WO2006075976A1 - Utilisation d'un anesthesique local pour corriger un comportement alimentaire humain, et procede d'utilisation associe - Google Patents

Utilisation d'un anesthesique local pour corriger un comportement alimentaire humain, et procede d'utilisation associe Download PDF

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Publication number
WO2006075976A1
WO2006075976A1 PCT/UA2005/000020 UA2005000020W WO2006075976A1 WO 2006075976 A1 WO2006075976 A1 WO 2006075976A1 UA 2005000020 W UA2005000020 W UA 2005000020W WO 2006075976 A1 WO2006075976 A1 WO 2006075976A1
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Prior art keywords
local anesthetic
active ingredient
eating
food
local
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PCT/UA2005/000020
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English (en)
Russian (ru)
Inventor
Igor Viktorovich Varaksin
Natalia Alexandrovna Sedova
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Private Enterprise 'slavyanskaya Klinika'
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Publication of WO2006075976A1 publication Critical patent/WO2006075976A1/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents

Definitions

  • the invention relates to the psychosomatic and psychotherapeutic fields of medicine, in particular, auxiliary medication for changing eating behavior in people interested in their figure, suffering from excess body weight.
  • Information on local anesthetics and their use is described in the medical literature, for example, “Anesthesia in the conditions of a dental clinic”, Bizyaev A.F., Ivanov C.Yu., Lepilin AB, Rabinovich CA, -M: GOU VUMNTs MZ RF, 2002. -144s : ill.
  • local anesthetics affect the functional state of sensitive nerve endings and conductors, changing their excitability and conductivity.
  • the susceptibility of neurons to local anesthetics varies.
  • Local anesthetics are used for pain relief, as they reduce or completely eliminate the flow of pain impulses from the site of intervention in the central nervous system, acting on sensitive nerve endings or fibers.
  • Non-myelinated and thin myelinated nerve fibers are most sensitive to these drugs.
  • painful, then olfactory, taste, temperature sensitivity is inhibited.
  • the feeling of touch and pressure on the tissue, tactile sensitivity is carried out by myelinated type A fibers, less sensitive to anesthetics.
  • local anesthetics cause a reversible temporary loss of sensation of pain, taste, cold, heat, and, last but not least, pressure.
  • the drug For the manifestation of local anesthetic activity, the drug must pass through the membrane of the nerve fiber, therefore, hydrolysis of the local anesthetic salt must occur in the tissues with the release of the base anesthetic, which is readily soluble in fats and penetrates through the phospholipid membrane.
  • the hydrolysis of the drug depends on its dissociation constant - pKa and acidity - the pH of the tissues.
  • Most local anesthetics have a pKa of 7.6–7.9; therefore, their hydrolysis occurs in a slightly alkaline medium of intercellular fluid.
  • a local anesthetic is all the more effective the higher its concentration on the outer membrane of the nerve fiber and the more active its hydrolysis, i.e. the closer the pKa of the anesthetic and the pH of the tissues.
  • a solution of local anesthetic of low concentration, introduced in a large volume, is widely distributed in tissues, which is used during infiltration anesthesia. However, its diffusion into the membrane of the nerve fiber is negligible.
  • an anesthetic concentrated solution is less distributed in the tissues, but diffuses better into the nerve fiber membrane, which is important when conducting conduction anesthesia, when it should act on the nerve conductors, and not on the ends of the sensory nerves.
  • local anesthetics are used, which penetrate well into tissues and act on sensitive nerve endings: pyromecain, anesthesin, lidocaine.
  • novocaine, trimecaine, lidocaine, mepivacaine, prilocaine, bupivacaine, ethidocaine, articaine are used.
  • Anestezin (Apeststesipum) Synonym: benzocaine.
  • the chemical composition is ethyl ester of para-aminobenzoic acid. Unlike other local anesthetics, it is poorly soluble in water and is used only for surface anesthesia. Anesthesia develops slowly, the effect is weak, but prolonged. Poorly absorbed. It is used to anesthetize wound, ulcer, burn surfaces and relieve itching. For anesthesia of mucous membranes, wound and burn surfaces 5-20% solutions in oil or glycerin, 5-10% ointments, pastes and powders are used. To anesthetize hard tissues of the tooth, powder or 50-70% anestezine paste is used.
  • anestezin is not irritating and practically non-toxic.
  • the maximum dose for topical application is 5 g (25 ml of a 20% solution).
  • lidocaine mepivacaine, prilocaine, ethidocaine, bupivacaine, articaine.
  • mepivacaine mepivacaine
  • prilocaine ethidocaine
  • bupivacaine articaine.
  • Their main advantage is that they diffuse better into the tissues at the injection site, act faster, have a larger anesthesia zone and a stronger interaction with the tissues, which prevents the local anesthetic from entering the blood stream.
  • Lidocaine Lidocaine (Lidosaipum)
  • Synonyms xicain, xylodont, xylocaine, lignocaine, lidocard, luan, octocaine.
  • Chemical composition 2-diethylamine-2 ', b'-acetoxylidide hydrochloride. Amide derivative of xylidine. It is used for all types of anesthesia and is considered the ancestor of all amide preparations. For infiltration and conduction anesthesia in dentistry, a 2% anesthetic solution is used. The drug actively dilates blood vessels, therefore, it is used in combination with vasoconstrictors. 10% aerosol solution, 5% gel, 2-5% ointment are used for application anesthesia of the oral mucosa.
