Actovegin

Last updated

Actovegin is a highly filtered extract obtained from calf blood which enhances aerobic oxidation in mammals. [1] This improves absorption of glucose and oxygen uptake in tissue, [1] which may enhance physical performance and stamina. Injecting it into the blood track is not allowed.[ clarification needed ] Local utilisation is allowed in countries like Canada and Sweden. Doctors like Hans-Wilhelm Müller-Wohlfahrt and Richard Steadman think Actovegin should be allowed in general. Others think there is not enough research, and persons from the World Anti-Doping Agency like Olivier Rabin is sceptical that it is having more than a placebo effect. [2] [3]

Contents

Actovegin made headlines from 2009 to 2011 when Canadian sports doctor Anthony Galea was charged with drug smuggling, conspiring to lie to federal agents, unlawful possession with intent to distribute and practising medicine without a licence in the United States. Galea pleaded guilty of bringing misbranded and unapproved drugs, including Nutropin, a human growth hormone, and Actovegin, into the United States. The discipline committee for the College of Physicians and Surgeons of Ontario (CPSO) suspended Galeas license for 9 months for professional misconduct. [4] [5] [6] [7]

Actovegin made headlines again in 2016, stemming from a 2011 incident, when American former professional athlete and fashion designer Nick Brandt-Sorenson was charged with a one count misdemeanor by the United States Department of Justice involving misbranding Actovegin into interstate commerce. [8] [9] [10] [11] Afterwards in 2016, USADA banned the working artist and fashion designer Nick Brandt-Sorenson for life after his third anti-doping offense of being uncooperative. [12]

On 08 Sept 2011, Swiss NYCOMED Actovegin® was awarded “Medication of the Year” in Ukraine, with sincere congratulations expressed by the Head of Committee on Public Health Supreme Council of Ukraine, the Minister of Public Health of Ukraine Aleksandr Anischenko and the Chairman of State Administration of Ukraine for Medicinal Products Aleksey Soloviov. [13]

As revealed by later testimony by riders, Actovegin was also regularly used by Lance Armstrong and the members of his U.S. Postal Service Pro Cycling Team on the 2000 Tour de France to enhance their performance. [14] One small-scale trial found that Actovegin did not improve human peak performance, at least in the short-term. [15] Actovegin can be useful to treat muscle injuries, . [16]

Mechanism of action

According to Gulevsky, et al., Actovegin "is highly purified hemodialysate extracted from vealer blood by ultrafiltration." [1]

Actovegin has been shown to improve the transport of glucose over a plasma membrane and the uptake of oxygen by tissues. [1] This can lead to aerobic oxidation, which provides a cell with access to more energy and potentially enhances its function. [1] Actovegin has large amounts of superoxide dismutase enzymes and magnesium. [17]

Uses and side effects

Nycomed, a Swiss drug company which manufactures Actovegin, [18] claims it can be used for circulation and nutrition disturbances, skin grafting, burns, and wound-healing impairment. [19] Actovegin has also been used as a performance enhancer. [20]

It has been investigated for use in treatment of polyneuropathy in diabetes, [21] and for stroke. [22] [23] One study found that when tissues suffer from hypoxia caused circulation abnormalities, Actovegin helps capillaries improve circulation by enhancing the neogenic mechanism in blood vessels. [17]

Anaphylactic shock has been observed in at least one patient treated with actovegin. [24]

There are reports suggesting that Actovegin have ergogenic ability, however one small trial found no apparent benefit from short-term use. [15]

Two studies certified Actovegin to have an anti-inflammatory effect. One of the two studies certified Actovegin to reduce Progressive muscular atrophy-induced inflammation in human cells. [25] [26]

Another study certified Actovegin to have a positive impact on the growth of muscle cells. [27] [28]

Manufacturing process

Actovegin is a deproteinated, pyrogen- and antigen-free hemodialysate of calf blood. It is manufactured from calf blood in several steps by ultrafiltration using various precipitation techniques and filters. The analysis of the final product shows that it contains a mixture of natural substances: both inorganic components such as common blood electrolytes (e.g. chloride, phosphate, sodium, potassium, calcium, and magnesium, several sources for nitrogen, amino acids, peptides, glucose, acetate and lactate) and organic components such as amino acids, a number oligopeptides, nucleosides, glycosphingolipids and products of the intermediary metabolism. [29]

Market approvals

As of July 2011, the drug was not approved for sale, importation, or use in the United States. [30] It is an unapproved drug in Canada as well.

