MX2015012879A - Formulaciones combinadas de neosaxitoxina para una anestesia local prolongada. - Google Patents
Formulaciones combinadas de neosaxitoxina para una anestesia local prolongada.Info
- Publication number
- MX2015012879A MX2015012879A MX2015012879A MX2015012879A MX2015012879A MX 2015012879 A MX2015012879 A MX 2015012879A MX 2015012879 A MX2015012879 A MX 2015012879A MX 2015012879 A MX2015012879 A MX 2015012879A MX 2015012879 A MX2015012879 A MX 2015012879A
- Authority
- MX
- Mexico
- Prior art keywords
- neostx
- bupivacaine
- combination
- epinephrine
- blockade
- Prior art date
Links
- PPEKGEBBBBNZKS-HGRQIUPRSA-N neosaxitoxin Chemical compound N=C1N(O)[C@@H](COC(=O)N)[C@@H]2NC(=N)N[C@@]22C(O)(O)CCN21 PPEKGEBBBBNZKS-HGRQIUPRSA-N 0.000 title abstract 4
- PPEKGEBBBBNZKS-UHFFFAOYSA-N Neosaxitoxin Natural products N=C1N(O)C(COC(=O)N)C2N=C(N)NC22C(O)(O)CCN21 PPEKGEBBBBNZKS-UHFFFAOYSA-N 0.000 title abstract 2
- 238000009472 formulation Methods 0.000 title abstract 2
- 238000002690 local anesthesia Methods 0.000 title abstract 2
- 239000000203 mixture Substances 0.000 title abstract 2
- 230000002035 prolonged effect Effects 0.000 title abstract 2
- 229960003150 bupivacaine Drugs 0.000 abstract 3
- 229960005139 epinephrine Drugs 0.000 abstract 3
- UCTWMZQNUQWSLP-VIFPVBQESA-N (R)-adrenaline Chemical compound CNC[C@H](O)C1=CC=C(O)C(O)=C1 UCTWMZQNUQWSLP-VIFPVBQESA-N 0.000 abstract 2
- 229930182837 (R)-adrenaline Natural products 0.000 abstract 2
- 239000003195 sodium channel blocking agent Substances 0.000 abstract 2
- LEBVLXFERQHONN-UHFFFAOYSA-N 1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide Chemical compound CCCCN1CCCCC1C(=O)NC1=C(C)C=CC=C1C LEBVLXFERQHONN-UHFFFAOYSA-N 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 230000036407 pain Effects 0.000 abstract 1
- 229940125794 sodium channel blocker Drugs 0.000 abstract 1
Classifications
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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
- A61K31/33—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
-
- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
-
- 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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
- A61K31/24—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
- A61K31/245—Amino benzoic acid types, e.g. procaine, novocaine
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P23/00—Anaesthetics
- A61P23/02—Local anaesthetics
-
- 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]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Emergency Medicine (AREA)
- Dermatology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Anesthesiology (AREA)
- Rheumatology (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
Debido a que los bloqueadores de los canales de sodio que actúan sobre el sitio 1 presentan una actividad única y no pueden usarse para extrapolar la dosis eficaz de otros bloqueadores de los canales de sodio que actúan sobre el sitio 1, se realizaron estudios para identificar las dosis de la neosaxitoxina ("NeoSTX") y de la bupivacaina, por sí sola o en combinación con epinefrina, que podrían resultar eficaces para aliviar el dolor durante un período de dos ó tres días en los seres humanos. Las combinaciones de bupivacaina y NeoSTX provocaron un bloqueo con una confiabilidad y una duración mayores que las que se observaron cuando se administró la NeoSTX sola. Con una combinación de tres compuestos, NeoSTX, bupivacaína y epinefrina, se obtuvo una anestesia local más prolongada que la que se obtuvo con una combinación de dos compuestos, NeoSTX y bupivacaína. La adición de epinefrina a la combinación de NeoSTX y bupivacaína tuvo como consecuencia una prolongación dramática en la duración del bloqueo completo ante los estímulos mecánicos. Sobre la base de estos resultados, se desarrollaron diversas formulaciones de dosificación combinadas específicas.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201361789054P | 2013-03-15 | 2013-03-15 | |
PCT/US2014/030372 WO2014145580A1 (en) | 2013-03-15 | 2014-03-17 | Neosaxitoxin combination formulations for prolonged local anesthesia |
Publications (1)
Publication Number | Publication Date |
---|---|
MX2015012879A true MX2015012879A (es) | 2016-06-24 |
Family
ID=50549480
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2015012879A MX2015012879A (es) | 2013-03-15 | 2014-03-17 | Formulaciones combinadas de neosaxitoxina para una anestesia local prolongada. |
Country Status (26)
Country | Link |
---|---|
US (4) | US10314833B2 (es) |
EP (2) | EP3492075B1 (es) |
JP (1) | JP6313420B2 (es) |
KR (4) | KR20150131330A (es) |
CN (1) | CN105142625B (es) |
AU (2) | AU2014232881B2 (es) |
CA (2) | CA3018668C (es) |
CL (1) | CL2015002534A1 (es) |
CY (1) | CY1121606T1 (es) |
DK (1) | DK2968225T3 (es) |
ES (1) | ES2727292T3 (es) |
HK (1) | HK1218384A1 (es) |
HR (1) | HRP20190419T1 (es) |
HU (1) | HUE042711T2 (es) |
IL (1) | IL241346B (es) |
LT (1) | LT2968225T (es) |
MX (1) | MX2015012879A (es) |
NZ (1) | NZ710890A (es) |
PE (1) | PE20160011A1 (es) |
PL (2) | PL2968225T3 (es) |
PT (1) | PT2968225T (es) |
RS (1) | RS58750B1 (es) |
RU (2) | RU2015143665A (es) |
SI (1) | SI2968225T1 (es) |
TR (1) | TR201903411T4 (es) |
WO (1) | WO2014145580A1 (es) |
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JP6313420B2 (ja) * | 2013-03-15 | 2018-04-18 | ザ チルドレンズ メディカル センター コーポレイション | 持続する局所麻酔のためのネオサキシトキシン併用製剤 |
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