  • Lidocaine has a pKa of 7.9; quickly hydrolyzes at weakly alkaline pH of tissues, easily penetrates tissue membranes, creating a high concentration at the receptor. The local anesthetic effect develops rapidly (after 2-4 minutes).
  • the drug can be used for all types of anesthesia.
  • the drug has been widely used as an antiarrhythmic agent.
  • the effective concentration for injection analgesia in dentistry is 2%, for terminal anesthesia - 4-10%. Without a vasoconstrictor, lidocaine dilates blood vessels, is rapidly absorbed.
  • Pulp anesthesia with 2% lidocaine lasts from 5 to 10 minutes, soft tissue anesthesia from 60 to 120 minutes, and with the addition of adrenaline hydrochloride (1: 50,000 or 1: 100,000), the duration of pulp anesthesia is 60 minutes.
  • lidocaine with a vasoconstrictor is more often used.
  • the maximum total dose for injection is up to 4.4 mg / kg, but not more than 300 mg.
  • lidocaine 200 mg
  • Pyromecain (Ruromesaipum) Synonym: bumecaine hydrochloride.
  • Xylidine derivative It is used mainly for conduction and infiltration analgesia. In terms of anesthetic activity, it is two to three times higher than novocaine, it acts faster and longer. Somewhat more toxic than novocaine, especially in high concentrations.
  • the drug does not irritate tissues.
  • the drug dilates blood vessels, therefore it is used with vasoconstrictors.
  • Mepivacaine (Merivasaipum)
  • physico-chemical properties and pharmacokinetics is close to lidocaine.
  • the dissociation constant of mepivacaine pKa 7.6
  • Mepivacaine unlike lidocaine, does not have a pronounced vasodilating effect, which determines the long duration of its effect and the possibility of use without a vasoconstrictor.
  • the duration of pulp anesthesia caused by 3% mepivacaine without a vasoconstrictor is 20-40 minutes, and soft tissue anesthesia is 2-
  • lidocaine When using lidocaine, these indicators are 5-10 minutes and 60-120 minutes, respectively. Adding a vasoconstrictor to a 2% solution of mepivacaine (1: 20,000 levonordephrine or 1: 200,000 adrenaline) lengthens pulp anesthesia for up to 60 minutes, and soft tissue anesthesia for up to 3
  • Ethidocaine (Etidosaipum) Synonym: duranest.
  • Chemical composition 4-methyl-3- [2-lopropylaminopropionamido] -2-thio-phencarboxylic acid methyl ester.
  • Amide group local anesthetic, thiophene derivative. It has good diffusion ability, but lipophilicity is lower than that of other amide anesthetics, therefore it is absorbed worse into the blood.
  • Articaine has a low pKa (7.8), so it hydrolyzes well in tissues and acts quickly (after 1-4 minutes).
  • the drug is 3-5 times more active and 1.5 times more toxic than novocaine. It has an optimal ratio of activity and toxicity indicators, the largest breadth of therapeutic effect. It is one of the most active and least toxic local anesthetics. Used for infiltration and conduction anesthesia.
  • lidocaine acts faster than lidocaine, has a higher diffusion ability and degree of binding to proteins, lower fat solubility, which reduces its toxicity. It has a vasodilating effect, it is used in combination with vasoconstrictors, added in minimal concentrations. Allergic reactions to articaine are quite rare. Articaine has the highest degree of diffusion, which has been confirmed in clinical practice. Due to easy diffusion in the tissue, articaine freely penetrates through the bone to the oral part of the alveolar process. High local anesthetic activity of the drug allows to reduce the content of vasoconstrictor in its solution to 1: 200000.
  • the low toxicity of articaine allows it to be used in a 4% solution having a high anesthetic activity, which provides the possibility of use for children, pregnant women and the elderly.
  • Preparations of 4% articaine: ultracain DS, alfacain H, septanest contain adrenaline at a concentration of 1: 200000, and ultracain DS-forte contains adrenaline at a concentration of 1: 100000.
  • a standard solution of lidocaine with an adrenaline of 1: 100000 provides a sufficient duration of anesthesia for most dental outpatient interventions.
  • a solution of mepivacaine with levonordephrine 1: 200000 has a longer effect, which is due to the lower vasodilating properties of this drug.
  • a 4% solution of articaine with epinephrine 1 -200000 also has anesthetic activity of sufficient duration, and an increase in the concentration of the vasoconstrictor to 1: 100000 allows you to prolong the effect of the drug.
  • the presented group of inventions is based on the following psychological factors and mechanisms. In the motivation of human nutritional behavior, the most significant are: expectations, self-efficacy, self-concept (self-fulfilling prophecies), internal dialogues, complex equivalents, value judgments. Expectations are a powerful frame of behavior. Expectations of the onset of positive emotions as a result of satiation (emotions of freedom, pleasure, relaxation, comfort, security, joy, stress relief, stress) play a crucial role among them. It is their unrealization in reality that forces (forces, moves, predetermines) to prolong and strengthen actions, in particular - to overeat.
  • the aim of this group of inventions is to terminate (destroy) the above psychological pattern of behavior, while respecting the environmental friendliness of the completion of the pattern - the subconscious desire to chew (to receive sensations from the oral cavity), avoiding the protest reactions that usually appear during any attempts at dietary correction.
  • the goal is also to change the human nutritional behavior using substances that are safe for consumption using methods of administration that do not require medical qualifications.
