Thyrozene

Hi-Tech Thyrozene

            Thyroid hormones are most likely one of the most misunderstood and underrated drug groups in the bodybuilder’s/ dieter’s arsenal. Based upon years of experiences, they certainly increase the rate and efficiency of fat loss during diet periods. And they act synergistically to increase the rate of lean tissue growth during mass gaining periods…if used correctly.

The noted positive physiological effects of reasonable dosages of thyroid hormones included:

• Increased protein synthesis rate
• Increased rate of fat oxidation
• Increased metabolization of proteins, carbohydrates, fats, and micronutrients
• Increased metabolic rate and calories expenditure
• Enhanced oxygen consumption by most body tissues
• Improved recovery time

The noted negative physiological effects of excessive dosages of thyroid hormones included:

• Loss of lean mass tissue
• Increased heart rate and palpitations
• Insomnia
• Diarrhea
• Vomiting

Thyroid hormones govern the body’s metabolic rate. This means that the metabolism of nutrients and subsequent cellular utilization or storage rate is dependent upon blood circulatory thyroid hormone levels. Higher levels result in elevated over all metabolic rate providing that other metabolic factors are accommodated also.

THYROID HORMONES AND CALORIE EXPENDITURE

            Thyroid hormones are effective with creating “oxidative phosphorylation.” This is a process by which cells/ mitochondria convert ADP (Adenosine Diphosphate) into ATP (Adenosine Triphosphate).  Basically this means adding another phosphate molecule to ADP so that it can be converted back into the body’s energy/ ATP.

            Thyroid hormones are powerful uncouplers of oxidative phosphorylation. Thyroid hormones increase cell/ mitochondrial substrate oxidation by effecting both cytochrome-C reducers and cytochrome-C oxidizers. This increases metabolic rate and substrate (nutrient/ food) use as fuel for either ATP or heat production. Heat production by a cell is referred to as thermalgenesis, in this case the conversion of fat into heat. Though other substrates such as glucose/ glycogen can be used for heat production also under adverse conditions.

THYROID HORMONES AND FAT OXIDATION

            Fat oxidation or thermalgenesis involves the conversion of fat calories into heat. In the case of thermalgenesis caused by thyroid hormones it is due to “special uncoupling proteins” found in fat, muscle, and organs called UCP-3. When UCP-3 is increased, the calorie expenditure through thermalgenesis increases. But decreases will result in an increase in fat stores. As example, supraphysiological T-3 levels increase UCP-3 600%  and below normal levels results in a 300% decrease. This is why calorie restricted diets significantly decrease in results after 2-4 weeks. The body down-regulates thyroid hormone production to save calories and reduce calorie expenditure as health. The result is less UCP-3 and slower metabolism.

            Thermalgenesis and oxidative phosphorylation uncoupling is the reason athletes used synthetic thyroid hormones during calorie restricted or diet phases. The individuals were able to ingest more calories than normal while still burning fat. It should be noted that a minimum of 2 grams of protein per pound of body weight was ingested dialing during exogenous thyroid hormone use to prevent excessive muscle catabolism or loss. Athletes commonly stacked adrenalgenic beta-agonist drugs like Clenbuterol, Ephedrine/ Norephedrine, or Phentermine to increase UCP-3 levels and act synergistically with thyroid hormones to favor fat oxidation and reduce muscle loss.

THYROID HORMONES ARE ANABOLIC AGENTS

            Many athletes were not aware of the fact that thyroid hormones are a true form of absolute anabolic. The usual method of employment for thyroid hormones was during pre-contest periods. Obviously, this is because increased thyroid hormone levels means elevated metabolic rate and resulting increased calorie expenditure or use. This explanation itself suggests the noted anabolic potential.

            Thyroid hormones govern or regulate our metabolic-rate or metabolism. Metabolic rate is the speed or rate at which all chemical and physical processes occur. This is true of every living cell in our bodies. This means that the rate of nutrient metabolism, absorption, and utilization is vastly dependent upon thyroid hormones. In fact, the levels of thyroid hormones in our body determines if the food we eat is stored as adipose (fat) tissue, utilized for regeneration and building, or burned as heat/ energy. Low thyroid hormone levels slow the healing/ growth process while increasing fat stores. Overly high thyroid hormone level results in tissue catabolism or wasting. But thyroid hormone levels matched to nutrient supply and demand were commonly considered to be seriously anabolic. Remember, training and chemical muscle enhancement protocols created a massive nutrient demand. If thyroid hormone levels are too low, no amount of calories will be an adequate supply simply because they are not metabolized at the necessary rate.