Related Research Articles

<span class="mw-page-title-main">Growth hormone</span> Peptide hormone that stimulates growth, cell reproduction and cell regeneration

Growth hormone (GH) or somatotropin, also known as human growth hormone in its human form, is a peptide hormone that stimulates growth, cell reproduction, and cell regeneration in humans and other animals. It is thus important in human development. GH also stimulates production of IGF-1 and increases the concentration of glucose and free fatty acids. It is a type of mitogen which is specific only to the receptors on certain types of cells. GH is a 191-amino acid, single-chain polypeptide that is synthesized, stored and secreted by somatotropic cells within the lateral wings of the anterior pituitary gland.

<span class="mw-page-title-main">Erythropoietin</span> Protein that stimulates red blood cell production

Erythropoietin, also known as erythropoetin, haematopoietin, or haemopoietin, is a glycoprotein cytokine secreted mainly by the kidneys in response to cellular hypoxia; it stimulates red blood cell production (erythropoiesis) in the bone marrow. Low levels of EPO are constantly secreted in sufficient quantities to compensate for normal red blood cell turnover. Common causes of cellular hypoxia resulting in elevated levels of EPO include any anemia, and hypoxemia due to chronic lung disease.

Carbohydrate metabolism is the whole of the biochemical processes responsible for the metabolic formation, breakdown, and interconversion of carbohydrates in living organisms.

<span class="mw-page-title-main">Exercise physiology</span>

Exercise physiology is the physiology of physical exercise. It is one of the allied health professions, and involves the study of the acute responses and chronic adaptations to exercise. Exercise physiologists are the highest qualified exercise professionals and utilise education, lifestyle intervention and specific forms of exercise to rehabilitate and manage acute and chronic injuries and conditions.

In competitive sports, doping is the use of banned athletic performance-enhancing drugs by athletic competitors, as a way of cheating. The term doping is widely used by organizations that regulate sporting competitions. The use of drugs to enhance performance is considered unethical, and is prohibited by most international sports organizations, including the International Olympic Committee. Furthermore, athletes taking explicit measures to evade detection exacerbate the ethical violation with overt deception and cheating.

<span class="mw-page-title-main">Anaerobic exercise</span> Physical exercise intense enough to cause lactate formation

Anaerobic exercise is a type of exercise that breaks down glucose in the body without using oxygen; anaerobic means "without oxygen". In practical terms, this means that anaerobic exercise is more intense, but shorter in duration than aerobic exercise.

<span class="mw-page-title-main">Altitude training</span>

Altitude training is the practice by some endurance athletes of training for several weeks at high altitude, preferably over 2,400 metres (8,000 ft) above sea level, though more commonly at intermediate altitudes due to the shortage of suitable high-altitude locations. At intermediate altitudes, the air still contains approximately 20.9% oxygen, but the barometric pressure and thus the partial pressure of oxygen is reduced.

<span class="mw-page-title-main">Trimetazidine</span> Drug for angina pectoris sold under many brand names

Trimetazidine is a drug for angina pectoris sold under many brand names. Trimetazidine is described as the first cytoprotective anti-ischemic agent developed and marketed by Laboratoires Servier (France). It is an anti-ischemic (antianginal) metabolic agent of the fatty acid oxidation inhibitor class, meaning that it improves myocardial glucose utilization through inhibition of fatty acid metabolism.

Blood doping is a form of doping in which the number of red blood cells in the bloodstream is boosted in order to enhance athletic performance. Because such blood cells carry oxygen from the lungs to the muscles, a higher concentration in the blood can improve an athlete's aerobic capacity (VO2 max) and endurance. Blood doping can be achieved by making the body produce more red blood cells itself using drugs, giving blood transfusions either from another person or back to the same individual, or by using blood substitutes.

