Pharmacologic Modulation of Sebaceous Gland Activity: Mechanisms and Clinical Applications

Dermatologic Clinics

Volumn 25, Issue 2, 2007, Pages 137-146

  Clarke, Shari B ^a   Nelson, Amanda M ^b   George, Rosalyn E ^a   Thiboutot, Diane M ^a,b  

^a PENN STATE COLLEGE OF MEDICINE   (United States)

^b PENN STATE CANCER INSTITUTE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANDROGEN; ANDROSTANOLONE; ANTIBIOTIC AGENT; BENZOYL PEROXIDE; CYPROTERONE ACETATE; DESOGESTREL PLUS ETHINYLESTRADIOL; DEXAMETHASONE; DIANE; DROSPIRENONE PLUS ETHINYLESTRADIOL; ETHINYLESTRADIOL PLUS LEVONORGESTREL; ETHINYLESTRADIOL PLUS NORETHISTERONE ACETATE; ETHINYLESTRADIOL PLUS NORGESTIMATE; FLUTAMIDE; ISOTRETINOIN; ORAL CONTRACEPTIVE AGENT; PREDNISONE; RETINOID; SPIRONOLACTONE;

ACNE FULMINANS; ACNE VULGARIS; ANDROGEN SYNTHESIS; ARTHRALGIA; BACTERIAL COLONIZATION; BLURRED VISION; BONE FRAGILITY; BRAIN PSEUDOTUMOR; BREAST TENDERNESS; CHEILITIS; DIURESIS; DRUG EFFICACY; DRUG HALF LIFE; DRUG INHIBITION; FATIGUE; FEMINIZATION; HAIR FOLLICLE; HEADACHE; HEPATITIS; HORMONAL REGULATION; HORMONAL THERAPY; HUMAN; HYPERKALEMIA; HYPERLIPIDEMIA; HYPERTRIGLYCERIDEMIA; LIBIDO DISORDER; LIVER TOXICITY; LOW DRUG DOSE; MENSTRUAL IRREGULARITY; MIGRAINE; MOOD CHANGE; MYALGIA; NAIL DISEASE; NIGHT BLINDNESS; NONHUMAN; PRIORITY JOURNAL; PROPIONIBACTERIUM ACNES; REVIEW; SEBACEOUS GLAND; SIDE EFFECT; SKIN ATROPHY; TERATOGENICITY; THROMBOEMBOLISM; VISUAL DISORDER; XEROPHTHALMIA; XEROSIS;

ACNE VULGARIS; ANDROGEN ANTAGONISTS; ANDROGENS; HUMANS; ISOTRETINOIN; SEBACEOUS GLAND DISEASES; SEBACEOUS GLANDS;

EID: 34147112692     PISSN: 07338635     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.det.2007.01.004     Document Type: Review

References (81)