3,5 Diiodo-L-tyrosine dihydrate

(Backdrop & Comments for Use)

The thyroid gland produces two active iodinated compounds, thyroxine (T4) and triiodothyronine (T3). Control of synthesis is regulated by a negative-feedback mechanism which commences when blood levels of these two compounds (hormones) are too low. When this occurs, the thyroid releasing hormone (TRH) in the hypothalamus is activated and released. TRH acts on the anterior pituitary stimulating the release of thyroid stimulating hormone (TSH). TSH acts on the thyroid gland stimulating the synthesis of T3 and T4. The precursor synthesis activity of T3 and T4 in the thyroid gland begins when tyrosine is iodoinated to form monoiodotyrosine and diiodotyrosine. These compounds are then coupled to form T3 and T4 which are stored in the thyroid gland in thyroglobulin. T3 and T4 are cleaved and released from the thyroglobulin into the circulation as needed.

The oral administration of 3,5-Diiodo-L-tyrosine results in the digestion of the compound in the intestine. Quantities of the iodide and tyrosine are absorbed in the circulation. Portions of iodide and tyrosine return to the thyroid gland where it is reutilized in the synthesis of more thyroid hormone. The amino acid, tyrosine, is also utilized to synthesize epinephrine and norepinephrine.

Optimal levels of iodine must be maintained to promote the best thyroid function. Too little or too much may impede or impair thyroid activity. The dosage of 3,5-diiodo-L-tyrosine dihydrate in Thyroid-Rx™ takes into consideration the amount of iodine that will be bioavailable to the thyroid. The dosage of tyrosine in Thyroid-Rx is quantified for maximum thyroid hormone synthesis if needed. And since tyrosine is required for epinephrine and norepinephrine synthesis, the bioavailability of it in Thyroid-Rx may modulate the synthesis of these sympathomimetic amines with basal metabolic activity enhancement and increased calorigenic effects such as thermogenesis and lipolysis.

COMPONENTS OF A FORMULATION FOR THYROID HORMONE STIMULATION & WEIGHT LOSS

3,5-Diidotyrosine         

            The components of this compound are useful as anti-obesity and lean-promotion agents. Tyrosine is a non-essential amino acid derived from the essential acid phenylalanine. Both are ketogenic and glucogenic. An essential amino acid cannot be synthesized in sufficient amount by the body and must be provided by diet. Non-essential amino acids are characterized in contrast. Ketogenic amino acids yield acetyl CoA, acetoacetyl CoA and aceto acetate. Glucogenic amino acids yield pyruvate or one of the intermediates of the citric acid cycle. These intermediates are substrates for gluconeogenesis, the net formulation of glycogen in liver and muscles.

            Dopamine, norepinephrine, and epinephrine, biologically active amines called catecholamines are synthesized from tyrosine. Dopamine and norepinephrine function as neurotransmitters in the brain and the autonomic nervous system. Norepinephrine and epinephrine are synthesized in the adrenal medulla. These two neurotransmitters regulate carbohydrate and lipid metabolism. Both are released from the adrenal gland and autonomic nervous system in response to exercise, fright, cold, and low levels of glucose. The effects of these catecholamines are coordinated response that prepares the individual to indulge in desired or needed ergogenics.

            The iodine composition given in optimal amounts or the recommended daily allowance promotes thyroid activity and health. This effect is potentiating to the other components of the formula. The synergism in this formulating makes it one of the best preparations for fighting obesity and promoting fitness. Tyrosine depletion modulates catecholamine neurotransmission which increases vulnerability to depression. It is proposed that an expansion of dopaminergic systems in human cognition is the basis of the origins of human intelligence, a derivation of synthesis from tyrosine. Tyrosine has been shown to be important for the human glucocorticoid receptor transactivation.

Forskolin

            Forskolin is a diterpene extracted from Coleus forskohlii, a prennial branched aromatic herb, distributed in the sub-tropical Himalayan region of Southeast Asia. This diterpene produces its pharmaceutical effects in the body by modulating two of the most widely recognized intracellular messenger systems, the adenyl cyclase and the calcium phosphatidylinositol systems.

