Ketoconazole

Ketoconazole is both an over-the-counter and a prescription medication. The over-the-counter form is used to treat dandruff. The prescription form is used to treat serious fungal infections that can spread to different parts of the body.

Ketoconazole belongs to a class of drugs called antifungals, which work by slowing the growth of fungi that cause infection.

This medication comes in tablet form and is taken once daily, with or without food. It is also available as a topical gel, cream, and foam and as a shampoo. A form of the shampoo is available without a prescription.

Common side effects of ketoconazole tablets include nausea, vomiting, stomach pain, and diarrhea. Ketoconazole tablets can also cause dizziness and drowsiness. Do not drive or operate heavy machinery until you know how it affects you.

Ketoconazole is a prescription medication used to treat fungal infections, including the following: blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, and paracoccidioidomycosis for patients in which other treatments have failed or who are intolerant to other therapies.

Ketoconazole tablets are not for people with fungal nail infections.

Ketoconazole is also available in topical forms - a gel, cream, foam, and shampoo - to treat forms of dermatitis and fungal infections of the skin. A form of the shampoo is available without a prescription for the treatment of dandruff.

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Ketoconazole may be found in some form under the following brand names:

• Extina

• Ketodan

• Kuric

• Nizoral

• Pharmaseb

• T8 Keto Flush

• Vital-Ketodine

• Xolegel

Serious side effects have been reported. See the “Ketoconazole Precautions” section.

Common side effects of ketoconazole tablets include:

• nausea
• vomiting
• stomach pain
• diarrhea
• headache
• drowsiness
• dizziness
• fever
• chills
• sensitivity to sunlight

Common side effects of ketoconazole shampoo include:

• rash
• worsening of dandruff

Common side effects of ketoconazole gel, cream, and foam include:

• redness, pain, and skin irritaion at the site of application

This is not a complete list of ketoconazole side effects. Ask your doctor or pharmacist for more information.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Tell your doctor about all the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements. Especially tell your doctor if you take:

• medications that use the enzyme CYP3A4 such as budesonide (Entocort), cyclosporine (Neoral, Gengraf, Sandimmune), darifenacin (Enablex), dihydroergotamine (Migranal), fentanyl (Abstral, Fentora, Onsolis, Actiq), pimozide (Orap), quinidine (Cardioquin, Duraquin, Quinact), sirolimus (Rapamune), tacrolimus (Prograf), terfenadine (Seldane), fluticasone (Flovent HFA, Flonase), eletriptan (Relpax), lovastatin (Mevacor), quetiapine (Seroquel), sildenafil (Viagra, Revatio), and simvastatin (Zocor)
• medications that block the enzyme CYP3A4 such as some macrolide antibiotics (clarithromycin, telithromycin), some HIV protease inhibitors (indinavir, nelfinavir, ritonavir, saquinavir), some HCV protease inhibitors (boceprevir, telaprevir), some azole antifungals (ketoconazole, itraconazole, posaconazole, voriconazole), conivaptan, delavirdine, and nefazodone
• medications that increase the activity of the enzyme CYP3A4 such as carbamazepine (Tegretol, Equetro, Carbatrol), phenobarbital, phenytoin (Dilantin), rifampin (Rifadin), St John's wort, and nimodipine (Nimotop)
• methylprednisolone (Medrol)
• midazolam (Versed)
• triazolam (Halcion)
• digoxin (Lanoxin)
• warfarin (Coumadin, Jantoven)
• phenytoin (Dilantin)
• rifampin (Rifadin)
• alcohol

This is not a complete list of ketoconazole drug interactions. Ask your doctor or pharmacist for more information.

Serious side effects have been reported with ketoconazole including the following:

• liver problems. Some people who were treated with ketoconazole had serious liver problems that led to death or the need for a liver transplant. Call your healthcare provider right away if you have any of the following symptoms:
  • loss of appetite or start losing weight
  • nausea or vomiting
  • feel tired
  • stomach pain or tenderness
  • dark urine or light colored stools
  • yellowing of your skin or the whites of your eyes
  • fever or rash
• changes in the electrical activity of your heart called QT prolongation. QT prolongation can cause irregular heartbeats that can be life threatening. This can happen when ketoconazole tablets are taken with certain medicines, such as dofetilide (Tikosyn), quinidine (Cardioquin, Duraquin, Quinact), and pimozide (Orap). Talk to your healthcare provider about other medicines you are taking before you start taking ketoconazole tablets. Tell your healthcare provider right away if you feel faint, light-headed, dizzy, or feel your heart beating irregularly or fast. These may be symptoms related to QT prolongation.
• adrenal insufficiency. Adrenal insufficiency is a condition in which the adrenal glands do not make enough steroid hormones. ketoconazole tablets may cause adrenal insufficiency if you take a high dose. Your healthcare provider will follow you closely if you have adrenal insufficiency or if you are taking prednisone or other similar medicines for long periods. Call your healthcare provider right away if you have symptoms of adrenal insufficiency such as tiredness, weakness, dizziness, nausea, and vomiting.
• serious allergic reactions. Some people can have a serious allergic reaction to ketoconazole tablets. Stop taking ketoconazole tablets and go to the nearest hospital emergency room right away if you have any signs or symptoms of a serious allergic reaction:
  • a rash
  • itching
  • hives
  • fever
  • swelling of the lips or tongue
  • chest pain
  • difficulty breathing
• muscle problems. Taking certain medicines with ketoconazole tablets may cause muscle problems. These medicines include simvastatin (Zocor) and lovastatin (Mevacor).

