WO2011041451A2 - Smoking cessation with body weight maintenance and nutritional supplement - Google Patents

Smoking cessation with body weight maintenance and nutritional supplement Download PDF

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Publication number
WO2011041451A2
WO2011041451A2 PCT/US2010/050774 US2010050774W WO2011041451A2 WO 2011041451 A2 WO2011041451 A2 WO 2011041451A2 US 2010050774 W US2010050774 W US 2010050774W WO 2011041451 A2 WO2011041451 A2 WO 2011041451A2
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component
vitamin
individual
tobacco
compound
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English (en)
French (fr)
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WO2011041451A3 (en
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Harlan Clayton Bieley
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Priority claimed from US12/571,391 external-priority patent/US20100021570A1/en
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Priority to CN201080043603XA priority Critical patent/CN102573821A/zh
Priority to JP2012532283A priority patent/JP2013506678A/ja
Priority to CA2776160A priority patent/CA2776160A1/en
Publication of WO2011041451A2 publication Critical patent/WO2011041451A2/en
Publication of WO2011041451A3 publication Critical patent/WO2011041451A3/en
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    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61K31/045Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/07Retinol compounds, e.g. vitamin A
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    • A61K31/137Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
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    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
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    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/525Isoalloxazines, e.g. riboflavins, vitamin B2
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    • A61K31/59Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
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    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
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    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
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    • A61K31/714Cobalamins, e.g. cyanocobalamin, i.e. vitamin B12
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Definitions

  • tobacco smoke contains heavy metals such as lead and cadmium. Cadmium causes the depletion of zinc and Vitamin D and can also interfere with the metabolism of Vitamin D. In addition, the body stores cadmium in fat and may retain it for a substantial amount of time. Tobacco smoke also specifically contains carbon monoxide, nitrogen oxide, hydrogen cyanide and ammonia, all of which are toxic and/or carcinogenic to an individual.
  • Tobacco smoking and in particular cigarette smoking, is responsible for the majority of lung cancers and is also associated with cancers of the mouth, pharynx, larynx, esophagus, stomach, pancreas, uterine cervix, kidney, ureter, bladder and colon, as well as leukemia.
  • cardiovascular diseases including stroke
  • sudden death cardiac arrest
  • peripheral vascular disease and aortic aneurysm.
  • ciliotoxic materials that irritate the lining of the respiratory system resulting in increased bronchial mucus secretion and chronic decreases in pulmonary and mucociliary function.
  • Smokers and non-smokers may also be exposed to environmental tobacco smoke, which is produced by inhalation of tobacco smoke by a smoker and then exhalation thereof into the environment (mainstream tobacco smoke) or emitted by a burning tobacco-containing product such as a cigarette (sidestream tobacco smoke).
  • mainstream tobacco smoke is produced by inhalation of tobacco smoke by a smoker and then exhalation thereof into the environment (mainstream tobacco smoke) or emitted by a burning tobacco-containing product such as a cigarette (sidestream tobacco smoke).
  • mainstream tobacco smoke and sidestream tobacco smoke are qualitatively similar since they are both derived from burning tobacco, there are some significant quantitative differences between the two types of smoke.
  • the temperature at which mainstream tobacco smoke is formed is much higher than the temperature at which sidestream tobacco smoke is formed.
  • tobacco and its additives are not the only part of the product that carries dangerous chemicals.
  • the paper used by cigarette manufacturers may be engineered to burn slowly. This can be accomplished, among other ways, by the addition of antimony to the paper.
  • smoking tobacco also impacts the body's ability to function normally by interfering with important body resources.
  • body substances such as, for example, vitamins, minerals, enzymes, amino acids, cofactors, precursors, neurotransmitters, cellular constituents, and the like are depleted, damaged, or interfered with in an individual directly as a result of smoking tobacco products and being exposed to environmental tobacco smoke.
  • depletion of, damage of, or interference with vital body substances can result in a variety of health problems and/or increase the risk for the health problems described above for smokers and those exposed to environmental tobacco smoke.
