Griseofulvin is a well-known antifungal medication primarily used to treat infections caused by dermatophytes, including ringworm, athlete's foot, and jock itch. It works by interfering with fungal cell division and preventing the fungus from growing and reproducing. Griseofulvin was derived from the mold Penicillium griseofulvum, making it one of the earliest natural antifungal agents introduced in clinical use.
Griseofulvin appears as an odorless, tasteless, and appears creamy coloured crystalline powder. It is insolluble in water and slightly solluble in organic solvents like aceton, benzene, methanol etc. Griseofulvin is classified chemically as a Spiro compound and exhibit a complex structure that contributes to its anti fungal properties.The molecular weight of griseofulvin is 352.8 gm/mol. The drug is marketed under various brand names, including Fulvicin, Fulcine, Griseofulvinum, Spirofulvin, Grizeofulvin, Likuden, Murfulvin, Grisetin, Biogrisin-FP, Amudane, etc.
Chemical structure of Griseofulvin:-
- The molecular formula of griseofulvin is, [C17H17ClO6].
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| Chemical Structure of griseofulvin |
- The IUPAC name of griseofulvin, (2S,5'R)-7-chloro-3',4,6-trimethoxy-5'-methylspiro[1-benzofuran-2,4'-cyclohex-2-ene]-1',3-dione.
Mechanism of action of Griseofulvin:-
griseofulvin exerts its antifungal effects through a multiple faceted mechanism, targeting fungal cell division and structural integrity. It is classified as a fungistatic agent, meaning it inhibits the growth and reproduction of fungi rather than killing them outright. Griseofulvin is particularly effective against dermatophytes such as Trichophyton, Microsporum, and Epidermophyton species. Key steps in its action are:
- Disruption of Microtubule Function: Griseofulvin binds to tubulin proteins in fungal cells, especially in the alpha and beta subunits of microtubules. This structures are essential for mitosis, the process of nuclear division. By interfering with spindle formation, griseofulvin halts metaphase progression, preventing fungal cell division.
- Inhibition of mitosis: The disruption of the miotic spindle result in arrested fungal cell replication, making the fungus unable to reproduce and spread, which gradually leads to its elimination when infected keratin is shed.
- Keratin binding: Griseofulvin binds to keratin precursor cells in the epidermis, nails, and hair. This binding creates a fungus resistant barrier, ensuring that newly formed keratin is protected from reinfection. As the body naturally replace infected tissue, the fungus loses its environment and dies off.
- Cytoplasmic and Nucleic acid disruption: It may also interfere with nucleic acid synthesis and cytoplasmic microtubule function, further impairing fungal cellular processes.
This unique combination of targeting mitosis and keratin protection makes griseofulvin effective in treating chronic dermatophytosis especially in scalp and nail infections.
Medical Uses of Griseofulvin:-
Griseofulvin is mainly prescribed for chronic and server dermatophytic infections that do not respond to topical agents. It is a first line oral antifungal for children and is frequently used when patients have widespread or recalcitrant infections.
Treated conditions are,
- Tinea capitis (scalp ringworm)
- Tinea corporis (body ringworm)
- Tinea pedis (athletes foot)
- Tinea cruris (joke itch)
- Tinea unguium/Onychomycosis (nail fungus, through newer options are preferred)
Common Side-effects of Griseofulvin:-
like all medicines, griseofulvin may cause side effects, particularly if taken in high dose or for extended periods. Some of the most commonly reported adverse effects include:
- Gastrointestinal issues: Nausea, vomiting, diarrhea, and loss of appetite
- Central nervous system effects: Dizziness, headache, fatigue, and insomnia
- Dermatological reactions: Skin rashes, itching, hives, and photosensitivity
- Liver complications: Jaundice and dark urine may indicate liver damage
- Hypersensitivity: Allergic reactions, including swelling and skin pain
Precautions and Warnings:-
- Pregnancy and breastfeeding: Griseofulvin Contraindicated in pregnancy due to potential teratogenic effects. Women of childbearing age should use effective contraception during and after treatment.
- liver diseases: Use cautiously in patients with pre existing liver conditions.
- Alcohol Consumption: Avoid alcohol while taking griseofulvin, as it may increase the risk of liver toxicity.
Conclusion:-
Griseofulvin remains valuable oral antifungal drug for treating superficial fungal infections, particularly when topical treatments fail or the infection is widespread. With its unique mechanism of disrupting fungal mitosis and strong affinity for keratinized tissue, it ensure long term clearance of stubborn dermatophyte infections. However, due to the potential for side effects and drug interactions, it should be used under medical supervision with proper dosage and duration.
If you are experiencing presistant fungal infections affecting your skin, hair, or nails, consult a healthcare professional to see if griseofulvin might be the right treatment option for you.
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