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Nizoral: profile and news
THE MANY PROBLEMS OF OILY SKIN Feb 6, 2006 The many problems of oily skin Feb 7, 2006 THE MANY PROBLEMS OF OILY SKIN Feb 6, 2006 No flaking? Don’t rule out dandruff Jan 22, 2006 Men spared side effect from pain reliever Nov 10, 2005 Dr. Gaff's Column Nov 28, 2005 Kline Study Predicts RX-to-OTC Switches For Antifungal Medications Nov 17, 2005 TREATMENT FOR DIARRHEA HINGES ON FINDING ITS CAUSE Oct 13, 2005 A Question Of Health Oct 11, 2005 A Question Of Health 11 Oct 2005 Ask Dr. H | Yeast infection isn't likely man's fault Sep 12, 2005 Unlikely men pass along yeast infections ASK DR. H MITCHELL HECHT Sep 20, 2005 Drugs in Development Sep 21, 2005 McNeil Consumer & Specialty Pharmaceuticals Statement Regarding ... Sep 13, 2005 Expiration Dates Observed on Foods, But Not Always on Medications Sep 20, 2005 TBWA/SMP is agency of the year Sep 25, 2005 McNeil Consumer & Specialty Pharmaceuticals Statement Regarding ... Sep 13, 2005 Parents May Not Be Aware of FDA Guidelines for Treating Children ... 08 Sep 2005 Satish Ramachandran joins FCB-Ulka Aug 23, 2005 Acmemeds.com Improves Itself With 101 New Added Medications Aug 20, 2005 Satish Ramachandran of Ambience Publicis to join FCB-Ulka Aug 23, 2005 Pendulum snaps back on stretching Jul 26, 2005 Illegal manufacturers of drugs arrested Jul 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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