Written by Ron Harris

14 July 2020

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supplementation drT

Ask Dr. Testosterone
By George Touliatos, MD

SUPPLEMENTATION

Several supplements promise wonders with flashy advertisements and fake pictures. Supplements themselves aren’t miraculous, but they assist in nutrition and they practically belong to sports nutrition. Supplements are necessary for the following reasons:

1) They cover nutritional needs based on poor nutrition or even malnutrition, excessive sweating and increased metabolism.

2) They assist in optimization of different systems, such as the endocrine with biosynthesis of hormones, or energy production in other tissues.

3) They boost immune response against viral infections, based on the crush of immunoglobulins during overtraining and periods of mental stress.

4) They even act as placebo effect, while the athlete believes he uses something special that gives him advantage over his opponents.

Supplements are not chemicals, of course, and therefore have not the plethora of side effects that medications have.

Supplements Worth Taking

Those that I recommend without any hesitation are the following:

Whey blend concentrate-isolate-hydrolysate, egg albumen, and micellar casein blend with different amino acid profile spectrums. Each of them has different time release, so by taking a protein blend during breakfast you can have a sustained release of amino acids.

Whey is rich in leucine, while casein in glutamine and albumen is rich in cysteine.

Whey concentrate is of slower absorption, but it also has a greater amount of carbs, fat and immunoglobulins. Unlike whey isolate or even hydrolysate that are highly absorbed and partially predigested. However, a protein over 90 percent of purity contains neglible amounts of carbs and we know that insulin is necessary for aminos transport into the muscles. Therefore, we realize that a whey concentrate at 70 percent of purity and five grams of carbs per scoop will have a slight kick on insulin to help utilize those aminos.

Amino acids of different sources (whey, egg, and beef, liver) are practical forms of protein consumption and predigested. They surely contribute to a positive nitrogen balance, having almost zero fat and carb content. They can be used either between, or with meals, as an extra source of protein. However, if used between meals they have to be taken with juice, for insulin production and optimal absorption, but they can be also in liquid form for maximum absorption.

Creatine monohydrate micro-ionized for optimal dilution and absorption is much more efficient than the esteric form, because monohydrate works through the osmotic effect. This is the influx of water from a hypertonic to a hypotonic environment and what actually takes place in muscle cells, under the influence of hyperglycemic carbs.

Creatine

Creatine monohydrate is the most anabolic supplement, increasing ATP stores, increasing strength in muscle performing anaerobic, explosive activity. Moreover, it has the ability to bring water intramuscularly, by the effect of osmosis (from a hypertonic to a hypotonic environment). Muscles consist 70 percent of water and creatine monohydrate use requires plenty of hydration.

The belief that creatine is responsible for water retention occurs only under overload. In such a case, water leaves from intracellular area and moves extracellular

The creatine loading phase takes place for five consecutive days (Monday to Friday) with 20 grams daily (split twice daily). While afterward, the maintenance phase occurs on a daily basis with 5 grams. The best timing to take creatine monohydrate is during higher insulin sensitivity, meaning post-workout and with breakfast (loading phase). The reason to take creatine right after the workout is first to enhance absorption and utilization, and second to stimulate the mTOR pathway of muscle growth.

Creatine monohydrate requires the presence of hyperglycemic carbohydrate in order to ensure insulin spike and influx into sarcoplasm. However, it’s preferable not to be used simultaneously with coffee, because it’s highly likely to be wasted in urine (caffeine diuretic effect). This is why other forms of creatine, such as esteric, are stacked in pre-workout formulas with CNS stimulants, because they don’t act osmotically like the monohydrate form.

Creatine is not banned from WADA, because first it is presented in red meat (the word for meat in Greek is “kreas,” coming from its creatine content), while it is a tripeptide consisting of arginine, methionine and glycine being synthesized in the kidneys and liver. Prolonged creatine abuse will elevate serum creatinine that will lower glomerular filtration rate GFR), and actually this is something that takes place under excessive red meat consumption.

Creatine has shown promising results in muscle inflammation and recovery post-workout, by lowering LDH linked with cellular death. Also, creatine has been associated with satellite cell proliferation, under maximum single reps, resembling myofibrial hypertrophy and hyperplasia.