  • the ability to sense the bitter taste of nicotine as well as possibly the added taste enhancers in tobacco smoke are important components for the desire to smoke tobacco.
  • Third, constantly drawing on willpower to reduce or cease what may be a long-term habit of smoking tobacco and experiencing nicotine cravings and withdrawal symptoms can create secondary problems related to smoking, such as an increase in stress and anxiety resulting in an increase in appetite.
  • Such an increase in appetite can result in undesirable increases in body weight, which, in turn, can result in even more health problems as well as an unattractive change in the individual's appearance.
  • the undesirable increases in body weight in itself can also have a detrimental effect on an individual's willpower to reduce or cease smoking tobacco.
  • Each of these effects, any of the effects in combination, and especially all of the effects in combination can be detrimental to an individual attempting to reduce or cease smoking tobacco.
  • Smoking cessation products have typically attempted to reduce nicotine cravings and withdrawal symptoms in several ways.
  • One method has been the use of nicotine-containing substances such as transdermal patches or chewing gum which permit individuals to satisfy the body's cravings for nicotine without damaging their lungs by inhaling tobacco smoke.
  • nicotine-containing substances such as transdermal patches or chewing gum which permit individuals to satisfy the body's cravings for nicotine without damaging their lungs by inhaling tobacco smoke.
  • smoking cessation products that do not use nicotine-containing substances include chemical substances that bind to specific cell receptor sites in the brain, thus preventing nicotine from binding to those cell receptor sites which assists in controlling nicotine cravings and withdrawal symptoms.
  • Such products typically contain bivalent negative sulfur compounds such as alkyl sulfides, colloidal sulfur, hydropersulfides, organic thio compounds or their salts.
  • FIG. 1 is a schematic illustration of a remedial compound and its synergistic effects
  • Fig. 2 is a top view of a tongue generally illustrating taste receptor areas
  • FIG. 3 is a schematic illustration of the synergistic effects of Fig. 1 and the manners in which such effects can be achieved; and [001 1]
  • Fig. 4 is a schematic illustration of a method of replenishing body substances, repairing body substances, or ameliorating the function of body substances depleted, damaged or impaired in an individual as a direct result of smoking tobacco or being exposed to environmental tobacco smoke; and
  • Fig. 5 is a schematic illustrating of a method of assisting an individual attempting to reduce or cease tobacco smoking.
  • FIG. 1 The drawings and description, in general, provide a system comprising a remedial compound 10, Fig. 1 , that synergistically reduces nicotine cravings or withdrawal symptoms 12 to assist an individual in ceasing smoking tobacco or at least reducing the amount of tobacco smoked on a daily basis, decreases stress and anxiety 14 in an individual attempting to cease or reduce smoking tobacco, alters the perceived taste of tobacco smoke 16 to deter continued smoking of tobacco, and suppresses the individual's appetite or has lipotropic effects to allow maintenance (including possibly loss) of body weight 18.
  • suppressing appetite avoids undesirable side effects from reducing or quitting smoking such as increased appetite and consequential weight gain
  • elements that have lipotropic effects enhance the body's ability of metabolize fat, thereby maintaining body weight (which includes suppressing the gain of body weight as well as losing body weight) while reducing or quitting smoking.
  • a nutritional supplement that replenishes depleted body substances 20, repairs damaged body substances 20, or ameliorates the function of body substances 20 that are impaired as a direct result of smoking tobacco or being exposed to environmental tobacco smoke.
  • Such body substances may include vitamins, minerals, enzymes, amino acids, cofactors, precursors, hormones, neurotransmitters, cellular constituents, and the like that are depleted, damaged, or impaired as a consequence of smoking tobacco or of being exposed to tobacco smoke in the environment (i.e., "second-hand" smoke). As indicated by dashed lines, at least some of the elements in the nutritional
  • the phrase "remedial” is used herein to define a remedy that is utilized, for example, to relieve a bodily disorder or restore an imbalance of one or more body substances to healthier or optimal conditions.