  • the purpose of the invention for use is to provide changes in human nutritional behavior by the use of substances that are safe for consumption, while ensuring the use of a method for the intake of these substances that does not require medical qualifications.
  • any toothpaste, any candy, any solution or any edible is added in a subtherapeutic dose: local (surface, contact) anesthetic: anestezin or articaine, or lidocaine, or mepivacaine, or pyromecaine, or trimecaine, or ethidocaine orally or locally anesthetizing drugs with any additives, such as vasoconstrictors, which are marketed for industry medical goals.
  • local anesthetic anestezin or articaine, or lidocaine, or mepivacaine, or pyromecaine, or trimecaine, or ethidocaine orally or locally anesthetizing drugs with any additives, such as vasoconstrictors, which are marketed for industry medical goals.
  • anesthetic anestezin or articaine, or lidocaine, or mepivacaine, or pyromecaine, or trimecaine, or ethidocaine orally or locally anesthetizing drugs with any additives, such as vasoconstrictors
  • Signs that are significant in some cases are the use of anestezin or articaine, or lidocaine, or mepivacaine, or pyromecaine, or trimecaine, or ethidocaine orally in a subtherapeutic dose:
  • the method is carried out by psychotherapeutic effects and diet therapy for 2 months.
  • psychocorrection is used, which is necessary for positive changes in the motivational-needful sphere of the person, leveling cognitive and emotional dissonance
  • psychotherapeutic effect is carried out by forming a dominant that changes the human nutritional behavior
  • diet therapy is prescribed with an energy value of 1200-1300 kcal / day.
  • Use a psycho-corrective effect both before a psychotherapy session, and in the rehabilitation period.
  • the following methods and techniques of psychotherapy are applied sequentially: rational, suggestive, behavioral (stress-psychotherapy with positive reinforcement), elements of holotropic therapy, neuro-linguistic programming.
  • the ratio of the main nutrients of proteins, fats, carbohydrates is 1.0: 0.9: 1.5.
  • the resulting stress response is verbally associated with the sensations that arise, after removing the patient from hypnotic immersion, pressure is applied in the region of the middle part of the superciliary arches to the pain, in the affirmative form i informs that the metabolism has changed, the appetite has decreased and the patient pronounces the self-awareness formula.
  • Common essential features is the implementation of rational psychotherapy with a focus on the formation of negative emotions towards - abuse of food supported by a substance that affects a person's senses, to achieve emotionally negative effects on the use of high-calorie foods and increase the effectiveness of treatment for obesity.
  • the disadvantages of this method are the possible complications associated with too intense multifaceted, stressful effects on the human body, in which it is difficult to control the reaction and health of the patient, the need for a course of treatment with a large number of procedures for which the patient must either visit a doctor daily or be treated in a stationary mode, while the restriction of food intake is directive, which creates discomfort for the patient and, after completing the course of treatment, the patient cannot count on anything helping him to refrain from returning to overeating .
  • the purpose of the presented method is to create for people suffering from excessive overeating, the opportunity, or having received from the doctor the initial settings and instruction, or independently - to correct their eating behavior, or, after a full course of psychotherapeutic treatment and treatment for obesity, maintain themselves for an unlimited time in form, applying the proposed method on their own.
  • the way to correct eating behavior is as follows: in any accessible way (verbally, in writing) information is conveyed to the consumer about the possibility, at his request, of influencing his eating behavior and adjusting his nutritional needs with the help of the proposed product containing a local anesthetic: either chewing gum or tooth paste, or a biologically active additive in a food product, or by biting a dose of anesthetic in capsules with a protective synthetic shell or in capsules with gel, protein or other edobnoy shell and mouthwash.
  • a local anesthetic either chewing gum or tooth paste, or a biologically active additive in a food product, or by biting a dose of anesthetic in capsules with a protective synthetic shell or in capsules with gel, protein or other edobnoy shell and mouthwash.
  • the essential features of the method are the correction of human nutritional behavior, including preliminary psychological preparation and instruction of a person, moreover, the eating process is interrupted at the moment, which is determined either by the doctor’s recommendations or independently, and a subtherapeutic dose of local anesthetic is orally taken: chewing gum containing local anesthetic as an active ingredient until satiety; rinsing the mouth with an aqueous solution or dental elixir containing a local anesthetic as an active ingredient; performing toothbrushing with toothpaste or tooth powder containing a local anesthetic as an active ingredient; having sucked a candy, tablet or pill containing a local anesthetic as the active ingredient, or having bitten a protective capsule, or eat a capsule with a gel, protein or other edible coating containing the necessary dose of local anesthetic.
