Momeking Ht

Uses

Hydroquinone is used -

• For the gradual bleaching of hyperpigmented skin conditions such as chloasma, melasma, freckles, senile lentigines and other unwanted areas of melanin hyperpigmentation.
• To reduce hyperpigmentation caused by photosensitization associated with inflammation or with the use of certain cosmetics.

Mometasone furoate is a corticosteroid used to treat asthma, allergic rhinitis, nasal congestion, nasal polyps, dermatitis, and pruritus.

There are 3 formulations of mometasone furoate with various indications. The inhaler is indicated for prophylaxis of asthma in patients ≥4 years. The nasal spray is indicated for treating nasal symptoms of allergic rhinitis in patients ≥2 years, treating symptoms of nasal congestion from seasonal allergic rhinitis in patients ≥2 years, treating nasal polyps in patients ≥18 years, and prophylaxis of seasonal allergic rhinitis in patients ≥12 years. The ointment is indicated for symptomatic treatment of dermatitis and pruritis in patients ≥2 years.

• For the treatment of acne vulgaris in which comedones, papules and pustules predominate.
• For the treatment of hyperpigmentation, roughness and fine wrinkling of photodamaged skin due to chronic sun exposure.
• For the treatment of Acute promyelocytic leukaemia

Momeking Ht is also used to associated treatment for these conditions: Acne Vulgaris, Melasma, Skin hyperpigmentation, Moderate Melasma, Severe MelasmaAllergic Rhinitis (AR), Asthma, Dermatitis, Dermatitis, Eczematous caused by superficial Fungal skin infection, Moderate to Severe Plaque Psoriasis, Polyps, Nasal, Pruritus, Psoriasis, Psoriasis, Moderate to Severe, Seasonal Allergies, Skin Diseases, Eczematous, Skin InfectionsAcne Vulgaris, Alopecia, Cornification and dystrophic skin disorders, FAB classification M3 Acute promyelocytic leukemia, Skin hyperpigmentation, Solar Lentigines, Facial fine wrinkling, Keratinization disorders of the feet, Keratinization disorders of the hand, Moderate Melasma, Mottled hyperpigmentation, Severe Melasma, Severe, recalcitrant Cystic acne, Tactile roughness of facial skin

How Momeking Ht works

Hydroquinone reduces melanin pigment production through inhibition of the tyrosinase enzyme, which is involved in the initial step of the melanin pigment biosynthesis pathway. Hydroquinone takes several months to take effect.

In asthma, mometasone is believed to inhibit mast cells, eosinophils, basophils, and lymphocytes. There is also evidence of inhibition of histamine, leukotrienes, and cytokines.

Corticosteroids diffuse across cell membranes into the cytosol of cells where they bind to glucocorticoid receptors to produce their activity. Mometasone furoate has a particularly high receptor affinity compare to other corticosteroids, 22 times higher than that of dexamethasone. Mometasone furoate binding to a glucocorticoid receptor causes conformational changes in the receptor, separation from chaperones, and the receptor moves to the nucleus. Once at the nucleus, receptors dimerize and bind to a DNA sequence known as the glucocorticoid response element which either increases expression of anti-inflammatory molecules or inhibits expression of pro-inflammatory molecules (such as interleukins 4 and 5). Mometasone furoate also reduces inflammation by blocking transcription factors such as activator-protein-1 and nuclear factor kappa B (NF-kappaB).