1. Fleischer Jr. A.B., Simpson J.K., McMichael A., et al. Are there racial and sex differences in the use of oral isotretinoin for acne management in the United States?. J Am Acad Dermatol 49 4 (2003) 662-666
2. Thiboutot D.M. Endocrinological evaluation and hormonal therapy for women with difficult acne. J Eur Acad Dermatol Venereol 15 Suppl 3 (2001) 57-61
3. James W.D. Clinical practice. Acne. N Engl J Med 352 14 (2005) 1463-1472
4. Haider A., and Shaw J.C. Treatment of acne vulgaris. JAMA 292 6 (2004) 726-735
5. Chia C.Y., Lane W., Chibnall J., et al. Isotretinoin therapy and mood changes in adolescents with moderate to severe acne: a cohort study. Arch Dermatol 141 5 (2005) 557-560
6. Amichai B., Shemer A., and Grunwald M.H. Low-dose isotretinoin in the treatment of acne vulgaris. J Am Acad Dermatol 54 4 (2006) 644-646
7. Rubinow D.R., Peck G.L., Squillace K.M., et al. Reduced anxiety and depression in cystic acne patients after successful treatment with oral isotretinoin. J Am Acad Dermatol 17 1 (1987) 25-32
8. Fogh K., Voorhees J.J., and Astrom A. Expression, purification, and binding properties of human cellular retinoic acid-binding protein type I and type II. Arch Biochem Biophys 300 2 (1993) 751-755
9. Allenby G., Bocquel M.T., Saunders M., et al. Retinoic acid receptors and retinoid X receptors: interactions with endogenous retinoic acids. Proc Natl Acad Sci U S A 90 1 (1993) 30-34
10. Levin A., Bosakowski T., Kazmer S., et al. 13-cis retinoic acid does not bind to retinoic acid receptors alpha, beta and gamma. Toxicologist 12 (1992) 181
11. Ott F., Bollag W., and Geiger J.M. Oral 9-cis-retinoic acid versus 13-cis-retinoic acid in acne therapy. Dermatology 193 2 (1996) 124-126
12. Hommel L., Geiger J.M., Harms M., et al. Sebum excretion rate in subjects treated with oral all-trans-retinoic acid. Dermatology 193 2 (1996) 127-130
13. Geiger J.-M., Hommel L., Harms M., et al. Oral 13-cis retinoic acid is superior to 9-cis retinoic acid in sebosuppression in human beings. J Am Acad Dermatol 34 3 (1996) 513-515
14. Zorn N.E., and Sauro M.D. Retinoic acid induces translocation of protein kinase C (PKC) and activation of nuclear PKC (nPKC) in rat splenocytes. Int J Immunopharmacol 17 4 (1995) 303-311
15. Imam A., Hoyos B., Swenson C., et al. Retinoids as ligands and coactivators of protein kinase C alpha. FASEB J 15 1 (2001) 28-30
16. Hoyos B., Imam A., Chua R., et al. The cysteine-rich regions of the regulatory domains of Raf and protein kinase C as retinoid receptors. J Exp Med 192 6 (2000) 835-845
17. Karlsson T., Vahlquist A., Kedishvili N., et al. 13-cis-retinoic acid competitively inhibits 3 alpha-hydroxysteroid oxidation by retinol dehydrogenase RoDH-4: a mechanism for its anti-androgenic effects in sebaceous glands?. Biochem Biophys Res Commun 303 1 (2003) 273-278
18. Knutson D.D. Ultrastructural observations in acne vulgaris: the normal sebaceous follicle and acne lesions. J Invest Dermatol 62 3 (1974) 288-307
19. Plewig G., Dressel H., Pfleger M., et al. Low dose isotretinoin combined with tretinoin is effective to correct abnormalities of acne. J Dtsch Dermatol Ges 2 1 (2004) 31-45
20. Dalziel K., Barton S., and Marks R. The effects of isotretinoin on follicular and sebaceous gland differentiation. Br J Dermatol 117 3 (1987) 317-323
21. Goldstein J.A., Socha-Szott A., Thomsen R.J., et al. Comparative effect of isotretinoin and etretinate on acne and sebaceous gland secretion. J Am Acad Dermatol 6 4 Pt 2 Suppl (1982) 760-765
22. Nelson A.M., Gilliland K.L., Cong Z., et al. 13-cis retinoic acid induces apoptosis and cell cycle arrest in human SEB-1 sebocytes. J Invest Dermatol 126 10 (2006) 2178-2189
23. Wozel G., Chang A., Zultak M., et al. The effect of topical retinoids on the leukotriene-B4-induced migration of polymorphonuclear leukocytes into human skin. Arch Dermatol Res 283 3 (1991) 158-161
24. Leyden J.J., McGinley K.J., and Foglia A.N. Qualitative and quantitative changes in cutaneous bacteria associated with systemic isotretinoin therapy for acne conglobata. J Invest Dermatol 86 4 (1986) 390-393
25. Coates P., Vyakrnam S., Ravenscroft J.C., et al. Efficacy of oral isotretinoin in the control of skin and nasal colonization by antibiotic-resistant propionibacteria in patients with acne. Br J Dermatol 153 6 (2005) 1126-1136
26. Seguin-Devaux C., Hanriot D., Dailloux M., et al. Retinoic acid amplifies the host immune response to LPS through increased T lymphocytes number and LPS binding protein expression. Mol Cell Endocrinol 245 1-2 (2005) 67-76
