Ciclomazole

Ciclomazole Uses, Dosage, Side Effects, Food Interaction and all others data.

Ciclopirox Olamine is a synthetic, broad-spectrum, antifungal agent. The chemical name is 6-cyclohexyl-1-hydroxy-4-methyl-2(1H)-pyridone, 2-aminoethanol salt.

Ciclopirox is a broad-spectrum antifungal medication that also has antibacterial and anti-inflammatory properties. Its main mode of action is thought to be its high affinity for trivalent cations, which inhibit essential co-factors in enzymes. Ciclopirox exhibits either fungistatic or fungicidal activity in vitro against a broad spectrum of fungal organisms, such as dermatophytes, yeasts, dimorphic fungi, eumycetes, and actinomycetes. In addition to its broad spectrum of action, ciclopirox also exerts antibacterial activity against many Gram-positive and Gram-negative bacteria. Furthermore, the anti-inflammatory effects of ciclopirox have been demonstrated in human polymorphonuclear cells, where ciclopirox has inhibited the synthesis of prostaglandin and leukotriene. Ciclopirox can also exhibit its anti-inflammatory effects by inhibiting the formation of 5-lipoxygenase and cyclooxygenase.

Clotrimazole is a broad spectrum antifungal. It also exhibits activity against Trichomonus, Staphylococci, Streptococci and Bacteroides. Clotrimazole kills fungi and yeasts by interfering with their cell membranes. It works by stopping the production of ergosterol, which is an essential component of fungal cell membranes resulting in increased membrane permeability and leakage of essential constituents of the fungal cells. Clotrimazole acts reliably on dermatophytes, yeasts and other fungi; it is also effective against Trichomonas vaginalis and Gram-positive microorganisms (streptococci/ staphylococci) and Gram-negative microorganisms (bacteroides/ Haemophilus vaginalis).

Clotrimazole is a broad-spectrum antifungal agent that inhibits the growth of pathogenic yeasts by changing the permeability of cell membranes. The action of clotrimazole is fungistatic at concentrations of drug up to 20 mcg/mL and may be fungicidal in vitro against Candida albicans and other species of the genus Candida at higher concentrations . Unfortunately, resistance to clotrimazole, which was rare in the past, is now common in various patient populations .

Clotrimazole is generally considered to be a fungistatic, and not a fungicidal drug, although this contrast is not absolute, as clotrimazole shows fungicidal properties at higher concentrations .

Ciclomazole
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Ciclomazole
Generic	Clotrimazole + betamethasone dipropionate + ciclopirox
Type	Kit
Therapeutic Class
Manufacturer
Available Country	United States
Last Updated:	September 19, 2023 at 7:00 am

Uses

Ciclopirox cream is used for the topical treatment of the following dermal infections:Tinea pedis, tinea cruris, and tinea corporis due to Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum and Microsporum canis Candidiasis moniliasis) due to Candida albicans; and tinea (pityriasis) versicolor due to Malassezia furfur.

The confirmed indication for Clotrimazole include:

All dermatomycoses due to dermatophytes (e.g. Trichophyton species).
All dermatomycoses due to yeasts (Candida species).
Dermatomycoses due to moulds and other fungi.
Skin diseases showing superinfections with these fungi.

To the dermatomycoses listed under 1-4 belong for example, interdigital myocoses (e.g. athlete’s foot), paronychias (associated with nail mycoses), myocoses in skin folds, Candida vulvitis, Candida balanitis, Pityriasis versicolor, erythrasma.

Clotrimazole rectal preparation is used for vaginal itching, burning and discharge associated with recurrent vaginal yeast infections (Vaginal candidiasis) and also in viginitis due to Candida species as well as Mycotic infections complicated by other microorganisms sensitive to the drug.

Clotrimazole Sterile Eye Ointment is used for the treatment of fungal keratitis due to filamentous fungi and Candida species.

Clotrimazole Ear Drop is used for the treatment of fungal infections of the ear.

Ciclomazole is also used to associated treatment for these conditions: Fungal skin infection, Pityriasis versicolor, Seborrheic dermatitis of the scalp, Tinea Corporis, Tinea Cruris, Tinea Pedis, Vulvovaginal Candidiasis, Cutaneous candidiasis, Mild Onychomycosis, Moderate OnychomycosisBalanitis candida, Candidiasis, Dermatitis, Dermatomycoses, Ear infection fungal, Erythrasma, Fungal Vaginal Infections, Fungal skin infection, Genital candidiasis, Inflammation, Mixed Vaginal Infections, Oropharyngeal Candidiasis, Pityriasis versicolor, Pyoderma, Ringworm, Skin Infections, Skin candida, Tinea Corporis, Tinea Cruris, Tinea Pedis, Tinea inguinalis, Trichophytosis, Vaginal Candidiasis, Vaginal Mycosis, Vulvitis, Cutaneous candidiasis, Infection mycotic, Susceptible Bacterial Infections, Symptomatic Tinea Corporis caused by Trichophyton mentagrophytes, Trichophyton rubrum, Epidermophyton floccosum, Symptomatic Tinea Cruris caused by Trichophyton mentagrophytes, Trichophyton rubrum, Epidermophyton floccosum, Symptomatic Tinea Pedis caused by Trichophyton mentagrophytes, Trichophyton rubrum, Epidermophyton floccosum, Tinea versicolor caused by Malassezia infection

