Ciclopirox - Dermal Infections - Indication, Dosage, and Pharmacological Aspects

Overview:

Ciclopirox is a topical antifungal medication with special properties. It has been in use for more than 30 years after receiving approval from the US FDA (Food and Drug Administration) in June 2004. Although its cream formulation is not frequently used, it is well known for treating nail fungus. The active ingredient, Ciclopirox, works differently from other antifungals in its mode of action. It modifies membrane permeability and interferes with cellular functions by chelating metal cations. Ciclopirox is a flexible treatment for a range of skin problems since, in addition to its antifungal actions, it also possesses antibacterial and anti-inflammatory qualities.

Available Doses and Dosage Forms:

• Shampoo: Available in concentrations of one percent or 1.5 percent, it is used to treat seborrheic dermatitis or dandruff.

• Cream: Available in a one percent concentration, used for yeast infections and dermatophytes (fungi that require keratin for growth).

• Lacquer: A type of liquid that is applied in an eight percent concentration to the diseased nail(s) to treat onychomycosis, a fungal infection of the nails.

For Patients:

What Is Dermal Infection?

One of the body's main organs, the skin, protects and shields the body from external threats. As a barrier to keep germs out, skin can become infected when they get through cuts, sores, or locations where the skin rubs against itself, particularly when the environment is damp. Infections can also be caused by inadequate blood supply or a weakened immune system as a result of disease or medical procedures. Skin infections can spread deeply into the skin and take on different sizes, encompassing smaller or greater areas.

How Does Ciclopirox Work?

An antifungal called Ciclopirox prevents the fungus that is causing the skin infection from growing and reproducing by denying it access to vital nutrients.

How Effective Is Ciclopirox?

• Ciclopirox gel is recommended for seborrheic dermatitis of the scalp and tinea corporis and interdigital tinea pedis caused by a particular fungus.

• Ciclopirox comes in various forms like a one percent nail lacquer, cream, gel, or suspension (0.77 percent).

• For the treatment of tinea versicolor (sun fungus), tinea corporis (body ringworm), tinea pedis (athlete's foot), and cutaneous candidiasis (fungal infection), the US FDA has approved Ciclopirox. Onychomycosis is treated using the nail lacquer.

• Trials conducted on patients with tinea pedis, tinea corporis, tinea cruris, pityriasis (tinea versicolor), and cutaneous candidiasis have demonstrated the effectiveness of Ciclopirox one percent cream (now 0.77 percent).

• Because of its high alcohol concentration, gel formulation works well with improved drying.

• Ciclopirox demonstrates antimicrobial and anti-inflammatory characteristics.

• It may not be the most economical option to treat onychomycosis when compared to oral antifungal therapy because nail lacquer needs to be used for nine to 12 months on a daily basis.

• In order to treat seborrheic dermatitis or dandruff, Cicloprix is also available as a shampoo.

What Are the Things to Inform the Doctor Before Taking Ciclopirox?

• Any allergies to Ciclopirox or other medications should be reported to the physician and pharmacist.

• Give out the whole list of all the medications used, including OTC (over-the-counter), prescription, and herbal or vitamin or supplement items.

• Mention, in particular, steroid lotions or ointments, drugs for fungal infections, inhalation steroids, and treatments for seizures.

• Inform the doctor if the patient is pregnant. If a pregnancy develops while taking Ciclopirox, contact the doctor right away.

• If pregnant or planning pregnancy, inform the doctor. Call the doctor immediately if pregnancy occurs while using Ciclopirox.

• If there is a significant burnt or damaged skin region, let the doctor know.

• Dry and clean nails are essential for therapy. Use different instruments for cleaning healthy and sick nails; never share nail care supplies.

• Avoid going barefoot in public places and wear well-fitting, low-heeled shoes with regular nail changes if having afflicted toenails.

• When engaging in activities like sports or being near powerful cleaning agents that could damage or irritate fingernails and toenails, wear protective shoes and gloves.

How Is Ciclopirox Administered?

• Once a day, ideally before going to bed, evenly apply Ciclopirox solution to the nails using the applicator brush and the surrounding skin.

• Be careful to trim the nails correctly before using Ciclopirox.

• Utilize Ciclopirox precisely as prescribed. Never take less or more medication than is recommended.

• Before putting on socks or stockings, wipe off the bottle top, replace it firmly, and allow the solution to dry for about 30 seconds.

• Apply Ciclopirox over the current medication on the nails for the upcoming dose.

• Use a cotton square or piece of tissue soaked in rubbing alcohol to remove Ciclopirox from the nail(s) once a week.

• Be aware that improvement may take six months or longer and that Ciclopirox may not be able to treat nail fungus entirely.

• Follow the doctor's instructions and keep taking the medication as prescribed.

• While receiving treatment, regularly trim the nails by routinely clipping out loose nail material as directed by the doctor.

• Avert contact with the eyes, nose, mouth, and vagina; only apply Cicloprix to the nails and surrounding skin.

• On nails that have been treated, do not apply makeup such as polish.

• Do not take a bath, take a shower, or go swimming for at least eight hours after using Ciclopirox.

