JP2004512260A - 局所麻酔／オピオイド製剤およびその使用方法 - Google Patents
局所麻酔／オピオイド製剤およびその使用方法 Download PDFInfo
- Publication number
- JP2004512260A JP2004512260A JP2001579789A JP2001579789A JP2004512260A JP 2004512260 A JP2004512260 A JP 2004512260A JP 2001579789 A JP2001579789 A JP 2001579789A JP 2001579789 A JP2001579789 A JP 2001579789A JP 2004512260 A JP2004512260 A JP 2004512260A
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- JP
- Japan
- Prior art keywords
- administered
- morphine
- dose
- lidocaine
- topical
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
Links
- 238000000034 method Methods 0.000 title claims abstract description 40
- 238000002690 local anesthesia Methods 0.000 title claims description 8
- 238000002360 preparation method Methods 0.000 title description 2
- 239000003589 local anesthetic agent Substances 0.000 claims abstract description 67
- 230000004044 response Effects 0.000 claims abstract description 33
- 229940005483 opioid analgesics Drugs 0.000 claims abstract description 31
- 239000000203 mixture Substances 0.000 claims abstract description 29
- 230000036592 analgesia Effects 0.000 claims abstract description 28
- 238000011200 topical administration Methods 0.000 claims abstract description 20
- 230000000699 topical effect Effects 0.000 claims abstract description 20
- 230000003502 anti-nociceptive effect Effects 0.000 claims abstract description 15
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 11
- 239000012049 topical pharmaceutical composition Substances 0.000 claims abstract description 10
- 206010061218 Inflammation Diseases 0.000 claims abstract description 5
- 230000004054 inflammatory process Effects 0.000 claims abstract description 5
- BQJCRHHNABKAKU-KBQPJGBKSA-N morphine Chemical compound O([C@H]1[C@H](C=C[C@H]23)O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O BQJCRHHNABKAKU-KBQPJGBKSA-N 0.000 claims description 200
- 229960005181 morphine Drugs 0.000 claims description 100
- NNJVILVZKWQKPM-UHFFFAOYSA-N Lidocaine Chemical compound CCN(CC)CC(=O)NC1=C(C)C=CC=C1C NNJVILVZKWQKPM-UHFFFAOYSA-N 0.000 claims description 83
- 229960004194 lidocaine Drugs 0.000 claims description 82
- 230000000202 analgesic effect Effects 0.000 claims description 27
- BLFLLBZGZJTVJG-UHFFFAOYSA-N benzocaine Chemical compound CCOC(=O)C1=CC=C(N)C=C1 BLFLLBZGZJTVJG-UHFFFAOYSA-N 0.000 claims description 24
- JAQUASYNZVUNQP-USXIJHARSA-N Levorphanol Chemical compound C1C2=CC=C(O)C=C2[C@]23CCN(C)[C@H]1[C@@H]2CCCC3 JAQUASYNZVUNQP-USXIJHARSA-N 0.000 claims description 22
- OROGSEYTTFOCAN-DNJOTXNNSA-N codeine Chemical compound C([C@H]1[C@H](N(CC[C@@]112)C)C3)=C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OC OROGSEYTTFOCAN-DNJOTXNNSA-N 0.000 claims description 22
- 229960003406 levorphanol Drugs 0.000 claims description 22
- 229960001736 buprenorphine Drugs 0.000 claims description 21
- RMRJXGBAOAMLHD-IHFGGWKQSA-N buprenorphine Chemical compound C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]11CC[C@]3([C@H](C1)[C@](C)(O)C(C)(C)C)OC)CN2CC1CC1 RMRJXGBAOAMLHD-IHFGGWKQSA-N 0.000 claims description 21
- -1 safentanil Chemical compound 0.000 claims description 15
- 108010092674 Enkephalins Proteins 0.000 claims description 14
