Appearex Tablets (Merz)

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DESCRIPTION AND MECHANISM OF ACTION

Appearex® is a biotin preparation (2.5 mg) available for oral administration as a small, easy-to-swallow tablet. Each Appearex® tablet contains as its active ingredient 2.5 mg of biotin, a dose clinically proven to improve nail strength and quality. ^1-4 Inactive ingredients include lactose monohydrate, cornstarch, povidone (K25), and magnesium stearate.

Biotin is a water-soluble vitamin component of the vitamin B complex. As an essential nutrient, biotin acts as a coenzyme for the body's carboxylation reactions and is a factor in maintaining healthy muscle, hair, nails, and skin. Its molecular formula is C ₁₀ H ₁₆ N ₂ O ₃ S, and its molecular weight is 244.308. It has the following structural formula:

The presumed mechanism of action by which Appearex® affects brittle nails is via the pharmacologic effects of biotin on all keratin structures. Biotin stimulates the differentiation of epidermal cells and is involved in keratinization. It is also believed that biotin increases the quantity of keratin matrix proteins in the nail, thereby improving keratin structure. ^3,5

PHARMACOKINETICS

ABSORPTION AND TRANSPORT:

Biotin is efficiently absorbed in the small intestine sodium-mediated carrier transport. ^6,7 Once absorbed, 80% of biotin is free, and the remaining 20% is bound to plasma proteins. ⁸ Cellular entry of biotin occurs by both diffusion and sodium-dependent transport.

DEGRADATION AND EXCRETION:

About 43% of biotin is excreted unchanged in the urine. ⁹ The remainder is excreted as degradation products including bisnorbiotin (30%), biotin sulfoxide (11%), and other small amounts of biotin sulfone, bisnorbiotin methylketone, and tetranorbiotin sulfoxide. ¹⁰

ADVERSE REACTIONS

Adverse reactions associated with biotin supplementation are rare in the medical literature; however, urticaria and gastrointestinal upset have been reported. As with any oral treatment, if patients experience any adverse reactions or side effects, they should inform their physicians immediately and discontinue use.

DRUG INTERACTIONS

The anticonvulsants carbamazepine, phenytoin, phenobarbital, and primidone may accelerate biotin metabolism, leading to a reduction in available biotin. Chronic use of these drugs has been associated with decreased plasma concentrations of biotin. ^11,12

The use of antibiotics may reduce the contribution of biotin made by bacteria within the large intestine.

PRECAUTIONS AND WARNINGS

Pregnant women and nursing mothers should consult their physicians before taking this product. Appearex® should not be used in patients with known allergy or hypersensitivity to any of its ingredients.

TOXICITY

No toxic effects have been reported, even at higher doses. ¹³

INDICATION AND USAGE

Appearex® is recommended for first-line treatment of weak, brittle, splitting, or soft nails.

Appearex® therapy should be taken regularly as directed to maintain strong, healthy nails. Clinical improvement is generally realized within 3 to 6 months. ^1-3 Cessation of therapy may result in deterioration of nail health within 6 to 9 months.

CONTRAINDICATION

Appearex® is contraindicated in patients allergic or hypersensitive to any of its ingredients.

DOSAGE AND ADMINISTRATION

Recommended treatment for adults is 1 tablet taken daily with water. For use in children under 12 years of age, consult a physician for guidance regarding proper dosing and administration.

HOW SUPPLIED

One Appearex® package contains 30 tablets (1 month's supply) enclosed in blister packs.

SUMMARY

Appearex®, for the treatment of weak, brittle, splitting, or soft nails, is pharmaceutical grade oral biotin that restores nail quality by promoting keratinization. It has been clinically proven to increase nail plate thickness, smooth brittle nail ridges, and improve overall nail quality. As a water-soluble essential vitamin the biotin in Appearex® is safe and well tolerated. For patients with brittle nails, one Appearex® tablet taken daily provides the additional biotin needed to manage onychoschizia/onychorrhexis.

REFERENCES

1. Hochman LG, Scher RK, Meyerson MS. Brittle nails: response to daily biotin supplementation. Cutis . 1993;51:303-305.
2. Floersheim GL. Treatment of brittle nails with biotin [in German]. Z Hautkr . 1989;64:41-48.
3. Gehring W. Effect of biotin on poor nail quality: a placebo-controlled double-blind clinical study [in German]. Aktuelle Dermatol . 1996;22:20-25.
4. Colombo VE, Gerber F, Bronhofer M, Floersheim GL. Treatment of brittle fingernails and onychoschizia with biotin: scanning electron microscopy. J Am Acad Dermatol . 1990;23:1127-1132.
5. Schmidt KH. Comparison of the operating mechanisms of different ingredients for treatment of brittle nails [in German]. Z Hautkr . 1993;68:517-520.
6. Stipanuk MH. Biochemical and Physiological Aspects of Human Nutrition . Philadelphia, Pa: WB Saunders Co; 2000;529-540.
7. Zempleni J, Mock DM. Bioavailability of biotin given orally to humans in pharmacologic doses. Am J Clin Nutr . 1999; 69:504-508.
8. Mock DM, Malik MI. Distribution of biotin in human plasma: most of the biotin is not bound to protein. Am J Clin Nutr . 1992;56:427-432.
9. Mock DM, Lankford GL, Cazin JJr. Biotin and biotin analogs in human urine: biotin accounts for only half of the total. J Nutr . 1993;123;1844-1851.
10. Zempleni J, McCormick DB, Mock DM. Identification of biotin sulfone bisnorbiotin methyl ketone, and tetranorbiotin-1-sulfoxide in human urine. Am J Clin Nutr . 1997;65:508-511.
11. Mock DM, Dyken ME. Biotin catabolism is accelerated in adults receiving long-term therapy with anticonvulsants. Neurology . 1997;49:1444-1447.
12. Mock DM, Mock NI, Nelson RP, Lombard KA. Disturbances in biotin metabolism in children undergoing long-term anticonvulsant therapy. J Pediatr Gastroenterol Nutr . 1998;16:245-250.
13. Marcus R, Coulston AM. Water-soluble vitamins. In: Hardman JG, Limbird LE, Gilman AG, eds. Goodman and Gilman's the Pharmacologic Basis of Therapeutics . 10 ^th ed. New York, NY: McGraw-Hill Medical Publishing Division; 2001:1753-1771.

5010814      Rev 05/04

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