Lutalyse® (dinoprost tromethamine)

Description:

Dinoprost tromethamine is a pharmaceutical form of the natural prostaglandin PGF2alpha. Prostaglandins are a series of natural oxygenated unsaturated cyclic fatty acids, which have a variety of hormone-like actions in the body. Among other things, PGF2alpha is involved in vasoconstriction, increasing protein synthesis in skeletal muscle tissue, and reducing adipose tissue mass. This hormone-like chemical also stimulates smooth muscle contraction, and is involved in pain, inflammation, fever, ovulation, gastric motility, and fluid absorption in the gastrointestinal tract. In veterinary medicine dinoprost tromethamine is most commonly used in estrus synchronization/fertility timing, for treating chronic endometriosis, and to induce abortion or labor.

Dinoprost is not widely used in human medicine, but is sometimes applied to terminate pregnancy or induce labor. Athletes and bodybuilders are attracted to dinoprost tromethamine for its strong thermogenic and musclebuilding properties. The anabolic effect of this drug has been substantiated by clinical studies, which have shown PGF2a to be a strong stimulator of protein synthesis, and key to both the immediate and long-term physiological adaptations to resistance training.1 2 3 4 Reports from athletes who have experimented with this agent generally support this compound being an excellent promoter of localized muscle growth, usually resulting in both increases in muscle size and definition. Dinoprost is also reported to be a very fast acting drug, with many claiming it has caused noticeable effect after being injected in a particular muscle group for only a couple of weeks. Clinical data also supports it being a substantially potent fat-loss drug, with PGF2a shown in studies to inhibit the stimulation of lipogenesis in fat cells.5 Again there is a great deal of anecdotal support for this property of dinoprost tromethamine among athletes and bodybuilders, with many claiming they notice a slight temperature elevation and marked fat loss during therapy.

History:

Dinoprost tromethamine was first introduced into clinical medicine in the early 1970s. The first approved use of the drug in human patients was to stimulate abortion during the second trimester. It has since remained of use for this purpose, but is most commonly associated these days with veterinary medicine. Here, it is widely applied to help farmers regulate the estrous cycle and fertility of various livestock. Interest in dinoprost tromethamine as an anabolic/thermogenic drug for athletes and bodybuilders did not appear until the late 1990s.

This likely occurred subsequent to the release of numerous medical studies linking PGF2alpha to muscle hypertrophy. Early theoretical concepts stemming from this research evolved into modern application protocols for the drug, which in spite of a high propensity to generate side effects, have proven to be highly successful for many athletes and bodybuilders.

Over the years dinoprost tromethamine has appeared as a human medicine under a wide number of trade names, including such popular drug products as Amoglandin (Sweden), Prostin (Sweden), Prostin F2 alpha (U.S., Australia, Israel, Italy, New Zealand, South Africa, and the United Kingdom), Minprostin F2a (Germany), Enzaprost (Greece, Poland) and Prostarmon (Japan). Prostin F2 is no longer sold in the U.S., however, and there is presently no FDA approved replacement available for human use. Veterinary versions are more widely available and tend to provide significantly more active drug for less money than their human counterpart medicines, and as a result have been the products most commonly associated with the physique- or performance-enhancing use of dinoprost tromethamine. Popular veterinary brands have included Lutalyse (Pharmacia Animal Health), Prostamate (Pfizer), Panacelan (Daiichi Pharmaceutical Co.) and Dinolytic (Upjohn). Several corporate mergers have taken place in this segment of the market, and the (now larger) conglomerate Pharmacia has emerged as the worldwide leader in dinoprost sales. Lutalyse is consequently the most common form of dinoprost tromethamine of use among the athletic/bodybuilding community.

How Supplied:

Dinoprost tromethamine is most commonly supplied in a multi-dose vial (5 mL-100 mL) in a dose of 5 mg per mL. It is prepared in a sterile solution of water with benzyl alcohol added as a preservative and sodium hydroxide and/or hydrochloric acid to adjust pH.