- URLZCHNOLZSCCA-VABKMULXSA-N Leu-enkephalin Chemical class C([C@@H](C(=O)N[C@@H](CC(C)C)C(O)=O)NC(=O)CNC(=O)CNC(=O)[C@@H](N)CC=1C=CC(O)=CC=1)C1=CC=CC=C1 URLZCHNOLZSCCA-VABKMULXSA-N 0.000 claims description 14
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims description 12
- 229960005274 benzocaine Drugs 0.000 claims description 12
- 239000003703 n methyl dextro aspartic acid receptor blocking agent Substances 0.000 claims description 12
- 229960004126 codeine Drugs 0.000 claims description 11
- OROGSEYTTFOCAN-UHFFFAOYSA-N hydrocodone Natural products C1C(N(CCC234)C)C2C=CC(O)C3OC2=C4C1=CC=C2OC OROGSEYTTFOCAN-UHFFFAOYSA-N 0.000 claims description 11
- 229940099433 NMDA receptor antagonist Drugs 0.000 claims description 10
- 150000001875 compounds Chemical class 0.000 claims description 9
- 229940127240 opiate Drugs 0.000 claims description 9
- USSIQXCVUWKGNF-UHFFFAOYSA-N 6-(dimethylamino)-4,4-diphenylheptan-3-one Chemical compound C=1C=CC=CC=1C(CC(C)N(C)C)(C(=O)CC)C1=CC=CC=C1 USSIQXCVUWKGNF-UHFFFAOYSA-N 0.000 claims description 8
- 210000001508 eye Anatomy 0.000 claims description 8
- 229960001797 methadone Drugs 0.000 claims description 8
- 210000004400 mucous membrane Anatomy 0.000 claims description 8
- QNAYBMKLOCPYGJ-UWTATZPHSA-N D-alanine Chemical compound C[C@@H](N)C(O)=O QNAYBMKLOCPYGJ-UWTATZPHSA-N 0.000 claims description 7
- MCMMCRYPQBNCPH-WMIMKTLMSA-N DPDPE Chemical compound C([C@H](N)C(=O)N[C@@H]1C(C)(C)SSC([C@@H](NC(=O)[C@H](CC=2C=CC=CC=2)NC(=O)CNC1=O)C(O)=O)(C)C)C1=CC=C(O)C=C1 MCMMCRYPQBNCPH-WMIMKTLMSA-N 0.000 claims description 7
- PKSODCLCMBUCPW-LVNBQDLPSA-N DSLET Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)NC(=O)CNC(=O)[C@@H](CO)NC(=O)[C@@H](N)CC=1C=CC(O)=CC=1)C1=CC=CC=C1 PKSODCLCMBUCPW-LVNBQDLPSA-N 0.000 claims description 7
- 108010065372 Dynorphins Proteins 0.000 claims description 7
- SCIFESDRCALIIM-VIFPVBQESA-N N-methyl-L-phenylalanine Chemical compound C[NH2+][C@H](C([O-])=O)CC1=CC=CC=C1 SCIFESDRCALIIM-VIFPVBQESA-N 0.000 claims description 7
- 108010093625 Opioid Peptides Proteins 0.000 claims description 7
- 102000001490 Opioid Peptides Human genes 0.000 claims description 7
- JMNJYGMAUMANNW-FIXZTSJVSA-N dynorphin a Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(O)=O)NC(=O)CNC(=O)CNC(=O)[C@@H](N)CC=1C=CC(O)=CC=1)C1=CC=CC=C1 JMNJYGMAUMANNW-FIXZTSJVSA-N 0.000 claims description 7
- 229960002428 fentanyl Drugs 0.000 claims description 7
- IVLVTNPOHDFFCJ-UHFFFAOYSA-N fentanyl citrate Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O.C=1C=CC=CC=1N(C(=O)CC)C(CC1)CCN1CCC1=CC=CC=C1 IVLVTNPOHDFFCJ-UHFFFAOYSA-N 0.000 claims description 7
- 229960000805 nalbuphine Drugs 0.000 claims description 7
- NETZHAKZCGBWSS-CEDHKZHLSA-N nalbuphine Chemical compound C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]1(O)CC[C@@H]3O)CN2CC1CCC1 NETZHAKZCGBWSS-CEDHKZHLSA-N 0.000 claims description 7
- 239000003399 opiate peptide Substances 0.000 claims description 7
- 101800005049 Beta-endorphin Proteins 0.000 claims description 6
- 102400000748 Beta-endorphin Human genes 0.000 claims description 6
- 102400000242 Dynorphin A(1-17) Human genes 0.000 claims description 6
- 108010049140 Endorphins Proteins 0.000 claims description 6
- 102000009025 Endorphins Human genes 0.000 claims description 6
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 6
