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Griseofulvin

Griseofulvin: A Timeless Antifungal Agent in Dermatological Therapy

Introduction

Fungal infections of the skin, hair, and nails—collectively known as dermatophytoses—affect millions globally. These infections, while not typically life-threatening, cause discomfort, cosmetic concerns, and sometimes social stigma. Over the decades, Griseofulvin has remained a reliable oral antifungal treatment for such superficial infections. Although newer antifungal drugs have emerged, Griseofulvin continues to be a cornerstone in dermatology, especially in resource-limited settings.

Griseofulvin

Griseofulvin is an oral antifungal antibiotic derived from the mold Penicillium griseofulvum. It has been used for decades to treat dermatophyte infections, particularly those unresponsive to topical therapies.

Key Facts:

  • Class: Antifungal antibiotic

  • Route of Administration: Oral (tablet, suspension)

  • First Introduced: 1959

  • Mechanism: Fungistatic (inhibits fungal growth)

Mechanism of Action

Griseofulvin exhibits its antifungal effects by:

  • Binding to fungal microtubules, interfering with mitosis and nuclear division

  • Depositing in keratin precursor cells, making the newly formed keratin resistant to fungal invasion

This action doesn't kill fungi outright but prevents their replication, allowing infected skin, hair, or nails to shed and be replaced by healthy, fungus-free tissue over time.

Spectrum of Activity

Griseofulvin is primarily effective against dermatophytes, including:

  • Trichophyton spp.

  • Microsporum spp.

  • Epidermophyton floccosum

It is not effective against:

  • Candida species

  • Malassezia

  • Non-dermatophyte molds

Clinical Indications

Griseofulvin is used when topical antifungals fail or when infections are widespread, chronic, or involve hair and nails.

1. Tinea Capitis (Scalp Ringworm)

  • Most common indication in children

  • Topicals can't penetrate the hair shaft, making oral therapy necessary

2. Tinea Corporis (Body Ringworm) and Tinea Cruris (Jock Itch)

  • Oral Griseofulvin is used for extensive or resistant infections

3. Tinea Pedis (Athlete’s Foot) and Tinea Manuum

  • Especially for moccasin-type infections that resist topicals

4. Tinea Unguium (Onychomycosis)

  • Effective in nail infections, though newer drugs like terbinafine are now preferred

Formulations and Dosage

Griseofulvin is available in:

  • Microsize formulations (125 mg, 250 mg tablets)

  • Ultramicrosize formulations (higher bioavailability, 125 mg, 250 mg)

Typical Dosages:

  • Microsize:

    • Adults: 500–1000 mg/day in divided doses

    • Children: 10–20 mg/kg/day

  • Ultramicrosize:

    • Adults: 330–660 mg/day

    • Children: 5–15 mg/kg/day

Administration Tips:

  • Best absorbed when taken with fatty meals

  • Duration depends on the site of infection:

    • Skin: 2–4 weeks

    • Scalp: 4–6 weeks

    • Nails: 6–12 months

Pharmacokinetics

  • Absorption: Incomplete; improved with high-fat meals

  • Metabolism: Hepatic (induces CYP450 enzymes)

  • Excretion: Urine and feces

  • Half-life: 9–24 hours (allows once-daily dosing)

Because it accumulates in keratin, Griseofulvin continues to act even after treatment is stopped, particularly useful in nail and scalp infections.

Efficacy and Clinical Outcomes

Numerous studies affirm Griseofulvin’s efficacy, particularly in:

  • Pediatric tinea capitis (still a first-line treatment)

  • Onychomycosis, when used long-term

  • Chronic dermatophytosis, particularly in tropical climates

However, its longer treatment durations, drug interactions, and lower cure rates compared to newer antifungals like terbinafine and itraconazole have somewhat limited its use.

Adverse Effects and Safety Profile

Griseofulvin is generally safe but has some side effects, especially with long-term use.

Common Side Effects:

  • Headache

  • Nausea

  • Diarrhea

  • Photosensitivity

  • Fatigue

Serious Side Effects:

  • Hepatotoxicity

  • Leukopenia (rare)

  • Proteinuria

  • Stevens-Johnson Syndrome (very rare)

Monitoring:

  • Liver function tests recommended for prolonged therapy

  • Complete blood count if therapy exceeds 6 weeks

Drug Interactions

Griseofulvin is a CYP450 inducer, leading to several potential interactions:

  • Decreases efficacy of: Oral contraceptives, warfarin, cyclosporine

  • Enhanced metabolism of: Barbiturates, alcohol

  • Avoid alcohol: May cause disulfiram-like reaction

Use in Special Populations

Pediatrics:

  • Widely used for tinea capitis

  • Generally well tolerated

Pregnancy:

  • Contraindicated (teratogenic effects in animals)

  • Avoid use in women who may become pregnant during and for at least one month post-therapy

Lactation:

  • Excreted in breast milk; use with caution

Geriatrics:

  • Safe when monitored, but consider hepatic function and polypharmacy risks

Griseofulvin vs. Newer Antifungals

Feature Griseofulvin Terbinafine Itraconazole
Fungistatic or cidal Fungistatic Fungicidal Fungistatic
Duration Long Shorter Moderate
Cost Low Moderate Moderate
Cure rate (nails) ~50–60% ~70–80% ~60–70%
CYP interactions High (induces) Low Moderate (inhibits)

While Griseofulvin is less effective for onychomycosis, it remains preferable in scalp infections, especially in children.

Emerging Resistance

Dermatophyte resistance to Griseofulvin is relatively rare but increasing, particularly in parts of India and Southeast Asia. Causes include:

  • Inappropriate use (subtherapeutic doses or short durations)

  • Self-medication

  • OTC availability

This highlights the need for correct diagnosis, appropriate dosing, and patient adherence.

Practical Tips for Patients

  1. Complete the full course, even if symptoms improve early.

  2. Take it with milk or a fatty meal for better absorption.

  3. Avoid sun exposure; use sunscreen or protective clothing.

  4. Do not consume alcohol during therapy.

  5. Inform your doctor if you're on hormonal contraceptives—use backup contraception.

Griseofulvin in Veterinary Medicine

Interestingly, Griseofulvin is also used in animals—particularly cats and dogs—for fungal infections like ringworm, showcasing its broad utility across species.

Cost and Accessibility

Griseofulvin is one of the most affordable oral antifungals, making it indispensable in:

  • Public health settings

  • Developing countries

  • Mass treatment programs for scalp ringworm in schools

Conclusion

Griseofulvin, despite its age, remains a trusted antifungal in dermatology. Its effectiveness in treating tinea capitis and its affordability ensure continued use in both high- and low-resource settings. While newer drugs may offer faster cures and better safety profiles, Griseofulvin holds its place as a veteran agent with time-tested reliability. As we confront rising cases of dermatophytosis—some chronic and resistant—Griseofulvin will continue to serve as an essential component of antifungal therapy, provided it is used judiciously and with adherence to proper protocols.