The Dangerous Counterfeit Muscles: The Ingredient from Blue Pills Is Not for Everyone, and It Is Also Found in Coffees

Bulging muscles are not always just the result of everyday hours of exercise in the gym; often, their volume and strength are also contributed by the consumption of dietary supplements that are – counterfeit and illegal. These are sildenafil citrates or their derivatives, drugs used to treat pulmonary arterial hypertension and male erectile dysfunction. They are also found in dietary supplements and even in instant coffee products. The counterfeit drug market is believed to be larger than the drug market, and in Interpol’s Operation Pangea against the sale of counterfeit drugs, as much as 48 percent of counterfeits for improving erections were discovered.

– Sildenafil is a vasodilator and belongs to the group of phosphodiesterase type 5 (PDE5) inhibitors. To improve the solubility of the drug, the formulation contains the drug in the form of a salt with citric acid. It is used to treat adult patients and children and adolescents aged one to 17 years who have high blood pressure in the blood vessels in the lungs (pulmonary arterial hypertension, which dilates the blood vessels in the lungs). Sildenafil is also used in the treatment of male erectile dysfunction (ED) – explains Prof. Dr. Ruža Frkanec from the Center for Research and Knowledge Transfer in Biotechnology at the University of Zagreb.

High-Potency Drugs

According to her, the discovery of sildenafil began with the research of the Nobel Prize winners in Medicine (Physiology) in 1998, Robert F. Furchgott, Louis J. Ignarro, and Ferid Murad ‘for discoveries of the connection of nitric oxide (NO) as a signaling molecule and the human cardiovascular system.’ They synthesized a new compound to develop a drug that could enhance the effects of NO on the cardiovascular system, later known as sildenafil. The U.S. Food and Drug Administration (FDA) approved the drug in 1998.

– Sildenafil and its derivatives or salts are high-potency pharmaceutical drugs that prolong the action of cGMP by inhibiting the hydrolytic breakdown of cyclic guanosine monophosphate (cGMP), resulting in increased relaxation of smooth muscles. There are two main brands of the drug that contain sildenafil: Viagra and Revatio. In addition to treating ED, Revatio treats pulmonary hypertension. Therapy is conducted under the supervision of a physician who determines the dose and adjusts it for the patient. However, a large number of products are available on the market that can be purchased without a prescription and are advertised as natural, herbal preparations for treating erectile dysfunction, which contain various amounts of added synthetic sildenafil that is not declared and can cause serious side effects. In addition to herbal preparations for treating or improving erections in men, sildenafil and its derivatives have been found in dietary supplements and even in instant coffee products – warns Frkanec.

Wide Use

Since the drug sildenafil is contraindicated in patients with cardiovascular diseases, diabetes, hyperlipidemia, and some other conditions associated with erectile disorders, explains Frkanec, such patients seek herbal products as alternative treatments, and manufacturers, to be competitive, illegally counterfeit the content of herbal preparations by adding sildenafil and its derivatives.

– By adding sildenafil and its derivatives to herbal preparations and dietary supplements, these products are advertised as extremely effective and potent preparations, either for treating erectile dysfunction or just enhancing erections or generally improving the overall condition of the body because they are vasodilators, increasing blood flow and relaxing smooth muscles. In addition to sildenafil, various derivatives of sildenafil are added to such products to avoid regulatory agency control. Some derivatives of sildenafil found in various products include homosildenafil, hydroxihomosildenafil, acetildenafil, methisosildenafil, thiosildenafil, and many others. Unlike proven and well-known drugs, the effectiveness and safety as well as side effects of such analogs are mostly unknown. Consumers who use such counterfeit products are at risk of developing serious side effects that can lead to death – warns Frkanec.

Dietary supplements and instant coffee products are consumed by a wide population, from young to older, healthy, but also sick individuals. In addition, dietary supplements are taken by professional athletes, as well as young people who engage in recreational sports and exercise in gyms.

