Nizoral

Nizoral (ketoconazole) is an antifungal medication that is often used to treat various fungal infections of the skin, hair, and nails. Ketoconazole belongs to the class of antifungal azole drugs.

Nizoral is available in various forms including creams, gels, shampoos, solutions and tablets.

The active ingredient ketoconazole penetrates fungal cells and disrupts their membranes, leading to their death. When using Nizoral, it is important to follow your doctor's instructions or package directions and avoid contact with eyes or other sensitive skin areas. A doctor should be consulted if side effects occur or symptoms worsen.

Indications Nizoral

1. Onychomycosis (fungal infection of the nails): Ketoconazole may be used to treat fungal nail infections that can cause changes in the color, texture, and thickness of the nails.
2. Athlete's foot (dermatophytosis feet): This is a fungal infection that manifests as redness, flaking, itching and cracking between the toes of the foot. Nizoral may help treat this condition.
3. Shingles(dermatophytosis of the body): Ketoconazole may be effective in treating various forms of lichen, such as ringworm or spotted lichen.
4. Candidal infections of the skin and mucous membranes: This includes fungal infections caused by the fungus Candida, such as thrush (vaginal candidiasis), stomatitis (inflammation of the oral mucosa) or candidiasis of the skin.
5. Seborrheic Dermatitis: Nizoral may also be used to treat seborrheic dermatitis, a skin condition characterized by periodic exacerbations of redness, burning, and flaking in the face, head, or other areas of the body.

Release form

1. Oral tablets: Used for the treatment of systemic fungal infections that do not respond to topical treatment. Nizoral tablets may be prescribed to treat conditions such as fungal infections of the skin, nails, internal organs (e.g. Fungal meningitis) and other systemic infections.
2. Cream/ointment for external use: It is applied directly to the affected skin areas for the treatment of various skin fungal infections such as dermatophytosis, candidiasis, pityriasis ("sun" lichen) and others. Nizoral cream or ointment provides targeted action on the infection, minimizing systemic side effects.
3. Shampoo: Nizoral Shampoo is used for the treatment and prevention of dandruff caused by fungal infections of the scalp, such as pityriasis versicolor and seborrheic dermatitis. The shampoo helps reduce itching, flaking and redness associated with these conditions.

Pharmacodynamics

1. Inhibition of ergosterol synthesis: Ketoconazole is an inhibitor of the enzyme cytochrome P450 14α-demethylase, which is involved in the synthesis of ergosterol, an important component of fungal cell membranes. Blocking of this enzyme leads to disruption of ergosterol synthesis, which weakens the cell membranes of fungi and leads to their death.
2. Broad spectrum of action: Ketoconazole is active against many species of dermatophytes, yeast-like and mold fungi including Candida spp., Trichophyton spp., Epidermophyton spp., Microsporum spp., Malassezia spp., Cryptococcus neoformans and others.
3. Prolonged action: Ketoconazole has a long duration of action, which allows it to remain active in the body for a long time after a single dose.
4. Treatment of fungal infections: Nizoral is effective in treating a variety of fungal infections including dermatomycosis, vaginal candidiasis, oral candidiasis, coccidiomycosis and others.
5. Systemic and topical application: The drug is available for both systemic and topical application in the form of creams, gels and shampoos, which allows its use for various localizations of fungal infections.
6. Antiseborrheic Action: Ketoconazole may also be effective against seborrhea associated with overgrowth of Malassezia fungi on the skin.

Pharmacokinetics

1. Absorption: Ketoconazole is usually well absorbed from the gastrointestinal tract after oral administration. However, its absorption may be delayed when taken with food, therefore it is recommended to take the drug on an empty stomach for maximum absorption.
2. Distribution: Ketoconazole is widely distributed in body tissues, including skin, lungs, kidneys and liver. It can also penetrate the blood-brain barrier.
3. Metabolism: Ketoconazole undergoes significant metabolism in the liver through the processes of hydroxylation and N-demethylation, with the formation of inactive metabolites.
4. Excretion: Ketoconazole and its metabolites are mainly excreted with bile and urine. Its elimination half-life from the body is about 2 hours.
5. Mechanism of action: Ketoconazole inhibits the enzymes required for ergosterol synthesis in the cell membranes of fungi, which leads to disruption of their structure and function and, as a consequence, to the death of fungi.

Dosing and administration

Pills

• Foradults: For systemic fungal infections, the usual starting dose is 200 mg (one tablet) once daily. Depending on the severity of the infection and response to treatment, the dose may be increased to 400 mg (two tablets) once daily. Tablets should be taken with meals to improve absorption.
• For children: Administration and dosage for children should be closely monitored by a physician and is usually calculated based on the child's body weight.

Cream/Ointment

• Apply a thin layer to clean and dry skin of the affected area and a little around it once or twice a day, depending on the doctor's instructions. The duration of treatment may vary from 2 to 6 weeks, depending on the type and severity of the infection.

Shampoo

• To treat dandruff or seborrheic dermatitis: Apply shampoo todamp hair, lather, leave on for 3-5 minutes, then rinse thoroughly. Use twice a week for 2-4 weeks.
• For the prevention of dandruff: Use once a week or as directed by a physician.

General recommendations

• When using Nizoral in any form, it is important to complete the course of treatment completely, even if symptoms have improved earlier. Stopping treatment prematurely may cause the infection to return.
• When taking Nizoral tablets, you should avoid alcohol and certain medicines that may interact with ketoconazole. Talk to your doctor about any medicines you are taking.
• In case of side effects or allergic reactions, you should contact your doctor immediately.

