Zetpil™ Melatonin 400mg SR Suppository


  • Most powerful antioxidant known to mankind.
  • Supraphysiologic dosages (higher amounts than the body can make or ingest through diet) MUST be achieved in order for melatonin to exert its antioxidant effect.
  • May support prevention of and treatments for cancer, heart disease, aging, diabetes, autism, and arthritis.
  • Melatonin is a diverse free radical scavenger that has the ability to squelch all known free radicals and cross all cellular structures, including the mitochondria.
  • Melatonin may be able to prevent and treat conditions caused by mitochondrial dysfunction.
  • Melatonin forms stable metabolites which are also free radical scavengers, resulting in a free radical scavenging cascade, unique only to melatonin.

Zetpil™ Suppository Advantage

Zetpil™ delivers nutrition via the rectum with the use of suppositories that have a unique, all- natural formulated base that has revolutionized not only this mode of delivery, but also the ability to obtain nutrients in a far more efficacious method.  These suppositories are a result of combining natural ingredients with a non-irritating, rapid melting (5-6 minutes), readily absorbable (superior retention), antioxidant base material (free radical scavenging ability) and delivers the nutrients directly into the bloodstream in less than 20 minutes in a highly effective manner. Oral supplements are exposed to the hazards of stomach acid, digestive enzymes, food-related breakdown, first pass metabolism, and other bioavailability issues in the gastro-intestinal system.

Additionally, many raw materials simply have a very low bioavailability , and only achieve around 10% or less (commonly <1%) absorption rates, even if the patient is in optimal health condition. Compromised health, age, or certain conditions that result in inability to take oral nutrients often preclude these patient populations from obtaining the necessary nutrition to stay healthy which often exacerbates chronic health issues.

Zetpil™ suppositories, as well as deep penetrating creams, are a NOW solution to delivering the necessary nutrients to patients, on a daily basis, that is both easy, comfortable and cost effective. The safety and noticeable effectiveness of these products will far outweigh any initial hesitation you have regarding this mode of delivery.

**NOTE: Melatonin currently is unavailable as intramuscular injections, nebulizer (nasal mist) or by intravenous administration anywhere in the world. Accordingly, the Zetpil ™ Melatonin Suppository is the only therapeutic melatonin option currently available.

What makes our Melatonin product different?

The Zetpil™ difference lies in our product’s ability to achieve therapeutic dosages via an alternate mode of delivery.  The impression of most lay people and physicians alike that the low oral dosages (2-10mgs) that help individuals sleep will also be able to exert melatonin’s powerful antioxidant effect is false.  Nothing could be further from the truth! 

Oral delivery of melatonin results in extremely low dosages absorbed as a result of low oral bioavailability, GI and liver metabolism of the compound, and lack of systemic circulation of therapeutic dosages.  It has been repeatedly proven in the research that dosage levels that trigger antioxidant activity cannot be achieved with oral delivery of melatonin.  Supraphysiologic dosages (higher amounts than the body can make or ingest through diet) MUST be achieved in order for melatonin to exert its antioxidant effect.  Research has hailed melatonin as the closest thing to a universal panacea (ie: cure for all ailments) ever researched by modern medicine which was the driving force for Zetpil™ to develop its Melatonin suppository and capitalize on all its potential health benefits.

What makes this product truly revolutionary is that therapeutic dosages of pharmaceutical grade Melatonin, embedded into our proprietary suppository base, can be delivered directly into the blood stream (via the many blood vessels that exist in the rectum),  potentially affecting an elevation of the serum melatonin levels.  Suppositories offer patient-friendly, cost-effective, and a natural, safe opportunity for repeated dosages of melatonin to be taken indefinitely! This breakthrough form of delivering melatonin truly raises the bar in effective antioxidant therapy for the patient population who desire an effective, affordable and potent antioxidant solution.

What is Melatonin?

Melatonin (N-acetyl-5-methoxytryptamine) is an indolamine (neurotransmitter) which is synthesized not only within the pineal gland in the brain, but has also been shown to be synthesized in many other parts of the body including, but not limited to, organs, the eye, gut, bone marrow, skin and immune cells.  The role of melatonin in circadian rhythm disturbances and sleep disorders is well established.

However, in the last several years, over 4,500 publications in peer-reviewed journals in the National Library of Medicine have confirmed melatonin, at higher dosages, to be the most powerful antioxidant in existence and the only universal free radical scavenger.

