Melapik Ever

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

Allantoin is a substance that is endogenous to the human body and also found as a normal component of human diets . In healthy human volunteers, the mean plasma concentration of allantoin is about 2-3 mg/l. During exercise, the plasma allantoin concentration rapidly increases about two fold and remains elevated . In human muscle, urate is oxidized to allantoin during such exercise . The concentration of allantoin in muscles increases from a resting value of about 5000 ug/kg to about 16000 ug/kg immediately after short-term exhaustive cycling exercise .

More specifically, allantoin is a diureide of glyoxylic acid that is produced from uric acid. It is a major metabolic intermediate in most organisms. Allantoin is found in OTC cosmetic products and other commercial products such as oral hygiene products, in shampoos, lipsticks, anti-acne products, sun care products, and clarifying lotions . Allantoin has also demonstrated to ameliorate the wound healing process in some studies .

There is no well controlled and appropriate data that can formally substantiate the pharmacodynamic properties of allantoin . Nevertheless, ongoing studies suggest that allantoin possesses moisturizing and keratolytic effects, as well as abilities to increase the water content of the extracellular matrix and enhance the desquamation of upper layers of dead skin cells, all of which are activities that can promote cell proliferation and facilitate wound healing .

Hydroquinone is a topical depigmentating agent that produces a reversible depigmentation of the skin by inhibiting enzymatic oxidation of tyrosine to 3,4-dihydroxyphenylalanine and suppressing melanocyte metabolic processes.

Tretinoin is structurally and pharmacologically related to vitamin A. Current evidence suggests that topical Tretinoin decreases cohesiveness of follicular epithelial cells with decreased microcomedone formation. Additionally, Tretinoin stimulates mitotic activity and increases turnover of follicular epithelial cells, causing extrusion of the comedones

Tretinoin, also known as all-trans-retinoic acid (ATRA), is a naturally occurring derivative of vitamin A (retinol). Retinoids such as tretinoin are important regulators of cell reproduction, proliferation, and differentiation and are used to treat acne and photodamaged skin and to manage keratinization disorders such as ichthyosis and keratosis follicularis. Tretinoin also represents the class of anticancer drugs called differentiating agents and is used in the treatment of acute promyelocytic leukemia (APL).

Trade Name Melapik Ever
Generic Tretinoin + Allantoin + Hydroquinone
Weight 0.0125%, 1%, 2%
Type Cream
Therapeutic Class
Manufacturer Klm Laboratories Pvt Ltd
Available Country India
Last Updated: September 19, 2023 at 7:00 am
Melapik Ever
Melapik Ever

Uses

Allantoin is an ingredient used in skin care products to relieve irritation and protect minor cuts, scrapes, and burns.

Allantoin is commonly applied in a variety of topical vehicles or applications such as cosmetic creams, toothpastes, mouthwashes, shampoos, lipsticks, anti-acne products, and lotions for the purpose of moisturizing skin, enhancing the smoothness of skin, stimulating the healing of wounds, and soothing irritated skin .

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.
  • 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

Melapik Ever is also used to associated treatment for these conditions: Scarring, Dental cleaning, Skin Lightening, Skin protectionAcne Vulgaris, Melasma, Skin hyperpigmentation, Moderate Melasma, Severe MelasmaAcne 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 Melapik Ever works

There is no well controlled data that can formally substantiate the method of action . However, ongoing studies suggest that there may exist a histological wound healing profile induced by allantoin in rats that leads to the amelioration and fastening of the reestablishment of normal skin . This facilitation of wound healing is supported by observations that wounds inflicted to rat subjects to which topical allantoin preparations were applied histologically demonstrated increased vasodilation, presence of inflammatory exudates, number of inflammatory cells, angiogenesis, fibroblast proliferation, and increased collagen deposition when compared to rat subjects with wounds that did not receive any allantoin administration .

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.

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

Melapik Ever 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

No studies on repeated dose toxicity and reproductive toxicity have been submitted. Moreover, studies show that the tumor incidence in allantoin treated animals did not differ largely from that found in untreated controls. As a result, further or additional toxicity, mutagenicity, or carcinogenicity tests are not required in view of the endogenous nature of allantoin and the general lack of overall toxicity .

Finally, as allantoin is a normal component of the diet in humans and is a substance of endogenous origin present in the body of humans, it is generally recognized as being a safe substance for humans .

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.

Elimination Route

In studies on human subjects, a recovery of 19% and 34% of allantoin in the urine was observed but only in two individuals and only after the administration of massive doses of allantoin . After intravenous administration, recovery in the urine was practically quantitative with doses of 75 to 600 mgm in the human model . After 240 mgm, excretion continued for 72 hours in human subjects and the results were similar in regards to subcutaneous injection .

1-31% (topical)

Half Life

When studied in cattle, sheep, and horses, the half-life of allantoin is in the range of 1 to 2.5 hours .

0.5-2 hours

Clearance

Some studies suggest that the average renal clearance of allantoin in normal, healthy human subjects is approximately 123 cc per minute . It is generally agreed upon that exogenously administered allantoin is rapidly excreted .

Elimination Route

Urinary clearance is the predominant excretion route .

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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