  • Distinctive features essential in all cases is the interruption of the eating process, at a time that is determined by the individual restriction of the amount of food consumed and the adoption of an oral subtherapeutic dose of a local anesthetic.
  • Distinctive features that are significant in some cases are that during the rehabilitation period or without prior treatment, they independently get acquainted with the action of a product containing a local anesthetic according to the instructions and take the product on their own, while for taking a subtherapeutic dose of a local anesthetic it is performed:
  • - chewing chewing gum which contains a local anesthetic in a subtherapeutic dose as an active ingredient, until the feeling of fullness; - rinsing the mouth with an aqueous solution or dental elixir containing a local anesthetic, as an active ingredient;
  • capsules having a gel or protein edible shell.
  • a product and method has been obtained for people suffering from excessive overeating, providing an opportunity, or having received initial settings and instruction from a doctor, or independently, to correct their eating behavior, and also, after passing a full course of psychotherapeutic treatment and treatment for obesity, maintain themselves for an unlimited time in shape, using the proposed method and product containing a local anesthetic on its own.
  • Example 1 The use of local anesthetics as a component of chewing gum. Chewing gum in the implementation of the proposed application is prepared, for example, as follows.
  • the production of chewing gum involves mixing the polymer base of the plasticizer, powdered sugar, aromatic and flavoring components, introducing the components into the resulting mass according to the recipe, and further molding the resulting mass in a heated state.
  • the entire mass of chewing gum is thoroughly mixed to a homogeneous state and enters the table, where it is cooled to 30-35 ° C and rolled into the formation.
  • the layers are fed to a rolling machine, from where the tourniquet is fed into a wrapping machine, where a round tourniquet is formed into a rectangular tourniquet, individual rubber bands are cut and the foil and wrapping are wrapped. Wrapped chewing gums are cooled as they go from wrapping to packaging. Chewing gum is obtained with good taste, does not stick to the teeth, stretches when chewing and provides a change in taste. On the package, information about the presence of a local anesthetic in the chewing gum composition is necessarily highlighted and the instructions describe the use of chewing gum for changing eating behavior.
  • a person who wants to adjust his eating behavior receives a consultation from a doctor or determines on his own how many calories he should limit when consuming food to ensure weight loss or keeping himself in shape.
  • Each meal is interrupted when the acceptable amount of food is reached and the patient begins to chew chewing gum with a local anesthetic.
  • a person does not feel discomfort.
  • a local anesthetic reduces the sensitivity of taste buds and a person stops chewing chewing gum, except that the feeling of fullness, which is physiologically lagging, comes when you try to continue the process of eating, the person does not feel its taste, completely loses its appetite and stops stress and dissatisfaction there is. As a result of such procedures, a person changes his food.
  • the abrasive titanium oxide or chalk
  • the abrasive is introduced into the paste at the rate of 30 ⁇ 15% of the total weight of the finished mixture.
  • Glycerin in an amount of 15 ⁇ 2.5% of the total mass of the finished mixture.
  • Fragrance is introduced in an amount of l ⁇ 0.5%, perfume oil l ⁇ 0, l% of the total mass of the finished mixture.
  • the pH of the composition should be in the range of 5.5-8.5, preferably 6.5-7.5. To give the paste plasticity, it is passed through a mill.
  • the resulting product of a homogeneous pasty consistency has a pleasant taste and smell.
  • the paste is packaged in metal or plastic tubes, be sure to highlight the information about the presence of a local anesthetic in the paste and describe the recommendations for use in the instructions.
  • the introduction of a local anesthetic when brushing your teeth blocks taste sensitivity. Toothpaste has a pronounced antimicrobial and antifungal effect. With prolonged use (from 3 months), the pattern of the previous human eating behavior breaks. At the same time, toothpaste does not have a toxic effect and is completely harmless to the body.
  • the new toothpaste was applied for 45 days in a group of 30 people undergoing outpatient treatment.
  • the average weight reduction was 3.5 kg.
  • Example 3 The use of local anesthetics as a mouthwash.
  • the dentifrice during the implementation of the proposed application is prepared, for example, as follows. 50 ml are poured into the container. boiled water cooled to 20-30 ° ⁇ , • add from 1 to 5 ml. 20% anestezin solution or from 2 to 10 ml.-2% lidocaine solution with the addition of adrenaline hydrochloride (1: 50,000 to 1: 100,000) and is used as a rinse for at least 1 min. at a certain moment, independently, according to the table of energy calorie content of food and its data. Clinical trials were carried out with the participation of 40 patients aged 22-35 years, over 45 days: average decrease in veca-2.5 kg. , and in the control group that did not use an anesthetic, the weight did not change.
  • Example 4 The use of local anesthetics in solid form. An anestezine tablet weighing 0.3 grams, which are produced on an industrial scale, is divided into 4, approximately equal parts. A quarter of the tablets are absorbed in the mouth at the time that is determined to interrupt the meal.
  • Example 5 The use of aerosol irrigation