- 230000001154 acute effect Effects 0.000 claims description 6
- WOPZMFQRCBYPJU-NTXHZHDSSA-N beta-endorphin Chemical compound C([C@@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H]1N(CCC1)C(=O)[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)CC=1C=CC(O)=CC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C1=CC=CC=C1 WOPZMFQRCBYPJU-NTXHZHDSSA-N 0.000 claims description 6
- CAHCBJPUTCKATP-FAWZKKEFSA-N etorphine Chemical compound O([C@H]1[C@@]2(OC)C=C[C@@]34C[C@@H]2[C@](C)(O)CCC)C2=C5[C@]41CCN(C)[C@@H]3CC5=CC=C2O CAHCBJPUTCKATP-FAWZKKEFSA-N 0.000 claims description 6
- 229950004155 etorphine Drugs 0.000 claims description 6
- AKXCFAYOTIEFOH-XTNAHFASSA-N n-[(e)-[(4r,4as,7ar,12bs)-4a,9-dihydroxy-3-prop-2-enyl-2,4,5,6,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinoline-7-ylidene]amino]benzamide Chemical compound C1(/[C@H]2[C@]34CCN(CC=C)[C@@H]([C@@]4(CC1)O)CC1=CC=C(C(O2)=C13)O)=N\NC(=O)C1=CC=CC=C1 AKXCFAYOTIEFOH-XTNAHFASSA-N 0.000 claims description 6
- 229960003981 proparacaine Drugs 0.000 claims description 6
- MMXZSJMASHPLLR-UHFFFAOYSA-N pyrroloquinoline quinone Chemical compound C12=C(C(O)=O)C=C(C(O)=O)N=C2C(=O)C(=O)C2=C1NC(C(=O)O)=C2 MMXZSJMASHPLLR-UHFFFAOYSA-N 0.000 claims description 6
- 150000003839 salts Chemical class 0.000 claims description 6
- 239000008009 topical excipient Substances 0.000 claims description 6
- AGTSSZRZBSNTGQ-ITZCFHCWSA-N (2s,3r)-2-[[(2s)-2-[[(2s)-2-[[(2s)-6-amino-2-[[(2s)-2-[[(2s)-5-amino-2-[[(2s)-2-[[(2s)-2-[[(2s)-2-[[(2s)-2-[[2-[[2-[[(2s)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomet Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)NC(=O)CNC(=O)CNC(=O)[C@@H](N)CC=1C=CC(O)=CC=1)C1=CC=CC=C1 AGTSSZRZBSNTGQ-ITZCFHCWSA-N 0.000 claims description 5
- HPZJMUBDEAMBFI-WTNAPCKOSA-N (D-Ala(2)-mephe(4)-gly-ol(5))enkephalin Chemical compound C([C@H](N)C(=O)N[C@H](C)C(=O)NCC(=O)N(C)[C@@H](CC=1C=CC=CC=1)C(=O)NCCO)C1=CC=C(O)C=C1 HPZJMUBDEAMBFI-WTNAPCKOSA-N 0.000 claims description 5
- 108700022183 Ala(2)-MePhe(4)-Gly(5)- Enkephalin Proteins 0.000 claims description 5
- MKXZASYAUGDDCJ-SZMVWBNQSA-N LSM-2525 Chemical group C1CCC[C@H]2[C@@]3([H])N(C)CC[C@]21C1=CC(OC)=CC=C1C3 MKXZASYAUGDDCJ-SZMVWBNQSA-N 0.000 claims description 5
- SYCBXBCPLUFJID-UHFFFAOYSA-N Pramoxine hydrochloride Chemical compound Cl.C1=CC(OCCCC)=CC=C1OCCCN1CCOCC1 SYCBXBCPLUFJID-UHFFFAOYSA-N 0.000 claims description 5
- KCLANYCVBBTKTO-UHFFFAOYSA-N Proparacaine Chemical compound CCCOC1=CC=C(C(=O)OCCN(CC)CC)C=C1N KCLANYCVBBTKTO-UHFFFAOYSA-N 0.000 claims description 5
- 101800001440 Rimorphin Proteins 0.000 claims description 5
- 102400000235 Rimorphin Human genes 0.000 claims description 5
- IFKLAQQSCNILHL-QHAWAJNXSA-N butorphanol Chemical compound N1([C@@H]2CC3=CC=C(C=C3[C@@]3([C@]2(CCCC3)O)CC1)O)CC1CCC1 IFKLAQQSCNILHL-QHAWAJNXSA-N 0.000 claims description 5
- 229960001113 butorphanol Drugs 0.000 claims description 5
- 230000001684 chronic effect Effects 0.000 claims description 5
- 229960001747 cinchocaine Drugs 0.000 claims description 5
- PUFQVTATUTYEAL-UHFFFAOYSA-N cinchocaine Chemical compound C1=CC=CC2=NC(OCCCC)=CC(C(=O)NCCN(CC)CC)=C21 PUFQVTATUTYEAL-UHFFFAOYSA-N 0.000 claims description 5
- 229960001985 dextromethorphan Drugs 0.000 claims description 5