  • the phrase "smoking tobacco” includes any means of inhaling and exhaling nicotine-containing tobacco smoke into and out of an individual's oral cavities and lungs such as via cigarettes, pipes, or the like. Also discussed herein is the effect of being exposed to tobacco smoke that is present in the environment, or "second-hand" smoke, as would be experienced by, for example, a non-smoking household member of a smoker.
  • synergy and its derivatives, as used in the present application, is defined as the interaction of two or more components to produce results that, in combination, are different, additive, and may often be greater than the expected or anticipated effect of each element utilized separately and individually.
  • synergistic behavior of such combined components or forces as a system has a novel effect unpredictable and unanticipated by the behavior of any individual component taken separately from the system.
  • the first component 30 of the compound 10 comprises at least one element that blocks nicotine receptor sites in the human body in an amount sufficient to assist in controlling cravings or withdrawal symptoms within an individual attempting to quit smoking tobacco resulting from deprivation of nicotine from that individual's body.
  • An example of such an element is bivalent negative sulfur 32 which may be selected from a group that includes, but is not limited to, Hydropersulfides, AlkyI sulfides, Colloidal sulfur, organic Thio compounds or their pharmaceutically acceptable salts.
  • Presently preferred Thio compounds include Thioglycerols, Thioglycols, and their pharmaceutically acceptable salts.
  • the second component 40 of the compound 10 comprises at least one element that increases serotonin levels in the human body such as, for example, amino acids derived from tryptophan 42 and, more specifically, 5-hydroxytryptophan (5-HTP) or related tryptophan derivatives, in an amount sufficient to assist in suppressing an individual's appetite, assist in reducing cravings for nicotine or withdrawal symptoms, and assist in reducing stress and anxiety in an individual attempting to cease or reduce smoking tobacco.
  • Smoking tobacco has also been shown to decrease the levels of serotonin in an individual, and this effect could also be present in an individual exposed to environmental smoke.
  • the second component of the compound also replenishes the depleted serotonin in such an individual's body.
  • 5-HTP can be derived from the amino acid L-tryptophan as noted above, it can also be derived from Griffonia simplicifolia seed extract or other sources. Tryptophan, including L-tryptophan and its derivatives, plays a vital role in our health in that it is an essential amino acid utilized by the human body for building proteins and enzymes, as well as serving as a precursor, along with cofactor tetrahydrobiopterin, to serotonin (5-hydroxytryptamine or 5-HT) and the hydrogen carriers NADH and NADPH.
  • Serotonin is a neurotransmitter that plays an important role in regulation of mood, appetite, body temperature, and the secretion of various hormones, and serotonin levels may be depleted in cigarette smokers and those exposed to environmental smoke. Whereas serotonin does not readily cross the blood brain barrier, serotonin precursors such as 5-HTP and L-tryptophan can cross the blood brain barrier. As a result, ingesting 5-HTP, L-tryptophan or related tryptophan derivatives increases levels of serotonin in the body.
  • 5-HTP is generally more efficient in the human body than L-tryptophan because 5-HTP bypasses the rate-limiting step of serotonin synthesis which utilizes the enzyme tryptophan hydroxylase.
  • Tryptophan including 5-HTP, L-tryptophan, and the like, has a variety of positive side effects when ingested by humans.
  • tryptophan can be used as a mood- and sleep-enhancer and is commonly used to treat depression and insomnia, thus playing a synergistic role in reducing stress and anxiety in individuals attempting to quit smoking tobacco.
  • Tryptophan can also increase pain tolerance and reduce appetite, in particular cravings for certain carbohydrates.
  • 5-HTP has a relatively small molecule size, thus allowing 5-HTP access to the brain through the bloodstream.
  • 5-HTP can be converted into serotonin, which acts on the different serotonin receptor sites in order to suppress an individual's appetite as well as helps reduce cravings for nicotine or withdrawal symptoms in an individual attempting to reduce or cease smoking tobacco.
  • 5-HTP is a naturally occurring element that is produced in the body from tryptophan and can be found in high-protein foods such as beef, chicken, fish, and dairy products.
  • 5-HTP for appetite suppression is relatively safer than utilizing non-naturally-occurring ingredients found in some conventional appetite suppressants.
