Ketoconazole used for. Ketoconazole Topical: Uses, Dosage, and Side Effects | Comprehensive Guide

12.03.197729.10.2021 by alexxlab

What is ketoconazole topical used for. How to apply ketoconazole topical correctly. What are the potential side effects of ketoconazole topical. When should you consult a healthcare provider before using ketoconazole topical. How to store and handle ketoconazole topical properly. What precautions should be taken while using ketoconazole topical. How to manage missed doses and potential overdose situations with ketoconazole topical.

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Understanding Ketoconazole Topical: An Antifungal Powerhouse

Ketoconazole topical is a potent antifungal medication designed for external use on the skin. This versatile treatment tackles a range of fungal infections, providing relief for countless individuals struggling with common skin conditions.

Primary Uses of Ketoconazole Topical

Ketoconazole topical is primarily prescribed for:

Athlete’s foot
Jock itch
Ringworm
Seborrhea (including dandruff and dry, flaking skin)
Pityriasis (a condition causing scaly, discolored patches on the skin)

Can ketoconazole topical be used for other purposes? Indeed, healthcare providers may occasionally prescribe this medication for off-label uses not listed in the standard medication guide. However, it’s crucial to use ketoconazole topical only as directed by a qualified medical professional.

Essential Precautions: When to Consult Your Healthcare Provider

Before incorporating ketoconazole topical into your treatment regimen, it’s vital to have an open dialogue with your healthcare provider. Certain conditions and factors may influence the safety and efficacy of this medication.

Key Considerations for Ketoconazole Topical Use

Are you a suitable candidate for ketoconazole topical treatment? Consider the following factors:

Allergies: Inform your doctor if you have a known allergy to ketoconazole or other antifungal medications.
Asthma or sulfite sensitivity: These conditions may affect your ability to use certain formulations of ketoconazole topical.
Pregnancy: Consult your doctor before using ketoconazole topical if you are pregnant or planning to become pregnant.
Breastfeeding: Ketoconazole topical is not recommended for use while breastfeeding.
Pediatric use: Always follow specific instructions when using this medication on children.

Do these precautions apply to everyone? While these guidelines are generally applicable, individual circumstances may vary. Your healthcare provider is best equipped to assess your specific situation and provide tailored advice.

Proper Application Techniques for Optimal Results

Maximizing the efficacy of ketoconazole topical hinges on correct application. Following the prescribed instructions meticulously ensures the best possible outcome while minimizing the risk of side effects.

Step-by-Step Guide to Applying Ketoconazole Topical

Thoroughly wash and dry the affected area before application.
Clean your hands before and after using the medication.
Apply a thin layer of the product to the affected skin and surrounding areas.
Avoid applying to open wounds or irritated skin.
If using the shampoo formulation, allow at least three days between applications.

Is it safe to use more product for faster results? Applying more ketoconazole topical than prescribed or using it more frequently will not accelerate healing and may increase the risk of side effects. Stick to the recommended dosage and frequency.

Navigating Potential Side Effects and Adverse Reactions

While ketoconazole topical is generally well-tolerated, it’s essential to be aware of potential side effects and know when to seek medical attention.

Common and Serious Side Effects

What side effects should you watch for when using ketoconazole topical?

Mild irritation, burning, or stinging at the application site (common)
Severe skin irritation or allergic reactions (rare but serious)
Signs of an allergic reaction: hives, difficulty breathing, swelling of face, lips, tongue, or throat (emergency)

When should you contact your healthcare provider about side effects? If you experience severe irritation, signs of an allergic reaction, or any unusual symptoms, seek medical attention immediately. For mild, tolerable side effects, consult your doctor if they persist or worsen over time.

Storage, Handling, and Special Considerations

Proper storage and handling of ketoconazole topical ensure its effectiveness and safety throughout its intended use period.

Guidelines for Ketoconazole Topical Storage

Store at room temperature
Protect from light
Do not refrigerate or freeze
Keep out of reach of children

Are there any special handling precautions? Some formulations of ketoconazole topical may be flammable. Avoid using near high heat, open flames, or while smoking. Allow the medication to dry completely on your skin before exposing the treated area to heat sources.

Managing Missed Doses and Potential Overdose Situations

Adherence to the prescribed treatment regimen is crucial for the effectiveness of ketoconazole topical. However, life sometimes interferes with the best-laid plans.

Addressing Missed Doses

How should you handle a missed dose of ketoconazole topical? If you forget to apply the medication, use it as soon as you remember. However, if it’s almost time for your next scheduled application, skip the missed dose and resume your regular schedule. Never apply a double dose to make up for a missed one.

Overdose Concerns

Is an overdose of ketoconazole topical dangerous? While an overdose is not typically expected to be harmful when used topically, accidental ingestion can be dangerous. If someone has swallowed the medication, contact emergency services or the Poison Help line immediately at 1-800-222-1222.

Lifestyle Considerations and Precautions During Treatment

To maximize the benefits of ketoconazole topical and minimize potential complications, certain lifestyle adjustments and precautions are recommended during treatment.

Key Precautions and Recommendations

Avoid tight-fitting, synthetic clothing over treated areas
Keep treated feet dry and wear breathable footwear
Follow sun exposure guidelines, especially when treating pityriasis
Avoid using potentially irritating skin products in conjunction with ketoconazole topical
Do not use other medications on treated areas unless directed by your doctor

How can these precautions improve treatment outcomes? By following these guidelines, you create an environment that supports healing and reduces the risk of complications or treatment interference.

Monitoring Treatment Progress and Seeking Further Medical Advice

Effective use of ketoconazole topical involves not just proper application, but also vigilant monitoring of your condition and open communication with your healthcare provider.

Assessing Treatment Effectiveness

When should you expect to see improvement? Most individuals begin to notice positive changes within 2 to 4 weeks of starting treatment. If you don’t see improvement within this timeframe or if your condition worsens, it’s crucial to consult your doctor.

What signs indicate a need for medical re-evaluation?

Lack of improvement after 4 weeks of treatment
Worsening of symptoms
Development of new symptoms or side effects
Spread of the infection to new areas

Regular check-ins with your healthcare provider ensure that your treatment plan remains effective and allows for timely adjustments if needed.

Ketoconazole topical stands as a powerful ally in the fight against various fungal skin infections. By understanding its proper use, potential side effects, and necessary precautions, patients can maximize the benefits of this medication while minimizing risks. Remember, while this guide provides comprehensive information, it’s no substitute for personalized medical advice. Always consult with your healthcare provider for guidance tailored to your specific needs and circumstances.

ketoconazole topical | Michigan Medicine

What is the most important information I should know about ketoconazole topical?

Follow all directions on your medicine label and package. Tell each of your healthcare providers about all your medical conditions, allergies, and all medicines you use.

What is ketoconazole topical?

Ketoconazole topical (for the skin) is an antifungal medicine used to treat infections such as athlete’s foot, jock itch, ringworm, and seborrhea (dry, flaking skin or dandruff).

Ketoconazole topical is also used to treat a fungal infection called pityriasis, which causes scaly discolored patches on the skin of the neck, chest, arms, or legs.

Ketoconazole topical may also be used for purposes not listed in this medication guide.

What should I discuss with my healthcare provider before using ketoconazole topical?

You should not use this medicine if you are allergic to ketoconazole.

Ask a doctor or pharmacist if this medicine is safe to use if you have:

asthma or a sulfite allergy;
an allergic reaction to an antifungal medicine, such as clotrimazole, econazole, or miconazole.

Ask a doctor before using this medicine if you are pregnant.

You should not breast-feed while using ketoconazole topical.

Always follow directions on the medicine label about using this medicine on a child.

How should I apply ketoconazole topical?

Use exactly as directed on the label, or as prescribed by your doctor.

Using more of this medicine or applying it more often than prescribed will not make it work any faster, and may increase side effects.

Do not take by mouth. Topical medicine is for use only on the skin. Do not use on open wounds or irritated skin. Rinse with water if this medicine gets in your eyes, nose, or mouth.

Read and carefully follow any Instructions for Use provided with your medicine. Ask your doctor or pharmacist if you do not understand these instructions.

Wash your hands before and after using this medicine.

Clean and dry the skin before applying ketoconazole cream, foam, or gel.

This medicine may be flammable. Do not use near high heat or open flame, or while smoking. Avoid heat or smoking until the medicine has completely dried on your skin.

Ketoconazole shampoo is not for daily use. Allow at least 3 days to pass between uses.

Use this medicine for the full prescribed length of time, even if your symptoms quickly improve. Skipping doses can increase your risk of infection that is resistant to medication.

Call your doctor if your symptoms do not begin to improve after 2 to 4 weeks of treatment, or if your condition gets worse.

Store ketoconazole topical at room temperature. Protect from light and do not refrigerate or freeze.

What happens if I miss a dose?

Use the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not use two doses at one time.

What happens if I overdose?

An overdose of ketoconazole topical is not expected to be dangerous. Seek emergency medical attention or call the Poison Help line at 1-800-222-1222 if anyone has accidentally swallowed the medication.

What should I avoid while using ketoconazole topical?

Do not get this medicine in your eyes. If contact does occur, rinse with water.

Avoid covering treated skin areas with tight-fitting, synthetic clothing (such as nylon or polyester) that doesn’t allow air to circulate to your skin. If you are treating your feet, wear clean cotton socks and sandals or shoes that allow for air circulation. Keep your feet as dry as possible.

You may need to avoid sunlight if you are treating pityriasis. Follow your doctor’s instructions.

Avoid using skin products that can cause irritation, such as harsh soaps, shampoos, hair coloring or permanent chemicals, hair removers or waxes, or skin products with alcohol, spices, astringents, or lime.

Avoid using other medications on the areas you treat with ketoconazole topical unless your doctor tells you to.

What are the possible side effects of ketoconazole topical?

Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have:

burning, stinging, or severe irritation after using this medicine;
redness, pain, or oozing of treated skin; or
shortness of breath.

Common side effects may include:

thinning hair;
changes in the color or texture of your hair;
dry skin; or
mild itching.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect ketoconazole topical?

Medicine used on the skin is not likely to be affected by other drugs you use. But many drugs can interact with each other. Tell each of your healthcare providers about all medicines you use, including prescription and over-the-counter medicines, vitamins, and herbal products.

Where can I get more information?

Your pharmacist can provide more information about ketoconazole topical.

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.
Every effort has been made to ensure that the information provided by Cerner Multum, Inc. (‘Multum’) is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum’s drug information does not endorse drugs, diagnose patients or recommend therapy. Multum’s drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.
Copyright 1996-2021 Cerner Multum, Inc. Version: 5.02. Revision date: 3/17/2020.

