Sertaconazole

Sertaconazole is an Antifungal agent belonging to the pharmacological class of Triazole Antifungals.

Sertaconazole has been approved to relieve symptoms and also for the treatment and maintenance of Cutaneous candidiasis, Seborrheic dermatitis, Tinea infections, Diaper dermatitis, candida, Tinea corporis, Tinea pedis.

In a pharmacokinetic trial involving 5 male subjects with interdigital tinea pedis (with a range of diseased area from 42 to 140 cm2 and a mean of 93 cm2), Sertaconazole cream, 2%, was topically applied to the affected skin every 12 hours for a total of 13 doses. The cream contained 0.5 grams of sertaconazole nitrate per 100 cm2. After the thirteenth dose, sertaconazole concentrations in the plasma were measured through serial blood sampling for 72 hours. The analytical method used had a limit of quantitation of 2.5 ng/mL, and the measured sertaconazole concentrations in plasma were found to be below this limit, indicating that the drug's systemic absorption was minimal or undetectable.

The common side effects of Sertaconazole include Burning, Swelling, Tenderness, Discoloration, Irritation, Dry skin.

Sertaconazole is available in the form of Topical cream.

Sertaconazole is approved in Germany, Japan, Malaysia, India, the U.K., the U.S., and China.

Sertaconazole, belonging to the pharmacological class of Triazole Antifungal, acts as an Antifungal agent.

Sertaconazole interacts with 14-α demethylase, which is a cytochrome P-450 enzyme essential for converting lanosterol to ergosterol in fungi. As ergosterol plays a crucial role in the integrity of the fungal cell membrane, inhibiting its synthesis increases cellular permeability, leading to leakage of cellular contents. Additionally, sertaconazole may inhibit endogenous respiration, interact with membrane phospholipids, hinder the transformation of yeasts into mycelial forms, impede purine uptake, and disrupt triglyceride and/or phospholipid biosynthesis.

Sertaconazole has been approved to relieve symptoms and also for the treatment and maintenance of Cutaneous candidiasis, Seborrheic dermatitis, Tinea infections, Diaper dermatitis, candida, Tinea corporis, Tinea pedis.

Sertaconazole is found to be available in the form of Topical cream.

Sertaconazole can be used in the following treatment:

• Cutaneous candidiasis
• Seborrheic dermatitis
• Tinea infections
• Diaper dermatitis, candida
• Tinea corporis
• Tinea pedis

Sertaconazole can help to relieve symptoms and also for the treatment and maintenance of Cutaneous candidiasis, Seborrheic dermatitis, Tinea infections, Diaper dermatitis, candida, Tinea corporis, Tinea pedis.

Sertaconazole is approved for use in the following clinical indications:

• Cutaneous candidiasis
• Seborrheic dermatitis
• Tinea infections
• Diaper dermatitis, candida
• Tinea corporis
• Tinea pedis

Cutaneous Candidiasis

• Topical treatment for cutaneous candidiasis (off-label use):
• Dosage: Apply to affected area(s) twice daily for 4 weeks .

Seborrheic Dermatitis

• Topical treatment for seborrheic dermatitis (off-label use):
• Dosage: Apply to affected area(s) twice daily for 4 weeks .

Tinea Infections

• Topical treatment for Tinea corporis/Tinea cruris (off-label use):
• Dosage: Apply to affected and surrounding area(s) 1 to 2 times daily until clinical resolution, typically 1 to 3 weeks.
• Topical treatment for Tinea pedis (labeled use)/Tinea manuum (off-label use):
• Dosage: Apply to affected and surrounding area(s) twice daily until 1 week after clinical resolution, typically for 4 weeks total .
• Topical treatment for Tinea versicolor (off-label use):
• Dosage: Apply to affected and surrounding area(s) twice daily for 4 week.

Sertaconazole is available in the following dosage forms and strengths:

• Topical cream : 2%

Topical cream.

• Dosage Adjustments in Pediatric Patients:

Diaper Dermatitis, Candida

• Limited Data Available: Infants ≥2 months and Children <2 years
• Cream 2%: Topical
• Dosage: Apply twice daily after a diaper change for 2 weeks
• Study Information: Based on an open-label, noncomparative study (n=27; mean age: 5.7 months; range: 2 to 22 months)
• Results: 88.8% of participants achieved complete cure; 1 patient had increased erythema but continued treatment

Tinea Corporis

• Limited Data Available: Children ≥2 years and Adolescents
• Cream 2%: Topical
• Dosage: Apply once daily for 2 weeks
• Study Information: Based on an open-label study (n=16; ages: 2 to 16 years; 14 patients with tinea corporis)
• Results: Clinical cure was achieved in 75% of patients at 2 weeks and 100% of patients at 4 weeks (2-week post-therapy completion follow-up assessment); no adverse effects were reported

Tinea Pedis

• Children ≥12 years and Adolescents
• Cream 2%: Topical

• Dosage: Apply between toes and to surrounding healthy skin twice daily for 4 weeks.

When taking Sertaconazole, there are certain dietary restrictions that should be followed to ensure the medication's effectiveness and safety:

• There are no specific food warnings associated with the use of Sertaconazole. It is a topical antifungal agent meant for external use on the skin. Since it is not ingested or absorbed systemically, there is generally no interaction with food.