27. Webster G.F. Complement activation in acne vulgaris. Consumption of complement by comedones. Infect Immun 26 (1979) 183-186
28. Mazzatenta C., Giorgino G., Rubegni P., et al. Solid persistent facial oedema (Morbihan's disease) following rosacea, successfully treated with isotretinoin and ketotifen. Br J Dermatol 137 6 (1997) 1020-1021
29. Cunliffe W.J. Management of adult acne and acne variants. J Cutan Med Surg 2 Suppl 3 (1998) 7-13
30. Pelwig G. Acneiform dermatoses. Dermatology 196 (1998) 102-107
31. Ellis C.N., and Krach K.J. Uses and complications of isotretinoin therapy. J Am Acad Dermatol 45 5 (2001) S150-S157
32. Craven N.M., and Griffiths C.E. Retinoids in the management of non-melanoma skin cancer and melanoma. Cancer Surv 26 (1996) 267-288
33. DiGiovanna J.J. Retinoid chemoprevention in the high-risk patient. J Am Acad Dermatol 39 2 Pt 3 (1998) S82-S85
34. Goldberg L.H., Hsu S.H., and Alcalay J. Effectiveness of isotretinoin in preventing the appearance of basal cell carcinomas in basal cell nevus syndrome. J Am Acad Dermatol 21 1 (1989) 144-145
35. Kraemer K.H., DiGiovanna J.J., Moshell A.N., et al. Prevention of skin cancer in xeroderma pigmentosum with the use of oral isotretinoin. N Engl J Med 318 25 (1988) 1633-1637
36. Schaller M., Korting H.C., Wolff H., et al. Multiple keratoacanthomas, giant keratoacanthoma and keratoacanthoma centrifugum marginatum: development in a single patient and treatment with oral isotretinoin. Acta Derm Venereol 76 1 (1996) 40-42
37. Motzer R.J., Schwartz L., Law T.M., et al. Interferon alfa-2a and 13-cis-retinoic acid in renal cell carcinoma: antitumor activity in a phase II trial and interactions in vitro. J Clin Oncol 13 8 (1995) 1950-1957
38. Stadler W.M., Kuzel T., Dumas M., et al. Multicenter phase II trial of interleukin-2, interferon-alpha, and 13-cis-retinoic acid in patients with metastatic renal-cell carcinoma. J Clin Oncol 16 5 (1998) 1820-1825
39. DiPaola R.S., Weiss R.E., Cummings K.B., et al. Effect of 13-cis-retinoic acid and alpha-interferon on transforming growth factor beta1 in patients with rising prostate-specific antigen. Clin Cancer Res 3 11 (1997) 1999-2004
40. Yung W.K., Kyritsis A.P., Gleason M.J., et al. Treatment of recurrent malignant gliomas with high-dose 13-cis-retinoic acid. Clin Cancer Res 2 12 (1996) 1931-1935
41. Kaba S.E., Langford L.A., Yung W.K., et al. Resolution of recurrent malignant ganglioglioma after treatment with cis-retinoic acid. J Neurooncol 30 1 (1996) 55-60
42. DiGiovanna J.J., Patronas N., Katz D., et al. Xeroderma pigmentosum: spinal cord astrocytoma with 9-year survival after radiation and isotretinoin therapy. J Cutan Med Surg 2 3 (1998) 153-158
43. Strauss J.S., Rapini R.P., Shalita A.R., et al. Isotretinoin therapy for acne: results of a multicenter dose-response study. J Am Acad Dermatol 10 3 (1984) 490-496
44. Stainforth J.M., Layton A.M., Taylor J.P., et al. Isotretinoin for the treatment of acne vulgaris: which factors may predict the need for more than one course?. Br J Dermatol 129 3 (1993) 297-301
45. Kus S. Vitamin E does not reduce the side-effects of isotretinoin in the treatment of acne vulgaris. Int J Dermatol 44 (2005) 248-251
46. Wysowski D.K., Pitts M., and Beitz J. Depression and suicide in patients treated with isotretinoin. N Engl J Med 344 6 (2001) 460
47. Marqueling A.L., and Zane L.T. Depression and suicidal behavior in acne patients treated with isotretinoin: a systematic review. Semin Cutan Med Surg 24 2 (2005) 92-102
48. Rappaport E.B., and Knapp M. Isotretinoin embryopathy-a continuing problem. J Clin Pharmacol 29 5 (1989) 463-465
49. Lammer E.J., Chen D.T., Hoar R.M., et al. Retinoic acid embryopathy. N Engl J Med 313 14 (1985) 837-841
50. Yu J., Gonzalez S., Martinez L., et al. Effects of retinoic acid on the neural crest-controlled organs of fetal rats. Pediatr Surg Int 19 5 (2003) 355-358
51. Pochi P.E., and Strauss J.S. Sebaceous gland response in man to the administration of testosterone, delta-4-androstenedione, and dehydroisoandrosterone. J Invest Dermatol 52 1 (1969) 32-36
52. Thiboutot D., Harris G., Iles V., et al. Activity of the type 1 5 alpha-reductase exhibits regional differences in isolated sebaceous glands and whole skin. J Invest Dermatol 105 2 (1995) 209-214
53. Thiboutot D., and Chen W. Update and future of hormonal therapy in acne. Dermatology 206 1 (2003) 57-67
54. Thiboutot D., Gilliland K., Light J., et al. Androgen metabolism in sebaceous glands from subjects with and without acne. Arch Dermatol 135 9 (1999) 1041-1045