- VOKSWYLNZZRQPF-GDIGMMSISA-N pentazocine Chemical compound C1C2=CC=C(O)C=C2[C@@]2(C)[C@@H](C)[C@@H]1N(CC=C(C)C)CC2 VOKSWYLNZZRQPF-GDIGMMSISA-N 0.000 claims description 5
- 229960005301 pentazocine Drugs 0.000 claims description 5
- 229940019974 pramoxine hydrochloride Drugs 0.000 claims description 5
- MFDFERRIHVXMIY-UHFFFAOYSA-N procaine Chemical compound CCN(CC)CCOC(=O)C1=CC=C(N)C=C1 MFDFERRIHVXMIY-UHFFFAOYSA-N 0.000 claims description 5
- 229960004919 procaine Drugs 0.000 claims description 5
- 229960002372 tetracaine Drugs 0.000 claims description 5
- GKCBAIGFKIBETG-UHFFFAOYSA-N tetracaine Chemical compound CCCCNC1=CC=C(C(=O)OCCN(C)C)C=C1 GKCBAIGFKIBETG-UHFFFAOYSA-N 0.000 claims description 5
- 102400000237 Alpha-neoendorphin Human genes 0.000 claims description 4
- 101800001617 Alpha-neoendorphin Proteins 0.000 claims description 4
- 108700022182 D-Penicillamine (2,5)- Enkephalin Proteins 0.000 claims description 4
- YQEZLKZALYSWHR-UHFFFAOYSA-N Ketamine Chemical compound C=1C=CC=C(Cl)C=1C1(NC)CCCCC1=O YQEZLKZALYSWHR-UHFFFAOYSA-N 0.000 claims description 4
- UIQMVEYFGZJHCZ-SSTWWWIQSA-N Nalorphine Chemical compound C([C@@H](N(CC1)CC=C)[C@@H]2C=C[C@@H]3O)C4=CC=C(O)C5=C4[C@@]21[C@H]3O5 UIQMVEYFGZJHCZ-SSTWWWIQSA-N 0.000 claims description 4
- 108700019895 Thr(6)- Leu(5) Ser(2) enkephalin Proteins 0.000 claims description 4
- 229960004193 dextropropoxyphene Drugs 0.000 claims description 4
- XLMALTXPSGQGBX-GCJKJVERSA-N dextropropoxyphene Chemical compound C([C@](OC(=O)CC)([C@H](C)CN(C)C)C=1C=CC=CC=1)C1=CC=CC=C1 XLMALTXPSGQGBX-GCJKJVERSA-N 0.000 claims description 4
- LBOJYSIDWZQNJS-CVEARBPZSA-N dizocilpine Chemical compound C12=CC=CC=C2[C@]2(C)C3=CC=CC=C3C[C@H]1N2 LBOJYSIDWZQNJS-CVEARBPZSA-N 0.000 claims description 4
- 229960003299 ketamine Drugs 0.000 claims description 4
- 229960000938 nalorphine Drugs 0.000 claims description 4
- DKJCUVXSBOMWAV-PCWWUVHHSA-N naltrindole Chemical compound N1([C@H]2CC3=CC=C(C=4O[C@@H]5[C@](C3=4)([C@]2(CC2=C3[CH]C=CC=C3N=C25)O)CC1)O)CC1CC1 DKJCUVXSBOMWAV-PCWWUVHHSA-N 0.000 claims description 4
- KZTDMJBCZSGHOG-XJIZABAQSA-N α-neoendorphin Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCCN)C(O)=O)NC(=O)CNC(=O)CNC(=O)[C@@H](N)CC=1C=CC(O)=CC=1)C1=CC=CC=C1 KZTDMJBCZSGHOG-XJIZABAQSA-N 0.000 claims description 4
- ZKMNUMMKYBVTFN-HNNXBMFYSA-N (S)-ropivacaine Chemical compound CCCN1CCCC[C@H]1C(=O)NC1=C(C)C=CC=C1C ZKMNUMMKYBVTFN-HNNXBMFYSA-N 0.000 claims description 3
- 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 claims description 3
- IJVCSMSMFSCRME-UHFFFAOYSA-N 3-methyl-2,4,4a,5,6,7,7a,13-octahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinoline-7,9-diol Chemical compound C12CCC(O)C3OC4=C5C32CCN(C)C1CC5=CC=C4O IJVCSMSMFSCRME-UHFFFAOYSA-N 0.000 claims description 3
- 101800005209 Deltorphin Proteins 0.000 claims description 3
- BHSURCCZOBVHJJ-NWOHMYAQSA-N Deltorphin A Chemical compound C([C@H](N)C(=O)N[C@H](CCSC)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(O)=O)C(N)=O)C1=CC=C(O)C=C1 BHSURCCZOBVHJJ-NWOHMYAQSA-N 0.000 claims description 3
- OGDVEMNWJVYAJL-LEPYJNQMSA-N Ethyl morphine Chemical compound C([C@H]1[C@H](N(CC[C@@]112)C)C3)=C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OCC OGDVEMNWJVYAJL-LEPYJNQMSA-N 0.000 claims description 3
- OGDVEMNWJVYAJL-UHFFFAOYSA-N Ethylmorphine Natural products C1C(N(CCC234)C)C2C=CC(O)C3OC2=C4C1=CC=C2OCC OGDVEMNWJVYAJL-UHFFFAOYSA-N 0.000 claims description 3
