sulconazole

Action and Spectrum

Actions and Spectrum: 

sulconazole is an antifungal medication used topically to treat various fungal skin infections. It belongs to the class of drugs known as imidazole antifungals.  

Mechanism of Action: 

• Inhibition of Ergosterol Synthesis: Fungal cell membranes contain ergosterol, a critical component that maintains the integrity and fluidity of the membrane. sulconazole works by inhibiting lanosterol 14α-demethylase, which synthesizes ergosterol from lanosterol. This inhibition disrupts the synthesis of ergosterol and leads to the accumulation of toxic sterol intermediates, ultimately causing damage to the fungal cell membrane. 
• Cell Membrane Disruption: As the fungal cell membrane becomes compromised due to the lack of ergosterol, it becomes leaky and less structurally stable. This disruption in the membrane’s integrity results in the loss of critical cellular components, electrolytes and ultimately leads to cell death. 

Spectrum of Activity:  

sulconazole has a relatively broad spectrum of activity against various fungal species, particularly those that cause superficial fungal infections of the skin. Its activity is primarily targeted at dermatophytes, which are fungi that commonly cause skin, hair, and nail infections. It’s also effective against some yeast and mold species. The specific organisms that sulconazole can target include: 

• Dermatophytes: Such as Trichophyton species, Microsporum species, and Epidermophyton species. 
• Yeast: Candida species, including some strains of Candida albicans. 
• Other Fungi: Some strains of Malassezia furfur are associated with conditions like pityriasis versicolor (a type of yeast infection that affects the skin). 

Drug Interaction

Adverse Reaction

Frequency defined 

1-10% 

Erythema 

Irritation 

Pruritus 

Burning 

Stinging/tingling 

Black Box Warning

Black box warning: 

None 

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

• Hypersensitivity or Allergy: Individuals with known hypersensitivity or allergic reactions to sulconazole or its components should not use this medication. 
• Open Wounds or Broken Skin: sulconazole is intended for use on intact skin. Applying it to open wounds, broken skin, or severely damaged skin areas could lead to increased medication absorption and may result in adverse effects. 
• Eye and Mucous Membranes: sulconazole is formulated for topical use on the skin and should not be applied to the eyes, mouth, nose, or other mucous membranes.  

Caution: 

• Allergic Reactions: While allergic reactions to sulconazole are rare, individuals with a history of hypersensitivity or allergic reactions to other antifungal medications or components of sulconazole should exercise caution and consider alternative treatments. 

Pregnancy / Lactation

Pregnancy consideration: In animal reproductive experiments using oral administration of high dosages, adverse effects have been noted. 

Pregnancy Category: C 

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: 

sulconazole inhibits the enzyme lanosterol 14α-demethylase, which synthesizes ergosterol, a key component of fungal cell membranes. This inhibition disrupts fungal cell membrane integrity, increasing permeability and ultimately inhibiting fungal growth. 

Pharmacodynamics:  

• Broad Spectrum Activity: sulconazole’s inhibitory effects extend to dermatophytes, yeasts, filamentous fungi, and dimorphic fungi. This wide range of activity makes it suitable for treating various fungal infections. 
• RIF Measurement: The relative inhibition factor (RIF) serves to quantify the inhibitory activity of antifungal drugs. sulconazole’s RIF values against pathogenic yeasts and Aspergilli were comparable to other imidazole antifungals. 
• Concentration-Dependent Fungicidal Potency: sulconazole’s effectiveness as a fungicide depends on its concentration and the growth phase of the fungal cells. This suggests that higher concentrations of sulconazole and specific growth conditions influence its ability to kill fungal cells. 
• Antibacterial Properties: Besides its antifungal effects, sulconazole has exhibited antibacterial properties in vitro. It has demonstrated inhibitory concentrations (MICs) below 12.5 mg/L against various Staphylococcus species, Streptococcus faecalis, and Gram-positive anaerobic bacteria.

Pharmacokinetics: 

Absorption 

The absorption of sulconazole through the skin is estimated to be within the range of 8.7% to 11.3% of the administered dose. The absorbed drug can then circulate through the body and affect fungal infections. 

Distribution 

Since it is used topically, the systemic distribution is limited compared to drugs taken orally or intravenously. 

Metabolism 

sulconazole might undergo some degree of metabolism in the body. 

Elimination and Excretion 

sulconazole is eliminated from the body through excretion processes. About 6.7% of the drug is excreted in the urine, and approximately 2% is eliminated in feces. A portion of the drug is processed by the kidneys and excreted in the urine, while a smaller portion is eliminated through the gastrointestinal tract. 

Adminstartion

Administration: 

Topical administration 

Only for external usage; keep away from the eyes. Apply a tiny quantity, then gently massage it into the afflicted region and any nearby skin. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: sulconazole 

Why do we use sulconazole? 

sulconazole is a topical antifungal medication for various fungal skin infections. It is applied directly to the affected skin area to help eliminate the fungal infection. Here are the primary uses of sulconazole: 

• Dermatophyte Infections: It is effective in treating infections caused by dermatophyte fungi, which commonly lead to conditions like ringworm (tinea corporis), jock itch (tinea cruris), and athlete’s foot (tinea pedis). These infections affect different body areas, including the skin, groin, and feet. 
• Yeast Infections: It is also used to treat infections caused by certain yeast species, such as Candida. It can be applied to areas affected by yeast infections, helping to alleviate symptoms and eliminate the underlying fungal overgrowth. 
• Pityriasis Versicolor: It can treat pityriasis versicolor, a superficial fungal infection that affects the skin and is caused by the yeast Malassezia furfur. This condition often leads to discolored patches on the skin.