Conjugated Linoleic Acid (CLA)

CLA is an UFA (omega-6) that is able to improve body composition and better analogy between skeletal muscle and adipose tissue. It actually deactivates the lipoprotein lipase enzyme, which is responsible for lipogenesis and fat storage. In this way, CLA can be useful under a DM2 patient with insulin resistance. Some studies show that CLA can help in testosterone synthesis, especially acting as catalyst in conversion of progesterone to androstenedione. Results, however, are directly proportional to the dose, duration and intensity of exercise

Glutamine

Glutamine, even though it is not an EAA, is considered as the one with the greatest abundance in skeletal muscle. Glutamine levels are going down under trauma and injuries, or even inflammation. Glutamine is beneficial for brain metabolism, gut health, immune response, GH production and cellular volumizing along with taurine, which also enhances in muscle glycogen synthesis when used post-workout.

Νiacin

Νiacin belongs to B complex vitamins (B3) and is widely used to improve HDL levels. Flushing niacin is based on allergic reaction by prostaglandins (inflammatory cytokines), dealing with skin reddening and itching. However, symptoms last less than 10 minutes and can be avoided if niacin is taken after a meal and not on an empty stomach. Moreover, niacin is a powerful vasodilator and capable of synthesizing tryptophan, that will eventually elevate melatonin. Niacin shouldn’t be taken at a dose of more than 500mg/24h because it can elevate transaminases and also A1C.

Caffeine

Caffeine belongs to the class of methylxanthines. It increases the aerobic capacity in a manner similar to the one of clenbuterol hydrochloride (bronchodilator, leading to the increase of VO2 max). It does not belong to the same class of substances (beta-2 stimulants), but has the ability to cause bronchodilation, so in doses >3mg/kg acts as an alternative solution for the treatment of paroxysmal asthmatic crisis.

Caffeine also stimulates the smooth muscle layer of the small intestine, which is regulated by the autonomic nervous system, so soon after we drink coffee with breakfast, an urge for defecation starts.

A fatal overdose of caffeine for a bodybuilder with a bodyweight of 100kg is approximately 10gr in a single dose (100mg/kg); while lethal levels in blood are found at around 80mg. Death occurs from cardiac arrest due to ventricular tachycardia – fibrillation. The intoxication of caffeine causes irritability-restlessness, tremor-trembling, rapid breathing-respiration, sweating, headaches, diarrhea syndromes, precordial chest pain and delirium. The abuse and addiction to caffeine is the most widespread and legal way of chemical enhancement, worldwide, on a daily basis.

Caffeine is able to pass through blood brain barrier and placenta. Caffeine acts synergistically as a catalyst to ephedrine hydrochloride and enhances beta oxidation of fatty acids, consequently lipolysis of the subcutaneous tissue. The peak of its concentration occurs within an hour, while its half-life is estimated around four hours. Proper dosage is estimated at 3mg/kg of bodyweight (300mg for a 100kg athlete). Even larger dosages (5mg/kg) increase the maximum strength and training intensity. At normal doses, caffeine has effects on learning and memory, improving reaction time, alertness, attention and concentration.

Caffeine is quite often combined with painkillers, such as paracetamol and multiplies the masking pain effect. It is also an antidote for a hangover crisis and migraine episode.

Yohimbe Bark

The yohimbe bark herb stimulates the alpha-2 adrenergic receptors. It causes positive inotropic, chronotropic action, through a sympathetic mimetic effect. Twenty years ago, its use was an alternative supplementation for erectile dysfunction, due to vascular issues. Yohimbine HCL – unlike clenbuterol and ephedrine HCL – causes peripheral vasodilation and vascular permeability. This solves the erectile dysfunctional problems in the corpus cavernosum (cavernous bodies) of the penis. At the same time, it prevents the return of blood to the heart through the venous system. Yohimbine was widely used, way before nitric oxide (NO) production drugs were manufactured.

In the sport of bodybuilding, Yohimbine HCL (yohimbe bark) is an ideal tool for boosting vascularity before getting on stage. Moreover, it enhances the process of beta oxidation and lipolysis in subcutaneous tissue. Its action is thermogenetic and therefore increases the BMR, leading to fat catabolism.