How Ciclomazole works

Unlike antifungals such as itraconazole and terbinafine, which affect sterol synthesis, ciclopirox is thought to act through the chelation of polyvalent metal cations, such as Fe³⁺ and Al³⁺. These cations inhibit many enzymes, including cytochromes, thus disrupting cellular activities such as mitochondrial electron transport processes and energy production. Ciclopirox also appears to modify the plasma membrane of fungi, resulting in the disorganization of internal structures. The anti-inflammatory action of ciclopirox is most likely due to inhibition of 5-lipoxygenase and cyclooxygenase. ciclopirox may exert its effect by disrupting DNA repair, cell division signals and structures (mitotic spindles) as well as some elements of intracellular transport.

Clotrimazole acts primarily by damaging the permeability barrier in the cell membrane of fungi. Clotrimazole causes inhibition of ergosterol biosynthesis, an essential constituent of fungal cell membranes. If ergosterol synthesis is either completely or partially inhibited, the cell is no longer able to construct an intact and functional cell membrane ,. Because ergosterol directly promotes the growth of fungal cells in a hormone‐like fashion, rapid onset of the above events leads to dose-dependent inhibition of fungal growth .

Though decreased ergosterol, due to the inhibition of lanosterol 14-demethylase (also known as CYP51) is accepted to be primarily responsible for the antimycotic properties of clotrimazole, this drug also shows other pharmacological effects. These include the inhibition of sarcoplasmic reticulum Ca2+‐ATPase, depletion of intracellular calcium, and blocking of calcium‐dependent potassium channels and voltage‐dependent calcium channels . The action of clotrimazole on these targets accounts for other effects of this drug that are separate from its antimycotic activities .

Dosage

Ciclomazole dosage

Gently massage Ciclopirox cream into the affected and surrounding skin areas twice daily, in the morning and evening for four weeks. Clinical improvement with relief of pruritus and other symptoms usually occurs within the first week of treatment. If a patient shows no clinical improvement after four weeks of treatment, the diagnosis should be redetermined. Patients with tinea versicolor usually exhibit clinical and mycological clearing after two weeks of treatment.

Topical

Wash skin with soap and water and dry thoroughly. Apply a thin layer of the cream or solution 2-3 times daily and gently massage over affected area as directed by the doctor. For Athlete’s foot, pay special attention to the spaces between the toes. Best results in Athlete's foot and ringworm are usually obtained with 4 weeks use of this product. The cream should be applied two or three times daily for one month or for at least two weeks after the disappearance of all signs of infection. If satisfactory results have not occurred within these times consultation with doctor is essential. For best results, follow directions and continue treatment for length of time indicated. The duration of treatment varies; it depends among other factors on the extent and localization of the disease.

Recommended duration of treatment :

Dermatomycoses: 3-4 weeks
Candida vulvitis and candida balanitis: 1-2 weeks
Erythrasma and pityriasis versicolor (approx.): 3 weeks
In fungal infection of the feet, to prevent relapses:Treatment should be continued for about 2 weeks beyond the disappearance of all signs of disease.

Clotrimazole cream is odourless, can be washed off and does not stain.

Rectal

First infections: In general, a 3-day treatment is sufficient for Candida vaginitis. On 3 consecutive nights, Clotrimazole 200 mg vaginal preparation is inserted as deeply as possible into the vagina. This is best achieved when lying on one's back with the knees slightly bent.

Re-infections: In general, a 6-day treatment is sufficient. This applies also to mixed infections with the above-mentioned causative organisms. On six consecutive nights, 1 Clotrimazole 100 mgvaginal preparation is inserted as deeply as possible into the vagina. If necessary, 2 Clotrimazole 100 mg(1 in the morning and 1 in the evening) or 1 Clotrimazole 200 mg daily can be used for 6-12 days. Treatment should be timed so as to avoid the menstrual period and be finished before the onset of menstruation. To avoid re-infection, the partner should undergo local treatment with Clotrimazole cream at the same time.

Clotrimazole 500 mg vaginal preparation: Single dose, complete treatment with one vaginal tablet. The tablet should be inserted as deeply as possible into the vagina. This is best achieved when lying on one's back with the knees slightly bent. It is recommended that the treatment should be timed so as to avoid the menstrual period. For prevention of re-infection the partner should be treated locally with Clotrimazole cream at the same time.

Clotrimazolevaginal preparation are colorless and do not stain the underwear.

Eye

Adult: It should be applied thinly and evenly to the conjunctival sac every 4 hours daily or as advised by a physician.

Children: Safety and effectiveness in children have been established for Clotrimazole when used as indicated and in the recommended dosage.