- VTUSIVBDOCDNHS-UHFFFAOYSA-N Etidocaine Chemical compound CCCN(CC)C(CC)C(=O)NC1=C(C)C=CC=C1C VTUSIVBDOCDNHS-UHFFFAOYSA-N 0.000 claims description 3
- GNJCUHZOSOYIEC-GAROZEBRSA-N Morphine-6-glucuronide Chemical compound O([C@H]1C=C[C@H]2[C@H]3CC=4C5=C(C(=CC=4)O)O[C@@H]1[C@]52CCN3C)[C@@H]1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O GNJCUHZOSOYIEC-GAROZEBRSA-N 0.000 claims description 3
- BRUQQQPBMZOVGD-XFKAJCMBSA-N Oxycodone Chemical compound O=C([C@@H]1O2)CC[C@@]3(O)[C@H]4CC5=CC=C(OC)C2=C5[C@@]13CCN4C BRUQQQPBMZOVGD-XFKAJCMBSA-N 0.000 claims description 3
- UQCNKQCJZOAFTQ-ISWURRPUSA-N Oxymorphone Chemical compound O([C@H]1C(CC[C@]23O)=O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O UQCNKQCJZOAFTQ-ISWURRPUSA-N 0.000 claims description 3
- ZDXGFIXMPOUDFF-XLIONFOSSA-N bremazocine Chemical compound C([C@]1(C2=CC(O)=CC=C2C[C@@H]2C1(C)C)CC)CN2CC1(O)CC1 ZDXGFIXMPOUDFF-XLIONFOSSA-N 0.000 claims description 3
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- VDANGULDQQJODZ-UHFFFAOYSA-N chloroprocaine Chemical compound CCN(CC)CCOC(=O)C1=CC=C(N)C=C1Cl VDANGULDQQJODZ-UHFFFAOYSA-N 0.000 claims description 3
- 229960004578 ethylmorphine Drugs 0.000 claims description 3
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- IMYHGORQCPYVBZ-NLFFAJNJSA-N lofentanil Chemical compound CCC(=O)N([C@@]1([C@@H](CN(CCC=2C=CC=CC=2)CC1)C)C(=O)OC)C1=CC=CC=C1 IMYHGORQCPYVBZ-NLFFAJNJSA-N 0.000 claims description 3
- 229950010274 lofentanil Drugs 0.000 claims description 3
- BUGYDGFZZOZRHP-UHFFFAOYSA-N memantine Chemical compound C1C(C2)CC3(C)CC1(C)CC2(N)C3 BUGYDGFZZOZRHP-UHFFFAOYSA-N 0.000 claims description 3
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- 229960002409 mepivacaine Drugs 0.000 claims description 3
- INWLQCZOYSRPNW-UHFFFAOYSA-N mepivacaine Chemical compound CN1CCCCC1C(=O)NC1=C(C)C=CC=C1C INWLQCZOYSRPNW-UHFFFAOYSA-N 0.000 claims description 3
- 229960002085 oxycodone Drugs 0.000 claims description 3
- 229960001807 prilocaine Drugs 0.000 claims description 3
- MVFGUOIZUNYYSO-UHFFFAOYSA-N prilocaine Chemical compound CCCNC(C)C(=O)NC1=CC=CC=C1C MVFGUOIZUNYYSO-UHFFFAOYSA-N 0.000 claims description 3
- 229960001549 ropivacaine Drugs 0.000 claims description 3
- 239000003860 topical agent Substances 0.000 claims description 3
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US20043700P | 2000-04-28 | 2000-04-28 | |
| PCT/US2001/013546 WO2001082914A2 (en) | 2000-04-28 | 2001-04-27 | Topical anesthetic/opioid formulations and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004512260A true JP2004512260A (ja) | 2004-04-22 |
| JP2004512260A5 JP2004512260A5 (enExample) | 2008-06-19 |
Family
ID=22741721
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001579789A Abandoned JP2004512260A (ja) | 2000-04-28 | 2001-04-27 | 局所麻酔／オピオイド製剤およびその使用方法 |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US6825203B2 (enExample) |
| EP (1) | EP1276475A2 (enExample) |
| JP (1) | JP2004512260A (enExample) |
| KR (1) | KR20030060771A (enExample) |
| AU (1) | AU2001257326A1 (enExample) |
| CA (1) | CA2407683C (enExample) |
| IL (1) | IL152473A0 (enExample) |
| WO (1) | WO2001082914A2 (enExample) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2003081872A (ja) * | 2001-09-13 | 2003-03-19 | Nippon Oruganon Kk | 掻痒治療薬 |
