Classifications

• • 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
• • 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
  • A61K31/33—Heterocyclic compounds
  • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole

Definitions

• THIS invention relates to the treatment of patients presenting with synaptic fatigue related conditions and to pharmaceutical compositions for use in such treat- ent. More particularly this invention relates to the treatment of a condition which the inventor has characterised as serotonin depletion illness [herein ⁇ after referred to as SDI] .
• SDI is a central neurochemical disorder involving the all important mid- line raphe nucleus in the medulla, the RAS, hypothalmus and the entire autonomic nervous system.
• SDI is a physical condition found mainly in urban societies where an abundance of sensory input [popular ⁇ ised as stress] exhausts the midline raphe nucleus in its production of serotonin [5-Hydroxytryptamine] and in this way causes sleep disturbances, hyperalgesia [defective pain modulation] and alteration of mood [depression and irritability].
• the inventor is of the view that conditions such as myofascial syndrome, fibromyalgia, fibrositis, masked depression, yuppie flu [epidemic myalgic encephalomyel- itis syndrome] and a host of chronic pain conditions as well as indications of altered immunity may be placed under one umbrella, namely that of SDI. cordingly it is suggested that SDI should be included in the differential diagnosis of a multiplicity of conditions which include:
• SDI is an easily recognisable clinical diagnosis and not a single laboratory or other special examination is necessary before institution of treatment.
• This invention provides for the use of a serotonin agonist in combination with sulpiride in the production of an intravenous infusion composition for use in the
• the serotonin agonist is preferably selected from the group consisting of the tricyclic anti-depressants, maprotiline hydrochloride and mianserin hydrochloride.
• the serotonin agonist is preferably amitriptyline.
• an intravenous infusion composition comprising amitriptyline in combination with sulpiride in a physiologically acceptable carrier.
• the carrier may be a normal saline solution.
• an intravenous infusion product in unit dosage form for use in the treatment of a stress related condition, including SDI comprising a container and an hypodermic needle secured thereto, the container containing a composition comprising between 10 and 50 mg amitriptyline and between 50 and 200 mg sulpiride in a normal saline carrier.
• the container may be in the form of an infusion bag.
• this aspect of the invention there is provided a three day treatment course of the infusion product of the invention com ⁇ prising three infusion products in unit dosage form as described above, the three containers each containing about 50 millilitres of normal saline, about 100 mg sulpiride and respectively about 10 mg to 40 mg amitriptyline.
• SUBSTITUTE SHEET amitriptyline dosage to a number of patients presenting with the typical synaptic fatigue symptoms described above.
• This treatment regimen usually resulted in excellent pain modulation, mood elevation and restor- ation of delta sleep after which the patients were kept on low dosage amitriptyline or another serotonin agonist [per os] for at least six months.
• the invention also relates to a method of treating SDI by the simultaneous or sequential intravenous infusion of a serotonin agonist and sulpiride as described above.
• SUBSTITUTE SHEET academic was suffering from chronic fatigue to such an extent that she was virtually bedridden for seven years and was diagnosed with myalgic encephalomyelitis. She had been extensively investigated and treated by her specialist physician for the previous seven years, using mainly vitamins and magnesium supplementation. She had been prescribed bed rest and the exclusion of various foodstuffs. One day after treatment according to the invention she felt so much better that she went for a run of several kilometers.
• a fifty-five year old bank manager with cluster headaches and accompanied Horner Syndrome was cured by the treatment according to the invention after many years of multiple examinations, hospital admissions and consultations.
• a forty-two year old housewife and a forty-four year old part-time worker presented with the same blood pictures after treatment failure, which was corrected after attending to their hormone picture.
• a thirty-five year old male divorce victim showed severe anger and rages. He sought psychological counseling because he felt self-destructive. He felt rested and self-contented after the first infusion of the composition according to the invention and recovered fully after the standard treatment.
• amitriptyline a serotonin agonist [it promotes the recycling of this important modulator] together with Sulpiride, which stimulates the secretion
• SUBSTITUTE SHEET of the endogenous opoids have a potent synergistic action.
• it is given intravenously to obtain bolus infusion over the blood brain barrier into the aquaductus of Sylvius so that the medicated cerebral spinal fluid will attend to the dry synaptic vesicles of not only the synaptic knobs in the medulla but also of the synaptic knobs of the dendrites and axons in other parts of the central nervous system.

Landscapes

• Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Epidemiology (AREA)
• Life Sciences & Earth Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Applications Claiming Priority (3)

Publications (1)

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ID=25581876

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• 1993
  • 1993-07-14 ZA ZA935078A patent/ZA935078B/xx unknown
  • 1993-07-15 EP EP93917128A patent/EP0651638A1/de not_active Withdrawn
  • 1993-07-15 WO PCT/US1993/006554 patent/WO1994002138A1/en not_active Application Discontinuation
  • 1993-07-15 AU AU46746/93A patent/AU4674693A/en not_active Abandoned

Non-Patent Citations (1)

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