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
  • A61K31/33—Heterocyclic compounds
  • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
  • A61K31/47—Quinolines; Isoquinolines
  • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
• • 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
  • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
  • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
  • A61K31/445—Non condensed piperidines, e.g. piperocaine
  • A61K31/4468—Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
• • 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
  • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
  • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P25/00—Drugs for disorders of the nervous system
  • A61P25/04—Centrally acting analgesics, e.g. opioids
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Definitions

• a pain signal arising as a result of tissue damage or disease is transferred to the central nervous system where it generates the sensation of pain.
• the magnitude of the pain signal is regulated by a system of nociceptive and anti-nociceptive receptors scattered throughout the membrane.
• Stimulatory tachykinin and amino acid receptors found on the neurons of the central and peripheral nervous systems constitute a significant component of the nociceptive receptor system and play a main role in the transfer of pain signals.
• Calcium channels play an important role in the stimulation of the nociceptive system.
• the transfer of a pain signals requires a change in the permeability of the cell membrane to calcium ions.
• the administration of weak type N calcium channel blockers such as flunnarizine or cinnarizine greatly enhances the analgesic effect of opioid analgesics.
• the simultaneous administration of calcium channel blockers with opioid analgesics greatly delays the drug tolerance of opioids.
• the combined administration of calcium channel blockers with opioids constitutes a novel, more effective solution in the treatment of pain, particularly of chronic pain such as cancer, neuropathic, rheumatoid, gout, and phantom pain or the like.
• the subject of the present invention are mixtures of calcium channel blockers with opioid analgesics for use in the treatment of chronic pain caused by disease or postoperative states or due to trauma.
• Example 1 A mixture was prepared of morphine hydrochloride and flunnarizine hydrochloride at a ratio of 1:5 by mass. This mixture was injected into mice intraperitoneally at a rate of 12 mg/kg. At the same time, a control group was examined which was given only morphine hydrochloride at a corresponding dose of 2 mg/kg. In both groups, the anti-nociceptive effect was examined using the tail withdrawal delay test from water at a temperature of 55°C. It turned out that the combination of flunnarizine and morphine increases the analgesic effect more than twofold.
• Example 2 A mixture was prepared of morphine hydrochloride and flunnarizine hydrochloride at a ratio of 1:5 by mass. This mixture was injected into mice intraperitoneally at a rate of 12 mg/kg. At the same time, a control group was examined which was given only morphine hydrochloride at a corresponding dose of 2 mg/kg. In both groups, the anti-nocicept
• mice We examined the degree of induction of tolerance to opioid analgesics in mice.
• the control group was given a twice-daily, intraperitoneal dose of 2 mg/kg of morphine hydrochloride.

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• Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Life Sciences & Earth Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Epidemiology (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Organic Chemistry (AREA)
• Pain & Pain Management (AREA)
• General Chemical & Material Sciences (AREA)
• Neurology (AREA)
• Neurosurgery (AREA)
• Engineering & Computer Science (AREA)
• Biomedical Technology (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Rheumatology (AREA)
• Emergency Medicine (AREA)
• Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Applications Claiming Priority (2)

Publications (1)

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Citations (3)

• 2009
  • 2009-05-07 PL PL387984A patent/PL387984A1/pl unknown
• 2010
  • 2010-05-07 WO PCT/PL2010/050016 patent/WO2010128873A1/en active Application Filing

Patent Citations (3)

Non-Patent Citations (6)

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