Ketoconazole Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing

Ketoconazole Topical: MedlinePlus Drug Information

Prescription ketoconazole comes as a cream and a shampoo to apply to the skin. Over-the-counter ketoconazole comes as a shampoo to apply to the scalp. Ketoconazole cream is usually applied once a day for 2 to 6 weeks. Prescription ketoconazole shampoo is usually applied one time to treat the infection. Over-the-counter ketoconazole shampoo is usually used every 3 to 4 days for up to 8 weeks, and then used as needed to control dandruff. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Use ketoconazole exactly as directed. Do not use more or less of it or use it more often than prescribed by your doctor.

One treatment with prescription ketoconazole shampoo may successfully treat your tinea versicolor infection. However, it may take several months for your skin color to return to normal, especially if your skin is exposed to sunlight. After your infection is treated, there is a chance that you will develop another tinea versicolor infection.

If you are using over-the-counter ketoconazole shampoo to treat dandruff, your symptoms should improve during the first 2 to 4 weeks of your treatment. Call your doctor if your symptoms do not improve during this time or if your symptoms get worse at any time during your treatment.

If you are using ketoconazole cream, your symptoms should improve at the beginning of your treatment. Continue to use ketoconazole cream even if you are feeling well. If you stop using ketoconazole cream too soon, your infection may not be completely cured and your symptoms may return.

Ketoconazole cream and shampoos are only for use on the skin or scalp. Do not let ketoconazole cream or shampoo get into your eyes or mouth, and do not swallow the medication. If you do get ketoconazole cream or shampoo in your eyes, wash them with plenty of water.

To use the cream, apply enough cream to cover the affected area and all of the skin around it.

To use the prescription shampoo, follow these steps:

Use a small amount of water to wet your skin in the area where you will apply ketoconazole shampoo.
Apply the shampoo to the affected skin and a large area around it.
Use your fingers to rub the shampoo until it forms a lather.
Leave the shampoo on your skin for 5 minutes.
Rinse the shampoo off of your skin with water.

To use the over-the-counter shampoo, follow these steps:

Be sure that your scalp is not broken, cut, or irritated. Do not use ketoconazole shampoo if your scalp is broken or irritated.
Wet your hair thoroughly.
Apply the shampoo to your hair.
Use your fingers to rub the shampoo until it forms a lather.
Rinse all of the shampoo out of your hair with plenty of water.
Repeat steps 2 to 5.

Ketoconazole : an antifungal medicine used to treat skin infections

Always follow the instructions that come with your medicine, or your doctor’s advice.

How long you use ketoconazole for and how often depends on the type of skin problem you have.

How often to use cream for athlete’s foot, jock itch and sweat rash

Use the cream once or twice a day on the infected skin and surrounding area. For athlete’s foot, you need to use it twice a day regularly.

Carry on using the cream for 3 days after your symptoms have cleared up, to stop the infection coming back.

How often to use shampoo or cream for seborrhoeic dermatitis

Use the shampoo twice a week for 2 to 4 weeks until your symptoms have cleared. Then use it once every 1 to 2 weeks, to stop them coming back.

Alternatively, you can use the cream once or twice a day, for 2 to 4 weeks, and then use the shampoo once every 1 to 2 weeks to stop your symptoms coming back.

How often to use shampoo for dandruff

Use the shampoo twice a week for 2 to 4 weeks, then once every 1 to 2 weeks to stop your dandruff coming back.

How often to use cream or shampoo for pityriasis versicolor

Use the shampoo once a day, for up to 5 days.

For treating small areas of skin, you can use the cream instead. Put the cream on once or twice a day for 2 to 3 weeks.

If your symptoms tend to return in sunlight, use the shampoo once a day for up to 3 days before going out in the sun.

How to use ketoconazole cream

Wash and dry the infected area of skin. If you’re treating your feet, make sure you dry between your toes.
Use your own towel or flannel. This stops you passing the infection on to anyone else.
Gently rub the cream into the infected area and surrounding skin. You’ll usually need a small amount, depending on the size of the area you’re treating. Be careful not to let the cream get into your eyes or mouth. If it does get into your eyes or mouth, rinse them with water.
Wash your hands afterwards. This stops you spreading the infection to other parts of your body or other people.

If you’re using any other creams, ointments or lotions on the same area of skin, do not put them on at the same time as ketoconazole cream. After putting on the ketoconazole cream, wait 30 minutes before you use different products on the same area. This gives the ketoconazole time to be absorbed into your skin.

How to use ketoconazole shampoo

Rinse your hair or the infected area of skin with water.
Shake the shampoo bottle, then squeeze a small amount onto the infected area.
If you’re treating your scalp, massage the shampoo into your scalp until it makes a lather.
Leave the shampoo on for 3 to 5 minutes, then wash it off with water. Try not to get the shampoo into your eyes or mouth. If it gets into your eyes or mouth, rinse them with water.
Wash your hands afterwards. This stops you spreading the infection to other parts of your body or other people.

What if I forget to use it?

If you forget to use your ketoconazole cream or shampoo, just skip the missed dose and then keep to your usual routine.

What if I use too much?

If you use too much ketoconazole shampoo or cream, or use it more often than you need to, it may make your skin irritated or red. If this happens, use less the next time.

Ketoconazole skin cream

What is this medicine?

KETOCONAZOLE (kee toe KON na zole) is an antifungal medicine. This cream is used to treat certain kinds of fungal or yeast infections of the skin.

This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

COMMON BRAND NAME(S): Kuric, Nizoral

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:

an unusual or allergic reaction to ketoconazole, itraconazole, miconazole, sulfites, other foods, dyes or preservatives
pregnant or trying to get pregnant
breast-feeding

How should I use this medicine?

This medicine is for external use only. Follow the directions on the prescription label. Wash your hands before and after use. If treating a hand or nail infection, wash hands before use only. Apply a thin layer of cream to cover the affected skin and surrounding area. You can cover the area with a sterile gauze dressing or bandage. Do not use an airtight bandage, such as a plastic covered bandage. Do not get the cream in your eyes. If you do, rinse out with plenty of cool tap water. Finish the full course prescribed by your doctor or health care professional even if you think your condition is better. Do not stop using except on the advice of your doctor or health care professional.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.

NOTE: This medicine is only for you. Do not share this medicine with others.

What if I miss a dose?

If you miss a dose, use it as soon as you can. If it is almost time for your next dose, use only that dose. Do not use double or extra doses.

What may interact with this medicine?

Interactions are not expected. Do not use any other skin products without telling your doctor or health care professional.

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Tell your doctor or health care professional if your symptoms do not begin to improve in 1 to 2 weeks.

If you are using this medicine for jock itch be sure to dry the groin completely after bathing. Do not wear underwear that is tight fitting or made from synthetic fibers like rayon or nylon. Wear loose fitting, cotton underwear.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:

allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
pain, tingling, numbness

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Keep container tightly closed. Throw away any unused medicine after the expiration date.

NOTE: This sheet is a summary. It may not cover all possible information. If you have questions about this medicine, talk to your doctor, pharmacist, or health care provider.

Ketoconazole – StatPearls – NCBI Bookshelf

Continuing Education Activity

Ketoconazole is a drug used in the management and treatment of fungal infections. It is in the imidazole antifungal class of medications. This activity describes the indications, actions, and contraindications of ketoconazole as a valuable agent in treating fungal infections. This activity will highlight the mechanism of action, adverse event profile, and other key factors pertinent to members of the interprofessional team in the treatment of patients with fungal infection.

Objectives:

Identify the mechanism of action of ketoconazole.
Describe the adverse effects of ketoconazole.
Review the appropriate monitoring of ketoconazole.
Summarize some interprofessional team strategies for improving care coordination and communication to advance ketoconazole and improve outcomes.

Access free multiple choice questions on this topic.

Indications

Ketoconazole has approval for use in the treatment of fungal infections of the skin and systemic fungal infections.[1] These include blastomycosis, histoplasmosis, paracoccidioidomycosis, coccidioidomycosis, and chromomycosis. The most common use of ketoconazole for skin infections is that of tinea versicolor.[2] Due to the advent of more effective fungal infection treatment options, ketoconazole is typically not the first-line medication anymore. It should only be an option when other first-line treatments are not available or not tolerated by the patient. [3]

The use of this drug requires a careful risk-benefit analysis when selecting ketoconazole as the treatment of fungal infections. Clinicians should avoid using ketoconazole in the treatment of onychomycosis, cutaneous dermatophyte, and candida infections.[3] Ketoconazole is not indicated in the treatment of fungal meningitis because it does not penetrate the cerebrospinal fluid. Some of the off-label uses of ketoconazole include Cushing syndrome and prostate cancer.[4]

Mechanism of Action

Ketoconazole works as an antifungal agent by inhibiting the cytochrome P450 14α-demethylase enzyme. This enzyme is responsible for inhibiting the biosynthesis of triglycerides and phospholipids by fungi.[5] More specifically, ketoconazole inhibits the synthesis of lanosterol, a necessary precursor for ergosterol biosynthesis. Ergosterol is needed to maintain the integrity of the membrane of fungi.[6] Without ergosterol, the fluidity of the membrane increase, which in turn prevents fungal growth. Ketoconazole, in high doses, can competitively bind to androgen receptors, such as that of testosterone and dihydrotestosterone, which can decrease the activity of testosterone and dihydrotestosterone in prostate cancer. Ketoconazole can also inhibit the enzymes 17-alpha-hydroxylase and 17,20-lyase, which are necessary for the synthesis of steroids in the adrenal cortex, including testosterone.[7]

Ketoconazole inhibits the activity of the enzyme 21-hydroxylase. This enzyme is essential for synthesizing mineralocorticoids and glucocorticoids, such as cortisol, in the adrenal cortex.[8] By inhibiting enzymes involved in cortisol synthesis, ketoconazole can be a treatment option for Cushing syndrome.[9]

Administration

Ketoconazole is available in tablet form and as a topical agent in creams, foams, and shampoos.[10] It is also available in mixture products. The oral form of ketoconazole is used for systemic administration and must be taken at least two hours before any antacids. [11] The high pH of the gastric contents would decrease absorption, so appropriate timing of administration is paramount to its absorption and subsequent efficacy. Adult and pediatric patients with achlorhydria should be given ketoconazole tablets with an acidic beverage to decrease pH and allow for optimal absorption.

Topical ketoconazole is only for external use. It should not be ingested or used intravaginally. The eyes and mucous membranes should also be avoided. Patients should apply the cream and gel only to the affected area and the areas immediately surrounding it. The foam should be applied directly to the infected area to avoid melting in the hands. Handwashing is necessary after the application of the cream and gel to prevent any adverse reactions from the medication. The shampoo application should be slathered onto the scalp and rinsed thoroughly.

