Stieproxal

Stieproxal Uses, Dosage, Side Effects, Food Interaction and all others data.

Ciclopirox Olamine is a synthetic, broad-spectrum, antifungal agent. The chemical name is 6-cyclohexyl-1-hydroxy-4-methyl-2(1H)-pyridone, 2-aminoethanol salt.

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

Salicylic acid has a potent keratolytic action and a slight antiseptic action when applied topically. It softens and destroys the stratum corneum by increasing endogenous hydration which causes the horny layer of the skin to swell, soften, and then desquamate. At high concentrations, salicylic acid has a caustic effect. It also possesses weak antifungal and antibacterial activity.

Salicylic acid treats acne by causing skin cells to slough off more readily, preventing pores from clogging up. This effect on skin cells also makes salicylic acid an active ingredient in several shampoos meant to treat dandruff. Use of straight salicylic solution may cause hyperpigmentation on unpretreated skin for those with darker skin types (Fitzpatrick phototypes IV, V, VI), as well as with the lack of use of a broad spectrum sunblock. Subsalicylate in combination with bismuth form the popular stomach relief aid known commonly as Pepto-Bismol. When combined the two key ingredients help control diarrhea, nausea, heartburn, and even gas. It is also very mildly anti-biotic.

Stieproxal
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Stieproxal
Generic	Ciclopirox + Salicylic Acid
Weight	1.5%w/v, 3%w/v
Type	Liquid
Therapeutic Class
Manufacturer	Glaxosmithkline
Available Country	Pakistan
Last Updated:	September 19, 2023 at 7:00 am

Uses

Ciclopirox cream is used for the topical treatment of the following dermal infections:Tinea pedis, tinea cruris, and tinea corporis due to Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum and Microsporum canis Candidiasis moniliasis) due to Candida albicans; and tinea (pityriasis) versicolor due to Malassezia furfur.

6% Salicylic Acid: This topical preparations treat the following common scaly conditions:

Chronic atopic dermatitis
Lichen simplex
Psoriasis
Seborrhoeic dermatitis
Ichthiosis

12% Salicylic Acid: This topical preparations treat the following common scaly conditions:

Warts (small excessive growths of skin caused by a type of virus. Warts often occur on the fingers or on the back of the hands).
Verruca (occurs only on the sole of the feet and can be painful. It often looks like a small white ring of skin with a black dot in the centre).
Corns and Calluses (are hard, thick pads of skin caused by pressure and friction. They usually occur on the feet due to poorly fitting shoes and can occur on the hands).

Stieproxal is also used to associated treatment for these conditions: Fungal skin infection, Pityriasis versicolor, Seborrheic dermatitis of the scalp, Tinea Corporis, Tinea Cruris, Tinea Pedis, Vulvovaginal Candidiasis, Cutaneous candidiasis, Mild Onychomycosis, Moderate OnychomycosisAcne, Actinic Keratosis (AK), Alopecia Areata (AA), Atopic Dermatitis (AD), Blackheads, Chronic Eczema, Chronic cutaneous lupus erythematosus, Corns, Dandruff, Dermatitis, Contact, Dermatitis, Eczematous, Dermatitis, Eczematous of the scalp, Discoid Lupus Erythematosus (DLE), Foot Callus, Fungal skin infection, Furuncle, Hand Eczema, Hyperkeratosis, Hyperkeratosis follicularis et parafollicularis, Infections, Fungal, Infections, Fungal of the Skin Folds, Infections, Fungal of the face, Infections, Fungal of the feet, Infections, Fungal of the hand, Keratosis Palmaris et Plantaris, Lichen, Lichen Plano-Pilaris, Lichen Planus (LP), Lichen simplex chronicus, Molluscum Contagiosum, Musculoskeletal Pain, Neurodermatitis, Palmo-Plantar Pustulosis, Plantar Warts, Pruritus, Psoriasis, Psoriasis Vulgaris (Plaque Psoriasis), Psoriasis of the scalp, Rash, Ringworm of the Skin, Ringworm of the scalp, Seborrheic Dermatitis, Seborrhoeic Dermatitis of the Scalp, Skin Infections, Bacterial, Verrucous Psoriasis, Warts, Calluses, Corticosteroid-responsive dermatoses, Keratinization disorders, Scaling, Scaling of skin, Scalp seborrhea, Superficial Fungal skin infection, Keratolysis

How Stieproxal works

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. Ciclopirox 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. ciclopirox may exert its effect by disrupting DNA repair, cell division signals and structures (mitotic spindles) as well as some elements of intracellular transport.

