Halskyn M

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

Miconazole topical cream is a broad-spectrum antimycotic which offers a high antifungal activity against dermatophytes, yeasts and other phyco-Asco and Adelomycetes, with a potent antibacterial activity against Gram-positive bacilli and cocci. Miconazole topical cream proved to be markedly effective in secondary infected mycoses, which under other treatments were resistant or reappeared. Miconazole topical cream does not stain skin or clothes.

The active ingredient, Miconazole, is a synthetic imidazole anti-fungal agent with a broad spectrum of activity against pathogenic fungi (including yeast and dermatophytes) and gram-positive bacteria (Staphylococcus and Streptococcus spp). It may act by interfering with the permeability of the fungal cell membranes. When administered orally, Miconazole is incompletely absorbed from the gastrointestinal tract, peak plasma levels of about 1 µg per ml have been achieved after a dose of 1 gm per day. Miconazole is inactivated in the body and 10-20% of an oral dose is excreted in the urine, mainly as metabolites, within 6 days. About 50% of an oral dose may be excreted unchanged in the faeces.

Miconazole is an azole antifungal that functions primarily through inhibition of a specific demethylase within the CYP450 complex. As miconazole is typically applied topically and is minimally absorbed into the systemic circulation following application, the majority of patient reactions are limited to hypersensitivity and cases of anaphylaxis. Patients using intravaginal miconazole products are advised not to rely on contraceptives to prevent pregnancy and sexually transmitted infections, as well as not to use tampons concurrently.

Ulobetasol is a highly potent corticosteroid. It is structurally related to clobetasol. Due to its high potency, it is mainly prescribed in the treatment of severe plaque psoriasis and corticosteroid responsive dermatoses.

Ulobetasol was granted FDA approval on 17 December 1990.

Corticosteroids bind to the glucocorticoid receptor, inhibiting pro-inflammatory signals, and promoting anti-inflammatory signals. Ulobetasol has a moderate duration of action as it is applied once or twice daily. Corticosteroids have a wide therapeutic window as patients may require doses that are multiples of what the body naturally produces. Patients taking corticosteroids should be counselled regarding the risk of hypothalamic-pituitary-adrenal axis suppression and increased susceptibility to infections.

Halskyn M
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	Halskyn M
Generic	Miconazole + Ulobetasol
Type	Cream
Therapeutic Class
Manufacturer	Win-medicare Pvt Ltd
Available Country	India
Last Updated:	September 19, 2023 at 7:00 am

Uses

Miconazole Topical Cream has an antibacterial effect on Gram-positive bacteria, it may be used in mycoses secondarily infected with such bacteria. Skin and nail infections due to dermatophytes, yeasts and other fungi such as: Tinea capitis, corporis, manuum, pedis, barbae, cruris, unguium or onychomycosis. Pityriasis versicolor, candidiasis of skin and nails, stomatitis angularis, otitis externa.

Miconazole Oral treatment and prevention of fungal infections of the oropharynx and gastrointestinal tract, and of super infections due to Gram-positive bacteria.

Ulobetasol is a lipocortin corticosteroid used to treat inflammatory and pruritic corticosteroid-responsive dermatoses.

Ulobetasol cream and ointment are indicated in the treatment of inflammatory and pruritic corticosteroid responsive dermatoses. Ulobetasol lotion is indicated in the treatment of plaque psoriasis.