| WO2009063897A1 (ja) * | 2007-11-14 | 2009-05-22 | Kyowa Hakko Bio Co., Ltd. | 皮膚の乾癬予防または改善剤 |
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| BR9912827A (pt) * | 1998-07-16 | 2001-05-02 | Sloan Kettering Inst Cancer | Composições tópicas compreendendo um analgésico opióide e um antagonista de nmda |
| KR20020001797A (ko) | 1999-03-23 | 2002-01-09 | 제임스 쿡 유니버시티 | 신체 기관의 정지, 보호 및 보존 |
| ES2357808T3 (es) * | 2001-06-07 | 2011-04-29 | Christine Dr. Sang | Tratamiento del dolor neuropático con antagonistas del receptor de n-metil-d-aspartato (nmda). |
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| US7147656B2 (en) | 2001-12-03 | 2006-12-12 | Xtent, Inc. | Apparatus and methods for delivery of braided prostheses |
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| EP1595541A1 (en) * | 2004-05-12 | 2005-11-16 | Alcasynn Pharmaceuticals Gmbh | Use of opioid receptor antagonist compounds for the prevention and/or treatment of diseases associated with the target calcineurin |
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| EP1702627A1 (en) * | 2005-03-18 | 2006-09-20 | Laboratorios Del Dr. Esteve, S.A. | Analgesic combination of sodium channel blockers with opioid antagonists |
| EP1928484B1 (en) * | 2005-08-26 | 2010-02-24 | The Board Of Trustees Of The Leland Stanford Junior University | Methods for treatment of headaches by administration of oxytocin |
| US20070093517A1 (en) * | 2005-10-24 | 2007-04-26 | Gary Newton | Local anesthetic compositions |
| JP2009527497A (ja) | 2006-02-17 | 2009-07-30 | ネイサン・ディー・ザスラー | 神経原性振戦を調節するための局所麻酔剤の新規適用 |
| AU2007227000A1 (en) | 2006-03-20 | 2007-09-27 | Xtent, Inc. | Apparatus and methods for deployment of linked prosthetic segments |
| KR101425579B1 (ko) | 2006-05-29 | 2014-08-13 | 하이버네이션 테라퓨틱스 리미티드 | 개선된 조직 유지법 |
| ES2539762T3 (es) | 2006-07-25 | 2015-07-03 | Hibernation Therapeutics, A Kf Llc | Tratamiento de traumatismos |
| TW200815004A (en) * | 2006-09-19 | 2008-04-01 | Chi Mei Foundation Hospital | Local anesthetic composition containing dextrorotatory morphinan derivative or pharmaceutically acceptable salts thereof |
| US20080220062A1 (en) * | 2006-10-23 | 2008-09-11 | Psivida, Inc. | Sustained release of agents for localized pain management |
| EP2117521B1 (en) * | 2006-11-03 | 2012-06-27 | Durect Corporation | Transdermal delivery systems comprising bupivacaine |
| US20080199510A1 (en) | 2007-02-20 | 2008-08-21 | Xtent, Inc. | Thermo-mechanically controlled implants and methods of use |
| CA2717162A1 (en) | 2007-03-02 | 2008-09-12 | Hibernation Therapeutics Limited | Transplants |
| US8486132B2 (en) | 2007-03-22 | 2013-07-16 | J.W. Medical Systems Ltd. | Devices and methods for controlling expandable prostheses during deployment |
| US8217141B2 (en) | 2007-05-17 | 2012-07-10 | Neopro Labs, Llc | Crystalline and amorphous forms of peptide |
| US20090036541A1 (en) * | 2007-08-02 | 2009-02-05 | Donald David Mardis | Applicator and chemical combination for better topical anesthesia |
| US9101503B2 (en) | 2008-03-06 | 2015-08-11 | J.W. Medical Systems Ltd. | Apparatus having variable strut length and methods of use |
| GB0808751D0 (en) * | 2008-05-14 | 2008-06-18 | Serentis Ltd | Topical compositions of opioid compound for use in wound healing |
