Penlac

Penlac - General Information

Penlac (also called Loprox®, Penlac® and Stieprox®) is a synthetic antifungal agent for topical dermatologic use. [Wikipedia]

Pharmacology of Penlac

Penlac 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. Penlac 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. Penlac can also exhibit its anti-inflammatory effects by inhibiting the formation of 5-lipoxygenase and cyclooxygenase.

Penlac for patients

Patients should have detailed instructions regarding the use of PENLAC® NAIL LACQUER (ciclopirox) Topical Solution, 8%, as a component of a comprehensive management program for onychomycosis in order to achieve maximum benefit with the use of this product.

The patient should be told to:

1. Use PENLAC® NAIL LACQUER (ciclopirox) Topical Solution, 8%, as directed by a health care professional. Avoid contact with the eyes and mucous membranes. Contact with skin other than skin immediately surrounding the treated nail(s) should be avoided. PENLAC® NAIL LACQUER (ciclopirox) Topical Solution, 8%, is for external use only.
2. PENLAC® NAIL LACQUER (ciclopirox) Topical Solution, 8%, should be applied evenly over the entire nail plate and 5 mm of surrounding skin. If possible, PENLAC® 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). Contact with the surrounding skin may produce mild, transient irritation (redness).
3. Removal of the unattached, infected nail, as frequently as monthly, by a health care professional is needed with use of this medication. Inform a health care professional if they have diabetes or problems with numbness in your toes or fingers for consideration of the appropriate nail management program.
4. Inform a health care professional if the area of application shows signs of increased irritation (redness, itching, burning, blistering, swelling, oozing).
5. Up to 48 weeks of daily applications with PENLAC® NAIL LACQUER (ciclopirox) Topical Solution, 8%, and professional removal of the unattached, infected nail, as frequently as monthly, are considered the full treatment needed to achieve a clear or almost clear nail (defined as 10% or less residual nail involvement).
6. Six months of therapy with professional removal of the unattached, infected nail may be required before initial improvement of symptoms is noticed.
7. A completely clear nail may not be achieved with use of this medication. In clinical studies less than 12% of patients were able to achieve either a completely clear or almost clear toenail.
8. Do not use the medication for any disorder other than that for which it is prescribed.
9. Do not use nail polish or other nail cosmetic products on the treated nails.
10. Avoid use near heat or open flame, because product is flammable.

Patient Insert and Instructions

PENLAC® NAIL LACQUER
(ciclopirox)
Topical Solution, 8%

Patients should have detailed instructions regarding the use of PENLAC NAIL LACQUER Topical Solution, 8%, as a component of a comprehensive management program for onychomycosis in order to achieve maximum benefit with the use of this product. Discuss your treatment plan with your health care professional for regular removal of the unattached, infected nail.

Before using this medication, tell your doctor if you:

• Are pregnant or nursing
• Are an insulin dependent diabetic or have diabetic neuropathy
• Have a history of immunosuppression
• Are immunocompromised (e.g., received an organ transplant, etc.)
• Require medication to control epilepsy
• Use or require topical corticosteroids on a repeated monthly basis
• Use steroid inhalers on a regular basis

Patient Information:

• Use PENLAC NAIL LACQUER Topical Solution, 8%, as directed by your health care professional.
• PENLAC NAIL LACQUER Topical Solution, 8%, is for external use only.
• Contact with skin other than skin immediately surrounding the treated nail(s) should be avoided.
• Avoid contact with the eyes and mucous membranes.
• Removal of the unattached, infected nail, as frequently as monthly, by your health care professional is needed with use of this medication to obtain maximal benefit with use of this product. If you have diabetes or problems with numbness in your toes or fingers, talk to your health care provider before trimming your nails or removing any nail material.
• Inform your health care professional if the area of application shows signs of increased irritation (redness, itching, burning, blistering, swelling, oozing).
• Up to 48 weeks of daily applications with PENLAC NAIL LACQUER Topical Solution, 8%, and professional removal, as frequently as monthly, of the unattached, infected nail are considered the full treatment time to achieve a clear or almost clear nail (defined as 10% or less residual nail involvement). Six months of therapy with professional removal of the unattached, infected nail may be required before initial improvement of symptoms is noticed.
• A completely clear nail may not be achieved with use of this medication. In clinical studies less than 12% of patients were able to achieve either a clear or almost clear toenail.
• Do not use nail polish or other nail cosmetic products on the treated nails.
• Avoid use near heat or open flame, because product is flammable.

Patient Instructions

2. Before starting treatment, remove any loose nail or nail material using nail clippers or nail files. If you have diabetes or problems with numbness in your toes or fingers, talk to your health care provider before trimming your nails or removing any nail material.
3. 
   
   
4. Apply PENLAC NAIL LACQUER Topical Solution, 8%, once daily (preferably at bedtime) to all affected nails with the applicator brush provided. Apply the lacquer evenly over the entire nail. Where possible, nail lacquer should also be applied to the underside of the nail and to the skin beneath it. Allow lacquer to dry (approximately 30 seconds) before putting on socks or stockings. After applying medication, wait 8 hours before taking a bath or shower.
5. Apply PENLAC NAIL LACQUER Topical Solution, 8%, daily over the previous coat.

Prescribing Information as of December 2004
Manufactured for:
Dermik Laboratories
A Division of Aventis Pharmaceuticals Inc.
Berwyn, PA 19312 USA
by:
Aventis Pharma Deutschland GmbH
D-65926 Frankfurt am Main
Germany
©Dermik Laboratories 2003

Penlac Interactions

No information provided.

Penlac Contraindications

PENLAC NAIL LACQUER Topical Solution, 8%, is contraindicated in individuals who have shown hypersensitivity to any of its components.

Additional information about Penlac

Penlac Indication: Used as a topical treatment in immunocompetent patients with mild to moderate onychomycosis of fingernails and toenails without lunula involvement, due to Trichophyton rubrum.
Mechanism Of Action: 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. Penlac 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.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Ciclopirox
Synonyms: ciclopiroxolamine; Ciclopiroxum [INN-Latin]; CPO; HOE 296b; HOE-296b; Ciclopirox Olamin; Ciclopirox-Olamin
Drug Category: Antifungal Agents
Drug Type: Small Molecule; Approved

Other Brand Names containing Ciclopirox: Loprox; Penlac; Penlac Nail Lacquer; Stieprox;
Absorption: 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.
Toxicity (Overdose): Oral LD₅₀ in rat is >10 ml/kg. Symptoms of overexposure include drowsiness and headache.
Protein Binding: Protein binding is 94-97% following topical administration.
Biotransformation: Glucuronidation is the main metabolic pathway of ciclopirox.
Half Life: 1.7 hours for 1% topical solution.
Dosage Forms of Penlac: Lotion Topical
Solution Topical
Cream Topical
Shampoo Topical
Chemical IUPAC Name: 6-cyclohexyl-1-hydroxy-4-methylpyridin-2-one
Chemical Formula: C12H17NO2
Ciclopirox on Wikipedia: https://en.wikipedia.org/wiki/Ciclopirox
Organisms Affected: Humans and other mammals; Yeast and other fungi