Use of melanotan I and II in the general population

In 2002 the media reported that the demand for synthetic melanocortin analogues melanotan I and melanotan II (melanotans) was likely to increase in the general population.1 This was mainly because of their ability to tan the skin, and—in the case of melanotan II—induce penile erections and increase sexual desire.2 In 2008, several workers at needle and syringe programmes in the United Kingdom contacted the substance use team at the Centre for Public Health, Liverpool, for information on “melanotan” after their clients reported injecting these drugs. Over the next year around 30 needle and syringe programmes in England and Wales and several drug workers and drug and alcohol action team commissioners have sought our advice in relation to the use of these drugs within the general population.

The prevalence of the use of these drugs is unknown. Even though the drugs are unlicensed they are easily available through online shops (including, until recently, eBay.co.uk) and are also sold and administered in tanning salons, beauty parlours, and hairdressers (personal communication to MC, 2008). Warnings over their sale and use have been issued by drug regulatory authorities in the United States and in Europe.3 4 5 6

A thriving online community of users exists—the most popular website (Melanotan.org) has more than 5000 members. On this website, current users discuss their experiences of using the drugs and prospective users seek advice about where they can buy them and what regimen they should use.

Most people use the melanotans to obtain a cosmetic skin tan. Some people use them for a range of conditions, including rosacea and fibromyalgia, after becoming disillusioned with existing medical treatments (Melanotan.org).

The melanotans are potent non-selective melanocortin (MC) receptor agonists with high affinity for MC1, MC3, MC4, and MC5 receptor subtypes.7 Their endogenous counterparts, the melanocortin peptides, help regulate a range of physiological systems, including the pigmentation system, energy homoeostasis, sexual functioning, the immune system, inflammation, and the cardiovascular system.7 8 The melanotans are thought to induce skin tanning by mimicking the actions of the melanocortin α-MSH (melanocyte stimulating hormone) on the MC1 receptors of melanocytes,7 which results in increased expression of eumelanin.9

Melanotan I (generic name afamelanotide) is currently undergoing phase III clinical trials as a “photoprotective” drug for the skin disorders erythropoietic protoporphyria and polymorphous light eruption.10 Melanotan II was being developed as a treatment for sexual dysfunction but was abandoned in favour of developing the metabolite bremelanotide (formerly known as PT-141).11 During clinical trials of bremelanotide, the drug was found to induce hypertension in some people, which led to this work being discontinued. It is now being developed as a treatment for haemorrhagic shock.11

Most users inject the melanotans subcutaneously after reconstitution with an excipient such as bacteriostatic water. In common with other illicitly supplied drugs, such as anabolic steroids,12 serious concerns exist about the quality of the preparations that are currently available—not only the drug content and dose, but also contaminants and sterility. Some users, especially those who are injecting drugs for the first time, are reusing or sharing injecting equipment, which places them and others at risk of infections, including blood borne viruses (personal communication to MC, 2008).

The health risks associated with the pharmacological effects of the melanotans are not clear. Adverse effects from short term administration in small clinical trials seem to be limited to transient facial flushing, nausea, and vomiting.2 One of the greatest concerns, however, is that these drugs are non-specific melanocortin receptor agonists that could interact with several physiological systems.7 This is particularly important because of the need for long term administration to maintain a tan.

We are now seeing a trend whereby some drugs undergoing preclinical and clinical development are being illicitly manufactured and supplied because of direct demand from the general population, thus short circuiting the safety mechanisms that are part of the normal drug life cycle. The use of the melanotans is part of a broader phenomenon of using a range of drugs not only for lifestyle reasons,12 but also as self prescribed medical treatments. The challenge to healthcare professionals is not only to recognise this new phenomenon and understand the complex forces that drive it, but also to develop strategies to engage with patients, and, more broadly, the general population to reduce associated harm and promote health. Such a response should include giving patients information and counselling about the dangers of using illicitly supplied drugs, along with reporting suspected adverse drug reactions (through the Yellow Card Scheme in the UK). Sterile injecting equipment and safer injecting advice must be provided for people who are injecting drugs. Finally, in the case of drugs that induce erections or increase sexual desire, or both (such as melanotan II), advice on safer sex should be provided.

Although action to reduce the illicit supply of such drugs should be an important part of any response, its effect will be limited unless the demand for these products is reduced. This, however, will require substantial changes in society’s attitudes, particularly towards drugs taken for lifestyle reasons—the demand for which seems to be insatiable.