| US8979917B2 (en) | 2008-09-25 | 2015-03-17 | Advanced Bifurcation Systems, Inc. | System and methods for treating a bifurcation |
| WO2010036982A1 (en) | 2008-09-25 | 2010-04-01 | Henry Bourang | Partially crimped stent |
| US8821562B2 (en) | 2008-09-25 | 2014-09-02 | Advanced Bifurcation Systems, Inc. | Partially crimped stent |
| US12324756B2 (en) | 2008-09-25 | 2025-06-10 | Advanced Bifurcation Systems Inc. | System and methods for treating a bifurcation |
| US8795347B2 (en) | 2008-09-25 | 2014-08-05 | Advanced Bifurcation Systems, Inc. | Methods and systems for treating a bifurcation with provisional side branch stenting |
| US8769796B2 (en) | 2008-09-25 | 2014-07-08 | Advanced Bifurcation Systems, Inc. | Selective stent crimping |
| US12076258B2 (en) | 2008-09-25 | 2024-09-03 | Advanced Bifurcation Systems Inc. | Selective stent crimping |
| US11298252B2 (en) | 2008-09-25 | 2022-04-12 | Advanced Bifurcation Systems Inc. | Stent alignment during treatment of a bifurcation |
| AU2011232361B2 (en) | 2010-03-24 | 2015-05-28 | Advanced Bifurcation Systems Inc. | Stent alignment during treatment of a bifurcation |
| EP2672932B1 (en) | 2011-02-08 | 2018-09-19 | Advanced Bifurcation Systems, Inc. | System for treating a bifurcation with a fully crimped stent |
| WO2012109382A2 (en) | 2011-02-08 | 2012-08-16 | Advanced Bifurcation Systems, Inc. | Multi-stent and multi-balloon apparatus for treating bifurcations and methods of use |
| CA2860373C (en) | 2011-04-29 | 2017-08-15 | Moberg Pharma Ab | Pharmaceutical compositions comprising a local anaesthetic such as bupivacaine for local administration to the mouth or throat |
| ES3034911T3 (en) | 2011-05-10 | 2025-08-26 | Itochu Chemical Frontier Corp | Non-aqueous patch |
| US11786455B2 (en) | 2011-05-10 | 2023-10-17 | Itochu Chemical Frontier Corporation | Non-aqueous patch |
| WO2012153396A1 (ja) | 2011-05-10 | 2012-11-15 | 伊藤忠ケミカルフロンティア株式会社 | 非水性貼付剤 |
| MX367430B (es) | 2011-09-27 | 2019-07-11 | Itochu Chemical Frontier Corp | Parche no acuoso. |
| AU2013201465B2 (en) | 2012-10-24 | 2016-03-03 | Rayner Intraocular Lenses Limited | Stable preservative-free mydriatic and anti-inflammatory solutions for injection |
| BR112016000804A2 (pt) | 2013-07-17 | 2017-08-22 | Hibernation Therapeuitics A Kf Llc | Método para tratar hemorragia, choque e lesão cerebral |
| TWI809304B (zh) | 2014-12-01 | 2023-07-21 | 奥默羅斯公司 | 用於抑制術後眼睛炎性病況的抗炎和散瞳前房溶液 |
| JP7030517B2 (ja) | 2015-01-07 | 2022-03-07 | トライジェミナ， インコーポレイテッド | マグネシウム含有オキシトシン製剤および使用の方法 |
| CN115814055A (zh) | 2016-04-12 | 2023-03-21 | 三叉神经股份公司 | 含镁催产素制剂和应用方法 |
| US11160799B2 (en) | 2019-10-22 | 2021-11-02 | Cessatech A/S | Pediatric combination |
| CN115135317A (zh) | 2020-01-22 | 2022-09-30 | 西洛斯治疗有限公司 | 减少nmda拮抗剂的副作用 |
| CN114373519A (zh) * | 2021-12-31 | 2022-04-19 | 苏州佩德生物医药有限公司 | 一种trpv3抑制剂的虚拟筛选方法、药物先导化合物及应用 |
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| US4446140A (en) | 1981-12-10 | 1984-05-01 | Nelson Research & Development Company | Method and composition for treating mouth pain |
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| DE4223004A1 (de) | 1992-07-13 | 1994-01-20 | Liedtke Pharmed Gmbh | Einzeldosierte halbfeste topische Arzneiform zur Transdermaltherapie |