Structural Characteristics:

Dinoprost tromethamine is the tromethamine salt of prosta,5,13dien-1-oic acid (PGF2alpha).

Side Effects:

Possible side effects or signs of dinoprost tromethamine overexposure may include such respiratory effects as bronchoconstriction, wheezing, coughing, lung irritation, rapid breathing, and anaphylaxis. Asthmatic individuals may be particularly susceptible to these effects. Dinoprost may also cause gastrointestinal disturbances such as abdominal cramping, diarrhea, vomiting and nausea. Other effects may include increased pulse rate, elevated blood pressure, chills, fever, and anorexia, and in women uterine contractions, vaginal bleeding, and uterine or urinary infections. Pregnant women should not take or handle dinoprost. Reports of side effects among athletes using dinoprost for physique- or performance-enhancing purposes are common, and often extreme. This includes pronounced soreness at the site of injection; often beginning with a dull burning almost immediately after the shot is given. Chills and flu-like feelings are also commonly reported during cycles, as are bouts of shortness of breath. Injections are also commonly followed by uncontrollable urges to urinate or defecate, including strong spasmodic contractions of the muscles involved in the control of these functions. Nausea and vomiting have also been commonly reported. For many, the cramping, diarrhea, pain, and general feelings of upset stomach, malaise, and discomfort make dinoprost a drug they experiment with only briefly. Others, however, continue on with the drug, and often report that side effects become more tolerable over time.

Administration:

As a human medication, dinoprost tromethamine is most commonly given intra-amniotically at a dose of 40 mg for the termination of pregnancy. It is also sometimes given orally to pregnant women at a dose of 30-100 mg to induce labor, although this tends to produce more side effects than other, more recently adopted, medications. When used for physique- or performanceenhancing purposes, dinoprost tromethamine is generally given by intramuscular injection. Most noted for its ability to generate localized growth, common sites of injection include the shoulders, biceps, triceps, calves, chest, back, and legs. The user will typically inject in only one site per day at the start of therapy, but this may be increased to 2 or more injections per day as they become more accustomed to the drug and its side effects. Therapy begins slowly, and is initiated with a low starting dose of approximately .5 milligram per injection. If the first injection were given without significant side effects, the next injection would be increased to 1 milligram. This is slowly increased by .5-1mg per application until a peak dose is reached. This might be a maximum of 5 mg per injection site.

Injection sites are also regularly rotated so that several days separate administration in the same muscle group. Note that for some, the pain after injection is so severe that training for that specific muscle group must be delayed for at least a few days. Individual sensitivity to the drug may, therefore, require modifications of their injection and training schedule to maximize results and comfort.

Availability:

Dinoprost tromethamine is available in the U.S. and many other nations as a prescription drug product. It is also found infrequently on the black market.

1 Prostaglandins and the control of muscle protein synthesis and degradation. Prostaglandins Leukot Essent Fatty Acids. 1990 Feb;39(2):95-104

2 Prostaglandin F2(alpha)stimulates growth of skeletal muscle cells via an NFATC2-dependent pathway. Horsley V, Pavlath GK. J Cell Biol. 2003 Apr 14; 161(1):111-8

3 Stretch-induced prostaglandins and protein turnover in cultural skeletal muscle. Vandenburgh HH, Hatfaludy S, Sohar I, Shansky J. Am J Physiol. 1990 Aug;259(2 Pt 1):C232-40.

4 Skeletal muscle PGF(2)(alpha) and PGE(2) in response to eccentric resistance exercise: influence of ibuprofen acetaminophen. Trappe TA, Fluckey JD, White F, Lambert CP, Evans WJ. J Clin Endocrinol Metab. 2001 Oct;86(10):5067-70.

5 Prostaglandins promote and block adipogenesis through opposing effects on peroxisome proliferator-activated receptor gamma. Reginato MJ, Krakow SL, Bailey ST, Lazar MA.J Biol Chem 1998 Jan 23;273(4):1855