<span class="mw-page-title-main">Sports nutrition</span> Study and practice of nutrition to improve performance

Sports nutrition is the study and practice of nutrition and diet with regards to improving anyone's athletic performance. Nutrition is an important part of many sports training regimens, being popular in strength sports and endurance sports. Sports nutrition focuses its studies on the type, as well as the quantity of fluids and food taken by an athlete. In addition, it deals with the consumption of nutrients such as vitamins, minerals, supplements and organic substances that include carbohydrates, proteins and fats.

Performance-enhancing substances, also known as performance-enhancing drugs (PEDs), are substances that are used to improve any form of activity performance in humans. A well-known example of cheating in sports involves doping in sport, where banned physical performance-enhancing drugs are used by athletes and bodybuilders. Athletic performance-enhancing substances are sometimes referred as ergogenic aids. Cognitive performance-enhancing drugs, commonly called nootropics, are sometimes used by students to improve academic performance. Performance-enhancing substances are also used by military personnel to enhance combat performance.

<span class="mw-page-title-main">AICA ribonucleotide</span> Chemical compound

5-Aminoimidazole-4-carboxamide ribonucleotide (AICAR) is an intermediate in the generation of inosine monophosphate. AICAR is an analog of adenosine monophosphate (AMP) that is capable of stimulating AMP-dependent protein kinase (AMPK) activity. The drug has also been shown as a potential treatment for diabetes by increasing the metabolic activity of tissues by changing the physical composition of muscle.

<span class="mw-page-title-main">Erythropoiesis-stimulating agent</span> Medicine that stimulates red blood cell production

Erythropoiesis-stimulating agents (ESA) are medications which stimulate the bone marrow to make red blood cells. They are used to treat anemia due to end stage kidney disease, chemotherapy, major surgery, or certain treatments in HIV/AIDS. In these situations they decrease the need for blood transfusions. The different agents are more or less equivalent. They are given by injection.

<span class="mw-page-title-main">Meldonium</span> Chemical compound

Meldonium is a limited-market pharmaceutical, developed in 1970 by Ivars Kalviņš at the USSR Latvia Institute of Organic Synthesis, and now manufactured by the Latvian pharmaceutical company Grindeks and several generic manufacturers. It is primarily distributed in Eastern European countries as an anti-ischemia medication.

Doping, or the use of restricted performance-enhancing drugs in the United States occurs in different sports, most notably in the sports of baseball and football.

<span class="mw-page-title-main">Diuretic</span> Substance that promotes the production of urine

A diuretic is any substance that promotes diuresis, the increased production of urine. This includes forced diuresis. A diuretic tablet is sometimes colloquially called a water tablet. There are several categories of diuretics. All diuretics increase the excretion of water from the body, through the kidneys. There exist several classes of diuretic, and each works in a distinct way. Alternatively, an antidiuretic, such as vasopressin, is an agent or drug which reduces the excretion of water in urine.

<span class="mw-page-title-main">Bemethyl</span> Chemical compound

Bemethyl, also commonly referred to in literature as bemitil, is a synthetic actoprotector which is also antihypoxant, antioxidant, and antimutagenic. Certified in Ukraine as a dietary supplement, bemethyl is commonly used in preparing for international competitions by Ukrainian national sport teams. Bemethyl is formulated as a hydrobromide salt. Its parent compound is 2-ethylsulfanyl-1H-benzimidazole.

The practice of doping in tennis involves the use of prohibited, performance-enhancing substances listed by the International Tennis Federation (ITF) and World Anti-Doping Agency (WADA). The practice is considered unsportsmanlike and unethical, with punishments for such offences ranging from official warnings to career bans, depending on the severity of the offence.

Doping in figure skating involves the use of illegal performance-enhancing drugs (PEDs), specifically those listed and monitored by the World Anti-Doping Agency (WADA). Figure skaters occasionally have positive doping results but it is not common. Bans can be enforced on figure skaters by the International Skating Union (ISU) and each country's individual skating federation. These bans can often be career ending due to the competitive nature of figure skating. A ban may be revoked if it can be proved that the skater tested positive for a prescribed medication. Some figure skaters will use PEDs to help with recovery time, allowing them to train harder and longer. Figure skating is an aesthetic sport that combines both athleticism and artistic licence, where weight-loss substances will have little effect on athletic performance but skaters may be perceived as more graceful and sleek, which is required for an athlete to be competitive.