Adverse Effects

Systemic ketoconazole administration most commonly causes gastrointestinal side effects.[12] These include nausea, vomiting, constipation, abdominal pain, dry mouth, flatulence, and tongue discoloration. It can also cause adrenal insufficiency due to its role in the inhibition of enzymes in the steroid synthesis pathway. Decreases in cortisol synthesis can lead to orthostatic hypotension.[13] In high doses, it can also cause gynecomastia in males.[14] Ketoconazole can cause severe liver injury and jaundice.[15]

Hypersensitivity reactions have also been reported, such as anaphylaxis and urticaria. High-dose ketoconazole has been shown to cause an increase in long bone fragility and lead to fracture. Other side effects include alcohol intolerance, decreased platelet count, epistaxis, fatigue, hot flash, hyperlipidemia, insomnia, myalgia, nervousness, paresthesia, and peripheral edema. Topical ketoconazole can cause dermatological reactions, including pruritis, stinging, and dryness at the application site. There are also reports of dry hair, dry scalp, and oily hair when using ketoconazole-containing shampoo. Less common adverse effects include abnormal hair texture, alopecia, angioedema, contact dermatitis, eye irritation, headache, hypersensitivity reaction, impetigo, and pyogenic granuloma. [16]

Contraindications

Ketoconazole is contraindicated in patients with acute or chronic liver disease due to its association with hepatotoxicity, which can be fatal. It is contraindicated in adrenal insufficiency because high doses of ketoconazole inhibit adrenocortical function.[17] Ketoconazole should not be given to patients with a known hypersensitivity reaction to ketoconazole.[15] Ketoconazole should never be co-administered with HMG-CoA reductase inhibitors because it can increase the risk of myopathy.[18]

Ketoconazole is contraindicated in patients taking benzodiazepines because it can increase plasma concentrations and lead to sedation. Ketoconazole should never be administered to patients on antiarrhythmic drugs, cisapride, pimozide, quinidine, and ranolazine because it can cause QT prolongation and torsade de pointes.[19] In patients with increased bone fragility, such as post-menopausal women and the elderly, ketoconazole should be used with caution to avoid the risk of fracture. The CYP3A4 liver enzyme metabolizes ketoconazole, and use requires caution in patients taking drugs that inhibit CYP3A4 or are metabolized by CYP3A4.[19] Ketoconazole can also be present in breast milk, so breastfeeding is not recommended when using the drug.[20]

Monitoring

Due to its hepatoxic effects, patients taking oral ketoconazole should have their hepatic function monitored, which is through hepatic function tests such as aspartate transaminase (AST), alanine transaminase (ALT), alkaline phosphatase (ALP), bilirubin, albumin, and prothrombin time (PT).

Hepatic function tests should take place at baseline, frequently during ketoconazole therapy, and after therapy has ceased. Period calcium and phosphorous levels are recommended for patients on long-term therapy with ketoconazole. The adrenal function also requires monitoring during treatment with ketoconazole. This monitoring is possible by measuring blood levels of sodium, potassium, cortisol, and adrenocorticotropic hormone (ACTH). [21]

Toxicity

The Food and Drug Administration warns that oral dosing of ketoconazole can lead to hepatotoxicity and adrenal insufficiency and that ketoconazole-associated hepatotoxicity is common. There are many off-label uses for ketoconazole. Therefore, careful selection of ketoconazole as a treatment is necessary due to serious hepatoxic side effects.[21]

Enhancing Healthcare Team Outcomes

Managing the administration and usage of ketoconazole requires an interprofessional team of healthcare professionals, including nurses, laboratory technologists, pharmacists, and several physicians in different specialties. Since the usage of ketoconazole can result in adverse effects such as hepatotoxicity and adrenal insufficiency, it is important to monitor liver and adrenal function in patients considered for ketoconazole treatment. This monitoring requires that each member of the healthcare team monitor patient for signs of acute liver failure not only with laboratory evidence but also clinically by recognizing the signs of liver dysfunction. In addition, since there are off-label and over-the-counter uses of ketoconazole, it is important to educate patients about the adverse effects of this drug and the proper use of the medication. Therefore, the interprofessional model for patient care when using ketoconazole therapy is crucial to driving optimal patient outcomes while reducing the potential for adverse effects. [Level 5]

References

1.: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. National Institute of Diabetes and Digestive and Kidney Diseases; Bethesda (MD): May 18, 2017. Antifungal Agents. [PubMed: 31643715]
2.: Borgers M, Degreef H, Cauwenbergh G. Fungal infections of the skin: infection process and antimycotic therapy. Curr Drug Targets. 2005 Dec;6(8):849-62. [PubMed: 16375669]
3.: Agut J, Palacín C, Salgado J, Casas E, Sacristán A, Ortiz JA. Direct membrane-damaging effect of sertaconazole on Candida albicans as a mechanism of its fungicidal activity. Arzneimittelforschung. 1992 May;42(5A):721-4. [PubMed: 1627191]
4.: Patel V, Liaw B, Oh W. The role of ketoconazole in current prostate cancer care. Nat Rev Urol. 2018 Oct;15(10):643-651. [PubMed: 30154429]
5.: Van Tyle JH. Ketoconazole. Mechanism of action, spectrum of activity, pharmacokinetics, drug interactions, adverse reactions and therapeutic use. Pharmacotherapy. 1984 Nov-Dec;4(6):343-73. [PubMed: 6151171]
6.: Hu Z, He B, Ma L, Sun Y, Niu Y, Zeng B. Recent Advances in Ergosterol Biosynthesis and Regulation Mechanisms in Saccharomyces cerevisiae. Indian J Microbiol. 2017 Sep;57(3):270-277. [PMC free article: PMC5574775] [PubMed: 28904410]
7.: Bhasin S, Sikka S, Fielder T, Sod-Moriah U, Levine HB, Swerdloff RS, Rajfer J. Hormonal effects of ketoconazole in vivo in the male rat: mechanism of action. Endocrinology. 1986 Mar;118(3):1229-32. [PubMed: 3081326]
8.: Engelhardt D, Weber MM, Miksch T, Abedinpour F, Jaspers C. The influence of ketoconazole on human adrenal steroidogenesis: incubation studies with tissue slices. Clin Endocrinol (Oxf). 1991 Aug;35(2):163-8. [PubMed: 1934533]
9.: Loli P, Berselli ME, Tagliaferri M. Use of ketoconazole in the treatment of Cushing’s syndrome. J Clin Endocrinol Metab. 1986 Dec;63(6):1365-71. [PubMed: 3023421]
10.: Piérard-Franchimont C, De Doncker P, Cauwenbergh G, Piérard GE. Ketoconazole shampoo: effect of long-term use in androgenic alopecia. Dermatology. 1998;196(4):474-7. [PubMed: 9669136]
11.: Khozeimeh F, Shahtalebi MA, Noori M, Savabi O. Comparative evaluation of ketoconazole tablet and topical ketoconazole 2% in orabase in treatment of Candida-infected denture stomatitis. J Contemp Dent Pract. 2010 Mar 01;11(2):017-24. [PubMed: 20228983]
12.: Sohn CA. Evaluation of ketoconazole. Clin Pharm. 1982 May-Jun;1(3):217-24. [PubMed: 6309466]
13.: Gupta AK, Daigle D, Foley KA. Drug safety assessment of oral formulations of ketoconazole. Expert Opin Drug Saf. 2015 Feb;14(2):325-34. [PubMed: 25409549]
14.: DeFelice R, Johnson DG, Galgiani JN. Gynecomastia with ketoconazole. Antimicrob Agents Chemother. 1981 Jun;19(6):1073-4. [PMC free article: PMC181611] [PubMed: 6267997]
15.: Gupta AK, Lyons DC. The Rise and Fall of Oral Ketoconazole. J Cutan Med Surg. 2015 Jul-Aug;19(4):352-7. [PubMed: 25775613]
16.: Choi FD, Juhasz MLW, Atanaskova Mesinkovska N. Topical ketoconazole: a systematic review of current dermatological applications and future developments. J Dermatolog Treat. 2019 Dec;30(8):760-771. [PubMed: 30668185]
17.: Daneshmend TK, Warnock DW. Clinical pharmacokinetics of ketoconazole. Clin Pharmacokinet. 1988 Jan;14(1):13-34. [PubMed: 3280211]
18.: Kempen HJ, van Son K, Cohen LH, Griffioen M, Verboom H, Havekes L. Effect of ketoconazole on cholesterol synthesis and on HMG-CoA reductase and LDL-receptor activities in Hep G2 cells. Biochem Pharmacol. 1987 Apr 15;36(8):1245-9. [PubMed: 3036162]
19.: Lee HC, Tl Huang K, Shen WK. Use of antiarrhythmic drugs in elderly patients. J Geriatr Cardiol. 2011 Sep;8(3):184-94. [PMC free article: PMC3390066] [PubMed: 22783304]
20.: McGregor JA, Pont A. Contraindication of ketoconazole in pregnancy. Am J Obstet Gynecol. 1984 Nov 15;150(6):793-4. [PubMed: 6093540]
21.: Yan JY, Nie XL, Tao QM, Zhan SY, Zhang YD. Ketoconazole associated hepatotoxicity: a systematic review and meta- analysis. Biomed Environ Sci. 2013 Jul;26(7):605-10. [PubMed: 23895707]

Ketoconazole shampoo (Dandrazol, Nizoral) | Medicine

About ketoconazole shampoo

Type of medicine	An antifungal medicine
Used for	Severe forms of dandruff; pityriasis versicolor
Also called	Dandrazol®; Nizoral®
Available as	Shampoo

Ketoconazole shampoo is helpful for persistent or more severe forms of dandruff. It contains an antifungal agent which kills the yeast-like germs (a type of fungus) which causes the flaking of the scalp.

Ketoconazole shampoo is also prescribed for a skin condition called pityriasis versicolor. Pityriasis versicolor is a skin rash which is also caused by a yeast-like germ. Although small numbers of this germ commonly live on the skin and do no harm, some people are prone to it multiplying on their skin more than usual, which leads to small pale or brown patches of skin developing. In some people, hot, sunny or humid weather seems to trigger the germ to multiply on the skin.

Ketoconazole shampoo is available on prescription, and you can also buy some brands without a prescription at pharmacies and other retail outlets. It can be used by adults and children over 12 years of age.

Before using ketoconazole shampoo

To make sure this is the right treatment for you, before you start using ketoconazole shampoo it is important that you speak with a doctor or pharmacist if:

You have ever had an allergic reaction to a medicine.
You are pregnant or breastfeeding. This is because, while you are expecting or feeding a baby, you should only use medicines on the recommendation of a doctor.
You are taking any other medicines or using any other medicated skin products. This includes any medicines you are taking which are available to buy without a prescription, as well as as herbal and complementary medicines.

How to use ketoconazole shampoo

Before you use the shampoo, read the manufacturer’s printed information leaflet from the pack. It will give you more information about ketoconazole shampoo and will provide you with a full list of the side-effects which you could experience from using it.
For dandruff, use the shampoo twice weekly for 2-4 weeks. Wet your hair well before you apply the shampoo. Massage the lather over your scalp and then leave it for about 3-5 minutes before you rinse it off. To help prevent the dandruff from returning, you can continue to use the shampoo once every 1-2 weeks.
For pityriasis versicolor, apply the shampoo to the skin patches once each day, for up to five days. Leave it on the skin for 3-5 minutes and then wash it off. For people who develop the rash after being out in the sun, the shampoo can subsequently be used as a way of preventing the rash from developing when planning to sunbathe. When used like this, it can be used for up to three days, in the same way as before.