            Adenyl cyclase is a cell membrane bound enzyme, which is activated by chemical signals initiated in cell membrane receptors by hormones and neurotransmitters. In vitro tissue studies of cardiac muscles have demonstrated that forskolin acts on the same receptors. Adenyl cyclase converts adenosine triphosphate (ATP) to 3,5-adenosine monophosphate (cyclic AMP or cAMP). cAMP-mediates the effect of certain hormones and neurotransmitters on target cells. For example, cAMP mediates the action of epinephrine on the degradation of glycogen stores in liver and muscle cells, the action of glucagons and glycogen stores in the liver, and the action of thyroid stimulating hormones (TSH) on the follicular cells of the thyroid gland to produce thyroid hormone (T3 and T4). The actions of thyroid hormones on target tissue are not cAMP-mediated events but are mediated by the hormone binding to DNA and modulating gene transcription. The lipolytic effect of epinephrine on adipocutes on fat cells is a cAMP-mediated event. Hormone-sensitive lipase is activated to hydrolyze fatty acids and glycerol from neutral triaglycerols.

            The calcium/ phosphatidylinositol system responds to hormones and neurotransmitters by activating a cell membrane bound phosphodiesterase called phospholipase C.  This enzyme cleaves membrane bound phosphatidylinositol 1,4,5-triphosphate to release two fragments, inositol 1,4,5-triphosphate and diaglycerol. These fragments have synergistic activity. Inositol 1,4,5-triphosphate binds to endoplasmic reticulum which releases CA²⁺ from intracellular stores. Complexes consisting of CA²⁺ and a binding protein, calmodulin, are formed. These complexes mediate the role of calcium in the contractile activity of skeletal and cardiac muscles. Several enzyme systems are regulated by this complex including adenyl cyclase, phosphodiesterase, and an ATP-dependent CA²⁺ and potassium pump. Xanthine derivates such as caffeine and thophylline inactivate phosphodiesterase. cAMP-mediation is enhanced by this inactivation because phosphodiesterase hydrolyzes and inactivates cAMP.

            Some of the pharmaceutical effects of forskolin include relaxation of smooth muscle in the wall of the bronchial tubes of the lung (bronchodilation), lowering blood pressure, and augmenting the contraction of cardiac muscle by positive inotropic activity. These effects coupled with increased cAMP-mediated degradation of glycegan stores to glucose suggest that forskolin, as a component of any weight loss and workout formulation, should be effective. Forskolin should potentiate the effects of hormones normally released in the body as a response to exercise such as epinephrine and glucagons. Enhancing cardiac muscle contraction increases vascular volume and promotes oxygenation of peripheral tissues. Increasing the availability of glucose by the degradation of glycogen stores in liver muscles enhances ergogenic capacity. Bronchodilation increases O₂ intake and availability.

            Recent recipients of a U.S. patent reported in their application that forskolin has efficacy for treating mood disorders. Mood disorders are known to promote overeating and obesity. If forskolin can impact these disorders, its efficacy as an anticorpulent agent is further enhanced and substantiated.

            As with all substances or preparations which stimulate metabolic activity, optional benefits can usually be best obtained by a cyclic or periodic administration of forskolin. Data suggest that continuous or sustained stimulation of the adenyl cyclase system produces an attenuated and desensitive response to the enzyme. Any person taking a prescribed medication should consult their physician before using this preparation.

GUGGULSTERONES

Reported Characteristics

            Guggulsterone are an extract of the herb Commiphora Mukul, clinically proven to restore lagging metabolic rate caused by dietary calorie deficiency such as during diet phases. Ayurvedic medicine has utilized the unprocessed herb for centuries to treat energy deficiencies related ailments.

            Guggulsterones Z and E seem to have the greatest effect upon stimulation of thyroid hormone, though other substrates of the herb commiphora mukul may effect different metabolic factors as well. Thus far, research suggests this is a result of Guggulsterones Z & E stimulation of TSH (Thyroid-Stimulating-Hormone) production. This results in an increase in Thyroid gland T-4 production and subsequent liver conversion to the more active T-3 hormone.