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| US5321012A (en) | 1993-01-28 | 1994-06-14 | Virginia Commonwealth University Medical College | Inhibiting the development of tolerance to and/or dependence on a narcotic addictive substance |
| US5523323A (en) | 1993-09-14 | 1996-06-04 | Maccecchini; Maria-Luisa | Use of partial agonists of the NMDA receptor to reduce opiate induced tolerance and dependence |
| US5635204A (en) | 1994-03-04 | 1997-06-03 | Montefiore Medical Center | Method for transdermal induction of anesthesia, analgesia or sedation |
| US5589480A (en) | 1994-08-17 | 1996-12-31 | Elkhoury; George F. | Topical application of opioid analgesic drugs such as morphine |
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| ATE214272T1 (de) | 1996-12-16 | 2002-03-15 | Alcon Lab Inc | Topische verwendung von kappa- opioidrezeptoragonisten zur behandlung von augenschmerz |
| US6008258A (en) | 1997-01-22 | 1999-12-28 | Cornell Research Foundation, Inc. | d-methadone, a nonopioid analegesic |
| US5834480A (en) | 1997-06-13 | 1998-11-10 | Elkhoury; George F. | Topical application of opioids for treatment of acne and sebaceous gland disorders |
| BR9912827A (pt) | 1998-07-16 | 2001-05-02 | Sloan Kettering Inst Cancer | Composições tópicas compreendendo um analgésico opióide e um antagonista de nmda |
| JP2000169378A (ja) * | 1998-12-10 | 2000-06-20 | Taisho Pharmaceut Co Ltd | 咽頭疾患用組成物 |
| US6383511B1 (en) * | 1999-10-25 | 2002-05-07 | Epicept Corporation | Local prevention or amelioration of pain from surgically closed wounds |
-
2001
- 2001-04-27 AU AU2001257326A patent/AU2001257326A1/en not_active Abandoned
- 2001-04-27 CA CA2407683A patent/CA2407683C/en not_active Expired - Fee Related
- 2001-04-27 IL IL15247301A patent/IL152473A0/xx unknown
- 2001-04-27 US US09/844,111 patent/US6825203B2/en not_active Expired - Lifetime
- 2001-04-27 JP JP2001579789A patent/JP2004512260A/ja not_active Abandoned
- 2001-04-27 WO PCT/US2001/013546 patent/WO2001082914A2/en not_active Ceased
- 2001-04-27 KR KR1020027014500A patent/KR20030060771A/ko not_active Ceased
- 2001-04-27 EP EP01930827A patent/EP1276475A2/en not_active Withdrawn
- 2001-10-11 US US09/975,812 patent/US6790855B2/en not_active Expired - Lifetime
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2003081872A (ja) * | 2001-09-13 | 2003-03-19 | Nippon Oruganon Kk | 掻痒治療薬 |
| WO2009063897A1 (ja) * | 2007-11-14 | 2009-05-22 | Kyowa Hakko Bio Co., Ltd. | 皮膚の乾癬予防または改善剤 |
| US8575190B2 (en) | 2007-11-14 | 2013-11-05 | Mitsubishi Gas Chemical Company, Inc. | Method of preventing or ameliorating psoriasis using pyrroloquinoline quinone compounds |
| JP5392089B2 (ja) * | 2007-11-14 | 2014-01-22 | 三菱瓦斯化学株式会社 | 皮膚の乾癬予防または改善剤 |
Also Published As
| Publication number | Publication date |
|---|---|
| EP1276475A2 (en) | 2003-01-22 |
| US20020004484A1 (en) | 2002-01-10 |
| CA2407683C (en) | 2010-04-13 |
| US6825203B2 (en) | 2004-11-30 |
| AU2001257326A1 (en) | 2001-11-12 |
| WO2001082914A2 (en) | 2001-11-08 |
| KR20030060771A (ko) | 2003-07-16 |
| US6790855B2 (en) | 2004-09-14 |
| US20020052319A1 (en) | 2002-05-02 |
| CA2407683A1 (en) | 2001-11-08 |
| IL152473A0 (en) | 2003-05-29 |
| WO2001082914A3 (en) | 2002-08-01 |
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