Nizoral: profile and news






THE MANY PROBLEMS OF OILY SKIN  Feb 6, 2006
...the skin yeast. Ketoconazole (Nizoral) and ciclopirox (Loprox) are available in foams, liquids, creams and ointments. The choice ... - Charlotte Sun-Herald,

The many problems of oily skin  Feb 7, 2006
Ketoconazole (Nizoral) and ciclopirox (Loprox) are available in foams, liquids, creams and ointments. Both of these medicines require a prescription. ... - Sarasota Herald-Tribune,

THE MANY PROBLEMS OF OILY SKIN  Feb 6, 2006
...the skin yeast. Ketoconazole (Nizoral) and ciclopirox (Loprox) are available in foams, liquids, creams and ointments. The choice ... - Charlotte Sun-Herald,

No flaking? Don’t rule out dandruff  Jan 22, 2006
...response to the anti-fungal cream, you may have the best results with an over-the-counter shampoo containing ketoconazole (brand name Nizoral), another anti ... - Fort Wayne Journal Gazette,

Men spared side effect from pain reliever  Nov 10, 2005
I had tried everything my doctor prescribed: Nizoral, Elidel, topical steroids in oils and shampoos and even an injection. Nothing worked until the tea. ... - Bradenton Herald,

Dr. Gaff's Column  Nov 28, 2005
Use of simvastatin (Zocor, Vytorin) with itraconazole (Sporanox), ketoconazole (Nizoral), erythromycin, clarithromycin (Biaxin), telithromycin (Ketek ... - KPCnews.com,

Kline Study Predicts RX-to-OTC Switches For Antifungal Medications  Nov 17, 2005
...also switch, including Pfizer's Diflucan, used for the treatment of vaginal fungal infections, and Johnson & Johnson's anti-dandruff shampoo Nizoral, which is ... - Yahoo! News (press release)

TREATMENT FOR DIARRHEA HINGES ON FINDING ITS CAUSE  Oct 13, 2005
...including Lamisil cream or selenium-sulfide lotion. In very bad cases, oral Nizoral is prescribed. There are so many elements of ... - Charlotte Sun-Herald,

A Question Of Health  Oct 11, 2005
The most effective treatment is designed to slow down the growth of the yeast. Two brands are available over the counter - Nizoral and Dandrazol. ... - Independent,

A Question Of Health  11 Oct 2005
The most effective treatment is designed to slow down the growth of the yeast. Two brands are available over the counter - Nizoral and Dandrazol. ... - Independent,

Ask Dr. H | Yeast infection isn't likely man's fault  Sep 12, 2005
And unless there's evidence of a yeast infection on the penis, an antifungal cream such as Nizoral or a pill such as Diflucan is usually not necessary. ... - Philadelphia Inquirer,

Unlikely men pass along yeast infections ASK DR. H MITCHELL HECHT  Sep 20, 2005
And unless there’s evidence of a possible yeast infection on the penis, use of an antifungal cream like Nizoral or a pill like Diflucan is usually not ... - Wilkes Barre Times-Leader,

Drugs in Development  Sep 21, 2005
Previous results from Connetics’ Phase III clinical trial with Extina demonstrated non-inferiority to Nizoral 2% Cream, comprised of ketoconazole, as ... - R&D Directions (subscription),

McNeil Consumer & Specialty Pharmaceuticals Statement Regarding ...  Sep 13, 2005
Other McNeil brands include IMODIUM(R) (loperamide HCI) AD Anti-Diarrheal, ST. JOSEPH(R) Adult Regimen Aspirin and NIZORAL(R) AD (ketoconazole) Shampoo. - PR Newswire (press release),

Expiration Dates Observed on Foods, But Not Always on Medications  Sep 20, 2005
...tablets). Other McNeil brands include IMODIUM(R) AD anti-diarrheal, ST. JOSEPH(R) 81 mg Adult Aspirin and NIZORAL(R) AD Shampoo. Johnson ... - PharmaLive.com (press release),

TBWA/SMP is agency of the year  Sep 25, 2005
Underground" TV commercials; Boysen "Pyramids" print ad; Adidas "Sculpture" poster; KFC "Demo" radio commercial; and in interactive, Nizoral "Scratch Boy". ... - INQ7 Interactive, Inc.,

McNeil Consumer & Specialty Pharmaceuticals Statement Regarding ...  Sep 13, 2005
Other McNeil brands include IMODIUM® (loperamide HCI) AD Anti-Diarrheal, ST. JOSEPH® Adult Regimen Aspirin and NIZORAL® AD (ketoconazole) Shampoo. - Yahoo! News (press release)

Parents May Not Be Aware of FDA Guidelines for Treating Children ...  08 Sep 2005
Other McNeil brands include IMODIUM(R) AD anti-diarrheal, ST. JOSEPH(R) 81 mg Adult Aspirin and NIZORAL(R) AD Shampoo. Methodology ... - PR Newswire (press release),

Satish Ramachandran joins FCB-Ulka  Aug 23, 2005
...and Tiger Balm. He has launched brands like Aciguard and Nizoral and has run CRM initiatives for Abbott and Marico. Commenting on ... - Televisionpoint.com,

Acmemeds.com Improves Itself With 101 New Added Medications  Aug 20, 2005
...generic) 600 mg,Motrin (generic) 800 mg,Naprosyn (generic) 375 mg,Naprosyn (generic) 500 mg,Naprosyn 375 mg,Naprosyn 500 mg,Nexium 20 mg,Nizoral (generic) 200 ... - PR Web (press release),

Satish Ramachandran of Ambience Publicis to join FCB-Ulka  Aug 23, 2005
Tiger Balm’. In addition, he has been responsible for the launch of several brands such as ‘Aciguard’ and ‘Nizoral’. He ... - agencyfaqs.com,

Pendulum snaps back on stretching  Jul 26, 2005
Many lotions and creams can cure tinea versicolor. Lamisil and Nizoral are two examples. A 2 percent solution of selenium sulfide also works. ... - Contra Costa Times

Illegal manufacturers of drugs arrested  Jul 21, 2005
...of the financial police the medicines were primarily drugs high in demand, such as Preduktal, Suprastini, Ketanov, Diazepam, Cipronal, Nizoral, and Buckthorn ... - Messenger.ge


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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