Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/151
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NIZORAL (Tablet)
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dailymed-instance:dosage |
Adults: The recommended starting dose of NIZORAL (ketoconazole)
Tablets is a single daily administration of 200 mg (one tablet). In very serious
infections or if clinical responsiveness is insufficient within the expected
time, the dose of NIZORAL Tablets may be increased to 400
mg (two tablets) once daily.<br/>Children: In small numbers of children over 2 years of age,
a single daily dose of 3.3 to 6.6 mg/kg has been used. NIZORAL Tablets
have not been studied in children under 2 years of age. There should be laboratory as well as clinical documentation
of infection prior to starting ketoconazole therapy. Treatment should be continued
until tests indicate that active fungal infection has subsided. Inadequate
periods of treatment may yield poor response and lead to early recurrence
of clinical symptoms. Minimum treatment for candidiasis is one or two weeks.
Patients with chronic mucocutaneous candidiasis usually require maintenance
therapy. Minimum treatment for the other indicated systemic mycoses is six
months. Minimum treatment for recalcitrant
dermatophyte infections is four weeks in cases involving glabrous skin. Palmar
and plantar infections may respond more slowly. Apparent cures may subsequently
recur after discontinuation of therapy in some cases.
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dailymed-instance:descripti... |
NIZORAL (ketoconazole) is a synthetic
broad-spectrum antifungal agent available in scored white tablets, each containing
200 mg ketoconazole base for oral administration. Inactive ingredients are
colloidal silicon dioxide, corn starch, lactose, magnesium stearate, microcrystalline
cellulose, and povidone. Ketoconazole is cis-1- acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxyl]phenyl]
piperazine and has thefollowing structural formula: Ketoconazole is
a white to slightly beige, odorless powder, soluble in acids, with a molecular
weight of 531.44.
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dailymed-instance:clinicalP... |
Mean peak plasma levels of approximately 3.5��g/mL
are reached within 1 to 2 hours, following oral administration of a single
200 mg dose taken with a meal. Subsequent plasma elimination is biphasic with
a half-life of 2 hours during the first 10 hours and 8 hours thereafter. Following
absorption from the gastrointestinal tract, NIZORAL (ketoconazole)
is converted into several inactive metabolites. The major identified metabolic
pathways are oxidation and degradation of the imidazole and piperazine rings,
oxidative O-dealkylation and aromatic hydroxylation. About 13% of the dose
is excreted in the urine, of which 2 to 4% is unchanged drug. The major route
of excretion is through the bile into the intestinal tract. In
vitro, the plasma protein binding is about 99% mainly to the albumin
fraction. Only a negligible proportion of ketoconazole reaches the cerebral-spinal
fluid. Ketoconazole is a weak dibasic agent and thus requires acidity for
dissolution and absorption. NIZORAL Tablets
are active against clinical infections with Blastomyces
dermatitidis, Candida spp., Coccidioides
immitis, Histoplasma capsulatum, Paracoccidioides brasiliensis, and Phialophora spp. NIZORAL Tablets
are also active against Trichophyton spp., Epidermophyton
spp., and Microsporum spp.
Ketoconazole is also active in vitro against
a variety of fungi and yeast. In animal models, activity has been demonstrated
against Candida spp., Blastomyces dermatitidis,
Histoplasma capsulatum, Malassezia furfur, Coccidioides immitis,
and Cryptococcus neoformans.<br/>Mode of Action: In vitro studies
suggest that ketoconazole impairs the synthesis of ergosterol, which is a
vital component of fungal cell membranes.
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dailymed-instance:supply |
NIZORAL (ketoconazole) is available
as white, scored tablets containing 200 mg of ketoconazole debossed "JANSSEN"
and on the reverse side debossed "NIZORAL". They are supplied in bottles of
100 tablets (NDC 50458-220-10). Store at controlled
room temperature 15�����25��C (59�����77��F). Protect from moisture. Keep out
of reach of children.
