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Monographs of Topical Drugs that Have Caused Contact Allergy/Allergic Contact Dermatitis
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Clotrimazole is a synthetic imidazole derivative with a broad spectrum of antimycotic activity. Topical clotrimazole preparations are indicated for the treatment of superficial fungal infections caused by dermatophytes or Candida albicans (including diaper rash and candidiasis vaginalis), and for treating pityriasis versicolor. The oral preparation of clotrimazole (troche, slowly dissolving tablets) is indicated for the local treatment of oropharyngeal candidiasis, and as a prophylactic drug to reduce the incidence of oropharyngeal candidiasis in patients immunocompromised by conditions such as chemotherapy, radiotherapy, or steroid therapy utilized in the treatment of leukemia, solid tumors, or renal transplantation. Troche preparations are not indicated for the treatment of any systemic mycoses. Clotrimazole has also become a drug of interest in treating several other diseases such as sickle cell disease, malaria and some cancers (1).
Pruritus Ani
Published in Peter Sagar, Andrew G. Hill, Charles H. Knowles, Stefan Post, Willem A. Bemelman, Patricia L. Roberts, Susan Galandiuk, John R.T. Monson, Michael R.B. Keighley, Norman S. Williams, Keighley & Williams’ Surgery of the Anus, Rectum and Colon, 2019
Shahab A. Siddiqi, Arifa M. Siddika
Many other TRP channels are involved in itch processing, and the same receptors are involved in regulation of the epidermal barrier. TRP channels partly explain the side effects of some drugs. Clotrimazole produces a burning itch sensation in some patients by activating TRPV1 and TRPA1 and inhibiting TRPM8, an inhibitor of itch. When applied topically, tacrolimus causes an increase in neuropeptide levels and TRPV1 activity, which produces a burning itch in some patients. Epidermal growth factor (EGF), TRPM6, magnesium and itch are all linked, explaining the itch caused by cetuximab, which blocks the EGF receptor. TRPA1 is involved in the itch induced by hydrogen peroxide and the retinoids, whereas stimulation of TRPM8 has an anti-pruritic effect. Menthol is found in many anti-pruritic lotions and activates TRPM8, resulting in a small subjective anti-pruritic effect. This limited effect is explained by the fact that menthol also activates TRPV3 and TRPA1, which are pruritic. Chloroquine activates TRPA1, may sensitise TRPV1 and indirectly inhibits TRPM8. Despite TRPM8 appearing to be anti-pruritic, the available evidence suggests that targeting this receptor would not have a beneficial effect in the treatment of itch.7 A topical TRPM8 agonist has been reported to help patients suffering from itch associated with vulvar lichen sclerosus, but this finding has yet to be reproduced.
Women's health
Published in Gina Johnson, Ian Hill-Smith, Chirag Bakhai, The Minor Illness Manual, 2018
Gina Johnson, Ian Hill-Smith, Chirag Bakhai
Combination packs of clotrimazole cream and pessary (e.g. Canesten Combi) and clotrimazole cream and fluconazolePCIQ capsule (e.g. Canesten Duo) can be bought over the counter (OTC) more cheaply than through a prescription (as the combination packs entail two prescription charges)
Miconazole for the treatment of vulvovaginal candidiasis. In vitro, in vivo and clinical results. Review of the literature
Published in Journal of Obstetrics and Gynaecology, 2023
Pedro Antonio Regidor, Manopchai Thamkhantho, Chenchit Chayachinda, Santiago Palacios
Optimum regimens for treating recurrent vulvovaginal candidiasis have not been established yet (Brunton 2011). Although each episode caused by C. albicans may respond to usual short-term intravaginal antifungal regimens or a single-dose of oral fluconazole, a more extended initial therapy may be necessary to achieve mycologic remission and chronic maintenance therapy may be required to prevent relapse. The CDC recommends the use of an initial intensive regimen consisting of 7–14 days of an intravaginal azole antifungal or a three-dose regimen of oral fluconazole (100-, 150- or 200 mg dose given every third day for a total of three doses) followed by a maintenance antifungal regimen (issued for six months). The CDC recommends oral fluconazole (100, 150 or 200 mg doses once weekly) for the maintenance regimen. If this oral regimen cannot be used, some clinicians recommend intravaginal clotrimazole (200 mg twice weekly or 500 mg once weekly) or other intravaginal treatments used intermittently. These maintenance regimens can effectively reduce recurrent infections; however, 30–50% of women will have recurrent disease once maintenance therapy is discontinued (Workowski and Bachmann 2022).
Emerging drug targets for sickle cell disease: shedding light on new knowledge and advances at the molecular level
Published in Expert Opinion on Therapeutic Targets, 2023
Gárdos channel and anion conductance inhibitors: The second important pathway is the Gárdos channel which is also found in red cells from normal individuals as well as SCD patients [49]. Usually, the Gárdos channel is quiescent because of low intracellular Ca2+ in red cells due to the high capacity PMCA coupled with a very low passive Ca2+ leak. Activation of Psickle in deoxygenated sickle cells alters this balance so that excess Ca2+ entry mediates a rise in [Ca2+]i and an increase in Gárdos channel activity. Effective inhibitors of the channel include compounds like the scorpion venom charybdotoxin and the antimicrobial clotimazole [51–54]. In clinical trials, prolonged aministration of clotrimazole led to signs of liver toxicity due to the presence of its imidazole group. Derivatives lacking this side group have been developed and ICA-17043/Senicapoc progressed to clinical trials in SCD patients . Senicapoc effectively increased red cell hydration. The end point chosen in these trials, however, was reduction in pain which was not forthcoming [220,221]. If some other indicator of efficacy had been chosen, such as increased Hb levels (as used for voxelotor) or specific tissue damage, the outcome might have been different. Senicapoc is currently being reassessed as possible treatment for hereditary xerocytosis, and continues to be an interesting option in SCD.
Risk of fetal malformation, spontaneous abortion, and adverse pregnancy outcomes after gestational terbinafine exposure: a systematic review
Published in Journal of Dermatological Treatment, 2022
Philipp Foessleitner, Alex Farr, Julia Deinsberger
When a fungal infection is diagnosed during pregnancy, it is important to identify the appropriate antifungal treatment. Topical azoles, including fluconazole, itraconazole, and clotrimazole, are recommended as first-line therapy during pregnancy (21–23). In cases of severe symptoms, recurrence, or when topical therapy fails, oral azoles are recommended in non-pregnant patients (21). However, the safety of oral azoles during pregnancy is controversial. Recent meta-analyses regarding this topic found an increased likelihood of heart and limb malformations and spontaneous abortion after gestational exposure to oral fluconazole (24,25). Additionally, oral itraconazole use during pregnancy was associated with an increased risk of eye defects (25). Furthermore, these agents have the ability to disrupt estrogen and testosterone synthesis, although it remains unclear if fetal corticosteroid synthesis is affected (10). Griseofulvin, another antifungal agent was shown be have teratogenic effects in animals; however, data on humans are limited (26). In light of these findings, terbinafine could offer a safe alternative as antifungal treatment during gestation.