Pre-workout Formulas

They are the new era in supplementation in the last decade. After the withdrawal of ephedra ma huang and yohimbine stimulants as part of fat-burning thermogenic formulas, nitric oxide formula replaced them.

They improve mentality and focus, vascularity and blood flow, while they can assist in fat burning and prolong anaerobic threshold that leads to fatigue. This is achieved by carnosine, metabolized to beta-alanine and the sodium bicarbonate that act as blood pH buffers and eliminate lactic acid.

Key components include caffeine, green tea, theobromine, octopamine, black peper, beta-alanine, carnosine, citrulline, arginine, red wine extract, tyrosine and the esteric form of creatine. They act on adrenergic receptors with a sympathetic mimetic effect, in other words by stimulating catecholamines (epi, norepi). However it’s the only class of supplements that can become potentially dangerous and fatal under critical conditions of heart arrhythmia and myocardial infarction.

They can also elevate systolic blood pressure, leading to cerebral hemorrhagic stroke.

They are also prohibited in bipolar patients, with emotional instability. CNS stimulants bring a euphoric effect, which as a matter of fact is highly addictive (psychotropic), leaving a withdrawal effect when their use is ceased abruptly.

Collagen

Hydrolyzed collagen type II is the basic component of connective tissue that degenerates with ageing and factors like smoking. This leads to degradation of tendons, ligaments and articular surfaces, along with skin, hair, nails. Collagen requires ascorbic acid for its synthesis and hyaluronic acid for its absorption, along with lysine and proline amino acids.

Colostrum

Colostrum is produced by cow’s milk and is actually the first class derived milk in cows that lactate. It is highly enriched with immuloglobulins, making it superior for immune response. Moreover, it is considered to be high in somatomedin (insulin-like growth factor), thus colostrum can become anabolic. It is ideal during infections, trauma and injuries stacked with echinacea, vitamin C, probiotics, vitamin D, NAC and DHEA under sickness.

Carnitine

Carnitine is an amino acid derivative, able to assist in the beta oxidation of fatty acids in mitochondria (the powerhouse of cell). Carnitine is able to improve energy production under low-pace cardiovascular activity (jogging). It is beneficial for myocardium and energy production (inotropic effect) because heart utilizes FFAs under resting conditions. Liquid form of carnitine on empty stomach is used along with a ECA stack in order to enhance fat loss before cardio.

Arginine-Citruline

Arginine is non-essential amino acid, playing role in nitric oxide production and vasodilation. Citruline is arginine’s precursor that unlike arginine is not destroyed in the stomach by gastric fluid. Moreover, citruline is capable of eliminating ammonia (NH3) dealing with fatigue. While large doses of arginine, along with ornithine and lysine, are able to stimulate GHRH under fasting conditions either in high-intensity weightlifting, or in REM sleep. Arginine and citruline are used alternatively to 5PDE drugs to improve blood flow in the penis and also to lower systemic blood pressure

Medium-Chain Triglycerides (MCTs)

MCTs are medium-chain triglycerides that belong to SFAs. They are fats in liquid form that being rapidly released as simple carbs, useful under a ketogenic state when carbs are absent.

Dehydroepiandrosterone (Dhea)

DHEA is a steroid prohormone released from the adrenal glands. It is called as the mother of all hormones, because it can participate in the synthesis of many steroid hormones. DHEA is an androgen that metabolizes to androgen and estrogen (androstenedione and estrone) in both sexes. However, in females the androgenic metabolite is prominent, since women are of low testosterone. Unlike men where androgens dominate, the estrogenic metabolite will be more prominent.

DHEA can be used for anti-aging and age management as part of hormone replacement therapy both in males and females, showing to be promising in dementia (Alzheimer's disease) and immune response. Moreover, it can improve libido by elevating free testosterone, through binding and lowering SHBG. DHEA can also fight against anemia and osteopenia. It has poor ergogenic effects, but as an androgen it might assist slightly with beta oxidation and improve body composition. Especially from its metabolite, 7-Keto DHEA, that has thermogenic properties. This substance in the form of cream has been found to increase the elasticity of the skin of the face and prevent aging and destruction of collagen connective tissue.

