Designer Anabolic/ Anti-catabolic Agents

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Designer Anabolic/ Anti-catabolic Agents

• Lecture 21

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What works?

• We know that
• Anabolic steroids (testosterone) increase FFM and
  muscular strength. They also have an
  anti-catabolic effect.
• Schedule III drug available legally with a
  prescription
• Prohormones (androstenedione and androstenediol)
  have some (maybe) effect increasing FFM or
  strength performance.
• Sale of androstenedione and androstenediol (but
  not DHEA) restricted by U.S. govt. in late 2005

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What works?

• We know that
• Anabolic steroids (testosterone) increase FFM and
  muscular strength. They also have an
  anti-catabolic effect.
• Prohormones (androstenedione and androstenediol)
  have no apparent effect on increasing FFM or
  strength performance.
• Creatine - will be talking about creatine on
  Wednesday)

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• Are there other products that work to increase
  FFM, strength and power?
• Anabolic (growth hormone secretagogues)
• Anti-catabolic (inhibitors of protein degradation)

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Popular Body Building Supplements

• Anabolic
• Growth Hormone secretagogues
• Zinc/Magnesium Aspartate (ZMA)
• Arginine alpha-ketoglutarate (AAKG)
• Anti-catabolics
• Beta-hydroxy beta-methylbutyrate (HMB)

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• Growth hormone (somatotropin)
• Stimulates bone and cartilage growth
• Facilitates protein synthesis
• Increasing amino acid transport into muscle
• Stimulating RNA formation
• Facilitating protein synthesis
• Also slows CHO breakdown and mobilizes fat as an
  energy source.
• Exercise stimulates an increase in circulating GH
  
• and preserves plasma glucose for the CNS.

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Growth Hormone Ergogenic Aid

• Use medically, children who suffer from GH
  deficiencies or kidney failure
• Reduced GH low FFM and high fat mass
• Increased GH in youth gigantism
• Acromegaly enlarged hands, feet and facial
  features.
• Synthetic growth hormone (recombinant DNA
  production) is used by athletes and bodybuilders
  to increase strength performance.

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Growth Hormone Performance

• Appealing to strength and power athletes because
  at physiological levels
• Stimulates amino acid uptake and protein
  synthesis
• Enhances fat breakdown
• Conserves glycogen reserves
• Also GH does not suppress the body's
• hypothalamic-pituitary-gonadal axis like
• anabolic steroids. Use can be continuous.

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• One study found that 6 weeks of resistance
• training with GH decreased body fat and increased
  
• FFM significantly (but second study found no
  effect).
• GH is illegal and very expensive. The hormone
• can only be obtained on the black market and can
• cost 500-4000/month.
• GH is usually stacked with anabolic steroids and
  is
• typically used with insulin to get maximum
  results.
• Body-builders use the combination to achieve the
• desired muscle size, vascularity and appearance
  of
• paper thin skin sucked to muscle.
• Growth hormone use can lead to diabetes

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Growth hormone secretagogues

• Use of amino acids to stimulate GH secretion.
• Arginine
• Lysine
• Ornithine
• Exercise increases GH concentrations so these
• amino acids are often taken before a workout to
• further accentuate the exercise-induced GH
  release.

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• Amino acid ingestion and GH
• Combination of arginine and lysine together seems
  to be more potent than either alone.
• Trained individuals have a blunted response
  (especially if they are strength trained eating a
  high protein diet)
• Women show a greater response than men
• Amino acid ingestion, GH and exercise
• Ingestion of amino acids before exercise does not
  increase GH more than exercise alone.
• Consuming a protein supplement before exercise
  and immediately after exercise had no effect on
  maintaining elevated GH concentrations.

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• May be a dosage or timing issue, further studies
  necessary... There are no well-designed studies
  using specific amino acids as GH secretagogues in
  conjunction with strength training.
• Alternatively, peptide and non-peptide compounds
  can also stimulate GH release.
• Ex synthetic hexapeptide (GHRP-6)
• These secretagogues do increase circulating GH
  and IGF-
• 1, there are no published studies indicating how
  use
• would affect athletic performance.

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Zinc/Magnesium Aspartate (ZMA)

• Popular supplement to promote anabolism at night.
  
• Zinc/magnesium deficiencies may reduce the
  production of testosterone and IGF-1 (regulates
  the action of GH)
• Shown that athletes in training may be zinc
  deficient. Zinc participates in metabolism and
  protection against free radical damage.
• Magnesium supplementation showed a decrease in
  cortisol (theoretically magnesium would be
  anti-catabolic).

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• Studies
• Brilla and Conte reported ZMA supplementation in
  football players during off-season resistance
  training promoted increases in testosterone,
  IGF-1 and muscular strength.
• Wilborn et al. (2004) double blind study design
• n42 resistance trained males
• matched according to FFM
• Took either ZMA or placebo prior to going to
  sleep during 8 weeks of strength training
• Results no significant differences between
  groups in hormone status, body comp, 1 RM bench
  press and leg press, muscular endurance or
  anaerobic capacity.
• - population was resistance trained.

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Arginine alpha-ketoglutarate (AAKG)

• Anabolic and anti-catabolic
• Arginine
• stimulates GH release
• Raises nitric oxide (NO) synthesis
• NO acts as a vasodilator. Hypothesized that NO
  supplementation would enhance blood flow, oxygen
  delivery and glucose uptake by working muscles.
• a-ketoglutarate
• Intermediate in the TCA cycle and is a precursor
  for the synthesis of glutamine and arginine.
• Limited data on athletic performance however,
  there is some data that suggests an
  anti-catabolic role. (similar to glutamine under
  conditions over severe stress, ex surgery)

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• Campbell et al. (2006)
• Randomized, double-blind, controlled study design
  
• 12g daily (4g, 3X per day) over 8 weeks of
  resistance training (4X per week)
• Measures were taken at 0, 4, 8 weeks in blood
  markers, 1 RM max strength, aerobic power,
  anaerobic endurance, total body water and body
  composition.

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Beta-hydroxy beta-methylbutyrate (HMB)

• HMB is a metabolite of the amino acid leucine.
• Found naturally in small quantities in catfish,
  citrus fruits and breast milk.
• Leucine is an essential amino acid that has the
  highest oxidation rate of all amino acids during
  exercise.
• HMB derived from leucine is converted to HMG-CoA
  in some tissues and serves as a key carbon source
  for cholesterol synthesis in various cell types.
• - saturating the cell with HMG-CoA would allow
  the cell to undergo the maximum growth response
  (athletes, muscle hypertrophy in response to
  resistance training)

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• Supplementing with 1.5-3g/d of calcium HMB has
  demonstrated increases in muscle mass and
  strength (especially in untrained individuals
  initiating a training program)
• Gains are typically 0.5 to 1kg greater than
  controls during 3-6 weeks of training.
• Also evidence that HMB is anti-catabolic. HMB in
  conjunction with creatine may have an additive
  effect but results are unclear.
• Large variability among athletes, more research
  is necessary.

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• Please check the website for a reading on
  tetrahydrogestrinone (THG), the designer anabolic
  steroid that BALCO constructed in 2002-2003.