Use Nizoral during pregnancy

1. Oral tablets: Used for the treatment of systemic fungal infections that do not respond to topical treatment. Nizoral tablets may be prescribed to treat conditions such as fungal infections of the skin, nails, internal organs (e.g. Fungal meningitis) and other systemic infections.
2. Cream/ointment for external use: It is applied directly to affected skin areas for the treatment of various skin fungal infections such as dermatophytosis, candidiasis, pityriasis ("sun" lichen) and others. Nizoral cream or ointment provides targeted action on the infection, minimizing systemic side effects.
3. Shampoo: Nizoral Shampoo is used for the treatment and prevention of dandruff caused by fungal infections of the scalp, such as pityriasis versicolor and seborrheic dermatitis. The shampoo helps reduce itching, flaking and redness associated with these conditions.

Contraindications

1. Hypersensitivity: People with known hypersensitivity to ketoconazole or other components of the drug should not use Nizoral due to the risk of allergic reactions.
2. Drugs interacting with ketoconazole: Nizoral may interact with other drugs such as terfenadine, astemizole, amprenavir, etc., which may lead to serious side effects. Patients should avoid concomitant use of Nizoral with such drugs if it is contraindicated.
3. Liver Disease: Patients with severe liver disease, such as cirrhosis or active liver damage, should consult a physician before using Nizoral, as it may increase the toxic effects on the liver.
4. Pregnancy and breastfeeding: There are limited data on the safety of ketoconazole during pregnancy and breastfeeding. The use of Nizoral during pregnancy or while breastfeeding should be done only on the recommendation of a doctor and only if clearly necessary.
5. Pediatric age: Safety and efficacy of Nizoral in children under 12 years of age have not been established, therefore use in this age group may be contraindicated.

Side effects Nizoral

1. Skin reactions: Include irritation, redness, itching or burning at the site of application. Skin rash or contact dermatitis may occur in some people.
2. Dry skin: The use of Nizoral may cause dry skin in the area of application.
3. Changes in hair texture: Some patients may experience changes in hair texture, including dryness, breakage, or loss of shine.
4. Eyeredness or itchy eyes: Some people may experience red eyes or itchy eyes after using Nizoral.
5. Redness, itching or irritation in the ear area: Some patients may experience various reactions in the ear area, including redness, itching or irritation.
6. Liver side effects: Rarely, Nizoral may cause side effects on the liver, including increased liver enzyme levels or hepatitis. If jaundice, abdominal pain, or other signs of liver problems occur, you should contact your doctor immediately.
7. GI side effects: May include nausea, vomiting, diarrhea, or abdominal discomfort.
8. Allergic reactions: Allergic reactions such as hives, swelling, or difficulty breathing may occur in some patients.

Overdose

1. Gastrointestinal disorders: nausea, vomiting, abdominal pain, diarrhea.
2. Liver failure: overdose may cause toxic effects on the liver, which may be manifested by increased levels of liver enzymes in the blood, jaundice, and other signs of liver failure.
3. Electrolyte disorders: overdose may cause various electrolyte disorders such as hypokalemia (decreased blood potassium levels) or hypomagnesemia (decreased blood magnesium levels).
4. Neurologic symptoms: headache, drowsiness, dizziness, dizziness, seizures, and other neurologic symptoms may be manifestations of overdose.
5. Other systemic complications: may include acute renal failure, arrhythmias, and other serious complications.

Treatment of ketoconazole overdose usually consists of symptomatic therapy, including measures to maintain vital functions of the body, correction of electrolyte disturbances, hydration, as well as the use of specific antidotes or antidotes if necessary.

Interactions with other drugs

1. Antifungal drugs: Combination of Nizoral with other antifungal drugs, such as terbinafine or fluconazole, may result in a stronger antimycotic effect and an increased risk of side effects.
2. Cyclosporine: Ketoconazole may increase the concentration of cyclosporine in the blood, which may lead to an increase in its toxicity, especially to the kidneys and liver.
3. Anticoagulants: Combination of Nizoral with anticoagulants, such as warfarin, may increase the risk of bleeding due to increased anticoagulant effect of warfarin.
4. Anti-inflammatory drugs (e.g. Dexamethasone): Nizoral may increase the effect of anti-inflammatory drugs, which may lead to an increased risk of side effects such as hyperglycemia or hypokalemia.
5. Anticonvulsants (e.g. Carbamazepine): Ketoconazole may decrease the concentration of anticonvulsants in the blood, which may lead to a decrease in their effectiveness and increase the risk of seizures.
6. Drugs processed by cytochrome P450: Ketoconazole is an inhibitor of cytochrome P450 and may increase the concentration of drugs metabolized by this enzyme in the blood, which may lead to an increase in their action or increase the risk of side effects.

Storage conditions

1. Temperature: Store Nizoral at room temperature, between 15 and 30 degrees Celsius (59-86 degrees Fahrenheit).
2. Dryness: Keep the preparation in a dry place. Avoid exposure to moisture, as moisture can adversely affect the stability and quality of the preparation.
3. Light: Store Nizoral in a dark place protected from direct sunlight. Exposure to light may also adversely affect the stability of the drug.
4. Packaging: Keep Nizoral in the original package or container in which it comes from the manufacturer. This will help protect the medicine from external influences.
5. Children: Keep Nizoral out of the reach of children to prevent accidental use.
6. Special Instructions: Follow the instructions on the package or your doctor's instructions about storing the medicine. Do not use expired medications, and keep track of the expiration date.