Dr. Testosterone
By George Touliatos, MD

CNS STIMULANTS

EPHEDRINE HYDROCHLORIDE (Ephedrine HCL)

It is administrated for allergic rhinitis (runny nose) and it belongs to the sympathomimetic central nervous system (CNS) stimulants, with adrenergic action. It stimulates b2 receptors, but with a smaller affinity on the receptors of the upper respiratory tract (trachea, bronchi). It has the ability to cause vasoconstriction, leading to blood pressure increase, through the production of adrenaline – epinephrine. It has similar effects with clenbuterol HCL.

It is combined as a stack, along with caffeine and aspirin – salicylic acid. Therefore, they act synergistically as catalysts (ECA: 25mg ephedrine, 250mg caffeine, 300mg aspirin), thus increasing the body temperature. However, in extreme cases this may lead to hyperpyrexia (an increase of body core temperature), or lower grade fever and reduction of the feeling of fatigue and physical pain. That resembles the action of amphetamines. The use of ECA stack dramatically increases systemic blood pressure, which is a serious contraindication for hypertensive patients.

Ephedrine alkaloids bring a state of euphoria to the CNS. This may develop into hypomania and restlessness feeling. Insomnia is very likely to occur, due to CNS overstimulation. The pupils of the eyes are contracted and peripheral vasoconstriction in limbs is responsible for poor vascularity. As a result, it’s a not a wise idea to use ephedrine HCL prior to sexual intercourse. Ephedrine causes peripheral vasoconstriction in the cavernous bodies of the penis. Occasionally, it gives an acute pain to perineum, which implies the stimulation of prostate gland.

Using ephedrine in a bodybuilding show will hinder vascularity and diminish the pumping effect of veins. It is advised that it be used before cardiovascular training, on an empty stomach, in order to maximize both intensity and the fat-burning process (beta oxidation of fatty acids).

Ephedrine’s action starts within half an hour, the peak of its action is within an hour of use, and its half-life is approximately estimated around three hours. Ephedrine HCL is a very useful tool when dieting, since it suppresses appetite and gives that satiety feeling.

YOHIMBINE HYDROCHLORIDE

The yohimbe bark herb stimulates the a2 adrenergic receptors. It causes positive inotropic, chronotropic action, through sympatheticomimetic 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 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 Basal Metabolic Rate (BMR), leading to fat catabolism.

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 VO2max). It does not belong to the same class of substances (b2 stimulants), but has the ability to cause bronchodilation, so in doses >3mg/kg acts an alternative solution for the treatment of paroxysmal asthmatic crisis.

Caffeine also stimulates 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.

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 body weight (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, improvingreaction 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.

THYROXINE T4 (Thyroxine)

It is a hormone produced in the thyroid gland, which determines the basal metabolic rate and is directly related to the weight loss-gain. It has a lipolytic ability, but also muscle catabolism as an adverse effect. Its administration should be done with extra caution, since the HPT axis gets easily disturbed and after a certain point the situation is irreversible. Tapering is a good way to get off from thyroid supplementation. Its abuse results in irregular heartbeat-tachycardia, insomnia, sweating, exophthalmos (eyes bulging), restlessness, muscle catabolism and regain of weight, as soon as someone stop its use. It’s a typical rebound effect, since BMR drops.

For proper gland health, it is advised to consume iodized salt, or even iodine in the form of kelp, along with the amino acid L-tyrosine, which is involved in biosynthesis of T3 (triiodothyronine). T3 is more potent than T4 (thyroxine), having a shorter half-life. Therefore, it should be used twice daily, unlike thyroxine. Considering that T4 makes T3, when we use thyroid hormones, if we do not grant T4 – but only T3, progressively its stocks will get decreased. Therefore, it is better to use T4, with which T3 will be formed as well. Of course, its combination is even stronger, but poses risks for the myocardium and muscle catabolism with prolonged overdose and without progressive reduction (for proper balance of the thyroid hormone TSH). The axis of the thyroid hormone is very sensitive and the TSH should be set in the middle of the normal range values. Hypo/hyperthyroidism is an outcome of various different evaluations (TSH, T4, FT4, T3, FT3, ANTI-TPO, ANTI-TG). Athletes have ended up being hypothyroid, due to the extensive abuse of T3.

AMPHETAMINES

Amphetamines belong to the psychotropic sympathomimetic stimulants. They stimulate the adrenergic receptors in myocardium and central nervous system (CNS). Their properties are similar to the ones of the alkaloid ephedrine, including euphoria-hypomania, anorexia-satiety, thermogenesis, increased fatty acid oxidation – lipolysis, alertness-restlessness, sleeplessness-insomnia, tachycardia-increased heart rate, arrhythmias-palpitations, tremors-trembling and tachypnea-increased respiration. They are highly effective for beta-oxidation because they induce brown adipose tissue (located beneath the scapula), the most important organ for non-shivering thermogenesis.

In medicine, they were initially prescribed and administrated for the clinical phenomenon of narcolepsy, where the individual shows drowsiness and psychosomatic fatigue with changes in their sleep schedule. In modern medicine, amphetamines were medically used as a method to suppress hunger and appetite, or even to boost BMR and fat-burning effect.   

Amphetamines are highly addictive, as several people have made extensive uses of it, like soldiers in the World War II, Afghanistan, the Gulf War, or even police officers in the United States during late shifts. Amphetamines were widely spread among university students in Europe and USA.

The reason why amphetamines are highly addictive is due to the increase of neurotransmitter dopamine. Dopamine is associated with the feeling of reward, initiative and self-confidence. Moreover, they increase the concentration of neurotransmitter serotonin linked with the feeling of joy and happiness. They also affect the limbic system dealing with emotional status.

In sports, amphetamines are widely used by track athletes in explosive sports (speed, throws, jumps), but also athletes who demand stamina and endurance (tennis, soccer, volleyball, cycling). They provide alertness and increase of fatigue threshold. Motor drivers (F1 and MotoGP) use them for improved concentration, alertness and focus. The side effects of their use are nausea, vomiting, diarrhea syndromes, palpitations – arrhythmias, hypomania and emotional instability. The peak of amphetamines action occurs within an hour. 

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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