sertaconazole

Action and Spectrum

Actions and Spectrum: 

The primary mechanism of action of sertaconazole involves inhibiting the synthesis of ergosterol, a key component of fungal cell membranes. Ergosterol is essential for maintaining the integrity and fluidity of the fungal cell membrane. sertaconazole achieves its antifungal effects through the following steps: 

• Inhibition of 14α-Demethylase: sertaconazole targets an enzyme called 14α-demethylase, which is involved in ergosterol biosynthesis. This enzyme is necessary for converting lanosterol into ergosterol in fungal cells. 
• Disruption of Membrane Integrity: By inhibiting 14α-demethylase, sertaconazole reduces the production of ergosterol in fungal cells. This disruption leads to the accumulation of toxic sterol intermediates and decreased ergosterol levels within the cell membrane. 
• Increased Membrane Permeability: The fungal cell membrane becomes less stable and more porous due to decreased ergosterol levels. This increased permeability affects various cellular processes and can lead to leakage of cellular contents, impaired transport, and eventual cell death. 

By targeting the synthesis of ergosterol and compromising fungal cell membrane integrity, sertaconazole effectively inhibits the growth and viability of fungal cells, leading to the resolution of fungal infections. 

Spectrum of Activity: sertaconazole has a broad spectrum of antifungal activity, making it effective against various fungal species that cause superficial skin infections.

Drug Interaction

Adverse Reaction

Frequency not defined 

Dry skin 

Erythema 

Desquamation 

Contact dermatitis 

Burning 

Vesiculation 

Hyperpigmentation 

Black Box Warning

Black box warning: 

None 

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

• Hypersensitivity or Allergy: Individuals with known hypersensitivity or allergy to sertaconazole or its components should not use sertaconazole products. 
• Open Wounds or Broken Skin: sertaconazole should not be applied to open wounds, broken skin, or areas with significant skin irritation. It’s essential to ensure the skin is intact before using the medication. 
• Eye and Mucous Membrane Contact: sertaconazole topical products are meant for external use only and should not come into contact with the eyes or mucous membranes. If accidental contact occurs, rinse thoroughly with water. 

Caution: 

• Allergic Reactions: Individuals known to be hypersensitive or allergic to sertaconazole or any of its components should avoid using sertaconazole-containing products. 
• Contact with Eyes and Mucous Membranes: sertaconazole topical products are meant for external use only and should not come into contact with the eyes, mouth, nose, or other mucous membranes. If accidental contact occurs, rinse thoroughly with water. 
• Skin Sensitivity and Irritation: Some individuals may experience skin sensitivity, redness, itching, or irritation due to using sertaconazole products. If you notice any signs of skin irritation or an allergic reaction, discontinue use and consult a healthcare provider. 

Pregnancy / Lactation

Pregnancy consideration: Insufficient data available 

Lactation: Excretion of the drug in human breast milk is unknown 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

sertaconazole exerts its antifungal effects primarily by inhibiting the synthesis of ergosterol, a key component of fungal cell membranes. sertaconazole’s mechanism of action involves the inhibition of the enzyme 14α-demethylase, which is responsible for converting lanosterol into ergosterol in fungal cells. By inhibiting this enzyme, sertaconazole disrupts ergosterol synthesis, leading to alterations in fungal cell membrane composition and increased membrane permeability. This disruption ultimately impairs vital cellular processes and leads to fungal cell death. 

Pharmacokinetics: 

Absorption 

sertaconazole is absorbed through the skin after topical application. Absorption levels are generally low due to their localized use. 

Distribution 

sertaconazole remains primarily at the application site and does not significantly distribute to systemic circulation or other tissues. 

Metabolism 

The metabolism of sertaconazole after topical application is minimal, reducing the potential for significant metabolic interactions. 

Elimination and Excretion 

Any absorbed sertaconazole is likely excreted through urine and feces, but the overall excretion is limited due to the low systemic absorption. 

Adminstartion

Administration: 

Topical administration 

• Apply a thin layer of the sertaconazole cream, lotion, or solution to the affected area. 
• Gently massage or spread the product until evenly distributed over the affected skin. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: sertaconazole 

Why do we use sertaconazole? 

sertaconazole is an antifungal medication used topically to treat various fungal skin infections. It is effective against various fungal species that can cause these infections. Here are some common uses of sertaconazole topical products: 

• Tinea Infections: sertaconazole is used to treat tinea infections, known as ringworm infections. Dermatophyte fungi cause these infections and can affect different areas of the body, such as the skin (tinea corporis), feet (tinea pedis or athlete’s foot), groin (tinea cruris or jock itch), and nails (tinea unguium or onychomycosis). 
• Candida Infections: sertaconazole is effective against Candida species, yeast-like fungi that can cause skin and mucous membranes infections. It treats conditions such as cutaneous candidiasis (skin yeast infections) and intertrigo (a rash that occurs in skin folds). 
• Pityriasis Versicolor (Tinea Versicolor): sertaconazole treats pityriasis versicolor, a fungal infection caused by Malassezia species. This condition leads to discolored patches on the skin, commonly on the chest, back, and shoulders. 
• Superficial Fungal Infections: sertaconazole can treat other superficial fungal infections caused by susceptible fungi that affect the skin. 
• Relief of Symptoms: In addition to treating the underlying fungal infection, sertaconazole can relieve symptoms such as itching, redness, inflammation, and discomfort associated with these infections.