Loprox

Topical Dermatological Antifungals
Topical Scalp Antifungals

For topical use only as directed. Not for ophthalmic, oral, or intravaginal use.
Applied to the skin as a lotion or cream.
Applied to the scalp as a shampoo.
Applied to the nails as a nail lacquer.

Cream, Gel, or Suspension
Wash hands before and after application, except when treating the infections of the hand(s).
Apply sparingly in a thin film and rub gently into affected area(s) of clean, dry skin. Restrict application to the affected areas and try to avoid normal surrounding skin.
Avoid use with occlusive wrappings or dressings.
Patients who fail to respond to topical treatment after 4 weeks should be re-evaluated.

Nail Lacquer
For topical use on fingernails and toenails and immediately adjacent skin only.
Ciclopirox should be used in conjunction with a comprehensive management program for onychomycosis which includes removal of the unattached, infected nails (as frequently as monthly) by a health care professional and weekly trimming of the nails by the patient.
Apply evenly over the entire nail plate and 5 mm of surrounding skin.
If possible, apply to the nail bed, hyponychium, and the under surface of the nail plate when it is free of the nail bed (e.g., onycholysis).
Apply daily over the previous coat. Remove the nail lacquer coat every 7 days with alcohol.
Patients should file away (with an emery board) loose nail material and trim nails, as required, every 7 days after ciclopirox is removed with alcohol.
Repeat this cycle throughout the duration of therapy.
To prevent the screw cap from sticking to the nail solution bottle, do not allow the solution to get into the bottle threads.
Close the nail solution bottle tightly after every use.
Storage: To protect from light, replace bottle into carton after each use.
 
Shampoo
Wet hair.
Apply to scalp as directed in dosage. Lather and leave on for 3 minutes; rinse.

ventricular tachycardia / Early / Incidence not known

erythema / Early / 1.0-46.0
contact dermatitis / Delayed / 0-5.0

pruritus / Rapid / 0-5.0
nail discoloration / Delayed / 1.0-2.0
alopecia / Delayed / 0-1.0
hair discoloration / Delayed / 0-1.0
rash / Early / 0-1.0
xerosis / Delayed / 0-1.0
acneiform rash / Delayed / 0-1.0
headache / Early / Incidence not known

Ciclodan, Ciclodan Nail Solution, Loprox, Loprox TS, Penlac

Rx

Antifungal agent; 1% cream or lotion used topically for tinea infections; 8% nail solution used for onychomycosis; 1% shampoo for seborrheic dermatitis of the scalp.

Apply once daily (preferably at bedtime or 8 hours before washing nails) to affected nails for up to 48 weeks.

Apply once daily (preferably at bedtime or 8 hours before washing nails) to affected nails for up to 48 weeks.

Wet hair and apply roughly 1 teaspoon (5 ml) to the scalp. Up to 10 ml may be used for long hair. Lather and leave on hair and scalp for 3 minutes. Rinse off. Repeat treatment twice per week for a total of 4 weeks, with a minimum of 3 days between applications. If there is no improvement after 4 weeks of treatment, the diagnosis should be reviewed.

Apply to affected scalp areas twice daily for 4 weeks.

Apply to affected area(s) twice daily for 4 weeks.

Apply to affected area(s) twice daily for 4 weeks.

Apply to affected area(s) twice daily for 4 weeks.

Apply to affected area(s) twice daily for 4 weeks.

Apply to affected area(s) twice daily for 4 weeks.

Apply to affected area(s) twice daily for 4 weeks.

Apply to affected area(s) twice daily for 2 weeks.

Apply to affected area(s) twice daily for 2 weeks.

No dosage adjustment is needed.

No dosage adjustment is needed.

There are no drug interactions associated with Ciclopirox products.

Ciclodan/Ciclopirox/Ciclopirox Olamine/Loprox Topical Cream: 0.77%
Ciclodan/Ciclopirox/Ciclopirox Olamine/Penlac Topical Sol: 8%
Ciclopirox/Ciclopirox Olamine/Loprox/Loprox TS Topical Susp: 0.77%
Ciclopirox/Loprox Topical Gel: 0.77%
Ciclopirox/Loprox Topical Shampoo: 1%

Maximum dosage is product specific; consult specific product labeling.

Maximum dosage is product specific; consult specific product labeling.

Maximum dosage is product specific. Safety and efficacy are product specific; consult specific product labeling.

>= 10 years: Maximum dosage is product specific. Safety and efficacy are product specific; consult specific product labeling.
< 10 years: Safety and efficacy have not been established.