  • tryptophan including its derivatives such as, for example, 5- HTP
  • tryptophan is a precursor used by the body to produce serotonin
  • its use in combination with the aforementioned first component of the compound that blocks nicotine receptor sites allows an individual to improve the chances of successfully and less painfully overcoming a tobacco smoking habit.
  • serotonin also inhibits nicotine cravings and withdrawal symptoms
  • the second component that increases serotonin levels in an individual acts synergistically with the first
  • One or more serotonin receptor agonists 44 may also or alternatively be utilized as the second component 40 of the compound 10 in order to increase serotonin levels in the human body.
  • serotonin receptor agonists activate serotonin receptors, mimicking the effect of the neurotransmitter serotonin in the human body.
  • serotonin receptor agonists include, but are not limited to, selective 5-HT receptor agonists such as Azapirones (e.g., Buspirone and the like) which is an agonist to the 5-HT1A receptor sites, Triptans (e.g., Sumatriptan and the like) which are agonists to the 5-HT1 B and 5-HT1 D receptor sites, Lasmiditan which is an agonist to the 5-HT1 F receptor sites, Trazodone which is an agonist to the 5- HT2 receptor sites, Lorcaserin which is an agonist to the 5-HT2C receptor sites, and Cisapride which is agonist to the 5-HT4 receptor sites.
  • selective 5-HT receptor agonists such as Azapirones (e.g., Buspirone and the like) which is an agonist to the 5-HT1A receptor sites, Triptans (e.g., Sumatriptan and the like) which are agonists to the 5-HT1 B and 5-HT1 D receptor sites, Lasmiditan which is an agonist
  • serotonin receptor agonists include, but are not limited to, non-selective 5-HT receptor agonists such as Ergotamine which is an agonist to the 5-HT1A, 5-HT1 D, 5-HT1 B, D2, and norepinephrine receptor sites; and psychedelic drugs (LSD, mescaline, and the like) which is an agonist at least to the 5-HT2A receptor sites.
  • non-selective 5-HT receptor agonists such as Ergotamine which is an agonist to the 5-HT1A, 5-HT1 D, 5-HT1 B, D2, and norepinephrine receptor sites
  • psychedelic drugs LSD, mescaline, and the like
  • a third component 50 of the compound 10 comprises a supplement that replenishes depleted body substances 20, repairs damaged body substances 20, or restores function of body substances 20 that are depleted, damaged, or their function impaired as a direct result of smoking or as a result of being exposed to environmental tobacco smoke.
  • the third component 50 of the compound 10 may also contribute to one or more of the synergies described above related to reducing nicotine cravings or withdrawal symptoms 12, decreasing stress and anxiety 14, altering the perceived taste of tobacco smoke 16, and maintaining body weight 18 in an individual attempting to reduce or cease smoking tobacco.
  • the supplement consists of one or more body substances 52 which may be vitamins, minerals, enzymes, amino acids, cofactors, precursors, hormones,
  • the supplement may consist of the following in any of their forms (some specific examples of these forms being given below): Alpha lipoic acid; Chromium in any of its forms including Chromium picolinate; Biotin; Tyrosine in any of its forms including N-acetyl tyrosine;
  • Tetrahydrobiopterin which is a cofactor; L-phenylalanine and/or DL-phenylalanine; Gymnema sylvestre (Gumar); Arginine; Green tea with Epigallocatechin gallate (EGCG); Butyrate in any of its forms including Sodium butyrate, sodium potassium butyrate, and calcium magnesium butyrate; Mucuna puriens (Cowage seed);
  • Magnesium in any of its forms including Magnesium glycinate, Magnesium malate, Magnesium taurate, and Magnesium citrate; N-acetylcysteine and/or Glutathione (which can be made by N-acetylcysteine); L-theanine; Magnolia officianalis; Taurine; Melatonin (a hormone and an antioxidant); Vitamin B-6 in any of its forms, activated and/or unactivated, including Pyridoxal-5-phosphate and Pyridoxine hydrochloride; Inositol; Vinpocetin; Glycine; Niacinamide; Valerian Root; Kava kava;
  • Vitamin C (buffered or in any other form); Vitamin B-12 in any of its forms including Methylcobalamin, Cyanocobalamin, and Hydroxocobalamin; Choline in any of its forms including Phosphatidylcholine and Choline citrate; Methionine in any of its forms including L-methionine; S-adenosylmethionine (SAM-e); Calcium; Vitamin E in any of its forms including Tocopherols and Tocotrienols such as Alpha tocopherol and Gamma tocoperhol; Folate in any of its forms including Folic acid, Folinic acid, L-methylfolate, and 5-methyl tetrahydrofolate; Manganese; Vitamin B2 in any of its forms including Riboflavin-5-phosphate; Vitamin A; Selenium in any of its forms including Selenomethionine; Zinc
  • Fig. 3 illustrates the synergistic effects 12, 14, 16, 18, 20 noted above with reference to Fig. 1 and the manners in which such effects can be achieved.
