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Percutaneous Absorption of Minoxidil in Man

Percutaneous Absorption of Minoxidil in Man Abstract • The percutaneous absorption and excretion of 1% and 5% solutions of minoxidil labeled with carbon 14 were measured in 12 adult male subjects. These subjects were randomly assigned to the 1% and 5% minoxidil testing groups, and all received nine topical applications to a bald area on the scalp, with the radioactive solutions applied on days 1 and 9. Urinary excretion of radioactivity was low, with mean values ranging from 1.6% to 3.9% of applied dose. No radioactivity could be detected in fecal samples. Recovery of radioactivity from the skin surface and from scalp and pillowcase washes was in the range of 41% to 45% of applied dose. No adverse reactions or notable abnormalities were noted in the subjects during the study. Although minoxidil is poorly absorbed through the skin, systemic doses in the range of 2.4 to 5.4 mg/day can be anticipated if application is made to entire scalp. (Arch Dermatol 1985;121:203-206) References 1. Mehta PK, Mamdani B, Sharsky RM, et al: Severe hypertension: Treatment with minoxidil . JAMA 1975;233:249-252.Crossref 2. Burton JL, Marshall A: Hypertrichosis due to minoxidil . Br J Dermatol 1979;101:593-597.Crossref 3. Zappacosta AR: Reversal of baldness in patient receiving minoxidil for hypertension . N Engl J Med 1980;303:1480-1481. 4. Weiss VC, West DP, Fu TS, et al: Alopecia areata treated with topical minoxidil . Arch Dermatol 1984;120:457-463.Crossref 5. Wester RC, Maibach HI, Guy RH, et al: Minoxidil stimulates cutaneous blood flow in human balding scalps: Pharmacodynamics measured by laser Doppler velocimetry and photopulse plethysmography . J Invest Dermatol 1984;82:515-517.Crossref 6. Baden HP, Kubilus J: Effect of minoxidil on cultured keratinocytes . J Invest Dermatol 1983;81:558-560.Crossref 7. Cohen RL, Alves MEAF, Weiss VC, et al: Direct effects of minoxidil on epidermal cells in culture . J Invest Dermatol 1984; 82:90-93.Crossref 8. Kligman AM, Christopers E: Preparation of isolated sheets of human stratum corneum . Arch Dermatol 1963;88:702-705.Crossref 9. Feldmann RJ, Maibach HI: Regional variation in percutaneous penetration of 14C cortisol in man . J Invest Dermatol 1967;48:181-183. 10. Maibach HI, Feldmann RJ, Milby TH, et al: Regional variation in percutaneous penetration in man . Arch Environ Health 1971;23:208-211.Crossref 11. Wester RC, Maibach HI, Bucks DAW, et al: Malathion percutaneous absorption after repeated administration to man . Toxicol Appl Pharmacol 1983;68:116-119.Crossref 12. Wester RC, Noonan PK, Maibach HI: Percutaneous absorption of hydrocortisone increases with long-term administration: In vivo studies in the rhesus monkey . Arch Dermatol 1980;116:186-188.Crossref 13. Thomas RC, Hsi RSP, Harpootlian H, et al: Metabolism of minoxidil, a new hypotensive agent: I. Absorption, distribution, and excretion following administration to rats, dogs, and monkeys . J Pharm Sci 1975;64:1360-1366.Crossref 14. Gottlieb TB, Thomas RC, Chidsey CA: Pharmacokinetic studies of minoxidil . Clin Pharmacol Ther 1972;13:436-441. 15. Wester RC, Noonan PK, Maibach HI: Frequency of application on percutaneous absorption of hydrocortisone . Arch Dermatol 1977;113:620-622.Crossref http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Archives of Dermatology American Medical Association