Getting the most from your treatment

Try not to get any of the shampoo into your eyes but if this happens, rinse it out with water as soon as possible.
If you are using the shampoo for dandruff and your symptoms are showing no signs of getting better after four weeks of using the shampoo, please speak with a doctor or pharmacist for further advice.

Can ketoconazole shampoo cause problems?

Along with their useful effects, most medicines can cause unwanted side-effects although not everyone experiences them. The table below contains some of the ones associated with ketoconazole shampoo. You will find a full list in the manufacturer’s information leaflet supplied with your medicine. The unwanted effects often improve as your body adjusts to the new medicine, but speak with your doctor or pharmacist if any of the following continue or become troublesome.

Ketoconazole shampoo side-effects (these affect less than 1 in 100 people)	What can I do if I experience this?
Mild irritation, dryness, changes to how your hair feels	If it continues or becomes troublesome, speak with a doctor or pharmacist for further advice

If you experience any other symptoms which you think may be due to the shampoo, speak with your doctor or pharmacist for further advice.

How to store ketoconazole shampoo

Keep all medicines out of the reach and sight of children.
Store in a cool, dry place, away from direct heat and light.

Important information about all medicines

This preparation is for external use only. If you suspect that someone might have swallowed some of it by accident, go to the accident and emergency department of your local hospital. Take the container with you, even if it is empty.

The shampoo is for you. Do not give it to other people even if their condition appears to be the same as yours.

If you are having an operation or dental treatment, please remember to tell the person carrying out the treatment which medicines you are taking/using.

Do not keep out-of-date or unwanted medicines. Take them to your local pharmacy which will dispose of them for you.

If you have any questions about the treatment, please speak with your pharmacist.

90,000 shampoo, cream, pills and more – Animal Expert Site – HowMeow

Ketoconazole is an antifungal agent It is sometimes prescribed in veterinary medicine, although it is also used in humans. A relatively common drug, ketoconazole can be purchased without a prescription. This means that many pet owners may want to use this product on their pets if they believe the dog may have a fungal infection.Although ketoconazole comes in various forms such as shampoo, cream, or oral preparations such as tablets, the method of administration depends on the veterinarian …

HowMeow brings you the different types of ketoconazole for dogs and helps explain its uses and dosages. An important factor in treating dogs with ketoconazole is its potential side effects, another reason why it is very important to follow the veterinarian’s recommendations …

Different types of ketoconazole.

Ketoconazole is an antifungal agent , also known as an antifungal drug. Because it is found in several different medicines, the dose of ketoconazole in any given formula will be different. Often sold under the brand name Nizoral . Although your veterinarian will prescribe this medication under various circumstances, it can also be bought without a prescription. While its availability may make it seem like it can be used freely, ketoconazole has various interactions and can be dangerous if misused….

The type of ketoconazole that your veterinarian prescribes depends on the application. However, in humans, ketoconazole tablets or pills are currently very rare but may be more common in veterinary medicine. Oral ketoconazole has the advantage of being faster than Topical ketoconazole . However, topical products help control the site of certain infections. The most common types of ketoconazole for dogs include:

Ketoconazole Shampoo Since most dogs are covered with fur / coat, washing with medicated shampoo can help solve the fungal problem.It can be used on the whole body or only in certain areas, but the instructions must be carefully followed independently.
Ketoconazole Tablets – This antifungal drug can also be found in pill or tablet form. It is a commonly used drug that passes into the dog’s bloodstream, which means that the dose must be carefully monitored.
Ketoconazole Cream Topical use of ketoconazole is common and preferred in human use.Due to the dog’s coat and its tendency to lick, topical cream is not always suitable, but depends on the individual dog …
Ketoconazole eye drops Since penetration of ketoconazole can be severe, eye drops are usually not used. Sold with product names such as Ketostar, it is usually found in a 0.5% solution and is used for more serious eye infections. Other treatments for an eye infection, such as natamycin, may be more appropriate in milder cases …

Topical medications, such as ketoconazole shampoo, are not necessarily treatments for fungal infections.Instead, they are used to treat the symptoms of infection. This reduces the spread of the fungus, but usually requires more systemic antifungal treatment to address the problem more directly. Ketoconazole shampoo may also contain chlorhexidine , which is a bactericidal disinfectant.

Regardless of the type or form, ketoconazole is the same active ingredient in these different products. treatment period In these cases, it is usually extended, usually more than two months.For topical application, ketoconazole cream also works like a shampoo. Mainly reduces the risk of infection and is used in combination with systemic treatment.

Why is ketoconazole used for dogs?

Since ketoconazole has antifungal effect, it is able to kill some fungi such as Microsporum Dogs . It is a type of fungus that causes various fungal infections of the skin (dermatophytosis ) like ringworm.However, it is also used to fight various fungal infections such as Malassezia pachydermatis . This type of yeast infection is associated with otitis media, which means it is commonly involved in ear infections …

This type of disease and infection is usually very contagious , It is therefore important that treatment is started as soon as possible. We will also have to follow the various hygiene measures necessary to prevent their spread. This can include isolating the animal until it is free of the contamination and disinfecting any areas it has previously used.Remember that fungal infections in dogs can be zoonotic, meaning they can be transmitted to humans.

In addition to ear infections and fungal infections, ketoconazole has also been useful in the treatment of hyperadrenocorticism, better known as Cushing’s syndrome …

Ketoconazole dosage for dogs

Ketoconazole tablets should be administered in doses of 5 mg per kg of body weight every 12 hours. Alternatively, it can be administered at a dose of 10 mg per kg of body weight if administered once a day. It is better to offer the medicine with food, as it is better absorbed in this way. Ketoconazole tablets or tablets come in a variety of sizes, usually 100 mg, 200 mg, or 400 mg. You may need to split them to give the correct dose.

Whatever Dose Still, if ketoconazole is given, it is important that you follow your veterinarian’s instructions carefully. Inadequate use of this or any medication can lead to serious consequences for the animal, such as poisoning or digestive problems …

Ketoconazole side effects for dogs

Ketoconazole, even at the recommended dose, can cause Adverse reactions .These side effects will vary based on the amount of dose, the individual dog’s overall health, and other factors. These include:

anorexia
vomiting
diarrhea
Liver problems
Hormonal imbalance
Neurological disorders
Fetal malformation

Because the medicine is strong, it may be harmful when processed. This is because it is toxic to the liver, leading to liver problems such as jaundice.Hormonal imbalances can also be a side effect of ketoconazole. The drug affects the metabolism of certain hormones and their compounds that affect testosterone levels. In the queue, testosterone imbalance can affect their reproductive ability and even affect their behavior.

In addition to the above side effects, ketoconazole is teratogenic and embryotoxic at high doses. This means that it can cause malformations in the fetus. For this reason, it should never be administered to pregnant dogs.Also not recommended for puppies under 2 months or any animal with liver disease. Ketoconazole has various contraindications for other medications, so it is very important that your veterinarian is informed if you are taking any other medications …

Other side effects of ketoconazole are less common in dogs. These include neurological problems such as apathy, lack of coordination, or tremors. In case of overdose, in addition to symptoms similar to those mentioned above, itching and lack of hair may also occur.Take your dog to the vet immediately if you suspect he has overdosed on ketoconazole.

This article is for informational purposes only. HowMeow has no authority to prescribe veterinary treatment or diagnose. We invite you to take your pet to the vet if it has any problems or pain.

90,000 16 reviews, instructions for use

Ketoconazole is a synthetic antifungal drug derived from imidazoldioxolan.It is used mainly in the treatment of acute and chronic vulvovaginal candidiasis, as well as for the prevention of fungal vaginal infections with reduced resistance of the body due to a violation of the vaginal microflora during antibiotic treatment. Has fungicidal (destructive) and fungistatic (slowing growth and development) action against Epidermophyton floccosum, Microsporum spp., Trichophyton spp., Candida spp., Cryptococcus spp., Pityrosporum spp. , Torulopsis, eumycetes and dimorphic fungi.The spectrum of action of ketoconazole is not limited to fungi, but also includes bacteria, including staphylococci and streptococci. The mechanism of action of the drug is to suppress the biosynthesis of the main structural element of the fungal membrane – ergosterol, as well as to change the lipid composition of the cell wall of the fungus. The degree of absorption into the systemic circulation with the intravaginal route of administration is insignificant.

Ketoconazole is available in the form of vaginal suppositories. The introduction is carried out deep into the vagina, 1 suppository 1 time per day.The duration of the drug course is on average 3-5 days, depending on the nature of the disease. In chronic vulvovaginal candidiasis, 1 suppository is used 1 time per day for 10 days. A direct contraindication to the use of ketoconazole is only the first trimester of pregnancy: in the second and third trimesters, the drug can be used, albeit with caution. The same goes for lactation and childhood from 12 to 18 years old. As for side reactions, they are quite rare and affect more of the woman’s sexual partner, manifesting in that allergic reactions in the form of hyperemia of the penis.It is important that the sexual partner also undergoes a course of treatment, otherwise re-infection may occur. Before starting pharmacotherapy, the doctor should warn the woman that the use of suppositories can reduce the effectiveness of mechanical contraception (for example, latex condoms and vaginal diaphragms).

Ketoconazole in the form of vaginal suppositories can be taken without fear of overdose, since the degree of absorption of the active substance into the systemic circulation is extremely low.For the same reason, undesirable drug interactions can not be expected from the drug in case of joint pharmacotherapy.

As already mentioned, ketoconazole is the first choice drug for vulvovaginal candidiasis or, as it is more commonly called, vaginal candidiasis. This is one of the most common “female” diseases: about 70% of women are somehow familiar with it firsthand. Adverse factors contributing to the development of vaginal candidiasis are hormonal “swing”, impaired immunity, changes in the vaginal microflora due to inappropriate use of antibiotics, etc.e. The main culprit of the disease is the naturally occurring yeast-like fungus Candida. It is very important to suppress vaginal candidiasis, as they say, “in the embryo”, because otherwise there is a high probability of its transition to a chronic form. Ketoconazole is one of those drugs that can successfully cope with this task. This fact has been repeatedly confirmed in controlled clinical trials. The halo of confidence in the drug is also created by the course form of its use, which falls within the framework of the traditions of domestic medicine (the use of a single dose of any drug traditionally causes distrust both on the part of clinicians and on the part of their patients).Here it is appropriate to give an example with sertaconazole, a single dose of which many doctors prefer a 5-day course of ketoconazole therapy. As for the specific figures, if we summarize the published data, the clinical efficacy of ketoconazole for vaginal candidiasis is about 90% against the background of a consistently high adherence of patients to the course of treatment.

