Spotnil Cream 0.01%+4%+0.05%

Uses

This cream is used for the short-term treatment of moderate to severe melasma of the face, in the presence of measures for sun avoidance, including the use of sunscreens.

Spotnil Cream 0.01%+4%+0.05% is also used to associated treatment for these conditions: Acute Otitis Media, Allergy Skin, Anal Fissures, Atopic Dermatitis (AD), Blisters, Chronic Disease of Skin, Dermatosis, Diabetic Macular Edema (DME), External Hemorrhoid, Friction and Pressure Injuries, Hemorrhoids, Internal, Non-infectious Posterior Uveitis Chronic Uveitis, Otitis Externa, Perianal erythema, Pruritus, Psoriasis of the scalp, Purulent Wounds, Scab, Seborrheic dermatitis of the scalp, Skin Infections, Bacterial, Skin Inflammation caused by Bacterial Infections, Skin Inflammation of the ear, Uveitis, Wound Infections, Anal eczema, Chronic eczematous otitis externa, Corticosteroid-responsive dermatoses, Postoperative Care, Perioperative management therapy, Postoperative treatmentAcne 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 Spotnil Cream 0.01%+4%+0.05% works

Fluocinolone acetonide is a corticosteroid and thus, it can be inferred that it acts by inhibiting the edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, fibroblast proliferation, collagen deposition, and scar formation.

Some reports have indicated that fluocinolone acetonide presents a high binding affinity for the glucocorticoid receptor. After binding the receptor, the newly formed receptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements in the promoter region of the target genes. This effect promotes the induction of phospholipase A2 inhibitory proteins (lipocortins). Through this mechanism of action, it is thought that fluocinolone induces mainly one of the lipocortins, annexin 1, which will later mediate the synthesis of inflammatory mediators such as prostaglandins and leukotrienes by inhibiting the release of arachidonic acid which is the precursor of all these inflammatory mediators. Hence, the induction of these proteins will prevent the release of arachidonic acid by phospholipase A2.

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

Spotnil Cream 0.01%+4%+0.05% dosage

Thiscream should be applied once daily at night. It should be applied at least 30 minutes before bedtime. A thin film of the cream should be applied to the hyperpigmented areas of melasma including about ½ inch of normal appearing skin surrounding each lesion.

Cream is for short-term (up to 8 weeks) treatment of moderate to severe melasma of the face. It is not for long-term (more than 8 weeks) or maintenance (continuous) treatment of melasma.

Application procedure:

• Apply this Cream at night, at least 30 minutes before bedtime.
• Gently wash your face with a mild cleanser. Don’t use a washcloth to apply the cleanser, just your fingers. Rinse and pat your skin dry.
• Put a small amount (pea sized or ½ inch or less) of this Cream on your fingertip. Apply a thin coat onto the discolored spot(s). Include about ½ inch of normal skin surrounding the affected area.
• Rub the medicine lightly and uniformly into your skin. The medicine should become invisible almost at once. If you can still see it, you are using too much.
• Do not use more this Cream or apply it more often than recommended by your doctor. Too much this Cream may irritate your skin and won’t give any faster or better results.
• Do not cover the treated area with anything after applying this Cream.
• You may also use a moisturizer and cosmetics during the day.
• Use a sunscreen of at least SPF 30 and a wide-brimmed hat or umbrella over the treated areas to protect from sun.

Side Effects

The most frequently reported events were erythema, desquamation, burning, itching, irritation, dryness, hypopigmentation, perioral dermatitis, allergic contact dermatitis, secondary infection, and skin atrophy at the site of application. The majority of these events were mild to moderate in severity.

Toxicity

Studies to determine the carcinogenic and its effect in fertility have not been performed. It is important to consider that several corticosteroids have been shown to present genotoxic potential but fluocinolone acetonide was shown to not be genotoxic in the Ames test and mouse lymphoma TK assay.

Precaution

This cream contains hydroquinone and tretinoin that may cause mild to moderate irritation such as skin reddening, peeling, mild burning sensation, dryness, and pruritus. Transient skin reddening or mild burning sensation does not preclude treatment. If a reaction suggests hypersensitivity or chemical irritation, the use of the medication should be discontinued.

This cream also contains the corticosteroid fluocinolone acetonide. Systemic absorption of topical corticosteroids can produce reversible hypothalamic-pituitary-adrenal (HPA) axis suppression with the potential for glucocorticosteroid insufficiency after withdrawal of treatment. Manifestations of Cushing’s syndrome, hyperglycemia, and glucosuria can also be produced by systemic absorption of topical corticosteroid while on treatment. If HPA axis suppression is noted, the use of this cream should be discontinued.

Interaction

Patients should avoid medicated or abrasive soaps and cleansers, soaps and cosmetics with drying effects, products with high concentration of alcohol and astringent, and other irritants or keratolytic drugs while on this cream treatment.

Volume of Distribution

This pharmacokinetic parameter is not relevant as the systemic absorption of fluocinolone acetonide is very minimal.

Elimination Route

When administered as an eye implant, fluocinolone acetonide presents a sustained delivery for even 12 months in which there can be observed a sustained release. The concentration of fluocinolone acetonide are generally higher in the vitreous and retina with a little dispersion to the aqueous humor.

There are reports indicating that topical administration of fluocinolone acetonide produces a percutaneous absorption which is determined by the vehicle, integrity of the epidermal barrier and the use of occlusive dressing.

Independently of the route of administration, the systemic absorption of fluocinolone acetonide is below 0.1 ng/ml which indicates that the systemic distribution is very minimal and the effect of fluocinolone is mainly local.

1-31% (topical)

Half Life

The reported half-life of fluocinolone acetonide ranges between 1.3-1.7 hours.

0.5-2 hours

Clearance

This pharmacokinetic parameter is not relevant as the systemic absorption of fluocinolone acetonide is very minimal and the concentration in urine is lower than the minimum quantitation limit.

Elimination Route

Fluocinolone acetonide is mainly excreted by the kidneys. It is important to mention that the systemically absorbed dose is very minimal.

Pregnancy & Breastfeeding use

Pregnancy: Category C. This cream contains the tretinoin, which may cause embryo-fetal death, altered fetal growth, congenital malformations, and potential neurologic deficits. There are no adequate and well-controlled studies in pregnant women. this cream should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Lactation: It is not known whether topical application of this cream could result in sufficient systemic absorption to produce detectable quantities of fluocinolone acetonide, hydroquinone, or tretinoin in human milk. Because many drugs are secreted in human milk, caution should be exercised when this cream is administered to a nursing woman.

Contraindication

Thid cream is contraindicated in individuals with a history of hypersensitivity, allergy, or intolerance to this product or any of its components.

Special Warning

Safety and effectiveness of this cream in pediatric patients have not been established.

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 at 20-25°C. Do not freeze.

Innovators Monograph

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