Salicylic acid directly irreversibly inhibits COX-1 and COX-2 to decrease conversion of arachidonic acid to precursors of prostaglandins and thromboxanes. Salicylate's use in rheumatic diseases is due to it's analgesic and anti-inflammatory activity. Salicylic acid is a key ingredient in many skin-care products for the treatment of acne, psoriasis, calluses, corns, keratosis pilaris, and warts. Salicylic acid allows cells of the epidermis to more readily slough off. Because of its effect on skin cells, salicylic acid is used in several shampoos used to treat dandruff. Salicylic acid is also used as an active ingredient in gels which remove verrucas (plantar warts). Salicylic acid competitively inhibits oxidation of uridine-5-diphosphoglucose (UDPG) with nicotinamide adenosine dinucleotide (NAD) and noncompetitively with UDPG. It also competitively inhibits the transferring of the glucuronyl group of uridine-5-phosphoglucuronic acid (UDPGA) to a phenolic acceptor. Inhibition of mucopoly saccharide synthesis is likely responsible for the slowing of wound healing with salicylates.

Dosage

Stieproxal dosage

Gently massage Ciclopirox cream into the affected and surrounding skin areas twice daily, in the morning and evening for four weeks. Clinical improvement with relief of pruritus and other symptoms usually occurs within the first week of treatment. If a patient shows no clinical improvement after four weeks of treatment, the diagnosis should be redetermined. Patients with tinea versicolor usually exhibit clinical and mycological clearing after two weeks of treatment.

Topical/Cutaneous (Adult)-

Hyperkeratotic and scaling skin conditions: As 1.8-3% preparation: Apply to affected area of the skin and/or scalp 1-4 times daily.

Acne: As 0.5-2% preparation: Apply thinly to affected area 1-3 times daily, reduce to once daily or every other day if dryness or peeling occur.

Warts and calluses:

As 12-40% plaster: Fit over the wart/callus for 48 hr, repeat process 48 hrly as needed until wart/callus is removed (up to 12 wk for warts or up to 14 days for calluses).
As 5-17% preparation in collodion-like vehicle: Apply a small amount to sufficiently cover wart/callus and allow to dry. Repeat 1-2 times daily until wart/callus is removed (up to 12 wk for warts or up to 14 days for calluses).
As 15% preparation in karaya gum-glycol plaster vehicle: Smoothen warts with emery board and place a drop of warm water prior to application. Apply the plaster in the evening and leave in place for at least 8 hr to be removed in the morning. Repeat process 24 hrly, if necessary up to 12 wk.

Ciclopirox cream is not for ophthalmic use.

Side Effects

Ciclopirox Olamine cream is well tolerated with a low incidence of side effects. The most frequently reported events are itching, redness, burning, dryness, or irritation of treated skin.

An allergic reaction (shortness of breath, closing of the throat, swelling of the lips, face or tongue or hives) or severe skin irritation.

Toxicity

Oral LD₅₀ in rat is >10 ml/kg. Symptoms of overexposure include drowsiness and headache.

Oral rat LD50: 891 mg/kg. Inhalation rat LC50: > 900 mg/m3/1hr. Irritation: skin rabbit: 500 mg/24H mild. Eye rabbit: 100 mg severe. Investigated a mutagen and reproductive effector.

Precaution

If a reaction suggesting sensitivity or chemical irritation occurs with the use of Ciclopirox Cream, treatment should be discontinued and appropriate therapy instituted.

For external use only. Avoid contact with eyes and other mucous membranes.

Interaction

There are no known drug interactions and none well documented.

Do not use other topical preparations on the treated area unless otherwise directed by your healthcare provider. They may interfere with treatment or increase skin irritation.

Volume of Distribution

The volume of distribution is about 170 mL/kg of body weight.

Elimination Route

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.

Half Life

1.7 hours for 1% topical solution.

Elimination Route

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.

About 10% is excreted unchanged in the urine.

Pregnancy & Breastfeeding use

Pregnancy Category B. There are no adequate or well-controlled studies in pregnant women. Therefore, Ciclopirox cream should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Lactation: It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Ciclopirox cream is administered to nursing women.

Pregnancy Category C. If used by nursing mothers, it should not be used on the chest area to avoid accidental contamination of the child.

Contraindication

Ciclopirox Olamine cream is contraindicated in individuals who have shown hypersensitivity to any of its components.

It should not be used in any patient known to be sensitive to Salicylic Acid or any other listed ingredients.

Special Warning

Salicylic Acid is used in children over 2 years.

Acute Overdose

An overdose of Salicylic Acid topical is unlikely to occur. If you do suspect an overdose or if the medication has been ingested, call a poison control center or emergency room for advice.