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Abstract

La présente invention se rapporte à l'utilisation d'un anesthésique local pour corriger un comportement alimentaire chez un être humain, et à un procédé d'utilisation associé. L'invention relève des domaines médicaux de la psychosomatique et de la psychothérapie, et se rapporte en particulier à une action médicamenteuse auxiliaire permettant de modifier un comportement alimentaire et destinée aux personnes en surpoids qui sont préoccupées par leur silhouette. L'invention consiste à utiliser un anesthésique local en dose subthérapeutique, ledit anesthésique se présentant sous la forme d'une substance destinée à corriger un comportement alimentaire humain, d'un ingrédient actif contenu dans une gomme à mâcher ou une préparation d'hygiène buccale, ou d'un additif actif pour aliments, associé à un vasoconstricteur. L'invention a également trait à un procédé de correction d'un comportement alimentaire humain, qui consiste à interrompre le processus de prise de nourriture à un moment défini par une limitation individuelle de la dose de nourriture consommée, et à ingérer par voie orale une dose subthérapeutique d'un anesthésique local. L'invention permet d'obtenir un produit et un procédé permettant aux personnes atteintes de suralimentation de corriger leur comportement alimentaire et de se maintenir en forme pendant un temps indéfini, soit après consultation et instructions d'un médecin, soit indépendamment, grâce au procédé et au produit contenant l'anesthésique local selon l'invention
PCT/UA2005/000020 2005-01-14 2005-05-25 Utilisation d'un anesthesique local pour corriger un comportement alimentaire humain, et procede d'utilisation associe WO2006075976A1 (fr)

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WO2013043143A1 (fr) * 2011-09-21 2013-03-28 Slyusar Viktor Timopheevich Méthode pour réduire le poids corporel excessif

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RU2056116C1 (ru) * 1995-03-29 1996-03-20 Надежда Петровна Бурмака Способ коррекции веса тела при алиментарном ожирении

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BUNYNA E.M. ET AL.: "Lechenie pervichnogo ozhireniya dlitelnym gozirovannym golodaniem v sochetanii s psikhoterapiey", ZHURNAL NEVPROLOGII I PSIKHIATRII IMENI S.S. KORSAKOVA, vol. 101, no. 12, 2001, pages 37 - 42 *
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MASHKOVSKY M.D.: "Lekarstvennye sredstva", MEDITSINA, 1986, MOSCOW, pages 324 - 326, AND 329 - 332 *

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