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Ketoconazole is authorised in the world under the following brand names: Extina, Fungarest, Fungoral, Ketoderm, Ketoisdin, Ketozole, Nizoral, Nizoral a-D, Nizoral a-D Shampoo, Nizoral Cream, Nizoral Shampoo, Orifungal, Orifungal M, Panfungol, Sebazole.

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Ketoconazole: Side Effects See also Antifungal azoles Ketoconazole was the first azole available for oral administration. However, it has been supplanted by newer azoles with fewer adverse effects and more reliable absorption from the gastrointestinal tract. Even after years of use, new adverse effects (often related to high doses and/or newer indications) continue to be reported. Ketoconazole is water-soluble at a pH of below 3. Its oral absorption is influenced by the acidity of the stomach contents, and the concomitant administration of histamine H2 receptor antagonists, proton pump inhibitors, antacids, or food affects its absorption. A high carbohydrate meal ingested with ketoconazole reduces total drug absorption, while a high lipid meal …

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Ketoconazole: Drug-Drug Interactions Aciclovir Ketoconazole seems to have a synergistic antiviral effect when it is taken with aciclovir. Alcohol A disulfiram-type reaction of ketoconazole with alcohol has been reported. Amphotericin Combination of ketoconazole with amphotericin reportedly leads to antagonism, particularly if ketoconazole therapy precedes amphotericin. Antacids Co-administration of antacids reduces the absorption of ketoconazole. Antihistamines Ketoconazole can increase the concentrations of astemi-zole and terfenadine by inhibition of CYP3A4. High concentrations of terfenadine can cause cardiac toxicity. Increased plasma concentrations of unmetabolized terfenadine prolong the QT interval and carry the risk of torsade de pointes and other fatal ventricular arrhythmias. Ebastine (10 and 20 mg/day) had no clinically important effect on QTC …

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Ketoconazole: Organs and Systems Respiratory Patients undergoing esophagectomy are at increased risk of acute lung injury, perhaps related to increased concentrations of thromboxane in the postpulmonary circulation. In 38 consecutive patients undergoing esophagectomy, perioperative ketoconazole, which inhibits thromboxane synthesis, reduced the incidence of acute lung injury. Nervous system Headache, dizziness, nervousness, and somnolence have been reported. The incidences are low. Encephalopathy can occur as a result of severe liver damage. Sensory systems Eyes Papilledema has been reported in one patient taking ketoconazole. The condition cleared on withdrawal of ketoconazole and recurred on resumption 2 months later. Psychological, psychiatric In one patient taking a high dosage for prostate cancer, weakness was associated …


Description of Medical Condition Pulmonary fungal infection endemic to the Southwest USA. Can become progressive and involve extrapulmonary sites, including bone, CNS, and skin. Known as the “great imitator.” Incubation period is 1 to 4 weeks after exposure. System(s) affected: Pulmonary, Nervous, Musculoskeletal, Skin/Exocrine, Endocrine/Metabolic Genetics: Unknown Incidence/Prevalence in USA: 100,000 cases per year. (0.5% extrapulmonary) Predominant age: All ages Predominant sex: Male = Female Medical Symptoms and Signs of Disease • Note: Over half of cases are subclinical • Anorexia • Arthralgias • Chest pain • Chills • Confusion • Cough, dry or productive • Cyanosis • Dyspnea • Erythema nodosum • Fatigue • Fever • Headache • Malaise • …

Candidiasis Mucocutaneous

Description of Medical Condition A mucocutaneous disorder caused by infection with various species of Candida. Candida is normally present, in very small amounts, in the oral cavity, gastrointestinal tract, and female genital tract. • Candida vulvovaginitis — infection on the vaginal mucosa, often associated with cutaneous vulvar involvement • Orophatyngeal candidiasis — infection of the oral cavity (“thrush”) and/or pharynx. • Candida esophagitis — usually associated with an immunosuppressed host • Gastrointestinal candidiasis — gastritis, sometimes with ulcers, usually associated with thrush. The small and large bowel can also be affected. • Angular cheilitis — fissures formed by Candida infection at the corners of the mouth. System(s) affected: Skin/Exocrine, Gastrointestinal Genetics: …