Gene doping is the hypothetical non-therapeutic use of gene therapy by athletes in order to improve their performance in those sporting events which prohibit such applications of genetic modification technology, and for reasons other than the treatment of disease. As of April 2015, there is no evidence that gene doping has been used for athletic performance-enhancement in any sporting events. Gene doping would involve the use of gene transfer to increase or decrease gene expression and protein biosynthesis of a specific human protein; this could be done by directly injecting the gene carrier into the person, or by taking cells from the person, transfecting the cells, and administering the cells back to the person.

References

  1. 1 2 3 4 5 Gulevsky, Alexander Kirillovich; Abakumova, Yelena Sergeevna; Moiseyeva, Natalya Nikolaevna; Ivanov, Yevgeniy Gennadievich (2011). "Influence of Cord Blood Fraction (below 5 kDa) on Reparative Processes during Subchronic Ulcerative Gastropathy". Ulcers. 2011: 1–9. doi: 10.1155/2011/214124 .
  2. ↑ Dopingfund in Göteborg, Polizei stellt Ermittlungen ein
  3. ↑ The doctor they call 'Healing Hans', ESPN, 2011-12-16.
  4. ↑ Fish, Mike (December 16, 2011). "Anthony Galea receives no jail time". ESPN. Retrieved December 16, 2011.
  5. ↑ Doheny, Kathleen. "FAQ on Actovegin: An Expert Explains How the Drug May Enhance Athletic Performance." WebMD Health News. December 16, 2009. Accessed 2011-09-16.
  6. ↑ Schmidt, Michael S.; Austen, Ian (2009-12-17). "Doctor Under Investigation Is Charged in Canada". The New York Times. Retrieved 2009-12-17.
  7. ↑ Canadian regulatory body suspends Dr. Anthony Galea for nine months following U.S. sports doping scandal, Daily News, 2017-12-06.
  8. ↑ "Former Pro Cyclist Pleads Guilty Misbranded/Non FDA Approved Drug Importation". Partnership for Safe Medicines. 2016-03-24. Retrieved 2023-03-01.
  9. ↑ "Former Pro Cyclist Pleads Guilty To Importing, Selling Performance Enhancing Drugs". www.cbsnews.com. 16 March 2016. Retrieved 2023-03-01.
  10. ↑ companies (2016-04-18). "Fitness app Strava faces an uproar over an elite cycling user linked to doping". Los Angeles Times. Retrieved 2023-03-01.
  11. ↑ Flax, Peter (2016-03-28). "Who is Thorfinn-Sassquatch? The mysterious case of a Los Angeles Strava legend". CyclingTips. Retrieved 2023-03-01.
  12. ↑ "L.A. cyclist who sold performance-enhancing drugs to be sentenced today". Daily News. 2016-07-20. Retrieved 2023-03-01.
  13. ↑ "Actovegin And Other NYCOMED Products Called The Medicines Of The Year at PANACEA-2011". www.newswire.com (Press release). Retrieved 2023-03-06.
  14. ↑ USADA v. Armstrong, Reasoned decision, section IV B 3.e (pp. 42–45)(USADA10 October 2012). Text
  15. 1 2 Lee P, Nokes L, Smith PM (2012). "No effect of intravenous Actovegin® on peak aerobic capacity". Int J Sports Med. 33 (4): 305–9. doi:10.1055/s-0031-1291322. PMID   22318562. S2CID   2760688.
  16. ↑ Lee, P.; Rattenberry, A.; Connelly, S.; Nokes, L. (2011). "Our Experience on Actovegin, is it Cutting Edge?". International Journal of Sports Medicine. 32 (4): 237–41. doi:10.1055/s-0030-1269862. PMID   21271496.
  17. 1 2 Nordvik, B. "Actovegin. New Aspects of Clinical Application." In Collected Book of Research and Practice Articles. S. A. Rumyantseva, ed. St. Petersburg, Russia: MAPO, 2002, p. 280.