Ketoconazole can cause dizziness and drowsiness. Do not drive or operate heavy machinery until you know how ketoconazole affects you.

Do not take ketoconazole if you:

• are allergic to ketoconazole or to any of its ingredients
• have liver problems
• are taking the following medications:
  • dofetilide (Tikosyn)
  • quinidine (Cardioquin, Duraquin, Quinact)
  • pimozide (Orap)
  • cisapride (Propulsid)
  • simvastatin (Zocor)
  • lovastatin (Mevacor, Altocor, Altoprev, Advicor)
  • eplerenone (Inspra)
  • dihydroergotamine (Migranal)
  • ergotamine (Cafergot, Ercaf)
  • nisoldipine (Sular)
  • triazolam (Halcion)
  • midazolam (Versed)
  • alprazolam (Xanax)

Medications can interact with certain foods. In some cases, this may be harmful and your doctor may advise you to avoid certain foods. In the case of ketoconazole, there are no specific foods that you must exclude from your diet when receiving this medication.

Before taking ketoconazole, tell your doctor about all of your medical conditions. Especially tell your doctor if you:

• are allergic to ketoconazole or to any of its ingredients
• have had an abnormal heart rhythm tracing (ECG) or if anyone in your family have or have had a heart problem called “congenital long QT syndrome”
• have liver problems
• have adrenal insufficiency
• are pregnant or plan to become pregnant
• are breastfeeding or plan to breastfeed. You should NOT do both.

Tell your doctor if you are pregnant or plan to become pregnant.

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.

Ketoconazole falls into category C. In animal studies, pregnant animals were given this medication and had some babies born with problems. There are no well-controlled studies that have been done in humans with ketoconazole, though. Therefore, this medication may be used if the potential benefits to the mother outweigh the potential risks to the unborn child.

Tell your doctor if you are breastfeeding or plan to breastfeed.

It is not known if ketoconazole crosses into human milk. Because many medications can cross into human milk and because of the possibility for serious adverse reactions in nursing infants with use of this medication, a choice should be made whether to stop nursing or stop the use of this medication. Your doctor and you will decide if the benefits outweigh the risk of using ketoconazole.

Take ketoconazole exactly as prescribed.

This medication comes in tablet form and is taken once daily, with or without food.

Ketoconazole tablets should only be used in children if prescribed by the healthcare provider who has determined that the benefits outweigh the risks.

This medication is also available as a shampoo to treat dandruff and flaking scalp.

This medication is also available a topical gel, cream, and foam to treat seborrheic dermatitis and fungal infections of the skin.

Alcohol may intensify some of the side effects of this medication.

If you miss a dose, take the missed dose as soon as you remember. If it is almost time for the next dose, skip the missed dose and take your next dose at the regular time. Do not take two doses of ketoconazole at the same time.

Take ketoconazole exactly as prescribed by your doctor. Follow the directions on your prescription label carefully.

The ketoconazole dose your doctor recommends will be based on the following:

• the condition being treated
• other medical conditions you have
• other medications you are taking
• how you respond to this medication
• your liver function
• your kidney function
• your age

The recommended dose for ketoconazole is 200 mg (one tablet) one daily. In very serious infections or if responsiveness is insufficient within the expected time, the dose of ketoconazole may be increased to 400 mg (two tablets) once daily.

In a small number of children over 2 years of age, a single daily dose of 3.3 to 6.6 mg/kg has been used. ketoconazole have not been studied in children under 2 years of age.

The recommended dose of the over-the-counter form of ketoconazole shampoo for the treatment of dandruff is the application of shampoo to wet hair; lather, rinse, and repeat. Use the shampoo every 3 to 4 days for up to 8 weeks, or as directed by a doctor.

The recommended dose of the prescription form of ketoconazole shampoo for the treatment of dandruff is one application onto damp skin. Leave shampoo in place for 5 minutes, then rinse with water.

The recommended dose of the topical gel and foam is application to the affected area twice daily. The recommended dose of the topical cream is application to the affected area once daily.

If you take too much ketoconazole, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.

• Store at room temperature between 15°–25°C (59°–77°F).
• Keep tablets dry.
• Protect topical forms of keotconazole from freezing.
• Keep this and all medicines out of the reach of children.

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.

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.

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.

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.