Indication

Zestra® helps to temporarily improve sexual desire/arousal in women suffering from female sexual interest/arousal disorder. This indication, approved by Health Canada (NPN 80034229), refers to the new classification of sexual disorders in the DSM-5. To know more about the changes in diagnostic criteria of sexual dysfunctions in the DSM-5, please consult Waguih William IsHak and Gabriel Tobia’s publication.

Mode of action

The active ingredients Zestra® help reproduce the normal physiological response of arousal by an increase in smooth muscle relaxation, i.e. vasodilatation joint with an increase in local neurosensitivity.

More specifically, borage oil (Borago officinalis) and evening primrose oil (Oenothera biennis), both of which contain a high concentration of gamma-linolenic acid (GLA), are believed to induce a high metabolization of prostaglandin-E1 (PGE1)1 in the skin of the application site (vulva). PGE1 increases nerve conduction and vascular smooth muscle dilation, resulting in enhanced desire, sensitivity and vulval engorgement.

Forskohlii (Coleus forskohlii)’s active ingredient, forskolin, stimulates the cellular production of cAMP. Osthol, the active ingredient in Du Huo (Angelica pubescen), enhances the increase in tissue cAMP and cGMP levels induced by forskolin. Within vascular smooth muscle cells,2 cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) contribute to local vasodilatation via relaxation of vascular smooth muscles by lowering intracellular calcium concentration.

  1. Dines, Prostaglandins, Leukotrienes, and essential Fatty Acid. 1996;55(3):159-75

  2. Teng, Naunyn Schmiedeberg’s Aerchive Pharmacologie. 1994;349(2):202-208

Clinical Trials

Zestra® has been established, in two randomized, placebo-controlled, double-blind clinical trials, to significantly improve woman’s desire, arousal and sexual satisfaction. In these clinical trials, 70% of women reported improved sexual satisfaction. This was achieved over multiple uses.

Results from the first clinical trial – a pilot study of women with and without sexual complaints – were published in 2003 by the Journal of Sex and Marital Therapy.

In 2007, a large clinical trial on 256 women, ages 21–65, with mixed desire/ interest/arousal/orgasm disorders, was conducted at 17 leading sexual health centres across the US. Results of this large-scale study were published in 2010 in the Journal of Sex and Marital Therapy. If you want more details regarding trial design, inclusion criteria, demographics, evaluation method and results, you can download the summary or the full publication.

These studies included women at different stages of life with a wide array of medical conditions, as well as women who were taking medications thought to be associated with lowering libido.

Safety

In the clinical studies, the only observed adverse event was genital burning (14%) in Zestra®-treated subjects, which subsided without treatment in 5 to 30 minutes.

Zestra® has been available in the US for 10 years and has shown an excellent safety profile.

The genital burning sometimes reported is often associated with improper application of the product. It is important for your patient to follow the instructions or watch the How to apply Zestra® video.

Furthermore, the active ingredients in Zestra® are very well-known, and side effects reported are rare, particularly in topical application.

This excellent safety profile establishes Zestra® as a first-line treatment of choice for your patients suffering from female sexual interest and arousal disorder.