What application does guggul

Although the majority of studies on guggulipid have been on its cholesterol lowering ability, it has also been identified as a weight loss agent. It activates lipolytic enzymes and increases T3 levels, presumably due to increased conversion of T4 to T3 in the liver, although it may also stimulate the thyroid directly

Quite a few studies have been done on both humans and animals accessing guggul’s ability to stimulate fat loss. Animal studies have shown a positive effect and human studies have either shown a benefit or have been equivocal. Unfortunately, many of these studies were inadequately controlled. A study that controlled for BMI, concurrent drug use, diet, and exercise found that people who took guggul lost 1.92 kg after 15 days compared with .32 kg in the control group.

How does guggul work?

As stated, orally administered guggulipid increases T3 (tryiidothyronine) levels in animal models. T3 is the conversion product of T4, which is produced by the thyroid gland. Thyroid hormone levels are intricately involved in metabolic homeostasis. Increased thyroid levels cause more fat to be burned and decreased levels increase the likelihood of fat being stored. When one normally goes on a diet, the body responds by decreasing T3 levels and thus decreasing metabolic rate. But if T3 levels are increased, diets are much more effective at causing fat loss. It has not been established ho guggulipid increases T3 levels, but the prevailing theory is that it is by decreasing lipid peroxidation.

Guggulipid standardized for E- and Z-guggulsterones – Most standard guggul extracts contain .5-2% E- and Z-guggulsterones. Since these are the primary hypolipidemic agents, it is probable that they are also primarily responsible for some of guggul’s other effects. Hence, increasing the total amount of E- and Z-guggulsterones may make the formulation much more potent. Products containing higher quantities of E- and Z-guggulsterones may be ideal, but two studies have shown that most products that claim to have higher quantities of E- and Z-guggulsterones than conventional extracts actually do not. So, if you are buying a guggul extract that claims to have higher quantities of the E and Z isomers, chances are it isn’t much more potent that other effects. Hence, increasing the total amount of E- and Z-guggulsterones may make the formulation much more potent. Products containing higher quantities of E- and Z-guggulsterones may be ideal, but two studies have shown that most products that claim to have higher quantities of E- and Z-guggulsterones than conventional extracts actually do not. So, if you are buying a guggul extract that claims to have higher quantities of the E and Z isomers, chances are it isn’t much more potent than other extracts despite label claims. Thyrozene™ utilizes a 98% standardized E- and Z-guggulsterones unheard of until now.

N-Acetyl-Thyronine Sodium

            N-Acetyl-Thyronine Sodium is a derivative of an amino acid for use to restore ones natural metabolic rate. N-Acetyl-Thyronine is a metabolite of the thyroid hormone (T3) and has thyroid hormone activity including various metabolic effects. It also inhibits the secretion of Thyroid-Stimulating Hormone (TSH) by the pituitary gland. The pharmacokinetics of N-Acetyl-Thyronine Sodium appear to be similar to those of thyroxine and triidothyronine. N-Acetyl-Thyronine Sodium is absorbed in the small intestine following ingestion. Most of the substance appears to be bound to serum proteins, including thyroxine-binding protein and albumin. It appears to be less firmly bound to serum proteins than are T4 or T3. N-Acetyl-Thyronine Sodium possesses a 6 hour half-life, this is usually divided into 3 or 4 equal dosages. N-Acetyl-Thyronine Sodium administration will not induce a true replacement metabolic rate like other thyroid hormones. This means anyone using this amazing compound is able to increase their metabolic rate only equivalent to the upper range considered normal and acceptable through administration. This is, in truth, a very significant increase and considered highly effective by all but a few users. This would make N-Acetyl-Thyronine Sodium one of the safest thyroid products available. Currently this amazing compound is only found in Thyrozene™ by Hi-Tech Pharmaceuticals, Inc.