Ciclopirox is a substituted pyridone antimycotic with activity against a broad spectrum of dermatophytes, yeasts, actinomycetes, molds, other fungi and some gram-positive and gram-negative bacteria. Although the exact cellular mechanisms are unknown, ciclopirox is thought to exert its antifungal and antibacterial activity by blocking fungal transmembrane transport, causing intracellular depletion of essential substrates (e.g., amino acids) and/or ions (e.g., potassium). Ciclopirox interferes with the synthesis of RNA and DNA. At high ciclopirox concentrations, the fungal cell membrane permeability is altered, allowing leakage of intracellular material. Ciclopirox does not inhibit synthesis nor cause lysis of the fungal cell wall. One in vitro study suggested that ciclopirox acts by chelation of polyvalent cations (Fe+3 or Al+3) resulting in inhibition of the metal-dependent enzymes that are responsible for the degradation of peroxides within the fungal cell; the clinical significance of this observation is not known.
 
Ciclopirox has fungicidal activity against in vitro isolates of Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, Microsporum canis, and Candida albicans. Ciclopirox also inhibits the growth of pathogenic dermatophytes, yeasts, and Malassezia furfur. Although not used for its antibacterial properties, ciclopirox has some activity against Trichomonas vaginalis and Mycoplasma.
 
In vitro susceptibility testing methods for determining ciclopirox MIC values against the dermatophytic molds, including Trichophyton rubrum species, have not been standardized or validated. Breakpoints to determine whether clinical isolates of Trichophyton rubrum are susceptible or resistant to ciclopirox have not been established. Due to variation in laboratory techniquies, Trichophyton rubrum and Trichophyton mentagrophytes species are associated with a broad range of ciclopirox MIC values (range 1-20 ug/mL).
 
Studies have not been conducted to evaluate drug resistance development in Trichophyton rubrum species exposed to ciclopirox. Studies assessing cross-resistance to ciclopirox and other known antifungal agents have not been performed.
 
The relevance of the antifungal properties of ciclopirox for the indication of seborrheic dermatitis is not known.

Ciclopirox olamine is administered topically and is distributed to the stratum corneum, epidermis, hair follicles, sebaceous glands, and dermis. Topical ciclopirox also penetrates into fingernails and toenails.

Studies investigating ciclopirox disposition after oral administration demonstrate that ciclopirox is primarily renally excreted as glucuronides (about 94%) or as unchanged drug. Fecal excretion is negligible.

Ciclopirox, when applied as a topical 1% solution is approximately 1.3% systemically absorbed when applied to 750 cm2 of back skin which is occluded for 6 hours. The drug half-live is 1.7 hours. Two days after application, only 0.01% of the dose is recovered in the urine. Penetration studies for Loprox 1% lotion in human cadaverous skin resulted in 0.8 to 1.6% of the dose in the stratum corneum 1.5 to 6 hours after application. Penetration studies demonstrate that the 1% cream has equivalent systemic absorption to the 1% lotion.
 
Systemic absorption of ciclopirox nail solution was determined in five patients with dermatophytic onychomycosis, after once daily application to all 20 digits and adjacent 5 mm of skin for six months. In this study, ciclopirox serum levels ranged from 12-80 ng/mL. Based on urinary data, the mean absorption of ciclopirox was <5% of the applied dose. One month after discontinuing treatment, the serum and urine ciclopirox concentrations were below the detection limit. The in vitro penetration of the ciclopirox nail solution was evaluated by application of radiolabeled ciclopirox to onychomycotic toenails that were avulsed; the drug penetrated to a nail depth of approximately 0.4 mm. As expected, nail plate concentrations decreased with nail depth. The clinical significance of these findings is unknown.

Ciclopirox is classified as an FDA pregnancy category B drug. There are no adequate or well-controlled studies in pregnant women. Animal studies involving mice, rats, rabbits, and monkeys revealed no embryotoxicity or teratogenicity effects following oral administration of doses ranging from 13—54 times the maximum recommended human dose. Ciclopirox should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Data are limited regarding use of ciclopirox during breast-feeding and its' excretion into breast milk is unknown. Topical application is not expected to result in significant maternal absorption, and thus should not be of great risk to a breast-feeding infant. However, it is rapidly absorbed following oral administration; therefore, nursing mothers should be instructed to avoid application topically to the breast while breast-feeding. Terbinafine, clotrimazole, and miconazole may be potential alternatives to consider during breast-feeding. However, site of infection, local susceptibility patterns, and specific microbial susceptibility should be assessed before choosing an alternative agent. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally ingested or administered drug, health care providers are encouraged to report the adverse effect to the FDA.