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Primary headaches represent some of the most costly diseases in modern society, and epidemiologic studies indicate that tension-type headache and migraine represent two different diseases, although coexisting in many patients. Limited knowledge of the underlying pathophysiology of tension-type headache is not yet available, and there is no specific treatment. Simple analgesics and nonsteroidal anti-inflammatory drugs (NSAIDs) for the treatment of acute headache and low dose tricyclic antidepressants are still the mainstays of treatment, although new promising therapies are emerging.

LipiGesic^™ H is formulated based on the current evidence indicating that the effects of stress, as well as anxiety and depression, can increase the frequency and severity of tension headaches. The combination of acetylsalicylic acid (aspirin) and St. John’s Wort delivered utilizing our sublingual gel delivery system can dramatically increase the speed and levels of relief for many tension headache sufferers. Ideal treatment for tension-type headaches is the medication that is most effective at the lowest dose and has the fewest potential side effects. LipiGesic^™ H fits that profile.

As many as 90% of American adults will develop a tension-type headache during their lifetime and over 38% (102,000,000) of American adults suffer from episodic and chronic tension-type headaches. This market represents a substantial opportunity for LipiGesic^™ H as an innovator in a market that has seen little innovation in decades.

Many people treat headaches with ordinary over-the-counter pain-relievers and get good relief. The familiar over-the-counter analgesics are mostly aspirin and aspirin-like drugs, such as naproxen and ibuprofen. This class of pain relievers is known as the nonsteroidal anti-inflammatory agents or NSAIDs. Although the oldest (and cheapest) of the NSAIDs, aspirin still soldiers on, relieving countless joint pains, backaches and, of course, headaches. One full century after its introduction, aspirin still has not been pushed out of the medicine cabinet by “new and improved” alternatives.
In the doses that most people take, aspirin not only reduces fevers but also relieves pain. Two aspirin can accomplish this with a dose of about 650 mg (about 1/45th of an ounce). At much higher doses (about 6-fold higher, and only when prescribed by a doctor), aspirin is an anti-inflammatory agent, about as powerful as hydrocortisone. But at a single tiny dose (about 1/400th of an ounce), aspirin prevents blood platelets from sticking together to form clots for about 5 days! Hence, aspirin is used in such varied diseases as the common cold, migraine, rheumatoid arthritis, and heart attack prevention, among others. And yet, for many years, how this powerful drug worked remained a mystery.

The 1950s and 1960s were the era when we really started understanding how hormones work. In the late 1960s a whole new family of hormones was discovered, called prostaglandins. These prostaglandins seemed to come from every cell in the body except red blood cells. It was thought that their role was to communicate between neighboring cells in the same tissue — unlike, for example, pituitary hormones, which are released into the bloodstream from the pituitary gland in the brain and travel to distant sites such as the kidneys and bones.

In 1971, the aspirin puzzle was cracked by Sir John Vane. He discovered that aspirin prevented the generation of these prostaglandins in the lungs of guinea pigs. It was quickly discovered that this happened in all the other cells that make prostaglandins, too.

Eventually the effects of aspirin were shown more precisely to be achieved by blocking the enzyme that made the prostaglandins. That enzyme has the unpronounceable name cyclooxygenase, which we call COX, because it is easier!

Amazingly enough, it turns out that there are (at least) two types of COX. We call them COX-1 and COX-2. Both COX-1 and COX-2 make prostaglandins, but COX-1 makes prostaglandins in the places where we want them (such as the stomach lining), whereas COX-2 makes prostaglandins in response to disease (such as infections or arthritis). The two enzymes perform the same chemistry, but they differ in the size of the molecular “mouth” into which the chemical ingredients must fit in order to be made into prostaglandins. COX-1 has a narrow mouth, whereas COX-2 is wide-mouthed (see diagram). A COX-3 has recently been discovered in the brain; we are not sure exactly what it does, but probably it works likes COX-2.