Tretinoin binds to alpha, beta, and gamma retinoic acid receptors (RARs). RAR-alpha and RAR-beta have been associated with the development of acute promyelocytic leukemia and squamous cell cancers, respectively. RAR-gamma is associated with retinoid effects on mucocutaneous tissues and bone. Although the exact mechanism of action of tretinoin is unknown, current evidence suggests that the effectiveness of tretinoin in acne is due primarily to its ability to modify abnormal follicular keratinization. Comedones form in follicles with an excess of keratinized epithelial cells. Tretinoin promotes detachment of cornified cells and the enhanced shedding of corneocytes from the follicle. By increasing the mitotic activity of follicular epithelia, tretinoin also increases the turnover rate of thin, loosely-adherent corneocytes. Through these actions, the comedo contents are extruded and the formation of the microcomedo, the precursor lesion of acne vulgaris, is reduced. Tretinoin is not a cytolytic agent but instead induces cytodifferentiation and decreased proliferation of APL cells in culture and in vivo. When Tretinoin is given systemically to APL patients, tretinoin treatment produces an initial maturation of the primitive promyelocytes derived from the leukemic clone, followed by a repopulation of the bone marrow and peripheral blood by normal, polyclonal hematopoietic cells in patients achieving complete remission (CR). The exact mechanism of action of tretinoin in APL is unknown.

Dosage

Momeking Ht dosage

Apply a thin film of Hydroquinone Cream to the effected area once daily, at least 30 minutes before bedtime. Gently wash the face and neck with a mild cleanser. Rinse and pat the skin dry. Apply Hydroquinone Cream to the hyperpigmented areas of melasma including about ½ inch of normal appearing skin surrounding eachlesion. Rub lightly and uniformly into the skin.

Therapy should be discontinued when control is achieved. During the day, use asunscreenof SPF 30, and wear protective clothing. Avoid sunlight exposure. Patients may use moisturizers and/or cosmetics during the day. Hydroquinone Cream is for topical use only. It is not for oral,ophthalmic, or intravaginal use.

Tretinoin cream: Tretinoin cream should be applied sparingly to the whole affected area once or twice daily. The skin should be thoroughly cleaned and dried before application. Patient should be advised that 6 to 8 weeks of treatment may be required before a therapeutic effect is observed. Moisturisers and cosmetics may be used during treatment with Cosmotrin cream but should not be applied to the skin at the same time. Astringent toiletries should be avoided.

Tretinoin gel: Tretinoin gel should be applied once or twice a day, before retiring, to the skin where lesions appear, using enough to cover the entire affected area lightly. The frequency of application can be adjusted to obtain maximum clinical efficacy with minimal erythema and scaling.

If Tretinoin gel is applied excessively, no more rapid or better results will be obtained and marked redness, peeling or discomfort may occur. Should this occur accidentally or through over-enthusiastic use, application should be discontinued for few days.

Patience is needed in this treatment, since the therapeutic effects will not usually be observed until after 6-8 weeks of treatment. During the early weeks of treatment, an apparent exacerbation of inflammatory lesions may occur. This is due to the action of the medication on deep, previously unseen comedones and papules. Once the acne lesions have responded satisfactorily, it should be possible to maintain the improvement with less frequent applications.

Moisturizers and cosmetics may be used during treatment with Tretinoin gel but should not be applied to the skin at the same time. The skin should be thoroughly washed before application of Tretinoin gel. Astringent toiletries should be avoided.

Capsule: The recommended dose is 45 mg/m2/day administered as two evenly divided doses until complete remission is documented. Therapy should be discontinued 30 days after achievement of complete remission or after 90 days of treatment, whichever occurs first.

If after initiation of treatment of Tretinoin the presence of the translocation is not confirmed by cytogenetics and/or by polymerase chain reaction studies and the patient has not responded to Tretinoin, alternative therapy appropriate for acute myelogenous leukemia should be considered.

Side Effects

No systemic adverse reactions have been reported. Occasional hypersensitivity (localized contact dermatitis) may occur in which case the medication should be discontinued.

True allergic contact dermatitis is rare but a primary irritant dermatitis, manifesting itself as irritation, erythema, peeling and sensation of warmth, is common. Slight stinging is common as a mild reaction in many people but usually settles with continuous use and/or reduction in the frequency of application of the drug.

Toxicity

Overdose with a mometasone furoate inhaler may occur with chronic overuse. Symptoms of chronic overuse may present as hypercorticism and adrenal suppression, and patients may not require any more treatment than monitoring.

