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Rx Only
FOR TOPICAL USE ONLY
NOT FOR OPHTHALMIC, ORAL OR INTRAVAGINAL USE
KEEP OUT OF REACH OF CHILDREN
DESCRIPTION
Ciclopirox Shampoo 1% contains the synthetic antifungal agent, ciclopirox.
Each gram (equivalent to 0.96 mL) of Ciclopirox Shampoo contains 10 mg ciclopirox in a shampoo base consisting of disodium laureth sulfosuccinate, laureth-2, purified water USP, sodium chloride USP and sodium laureth sulfate.
Ciclopirox Shampoo is a colorless to yellowish, translucent solution. The chemical name for ciclopirox is 6-cyclohexyl-1-hydroxy-4-methyl-2(1H)-pyridone, with the empirical formula C12H17NO2 and a molecular weight of 207.27. The CAS Registry Number is [29342-05-0]. The chemical structure is:
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CLINICAL PHARMACOLOGY
Mechanism of Action
Ciclopirox is a hydroxypyridone antifungal agent although the relevance of this property for the indication of seborrheic dermatitis is not known. Ciclopirox acts by chelation of polyvalent cations (Fe3+ or Al3+), resulting in the inhibition of the metal-dependent enzymes that are responsible for the degradation of peroxides within the fungal cell.
Pharmacokinetics and Pharmacodynamics
In a study in patients with seborrheic dermatitis of the scalp, application of 5 mL ciclopirox shampoo 1% twice weekly for 4 weeks, with an exposure time of 3 minutes per application, resulted in detectable serum concentrations of ciclopirox in 6 out of 18 patients. The serum concentrations measured throughout the dosing interval on Days 1 and 29 ranged from 10.3 ng/mL to 13.2 ng/mL. Total urinary excretion of ciclopirox was less than 0.5% of the administered dose.
CLINICAL STUDIES
In two randomized, double-blind clinical trials, patients 16 years and older with seborrheic dermatitis of the scalp applied Ciclopirox Shampoo or its vehicle two times per week for 4 weeks. Patients who were immunocompromised, those with psoriasis or atopic dermatitis, women of childbearing potential not using adequate contraception, and pregnant or lactating women were excluded from the clinical studies. An evaluation of the overall status of the seborrheic dermatitis, and the presence and severity of erythema or inflammation, and scaling, was made at week 4, using a scale of 0 = none, 1 = slight, 2 = mild, 3 = moderate, 4 = pronounced, and 5 = severe. Effective treatment was defined as achieving a score of 0 (or a score of 1 if the baseline score was ≥ 3) simultaneously for status of the seborrheic dermatitis, erythema or inflammation, and scaling at Week 4. Ciclopirox shampoo was shown to be statistically significantly more effective than vehicle in both studies. Efficacy results for the two studies are presented in the following table.
| Effective Treatment Rates at Week 4 in Studies 1 and 2 |
|
Ciclopirox Shampoo |
Vehicle |
| Study 1 |
220/380 (58%) |
60/192 (31%) |
| Study 2 |
65/250 (26%) |
32/249 (13%) |
Efficacy for black patients was not demonstrated, although only 53 black patients were enrolled in the two pivotal studies.
Microbiology
Ciclopirox is fungicidal in vitro against Malassezia furfur (Pityrosporum spp.), P. ovale, and P. orbiculare. Ciclopirox acts by chelation of polyvalent cations (Fe3+ or Al3+), resulting in the inhibition of the metal-dependent enzymes that are responsible for the degradation of peroxides within the fungal cell.
The clinical significance of antifungal activity in the treatment of seborrheic dermatitis is not known.
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