Penlac Information
Penlac (Ciclopirox) Description
Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, contains a synthetic antifungal agent, ciclopirox. It is intended for topical use on fingernails and toenails and immediately adjacent skin.
Each gram of Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, contains 80 mg ciclopirox in a solution base consisting of ethyl acetate, NF; isopropyl alcohol, USP; and butyl monoester of poly[methylvinyl ether/maleic acid] in isopropyl alcohol. Ethyl acetate and isopropyl alcohol are solvents that vaporize after application.
Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, is a clear, colorless to slightly yellowish solution.
The chemical name for ciclopirox is 6-cyclohexyl-1-hydroxy-4-methyl-2(1H)-pyridone, with the empirical formula CHNO and a molecular weight of 207.27. The CAS Registry Number is [29342-05-0]. The chemical structure is:
Penlac (Ciclopirox) Clinical Pharmacology
(1–2)
One study was conducted evaluating 8% ciclopirox against new and established and infections in ovine hoof material. After 10 days of treatment the growth of and in the established infection model was very minimally affected. Elimination of the molds from hoof material was not achieved in either the new or established infection models.
In vitro
Trichophyton rubrum
Trichophyton rubrum
As demonstrated in pharmacokinetic studies in animals and man, ciclopirox olamine is rapidly absorbed after oral administration and completely eliminated in all species via feces and urine. 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. Thus, glucuronidation is the main metabolic pathway of this compound.
Systemic absorption of ciclopirox was determined in 5 patients with dermatophytic onychomycoses, after application of Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, to all 20 digits and adjacent 5 mm of skin once daily for six months. Random serum concentrations and 24 hour urinary excretion of ciclopirox were determined at two weeks and at 1, 2, 4 and 6 months after initiation of treatment and 4 weeks post-treatment. In this study, ciclopirox serum levels ranged from 12–80 ng/mL. Based on urinary data, mean absorption of ciclopirox from the dosage form was
In two vehicle-controlled trials, patients applied Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, to all toenails and affected fingernails. Out of a total of 66 randomly selected patients on active treatment, 24 had detectable serum ciclopirox concentrations at some point during the dosing interval (range 10.0–24.6 ng/mL). It should be noted that eleven of these 24 patients took concomitant medication containing ciclopirox as ciclopirox olamine (Loprox Cream, 0.77%).
The penetration of the Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, was evaluated in an investigation. Radiolabeled ciclopirox applied once to onychomycotic toenails that were avulsed demonstrated penetration up to a depth of approximately 0.4 mm. As expected, nail plate concentrations decreased as a function of nail depth. The clinical significance of these findings in nail plates is unknown. Nail bed concentrations were not determined.
Penlac (Ciclopirox) Indications And Usage
Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, as a component of a comprehensive management program, is indicated as topical treatment in immunocompetent patients with mild to moderate onychomycosis of fingernails and toenails without lunula involvement, due to . The comprehensive management program includes removal of the unattached, infected nails as frequently as monthly, by a health care professional who has special competence in the diagnosis and treatment of nail disorders, including minor nail procedures.
Penlac (Ciclopirox) Contraindications
Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, is contraindicated in individuals who have shown hypersensitivity to any of its components.
Penlac (Ciclopirox) Warnings
Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, is not for ophthalmic, oral, or intravaginal use. For use on nails and immediately adjacent skin only.
Penlac (Ciclopirox) Precautions
If a reaction suggesting sensitivity or chemical irritation should occur with the use of Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, treatment should be discontinued and appropriate therapy instituted.
So far there is no relevant clinical experience with patients with insulin dependent diabetes or who have diabetic neuropathy. The risk of removal of the unattached, infected nail, by the health care professional and trimming by the patient should be carefully considered before prescribing to patients with a history of insulin dependent diabetes mellitus or diabetic neuropathy.
Penlac (Ciclopirox) Adverse Reactions
In the vehicle-controlled clinical trials conducted in the US, 9% (30/327) of patients treated with Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, and 7% (23/328) of patients treated with vehicle reported treatment-emergent adverse events (TEAE) considered by the investigator to be causally related to the test material.
The incidence of these adverse events, within each body system, was similar between the treatment groups except for Skin and Appendages: 8% (27/327) and 4% (14/328) of subjects in the ciclopirox and vehicle groups reported at least one adverse event, respectively. The most common were rash-related adverse events: periungual erythema and erythema of the proximal nail fold were reported more frequently in patients treated with Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, (5% [16/327]) than in patients treated with vehicle (1% [3/328]). Other TEAEs thought to be causally related included nail disorders such as shape change, irritation, ingrown toenail, and discoloration.
The incidence of nail disorders was similar between the treatment groups (2% [6/327] in the Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, group and 2% [7/328] in the vehicle group). Moreover, application site reactions and/or burning of the skin occurred in 1% of patients treated with Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, (3/327) and vehicle (4/328).
A 21-Day Cumulative Irritancy study was conducted under conditions of semi-occlusion. Mild reactions were seen in 46% of patients with the Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, 32% with the vehicle and 2% with the negative control, but all were reactions of mild transient erythema. There was no evidence of allergic contact sensitization for either the Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, or the vehicle base. In a separate study of the photosensitization potential of Penlac (Ciclopirox) ® NAIL LACQUER (ciclopirox) Topical Solution, 8% in a maximized test design that included the occluded application of sodium lauryl sulfate, no photoallergic reactions were noted. In four subjects localized allergic contact reactions were observed. In the vehicle-controlled studies, one patient treated with Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, discontinued treatment due to a rash, localized to the palm (causal relation to test material undetermined).
Use of Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, for 48 additional weeks was evaluated in an open-label extension study conducted in patients previously treated in the vehicle-controlled studies. Three percent (9/281) of subjects treated with Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, experienced at least one TEAE that the investigator thought was causally related to the test material. Mild rash in the form of periungual erythema (1% [2/281]) and nail disorders (1% [4/281]) were the most frequently reported. Four patients discontinued because of TEAEs. Two of the four had events considered to be related to test material: one patient's great toenail "broke away" and another had an elevated creatine phosphokinase level on Day 1 (after 48 weeks of treatment with vehicle in the previous vehicle-controlled study).
Penlac (Ciclopirox) Dosage And Administration
Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, should be used as a component of a comprehensive management program for onychomycosis. Removal of the unattached, infected nail, as frequently as monthly, by a health care professional, weekly trimming by the patient, and daily application of the medication are all integral parts of this therapy. Careful consideration of the appropriate nail management program should be given to patients with diabetes (see ).
Patients should file away (with emery board) loose nail material and trim nails, as required, or as directed by the health care professional, every seven days after Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, is removed with alcohol.
Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, should be applied once daily (preferably at bedtime or eight hours before washing) to all affected nails with the applicator brush provided. The Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, should be applied evenly over the entire nail plate.
If possible, Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, should be applied to the nail bed, hyponychium, and the under surface of the nail plate when it is free of the nail bed (e.g., onycholysis).
The Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, should not be removed on a daily basis. Daily applications should be made over the previous coat and removed with alcohol every seven days. This cycle should be repeated throughout the duration of therapy.
Penlac (Ciclopirox) How Supplied
Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, is supplied in 3.3 mL (NDC 0066-8008-01) and 6.6 mL (NDC 0066-8008-02) glass bottles with screw caps which are fitted with brushes.
Penlac (Ciclopirox) NAIL LACQUER (ciclopirox) Topical Solution, 8%, should be stored at room temperature between 59° and 86° F (15° and 30° C).
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