🧪 Composition
Ketoconazole Cream:
- Active Ingredient:
- Ketoconazole USP 2% w/w
- Preservatives:
- Benzoate BP (Methyl Paraben)
- Propyl Hydroxy Benzoate BP (Propyl Paraben)
- Excipients:
- Cetomacrogol 1000 BP
- Cetostearyl Alcohol BP
- Methyl Hydroxy BP
- Sodium Dihydrogen Phosphate Dihydrate BP
- Anhydrous Sodium Sulphite BP
- Soft Paraffin BP (White Petroleum Jelly)
- Chlorocresol BP (PCMC)
- Propylene Glycol
Ketoconazole Tablets:
- Active Ingredient:
- Ketoconazole USP 200mg
- Excipients:
- Povidone BP
- Colloidal Anhydrous Silica BP
- Magnesium Stearate BP
- Hypromellose BP
- Lactose BP
- Maize Starch BP
- Microcrystalline Cellulose BP
- Purified Talc BP
- Titanium Dioxide BP
- Macrogol 4000 BP
- Propylene Glycol BP
🧬 Pharmacological Category & Action
- Category: Synthetic imidazole dioxolane derivative
- Action:
- Inhibits biosynthesis of ergosterol in fungi
- Alters lipid composition of fungal membranes
- Results in membrane defects
- Fungicidal activity against dermatophytes, yeasts, and other pathogenic fungi
🎯 Therapeutic Indications
Ketazol Cream:
- Topical treatment of:
- Ringworm of the body
- Tinea cruris
- Athlete's foot
- Yeasts and fungus
- Candida infections
Ketazol Tablets:
- Systemic fungal infections:
- Severe recalcitrant cutaneous dermatophyte infections unresponsive to topical therapy or oral griseofulvin
- Serious chronic infections of skin, hair, nails caused by sensitive dermatophytes and/or yeasts
- Serious mycoses of the gastrointestinal tract not responsive to other therapy
🚫 Contraindications
- Hypersensitivity to Ketazol or any of its ingredients
- Tablets contraindicated in patients with pre-existing liver disease
💊 Dosage & Administration
Ketazol Cream:
| Condition | Frequency & Duration |
|---|---|
| Cutaneous candidiasis, Tinea spp. | Apply once daily to affected area |
| Seborrhoeic dermatitis | Apply once or twice daily |
| Tinea versicolor | 2–3 weeks |
| Yeast infection | 2–3 weeks |
| Tinea cruris | 2–4 weeks |
| Tinea corporis | 3–4 weeks |
| Tinea pedis | 4–6 weeks |
| Seborrhoeic dermatitis (maintenance) | Once or twice weekly |
Continue treatment until a few days after symptoms disappear. Reassess diagnosis if no improvement after 4 weeks.
Ketazol Tablets:
| Indication | Dosage & Duration |
|---|---|
| Chronic/recurrent vaginal candidiasis | 2 tablets (400mg) once daily with meal for 5 days |
| All other indications | 1 tablet (200mg) daily |
| If response insufficient | Increase to 400mg daily |
Continue until 1 week after symptoms disappear and cultures are negative.
| Condition | Duration |
|---|---|
| Serious chronic mycoses of skin/hair | 1–2 months |
| Systemic candidiasis | 1–2 months |
| Chronic mucocutaneous candidiasis | 6–12 months |
| Coccidioidomycosis, paracoccidioidomycosis, histoplasmosis | 2–6 months |
| Dermatophytes | 4 weeks |
🧫 Pharmacokinetic Properties
| Property | Tablets | Cream |
|---|---|---|
| Absorption | Incomplete | Negligible |
| Pre-systemic metabolism | Significant | — |
| Plasma half-life | 6–10 hours | — |
| Volume of distribution | 0.36 L/kg | Not detectable |
| Plasma protein binding | 99% | — |
| Elimination | Via bile | — |
⚠️ Adverse Reactions
Cream:
- Pruritus
- Irritation
- Burning sensation
- Rare: Contact dermatitis
Tablet:
- GI: Nausea, vomiting, constipation
- CNS: Headache, dizziness, drowsiness, photophobia, paraesthesia
- Hematologic: Thrombocytopenia
- Skin: Exanthema, itching, rash, urticaria
- Hormonal: Transient decreased libido, reversible gynaecomastia, oligospermia
- Others: Alopecia, anaphylactoid reactions, increased liver enzymes
⚠️ Warnings & Precautions
General:
- Avoid alcohol (disulfiram-like reaction possible)
- Monitor for hepatitis symptoms—discontinue if detected
Pregnancy & Lactation:
- Not safe during pregnancy or nursing
Paediatric Use:
- Tablets not recommended for children (safety not proven)
🔄 Drug Interactions
Cream:
- None reported with local application
Tablets:
- ↓ Blood levels with rifampicin or isoniazid
- May require dose adjustment of:
- Cyclosporin
- Anticoagulants
- Methylprednisolone
- Tacrolimus
- Indinavir
- Busulphane
- Contraindicated with:
- Terfenadine
- Astemizole
- Cisapride
- Oral midazolam
- Triazolam
- IV midazolam: Use with caution
- Didanosine: Administer ketoconazole 2 hours before
- ↑ Concentrations of saquinavir and ritonavir—monitor closely
🚨 Overdosage & Treatment
Cream:
- Excessive use may cause erythema, oedema, burning sensation
- Symptoms resolve upon discontinuation
Tablet:
- Accidental overdose:
- Supportive/symptomatic treatment
- Gastric lavage with sodium bicarbonate
📦 Storage Conditions
- Do not store above 30°C
- Protect from sunlight
- Keep out of reach of children
📦 Presentation
| Product | Packaging | Regulatory Info |
|---|---|---|
| Ketazol Cream | Tube of 30gm / 15gm | Zambia Lic. No.: 075/024 |
| NAFDAC Reg. No.: A4-2136 | ||
| PPB Reg. No.: H2015/CTD029/247 | ||
| Malawi License No.: PMPB/PL503/25 | ||
| Scheduling Status in Malawi: PIM | ||
| Ketazol Tablets | Pack of 10 tablets | Zambia Lic. No.: 075/039 |
| NAFDAC Reg. No.: A4-5572 |
📅 Publication Date
25/08/2021