• Ciclopirox solution can catch fire; therefore, use caution when applying it near heat sources or open flames like cigarettes.

What Are the Side Effects of Ciclopirox?

• Rare occurrences of burning sensation, irritation, redness, pain, or pruritus with minimal therapy discontinuation.

• Allergic contact dermatitis to Ciclopirox is rare, with only isolated anecdotal reports.

• Common side effects include redness at the application site.

• Serious and uncommon side effects include irritation, itching, burning, blistering, swelling, or oozing at the application site.

• Pain in the treated nail(s) or the surrounding area.

• Discoloration or change in the shape of nail(s).

• Ingrown nails.

Missed Dose:

• When an individual forgets to take a medication, they should take it as soon as they do.

• When it is time for the next dose, skip the missed one and continue on the regular schedule.

• Never take two doses to make up for one that has been missed.

Overdose:

Ciclopirox topical overdose is not harmful. But before taking the medication, speak with the doctor.

Storage:

• Keep this medication out of the reach of children, especially those that are in non-child-resistant packaging and in its original, tightly-sealed container.

• Use safety caps and store medications in a secure, elevated place to prevent accidental ingestion by young children.

• Do not freeze; store at 15 to 30 degrees Celsius (59 to 86 degrees Fahrenheit).

• Avoid overheating and wetness by keeping it at room temperature (not in the bathroom).

• Keep the bottle sealed and out of direct sunlight.

• Safely dispose of any unnecessary medication to stop dogs or other people from accidentally consuming it.

• When possible, employ a medication take-back program rather than flushing it down the toilet.

• For disposal choices, speak with the neighborhood recycling and trash department or pharmacy.

For Doctors:

Indication:

• Dermatophytic (Tinea) Infections: Comparable to Clotrimazole, one percent Ciclopirox cream showed better mycological and overall response rates in tinea corporis or cruris.

• Tinea Pedis: Ciclopirox gel was found to be more effective in lowering signs and symptoms, obtaining a higher mycologic cure, complete cure, and bacterial count reduction in a randomized clinical investigation.

• Pityriasis Versicolor (PV): One proven effective and safe treatment for PV is one percent Ciclopirox cream administered twice daily for 14 days.

• Seborrheic Dermatitis (SD): Based on consistent efficacy in high-quality RCTs (randomized, controlled trials), which demonstrated better outcomes than placebo, topical Ciclopirox was strongly recommended for face SD. When it came to lowering the severity scores of atopic dermatitis of the head and neck, Ciclopirox cream outperformed a placebo.

• Vulvovaginal Candidiasis (VVC): Due to its antifungal action against common candida species and efficacy against azole-resistant Candida species, Ciclopirox has been a well-liked treatment for Vancomycin-induced candidiasis. In mixed genital infections, Ciclopirox cream and pessaries exhibited comparable efficaciousness to Miconazole, Terconazole creams, and Clotrimazole vaginal tablets.

• Extravaginal Candidal Infection: A one percent cream of Ciclopirox outperformed a placebo in a randomized controlled trial, and its total cure rates were higher than those of Clotrimazole. A statistically significant improvement in severity scores and mycological cure was observed in newborns when a topical suspension of 0.77 percent Ciclopirox was administered twice a day for seven days.

• Pediatric Population: In children aged three months to ten years, one percent Ciclopirox cream was found to be a safe and effective treatment for superficial cutaneous mycotic infections, particularly those caused by Candida species. This information was based on phase III research.

Dosing Considerations:

• Onychomycosis - Fingernail (Adults): All affected nails and surrounding skin should get a once-daily application of eight percent topical solution, ideally at nighttime or eight hours before washing. The entire nail plate and five millimeters (mm) of surrounding skin should be equally covered. Reapply over the prior coat and use alcohol to remove it every seven days instead of removing the product every day. A full course of therapy can result in clear or nearly clear nails after up to 48 weeks of professional removal and daily treatments.

• Onychomycosis - Toenail (Adults): Same application as for fingernails.

• Seborrheic Dermatitis (Adults): Apply 0.77 percent topical gel twice a day for four weeks to the afflicted areas of the scalp. Apply roughly five mL (milliliters) of topical shampoo to the scalp after wetting the hair, and let it sit for three minutes. Repeat twice a week for four weeks.

• Cutaneous Candidiasis (Adults): Apply a topical cream or suspension with 0.77 percent on afflicted and adjacent skin areas twice a day. Improvement in clinical status typically happens in the first week.

• Tinea Cruris (Adults): Treat afflicted and surrounding skin areas twice a day with a topical cream or suspension containing 0.77 percent. Within the first week, there is a clinical improvement and symptom reduction.

• Tinea Versicolor (Adults): Apply a 0.77 percent topical cream or solution twice a day to the skin areas that are afflicted and the surrounding skin. Improvement in clinical status typically happens in the first week.

• Tinea Corporis (Adults): The same protocol as that for tinea cruris. For four weeks, treat interdigital tinea pedis and tinea corporis with 0.77 percent topical gel.

• Tinea Pedis (Adults): Use the same treatment as for tinea cruris for tinea pedis. For four weeks, treat interdigital tinea pedis and tinea corporis with 0.77 percent topical gel.