Hi-Tech Thyrozene™

            The term glandulars are used in the nutritional supplement marketplace refers to dried and ground-up raw animal glandular and nonglandular tissues or extracts of these tissues. Glandulars are believed by some to improve the function of the gland or organ from which the extract was produced. Most of these substances are derived from bovine sources; some are derived from ovine sources and some from porcine sources. Dessicated thyroid is still used by many physicians in the management of hypothyroidism. Dessicated thyroid is the cleaned, dried and powdered thyroid gland, purified of fat and connective tissue; the most active is derived from porcine. Many doctors claim the natural form of thyroid hormone (dessicated procine or bovine gland such as Hi-Tech Thyrozene™) is more effective. For example, Dr. Alan Gaby states that 38% of the iodine present in the thyroid gland is in the form of diidotyrosine, also found in the blood. You can read about diidotyrosine’s effect earlier in this article. One problem with these natural glandulars is many of their active constituents are destroyed during processing. Hi-tech Thyrozene has overcome that through a proprietary extraction process recently developed. Below you will see a graph for guidance on selecting a proper dosage. The basic “rule of thumb” in converting thyroid doses is that 100 mcg of T4 is routinely equivalent to 25 mcg of T3 or 1 grain (60 mg) of dessicated thyroid (Hi-Tech Thyroid).

            The consistency from batch-to-batch of Hi-Tech Thyrozene™ is remarkable. Hi-tech Thyrozene is made from dessicated (dried) pork thyroid glands. The amount of thyroid hormone present in the thyroid gland may vary from animal to animal. To ensure that Hi-Tech Thyrozene is consistently potent from tablet to tablet and lot to lot, analytical tests are performed on the thyroid powder (raw material) and on the actual tablets (finished product) to measure actual T4 and T3 activity. Different lots of thyroid powder are mixed together and analyzed to achieve the desired ratio of T4 and T3 in each lot of tablets. The ration of T4 to T3 equals 4.25:1 (4.25 parts of T4 to one part of T3). To meet quality standards it must also pass bacteriological testing and must meet other product quality tests. As a natural product obtained from porcine thyroid glands, Hi-Tech Thyrozene™ tablets may have a strong, characteristic odor. This does not indicate that it is spoiled or defective in any way. Each tablet provides 38 mcg of levothyroxine (T4) and 9 mg liothronine (T3). T3 is approximately four times as potent on a microgram for microgram basis. This product has potentially more thyroid activity than any other product ever offered. It also contains trace levels of T-2 (L-diiodothyronine) and tricana (Triiodothyroacetic Acid) due to these substances naturally occurring in the porcine thyroid powder. Some people would assume that the low percentage of T-4 and T-3 provided by Hi-Tech Thyrozene™ would only be moderately effective. In fact, the combination is often considered more effective than either drug alone and is at the correct human ratio. The trace levels of T-2 and Tricana create a complete synergistic and effective thyroid product. Most people will notice results very quickly with this compound!

Summation

                                                                      Thyrozene™ by Hi-Tech Pharmaceuticals

                                                                        is a unique matrix of cutting-edge

                                                                        nutraceuticals designed to stimulate thyroid

                                                                        function for the production of thyroid

                                                                        hormones including triidothyronine and

                                                                        thyroxine. This unique matrix includes the

                                                                        amino acid derivative, N-Acetyl-Thyronine

                                                                        sodium, 98% pure guggulsterones,

                                                                        forskohlin, 3,5 diido-L-tyrosine, and the

                                                                        revolutionary Hi-Tech Thyroid™ powder.

                                                                        The thyroid gland assists the human body

                                                                        with the regulation of metabolism. By

                                                                        increasing metabolism (and thyroid

                                                                        function), every tissue in the body is stimulated to produce and increase oxygen utilization at the cellular level. By increasing the oxygen the oxygen level at the cellular level and overall metabolic function, the body is stimulated to increase fat burning activity. Thyrozene™ is fantastic for fat loss and causes brown-fat thermogenesis. Through the process of oxidative phosphorylation, it penetrates into the inner membrane of brown-fat tissue and uncouples it. Brown fat is the stubborn fat, that is always the hardest to lose. It occurs mostly in the problem areas; abs, obliques, glutes, and thighs. The reason why brown fat is so difficult to access is because it is there to protect you in case of a famine situation the components in this formulation are powerful punches against lipogenesis and for lipodegradation. Appetite suppression, the basal metabolic rate, thermogenesis and other endogenous energizing activities and enhanced. This formulation promotes weight loss and leanness. It is an ideal adjunct for body-building rigors, aerobics, and other ergogenics. Perhaps, more importantly, it is a formula that may be beneficial to sedentary and disabled persons in their efforts to lose weight. Thyrozene™ is the future of metabolic stimulation and is synergistic with ephedrine, caffeine, and Synephrine for those who want rapid results.

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