  18. ↑ "Nycomed May Invest 35 Million Euros in Ukrainian Production Capacities." The Pharma Letter. 3 May 2011. Accessed 2011-09-16.
  19. ↑ "Actovegin." Nycomed. 2011. Accessed 2011-09-16.
  20. ↑ Tsitsimpikou, Christina; Tsiokanos, Athanasios; Tsarouhas, Konstantinos; Schamasch, Patrick; Fitch, Kenneth D; Valasiadis, Dimitrios; Jamurtas, Athanasios (2009). "Medication Use by Athletes at the Athens 2004 Summer Olympic Games". Clinical Journal of Sport Medicine. 19 (1): 33–8. doi:10.1097/JSM.0b013e31818f169e. PMID   19124981. S2CID   40623178.
  21. ↑ Ziegler, D.; Movsesyan, L.; Mankovsky, B.; Gurieva, I.; Abylaiuly, Z.; Strokov, I. (1997). "Treatment of Symptomatic Polyneuropathy With Actovegin in Type 2 Diabetic Patients". Diabetes Care. 33 (11): 1809–14. doi:10.2337/dc09-0545. PMC   2713653 . PMID   9470838.
  22. ↑ Derev'yannykh, E. A.; Bel'skaya, G. N.; Knoll, E. A.; Krylova, L. G.; Popov, D. V. (2008). "Experience in the use of actovegin in the treatment of patients with cognitive disorders in the acute period of stroke". Neuroscience and Behavioral Physiology. 38 (8): 873–5. doi:10.1007/s11055-008-9051-0. PMID   18802768. S2CID   8234398.
  23. ↑ Guekht, A; Skoog, I; Edmundson, S; Zakharov, V; Korczyn, AD (2017). "ARTEMIDA Trial (A Randomized Trial of Efficacy, 12 Months International Double-Blind Actovegin): A Randomized Controlled Trial to Assess the Efficacy of Actovegin in Poststroke Cognitive Impairment". Stroke. 48 (5): 1262–1270. doi:10.1161/STROKEAHA.116.014321. PMC   5404405 . PMID   28432265.
  24. ↑ Maillo, Luis (2008). "Anaphylactic Shock with Multiorgan Failure in a Cyclist after Intravenous Administration of Actovegin". Annals of Internal Medicine. 148 (5): 407. doi: 10.7326/0003-4819-148-5-200803040-00022 . PMID   18316765.
  25. ↑ "Comprehensive Analytics of Actovegin® and Its Effect on Muscle Cells". 11 September 2017.{{cite journal}}: Cite journal requires |journal= (help)
  26. ↑ Reichl, F. X.; Högg, C.; Liu, F.; Schwarz, M.; Teupser, D.; Hickel, R.; Bloch, W.; Schweikl, H.; Thomas, P.; Summer, B. (July 2020). "Actovegin® reduces PMA-induced inflammation on human cells". European Journal of Applied Physiology. 120 (7): 1671–1680. doi:10.1007/s00421-020-04398-2. PMC   8497287 . PMID   32447451.
  27. ↑ Reichl, F. X.; Holdt, L. M.; Teupser, D.; Schütze, G.; Metcalfe, A. J.; Hickel, R.; Högg, C.; Bloch, W. (2017). "Comprehensive Analytics of Actovegin® and Its Effect on Muscle Cells". International Journal of Sports Medicine. 38 (11): 809–818. doi: 10.1055/s-0043-115738 . PMID   28895623.
  28. ↑ Fiedler, Matthias (29 April 2021). "The eternal medicine man". Der Spiegel (in German).
  29. ↑ Buchmayer F, Pleiner J, Elmlinger MW, Lauer G, Nell G, Sitte HH (2011). "Actovegin: a biological drug for more than 5 decades". Wien Med Wochenschr. 161 (3–4): 80–8. doi:10.1007/s10354-011-0865-y. PMID   21404144. S2CID   20989513.
  30. ↑ Kovaleski, Serge. "Canadian Doctor Tied to Professional Athletes Guilty of Drug Charge." New York Times. July 6, 2011. Accessed 2011-09-16.
This page is based on this Wikipedia article
Text is available under the CC BY-SA 4.0 license; additional terms may apply.
Images, videos and audio are available under their respective licenses.