Griseofulvin

• Introduction 

• Illustrated mechanism of action 

• Examples of Medication Brand Names (with Images)

• Indication

• Side Effects 

• Precautions & Contraindications 

• Monographs

• Reference 

Introduction

Griseofulvin is one of the oldest oral antifungal agents, primarily used to treat superficial fungal infections involving the skin, hair, and nails, especially those caused by

dermatophytes such as Trichophyton, Microsporum, and Epidermophyton species. It was first discovered in the 1930s and introduced for clinical use in the 1950s. Despite the emergence of newer antifungal agents, Griseofulvin continues to be used due to its unique mechanism of action and effectiveness in specific cases.

It works by disrupting the mitotic spindle in fungal cells, thereby inhibiting cell division. Griseofulvin also binds to keratin precursor cells in human tissues, making newly formed keratin resistant to fungal invasion. This means it must be taken for several weeks or even months to allow healthy, fungus-free skin, hair, or nails to grow out.

While effective, it has limitations such as a narrow spectrum of activity slow onset of action, and the need for long treatment durations، It is generally reserved for cases where topical antifungals have failed or where the infection is extensive or involves hair and nails.

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Indications of Griseofulvin:

Griseofulvin is indicated for the treatment of dermatophytic infections (tinea infections) of the skin, hair, and nails that are caused by susceptible species of dermatophytes, particularly when topical therapy is ineffective or impractical. These include:

1. Tinea corporis – ringworm of the body 

2. Tinea capitis – scalp ringworm 

3. Tinea cruris – jock itch 

4. Tinea pedis – athlete’s foot 

5. Tinea unguium (onychomycosis) – fungal infection of the nails 

6. Tinea barbae – fungal infection of the beard area 

Note: Griseofulvin is not effective against Candida (yeast) infections or deep/systemic fungal infections. It’s also typically used only when oral therapy is needed, such as in widespread or stubborn infections, or those involving hair and nails. 

Side Effects of Griseofulvin:

Griseofulvin is generally well tolerated, but like all medications, it can cause side effects. These may range from mild to serious and include:

Common side effects:

- Headache (most frequent)

- Nausea or vomiting

- Diarrhea

- Dizziness or fatigue

- Skin rash or itching

- Photosensitivity (increased sensitivity to sunlight)

Less common or rare side effects:

- Hepatotoxicity (liver toxicity)

- Proteinuria or leukopenia (in rare cases)

- Mental confusion or insomnia

- Peripheral neuropathy (nerve problems)

- Stevens-Johnson syndrome (very rare but serious skin reaction)

Important warnings:

- Griseofulvin can cause liver enzyme abnormalities, so liver function should be monitored during prolonged use.

- It may reduce the effectiveness of oral contraceptives—additional contraceptive methods are advised.

- It should be used with caution in patients with liver disease, porphyria, or systemic lupus erythematosus (SLE).

Precautions and Contraindications of Griseofulvin:

 Precautions:

1. Liver Function:

   - Use with caution in patients with liver impairment; monitor liver enzymes during long-term therapy.

2. Photosensitivity:

   - Patients should avoid excessive sun exposure and use sunscreen due to the risk of photosensitivity reactions.

3. Pregnancy and Contraception:

   - Not recommended in pregnancy (Category X) due to teratogenic effects.

   - Women of childbearing age should use effective contraception during treatment and for at least 1 month after stopping.

   - Men should avoid fathering a child during therapy and for 6 months after due to potential sperm effects.

4. Alcohol Use:

   - Concomitant use with alcohol may trigger a disulfiram-like reaction (flushing, headache, nausea, vomiting).

5. Children:

   - Generally safe in children but should be used with caution and appropriate dosing.

6. Drug Interactions:

   - Can reduce the effectiveness of oral contraceptives and warfarin.

   - May interact with barbiturates and other enzyme-inducing drugs.

-Contraindications:

1. Known hypersensitivity to griseofulvin or any of its components.

2. Severe liver disease

3. Porphyria

4. Systemic lupus erythematosus (SLE)

5. Pregnancy9

6. Use in breastfeeding is generally avoided unless the benefits clearly outweigh the risks.

Reference

https://www.medscape.com/

https://www.drugs.com/griseofulvin.html

https://www.drugs.com/griseofulvin.htmlhttps://www.drugs.com/griseofulvin.html

https://www.medscape.com/druginfo/griseofulvin

https://www.rxlist.com/consumer_griseofulvin/drugs-condition.htm

https://pubchem.ncbi.nlm.nih.gov/compound/Griseofulvin

https://www.who.int/publications/i/item/WHO-MHP-HPS-EML-2023.02