Epoetin Alfa History
Epoetin alfa was developed by the biotechnologies firm Amgen, and first introduced to the U.S. market in 1984. The release of the drug is regarded as a breakthrough in the treatment of anemia, which beforehand was being addressed mainly with agents that indirectly or nonspecifically targeted red cell production, such as oxymetholone, which may present a number of unwanted side effects to the patient. Epoetin alfa marked the development of the first drug that specifically and effectively stimulated the process of erythropoiesis (red blood cell production). Its success was rapid and far reaching. Epoetin alfa has since been introduced to a wide number of different countries. The most popular trade names include Procrit (distributed by Ortho, manufactured by Amgen), Epogen (Amgen), and Eprex (Johnson & Johnson). In addition to these, more than one dozen other trade names are also used to market epoetin alfa.
In 2002 the subcutaneous use of Eprex, which is sold only outside the United States, was linked to a rare disease called pure red-cell aplasia. This is a condition where the body loses its ability to produce red blood cells. Those that suffer from pure red-cell aplasia usually become dependant on continual blood transfusions for survival. Close to 200 people taking Eprex were identified as developing this rare condition, far in excess of normal expected numbers. Internal investigations by Johnson & Johnson linked the high numbers to changes in the product that were made to satisfy European regulations limiting the use of albumin. According to a company spokesperson, a chemical reaction between the new stabilizer that replaced albumin and the rubber stopper allowed organic compounds to leech into the vials. The company subsequently replaced its original stoppers with coated rubber to prevent this reaction. The incidence of pure-red cell anemia in patients receiving erythropoietin seems to have been reduced as a result, although warnings about this reaction remain on the prescribing information for all products sold in the U.S.
How is Epoetin Alfa Supplied
Epoetin alfa is supplied as a dry sterile powder that requires reconstitution with sterile diluent before injection. It is most commonly found in single- and multi-dose ampules and vials containing 2,000-40,000 Units/ml.
Structural Characteristics of Epoetin Alfa
Epoetin alfa is a single chain polypeptide hormone containing 165 amino acids. It is identical in structure to the alpha glycoform of human erythropoietin.
Epoetin Alfa Warnings (Death, Viral Disease)
The misuse of epoetin alfa for physique- or performance-enhancing purposes is characterized as a high-risk practice. Like traditional blood doping methods, epoetin alfa can produce an abnormally high concentration of hemoglobin in the blood (polycythemia), which may result in heart attack, stroke, seizure, or death.
Many forms of epoetin alfa contain albumin, a purified human blood product. Although effective donor screening and product manufacturing procedures are in place, it still carries an extremely remote risk for transmission of viral disease.
Epoetin Alfa Side Effects
Side effects associated with the use of epoetin alfa may include flu-like symptoms such as fever, chills, headache, muscle pain, weakness, or dizziness. Such effects tend to be more pronounced at the initiation of therapy. Other side effects include rash, swelling of the skin, nausea, vomiting, diarrhea, high blood pressure, hyperkalemia (excess potassium in the blood), and irritation at the site of injection. In some instances epoetin alfa has been associated with thromboembolism, deep-vein thrombosis, pulmonary embolism, heart attack, and cerebrovascular accidents.
Epoetin Alfa Administration
Epoetin alfa injectable solution is given by subcutaneous or intravenous injection. The two paths of administration have greatly different effects on the blood level of the drug. When given by IV infusion, peak blood levels of the drug are reached within 15 minutes, and the elimination half-life ranges from 4 or 13 hours. When administered via the subcutaneous route, peak blood levels are reached between 5 and 24 hours, and the elimination half-life is approximately 24 hours. Given an equal dose, the peak plasma concentration of epoetin alfa will be significantly lower than the intravenous method. When used medically to treat severe anemia associated with chronic renal failure, the recommended starting dosage range is 50 to 100 Units/kg of bodyweight, given 3 times per week. The dosage is subsequently adjusted based on changes in hematocrit.
Healthy athletes using epoetin alfa for performanceenhancing purposes generally start on the very low end of the therapeutic spectrum, and adjust according to changes in hematocrit. This may entail initiating therapy with as little as 5 to 10 Units/kg of bodyweight, taken 3 times per week. Note that it is considered very important to monitor blood cell counts closely during the entire intake of epoetin alfa to help ensure hematocrit is not allowed to increase to an unhealthy level.
Epoetin Alfa Availability
Epoetin alfa is a very expensive compound, and its use is additionally isolated to certain athletic fields. As such, it is not widely traded on the black market. Given the high cost of this drug, however, it is a lucrative target for counterfeiters.
Newbies Research Guide reference
Description: Epogen or EPO comes in 2000, 3000, 4000, and 10,000 IU vials. EPO is an injectable protein hormone that acts on bone marrow to stimulate red blood cell production. This is a new drug which is being experimented with by some elite athletes especially distance runners and elite cyclists. It was developed for patients suffering aneniia due to disease. It has been very effective for what it is designed for and sometimes is used as a replacement for blood trans- fusions. Athletes use this drug to dramatically increase red blood cells which are the oxygen carrying components of blood. Athletes are well aware that if they can increase the oxygen-storing ability of their blood they can increase performance. This is the theory behind blood doping. EPO does the same thing but is more convenient considering the use of EPO just requires a number of injections. Blood doping requires drawing out approximately a liter of blood, freezing it, then thawing it and reinfusing it several weeks later. Unfortunately, EPO has some serious dangers associated with it. It is suspected to be the cause of over half a dozen deaths amongst a circle of elite Dutch cyclists. EPO has a dramatic effect on hematocrit which is the percentage of red blood cells in blood. A hematocrit of 40 means that 40% of the volume of blood is composed of red blood cells which is about normal. Athletes not uncommonly have a higher-than-average hematocrit. When an athlete injects EPO, there hematocrit can rise as much as 40%. This results in an especially high concentration of RBCS. The danger sets in when this hematocrit level gets too high. At this point, blood could literally ‘clog up’ an artery leading to a vascular disaster in the form of a heart attack stroke, cardiac failure, or a condition called pulmonary edema; this is a form of water logging of the lungs because of left ventricular failure. The potential for arterial accidents becomes even greater when an athlete gets dehydrated. Obviously, marathon runners and cyclists lose large amounts of fluid during competition. This loss of fluid can raise the concentration of hematocrit even more, increasing the risk of a fatality. EPO use is most widespread amongst endurance athletes yet a number of weightlifters have been experimenting with it.
Effective Dose: Between 50-300 IU/kg of bodyweight. Not to be used for more than 6 weeks. Will start seeing effects after week 2.
Street Price: I don’t have a clue on the street price of this compound. Dan Duchaine did say in his Underground BodyOpus book that the cost was most than Growth Hormone though.
Wlliam Llewellyn (2011) - Anabolics
Newbies Research Guide