Clobetasol propionate / Ketoconazole – instructions for use, dosage, composition, analogs, side effects / Pillintrip

Clobetasol propionate (Clobetasol propionate propionate scalp application) application should be applied to the affected areas of the scalp twice a day, once in the morning and once at night.Application not associated with occlusive dressings may be used.

Geriatric use: in studies in which geriatric patients (65 years of age and older, see, precautions ) were treated with clobetasol propionate (clobetasol propionate for use), safety did not differ from that in younger patients, therefore dose adjustment is not recommended.

How Delivered

Clobetasol Propionate (Clobetasol Propionate Scalp Application, 0. 05% comes in squeeze plastic bottles, 25ml (NDC 0173-0432-00) and 50ml (NDC 0173-0432-01). Store 4 ° to 25 ° C. Do not use near open flame.

Glaxo Wellcome Inc. Research Triangle Park, NC 27709. August 2000. FDA rev Date: 4/2/2003

Usual Adult Dose for Blastomycosis

Initial Dose: 200 mg orally once a day

If the clinical response is insufficient within the expected time: the dose can be increased to 400 mg orally once a day …

Duration of therapy: 6 months (typical duration for systemic infection)

Comments :

-Ketoconazole is only recommended if no other effective antifungal therapy is available or tolerated and the benefits outweigh the risks.

– Ketoconazole should not be used for fungal meningitis (poorly penetrates the cerebrospinal fluid).

– Infectious Diseases Society of America (IDSA) guidelines recommend amphotericin B and itraconazole as preferred treatments for blastomycosis and histoplasmosis.

Use: for the treatment of the following systemic fungal infections in patients who have failed or cannot tolerate other treatments: blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, paracoccidioidomycosis

Usual adult oral dose for chromomycosis

single dose

day

If the clinical response is insufficient within the expected time: the dose can be increased to 400 mg orally once a day.

Duration of therapy: 6 months (typical duration for systemic infection)

Comments :

-Ketoconazole is only recommended if no other effective antifungal therapy is available or tolerated and the benefits outweigh the risks.

– Ketoconazole should not be used for fungal meningitis (poorly penetrates the cerebrospinal fluid).

– Infectious Diseases Society of America (IDSA) guidelines recommend amphotericin B and itraconazole as preferred treatments for blastomycosis and histoplasmosis.

Uses: for the treatment of the following systemic fungal infections in patients who have failed or cannot tolerate other treatments: blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, paracoccidioidomycosis

Usual adult dose for coccidioidomycosis 2002 Initial dose

9000 day

If the clinical response is insufficient within the expected time: the dose can be increased to 400 mg orally once a day.

Duration of therapy: 6 months (typical duration for systemic infection)

Comments :

-Ketoconazole is only recommended if no other effective antifungal therapy is available or tolerated and the benefits outweigh the risks.

– Ketoconazole should not be used for fungal meningitis (poorly penetrates the cerebrospinal fluid).

– Infectious Diseases Society of America (IDSA) guidelines recommend amphotericin B and itraconazole as preferred treatments for blastomycosis and histoplasmosis.

If the clinical response is insufficient within the expected time: the dose can be increased to 400 mg orally once a day.

Duration of therapy: 6 months (typical duration for systemic infection)

Comments :

-Ketoconazole is only recommended if no other effective antifungal therapy is available or tolerated and the benefits outweigh the risks.

– Ketoconazole should not be used for fungal meningitis (poorly penetrates the cerebrospinal fluid).

– Infectious Diseases Society of America (IDSA) guidelines recommend amphotericin B and itraconazole as preferred treatments for blastomycosis and histoplasmosis.

If the clinical response is insufficient within the expected time: the dose can be increased to 400 mg orally once a day.

Duration of therapy: 6 months (typical duration for systemic infection)

Comments :

-Ketoconazole is only recommended if no other effective antifungal therapy is available or tolerated and the benefits outweigh the risks.

– Ketoconazole should not be used for fungal meningitis (poorly penetrates the cerebrospinal fluid).

– Infectious Diseases Society of America (IDSA) guidelines recommend amphotericin B and itraconazole as preferred treatments for blastomycosis and histoplasmosis.

Usual pediatric dose for blastomycosis

and older: 30002 2.3 up to 6.6 mg / kg orally once a day

Duration of therapy: 6 months (usual duration for systemic infection)

Comments :

– Ketoconazole should only be used if the benefits outweigh the risks.

– Ketoconazole should not be used for fungal meningitis (poorly penetrates the cerebrospinal fluid).

– IDSA guidelines recommend amphotericin B and itraconazole as preferred treatments for blastomycosis and histoplasmosis.

Usual Pediatric Dose for Chromomycosis

and over

3. 3 years up to 6.6 mg / kg orally once a day

Duration of therapy: 6 months (usual duration for systemic infection)

Comments :

– Ketoconazole should only be used if the benefits outweigh the risks.

– Ketoconazole should not be used for fungal meningitis (poorly penetrates the cerebrospinal fluid).

– IDSA guidelines recommend amphotericin B and itraconazole as preferred treatments for blastomycosis and histoplasmosis.

Usual Pediatric Dose for Coccidioidomycosis 2, 31 and

9000 over up to 6.6 mg / kg orally once a day

Duration of therapy: 6 months (usual duration for systemic infection)

Comments :

– Ketoconazole should only be used if the benefits outweigh the risks.

– Ketoconazole should not be used for fungal meningitis (poorly penetrates the cerebrospinal fluid).

– IDSA guidelines recommend amphotericin B and itraconazole as preferred treatments for blastomycosis and histoplasmosis.

Usual pediatric dose for histoplasmosis 2

up to 6.6 mg / kg orally once a day

Duration of therapy: 6 months (usual duration for systemic infection)

Comments :

– Ketoconazole should only be used if the benefits outweigh the risks.

– Ketoconazole should not be used for fungal meningitis (poorly penetrates the cerebrospinal fluid).

– IDSA guidelines recommend amphotericin B and itraconazole as preferred treatments for blastomycosis and histoplasmosis.

Usual Pediatric Dose: for paracoccidioidomycosis and older

,39015 and older

,32 9015 up to 6. 6 mg / kg orally once a day

Duration of therapy: 6 months (usual duration for systemic infection)

Comments :

– Ketoconazole should only be used if the benefits outweigh the risks.

– Ketoconazole should not be used for fungal meningitis (poorly penetrates the cerebrospinal fluid).

– IDSA guidelines recommend amphotericin B and itraconazole as preferred treatments for blastomycosis and histoplasmosis.

Renal dose adjustment

9050 No data available

901 chronic liver disease: contraindicated

If ALT rises above the upper normal limit (elbow joint) or 30% above baseline or if symptoms of liver injury occur: Discontinue therapy.

Dose adjustment

– When used with drugs that reduce gastric acid: Caution is advised. Antifungal activity should be monitored and the dose of ketoconazole increased as needed.

-When used with potent cyp450 3A4 inducers: Antifungal activity should be monitored and the dose of ketoconazole increased as needed.

-When used with strong inhibitors of CYP450 3A4: Caution should be exercised.Patients should be closely monitored for signs / symptoms of increased or prolonged exposure to ketoconazole and reduce the dose of ketoconazole as needed, and plasma levels of ketoconazole should be measured if necessary.

Precautions

BOXED WARNINGS :

– LIMITED USE: The use of ketoconazole is only recommended if no other effective antifungal therapy is available or tolerated and the benefits outweigh the risks.

– HEPATOTOXICITY: Severe hepatotoxicity (including cases leading to death or requiring liver transplantation) reported with oral ketoconazole. Some patients had no obvious risk factors for liver disease. Patients using ketoconazole should be informed of the risk and closely monitored.

– QT prolongation: simultaneous administration of ketoconazole with dofetilide, quinidine, pimozide, cisapride, methadone, disopyramide, dronedarone or ranolazine is contraindicated.Ketoconazole can increase plasma levels of these drugs and prolong QT intervals, sometimes resulting in life-threatening ventricular dysrhythmias (eg, torsades de pointes).

Safety and efficacy have not been proven in patients under 2 years of age.

Refer to WARNINGS section for dose precautions.

Dialysis

Data not available

Other comments

Management-Consulting :

– Take your food with you.

– Administer ketoconazole with an acidic drink (for example, cola without a diet) if stomach acid is low (for example, in patients with achlorhydria due to certain diseases, in patients using acid secretion suppressors or acid-neutralizing therapy), inject acid neutralizing agents at least 1 hour before or 2 hours after ketoconazole.

Memory requirement :

– Protect against moisture.

general :

-Before starting therapy with ketoconazole, there must be laboratory as well as clinical documentation of the infection.

– The therapy should be continued until the active fungal infection has subsided.

– Ketoconazole requires acid for dissolution and absorption, absorption is impaired when gastric acid production is reduced.

– Ketoconazole has the potential to interact with many drugs, such interactions can be serious and / or life-threatening, the manufacturer’s product information should be consulted.

Observation :

– Endocrine: adrenal function in patients with adrenal insufficiency, with borderline adrenal function or with prolonged stress

– General information: antifungal activity and / or plasma levels of ketoconazole with concomitant administration of certain drugs

Hematologic: laboratory tests such as prothrombin time, INR (at the beginning of the study)

– Hepatic: laboratory tests such as serum-GGT, alkaline phosphatase, ALT, AST, total bilirubin (at the beginning of the study), tests for viral hepatitides ( at the start of the study), serum-ALT (weekly during therapy), a complete set of liver tests (if ALT is increased to above the elbow or 30% above baseline or if symptoms of liver injury develop), for recurrent liver injury (often if the drug restarts after interruption due to increased ALT or symptoms of liver injury)

Counseling Patients :

– Report signs / symptoms suggestive of liver dysfunction (including unusual fatigue, anorexia, nausea and / or vomiting, abdominal pain, jaundice, dark urine, pale stools).

– Do not drink alcohol during therapy.

NDDA – Drug Safety Information

Safety Information LS

19.05.2014

Ketoconazole Precautions

Ketoconazole tablets should be used only when therapy with other antifungal agents is ineffective or poorly tolerated by the patient and the potential benefit of oral administration of ketoconazole outweighs the potential risk.

Hepatotoxicity . Serious hepatotoxicity has been reported with oral use of ketoconazole, including fatal cases or requiring liver transplantation. Patients taking ketoconazole tablets should be advised of the possible risk of liver dysfunction.

Prolongation of the QT interval and interactions leading to prolongation of the QT interval. The combined use of the following drugs with ketoconazole is contraindicated: dofetilide, quinidine, pimozide, cisapride, methadone, disopyramide, dronedarone, ranolazine. Ketoconazole can lead to an increased plasma concentration of these drugs and a prolongation of the QT interval, which sometimes leads to life-threatening ventricular arrhythmia – torsade de pointes.

After an analysis of the safety profile of ketoconazole-containing medicinal products (oral forms), Committee on Medicines for Human Use of the European Medical Agency ( CHMP EMA ) recommended to suspend the registration certificates of the above medicinal products on the territory of the European Union.