Patient and professional understanding of this unique and powerful signaling molecule must extend beyond jet lag and sleep aid. Some of its multiple beneficial functions may include powerful antioxidant, DNA protectant, immune function gatekeeper, and a natural oncostatic (anti-cancer) molecule. The research conducted in these regards has unequivocally documented melatonin’s ability to detoxify ALL harmful free radicals which cause molecular damage leading to disease and dysfunction.

What are “free radicals” and “oxidative stress”?

During respiration your body constantly reacts with oxygen for your cells to produce energy.  A natural consequence of this activity is that highly reactive, unstable molecules are produced known as “free radicals”.  Approximately 80% of all free radical production in the body is a result of this essential energy-generating process. Environmental stresses (ie: UV damage, pollution, radiation), emotional stress, inflammation and pharmaceutical drugs also directly cause the production of free radicals.

These free radicals (also called reactive oxygen/nitrogen species- ROS/RNS) are the nasty organic molecules responsible for aging, DNA and tissue damage, and many other types of diseases.  They are called “free” because they drift around the body with at least one unpaired electron in its outermost shell until they stabilize, and “radical” because there is a large compilation of molecules from which they can snatch electrons from.  As these free radicals accumulate they begin to overwhelm the body’s ability to safely stabilize them which results in oxidative stress, or damage.

How can you minimize this destructive damage?

Antioxidants.  Powerful antioxidants help these unstable molecules from binding with healthy molecules.  However, there is a catch.  What constitutes a “powerful” antioxidant may not be what you have been led to believe.  One of the biggest myths touted by the nutrition industry is that all antioxidants are created equal and nothing could be further from the truth. 

Many antioxidant vitamins commonly praised in mainstream medicine, such as C, E and A, are considered classical antioxidants and, in theory, are supposed to be effective in combating free radical damage.  However, in the process of squelching free radicals these nutrients transform from a reduced state to an oxidized state, lose their spare electron (now molecularly unstable) and ultimately become free radicals themselves  During this process of transforming from an antioxidant to a free radical these classical antioxidants also DEPLETE one of the most basic cellular antioxidants- glutathione.  There is no commonsense benefit to exhausting glutathione, especially since glutathione is far more powerful than the classic antioxidants.

Melatonin’s unique physical properties also set it apart from classical antioxidants.  Its small molecular size and amphiphilic properties (able to be dissolved in both fat and water) allow this molecule to penetrate all cells and cellular compartments, most notably the mitochondria.  Given that much evidence exists to show a direct relationship between mitochondrial dysfunction, aging, oxidative damage and low melatonin concentrations, melatonin should justly take its place as the most powerful antioxidant known to mankind.

What makes Melatonin so Powerful?

To this end, Melatonin still supersedes even glutathione in the battle for antioxidant status because melatonin itself increases the body’s own glutathione production.  Simply put, melatonin has the ability to induce an “antioxidant avalanche” of sorts with its own unique free radical scavenging properties, its ability to increase our body’s own antioxidant defenses (ie: glutathione), and by producing metabolites which are equally as powerful to continue the battle against oxidative damage.

More importantly, the research has demonstrated unequivocally that melatonin is completely non-toxic and is safe to take with most if not all medications. This combination of effectiveness and safety makes the use of melatonin a key compound in the treatment of numerous disease states, chronic diseases, and age-related diseases in humans where free radicals are a fundamental component.

An average human being contains about 1014 cells (one hundred trillion, or 100,000,000,000,000).  Each of these cells receives tens of thousands of potential DNA insults every day.  A huge part of free radical-based disease prevention (ie: cancer, neurodegenerative and cardiovascular diseases) lies in being able to continually prevent that DNA damage.  Melatonin confers unique and unparalleled protection to those hundred trillion cells on a daily basis.

Why can’t I take a generic melatonin supplement?

Most people are convinced that low oral dosages of melatonin (2mg- 10 mg), which is enough to help moderate jet lag, can also exert the additional antioxidant benefits of melatonin.  This is simply not true

Not only is the oral bioavailability of melatonin <15%, but when melatonin is taken orally it must also undergo further metabolism in the liver. The liver does not release melatonin efficiently and much of this melatonin is essentially “trapped” in the liver.  So, the poor absorption rate and the difficulty in breaking down orally-ingested melatonin in the liver make it nearly impossible for individuals to achieve all of the anti-oxidative benefits of melatonin when taken orally. In fact, research has deemed melatonin to be classified by pharmacologists as a low permeability compound (ie: poor absorption) due to its low oral bioavailability. 

What about sublingual Melatonin?

Unfortunately, the vast majority of these products on the market are low dosages that are combined with a form of sugar, sometimes alcohol and preservatives. There is no scientific basis to believe these additives increase absorption in any appreciable amount capable of exerting any antioxidant activity.

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