DHEA should be supplemented accordingly to the serum levels of S-DHEA, the prominent form in blood. It is better to be split into a.m./p.m. doses, in order to avoid spiking of E1, but also to have steady levels in blood.

DHEA metabolizes to 7-Keto DHEA that has a thermogenic effect and is available as a fat-loss supplement. However it has no effect on steroid metabolism, thus it doesn’t interfere with sex hormones (androgens or estrogens).

Alpha-Lipoic Acid (ALA)

ALA is among the strongest antioxidants, helping to regulate blood sugars levels by acting as an insulin mimicker. It also helps to restore synthesis of glutathione in the liver and fights against free radical cellular damage. It acts synergistically with other antioxidant vitamins like ascorbic acid and tocopherol, coenzyme Q10. ALA is capable of improving insulin sensitivity, by improving glucose uptake by muscle cells and preventing glucose uptake by fat cells, or adipocytes.

Glutathione

Glutathione is the most powerful antioxidant in human body, synthesized inthe liver by three aminos (glutamine, cysteine and glycine); therefore it is considered as tripeptide. Its precursor is N-Acetyl Cysteine that along with glutamine can formulate glutathione.

Glutathione prevents oxidation of erythrocytes, boosts immune system and aging.

Milk thistle also helps liver to synthesize more efficiently glutathione.

Glutathione is quite fragile in the gastric environment so it is preferable to be administrated parenthetically, meaning intramuscular, or even via intravenous. Glutathione is ideal for liver detoxification under alcohol drinking and AAS use.

Melatonin

Melatonin is a hormone produced by the pineal gland during darkness, and is responsible for introduction into sleep. It is considered to be a powerful antioxidant as well, while tryptophan acts as melatonin’s precursor, through its conversion to serotonin.

Melatonin is ideal to deal with jet lag under long trips with different time zones. It is capable of enhancing natural GH release under REM sleep, while it acts synergistically with other antioxidants like vitamin C. Furthermore, it’s also a natural booster of immune response, by activating T/B cells of thymus gland.

VITAMINS

Vitamin C or ascorbic acid is a powerful antioxidant that helps in collagen synthesis and can also lower post-workout cortisol. Ascorbic acid plays a significant role in the prevention of upper respiratory infections against viruses. It is water soluble, therefore it’s not accumulated (unlike ADEK), but wasted in the urine instead. Like B complex, the best form is also esteric, that is not affected by gastric fluid. Under its deficiency, scurvy develops, which was a common disease among sailors in the 19th century.

Vitamin D3 or calciferol is a prohormone and requires fatty meal for its absorption, but also UV light and cholesterol for its synthesis. It’s better to be stacked along with vitamin K2 in order to lead calcium toward bone tissue and not arterial endothelium. D3/K2 dosage has to be administrated accordingly to 1, 25(OH) D3 serum levels, the active form of vitamin D. Low vitamin D is associated with increased overall mortality rates, low bone mineral density and osteoporosis, and bone fractures. While it has promising results under hypogonadism and HPTA restoration.

Vitamin E, known as tocopherol, is important in fertility to both men and women. It improves spermatozoa motility and zygote stability in uterus. Like vitamin D, it’s better to be taken after meal for better absorption, but not under prolonged periods because it can lead to toxicity. Vitamin E prevents oxidation of erythrocytes.

Vitamin A, known as retinol, has a significant role in vision under darkness, while it can heal a cornea ulcer. Moreover, it is the basis of most powerful medication against acne, Accutane (retinoic acid). Because vitamin A can become toxic and accumulate in the liver, we can use its precursor antioxidant beta-carotene.

Cobalamin or B12 vitamin is considered as the vitamin of vitality. It has major role in erythrocytosis taking place in red bone marrow. B12, along with folic acid and iron, can boost hemoglobin synthesis and improve stamina, and VO2 max. Cobalamin can be injected both IM/IV.

Zinc is an important mineral, participating in hundreds of biochemical procedures, among them is the synthesis of testosterone, while magnesium plays a role in muscle relaxation, thus taken before sleep (ZMA).

