New Developments in Hormonal Therapy for Acne
J. K. L. Tan, MD, FRCPC

Abstract
Oral contraceptives (OCs) are a valuable option for the treatment of women with acne. The use of OCs can be considered across the spectrum of acne disease severity in women. In Canada, three preparations are approved for mild-to-moderate acne, and a fourth is indicated for severe acne. These formulations contain estrogen in the form of ethinyl estradiol and a progestin. In Canada, the most recently approved OC is ethinyl estradiol 0.03mg and drospirenone 3mg (Yasmin, Bayer). With the accumulating evidence on the efficacy and safety of drospirenone-containing hormonal preparations, this formulation provides dermatologists with a new treatment option for acne and other hyperandrogenic disorders.

For many years, oral contraceptives (OCs) have been used by dermatologists as a treatment option for women with acne. OCs that are indicated for use in acne are effective across the spectrum of disease severity :
  1. in mild acne as an adjunct to topical therapy for female patients desiring contraception
  1. in moderate acne as a form of systemic therapy
  1. in severe acne
  1. as a primary form of therapy
  1. as one of two preferred forms of contraception in women treated with systemic isotretinoin.
From their inception, these preparations have evolved to include less estrogen and incorporate progestins with less intrinsic androgenicity. These modifications were undertaken to reduce the potential risk of thromboembolic events, hepatic tumors, hypertension, altered glucose metabolism, and androgenic side-effects.

OCs for the Treatment of Acne
In Canada, four hormonal preparations are presently indicated for the treatment of acne. These preparations all contain estrogen and progestins with either minimal androgenicity (i.e., ethinyl estradiol/ norgestimate, and ethinyl estradiol/ levonorgestrel) or antiandrogenic potential (i.e., ethinyl estradiol/ cyproterone acetate, and most recently, ethinyl estradiol/ drospirenone). Their demonstrated efficacy and long-term safety profile advocate their use in various grades of acne in women. Evidence supporting the use of these agents in acne was recently reviewed in the Journal of Cutaneous Medicine and Surgery, and is summarized briefly here.

Ethinyl Estradiol/ Norgestimate (Ortho Tri-Cyclen
Ethinyl estradiol 0.035mg with norgestimate in increasing doses, 0.180mg/ 0.215mg/ 0.250mg (Ortho Tri-Cyclen, Ortho- McNeil), was shown to be efficacious in moderate facial acne in two randomized placebo-controlled trials involving 324 subjects who were treated for 6 cycles. Significant improvements in lesion counts and investigator global assessment scores were observed. Inflammatory lesions were reduced by 56%, noninflammatory lesions by 41%, and 32% achieved excellent improvement. Norgestimate has low intrinsic androgenicity with low binding affinity for androgen receptors, whereas it is strongly selective and avidly bound to progesterone receptor sites.

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