The dietary restriction should be individualized as per patient requirements.

Sertaconazole may be contraindicated under the following conditions:

• Hypersensitivity to the active substance or to any of the excipients.

In the case of local adverse reactions or irritation development, discontinuation of the treatment is recommended, and appropriate therapy should be initiated.

The excretion of sertaconazole in human milk is not established. Since many drugs are excreted in human milk, caution should be exercised when prescribing Sertaconazole cream, 2%, to nursing women.

Pregnancy:

Pregnancy Category C.

It is important to note that there have not been sufficient studies conducted on the effects of Sertaconazole cream during pregnancy. Therefore, it should only be used if the potential benefits outweigh any potential risks to the fetus.

Studies on reproductive effects of Sertaconazole cream have not been conducted, but tests on rats and rabbits showed no signs of harm at an oral dose of 160 mg/kg/day. However, in rats, there was a decrease in live births and an increase in stillborns at doses of 80 and 160 mg/kg/day.

There are certain food-related warnings and precautions to consider when using Sertaconazole:

• There are no specific food warnings associated with the use of Sertaconazole. It is a topical antifungal agent meant for external use on the skin. Since it is not ingested or absorbed systemically, there is generally no interaction with food.

The adverse reactions related to Sertaconazole can be categorized as follows:

Common:

• Skin irritation or burning at the application site
• Itching or redness in the treated area

Less Common:

• Dry skin
• Discoloration of the skin

Rare Side:

• Swelling
• Tenderness

The clinically relevant drug interactions of Sertaconazole is briefly summarized here

• The combination of sertaconazole and nystatin is considered duplication of therapy when both drugs are used through a similar route, and it is typically avoided due to this reason.

The following are the side effects involving Sertaconazole:

• Burning
• Swelling
• Tenderness
• Discoloration
• Irritation
• Dry skin

The use of Sertaconazole should be prudent in the following group of special populations:

Pregnancy:

Pregnancy Category C.

It has not been determined through proper and thorough research whether Sertaconazole cream is safe for pregnant women to use. If a potential benefit outweighs any potential risk to the fetus

, then only should Sertaconazole cream be considered for use during pregnancy. There is no available information on the effects of Sertaconazole cream on reproduction. Sertaconazole nitrate has been shown to not cause any harm to rats and rabbits, even at an oral dose that is 40 to 80 times higher than the maximum recommended human dose, based on body surface area. However, in a study on rats, a decrease in live births and an increase in still-born pups were observed at doses of 80 and 160 mg/kg/day sertaconazole nitrate.

Lactation

The excretion of sertaconazole in human milk is not established. Since many drugs are excreted in human milk, caution should be exercised when prescribing Sertaconazole cream, 2%, to nursing women.

Pediatric

The effectiveness and safety of Sertaconazole cream, 2%, have not been determined in pediatric patients under the age of 12 years.

Geriatric Use

Clinical trials of Sertaconazole cream, 2%, did not enroll an adequate number of subjects aged 65 and older to assess whether their response differs from that of younger subjects.

The physician should be vigilant about the knowledge pertaining to the identification and treatment of overdosage of Sertaconazole.

Information on the specific symptoms and effects of overdosage with sertaconazole is limited. However, in case of accidental ingestion or excessive topical application leading to overdose, it is advised to seek immediate medical attention.

Pharmacodynamics:

Sertaconazole is an antifungal agent of the Triazole/triazole type. It acts as a highly selective inhibitor of fungal cytochrome P-450 sterol C-14 α-demethylation by targeting the enzyme cytochrome P450 14α-demethylase. This enzyme plays a crucial role in converting lanosterol to ergosterol, which is essential for fungal cell wall synthesis. The inhibition of this process results in a reduction of normal sterols and the accumulation of 14 α-methyl sterols in fungi, contributing to the fungistatic activity of sertaconazole. Notably, the inhibitory effect of fluconazole on mammalian cell demethylation is significantly less sensitive compared to its impact on fungi. In vitro, sertaconazole has demonstrated activity against Cryptococcus neoformans and Candida spp. Additionally, it has shown fungistatic activity in both normal and immunocompromised animal models for systemic and intracranial fungal infections caused by Cryptococcus neoformans and for systemic infections resulting from Candida albicans.

Pharmacokinetics:

In a pharmacokinetic trial involving 5 male subjects with interdigital tinea pedis (with a range of diseased area from 42 to 140 cm2 and a mean of 93 cm2), Sertaconazole cream, 2%, was topically applied to the affected skin every 12 hours for a total of 13 doses. The cream contained 0.5 grams of sertaconazole nitrate per 100 cm2. After the thirteenth dose, sertaconazole concentrations in the plasma were measured through serial blood sampling for 72 hours. The analytical method used had a limit of quantitation of 2.5 ng/mL, and the measured sertaconazole concentrations in plasma were found to be below this limit, indicating that the drug's systemic absorption was minimal or undetectable.

1. https://go.drugbank.com/drugs/DB01153
2. https://reference.medscape.com/drug/Sertaconazole-sertaconazole-topical-343491
3. https://www.goodrx.com/Sertaconazole/what-is
4. https://www.rxlist.com/Sertaconazole-drug.htm
5. https://www.drugs.com/mtm/sertaconazole-topical.html