  • nicotine cravings or withdrawal symptoms can be reduced 12 by any of the following: an element 100 that blocks nicotine receptor sites, an element 102 that increases serotonin levels or participates in the action of serotonin, or a sensory substitute 104.
  • the first component 30, Fig. 1 of the compound 10 which is a bivalent negative sulfur 32 blocks nicotine receptor sites 100, Fig. 3.
  • An element 102 that increases serotonin levels is the second
  • component 40, Fig. 1 of the compound 10 such as 5-HTP, which is a serotonin precursor.
  • Other elements 102 that increase serotonin levels or participate in the action of serotonin include Magnesium, which prolongs the effects of 5-HTP; Inositol, which acts on receptors linked to serotonin signaling; Vinpocetin, which directly raises serotonin levels; and S-adenosylmethionine (SAMe) which augments serotonin reuptake inhibitors.
  • An element 104 that acts as a sensory substitute is Vitamin C. As a sensory substitute, Vitamin C (specifically as ascorbic acid) has been shown to enhance smoking reduction by reducing nicotine cravings or withdrawal symptoms.
  • stress and anxiety may be decreased 14 by utilizing an element 110 that increases GABA or participate the action of GABA.
  • GABA, GABA agonists, and other elements that increase GABA generally help reduce stress and anxiety in an individual and thus may also be utilized synergistically with the first and second components as well as other elements of the third component of the compound to help reduce stress and anxiety in an individual attempting to reduce or cease smoking tobacco.
  • L-theanine and N- acetylcysteine do not directly increase GABA, but instead are GABA modulators that dampens glutamate.
  • L-theanine is a glutamate antagonist and also acts to increase dopamine levels and decrease Norepinephrine levels which results in reduced stress and anxiety in an individual.
  • Magnolia officianalis works on the GABA A site to reduce anxiety, and also works on the Adenosine A1 sites which can lower stress and anxiety.
  • Other GABA agonists include Magnesium, Vitamin B6, Inositol, Taurine, and Melatonin (which increases GABA and Taurine).
  • Alpha lipoic acid increases PGC1 -alpha which increases GABA.
  • Elements that bind to GABA receptors and directly increase GABA include Glycine, Niacinamide, Valerian root, Kava kava, and green tea with Epigallocatechin gallate (EGCG).
  • an element 1 12, Fig. 3 that increases or participates in the action of serotonin. Not only does increasing serotonin decrease nicotine cravings and withdrawal symptoms, but it also decreases stress and anxiety.
  • an element 1 12 that increases serotonin levels is the second component 40, Fig. 1 , of the compound 10 that increases serotonin such as 5-HTP, which is a serotonin precursor.
  • Other elements 1 12 that increase serotonin levels or participate in the action of serotonin include Magnesium, which prolongs the effects of 5-HTP; Inositol, which acts on receptors linked to serotonin signaling; Vinpocetin, which directly raises serotonin levels; and S-adenosylmethionine (SAMe), which augments serotonin reuptake inhibitors.
  • SAMe S-adenosylmethionine
  • Another way to decrease stress and anxiety 14 is by utilizing an element 1 14, Fig. 3, that decreases Cortisol.
