Incomplete Reversal of Pancuronium Neuromuscular Blockade by Neostigmine, Pyridostigmine, and Edrophonium
Three clinically used anticholinesterases—neostigmine, pyridostigmine, and edrophonium—were tested for their ability to reverse two levels (60% and 95%) of neuromuscular blockade produced by pancuronium. A controlled in vitro environment of the rat diaphragm-phrenic nerve system was used for the stu...
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| Veröffentlicht in: | Anesthesia and analgesia 1987-07, Vol.66 (7), p.594-598 |
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| container_title | Anesthesia and analgesia |
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| creator | Bartkowski, Richard R. |
| description | Three clinically used anticholinesterases—neostigmine, pyridostigmine, and edrophonium—were tested for their ability to reverse two levels (60% and 95%) of neuromuscular blockade produced by pancuronium. A controlled in vitro environment of the rat diaphragm-phrenic nerve system was used for the studies. Concentrations of anticholinesterases spanned the clinical range and were extended beyond to establish dose-response curves. Neostigmine was the most potent reversal drug (ED50 for 95% block 5.5 ± 4 nM), followed by pyridostigmine (0.27 ± 0.06 μM) and edrophonium (2.1 ± 0.05 μM). The three drugs were equally effective at reversal of block and fade as measured by train-of-four stimulation. The dose-response curves for all three drugs showed a ceiling effect for reversal of tension and fade. Supraclinical concentrations of drug did not effect complete reversal, especially at 95% block. High concentrations of anticholinesterase led to randomly appearing hyperactivity manifested by spontaneous twitching and repetitive firing with severe fade on stimulation. |
| doi_str_mv | 10.1213/00000539-198707000-00002 |
| format | Article |
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A controlled in vitro environment of the rat diaphragm-phrenic nerve system was used for the studies. Concentrations of anticholinesterases spanned the clinical range and were extended beyond to establish dose-response curves. Neostigmine was the most potent reversal drug (ED50 for 95% block 5.5 ± 4 nM), followed by pyridostigmine (0.27 ± 0.06 μM) and edrophonium (2.1 ± 0.05 μM). The three drugs were equally effective at reversal of block and fade as measured by train-of-four stimulation. The dose-response curves for all three drugs showed a ceiling effect for reversal of tension and fade. Supraclinical concentrations of drug did not effect complete reversal, especially at 95% block. High concentrations of anticholinesterase led to randomly appearing hyperactivity manifested by spontaneous twitching and repetitive firing with severe fade on stimulation.</description><identifier>ISSN: 0003-2999</identifier><identifier>EISSN: 1526-7598</identifier><identifier>DOI: 10.1213/00000539-198707000-00002</identifier><identifier>PMID: 3605668</identifier><identifier>CODEN: AACRAT</identifier><language>eng</language><publisher>Hagerstown, MD: International Anesthesia Research Society</publisher><subject>Anesthetics. Neuromuscular blocking agents ; Animals ; Biological and medical sciences ; Dose-Response Relationship, Drug ; Edrophonium - pharmacology ; Electric Stimulation ; In Vitro Techniques ; Male ; Medical sciences ; Neostigmine - pharmacology ; Nerve Block ; Neuropharmacology ; Pancuronium - antagonists & inhibitors ; Pharmacology. Drug treatments ; Phrenic Nerve - drug effects ; Pyridostigmine Bromide - pharmacology ; Rats ; Rats, Inbred Strains</subject><ispartof>Anesthesia and analgesia, 1987-07, Vol.66 (7), p.594-598</ispartof><rights>1987 International Anesthesia Research Society</rights><rights>1987 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttp://ovidsp.ovid.com/ovidweb.cgi?T=JS&NEWS=n&CSC=Y&PAGE=fulltext&D=ovft&AN=00000539-198707000-00002$$EHTML$$P50$$Gwolterskluwer$$H</linktohtml><link.rule.ids>314,776,780,4594,27903,27904,65210</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=8247026$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/3605668$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Bartkowski, Richard R.</creatorcontrib><title>Incomplete Reversal of Pancuronium Neuromuscular Blockade by Neostigmine, Pyridostigmine, and Edrophonium</title><title>Anesthesia and analgesia</title><addtitle>Anesth Analg</addtitle><description>Three clinically used anticholinesterases—neostigmine, pyridostigmine, and edrophonium—were tested for their ability to reverse two levels (60% and 95%) of neuromuscular blockade produced by pancuronium. A controlled in vitro environment of the rat diaphragm-phrenic nerve system was used for the studies. Concentrations of anticholinesterases spanned the clinical range and were extended beyond to establish dose-response curves. Neostigmine was the most potent reversal drug (ED50 for 95% block 5.5 ± 4 nM), followed by pyridostigmine (0.27 ± 0.06 μM) and edrophonium (2.1 ± 0.05 μM). The three drugs were equally effective at reversal of block and fade as measured by train-of-four stimulation. The dose-response curves for all three drugs showed a ceiling effect for reversal of tension and fade. Supraclinical concentrations of drug did not effect complete reversal, especially at 95% block. High concentrations of anticholinesterase led to randomly appearing hyperactivity manifested by spontaneous twitching and repetitive firing with severe fade on stimulation.