Bruximol

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

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

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

Bruximol
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	Bruximol
Availability	Prescription only
Generic	Ciclopirox
Ciclopirox Other Names	Ciclopirox, Ciclopiroxum
Related Drugs	prednisone, dexamethasone, hydrocortisone topical, nystatin topical, clotrimazole topical, ketoconazole topical, terbinafine, terbinafine topical, Decadron, itraconazole
Type	Suppositories
Formula	C₁₂H₁₇NO₂
Weight	Average: 207.2689 Monoisotopic: 207.125928793
Protein binding	Protein binding is 94-97% following topical administration.
Groups	Approved, Investigational
Therapeutic Class	Topical Antifungal preparations
Manufacturer	Scharper Pharmaceuticals (pvt) Ltd,
Available Country	Pakistan
Last Updated:	September 19, 2023 at 7:00 am

Uses

Bruximol 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.

Bruximol 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 Onychomycosis

How Bruximol 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. Bruximol 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.

Dosage

Bruximol dosage

Gently massage Bruximol 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.

Bruximol cream is not for ophthalmic use.

Side Effects

Bruximol 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.

Toxicity

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

Precaution

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

Interaction

There are no known drug interactions and none well documented.

Food Interaction

No interactions found.

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. Bruximol 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.

Pregnancy & Breastfeeding use

Pregnancy Category B. There are no adequate or well-controlled studies in pregnant women. Therefore, Bruximol 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 Bruximol cream is administered to nursing women.