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Antiseptics, antibiotics and chemotherapy
Published in Michael J. O’Dowd, The History of Medications for Women, 2020
Griseofulvin was discovered by Raistrick and his colleagues in 1939 in an isolate of Penicillium griseofulvum. Griseofulvin was first used to treat fungal disease in plants and it was not until 1958 that it was employed in the treatment of animal and human mycoses.
Antifungal Drugs and Susceptibility Testing of Fungi
Published in Rossana de Aguiar Cordeiro, Pocket Guide to Mycological Diagnosis, 2019
Débora de Souza Colares Maia Castelo-Branco, Glaucia Morgana de Melo Guedes, Marcos Fábio Gadelha Rocha
Griseofulvin, a metabolic product of Penicillium griseofulvum, prevents fungal growth by binding to microtubular proteins, which leads to the disruption of the spindle apparatus, thus inhibiting fungal cell mitosis. This compound was the first oral agent available for the treatment of dermatomycoses and is only used for noninvasive dermatophyte infections, because the drug concentrates in keratinocytes (Table 2.1).
Topical Products Applied to the Nail
Published in Heather A.E. Benson, Michael S. Roberts, Vânia Rodrigues Leite-Silva, Kenneth A. Walters, Cosmetic Formulation, 2019
Apoorva Panda, Avadhesh Kushwaha, H.N. Shivakumar, S. Narasimha Murthy
Griseofulvin is fungistatic in nature and is unable to show its fungicidal activity at higher concentrations. It is occasionally used in the treatment of ungual infections, as it is effective against dermatophytes. The recommended oral dose of griseofulvin is 500 mg per day for 6–9 months for the infection in the fingernail and for a time period of 12–18 months for the infection in the toe nail. The common side effects observed with griseofulvin include urticaria, erythema multiforme, headache, hepatotoxicity and photosensitivity (Kushwaha et al., 2015 ; Roberts et al., 2003).
Treatment of cutaneous lichen planus (part 2): a review of systemic therapies
Published in Journal of Dermatological Treatment, 2019
Yasmeen Thandar, Rivesh Maharajh, Firoza Haffejee, Anisa Mosam
In patients who have demonstrate no response to first-line treatment such as the systemic corticosteroids and methotrexate, low-molecular-weight heparins may alternatively be considered as a treatment option. Amongst the immunomodulatory drugs, sulphasalazine can be considered as a moderate choice of treatment for generalized CLP, whereas thalidomide should be used with caution and warrants further investigation. Antifungal drugs such as griseofulvin have produced variable results and remains an ‘add-on’ treatment. Hydroxychloroquine has demonstrated superiority to griseofulvin and maybe useful in the clinical distinct actinic subtype of CLP. Antibiotics like metronidazole and dapsone should not be considered as an early treatment choice for CLP as more superior treatment options exists.
Nanotechnological interventions in dermatophytosis: from oral to topical, a fresh perspective
Published in Expert Opinion on Drug Delivery, 2019
Riya Bangia, Gajanand Sharma, Sunil Dogra, Om Prakash Katare
Griseofulvin is a drug that has activity only against dermatophytes. This antifungal drug is generally considered the drug of choice for treating tinea capitis, especially Microsporum species. The mechanism of action of griseofulvin involves interference with the structure as well as function of microtubules and inhibiting cell division (Figure 1). Griseofulvin is majorly delivered to the skin through sweat and the antifungal binds to it weakly. Griseofulvin diffuses to some extent through the basal layer [47]. Griseofulvin is recommended to be administered continuously until the cure is obtained as the tissue levels in skin corresponds to the fall in plasma levels after discontinuing the antifungal agent. In the cases of chronic superficial mycotic infections and onychomycosis, failures in therapy and development of resistance to the medication are usually reported. The cure rates can be improved significantly by administering higher dosages, above 500 mg/day. Serious side effects are witnessed rarely [48]. A comparative study was conducted by Faergemann et al. for activity against tinea corporis or tinea cruris, between 150 mg fluconazole weekly administration and 500 mg griseofulvin daily administration for 4–6 weeks, in a double-blind trial. Their findings demonstrated that fluconazole and griseofulvin were effective with mycological cure rates of 78% and 80%, respectively [49]. Another study carried out by Cole et al. in 50 patients with tinea corporis depicted the cure rate of 87% with terbinafine, in comparison with that of 73% with griseofulvin [50].
Nano- and microcrystals of griseofulvin subcutaneously administered to rats resulted in improved bioavailability and sustained release
Published in Drug Development and Industrial Pharmacy, 2019
Kalle Sigfridsson, Hanna Rydberg, Marie Strimfors
In this study we investigate s.c. delivery of griseofulvin, an uncharged compound in the physiological interval with a solubility of approximately 40 µM. Griseofulvin, introduced in 1958 [25], is a widely used oral antifungal agent for the treatment of dermatophytic infections. The absorption of this drug has been the subject of extensive interest; however, the reported data after oral administration have been confusing and the interpretation not straight forward. For example, Davis et al. showed that 30–64% of an oral dose was found in the feces of the rats to which the drug was administered [26]. In another study, Rowland et al. found that the absorption in man occurred up to 30 h after administration and that 27–72% of the administered dose was absorbed [27]. Different approaches have been tried to increase the absorption, including particle size reduction, concomitant administration of fat and different kinds of polyethylene glycol, but only minor changes in bioavailability have been demonstrated and there is still a significant variation between individuals [28–30]. In this work, griseofulvin was used as a model compound for s.c. injection of a BCS II drug (low solubility, high permeability [31]) at two different doses, using two different formulations of various particle sizes. Furthermore, the griseofulvin was administered p.o. and intravenously (i.v.) to calculate the bioavailability for griseofulvin after both p.o. and s.c. administration. An additional aim with the s.c. injection was to develop an extended release formulation, as well as an administration route, that aimed to achieve a general therapeutic level of approximately 1 µM over 48 h or above with only minor variability between individuals.