Bodybuilders, dieters and athletes are always on the look out for that one compound that will help them reach their physical goals. The market is a very complex one. With the supplement industry not requiring FDA approval on their products, compounds are being released for every niche and purpose without any true studies done for safety or efficacy. Diet aids seem to have the biggest advantage for this with the ability to take advantage of those people who are looking for anything out there that can help them shed those extra 10-15 pounds. With new Jamaican Jambalayan derived Hoodia products being released, people are starting to forget products that already exist in the marketplace which have already been proven to be safe and efficacious.

A pharmaceutical product which has gained much popularity as of lately, however not in a good way, is Pseudoephedrine. Pseudoephedrine, being FDA approved as an over-the-counter oral decongestant, is closely related to the once powerful weight loss supplement ephedrine. The truth was ephedrine (and its ephedra alkaloids) worked. It not only promoted thermogensis in humans, but was a potent appetite suppressant. Unfortunately today, ephedra is not an easy compound to obtain. It is scarcely available as an OTC pharmaceutical, used as a bronchodilator, and in some states is still available as an herbal product. Pseudoephedrine on the other hand is still widely available in the U.S., and even though it does have some restrictions, it can still be obtained with quite ease. In this article we will discuss the pharmaceutical properties of pseudoephedrine, restrictions on its purchase, and its use as an appetite suppressant.

Pharmacology

Pseudoephedrine is a sympathomimetic amine and a (1S,2S)- diasteromer of ephedrine. It is available over-the-counter as a decongestant and is commonly found in combination with other medications (ie. antihistamines, cough and cold preparations). Being a sympathomimetic amine, it stimulates the sympathetic nervous system by displacing norepinephrine from storage vesicles in presynaptic neurons to activate postsynaptic adrenergic receptors. Pseudoephedrine is also an ?1a, ?2a and ?2-receptor agonist. By selectively activating the alpha receptors in the mucosa tract of the respiratory and nasal pathways, pseudoephedrine produces vasoconstriction shrinking membranes and relieving congestion. Activation of the beta2 receptor causes bronchodilation, which is relaxation of the bronchial smooth muscle, which allows the user to breathe easier. Pseudoephedrine has less pressor activity and a lower affinity for the central nervous system when compared to ephedrine so one should not to see much, if any, of a stimulating effect at recommended doses.

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Pharmacokinetics

Pseudoephedrine is readily absorbed from the GI tract with very little first pass metabolism. It is excreted mostly unchanged in the urine with few metabolites from being metabolized hepatically. The half-life is approximately 4-6 hours being dependant on urinary pH. If urine pH is less than 6 then the half-life may be decreased, as opposed to being increased when the urine pH is greater than 8. Pseudoephedrine has also been shown not to bind to plasma protein when the concentration is between 50-2000ng/mL.
Therapeutic Uses

Pseudoephedrine is commonly used for the following:

• Relief from nasal or sinus congestion;
• Relief of ear congestion;
• Treatment of vasomotor rhinitis (non-allergic rhinitis); and
• First line treatment for Priapism (erection lasting more then four hours)