55. Shaw J.C., and White L.E. Long-term safety of spironolactone in acne: results of an 8-year followup study. J Cutan Med Surg 6 6 (2002) 541-545
56. Yemisci A., Gorgulu A., and Piskin S. Effects and side-effects of spironolactone therapy in women with acne. J Eur Acad Dermatol Venereol 19 2 (2005) 163-166
57. Tremblay M.R., Luu-The V., Leblanc G., et al. Spironolactone-related inhibitors of type II 17beta-hydroxysteroid dehydrogenase: chemical synthesis, receptor binding affinities, and proliferative/antiproliferative activities. Bioorg Med Chem 7 6 (1999) 1013-1023
58. Zouboulis C.C., Akamatsu H., Stephanek K., et al. Androgens affect the activity of human sebocytes in culture in a manner dependent on the localization of the sebaceous glands and their effect is antagonized by spironolactone. Skin Pharmacol 7 1-2 (1994) 33-40
59. Archer J.S., and Chang R.J. Hirsutism and acne in polycystic ovary syndrome. Best Pract Res Clin Obstet Gynaecol 18 5 (2004) 737-754
60. Harper J.C. Antiandrogen therapy for skin and hair disease. Dermatol Clin 24 2 (2006) 137-143 v
61. Shaw J.C. Low-dose adjunctive spironolactone in the treatment of acne in women: a retrospective analysis of 85 consecutively treated patients. J Am Acad Dermatol 43 3 (2000) 498-502
62. Hughes B.R., and Cunliffe W.J. Tolerance of spironolactone. Br J Dermatol 118 5 (1988) 687-691
63. Yamamoto A., and Ito M. Topical spironolactone reduces sebum secretion rates in young adults. J Dermatol 23 4 (1996) 243-246
64. Lubbos H.G., Hasinski S., Rose L.I., et al. Adverse effects of spironolactone therapy in women with acne. Arch Dermatol 134 9 (1998) 1162-1163
65. Haroun M. Hormonal therapy of acne. J Cutan Med Surg 8 Suppl 4 (2004) 6-10
66. Stewart M.E., Greenwood R., Cunliffe W.J., et al. Effect of cyproterone acetate-ethinyl estradiol treatment on the proportions of linoleic and sebaleic acids in various skin surface lipid classes. Arch Dermatol Res 278 6 (1986) 481-485
67. Poulin Y. Practical approach to the hormonal treatment of acne. J Cutan Med Surg 8 Suppl 4 (2004) 16-21
68. Cunliffe W.J., and Bottomley W.W. Antiandrogens and acne. A topical approach?. Arch Dermatol 128 9 (1992) 1261-1264
69. Huber J., and Walch K. Treating acne with oral contraceptives: use of lower doses. Contraception 73 1 (2006) 23-29
70. Dodin S., Faure N., Cedrin I., et al. Clinical efficacy and safety of low-dose flutamide alone and combined with an oral contraceptive for the treatment of idiopathic hirsutism. Clin Endocrinol (Oxf) 43 5 (1995) 575-582
71. Wysowski D.K., Freiman J.P., Tourtelot J.B., et al. Fatal and nonfatal hepatotoxicity associated with flutamide. Ann Intern Med 118 11 (1993) 860-864
72. Garcia Cortes M., Andrade R.J., Lucena M.I., et al. Flutamide-induced hepatotoxicity: report of a case series. Rev Esp Enferm Dig 93 7 (2001) 423-432
73. Muderris I.I., Bayram F., and Guven M. Treatment of hirsutism with lowest-dose flutamide (62.5 mg/day). Gynecol Endocrinol 14 1 (2000) 38-41
74. Thornton M.J., Taylor A.H., Mulligan K., et al. The distribution of estrogen receptor beta is distinct to that of estrogen receptor alpha and the androgen receptor in human skin and the pilosebaceous unit. J Investig Dermatol Symp Proc 8 1 (2003) 100-103
75. Pelletier G., and Ren L. Localization of sex steroid receptors in human skin. Histol Histopathol 19 2 (2004) 629-636
76. Hay J.B., Hodgins M.B., and Donnelly J.B. Human skin androgen metabolism and preliminary evidence for its control by two forms of 17 β-hydroxysteroid oxidoreductase. J Endocrinol 93 3 (1982) 403-413
77. Sawaya M.E., and Price V.H. Different levels of 5α-reductase type I and II, aromatase, and androgen receptor in hair follicles of women and men with androgenetic alopecia. J Invest Dermatol 109 (1997) 296-300
78. Kariya Y., Moriya T., Suzuki T., et al. Sex steroid hormone receptors in human skin appendage and its neoplasms. Endocr J 52 3 (2005) 317-325
79. Thiboutot D. New treatments and therapeutic strategies for acne. Arch Fam Med 9 2 (2000) 179-187
80. Davies S., Dai D., Wolf D.M., et al. Immunomodulatory and transcriptional effects of progesterone through progesterone A and B receptors in Hec50co poorly differentiated endometrial cancer cells. J Soc Gynecol Investig 11 7 (2004) 494-499
81. van Vloten W.A., van Haselen C.W., van Zuuren E.J., et al. The effect of 2 combined oral contraceptives containing either drospirenone or cyproterone acetate on acne and seborrhea. Cutis 69 4 Suppl (2002) 2-15