Conasyd

Approved Indications:

• Vaginal Candidiasis (Vulvovaginal Candidiasis): Treatment of uncomplicated infections caused by Candida albicans and other susceptible yeasts.
• Cutaneous Candidiasis: Topical treatment of superficial fungal infections of the skin including candidal intertrigo and diaper dermatitis.
• Tinea Pedis (Athlete’s Foot): Topical treatment for dermatophyte infections caused by Trichophyton rubrum, T. mentagrophytes, and Epidermophyton floccosum.
• Tinea Cruris (Jock Itch) and Tinea Corporis (Ringworm): Used to treat fungal infections of the groin and body.

Off-label/Clinically Accepted Uses:

• Onychomycosis (Nail Fungal Infections): Occasionally used off-label in topical formulations for localized infections, although less effective than systemic agents.
• Recurrent Vaginal Candidiasis: In some regimens, tioconazole may be part of maintenance therapy.

Adults:

• Vaginal Candidiasis:
  Tioconazole 6.5% vaginal ointment
  ▸ Dose: One full applicator (approximately 5 g) intravaginally as a single dose at bedtime.
  ▸ Route: Intravaginal
  ▸ Frequency: Once (single-dose therapy)
  ▸ Duration: One night; symptoms usually resolve in 3–7 days.
• Cutaneous Mycoses (Tinea corporis, cruris, pedis, candidiasis):
  Tioconazole 1% cream
  ▸ Dose: Apply a thin layer to the affected area twice daily.
  ▸ Duration: 2–4 weeks depending on clinical response.

Pediatrics:

• Safety and efficacy in children under 12 years have not been fully established for vaginal formulations.
• For topical cream, pediatric use may be considered in superficial infections under physician supervision.

Elderly:

• No dosage adjustment necessary; use as in adults.

Renal/Hepatic Impairment:

• No dose adjustment necessary for topical use due to minimal systemic absorption.

Tioconazole is an imidazole antifungal agent that inhibits the synthesis of ergosterol, an essential component of fungal cell membranes. It interferes with the fungal cytochrome P450 enzyme lanosterol 14α-demethylase, disrupting membrane integrity and increasing membrane permeability. This leads to leakage of essential intracellular components and ultimately fungal cell death. Its fungicidal activity is primarily due to its ability to interfere with the biosynthesis of lipids required for membrane formation.

• Absorption:
  ▸ Vaginal application results in approximately 10% systemic absorption.
  ▸ Topical skin application has minimal systemic absorption.
• Distribution:
  ▸ Limited systemic distribution; primarily remains localized at the application site.
• Metabolism:
  ▸ Once absorbed, metabolized hepatically via oxidative pathways (not significantly via CYP450 enzymes).
• Elimination:
  ▸ Primarily eliminated via the feces; small amounts may appear in urine.
  ▸ Elimination Half-life: Variable; systemic data limited due to minimal absorption.
• Onset of Action:
  ▸ Symptom relief often begins within 24–72 hours after administration.

• Pregnancy:
  ▸ Classified as FDA Pregnancy Category C (based on older classification).
  ▸ Animal studies have shown adverse fetal effects; adequate human studies are lacking. Use only if benefits outweigh risks.
• Lactation:
  ▸ Not known whether tioconazole is excreted in breast milk.
  ▸ Given its minimal systemic absorption after topical or vaginal use, risk to breastfeeding infants is considered low.
  ▸ Caution is advised, especially if applied to areas near the breast or nipples.

• Primary Class: Antifungal agent
• Subclass: Imidazole antifungal (topical/vaginal)
• Generation: First-generation imidazole derivative

• Known hypersensitivity to tioconazole or any imidazole derivatives
• Hypersensitivity to any component of the formulation
• Use in children under 12 years for vaginal application (unless prescribed by a physician)

• Hypersensitivity Reactions: Stop use if irritation, burning, or rash develops; may indicate allergic reaction.
• Not for Ophthalmic Use: Avoid contact with eyes; rinse thoroughly with water if accidental exposure occurs.
• Not for Oral Use: For topical and vaginal use only.
• Recurrent Infections: Recurrent vaginal candidiasis may require medical evaluation for underlying causes (e.g., diabetes, immunosuppression).
• Systemic Absorption in Damaged Skin: Use caution when applying to large areas or broken skin.

Common (≥1%):

• Local (Topical/Vaginal):
  ▸ Burning sensation
  ▸ Itching
  ▸ Irritation
  ▸ Vulvar or perineal discomfort
  ▸ Skin redness or stinging

Less Common:

• Vaginal discharge
• Swelling at the application site
• Abdominal cramps (vaginal use)

Rare but Serious:

• Hypersensitivity reactions (rash, angioedema, urticaria)
• Anaphylaxis (extremely rare)
• Severe contact dermatitis

Onset: Typically occurs within the first 1–3 days of use
Severity: Usually mild to moderate and self-limiting

• Drug–Drug:
  ▸ Minimal due to low systemic absorption.
  ▸ Avoid concurrent vaginal products (e.g., spermicides, other antifungals) which may reduce efficacy.
  ▸ May weaken latex condoms or diaphragms—use alternative contraception for at least 72 hours after use.
• Drug–Alcohol:
  ▸ No known interaction with alcohol (unlike metronidazole-type agents).
• Enzyme Systems:
  ▸ Limited systemic activity; not a significant CYP450 inducer or inhibitor.

• EMA & FDA: No recent changes in approved indications or major safety warnings in the last 3 years.
• Clinical Practice Guidelines (CDC): Single-dose tioconazole remains a recommended option for uncomplicated vulvovaginal candidiasis.
• Pharmacovigilance: Continued surveillance for hypersensitivity reactions has been emphasized, particularly in recurrent users.

• Temperature: Store below 25°C (77°F); do not freeze.
• Humidity/Light Protection: Keep in a tightly closed container; protect from excessive moisture and direct light.
• Handling Precautions:
  ▸ Do not use expired products.
  ▸ Wash hands before and after application.
  ▸ For vaginal applicators, discard after single use (disposable).