  • One such element is
  • Adaptogens 116 help the body adapt to stress, support normal functions, and restore balance and thus act to decrease stress and anxiety 14.
  • Such adaptogens include Bacopa monnieri, Rhodiola rosea, Holy basil, and
  • At least one of the first, second and third components 30, 40, 50 also appears to alter the perceived taste of tobacco smoke 16, Figs. 1 and 3.
  • the specific effect regarding taste may vary among individuals, an observed effect as a result of an individual ingesting some combination of the first, second and/or third components 30, 40, 50 has been an enhancement of the certain taste receptors 62 on upper side 64 the tongue 60, Fig. 2, in regions 70 on the tongue 60 that detect sourness located generally at the right and left sides 80, 82 of the tongue 60, thus making tobacco smoke taste "sour" to the individual.
  • Other taste receptors, those on the tongue 60 (generally illustrated as 62 in Fig.
  • These other taste receptors may be in a region 72 that detects sweetness (a region that partially overlaps the sour regions 70) at the front (e.g., tip) 84 of the tongue 60, a region 74 that detects bitterness toward the rear 86 of the tongue 60, and a region 76 that detects saltiness (notably a region that partially overlaps each of the other regions 70, 72, 74) around the edges 88 of the tongue 60.
  • the souring effect has also been observed to increase with continued ingestion of the first, second and/or third components 30, 40, 50, e.g., letting the component(s) build up in the individual's bloodstream.
  • Other individuals who have ingested some combination of the first, second, and/or third components 30, 40, 50 have noted an "unpleasant bitter” taste (which may be due to an enhancement of taste receptors 62 that detect sourness as well) when smoking tobacco. Again, this effect has been observed to increase with continued ingestion of the first and second components together.
  • the taste of tobacco smoke that is altered by ingesting the first, second, and/or third components, or some combination thereof can be consistently and generically described as "unpleasant" such that the individual is discouraged from smoking due to the unpleasantness of the taste of the smoke.
  • This unexpected result is achieved through the synergistic interaction among some combination of the first, second and/or third components within an individual's body, and may be enhanced and/or exacerbated with the continued ingestion of these components.
  • certain elements suppress appetite 22 or have lipotropic effects 24, thus maintaining body weight 18 (either by suppressing body weight gain or causing loss of body weight) in an individual attempting to reduce or cease smoking tobacco.
  • Suppressing appetite 22 can be achieved by regulating blood sugar metabolism 120, thereby decreasing appetite 22 since cravings for certain carbohydrates such as sugars are decreased.
  • Alpha lipoic acid is such an element that improves blood sugar metabolism 120 in that it stimulates uptake of glucose via stimulation of GLUT 4 protein, which is a primary glucose transporter in muscle, cardiac and fat cells.
  • Alpha lipoic acid is also an up-regulator cofactor for insulin, thyroid, GABA, and other catecholamines. Chromium, in particular
  • Chromium picolinate acts synergistically with Biotin to regulate blood sugar metabolism 120 by improving glucose tolerance, thus suppressing appetite 22.
  • Butyrate and Gymnema sylvestre also regulate blood sugar metabolism 120 through increased insulin sensitivity.
  • Suppressing appetite 22 can also be achieved by increasing or participating in the action of serotonin 122, which have been described above and include second component 40, Fig. 1 , of the compound 10 such as 5-HTP, which is a serotonin precursor; Magnesium, which prolongs the effects of 5-HTP; Inositol, which acts on receptors linked to serotonin signaling; Vinpocetin, which directly raises serotonin levels; and S-adenosylmethionine (SAMe), which augments serotonin reuptake inhibitors. Suppressing appetite 22 can further be achieved by increasing or participating in the action of dopamine 124.
  • 5-HTP which is a serotonin precursor
  • Magnesium which prolongs the effects of 5-HTP
  • Inositol which acts on receptors linked to serotonin signaling
  • Vinpocetin which directly raises serotonin levels
  • SAMe S-adenosylmethionine
  • 5-HTP not only increases serotonin, but it also increases dopamine and norepinephrine, all of which decrease cravings for certain carbohydrates.
