K Doc 200mg Tablet

• Active Ingredient: Ketoconazole 200 mg
• Inactive Ingredients: May include colloidal silicon dioxide, corn starch, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and povidone (specific excipients may vary by manufacturer; consult the product leaflet for exact details).

Therapeutic Class

• Azole antifungal

Mechanism of Action

Ketoconazole works by inhibiting the synthesis of ergosterol, a critical component of fungal cell membranes. This disrupts the fungal cell membrane's structure and function, leading to cell death and preventing further fungal growth. It is effective against a wide range of fungi and yeasts.

Indications

K DOC 200 mg Tablet is used to treat serious fungal or yeast infections, including:

• Systemic fungal infections such as:
  • Candidiasis (e.g., oral thrush, chronic mucocutaneous candidiasis)
  • Blastomycosis
  • Coccidioidomycosis (Valley fever)
  • Histoplasmosis
  • Chromoblastomycosis
  • Paracoccidioidomycosis
• Severe fungal infections of the skin, nails, hair, or mucous membranes (e.g., ringworm, yeast infections) when topical treatments or other antifungals are ineffective or not tolerated.
• In some cases, it may be used for conditions like Cushing’s syndrome (under specialist supervision) or severe seborrheic dermatitis.

• Dosage and Administration

• Adults: The typical starting dose is 200 mg once daily, taken orally with a meal to enhance absorption. The dose may be increased to 400 mg once daily if clinical response is inadequate, as determined by a healthcare provider. Treatment duration varies (e.g., 1–2 weeks for candidiasis, up to 6 months for systemic infections).
• Children (2 years and older): Dose is based on body weight, typically 3.3–6.6 mg/kg/day, as prescribed by a doctor. Safety and efficacy are not established in children under 2 years.
• Administration: Swallow the tablet whole with water, preferably with food to reduce stomach upset and maximize absorption. Avoid taking with antacids or acid-reducing medications within 2 hours, as they may reduce absorption.
• Important: Complete the full course of treatment, even if symptoms improve, to prevent recurrence or resistance.

• Pharmacokinetics

• Absorption: Peak plasma concentrations (~3.5 mcg/mL) are reached within 1–2 hours after a 200 mg dose taken with a meal. Absorption is optimal in an acidic environment and reduced in patients with low gastric acidity.
• Distribution: Widely distributed in tissues, including skin, nails, and saliva, but poorly penetrates the cerebrospinal fluid (not suitable for fungal meningitis).
• Metabolism: Primarily metabolized in the liver via CYP3A4 to inactive metabolites.
• Excretion: Over 95% is eliminated through hepatic metabolism, with only 2–4% excreted unchanged in urine. Elimination half-life is biphasic (2 hours initially, 8 hours thereafter).

• Contraindications

• Hypersensitivity to Ketoconazole or any tablet components.
• Co-administration with drugs metabolized by CYP3A4 that prolong the QT interval (e.g., dofetilide, quinidine, pimozide, cisapride) due to risk of life-threatening arrhythmias like torsades de pointes.
• Use with statins (e.g., simvastatin, lovastatin), as it may increase the risk of rhabdomyolysis.
• Acute or chronic liver disease, or liver enzyme levels >2 times the upper limit of normal.
• Pregnancy and breastfeeding, unless benefits outweigh risks (teratogenic in animal studies; passes into breast milk).

• Precautions

• Liver Function: Ketoconazole can cause hepatotoxicity, including fatal liver injury or the need for transplantation. Liver function tests should be monitored before and during treatment. Stop treatment if signs of liver injury (e.g., jaundice, dark urine, abdominal pain) occur.
• Heart Rhythm: May prolong the QT interval, increasing the risk of serious arrhythmias. Avoid in patients with congenital long QT syndrome or those taking QT-prolonging drugs.
• Adrenal Insufficiency: High doses may suppress adrenal function, causing symptoms like tiredness, weakness, or nausea. Monitor closely if high doses are used.
• Drug Interactions: Ketoconazole is a potent CYP3A4 inhibitor and may increase levels of drugs like statins, benzodiazepines, or calcium channel blockers. Always inform your doctor of all medications, including OTC drugs and supplements.
• Alcohol: Avoid alcohol, as it increases the risk of liver damage and may cause flushing, rash, or nausea.
• Gastric Acidity: Absorption is reduced in patients with low stomach acid (e.g., those taking proton pump inhibitors or H2 blockers). Taking with an acidic beverage (e.g., non-diet cola) may improve absorption.

• Side Effects

• Common: Nausea, vomiting, stomach pain, headache, dizziness, or rash.
• Serious: Hepatotoxicity (liver damage, jaundice, dark urine).
• Allergic reactions (rash, hives, swelling, difficulty breathing).
• QT prolongation or irregular heartbeats.
• Adrenal insufficiency (fatigue, weakness, low blood pressure).