Ketoconazole

Cutaneous Candidiasis, Oral Candidiasis ... show more

DRUG STATUS

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Approvals

US(FDA), UK(BNF)

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Essential Medicine

YES

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Teratogenicity

Unlisted

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Pharmaceutical Class

Azole Antifungal

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Drug Ingredient

Ketoconazole

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Summary

  • Ketoconazole is a strong medicine used for treating serious fungal infections deep inside the body. It's typically used when other treatment options have not worked or are not tolerated by the patient. However, it's not effective for fungal infections of the skin, nails, or the membranes around the brain and spinal cord.

  • Ketoconazole works by inhibiting a fungal enzyme called lanosterol 14-demethylase. This blocks the synthesis of ergosterol, a key component of the fungal cell membrane. Without ergosterol, the fungal cell membrane is disrupted, leading to cell death.

  • For adults, the dosage typically starts at 200 milligrams per day, which can be increased to 400 milligrams if needed. For children over two years old, the dosage is calculated based on weight, typically between 3.3 and 6.6 milligrams per kilogram of body weight. This medicine is not recommended for children under two years old.

  • Common side effects of Ketoconazole include upset stomach, headache, diarrhea, and abnormal liver test results. Rare but serious side effects include liver damage, severe allergic reactions, low adrenal gland function at high doses, and muscle issues when taken with certain other medicines. In rare cases, it can also cause a dangerous heart rhythm problem.

  • Ketoconazole can cause serious problems, including liver damage. It's important to avoid alcohol and other medicines that can harm the liver while taking it. It should not be taken with certain other medications like dofetilide, quinidine, pimozide, lurasidone, cisapride, methadone, disopyramide, dronedarone, or ranolazine as it can cause heart problems. If you experience a rash, itching, swelling, fever, chest pain, or trouble breathing, seek medical attention immediately.

Indications and Purpose

What is Ketoconazole used for?

Ketoconazole is a strong medicine that fights serious fungal infections deep inside the body. It's only used when other medicines haven't worked or if the patient can't tolerate them. It doesn't work for fungal infections of the skin, nails, or the membranes around the brain and spinal cord.

How does Ketoconazole work?

Ketoconazole inhibits the fungal enzyme lanosterol 14α-demethylase, blocking ergosterol synthesis. This disrupts the fungal cell membrane, leading to cell death.

Is Ketoconazole effective?

Studies and clinical trials confirm Ketoconazole's effectiveness for treating systemic fungal infections. However, its use is reserved for situations where alternative antifungal therapies are not viable due to potential severe side effects.

How does one know if Ketoconazole is working?

Improvement in symptoms, lab tests, or imaging may indicate effectiveness. Follow-up with a healthcare provider for monitoring and evaluation.

Directions for Use

What is the usual dose of Ketoconazole?

For grown-ups, the medicine starts at 200 milligrams a day, maybe going up to 400 milligrams if needed. For kids older than two, the amount depends on their weight—it's between 3.3 and 6.6 milligrams for every kilogram they weigh. Doctors don't give this medicine to children younger than two.

How do I take Ketoconazole?

Take your ketoconazole pill once a day. Don't drink alcohol while you're taking it. If you're also taking medicine that reduces stomach acid, drink it with something acidic like regular cola (not diet). If you take something to reduce stomach acid, wait at least an hour before or two hours after taking your ketoconazole pill.

For how long do I take Ketoconazole?

The typical duration for systemic fungal infections is around six months or until the infection has resolved, as directed by a healthcare provider..

Ketoconazole can harm your liver. To be safe, your doctor will check your liver function (ALT levels) every week while you're taking it. If your liver tests show problems or you feel unwell, you'll need to stop taking the medicine. Your doctor will then do more tests to make sure your liver is okay. 

How long does it take for Ketoconazole to start working?

Peak plasma concentrations are typically reached within 1-2 hours after administration. Clinical effectiveness may vary based on the severity of the infection and response to treatment.

How should I store Ketoconazole?

Keep the ketoconazole pills in a cool, dry place. The best temperature is between 68°F and 77°F (20°C and 25°C), but it's okay if it gets a little warmer or cooler, between 59°F and 86°F (15°C and 30°C). Just make sure they don't get wet.

Warnings and Precautions

Who should avoid taking Ketoconazole?

Ketoconazole can cause serious problems for some people. If you've had a bad reaction to it before, don't take it. It can also cause liver damage, even if you're healthy, so your doctor will need to check your liver. Avoid alcohol and other medicines that hurt the liver while taking it. Don't take it with certain other medications (dofetilide, quinidine, pimozide, lurasidone, cisapride, methadone, disopyramide, dronedarone, or ranolazine) because it can cause heart problems. Only take the amount your doctor tells you to. If you have a rash, itching, swelling, fever, chest pain, or trouble breathing, go to the hospital right away. 

Can I take Ketoconazole with other prescription drugs?

Ketoconazole is a medicine that can cause other medicines to build up to dangerously high levels in your blood. This can lead to serious side effects. For example, it can make sleeping pills much stronger, causing excessive sleepiness. It can also increase the risk of muscle problems with certain cholesterol medicines, and cause serious problems with blood circulation and heart rhythm. Because of this risk, it shouldn't be taken with many other medications. Also, people with liver problems shouldn't take ketoconazole at all.

Can I take Ketoconazole with vitamins or supplements?

Consult your doctor. Some supplements may interact with Ketoconazole by altering its absorption or efficacy.

Can Ketoconazole be taken safely while pregnant?

Ketoconazole is a medicine that shouldn't be used during pregnancy unless absolutely necessary. Studies haven't proven it's safe for pregnant women. A doctor would only prescribe it if the benefits to the mother were much greater than the possible harm to the baby. 

Can Ketoconazole be taken safely while breastfeeding?

If you're taking ketoconazole pills, you shouldn't breastfeed. The medicine can get into your breast milk and might harm your baby. Talk to your doctor to figure out the best choice for you and your baby.

Is Ketoconazole safe for the elderly?

Ketoconazole is a strong medicine with serious side effects, so it's only used when other options don't work. Older people, like everyone else taking it, need close monitoring of their liver because it can be harmed. Doctors will check liver function regularly. Avoid alcohol and other medicines that can hurt the liver while taking ketoconazole. Stop taking it immediately if you have liver problems.

Is it safe to exercise while taking Ketoconazole?

Taking the medicines ketoconazole and simvastatin or lovastatin together can sometimes cause muscle problems. We don't know if this risk changes with how much you exercise.

Is it safe to drink alcohol while taking Ketoconazole?

Ketoconazole is a medicine. Alcohol can make it harder for your body to use ketoconazole properly, meaning the medicine might not work as well. It can also increase the chance of getting side effects. So, it's best to avoid drinking alcohol while you're taking this medicine.