Description of Medical Condition An uncommon, systemic, fungal infection with a broad range of manifestations including pulmonary, skin, bone and genitourinary involvement System(s) affected: Skin/Exocrine, Pulmonary, Musculoskeletal, Renal/Urologic, Endocrine/Metabolic Genetics: N/A Incidence/Prevalence in USA: Ranges from 0.4-4 cases per 100,000 population per year. Higher prevalence in states bordering the Mississippi and Ohio Rivers. Sporadic cases occurring in other areas. Predominant age: Adults, but 10-20% of cases occur in children Predominant sex: Male > Female Medical Symptoms and Signs of Disease • Acute infection – Onset may be abrupt or insidious – May be asymptomatic and self-limiting – Incubation period 30-45 days – Fever, chills, myalgias, arthralgias – Cough initially nonproductive, then …

Antifungal Agents

Fungi are eukaryotes, and they share many of the structural and metabolic characteristics of human cells. As a result, designing agents that affect fungi without harming human cells has proved difficult. One major difference between the two cell types is the primary sterol building block used to form the plasma membrane. The fungal plasma membrane consists of ergosterols; the major sterol component of the human plasma membrane is cholesterol. This difference has been exploited in the development of two classes of drugs. The polyenes act by binding to ergosterol and disrupting the fungal membrane. These agents are fungicidal. The azoles inhibit ergosterol synthesis, and lowered ergosterol levels results in fungal membrane …

Antimicrobial therapy: general principles

A wide variety of antimicrobial agents is available to treat established infections caused by bacteria, fungi, viruses, or parasites. This section will cover the general principles of antimicrobial therapy and will also include illustrative clinical problems to emphasize proper decision-making in using antimicrobials. Determinants of Antimicrobial Efficacy Measurement of antimicrobial activity in vitro Susceptibility testing is indicated for any bacterial pathogen warranting chemotherapy. Drugs that irreversibly destroy the ability of an organism to replicate, and perhaps in the process destroy the structural integrity of the organism, are microbicidal. Drugs that reversibly impair replicating ability, with this function being restored when drug concentrations fall below critical inhibitory levels, are microbiostatic. In quantitative …

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Ketoconazole • Ketoconazole, a synthetic imidazole derivative, is an azole antifungal agent. Dosage and Administration • Administration Ketoconazole is administered orally. To ensure absorption in patients with achlorhydria, it has been recommended that each 200 mg of ketoconazole be dissolved in 4 mL of 0.2N hydrochloric acid solution or taken with 200 mL of 0.1N hydrochloric acid. The resultant solution should be administered via a plastic or glass straw to avoid contact with the teeth, and a glass of water should be administered immediately after the solution. Alternatively, some clinicians have recommended that each 200 mg of ketoconazole be given with 680 mg or more of glutamic acid hydrochloride. Other clinicians …

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Ketoconazole: Cautions • GI Effects The most frequent adverse reactions to ketoconazole are nausea and/or vomiting which have been reported in 3-10% of patients receiving the drug. Abdominal pain, constipation, flatulence, GI bleeding, and diarrhea have also been reported in 1% or less of patients receiving the drug. Adverse GI effects appear to be dose related, are reported less frequently when ketoconazole is administered with food, and usually subside with continued therapy with the drug. • Hepatic Effects Transient increases in serum AST (SGOT), ALT (SGPT), and alkaline phosphatase concentrations have been reported during ketoconazole therapy. Hepatotoxicity, which may be hepatocellular (in most cases), cholestatic, or a mixed pattern of injury, …

Dosage forms of Ketoconazole:
Ketoconazole 2% cream Nizoral 2% cream Apo-Ketoconazole 200 mg Tablet Novo-Ketoconazole 200 mg Tablet
Nu-Ketocon 200 mg Tablet Kuric 2% cream Ketoconazole 200 mg tablet Extina 2% foam
Nizoral 200 mg tablet Ketoconazole powder Ketoconazole 2% Cream 15 gm Tube Ketoconazole 2% Shampoo 120ml Bottle
Ketoconazole 2% Cream 30 gm Tube Ketoconazole 2% Cream 60 gm Tube Nizoral 2% Shampoo 120ml Bottle Extina 2% Foam 50 gm Can
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Synonyms of Ketoconazole:

2%, Ketocanazole, Ketoconazol, Ketoconazol [INN-Spanish], Ketoconazole, Ketoconazole [Usan:Ban:Inn:Jan], Ketoconazolum [INN-Latin]

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