Ketoconazole is indicated only for the treatment of life-threatening systemic (deep) mycoses: blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, paracoccidioidomycosis, when the benefit exceeds the risk, when other alternative therapy is not available or is not tolerated (poorly tolerated).
Oral ketoconazole is not indicated for the treatment of any form of candidiasis and superficial fungal infections of the skin and nails. These indications are excluded from the “Indications” section of the instructions for medical use of oral forms of ketoconazole.
Ketoconazole is contraindicated in acute and chronic liver diseases.
Mandatory monitoring of liver function:

Before starting ketoconazole therapy, it is necessary to assess the level of ALT, AST, total bilirubin, alkaline phosphatase, prothrombin time, INR (international non-proprietary ratio).
During therapy, ALT should be monitored weekly throughout the course of treatment.
If there is an increase in ALT above the upper limit of normal, or a 30% increase in baseline, or the patient develops symptoms of liver dysfunction, the use of ketoconazole should be discontinued and a complete liver examination performed. Tests must be repeated until all indicators are normalized.

Information source
fda.gov

Ema. europa. eu

FDA Safety Statement: Anticonvulsant drug can cause severe skin damage.

The FDA warns that the anticonvulsant drug Onfi (ONFI) -clobazam, can cause a rare but serious complication in the form of specific skin reactions that can lead to permanent damage to health and death. The FDA has approved changes to the ONFI instructions for use. Patients should seek immediate medical attention if they develop rashes, blisters, peeling skin, mouth ulcers, or hives. Healthcare providers should discontinue ONFI and consider alternative therapy at the first sign of rash if no other etiologic factor is evident.

These rare but serious skin reactions, called Stevens Johnson Syndrome (SJS) and Toxic Epidermal Necrolysis (TEN), can occur at any time while you are taking ONFI. All cases of SJS and TEN reported to the FDA resulted in hospitalization, in one case the consequences resulted in blindness and in one death.

ONFI is a benzodiazepine drug used in combination with other medicines to treat seizures associated with severe epilepsy (Lennox-Gastaut syndrome).In general, serious skin reactions have not been associated with other benzodiazepines.

Abrupt discontinuation of ONFI can cause serious consequences such as persistent convulsions, hallucinations (auditory or visual), muscle twitching, nervousness, abdominal cramps, muscle spasms.

The drug is approved as an adjunctive treatment (which is as an adjunct to the main anticonvulsants) for patients aged 2 years and older with Lennox-Gastaut syndrome, a severe form of epilepsy.

This drug has been on the pharmaceutical world market for 40 years, exists under various brand names for the treatment of anxiety and seizures.

www.fda.gov

Taking incretin mimetics does not increase the risk of cancer and inflammatory diseases of the pancreas

According to a report by the FDA and EMA, incretinomimetics do not increase the risk of cancer and inflammatory diseases of the pancreas. US and European regulators have conducted a joint study to investigate this issue, the results of which are published in the New England Journal of Medicine. Incretinomimetics are agonists of the glucagon-like pethid-1 receptor (eg, Victoza, Januvia). They are prescribed for patients with diabetes mellitus, help to lower blood glucose levels by stimulating the production of insulin after meals and slowing down absorption in the gastrointestinal tract.

This study was initiated after the publication of information on the increased incidence of pancreatitis and pancreatic cancer among patients taking incretinomimetics.The experts reviewed the results of all available studies of drugs in this group. FDA experts analyzed data from 200 studies, in which a total of 28 thousand people took part, EMA experts studied the results of 25 studies involving 16 thousand patients. The results obtained indicate that there is no relationship between the intake of inkertinomimetics and the risk of developing pancreatic diseases.

Also, regulators ordered additional studies of the safety of these drugs.Thus, a toxicological study was initiated, during which several thousand laboratory animals received incretinomimetics in very high doses for a long period of time. However, neither healthy rodents, nor animals with diabetes mellitus showed an oncogenic effect when taking high doses of this group of drugs.

Currently, there is a warning about an increased risk of pancreatic disease in the instructions for medicines.Regulators note that they must remain in force, while new restrictions and contraindications will not appear in them.

Information source

fda.gov

clinicl – pharmacy . ru

New information from the safety section of the drug Zelboraf ( Vemurafenib) – risk of liver damage

Roche has informed healthcare professionals about the risk of liver damage associated with the use of the drug Zelboraf ( v emurafenib).

Summary

There have been reports of liver damage while taking the drug Zelboraf, including cases of severe liver damage.
It is necessary to monitor the level of transaminases, alkaline phosphatase and bilirubin before starting therapy with Zelboraf, monthly throughout the course of treatment or when clinical symptoms occur.
According to the current instructions for the medical use of the drug Zelboraf, if pathological changes in laboratory parameters characterizing liver function are detected, it is necessary to reduce the dose, temporarily suspend or completely stop taking the drug.

The information obtained further confirms the possibility of using the term “liver damage” when describing the risk of hepatotoxicity of the drug Zelboraf (the current instructions for medical use indicate the term “pathological changes in laboratory parameters characterizing liver function”). Health care providers should monitor the level of transaminases, alkaline phosphatase and bilirubin before starting Zelboraf therapy, monthly throughout the course of treatment, or as clinically indicated. If liver damage is detected, it is necessary to reduce the dose, temporarily suspend or completely stop taking the drug, in accordance with the current instructions for the medical use of the drug Zelboraf.

The drug Zelboraf is registered in the Republic of Kazakhstan for the treatment of inoperable or metastatic melanoma, in the cells of which the BRAF mutation was detected.

Source:

1. Important drug warning; risk of liver injury reported with Zelboraf (vemurafenib) Roche January 2014

2. rceth . by

The use of paracetamol during pregnancy increases the risk of developing attention deficit hyperactivity disorder in a child

Danish scientists believe that attention deficit hyperactivity disorder (ADHD) in children may be caused by the mother’s intake of paracetamol during pregnancy.

Recent laboratory studies have shown that paracetamol can affect the levels of various hormones in animals. If these changes occur during pregnancy, then this can adversely affect the development of the central nervous system of the fetus. Scientists conducted a study to test the link between a mother’s intake of paracetamol during pregnancy and the development of attention deficit hyperactivity disorder in her baby.

The authors of the work studied the data of 64 thousand children born from 1996 to 2002, as well as their mothers. The children were recruited into the Danish National Birth Cohort National Newborn Health Study.It turned out that 56% of women took paracetamol during pregnancy. Their children were diagnosed with hyperkinetic disorder (severe ADHD) 37% more often.

Also, scientists note that this group of study participants was 29% more likely to be prescribed drugs for the treatment of attention deficit hyperactivity disorder. Analysis of the data showed that by the age of seven, children whose mothers took paracetamol during pregnancy were 13% more likely to have behavioral changes characteristic of the disease. Moreover, the more often a woman used this drug, the stronger the relationship was. The same pattern was found in women who took paracetamol for more than one trimester of pregnancy. One of the study’s authors, Jorn Olsen, an epidemiologist at the University of Aarhus, believes that the risk of developing ADHD is low, but women should consider it and not take paracetamol without good reason. Scientists also note that the main reasons for using paracetamol – inflammatory or infectious diseases in women during pregnancy can also have a negative effect on the fetus.Therefore, the identified relationship needs additional study and confirmation. The results of the study were published in the journal JAMA Pediatrics.

Source:

clinicl – pharmacy . ru

Information on the safety of use of the medicinal product Temozolomide ( temozolomide) – risk of liver damage

Merck Sharp & Dohme Limited , original drug manufacturer Temodal ®, with the approval of the European Medical Agency, informed healthcare professionals about cases of liver damage, including fatal liver failure with temozolomide and the need to monitor liver function indicators . ..

Temozolomide is a drug for the treatment of malignant gliomas. Indicated for treatment:

adult patients with newly diagnosed glioblastoma multiforme as part of a combination treatment with radiation therapy and subsequent monotherapy;
children aged 3 years and older, adolescents, adult patients with malignant glioma in the form of glioblastoma multiforme or anaplastic astrocytoma, in the presence of a relapse or progression of the disease after standard therapy.

An analysis of serious cases of hepatotoxicity reported during post-marketing safety monitoring around the world was carried out. A total of 44 cases of liver damage, including fatal liver failure, associated with the use of temozolomide were identified. Hepatic impairment developed approximately several weeks after the start of therapy (42-77 days of admission) or after discontinuation of the drug. Cases of non-fatal hepatotoxicity were reported at different times from the start of temozolomide therapy (up to 112 days).

The approved instructions for medical use contain information on the risk of hepatotoxicity during therapy with temozolomide, however, information on the risk of developing fatal hepatocellular liver damage, liver failure, and measures to reduce these risks are not included.

The following information is recommended in the “Warnings and special instructions” section: “

Hepatotoxicity

“There have been reports of cases of liver damage, including fatal liver failure, in patients taking temozolomide.Liver function indices should be assessed:

before starting therapy. If laboratory parameters are abnormal before starting therapy with temozolomide, it is necessary to carefully assess the benefit-risk ratio when prescribing temozolomide, including the possibility of developing liver failure with a fatal outcome;
patients receiving a 42-day course of treatment with temozolomide, it is necessary to monitor liver function indicators in the middle of the course;
all patients receiving temozolomide should be monitored after each course of treatment.
in patients with significant deviations in laboratory test indicators, it is necessary to assess the benefit-risk ratio to decide whether to continue therapy.

Hepatotoxicity may develop several weeks after the last dose of temozolomide. ”

10 drugs are registered in the State Register of the Republic of Kazakhstan under the international non-proprietary name.

Source:

Merck Sharp & Dohme Limited Dear healthcare provider Severe liver toxicity associated with temozolomide (Temodal®) 12 December 2013
Summary of Product Characteristics last updated on the eMC: 22/01/2014 PC Temodal Capsules
rceth.by

Ketoconazole BP EP Raw Material API Manufacturers and Suppliers – Price

Product Name: Ketoconazole API

CAS Number: 65277-42-1

Characteristics: White or off-white powder.

Assay: 99% -101% Ketoconazole

Molecular Formula: C26h38Cl2N4O4

Composition:

Package:

Package: 25Kgs / Fiber Drum

Synonyms: Ketoconazole; ketoderm; fungarest;

Density: 1.38 g / cm3

Melting point: 146 ° C

Stability: Stable at room temperature in closed containers under normal storage and handling conditions.

Transport brand: UN 2811 6.1 / PG 3

KEY Words: Ketoconazole BP EP Raw Material API

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Description Ketoconazole BP EP Raw Material API:

Ketoconazole BP EP. The Raw Material API is a broad spectrum antimicrobial agent used for a long time at high doses, especially in immunocompromised patients. It is a racemate consisting of equimolar amounts of (2R, 4S) – and (2S, 4R) -ketoconazole with chiral centers on the acetal ring.

