic drugs comparable to new drugs, study finds Sep 20, 2005 Why New Drugs Don't Live Up to the Hype Sep 30, 2005 Schizophrenia Drugs Still Fall Short Sep 19, 2005 Newer antipsychotic not always better Sep 27, 2005 Old and New Schizophrenia Drugs: Study Shows Patient Satisfaction ... Sep 26, 2005 Most newer schizophrenia drugs no better - study Sep 19, 2005 Differences seen in anti-psychotic drugs Sep 19, 2005 Most newer schizophrenia drugs no better - study Sep 19, 2005 Most newer schizophrenia drugs no better - study Sep 20, 2005 Zyprexa Edges Four Other Agents With Modest Benefit for ... Sep 19, 2005 Royal Dutch Shell to Restructure Sep 20, 2005 Study: Old medication as effective as new for treating ... Sep 19, 2005 Old schizophrenia drugs as good as new Sep 20, 2005 Antipsychotic Drugs for Schizophrenia Sep 20, 2005 Duke, UNC authors say schizophrenia, depression drugs aren't much ... Sep 19, 2005 Schizophrenia: CATIE study compares the effectiveness and side ... Sep 25, 2005 Eli Lilly: double-edged results for Zyprexa Sep 23, 2005 Many meds don't mix with the sun Sep 21, 2005 Other information Indication For the treatment of the following systemic fungal infections: candidiasis, chronic mucocutaneous candidiasis, oral thrush, candiduria, blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, and paracoccidioidomycosis Pharmacology Ketoconazole, like clotrimazole, fluconazole, itraconazole, and miconazole, is an imidazole antifungal agent. Mechanism Of Action Ketoconazole interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary for the conversion of lanosterol to ergosterol. This results in inhibition of ergosterol synthesis and increased fungal cellular permeability. Other mechanisms may involve the inhibition of endogenous respiration, interaction with membrane phospholipids, inhibition of yeast transformation to mycelial forms, inhibition of purine uptake, and impairment of triglyceride and/or phospholipid biosynthesis. Ketoconazole can also inhibit the synthesis of thromboxane and sterols such as aldosterone, cortisol, and testosterone. Drug Category Antifungals; Antifungals; ATC:D01AC08; ATC:G01AF11; ATC:J02AB02 Brand Names/Synonyms DRG-0073; Extina; Fungarest; Fungoral; KETOCONAZOLE, 99%; KW-1414; Ketocanazole; Ketoconazol; Ketoconazol [Inn-Spanish]; Ketoconazole; Ketoconazole [Usan:Ban:Inn:Jan]; Ketoconazolum [Inn-Latin]; Ketoderm; Ketoisdin; Ketozole; Nizoral; Nizoral Cream; Nizoral Shampoo; Nizoral a-D; Nizoral a-D Shampoo; Orifungal; Orifungal M; Panfungol Dosage Forms Oral tablets, Shampoo, Cream, Suspension; Absorption Moderate Interactions -->Interactions for Ketoconazole: Ketoconazole is a potent inhibitor of the cytochrome P450 3A4 enzyme system. Coadministration of NIZORAL® Tablets and drugs primarily metabolized by the cytochrome P450 3A4 enzyme system may result in increased plasma concentrations of the drugs that could increase or prolong both therapeutic and adverse effects. Therefore, unless otherwise specified, appropriate dosage adjustments may be necessary. The following drug interactions have been identified involving NIZORAL® Tablets and other drugs metabolized by the cytochrome P450 3A4 enzyme system: Ketoconazole tablets inhibit the metabolism of terfenadine, resulting in an increased plasma concentration of terfenadine and a delay in the elimination of its acid metabolite. The increased plasma concentration of terfenadine or its metabolite may result in prolonged QT intervals. Pharmacokinetic data indicate that oral ketoconazole inhibits the metabolism of astemizole, resulting in elevated plasma levels of astemizole and its active metabolite desmethylastemizole which may prolong QT intervals. Coadministration of astemizole with ketoconazole tablets is therefore contraindicated. Human pharmacokinetics data indicate that oral ketoconazole potently inhibits the metabolism of cisapride resulting in a mean eight-fold increase in AUC of cisapride. Data suggest that coadministration of oral ketoconazole and cisapride can result in prolongation of the QT interval on the ECG. Therefore concomitant administration of ketoconazole tablets with cisapride is contraindicated. Ketoconazole tablets may alter the metabolism of cyclosporine, tacrolimus, and methylprednisolone, resulting in elevated plasma concentrations of the latter drugs. Dosage adjustment may be required if cyclosporine, tacrolimus, or methylprednisolone are given concomitantly with NIZORAL® Tablets. Coadministration of NIZORAL® Tablets with midazolam or triazolam has resulted in elevated plasma concentrations of the latter two drugs. This may potentiate and prolong hypnotic and sedative effects, especially with repeated dosing or chronic administration of these agents. These agents should not be used in patients treated with NIZORAL® Tablets. If midazolam is administered parenterally, special precaution is required since the sedative effect may be prolonged. Rare cases of elevated plasma concentrations of digoxin have been reported. It is not clear whether this was due to the combination of therapy. It is, therefore, advisable to monitor digoxin concentrations in patients receiving ketoconazole. When taken orally , imidazole compounds like ketoconazole may enhance the anticoagulant effect of coumarin-like drugs. In simultaneous treatment with imidazole drugs and coumarin drugs, the anticoagulant effect should be carefully titrated and monitored. Because severe hypoglycemia has been reported in patients concomitantly receiving oral miconazole (an imidazole) and oral hypoglycemic agents, such a potential interaction involving the latter agents when used concomitantly with ketoconazole tablets (an imidazole) can not be ruled out. Concomitant administration of ketoconazole tablets with phenytoin may alter the metabolism of one or both of the drugs. It is suggested to monitor both ketoconazole and phenytoin. Concomitant administration of rifampin with ketoconazole tablets reduces the blood levels of the latter. INH (Isoniazid) is also reported to affect ketoconazole concentrations adversely. These drugs should not be given concomitantly. After the coadministration of 200 mg oral ketoconazole twice daily and one 20 mg dose of loratadine to 11 subjects, the AUC and Cmax of loratadine averaged 302% (± 142 S.D.) and 251% (± 68 S.D.), respectively, of those obtained after co-treatment with placebo. The AUC and Cmax of descarboethoxyloratadine, an active metabolite, averaged 155% (± 27 S.D.) and 141% (± 35 S.D.), respectively. However, no related changes were noted in the QT0 on ECG taken at 2, 6, and 24 hours after the coadministration. Also, there were no clinically significant differences in adverse events when loratadine was administered with or without ketoconazole. Rare cases of a disulfiram-like reaction to alcohol have been reported. These experiences have been characterized by flushing, rash, peripheral edema, nausea, and headache. Symptoms resolved within a few hours. Chemical IUPAC Name 1-[4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]ethanone Chemical Formula C26H28Cl2N4O4 Half Life 2 hours Drug Type Approved Drug # Accession No APRD00401 CAS Registry Number 65277-42-1 |
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