Ear

Instill 2-3 drops of Clarizol Ear Drops in the affected ear two or three times daily.The treatment should be continued for at least two weeks after the disappearance of all signs of infection to prevent re-infection.

Ciclopirox cream is not for ophthalmic use.

For the treatment to become a complete success, reliable and sufficiently long application of Clotrimazole cream is important. The duration of treatment varies; it depends among other factors on the extent and localisation of the disease.

Side Effects

Ciclopirox Olamine cream is well tolerated with a low incidence of side effects. The most frequently reported events are itching, redness, burning, dryness, or irritation of treated skin.

Clotrimazole is generally well tolerated after local application but the few side effects have been reported infrequently like erythema, stinging, blistering, peeling, oedema, pruritus, urticaria and general irritation.

Since there is practically no Clotrimazole absorption through the vaginal skin, no systemic effect is expected. The local tolerance of Clotrimazole vaginal tablet is generally good. Local irritation or burning sensation may occur in a very few cases but these symptoms are not considered harmful.

Rarely patients may experience burning or irritation immediately after applying the ointment.

Toxicity

Oral LD₅₀ in rat is >10 ml/kg. Symptoms of overexposure include drowsiness and headache.

Symptoms of overdose include erythema, stinging, blistering, peeling, edema, pruritus, urticaria, burning, and general irritation of the skin, and cramps. As with all topical agents, skin sensitization may result .

Oral LD50 (rat): 708 mg/kg; Intraperitoneal LD50 (rat): 445 mg/kg; Subcutaneous LDLO (rat): 10 g/kg; Oral LD50 (mouse): 761 mg/kg; Subcutaneous LDLO (mouse): 10 g/kg; Intraperitoneal LD50 (mouse): 108 mg/kg;

Overdose

This drug poses no risk of acute intoxication, as it is unlikely to occur following a single vaginal or dermal application of an overdose (application over a large area under conditions favorable to absorption) or accidental oral ingestion. There is no specific antidote .

Effects on Fertility

No human studies of the effects of clotrimazole on fertility have been conducted; however, animal studies have not shown any effects on the drug on fertility .

Use in Pregnancy

There are limited data regarding the use of clotrimazole in pregnant women. Animal studies do not show direct or indirect harmful effects on reproduction. Although the topical application of clotrimazole may result in very low serum and tissue levels, the use of clotrimazole topical cream by pregnant women is not recommended unless it is advised by the prescribing physician. Clotrimazole topical cream should not be used in the first trimester of pregnancy unless it is considered by the physician to be essential to patient well-being .

Use in Breastfeeding

Available pharmacodynamic/toxicological studies in animals have shown excretion of clotrimazole/metabolites in breastmilk. Clotrimazole should not be administered during breastfeeding. Although the topical application of clotrimazole has resulted in very low serum and tissue levels, the use of clotrimazole topical cream by lactating women is not recommended unless it recommended by the prescribing physician .

Precaution

If a reaction suggesting sensitivity or chemical irritation occurs with the use of Ciclopirox Cream, treatment should be discontinued and appropriate therapy instituted.

If local intolerance develops, consider withdrawal of the medicine and institution of appropriate therapy. Clotrimazole solution is not intended for ophthalmic use. Avoid contact with eyes upon topical application. Children 3 yrs. Pregnancy, lactation. If irritation or sensitivity develops with the use of Clotrimazole ointment, treatment should be discontinued.

Interaction

There are no known drug interactions and none well documented.

There have been reports of a heat reaction when this medication used concomitantly with Sofradex drops in the ear.

Antagonism with polyene antibiotics.

Volume of Distribution

The topical form is minimally absorbed in the serum and tissues . Clotrimazole is a lipophilic drug , and has been shown to be secreted in breastmilk in animal studies . There are limited data available regarding the volume of distribution following oral troche administration.

Elimination Route

Rapidly absorbed after oral administration. Mean absorption of ciclopirox after application to nails of all twenty digits and adjacent 5 millimeters of skin once daily for 6 months in patients with dermatophytic onychomycoses was less than 5% of the applied dose. Ciclopirox olamine also penetrates into hair and through the epidermis and hair follicles into sebaceous glands and dermis.

Because clotrimazole is generally not significantly absorbed, drug interactions are not a major issue with its use .

Half Life

1.7 hours for 1% topical solution.

Elimination Route

Most of the compound is excreted either unchanged or as glucuronide. After oral administration of 10 mg of radiolabeled drug (14C-ciclopirox) to healthy volunteers, approximately 96% of the radioactivity was excreted renally within 12 hours of administration. Ninety-four percent of the renally excreted radioactivity was in the form of glucuronides.

Mainly hepatic .

Pregnancy & Breastfeeding use

Pregnancy Category B. There are no adequate or well-controlled studies in pregnant women. Therefore, Ciclopirox cream should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Lactation: It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Ciclopirox cream is administered to nursing women.

Pregnancy:Clotrimazole is recommended during pregnancy only after first consulting a doctor.

Lactation:Because systemic absorption of clotrimazole following topical application is marginal, there should be no risk for the infant during lactation.