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Ketoconazole BP EP. API starting material is a synthetic imidazole antifungal drug mainly used to treat fungal infections. Ketoconazole is currently marketed as a tablet for oral use, as well as in various topical preparations such as creams (used to treat tinea, cutaneous candidiasis, including candidiasis and pyrithiasis versicolor) and shampoos (used primarily to treat dandruff-seborrheic scalp dermatitis).

Uses and Applications:

Medical Use

-Antifungal

Ketoconazole BP EP. The API starting material is for fungal infections of the skin and mucous membranes such as athlete’s foot, ringworm, candidiasis (yeast infection or thrush), jock itch and versicolor dash. Topical Ketoconazole BP EP. The API starting material is also used to treat dandruff (seborrheic dermatitis of the scalp) and seborrheic dermatitis elsewhere on the body, possibly acting under these conditions to suppress levels of the fungus Malassezia furfur on the skin.

-Systems Antifungal

Ketoconazole BP EP Raw Material API will help fight many types of fungi that can lead to human diseases such as Candida, Histoplasma, Coccidioides and Blastomyces (although it is inactive against Aspergillus). In the 1970s, Ketoconazole BP EP Raw Material API was the first orally active azole antifungal ingredient. However, it has largely been replaced as a first-line systemic antifungal by other azole antifungals such as itraconazole due to the greater toxicity of ketoconazole, lower absorption and more limited spectrum of activity.

Ketoconazole is used orally in doses ranging from 200 to 400 mg per day in the treatment of superficial and deep fungal infections.

Antiandrogen and antiglucocorticoids

Side effects of ketoconazole are sometimes used in the treatment of non-fungal conditions. While Ketoconazole BP EP. The API starting material blocks the synthesis of sterol-ergosterol in fungi, in humans at high doses (> 800 mg / day), it strongly inhibits the activity of several enzymes needed to convert cholesterol to steroid hormones such as testosterone and cortisol.In particular, ketoconazole has been shown to inhibit the cholesterol side chain cleavage enzyme that converts cholesterol to pregnenolone, which converts pregnenolone to androgens. Based on these antiandrogenic and antiglucocorticoid effects, Ketoconazole BP EP Raw Material API has been used with some success as a second line treatment for certain forms of prostate cancer and to suppress glucocorticoid synthesis in the treatment of Cushing’s syndrome. However, in the treatment of prostate cancer, simultaneous administration of glucocorticoids is necessary to prevent adrenal insufficiency.Ketoconazole BP EP. At lower dosages for the treatment of hirsutism and in combination with analogs of GnRH, previously limited male puberty, the raw material API has been used. In any case, the risk of hepatotoxicity with ketoconazole limits its use in all of these indications, especially in those that are benign, such as hirsutism.

-Hair loss

Ketoconazole is also added to shampoo in combination with an oral 5α-reductase inhibitor. It has been used with a label for the treatment of androgenetic alopecia.Antifungal properties of the drug Ketoconazole BP EP. The API starting material reduces the microflora of the scalp and therefore can reduce follicular inflammation that contributes to baldness.

Limited clinical trials suggest that ketoconazole shampoo, used alone or in combination with other treatments, may be beneficial in reducing hair loss.

– Veterinary Use

Ketoconazole BP EP Raw Material API is also sometimes prescribed by veterinarians for use on pets, often as unopened tablets, which may need to be cut to a smaller size for correct dosage.

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Ketoconazole BP EP. Raw Material API is an antifungal drug that fights infections caused by fungus. But it is not intended to treat fungal infections of the nails or toenails. Ketoconazole BP EP. The Raw Material API is also not used to treat prostate cancer or Cushing’s syndrome.

Ketoconazole BP EP. The API starting material should only be used when you cannot use other antifungal agents.This can be very bad for your liver.

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Ketoconazole is used to treat certain serious fungal infections in the body. Ketoconazole belongs to a class of drugs called azole antifungals. It works by stopping the growth of the fungus.

Ketoconazole should not be used to treat fungal infections of the skin and nails due to the risk of serious side effects and drug interactions.

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Mechanism of action of ketoconazole BP EP. Raw Material API:

Ketoconazole is structurally similar to imidazole and interferes with fungal synthesis of ergosterol, a constituent of cell membranes, as well as some enzymes. It is fungal specific because the mammalian equivalent pathway leading to cholesterol biosynthesis is insensitive to ketoconazole. However, other mammalian cytochrome P450 enzymes may be sensitive to ketoconazole, and inhibition of steroid hormone synthesis is a possible side effect of ketoconazole treatment.

Like all azole antifungal agents, ketoconazole works primarily by inhibiting an enzyme, cytochrome P450 14-alpha demethylase. This enzyme is in the sterol biosynthetic pathway that leads from lanosterol to ergosterol. It was found that fluconazole and itraconazole have a greater affinity for the membrane of fungal cells than ketoconazole, and therefore lower doses of these azoles are required to kill fungi.

———————

Fluconazole and itraconazole belong to a class of drugs called antifungal drugs.A drug class is a group of drugs that work in a similar way. These drugs are often used to treat these conditions. Ketoconazole works to stop fungi and yeast from getting infected.

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Fengchen Group is a leading Ketoconazole BP EP API Powder supplier from China. We specialize in bulk and bulk quantities ensuring that all of our customers have the right Ketoconazole BP EP Powder API Supplier when they need it.When you are going to buy or purchase Ketoconazole BP EP Powder API, please turn to Fengchen Group.

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Certificate of Analysis

-0845 ~

10 °

0.03

8000

Staphylococcus

8000

Staphylococcus

8000 9000 Analysis
Ketoconazole

Product name	Ketoconazole
Test item	Standard	Result
Appearance Ketoconazole	White or Near White Powder	000 945		000 Conforms to requirements	000 Practically insoluble in water, freely soluble in methylene chloride, soluble in methanol, slightly soluble in alcohol	Meets requirements
Identification Ketoconazole		IR-spectrophotometry 9000 Meets requirements
Solution appearance	Clear and no more color than BY4	Meets requirements
Optical rotation	+ 0.01 °
Related substances	≤ 0.5%	0.23%
Heavy metal	≤ 20 ppm 08
Loss from drying	≤ 0.5%	0.11%
Sulphated ash	≤ 0.1%
General aerobic germ counter	≤ 100cfu / g	qualified
Total yeast and mold	908/482 ≤ 1003000		/9000 g 9000 qualified E. coli	Absent per gram 9084 8	qualified
Pseudomonas aeruginosa	Absent per gram	Qualified
Staphylococcus	99.0% – 101.0%	99.98%

——————– ——————

High Quality, Pure Ketoconazole BP EP Powder / Substance API Raw Material Factory in China; China Ketoconazole BP EP API Powder Raw Material Supplier in China.China Ketoconazole BP EP Raw Material Powder Manufacturers in China.

Ketoconazole [LifeBio.wiki]

Ketoconazole is a synthetic imidazole antifungal drug primarily used to treat fungal infections. Ketoconazole is sold commercially as tablets for oral administration (although this use has been discontinued in several countries) and various topical preparations such as creams (used to treat lichen, cutaneous candidiasis, including paronychia and pityriasis versicolor) and shampoos ( used primarily for the treatment of dandruff-seborrheic dermatitis of the scalp).¹⁾
The less toxic and usually more effective triazole antifungals fluconazole and itraconazole are generally preferred for systemic use. In 2013, the European Medicines Agency (CHMP) Committee recommended a ban on the systemic use of oral ketoconazole in humans across the European Union, after the conclusion that the risk of serious liver injury from systemic use of ketoconazole outweighed its benefits. Ketoconazole oral formula was discontinued in Australia in 2013, and in China in 2015 ²⁾.

Trade names: Nizoral
Application: oral (tablets), topically (cream, shampoo, solution)
Legal status:
UK: POM (prescription only)
USA: Dispensed without a prescription
Pharmacokinetic data
Bioavailability:
Oral: 37-97%
Protein binding: 84 to 99%
Metabolism: Extensive hepatic (mainly oxidation, O-dealkylation)
Metabolites: N-deacetylketoconazole
Biological half-life: biphasic
Excretion: biliary (main) and renal
Formula: C ₂₆ H ₂₈ Cl ₂ N ₄ O ₄
Molar mass: 531.431 g / mol
Chirality: racemic mixture

Medical use

Antifungal agent

Local antifungal

Topically, ketoconazole is usually prescribed to treat fungal infections of the skin and mucous membranes, such as foot rubrophy, ringworm, candidiasis (yeast infection or thrush), athlete’s foot, and pityriasis versicolor.Topically, ketoconazole is also used as a remedy for dandruff (seborrheic dermatitis of the scalp) and seborrheic dermatitis elsewhere on the body, possibly suppressing levels of the fungus Malassezia furfur on the skin. ³⁾

Systemic antifungal agent

Ketoconazole is active against many fungal species that can cause human disease, such as Candida, Histoplasma, Coccidioides, and Blastomyces (although it is inactive against Aspergillus).First synthesized in 1977, ketoconazole was the first orally active azole antifungal drug. However, ketoconazole has largely been replaced as a first-line systemic antifungal by other azole antifungals such as itraconazole due to the greater toxicity of ketoconazole, lower absorption and more limited spectrum of activity. ⁴⁾
Ketoconazole is used orally at doses ranging from 200 to 400 mg per day to treat superficial and deep fungal infections.

Antiandrogen and antiglycocorticoid

The side effects of ketoconazole are sometimes used in the treatment of non-fungal diseases. While ketoconazole blocks the synthesis of erythrosterol in humans at high doses (over 800 mg / day), it strongly inhibits the activity of several enzymes needed to convert cholesterol to steroid hormones such as testosterone and cortisol. Ketoconazole has been shown to inhibit the side chain cholesterol cleavage enzyme that converts cholesterol to pregnenolone, 17α-hydroxylase and 17,20-lyase, which convert pregnenolone to androgens, and 11β-hydroxylase, which converts 11-deoxycortisol to cortisol.All of these enzymes are mitochondrial cytochrome p450 enzymes. Based on these antiandrogenic and antiglucocorticoid effects, ketoconazole has been used with some success as a second line treatment for certain forms of prostate cancer ⁵⁾ and to suppress glucocorticoid synthesis in the treatment of Cushing’s syndrome. However, in the treatment of prostate cancer, the simultaneous use of glucocorticoids is necessary to prevent adrenal insufficiency.Ketoconazole has additionally been used at lower doses for the treatment of hirsutism and in combination with a GnRH analog, precocious puberty in men. In any case, the risk of hepatotoxicity with ketoconazole limits its use in all of these indications, especially in those that are benign such as hirsutism.