Aspirin is a small molecule that can fit into both the small mouth of COX-1 as well as the large mouth of COX-2. That is why aspirin has both bad effects on stomach lining (by blocking COX-1) as well as good effects by blocking COX-2 (relieving headache or fever). The newer COX-2 drugs are larger and bulkier molecules. Thus, drugs like rofecoxib (Vioxx) and celecoxib (Celebrex) can only fit into wide-mouthed COX-2, but not into narrow-mouthed COX-1. The idea, then, is that these newer drugs still let COX-1 carry on making prostaglandins that keep the stomach healthy, but block COX-2 from making prostaglandins causing headache and fever.

However, the way that drugs fit into the mouths of enzymes is not a simple as putting a peg into a hole. It is a sort of “forced fit” due to the complicated electrochemical forces at work. If the concentration is high enough, even a big bulky drug can be jammed into a few narrow-mouthed COX-1 enzymes. So, the newer drugs are not entirely free of side effects, and some people will still get an upset stomach after using a COX-2 drug. The newer drugs are, of course, also much more expensive than aspirin. The bottom line is that if you are a patient who can take aspirin (or a related NSAID, such as naproxen or ibuprofen), then there is usually no reason to switch to an expensive COX-2 drug.

St. John's Wort

St. John's Wort has a complex and diverse chemical make-up. Hypericin and pseudohypericin are believed to have antidepressive and antiviral properties. Other constituents, such as xanthones and flavonoids, may also contribute to the medicinal actions of St. John's Wort. The following are the active constituents:

• Essential oil, containing caryophyllene, methyl-2-octane, n-nonane, n-octanal, n-decanal, a- and b-pinene, and traces of limonene and myrcene
• Hypericins, prenylated phloroglucin derivatives; hypericin, pseudohypericin and hyperforin
• Miscellaneous; flavonoids, () and (-) - epicatechin.

Hypericum extract contains numerous active compounds that together create the antidepressant and antianxiety effects. Hypericum is the first known substance to enhance three key neurotransmitters- serotonin, norepinephrine, and dopamine. Preliminary research suggests that St. John's Wort also lowers levels of the stress hormone cortisol and enhances the activity of gamma-aminobutyric acid (GABA), a naturally occurring tranquilizer in the brain. It is a very mild, clinically insignificant monoamine oxidase (MAO) inhibitor.

Hypericum was recommended by Hippocrates for "nervous unrest." It has a 2400-year history of folk use for anxiety; sleep disturbances, and worry. Modern medical research has shown that Hypericum can be as effective as prescription antidepressants for mild to moderate depression. However, unlike prescription antidepressants, Hypericum's side effects are few and mild. The standardized extract of St. John's Wort (containing 0.14 percent hypericin) has significant support in the treatment of mild to moderate depression. The official German Commission E monograph for St. John's Wort lists psychovegetative disturbances, depressive states, fear, and nervous disturbances as clinical indications for the extract. Clinical studies have shown significant improvement in symptoms of anxiety, apathy, hypersomnia, and insomnia, anorexia, psychomotor retardation, depression feelings of worthlessness. Clinical double blind studies indicated that St. John's Wort extract (0.3% hypericin) at a dosage of 300 milligrams three times daily is as effective in relieving symptoms of depression as standard antidepressants but is much better tolerated with fewer side effects.

Hypericum is now the number one antidepressant, natural or synthetic, prescribed by German physicians. In Germany, Hypericum accounts for over 50 percent of the antidepressant market, while Prozac is down to 2 percent. 

In addition to Hypericum's mood-elevating properties, Germany's Commission E has approved this herb for the treatment of anxiety and sleep disorders. In two clinical studies, Hypericum demonstrated anti-anxiety effects comparable to those of Valium (diazepam). Yet Hypericum is not addictive and does not impair cognitive functions. 

Taken internally, St. Johns Wort has a sedative and pain reducing effect, which gives it a place in the treatment of neuralgia, anxiety, tension and similar problems. It is especially regarded as an herb to use where there are menopausal changes triggering irritability and anxiety. In addition to neuralgic pain, it will ease fibrositis, sciatica and rheumatic pain.