  • Tyrosine and its derivatives increase dopamine by being converted, with Tetrahydrobiopterin as a cofactor, within the body to the
  • catecholamine neurotransmitters dopamine, norepinephrine, and epinephrine
  • L-phenylalanine and/or DL- phenylalanine also increase dopamine as well as norepinephrine.
  • Arginine increases dopamine since it is a dopamine agonist.
  • Green tea with Epigallocatechin gallate (EGCG) augments dopamine, and Mucuna puriens (Cowage seed) contains naturally-occurring levodopa (L-Dopa), which is an intermediate in dopamine synthesis.
  • Gymnema sylvestre (Gumar), as well as regulating blood sugar metabolism as described above, also suppresses appetite 22 by decreasing the sensitivity of taste receptors that detect sweetness 126, which decreases the desire for sweet foods including those containing sugars. As shown in Fig. 2, at least some of the sweetness taste receptors are located at the tip 84 of the tongue 60 as indicated at 72.
  • elements that have lipotropic effects 24 can also allow an individual attempting to reduce or cease smoking to maintain body weight 18 by enhancing the body's ability of metabolize fat 128.
  • Such elements 128 include Vitamin B6, Vitamin B12, Choline (including Phosphatidylcholine and other forms of Choline), Inositol, Methionine, and S-adenosylmethionine (SAMe). Methionine and SAMe are each used in the methionine/methylation cycle which activates serotonin and melatonin production.
  • a supplement that replenishes depleted body substances 20, repairs damaged body substances 20, or ameliorates the function of body substances 20 may include nutrients that are depleted 26 from an individual's body as well as cellular constituents such as, for example, enzymes and cofactors that are depleted, damaged, or their function impaired 28 due to smoking tobacco or being exposed to environmental tobacco smoke.
  • Nutrients that are depleted 26 from an individual's body include (in any of their forms noted above) Vitamin B6, Biotin, Vitamin B12, Melatonin, Dopamine, Serotonin, Choline, Calcium, Vitamin E, Folate, Magnesium, Manganese, Vitamin B2, Vitamin A, Vitamin C, Selenium, Zinc, Carotenoids, Bioflavonoids, Vitamin D, Glutathione (which can be made from N-acetylcysteine), and S-adenosylmethionine (SAMe).
  • Vitamin B6 Biotin, Vitamin B12, Melatonin, Dopamine, Serotonin, Choline, Calcium, Vitamin E, Folate, Magnesium, Manganese, Vitamin B2, Vitamin A, Vitamin C, Selenium, Zinc, Carotenoids, Bioflavonoids, Vitamin D, Glutathione (which can be made from N-acetylcysteine), and S-adenosylmethionine (SAM
  • Cellular constituents that are depleted, damaged, or their function impaired 28 include vascular endothelium which can be improved by CoQ.10 and Melatonin, Catalase, which can be increased by Bacopa; Glutathione reductase and Glutathione peroxidase, which can be increased by N- acetylcysteine; Sulfhydryl moiety, which is critical for enzyme function; Superoxide dismutase; and Peroxisomal enzyme (alkyl DHAP), which can be increased by Butyrate.
  • Catalase which can be increased by Bacopa
  • Glutathione reductase and Glutathione peroxidase which can be increased by N- acetylcysteine
  • Sulfhydryl moiety which is critical for enzyme function
  • Superoxide dismutase and Peroxisomal enzyme (alkyl DHAP), which can be increased by Butyrate.
  • Choline and in particular Phosphatidylcholine, maintains and reestablishes cellular membranes which may be lost or damaged due to tobacco smoking or exposure to second-hand tobacco smoke. This element does so by increasing polyunsaturated fats in the cell membrane, thereby helping to restore the cell membrane.