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dailymed-instance:genericDr... | |
dailymed-instance:boxedWarn... |
WARNING: When used orally, ketoconazole has been associated
with hepatic toxicity, including some fatalities. Patients receiving this
drug should be informed by the physician of the risk and should be closely
monitored. See WARNINGS and PRECAUTIONS sections. Coadministration
of terfenadine with ketoconazole tablets is contraindicated. Rare cases of
serious cardiovascular adverse events, including death, ventricular tachycardia
and tordades de pointes have been observed in patients taking ketoconazole
tablets concomitantly with terfenadine, due to increased terfenadine concentrations
induced by ketoconazole tablets. See CONTRAINDICATIONS, WARNINGS, and PRECAUTIONS sections. 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. See CONTRAINDICATIONS, WARNINGS, and PRECAUTIONS sections. Coadministration of cisapride with ketoconazole is contraindicated.
Serious cardiovascular adverse events including ventricular tachycardia, ventricular
fibrillation and torsades de pointes have occurred in patients taking ketoconazole
concomitantly with cisapride. See CONTRAINDICATIONS, WARNINGS, and PRECAUTIONS sections.
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dailymed-instance:overdosag... |
In the event of accidental overdosage, supportive
measures, including gastric lavage with sodium bicarbonate, should be employed.
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dailymed-instance:genericMe... |
ketoconazole
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dailymed-instance:fullName |
NIZORAL (Tablet)
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dailymed-instance:adverseRe... |
In rare cases, anaphylaxis
has been reported after the first dose. Several cases of hypersensitivity
reactions including urticaria have also been reported. However, the most frequent
adverse reactions were nausea and/or vomiting in approximately 3%, abdominal
pain in 1.2%, pruritus in 1.5%, and the following in less than 1% of the patients:
headache, dizziness, somnolence, fever and chills, photophobia, diarrhea,
gynecomastia, impotence, thrombocytopenia, leukopenia, hemolytic anemia, and
bulging fontanelles. Oligospermia has been reported in investigational studies
with the drug at dosages above those currently approved. Oligospermia has
not been reported at dosages up to 400 mg daily, however sperm counts have
been obtained infrequently in patients treated with these dosages. Most of
these reactions were mild and transient and rarely required discontinuation
of NIZORAL (ketoconazole) Tablets. In contrast, the rare
occurrences of hepatic dysfunction require special attention . In
worldwide postmarketing experience with NIZORAL Tablets there
have been rare reports of alopecia, paresthesia, and signs of increased intracranial
pressure including bulging fontanelles and papilledema. Hypertriglyceridemia
has also been reported but a causal association with NIZORAL Tablets
is uncertain. Neuropsychiatric disturbances,
including suicidal tendencies and severe depression, have occurred rarely
in patients using NIZORAL Tablets. Ventricular
dysrhythmias (prolonged QT intervals) have occurred with the concomitant use
of terfenadine with ketoconazole tablets. (See BOX
WARNING, CONTRAINDICATIONS,
and WARNINGS sections.) Data suggest
that coadministration of ketoconazole tablets and cisapride can result in
prolongation of the QT interval and has rarely been associated with ventricular
arrhythmias.
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dailymed-instance:indicatio... |
NIZORAL (ketoconazole) Tablets are
indicated for the treatment of the following systemic fungal infections: candidiasis,
chronic mucocutaneous candidiasis, oral thrush, candiduria, blastomycosis,
coccidioidomycosis, histoplasmosis, chromomycosis, and paracoccidioidomycosis.
NIZORAL Tablets should not be used for fungal meningitis
because it penetrates poorly into the cerebral-spinal fluid. NIZORAL Tablets are also indicated for the
treatment of patients with severe recalcitrant cutaneous dermatophyte infections
who have not responded to topical therapy or oral griseofulvin, or who are
unable to take griseofulvin.
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NIZORAL
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