Zalain

Approved Indication:

• Vulvovaginal Candidiasis (VVC):
• Treatment of acute, recurrent, and chronic vulvovaginal candidiasis caused by Candida albicans and other Candida species in adult women.

Clinically Accepted Off-label Uses:

• Mixed Vaginitis:
• Occasionally used in conjunction with other agents for mixed vaginal infections involving Candida spp. and Gardnerella vaginalis.
• Azole-Refractory Candida Infections:
• Employed topically in patients with partial resistance or intolerance to other azoles, due to broad-spectrum antifungal activity and local effect.

Adult Women (Non-Pregnant):

• Dose: One 300 mg Sertaconazole nitrate vaginal ovule, administered as a single intravaginal dose.
• Frequency: A second dose may be given after 7 days if symptoms persist or recur.
• Route: Vaginal insertion, preferably at bedtime while lying down.
• Duration: Typically one dose; extended treatment is rarely required.

Elderly:

• No dose adjustment necessary; follow adult dosing.

Pediatric Use:

• Not recommended in girls under the age of menarche due to lack of safety data.

Pregnancy:

• Use only if clearly needed (see section 5).

Renal or Hepatic Impairment:

• No dose adjustment is required due to negligible systemic absorption.

Special Instructions:

• Avoid use during menstruation.
• Do not engage in sexual intercourse during treatment.
• Do not use vaginal douches, tampons, or other vaginal products during the treatment course.

Sertaconazole nitrate is an imidazole antifungal that exerts its effect by inhibiting the synthesis of ergosterol, a key structural component of fungal cell membranes. It blocks the enzyme lanosterol 14α-demethylase, impairing ergosterol formation and disrupting membrane integrity. This leads to increased membrane permeability and leakage of vital intracellular substances, resulting in fungal cell death. Sertaconazole also binds to non-sterol lipids in fungal membranes, enhancing its fungicidal activity. Additionally, it exhibits anti-inflammatory and antipruritic effects, contributing to symptom relief in vulvovaginal infections.

• Absorption: Minimal systemic absorption through the vaginal mucosa; plasma concentrations are typically undetectable.
• Distribution: Acts locally in the vaginal tissues; not systemically distributed.
• Metabolism: Not significantly metabolized due to poor systemic absorption.
• Excretion: Primarily eliminated through vaginal secretions.
• Onset of Action: Symptom improvement usually begins within 24 to 72 hours post-administration.
• Half-life: Not applicable due to negligible systemic presence.
• Bioavailability: Very low with intravaginal route.

• Pregnancy:
• FDA Category: Not assigned under the revised FDA labeling system.
• Clinical Use: Should be used during pregnancy only if clearly indicated. Minimal systemic absorption suggests low risk, but clinical data are limited, especially during the first trimester.
• Lactation:
• Breastfeeding Safety: Systemic absorption is negligible, making excretion into breast milk unlikely. No adverse effects reported in breastfed infants.
• Recommendation: Use with caution during lactation. Avoid direct application near the breast.

• Primary Class: Topical Antifungal
• Subclass: Imidazole Antifungal Agent (Vaginal)

• Known hypersensitivity to Sertaconazole or any component of the formulation
• Hypersensitivity to other imidazole antifungal agents
• Use in premenarchal girls
• Active menstruation at time of administration

• Hypersensitivity: Discontinue use if signs of allergic reaction occur (e.g., swelling, rash, or itching).
• Use in Pregnancy: Use only when clearly necessary. Avoid during the first trimester unless benefits outweigh risks.
• Concurrent Vaginal Conditions: Consider alternative treatments in case of suspected mixed infections that require systemic therapy.
• Sexual Activity: Sexual intercourse should be avoided during treatment to reduce risk of irritation or reinfection.
• Monitoring: Clinical reassessment is advised if symptoms persist beyond 7 days or recur frequently.

Common (Localized):

• Vaginal burning or stinging
• Itching or discomfort
• Increased vaginal discharge
• Local erythema

Less Common:

• Vulvovaginal swelling
• Urticaria

Rare or Serious:

• Allergic hypersensitivity reactions (e.g., angioedema) – rare but possible

Timing and Severity:

• Most side effects are mild, occur within hours post-dose, and resolve spontaneously.

• Drug-Drug Interactions:
• No clinically significant systemic drug interactions reported due to limited absorption.
• Drug-Food Interactions:
• Not applicable for vaginal use.
• Drug-Alcohol Interactions:
• No known interactions.
• Enzyme Involvement:
• Not known to affect hepatic cytochrome P450 enzymes (e.g., CYP3A4) systemically.

• FDA/EMA: No recent changes in indication, dosage, or safety labeling for vaginal Sertaconazole.
• Clinical Reviews: Emphasize the convenience and high compliance associated with single-dose vaginal antifungals like Sertaconazole.
• Bangladesh (Medex.com.bd):
• Available in 300 mg vaginal ovule form under several brands including Sertovag, Vaginil-S, etc.

• Temperature: Store at below 25°C (77°F)
• Humidity: Store in a dry place, protect from moisture
• Light Protection: Keep away from direct sunlight
• Handling Instructions:
• Do not refrigerate or freeze
• Keep the ovule in its original packaging until use
• Use immediately after opening the blister
• Reconstitution: Not applicable