  • CoQ10 helps repair and rebuild vascular endothelium and other cellular constituents damaged by tobacco smoking. Melatonin reduces
  • exemplary daily dosage ranges for a daily dosage of each of the above-described elements will now be listed. These ranges are not intended to be limiting, and the daily dosage of any of these elements may depend on such factors as the amount of exposure to tobacco smoke for smokers and those exposed to environmental smoke including daily amount and total amount of exposure, body weight, age, biochemical sensitivity and uniqueness, physical condition, severity of withdrawal symptoms, and the like. Thus, the element and amount thereof given can be changed to suit an individual's unique biochemical diversity.
  • the exemplary daily dosage ranges are as follows, in any form including those stated above:
  • Beta-cryptoxanthin 1 - 20 mg Zeaxanthin, 1 -8 mg Lycopene or 1 -40 mg Lutein
  • Bioflavonoid and/or any element that increases a Bioflavonoid including 10-750 mg Quercetin, 10-1 ,000 mg Hesperidin, 10-900 mg Garlic, and 10-360 mg Pycnogenol
  • the compound 10 can be administered orally in a pill, capsule, gelatine, powder, or liquid form twice per day two hours before or after a meal to maximize absorption thereof by the body.
  • Alternative methods of administration could be intravenous, via suppository, transdermal patch, cream, gel, ointment, chewing gum, lozenge, and the like.
  • Methods for delivering the compound 10 may utilize modified cellulase binders; hydroxypropyl methyl cellulose; liposomes; hypromellose materials for tablet binders, film coating, or as a matrix for the use in extended- release tablet formulations; nanotechnology delivery systems; hydrocolloids; and the like.
  • the compound 10 could be sweetened with sugar or low glycemic index sugar such as sucralose, stevia, agave nectar, xylitol, or the like.
  • Fig. 4 schematically illustrates a method 130 of replenishing body substances, repairing body substances, or ameliorating the function of body substances depleted, damaged, or their function impaired as a direct result of smoking tobacco or being exposed to environmental tobacco smoke.
  • the method 130 comprises a step 132 of administering a supplement 134 comprising a
  • the supplement 134 comprises one or more vitamins, minerals, enzymes, amino acids, cofactors, precursors, neurotransmitters, and cellular constituents.
  • the supplement 134 replenishes, repairs, or ameliorates the function of multiple body substances depleted, damaged or their function impaired in the individual as a direct result of smoking tobacco or being exposed to environmental tobacco smoke.
  • the supplement 134 may include nutrients that are depleted 26 from an individual's body as well as cellular constituents such as, for example, enzymes and cofactors that are depleted or damaged 28, Fig. 3, due to smoking tobacco or being exposed to environmental tobacco smoke.
  • Nutrients that are depleted 26, Fig. 3, from an individual's body include (in any of their forms noted above) Vitamin B6, Biotin, Vitamin B12, Melatonin, Pantothenic acid, Dopamine, Serotonin, Choline (which maintains, reestablishes, and helps restore cellular membranes as described above), Calcium, Vitamin E, Folate, Magnesium, Manganese, Vitamin B2, Vitamin A, Vitamin C, Selenium, Zinc,
  • Carotenoids, Bioflavonoids, Vitamin D, and Glutathione which can be made from N- acetylcysteine.
  • Cellular constituents that are depleted, damaged, or their function impaired 28 include vascular endothelium which can be improved by CoQ10 and Melatonin, Catalase which can be replenished by Bacopa, Glutathione reductase which can be replenished by N-acetylcysteine, Sulfhydryl moiety which is critical for enzyme function, Superoxide dismutase, and Peroxisomal enzyme (alkyl DHAP) which can be replenished by Butyrate.
  • FIG. 5 schematically illustrates a method 140 of assisting an individual attempting to reduce or cease tobacco smoking comprising the step 142 of
  • the compound 144 comprises a first component 30, Fig. 1 , comprising at least one element that blocks nicotine receptor sites in the individual. Such a first component 30 may be as described above relative to Fig. 1.
  • the compound 144 also comprises a second component 40, Fig. 1 , comprising at least one element that increases serotonin levels in the individual. Such a second component 40 may be as described above relative to Fig. 1 .
  • the compound 144 further comprises a third component 50, Fig.

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