• Onychomycosis - Fingernail (Pediatric, 12 Years or Older): Use the same treatment as for adult fingernails.

• Onychomycosis - Toenail (Pediatric, 12 Years or Older): Apply the same treatment as for adult toenails.

• Seborrheic Dermatitis (Pediatric, 16 Years or Older): The same treatment is used in adults.

• Cutaneous Candidiasis (Pediatric, 10 Years or Older): The same treatment is used for cutaneous candidiasis in adults as it is in children aged ten or older.

• Tinea Cruris (Pediatric, 10 Years or Older): Use the same treatment as in adults.

• Tinea Versicolor (Pediatric, 10 Years or Older): Apply the same treatment as for adult tinea versicolor.

• Tinea Corporis (Pediatric, 10 Years or Older): Use the same treatment as in adults. For interdigital tinea pedis and tinea corporis, apply 0.77 percent topical gel and treat for four weeks.

• Tinea Pedis (Pediatric, 10 Years or Older): Use the same treatment as in adults. For interdigital tinea pedis and tinea corporis, apply topical gel containing 0.77 percent and treat for four weeks.

What Are the Pharmacological Aspects of Ciclopirox?

• Pharmacodynamics: Broad-spectrum antifungal Ciclopirox also has antibacterial and anti-inflammatory qualities. Its strong affinity for trivalent cations is its main mechanism of action, which inhibits vital cofactors of enzymes. Ciclopirox exhibits fungicidal or fungistatic action in vitro against a range of fungal species, such as actinomycetes, dermatophytes, yeasts, and dimorphic fungi. It demonstrates antibacterial action against a variety of gram-positive and gram-negative bacteria in addition to its broad antifungal spectrum. Furthermore, Ciclopirox inhibits the formation of prostaglandin and leukotriene, which have anti-inflammatory properties, in human polymorphonuclear cells. It reduces inflammation even further by preventing the synthesis of cyclooxygenase and 5-lipoxygenase.

• Mechanism of Action: Ciclopirox is thought to work by chelating polyvalent metal cations, such as Fe3+ (ferric cation) and Al3+ (aluminum cation), which inhibits a number of enzymes, including cytochromes, which are metal-dependent enzymes responsible for peroxide degradation within fungal cells. This alteration of the fungal plasma membrane alters internal structures and disrupts cellular functions like mitochondrial electron transport and energy production. This is in contrast to antifungals like Itraconazole and Terbinafine, which affect sterol synthesis. Its anti-inflammatory properties are probably due to inhibition of cyclooxygenase and 5-lipoxygenase. Ciclopirox may also interfere with signals related to cell division, DNA (deoxyribonucleic acid) repair, and intracellular transport components such as mitotic spindles. In vitro experiments showed that Ciclopirox inhibited the release of PGE2 (prostaglandin E2) in a cell culture model, as well as the 5-lipoxygenase inflammatory mediators 5-HETE (5-hydroxyeicosatetraenoic acid) and LTB4 (leukotriene B4). In an arachidonic acid-induced mouse ear edema model, Ciclopirox successfully reduced inflammation in vivo. The clinical importance of these observations is still up for debate.

• Pharmacokinetics: The pharmacokinetics of 0.77 percent Ciclopirox Gel and Ciclopirox Cream, in an examination of 18 healthy males, showed that the gel had a higher systemic absorption of Ciclopirox than the cream. Five grams of Ciclopirox Cream generated 18.62 (±13.56) ng/mL total Ciclopirox, while five grams of Ciclopirox Gel produced a mean (±SD (standard deviation)) peak serum concentration of 25.02 (±20.6) ng/mL (nanogram per milliliter) total Ciclopirox. In 48 hours, about three percent of the administered Ciclopirox was eliminated in the urine, with a 5.5-hour renal elimination half-life. 16 males participated in a tinea cruris trial, applying around 15 grams of Ciclopirox Gel daily for 14.5 days. The mean (+SD) dose-normalized Cmax values were 100 (+42) ng/mL on day one and 238 (+144) ng/mL on day 15. In the ten hours following dosage on day one, about ten percent of the given amount was eliminated in the urine.

Warnings and Precautions:

• As the medication may include inactive substances that could trigger allergic reactions, let the pharmacist or healthcare professional know about any known allergies before starting Ciclopirox treatment.

• Before utilizing this drug, give the doctor or pharmacist a complete medical history.

• It is important for anyone contemplating surgery to let their doctors or dentists know about everything they use, including over-the-counter, prescription, and herbal medications.

• Use this drug sparingly during pregnancy, and talk to the doctor about the advantages and disadvantages.

• Before nursing a baby, see the doctor because it is unknown if Ciclopirox topical enters the breast milk.

• Adherence to the directions on the label and package of the medication is essential. Let all medical professionals know about any allergies, current prescriptions, and medical problems.

• Do not apply Ciclopirox topical on a child without consulting a physician.

• Age limits apply to some formulations which are not recommended for use are as follows:

1. Shampoo and Gel - Below 16 years.

2. Nail Lacquer - Below 12 years.

3. Cream and Lotion - Below 10 years.