</description><subject>Anesthetics. Neuromuscular blocking agents</subject><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Dose-Response Relationship, Drug</subject><subject>Edrophonium - pharmacology</subject><subject>Electric Stimulation</subject><subject>In Vitro Techniques</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Neostigmine - pharmacology</subject><subject>Nerve Block</subject><subject>Neuropharmacology</subject><subject>Pancuronium - antagonists & inhibitors</subject><subject>Pharmacology. Drug treatments</subject><subject>Phrenic Nerve - drug effects</subject><subject>Pyridostigmine Bromide - pharmacology</subject><subject>Rats</subject><subject>Rats, Inbred Strains</subject><issn>0003-2999</issn><issn>1526-7598</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1987</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp1kUtLxTAQhYMoen38BCELcWU1jzZplnrxBaIiui5pMvVW06YmrXL_vVEv4sbZzJw5H7M4gxCm5Jgyyk_IVxVcZVSVksgksq8NW0MzWjCRyUKV62iWVjxjSqkttB3jS5KUlGITbXJBCiHKGWqve-O7wcEI-AHeIUTtsG_wve7NFHzfTh2-hTR1UzST0wGfOW9etQVcL5Pj49g-d20PR_h-GVr7R-ve4nMb_LD4PrOLNhrtIuyt-g56ujh_nF9lN3eX1_PTm2xgJWGZAaVyagtptLWc5oo2Rua5zaXU1gCzDWM1ZZYxTWrd1IaInLCScy5qLRTwHXT4c3cI_m2COFZdGw04p3vwU6ykFJQISRK4vwKnugNbDaHtdFhWq2ySf7DydTTaNSFF0sZfrGS5JEwkLP_BPrwbU36vbvqAUC1Au3FR_fco_gmr1IWN</recordid><startdate>198707</startdate><enddate>198707</enddate><creator>Bartkowski, Richard R.</creator><general>International Anesthesia Research Society</general><general>Lippincott</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>7X8</scope></search><sort><creationdate>198707</creationdate><title>Incomplete Reversal of Pancuronium Neuromuscular Blockade by Neostigmine, Pyridostigmine, and Edrophonium</title><author>Bartkowski, Richard R.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-p2802-ce9941d57cadd31491fc744d477adce2df22b12d22a0bafbc0640283336ba69e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1987</creationdate><topic>Anesthetics. Neuromuscular blocking agents</topic><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Dose-Response Relationship, Drug</topic><topic>Edrophonium - pharmacology</topic><topic>Electric Stimulation</topic><topic>In Vitro Techniques</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Neostigmine - pharmacology</topic><topic>Nerve Block</topic><topic>Neuropharmacology</topic><topic>Pancuronium - antagonists & inhibitors</topic><topic>Pharmacology. Drug treatments</topic><topic>Phrenic Nerve - drug effects</topic><topic>Pyridostigmine Bromide - pharmacology</topic><topic>Rats</topic><topic>Rats, Inbred Strains</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Bartkowski, Richard R.</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>MEDLINE - Academic</collection><jtitle>Anesthesia and analgesia</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Bartkowski, Richard R.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Incomplete Reversal of Pancuronium Neuromuscular Blockade by Neostigmine, Pyridostigmine, and Edrophonium</atitle><jtitle>Anesthesia and analgesia</jtitle><addtitle>Anesth Analg</addtitle><date>1987-07</date><risdate>1987</risdate><volume>66</volume><issue>7</issue><spage>594</spage><epage>598</epage><pages>594-598</pages><issn>0003-2999</issn><eissn>1526-7598</eissn><coden>AACRAT</coden><abstract>Three clinically used anticholinesterases—neostigmine, pyridostigmine, and edrophonium—were tested for their ability to reverse two levels (60% and 95%) of neuromuscular blockade produced by pancuronium. A controlled in vitro environment of the rat diaphragm-phrenic nerve system was used for the studies. Concentrations of anticholinesterases spanned the clinical range and were extended beyond to establish dose-response curves. Neostigmine was the most potent reversal drug (ED50 for 95% block 5.5 ± 4 nM), followed by pyridostigmine (0.27 ± 0.06 μM) and edrophonium (2.1 ± 0.05 μM). The three drugs were equally effective at reversal of block and fade as measured by train-of-four stimulation. The dose-response curves for all three drugs showed a ceiling effect for reversal of tension and fade. Supraclinical concentrations of drug did not effect complete reversal, especially at 95% block. High concentrations of anticholinesterase led to randomly appearing hyperactivity manifested by spontaneous twitching and repetitive firing with severe fade on stimulation.</abstract><cop>Hagerstown, MD</cop><pub>International Anesthesia Research Society</pub><pmid>3605668</pmid><doi>10.1213/00000539-198707000-00002</doi><tpages>5</tpages></addata></record> |
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| ispartof | Anesthesia and analgesia, 1987-07, Vol.66 (7), p.594-598 |
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| source | MEDLINE; Journals@Ovid LWW Legacy Archive; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; Journals@Ovid Complete |
| subjects | Anesthetics. Neuromuscular blocking agents Animals Biological and medical sciences Dose-Response Relationship, Drug Edrophonium - pharmacology Electric Stimulation In Vitro Techniques Male Medical sciences Neostigmine - pharmacology Nerve Block Neuropharmacology Pancuronium - antagonists & inhibitors Pharmacology. Drug treatments Phrenic Nerve - drug effects Pyridostigmine Bromide - pharmacology Rats Rats, Inbred Strains |
| title | Incomplete Reversal of Pancuronium Neuromuscular Blockade by Neostigmine, Pyridostigmine, and Edrophonium |
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