Use for unregistered indications

Hair loss

Ketoconazole shampoo in combination with an oral 5α-reductase inhibitor has been used off-label for the treatment of androgenetic alopecia.The antifungal properties of ketoconazole reduce the microflora of the scalp and therefore may reduce the follicular inflammation that contributes to baldness. Limited clinical research suggests that ketoconazole shampoo, used either alone or in combination with other treatments, may be helpful in reducing hair loss. At least one study has been conducted showing that ketoconazole may be beneficial for the temporary decrease in erectile function in patients undergoing postoperative penile surgery.⁶⁾

Veterinary use

Ketoconazole is also sometimes prescribed by veterinarians for use in pets, often as a tasteless tablet that may need to be cut to a smaller size for correct dosage. ⁷⁾

Side Effects

Ketoconazole is a pregnancy category C drug because animal testing has shown that it induces teratogenesis when given in high doses.It was reported that systemic administration of ketoconazole to two pregnant women for the treatment of Cushing’s syndrome had no side effects, but this small sample does not allow for any meaningful conclusions. A follow-up study in Europe showed no risk to infants of mothers who received ketoconazole. In July 2013, the US Food and Drug Administration (FDA) issued a warning that taking ketoconazole could lead to severe liver injury and adrenal problems.Nizoral oral tablets are not recommended as the first line of treatment for any fungal infection. Nizoral should be used to treat certain fungal infections known as endemic mycoses only when alternative antifungal treatments are unavailable or poorly tolerated. Nizoral’s topical formulas have not been associated with liver damage, adrenal problems, or drug interactions. These formulations include creams, shampoos, foams and gels applied to the skin, as opposed to Nizoral tablets, which are taken orally.⁸⁾

Pharmacology

As an antifungal agent, ketoconazole is structurally similar to imidazole and interferes with the fungal synthesis of ergosterol, which makes up the membranes of fungal cells, as well as some enzymes. Like all azole antifungal agents, ketoconazole works primarily by inhibiting the cytochrome P450 enzyme 14α-demethylase (CYP51A1). This enzyme is involved in the sterol biosynthetic pathway that leads from lanosterol to ergosterol.Lower doses of fluconazole and itraconazole are required to kill fungi compared to ketoconazole because they have been shown to have a greater affinity for fungal cell membranes. As an antiandrogen, ketoconazole acts through at least two mechanisms. First and foremost, high oral doses of ketoconazole (eg, 400 mg three times daily) block testicular and adrenal biosynthesis, resulting in a decrease in circulating testosterone levels. ⁹⁾ This effect is caused by inhibition of 17α-hydroxylase and 17,20-lyase, which are involved in the synthesis and degradation of steroids, including testosterone precursors.Due to its effectiveness in lowering systemic androgen levels, ketoconazole has been used with some success as a treatment for androgen-dependent prostate cancer. Second, ketoconazole is an androgen receptor antagonist that competes with androgens such as testosterone and dihydrotestosterone (DHT) to bind to the androgen receptor. This effect was found to be rather weak even with high oral doses of ketoconazole. Ketoconazole, along with miconazole, acts as a glucocorticoid receptor antagonist.Ketoconazole is a racemic mixture of cis- (2S, 4R) – (-) and cis- (2R, 4S) – (+) enantiomers. The cis (2S, 4R) isomer inhibited progesterone 17α, 20-lyase more strongly than its enantiomer (IC50 values 0.05 and 2.38 μM, respectively) and inhibited 11β-hydroxylase (IC50 values 0.152 and 0.608 μM, respectively). Both isomers were relatively weak inhibitors of human placental aromatase.

Resistance

Resistance has been observed in a number of clinical fungal isolates, including Candida albicans.Experimentally, resistance usually results from mutations in the sterol biosynthetic pathway. Defects in the enzyme 5-6 sterol desaturase reduce the toxic effect of azole inhibition at the stage of 14-alpha demethylation. Multidrug resistance (MDR) genes may also play a role in lowering cellular drug levels. Because azole antifungals act at the same point in the sterol pathway, resistant isolates are usually cross-resistant to all members of the azole family.¹⁰⁾

Pharmacokinetics

When administered orally, ketoconazole is best absorbed at highly acidic levels, so antacids or other causes of decreased gastric acid levels decrease absorption of the drug. Absorption can be increased by taking the drug with an acidic drink, such as cola ¹¹⁾. Ketoconazole is highly lipophilic and tends to accumulate in adipose tissue.

History

Ketoconazole was discovered in 1976 by Janssen Pharmaceutica.It was originally introduced in 1977 and later in the United States in 1981. It was introduced as a prototype among the antifungal agents of imidazole. Oral ketoconazole has been replaced by oral itraconazole in many mycoses ¹²⁾.

: Tags

References:

¹⁾
Rossi, S, ed. (2013). Australian Medicines Handbook (2013 ed.). Adelaide: The Australian Medicines Handbook Unit Trust.ISBN 978-0-9805790-9-3.

²⁾
“国家食管理总局关于停止生产销售使用酮康唑口服制剂的公告（2015 年第 85 号）” (in Chinese). China Food and Drug Administration. 2015-06-25. Retrieved 2015-07-02

³⁾
Young BK, Brodell RT, Cooper KD (2013). Therapeutic Shampoos. In Wolverton SE. Comprehensive Dermatologic Therapy (3rd ed.). Philadelphia: Saunders. pp. 562-569. ISBN 978-1-4377-2003-7.

⁴⁾
Kauffman CA (2004). “Introduction to the Mycoses”. In Goldman L; Ausiello, D.Cecil Textbook of Medicine (22nd ed.). Philadelphia: Saunders. p. 2043. ISBN 0-7216-9652-X.

⁵⁾
Zelefsky MJ, Eastham JA, Sartor OA, Kantoff P (2008). DeVita VT, Lawrence TS, Rosenberg SA, eds. Cancer: Principles & Practice of Oncology (8th ed.). Philadelphia: Lippincott Williams & Wilkins. p. 1443. ISBN 9780781772075.

⁶⁾
Evans, K. C .; Peterson, A. C .; Ruiz, H. E .; Costabile, R. A. (2004-08-01). “Use of oral ketoconazole to prevent postoperative erections following penile surgery.”International Journal of Impotence Research. 16 (4): 346-349. doi: 10.1038 / sj.ijir.30. ISSN 0955-9930. PMID 14973533

⁷⁾
KuKanich B (January 2008). “A review of selected systemic antifungal drugs for use in dogs and cats”

⁸⁾
“FDA limits usage of Nizoral (ketoconazole) oral tablets due to potentially fatal liver injury and risk of drug interactions and adrenal gland problems.” FDA Drug Safety Communication. U.S. Food and Drug Administration.July 26, 2013. Retrieved November 23, 2013.

⁹⁾
Witjes FJ, Debruyne FM, Fernandez del Moral P, Geboers AD (May 1989). “Ketoconazole high dose in management of hormonally pretreated patients with progressive metastatic prostate cancer. Dutch South-Eastern Urological Cooperative Group “. Urology. 33 (5): 411-5. doi: 10.1016 / 0090-4295 (89)

-X. PMID 2652864

¹⁰⁾
Sanglard D, Ischer F, Monod M, Bille J (February 1997). “Cloning of Candida albicans genes conferring resistance to azole antifungal agents: characterization of CDR2, a new multidrug ABC transporter gene.”Microbiology. 143 (Pt 2) (Pt 2): 405-16. doi: 10.1099 / 00221287-143-2-405. PMID

¹¹⁾
Chin TW, Loeb M, Fong IW (August 1995). Effects of an acidic beverage (Coca-Cola) on absorption of ketoconazole. Antimicrobial Agents and Chemotherapy. 39 (8): 1671-5. doi: 10.1128 / AAC.39.8.1671. PMC 162805Freely accessible. PMID 7486898

¹²⁾
David E. Golan (2008). Principles of Pharmacology: The Pathophysiologic Basis of Drug Therapy. Lippincott Williams & Wilkins.pp. 624–. ISBN 978-0-7817-8355-2.

nizoral ketoconazole.txt · Last modified: 2021/06/11 17:37 – dr.cookie

Ketoconazole for dogs: dosage, instructions

Ketoconazole is an antifungal drug primarily used to treat fungal infections in dogs, although it has additional properties that may help treat obstructive alopecia (hair loss).

The drug is obtained from the organic compound imidazole – a substance that prevents the growth of fungal infections.

How can it be used?

As an antifungal agent it is used to treat fungal infections, both internal and external. In addition, it can be used to treat the following diseases:

Cushing’s syndrome (neuroendocrine disease characterized by increased production of adrenal hormones) – rarely,
baldness (alopecia),
histoplasmosis (a disease caused by the fungus Histoplasma capsulatum , the disease primarily affects the lungs),
blastomycosis (a disease from the group of systemic mycoses, occurring with primary damage to the lungs and hematogenous dissemination of a fungal infection into internal organs, bones and skin),
meningitis (inflammation of the lining of the brain and spinal cord).

What is the difference between Cushing’s syndrome / disease?

Cushing’s disease and Cushing’s syndrome are two different diseases. Cushing’s syndrome occurs when a dog is exposed to high levels of cortisol for an extended period of time, while Cushing’s disease is when the adrenal or pituitary gland causes the body to produce too much cortisol. Cushing’s syndrome can occur as a result of Cushing’s disease.

Fungistatic versus fungicide: what’s the difference?

Imidazole derivatives, including ketoconazole, are usually fungistatic (delay and arrest of fungal growth).This means that instead of directly killing the fungus, they restrict its growth and rely on natural processes to clear the infection out of the body. When used in higher doses, they can become fungicidal, with the property of inhibiting (suppressing) the development of pathogenic fungi and attacking cell membranes. Fungistatic drugs are more commonly used because they are safer, but they may not be a good option for treating life-threatening infections or when the dog’s immune system is weakened.

Safe dosage

Do not give ketoconazole unless directed by your veterinarian.

In most cases, it can be used topically to treat an external fungal infection. For internal infections, a dose of 4.8 mg / kg twice a day is often prescribed (this is the usual dose for the treatment of systemic coccidioidomycosis – fungal diseases), but higher doses of up to 22 mg / kg or more can be used. For safety reasons, use gloves and wash your hands thoroughly after handling the animal.

Example: A dog weighing 22.7 kg is given a dose of 109 mg, which is approximately half of the usual 200 mg tablet.

Is it safe?

Ketoconazole is prescribed by veterinarians and is considered safe to use. Ketoconazole creams and shampoos show less side effects, and after topical application, skin irritation occurs in rare cases.

Contraindications

There are not many contraindications associated with this medication, it is not recommended for dogs with liver problems, especially when given at higher doses.

Safety Rules

Before using the drug, for the safety of the treatment regimen and the recommended dosage, consult your veterinarian.

Minimizing the risk of hypocorticolism

In order to avoid the development of symptoms of Addison’s disease (chronic insufficiency of the adrenal cortex), it is recommended to prescribe Prednisone, since the drug inhibits the production of cortisol.

Side effects in dogs

Some side effects may occur when using the drug.

Most common :

no appetite,
nausea,
diarrhea,

90,026 vomiting;

rare:

liver damage,
coat color changes,
infertility (in males),
skin irritation.

Watch for signs of drowsiness in conjunction with a yellow tinge to the gums and discoloration (to white) of the eye. These signs often indicate liver damage and require immediate veterinary attention.