Halskyn M is also used to associated treatment for these conditions: Acne Vulgaris, Dermatophytosis, Dermatophytosis of nail, Diaper Dermatitis, Excessive sweating and body odor, Fungal skin infection, Gastrointestinal candidiasis, Infection Mixed, Infections, Fungal of the Skin Folds, Nail candida, Oropharyngeal Candidiasis, Pityriasis versicolor, Ringworm, Seborrheic Dermatitis, Skin candida, Tinea Capitis, Tinea Corporis, Tinea Cruris, Tinea Pedis, Vaginal Candidiasis, Cutaneous candidiasisPsoriasis Vulgaris (Plaque Psoriasis), Corticosteroid responsive, Inflammatory Dermatosis, Corticosteroid responsive, pruritic Dermatosis

How Halskyn M works

Miconazole is an azole antifungal used to treat a variety of conditions, including those caused by Candida overgrowth. Unique among the azoles, miconazole is thought to act through three main mechanisms. The primary mechanism of action is through inhibition of the CYP450 14α-lanosterol demethylase enzyme, which results in altered ergosterol production and impaired cell membrane composition and permeability, which in turn leads to cation, phosphate, and low molecular weight protein leakage.

In addition, miconazole inhibits fungal peroxidase and catalase while not affecting NADH oxidase activity, leading to increased production of reactive oxygen species (ROS). Increased intracellular ROS leads to downstream pleiotropic effects and eventual apoptosis.

Lastly, likely as a result of lanosterol demethylation inhibition, miconazole causes a rise in intracellular levels of farnesol. This molecule participates in quorum sensing in Candida, preventing the transition from yeast to mycelial forms and thereby the formation of biofilms, which are more resistant to antibiotics. In addition, farnesol is an inhibitor of drug efflux ABC transporters, namely Candida CaCdr1p and CaCdr2p, which may additionally contribute to increased effectiveness of azole drugs.

The short term effects of corticosteroids are decreased vasodilation and permeability of capillaries, as well as decreased leukocyte migration to sites of inflammation. Corticosteroids binding to the glucocorticoid receptor mediates changes in gene expression that lead to multiple downstream effects over hours to days.

Glucocorticoids inhibit phospholipase 2 and neutrophil apoptosis and demargination, resulting in decreased formation of arachidonic acid derivatives. They also inhibit NF-Kappa B and other inflammatory transcription factors while promoting anti-inflammatory genes like interleukin-10.

Lower doses of corticosteroids provide an anti-inflammatory effect, while higher doses are immunosuppressive. High doses of glucocorticoids for an extended period bind to the mineralocorticoid receptor, raising sodium levels and decreasing potassium levels.

Dosage

Halskyn M dosage

For oral administration: Dosage is based on 15 mg/kg/day.

Adults: 1-2 tea-spoonfuls of gel four times daily
Children aged 6 years and over: One tea-spoonful of gel four times daily
Children aged 2-6 years: One tea-spoonful of gel twice daily
Infants under 2 years: Half tea-spoonful of gel twice daily.

For localised lesions of the mouth:

A small amount of gel may be applied directly to the affected area with a clean finger. For topical treatment of the oropharynx, the gel should be kept in the mouth for as long as possible. Treatment should be continued for up to 2 days after the symptoms have cleared.

For oral candidasis, dental prostheses:

Should be removed at night and brushed with the gel.

The dosage is same for all the ages.

For skin infections: Apply some cream to the lesions twice daily and rub it well with finger until it has fully penetrated the skin. All lesions usually disappear after 2 to 5 weeks. Prolong treatment for some 10 days to prevent relapse.

For nail infections: Clip infected nail as shortly as possible. Apply some cream once daily to the infected nail and rub with your finger, cover nail with a non-perforated occlusive plastic bandage.

Also after loosening of the infected nail (from 2-3 weeks onwards) uniterrupted treatment should be continued until the growth of a new nail has set in and definite cure can be observed (usually after seven months or more).

Side Effects

Topical application of Miconazole Nitrate has almost no side effect.

For oral gel: Occasionally, nausea and vomiting have been reported, and with long term treatment, diarrhoea. In rare instances, allergic reactions have been reported. There are isolated reports of hepatitis, for which the causal relationship with Miconazole has not been established.

Toxicity

Miconazole overdose has not been reported. Patients experiencing an overdose are at an increased risk of severe adverse effects such as headache, skin irritation, diarrhea, nausea, vomiting, abdominal pain, and dysgeusia. Symptomatic and supportive measures are recommended.