Frequent Side Effects

According to Frkanec, the consumption of counterfeit products to which sildenafil or its derivatives (but also other drugs, for example, for weight loss) have been added, and which are taken long-term and even excessively, can lead to serious harmful and even fatal health consequences. This is especially dangerous for adolescents and young people who are in development and of reproductive age.

– When using PDE5 inhibitors, including sildenafil, vardenafil, and tadalafil, frequent side effects have been reported in healthy men between 18 and 60 years, including flushing, headache, digestive disturbances, muscle or back pain, and visual disturbances. Visual disturbances can be partial, sudden, temporary, or permanent reduction or loss of vision in one or both eyes. Cases of prolonged erections as well as priapism, i.e., painful persistent erections without sexual arousal, have been reported. Long-term consumption of sildenafil and higher doses have been shown to cause chronic liver and kidney damage, and for numerous derivatives of sildenafil, no safety and efficacy studies have been conducted, and there are no available data on side effects – explains Frkanec.

Without Verification and Restrictions

However, there is no restriction on taking dietary supplements that contain sildenafil or its derivatives because no one controls this. They are freely sold and can be purchased without a prescription in pharmacies and online stores.

– People believe that such products are safer than synthetic drugs that can only be purchased in pharmacies, and it is believed that more than fifty percent of adults today consume them as a substitute for a balanced diet, improving overall health, enhancing appearance, or delaying the onset of disease. The ingredients that make up dietary supplements are vitamins, minerals, essential fatty acids, fibers, amino acids, and nitrogen compounds, as well as numerous plant species. In addition to the listed ingredients, dietary supplements may also contain other ingredients, but according to prescribed food rules. The composition of dietary supplements should be printed on the packaging, and it is also recommended to label the minimum, maximum, and recommended daily doses of vitamins and minerals for healthy adults. In the rest of Europe, as well as in Croatia, dietary supplements are considered food, so no approval is required for marketing – warns Frkanec.

Regulations on food apply to dietary supplements, and the same rules regarding general labeling, food additives, contaminants, new food, and food and health claims apply… In Croatia, the composition, labeling, and marketing are regulated by the Law on Food and Health Claims and Food Enriched with Nutrients. The Regulation on Dietary Supplements applies the provisions of Directive 2002/46/EC of the European Parliament and Council to harmonize the laws of member states. Added vitamins and minerals and all their chemical forms used in the production of dietary supplements are prescribed by the Regulation of the Commission (EC) of the European Parliament and Council. However, untested products can still be placed on the market, which is the result of unclear legal provisions for regulation and verification of effectiveness. The U.S. Food and Drug Administration (FDA) also does not consider dietary supplements to be drugs. Although manufacturers must have evidence that products are not harmful, they can be released to the market before verification, which raises questions about their quality and safety.

Advice for Users

In choosing products for improving erections and sexual abilities, users should know that there are two types of products available on the market: those that may be safe but do not work, and those that may work but are not safe. Therefore, the advice is to avoid them all.

– Users who feel a significant improvement in erection or other effects after consuming a herbal product for improving erections or sexual abilities should suspect counterfeiting and the addition of unauthorized drugs in unknown doses to the product they consumed and report everything to the relevant regulatory agency HALMED. Users and consumers of various herbal preparations and dietary supplements should avoid purchasing such products online from unknown and unauthorized manufacturers, and when purchasing them in authorized pharmacies, they must pay attention to the composition and recommended doses. They should also follow public information sources about possible product withdrawals from the market due to counterfeiting and the possible content of potentially dangerous ingredients – warns Frkanec and emphasizes the need for greater cooperation and information exchange between various health authorities and experts, academia, researchers, and industry, as well as public education of patients and dietary supplement users.

According to her, these are key steps in efforts to stop the trend of counterfeiting herbal products and dietary supplements with drugs and their derivatives, as is the case with sildenafil. Furthermore, lawmakers should revise the law regulating dietary supplements so that manufacturers are not allowed to claim that a product will improve someone’s sexual function (or any other) until data supporting such a claim is provided.