In animal studies of pregnancy, some fetal toxic effects were seen at or above the maximum recommended human dose, though rodents are more sensitive to these effects than humans. The benefits and risks of use should be considered in pregnant patients

It is unknown if mometasone furoate is excreted in breast milk but other corticosteroids are and therefore caution should be exercised when administering to nursing mothers.

Safety and effectiveness in pediatric populations has been established through clinical trials, though there may be a reduction in expected growth of about 1cm per year depending on the dose and duration of treatment. Pediatric patients should be titrated to the lowest effective dose for mometasone furoate inhalers.

A trial of geriatric patients showed no difference in safety or efficacy compared to younger patients, however patients of an even greater age may still be more sensitive to mometasone furoate.

The use of a mometasone furoate inhaler in moderate or severe hepatic impairment rarely leads to detectable plasma concentrations though caution may be prudent with increasing degrees of severity.

The effects of mometasone furoate in renal impairment, and across gender and race have not been studied.

Precaution

Hydroquinone is a skin bleaching agent which may produce unwanted cosmetic effects if not used as directed. The physician should be familiar with the contents of this insert before prescribing or dispensing this medication.

Test for skin sensitivity before using by applying a small amount to an unbroken patch of skin to check in 24 hours. Minor redness is not a contraindication, but where there is itching or vesicle formation or excessive inflammatory response, further treatment is not advised. If no bleaching or lightening effect is noted after 2 months of treatment, the medication should be discontinued.

Contact with the eyes and lips should be avoided. Hydroquinone should not be applied to cut or abraded skin.

Interaction

Particular caution should be exercised in using preparations containing peeling agents (i.e. sulfur, resorcinol, benzoyl peroxide or salicylic acid). Use of topical preparations with high concentrations of alcohol, menthol, spices or lime- such as shaving lotions, astringents and perfume- should be avoided, especially during initial therapy.

Volume of Distribution

Steady state volume of distribution of 152L.

Elimination Route

1-31% (topical)

Half Life

The terminal half life of an inhaled dose is approximately 5 hours though it has been reported as 5.8 hours by other sources.

0.5-2 hours

Clearance

The clearance rate of mometasone furoate is not readily available, though it may be close to 90L/h.

Elimination Route

For an inhaled dose, approximately 74% is excreted in the feces and 8% is excreted in the urine.

Pregnancy & Breastfeeding use

Pregnancy Category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Lactation: It is not known whether topical hydroquinone is absorbed or excreted in human milk. Caution is advised when topical hydroquinone is used by a nursing mother.

Tretinoin is contraindicated in pregnancy or suspected pregnancy. The drug should be avoided by breast feeding mothers.

Contraindication

Hydroquinone is contraindicated to patients with prior history of hypersensitivity or allergic reaction to hydroquinone or other ingredients in the preparation.

Tretinoin is contraindicated in patients who are allergic to this drug. It is contraindicated in pregnancy or suspected pregnancy. It is also contraindicated in personal or familial history of cutaneous epithelioma.

Local irritation: The presence of cutaneous irritative signs (e.g. erythema, peeling, pruritus, sunburn, etc.) should prohibit initiation or recommencement of treatment with Tretinoin until the symptoms resolve. Tretinoin has been reported to cause severe irritation on eczematous skin and should be used with caution in patients with this condition.

Exposure to sunlight: Exposure to sunlight, including ultraviolet sun-lamps, should be avoided or minimised during the use of Tretinoin.

General precaution: Before application of Tretinoin, areas to be treated should be cleansed thoroughly. Abstain from washing the treated area frequently; twice daily is sufficient. Use of mild soap is recommended. Dry the skin without rubbing.

Avoid contact with eyes, eyelids, nostrils, mouth and mucous membranes. If contact in these areas occurs, careful washing with water is recommended.

Acute Overdose

There have been no systemic reactions from the use of topical hydroquinone. Some patients may experience a transient reddening of skin and mild burning sensation which does not preclude treatment.

Storage Condition

Store between 20-25° C. Protect from light.

Store in a cool and dry place, away from light. Keep out of reach of children.

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