Percutaneous Absorption of Minoxidil in Man

Archives of Dermatology , Volume 121 (2) – Feb 1, 1985

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Publisher
American Medical Association
Copyright
Copyright © 1985 American Medical Association. All Rights Reserved.
ISSN
0003-987X
eISSN
1538-3652
DOI
10.1001/archderm.1985.01660020061018
Publisher site
See Article on Publisher Site

Abstract

Abstract • The percutaneous absorption and excretion of 1% and 5% solutions of minoxidil labeled with carbon 14 were measured in 12 adult male subjects. These subjects were randomly assigned to the 1% and 5% minoxidil testing groups, and all received nine topical applications to a bald area on the scalp, with the radioactive solutions applied on days 1 and 9. Urinary excretion of radioactivity was low, with mean values ranging from 1.6% to 3.9% of applied dose. No radioactivity could be detected in fecal samples. Recovery of radioactivity from the skin surface and from scalp and pillowcase washes was in the range of 41% to 45% of applied dose. No adverse reactions or notable abnormalities were noted in the subjects during the study. Although minoxidil is poorly absorbed through the skin, systemic doses in the range of 2.4 to 5.4 mg/day can be anticipated if application is made to entire scalp. (Arch Dermatol 1985;121:203-206) References 1. Mehta PK, Mamdani B, Sharsky RM, et al: Severe hypertension: Treatment with minoxidil . JAMA 1975;233:249-252.Crossref 2. Burton JL, Marshall A: Hypertrichosis due to minoxidil . Br J Dermatol 1979;101:593-597.Crossref 3. Zappacosta AR: Reversal of baldness in patient receiving minoxidil for hypertension . N Engl J Med 1980;303:1480-1481. 4. Weiss VC, West DP, Fu TS, et al: Alopecia areata treated with topical minoxidil . Arch Dermatol 1984;120:457-463.Crossref 5. Wester RC, Maibach HI, Guy RH, et al: Minoxidil stimulates cutaneous blood flow in human balding scalps: Pharmacodynamics measured by laser Doppler velocimetry and photopulse plethysmography . J Invest Dermatol 1984;82:515-517.Crossref 6. Baden HP, Kubilus J: Effect of minoxidil on cultured keratinocytes . J Invest Dermatol 1983;81:558-560.Crossref 7. Cohen RL, Alves MEAF, Weiss VC, et al: Direct effects of minoxidil on epidermal cells in culture . J Invest Dermatol 1984; 82:90-93.Crossref 8. Kligman AM, Christopers E: Preparation of isolated sheets of human stratum corneum . Arch Dermatol 1963;88:702-705.Crossref 9. Feldmann RJ, Maibach HI: Regional variation in percutaneous penetration of 14C cortisol in man . J Invest Dermatol 1967;48:181-183. 10. Maibach HI, Feldmann RJ, Milby TH, et al: Regional variation in percutaneous penetration in man . Arch Environ Health 1971;23:208-211.Crossref 11. Wester RC, Maibach HI, Bucks DAW, et al: Malathion percutaneous absorption after repeated administration to man . Toxicol Appl Pharmacol 1983;68:116-119.Crossref 12. Wester RC, Noonan PK, Maibach HI: Percutaneous absorption of hydrocortisone increases with long-term administration: In vivo studies in the rhesus monkey . Arch Dermatol 1980;116:186-188.Crossref 13. Thomas RC, Hsi RSP, Harpootlian H, et al: Metabolism of minoxidil, a new hypotensive agent: I. Absorption, distribution, and excretion following administration to rats, dogs, and monkeys . J Pharm Sci 1975;64:1360-1366.Crossref 14. Gottlieb TB, Thomas RC, Chidsey CA: Pharmacokinetic studies of minoxidil . Clin Pharmacol Ther 1972;13:436-441. 15. Wester RC, Noonan PK, Maibach HI: Frequency of application on percutaneous absorption of hydrocortisone . Arch Dermatol 1977;113:620-622.Crossref

Journal

Archives of DermatologyAmerican Medical Association

Published: Feb 1, 1985

References