Miconazole has an oral LD₅₀ of 500 mg/kg in rats.

Data regarding acute overdoses of glucocorticoids are rare. Chronic high doses of glucocorticoids can lead to the development of cataract, glaucoma, hypertension, water retention, hyperlipidemia, peptic ulcer, pancreatitis, myopathy, osteoporosis, mood changes, psychosis, dermal atrophy, allergy, acne, hypertrichosis, immune suppression, decreased resistance to infection, moon face, hyperglycemia, hypocalcemia, hypophosphatemia, metabolic acidosis, growth suppression, and secondary adrenal insufficiency. Overdose may be treated by adjusting the dose or stopping the corticosteroid as well as initiating symptomatic and supportive treatment.

Precaution

If the concomitant use of Miconazole and anticoagulants is envisaged, the anticoagulant effect should be carefully monitored and titrated. It is advisable to monitor Miconazole and phenytoin levels, if they are used concomitantly. Particularly in infants and young children, caution is required to ensure that the gel does not obstruct the throat. Hence, the gel should not be applied to the back of the throat and the full dose should be divided into smaller portions. Observe the patient for possible choking.

Interaction

Miconazole can inhibit the metabolism of drugs metabolised by the Cytochrome P450-3A and -2C9 families. This can result in an increase or prolongation of their effects, including side effects. Miconazole Oral Gel should not be used during treatment with the following drugs: terfenadine, astemizole,mizolastine, cisapride, triazolam, oral midazolam, dofetilide, quinidine, pimozide, CYP3A4 metabolised HMG-CoA reductase inhibitors such as simvastatin and lovastatin.

Volume of Distribution

A 1200 mg miconazole vaginal suppository resulted in a calculated apparent volume of distribution of 95 546 L while a 100 mg vaginal cream yielded an apparent volume of distribution of 10 911L.

Elimination Route

Miconazole given to healthy volunteers as a single 50 mg oral tablet produced a mean C_max of 15.1 ± 16.2 mcg/mL, a mean AUC_0-24 of 55.2 ± 35.1 mcg*h/mL, and a median T_max of 7 hours (range 2.0-24.1). In these patients measurable plasma concentrations ranged from 0.5 to 0.83 mcg/mL.

Topical miconazole is absorbed poorly into the systemic circulation. In pediatric patients aged 1-21 months given multiple topical applications of miconazole ointment for seven days, the plasma miconazole concentration was less than 0.5 ng/mL in 88% of the patients, with the remaining patients having a concentration of 0.57 and 0.58 ng/mL, respectively. Similarly, patients. administered with a vaginal 1200 mg ovule had a mean C_max of 10.71 ng/mL, mean T_max of 18.4 hours, and mean AUC_0-96 of 477.3 ng*h/mL.

Ulobetasol lotion reaches a C_max of 201.1 ± 157.5 pg/mL, with a T_max of 3 hours, and an AUC of 1632 ± 1147 pg*h/mL. Absorption can be influenced by skin integrity, the vehicle used, inflammation, or disease processes.

Half Life

Miconazole has a terminal half-life of 24 hours.

In vitro experiments show halobetasol propionate, a derivative of ulobetasol, has a half life of 33 minutes.

Elimination Route

Miconazole is excreted through both urine and feces; less than 1% of unchanged miconazole is recovered in urine.

Corticosteroids are eliminated predominantly in the urine.

Pregnancy & Breastfeeding use

In animals, Miconazole has shown no teratogenic effects but is foetotoxic at high oral doses. The significance of this to man is unknown. However, as with other imidazoles, Miconazole Oral Gel should be avoided in pregnant women if possible. The potential hazards should be balanced against the possible benefits. It is not known whether Miconazole is excreted in human milk. Caution should be exercised when prescribing Miconazole Oral Gel to nursing mothers.

Only small amounts of Miconazole cream are absorbed following local administration. However as with other imidazoles, Miconazole nitrate should be used with caution during pregnancy.