Clotrimazole and clobetasol in the treatment of fungal infections and psoriasisDear Colleagues, this week we will examine together examples of formulations containing two active substances used in the treatment of psoriasis and fungal infections, which are among the most common diseases in Dermatology. Before moving on to the formulas, let us provide brief information about clotrimazole, an antifungal, and clobetasol, a potent corticosteroid.Clotrimazole; is an imidazole derivative with broad-spectrum antimycotic activity. Clotrimazole acts against fungi by inhibiting ergosterol synthesis. Inhibition of ergosterol synthesis leads to structural and functional disruption of the cytoplasmic membrane.
Clotrimazole has broad-spectrum antimycotic activity in vitro and in vivo against dermatophytes, yeasts, molds, etc. Examples of such infections include mycoses of the feet and hands (Athlete’s foot, Tinea manuum), paronychias, mycoses of the skin and skin folds (Tinea corporis, Tinea cruris), superficial candidiasis of the skin (Candida balanitis, Candida vulvitis), Pityriasis versicolor, erythrasma, and seborrheic dermatitis associated with the pathogens mentioned above. Clotrimazole is also used in skin diseases secondarily infected with susceptible bacteria.
In addition to its antimycotic effect, clotrimazole is also effective against Trichomonas vaginalis, Gram-positive microorganisms (Streptococci / Staphylococci), and Gram-negative microorganisms (Bacteroides / Gardnerella vaginalis). Clotrimazole is a white to pale yellow powder. Its solubilities according to the British Pharmacopoeia (BP): Practically insoluble in water; soluble in alcohol and methylene chloride; slightly soluble in ether. Its solubilities according to the United States Pharmacopeia (USP): Practically insoluble in water; freely soluble in acetone, alcohol, chloroform, and methyl alcohol.Clobetasol; is a synthetically fluorinated corticosteroid applied topically. It is used in the treatment of inflammatory and pruritic manifestations of moderate to severe corticosteroid-responsive dermatoses and psoriasis. Clobetasol is the most potent topical corticosteroid and is only used for short-term treatment. Like all topical corticosteroids, clobetasol exhibits anti-inflammatory, antipruritic, and vasoconstrictive effects. In the treatment of allergic conditions, they reduce the allergic responses of certain cell types associated with allergic reactions, such as mast cells and eosinophils. When used long-term, potent topical corticosteroids may cause thinning of the epidermis due to tissue atrophy and decreased collagen formation. When used in sufficient quantities over a prolonged period, they can be absorbed systemically. Therefore, clobetasol, being a very potent topical corticosteroid, can undergo systemic absorption and exhibit pharmacological effects characteristic of systemic glucocorticoids. Clobetasol is applied topically as a cream, gel, ointment, or topical solution. Clobetasol propionate is a cream-to-white crystalline powder. It is practically insoluble in water; slightly soluble in alcohol; soluble in acetone, dimethyl sulfoxide, chloroform, methyl alcohol, and dioxane; and sparingly soluble in ether.
A formula used for fungal skin infections in the Serbian National Formulary;Clotrimazole solution 1%
Formula:
Rp.
Clotrimazole 1 g
Ethanol 96% 50 g
Propylene glycol 10 g
Distilled water q.s. ad. 100 g
Preparation of the formula:Clotrimazole is dissolved in ethanol with stirring. Propylene glycol and distilled water are added, and the solution is filtered through filter paper. It should be stored in tightly closed amber glass or plastic dropper bottles below 25°C, protected from light. It is used for fungal skin infections.If we examine a formula used in the treatment of seborrheic dermatitis published in ACTAS, the official journal of the Spanish Academy of Dermatology and Venereology;
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Rp.
Clotrimazole 1%
Hydrocortisone 1%
Cream gel csp 40 gCream gels are vehicle emulsions used in the treatment of conditions affecting the facial skin (such as rosacea, seborrheic dermatitis, and perioral dermatitis). Corticosteroids, antibiotics, calcineurin inhibitors, and many other active pharmaceutical ingredients are suitable for these vehicles. They are cosmetically favorable vehicles as they leave a less greasy feel on the skin.Other formulas used in the treatment of psoriasis and fungal infections of the nails and scalp, also published in ACTAS, the official journal of the Spanish Academy of Dermatology and Venereology;
A formula used in the treatment of nail psoriasis;
Rp.
Clobetasol 8%
Salicylic acid 3%
Nail lacquer csp 20 mlNail lacquers are polymer-structured alcohol-containing bases with strong solvent properties and a volatile component. They can contain significant concentrations of active ingredients. As the solvent evaporates, a film layer with a high concentration of the active ingredient remains on the nail. Consecutive applications can achieve adequate therapeutic concentrations in the nail bed and nail matrix. Antifungal nail lacquers have been adapted to treat onychomycosis, psoriasis, lichen planus, and similar conditions.A formula used in the treatment of nail fungus;
Rp.
Clotrimazole 6%
Nail lacquer csp 20 ml
A formula used for scalp psoriasis;
Rp.
Clobetasol 0.05%
Clotrimazole 1%
Salicylic acid 3%
Hair oil csp 100 mlThe advantages of hair oils in treatment have been proven. These products are traditional oily bases containing high-quality cosmetic lipids and volatile silicones; they penetrate the skin within a few minutes after application, and the oily appearance on the scalp disappears. However, we must keep in mind as a disadvantage of these oils on the scalp that some active ingredients cannot dissolve in them.A formula used for ear canal eczema;
Rp.
Tacrolimus 0.03%
Clotrimazole 1%
Ear oil csp 40 mlOils are more effective than emulsions in reaching the inner parts of the ear in ear medication applications.Other formulas used in the treatment of psoriasis;
A formula used in the treatment of nail psoriasis;
Rp.
Clobetasol propionate 8%
Clotrimazole 2%
Nail lacquer csp. 10 ml
A formula used in the treatment of scalp psoriasis;
Rp.
Clobetasol propionate 0.05%
Betamethasone valerate 0.1%
Clotrimazole 1%
Salicylic acid 2%
Hair oil csp. 100 ml
Formula used in the treatment of external ear canal psoriasis;
Rp.
Betamethasone valerate 0.1%
Clotrimazole 1%
Ichthyol 1%
Ear oil csp. 20 ml
Finally, a Clotrimazole-containing formula for co-occurring acne and seborrheic dermatitis;
Rp.
Erythromycin 2%
Clotrimazole 1%
Beeler base cream csp. 50 gWishing you a great week…Source:1- Farmaceutsko Društvo Srbije 2008 (Pharmaceutical Association of Serbia 2008)
2- ACTOS (Actas Dermosifiliogr. 2013;104(9):738—756)
RxMediaPharma®2019 Interactive Drug Information SourceSpec. Pharm. Ahmet Nezihi Pekcan
Pekcan Pharmacy – Konya
[email protected]
Tel: (332) 3520657
http://www.majistralformul.com/