EFAs (omega 3-6-9) such as ALA, LA, OA, CLA, GLA, DHA, EPA and ARA, have a wide range of health benefits, but also help in muscle growth.

Joint formula with:

1) glucosamine

2) chondroitin

3) MSM

4) shark cartilage

5) hydrolyzed collagen

6) hyaluronic acid

7) tumeric

BCAAs with leucine, isoleucine and valine but in 4/1/1 or 8/1/1 analogy. BCAAs can act either as anticatabolic, but also as energy production, since they aren’t metabolized in the liver, but directly into the muscles.

Leucine is known as the most anabolic of essential amino acids, the one that stimulates mTOR, the rapamycin muscle growth pathway.

HMB, known as beta-hydroxybutyric acid, the metabolite of leucine, is capable of stimulating mTOR and GH/IGF-1 axis.

Good sources of some minerals and elements:

=> Potassium: bananas

=> Iodine: haddock

=> Iron: cocoa (trivalent), beef

=> Selenium: turkey

=> Zinc: oysters

=> Vegetable fibers: broccoli

=> Omega-3 fatty acids: salmon, sardines

Foods sources rich in vitamins and metal trace elements:

=> Vitamin A (retinol): apricots

=> Vitamin B1 (thiamine): brown rice

=> Vitamin B2 (riboflavin): liver

=> Vitamin B3 (niacin): chicken

=> Vitamin B5 (pantothenic acid): peanuts

=> Vitamin B6 (pyridoxine): oatmeal

=> Folic acid: spinach

=> Vitamin B12 (cobalamin): mackerel

=> Vitamin C (ascorbic acid): peppers

=> Vitamin D (calciferol): salmon

=> Vitamin E (tocopherol): olive oil

=> Vitamin K: tomatoes

=> Calcium: emmental cheese

=> Magnesium: giant beans

TABLE OF SUPPLEMENTS

*Anabolic supplements*	creatine monohydrate leucine
*Anti-catabolic supplements*	BCAAs Glutamine HMB
*Vasodilatory supplements*	arginine citruline yohimbine ginko biloba niacin B3 red wine
*Thermogenic supplements*	Ma huang caffeine 7-keto DHEA synephrine green tea octopamine
*Lipotropic supplements*	CLA carnitine choline inositol lecithin
*Joint aid*	hydrolyzed collagen glucosamine chondroitin hyaluronic acid ΜSM shark cartilage
*Nootropics*	tyrosine phenylalanine acetyl carnitine
GH boosters	Arginine-ornithine-lysine GABA
Liver protectants	milk thisle liv 52 TUDCA N-acetylcysteine glutathione Alpha-Lipoic Acid
Sleeping agents	melatonin 5HTP magnesium GABA
Insulin mimickers	ALA
Testosterone boosters	D Aspartic acid Tribulus terestis MACA ZMA
*Αntioxidants*	beta carotene ascorbic acid tocopherol selenium lycopene NAC ALA Q10 silimarin glutathione green tea Godji berry
*Cardiovascular support*	omega-3,6,9 EFAs phytosterols krill oil policosanol bergamont red rice yeast Β3 niacin resveratrol
*EPO boosters*	hemic iron (+ascorbic acid) folate cobalamin (B12)
*Lactate buffers*	Sodium bicarbonate (baking soda) carnosine beta-alanine
*Diuretics*	green tea caffeine uva ursi dandelion pyridoxine B6

George Touliatos, MD is an author, lecturer, champion competitive bodybuilder and expert in medical prevention regarding PED use in sports. Dr. Touliatos specializes in medical biopathology and is the medical associate of Orthobiotiki.gr and Medihall.gr, Age Management and Preventive Clinics in Athens, Greece. Heis the author of four Greek books on bodybuilding, has extensively developed articles for www.anabolic.org and is the medical associate for the book Anabolics, 11th Edition (2017). Dr. Touliatos has been a columnist for the Greek editions of MuscleMag and Muscular Development magazines, and has participated in several seminars across Greece and Cyprus, making numerous TV and radio appearances, doing interviews in print and online. His personal website is https://gtoul.com/

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