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词条 Tetracaine
释义

  1. Medical uses

  2. Mechanism

  3. References

{{Drugbox
| verifiedrevid = 470603479
| IUPAC_name = 2-(dimethylamino)ethyl 4-(butylamino)benzoate
| image = Tetracaine2DCSD.svg
| tradename = Pontocaine, Ametop, Dicaine, others
| Drugs.com = {{drugs.com|monograph|tetracaine}}
| MedlinePlus = a682640
| pregnancy_AU =
| pregnancy_US =
| pregnancy_category =
| legal_AU =
| legal_CA =
| legal_UK =
| legal_US =
| legal_status = Rx Only
| routes_of_administration = topical
| bioavailability =
| protein_bound = 75.6
| metabolism =
| elimination_half-life =
| excretion =
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 94-24-6
| CAS_supplemental =
{{CAS|136-47-0}} (hydrochloride)
| ATC_prefix = C05
| ATC_suffix = AD02
| ATC_supplemental = {{ATC|D04|AB06}} {{ATC|N01|BA03}} {{ATC|S01|HA03}}
| PubChem = 5411
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank = DB09085
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 5218
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 0619F35CGV
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D00551
| ChEBI_Ref = {{ebicite|correct|EBI}}
| ChEBI = 9468
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 698
| PDB_ligand = TE4
| C=15 | H=24 | N=2 | O=2
| molecular_weight = 264.363 g/mol
| smiles = O=C(OCCN(C)C)c1ccc(NCCCC)cc1
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 1S/C15H24N2O2/c1-4-5-10-16-14-8-6-13(7-9-14)15(18)19-12-11-17(2)3/h6-9,16H,4-5,10-12H2,1-3H3
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = GKCBAIGFKIBETG-UHFFFAOYSA-N
}}Tetracaine, also known as amethocaine, is a local anesthetic used to numb the eyes, nose, or throat.[1] It may also be used before starting an intravenous to decrease pain from the procedure.[1] Typically it is applied as a liquid to the area.[1] Onset of effects when used in the eyes is within 30 seconds and last for less than 15 minutes.[2]

Common side effects include a brief period of burning at the site of use.[2] Allergic reactions may uncommonly occur.[6] Long term use is generally not recommended as it may slow healing of the eye.[2] It is unclear if use during pregnancy is safe for the baby.[2] Tetracaine is in the ester-type local anesthetic family of medications.[3] It works by blocking the sending of nerve impulses.[2]

Tetracaine was patented in 1930 and came into medical use in 1941.[4] It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.[5] The wholesale cost in the developing world is about US$1.34–1.63 per 10 ml bottle.[6] In the United Kingdom the eye drops cost the NHS about 0.49 pounds per dose.[1]

Medical uses

A systematic review investigated tetracaine for use in emergency departments, especially for starting intravenous lines in children, in view of its analgesic and cost-saving properties. However, it did not find an improvement in first-attempt cannulations.[7]

Tetracaine is the T in TAC, a mixture of 5 to 12% tetracaine, 0.05% adrenaline, and 4 or 10% cocaine hydrochloride used in ear, nose, and throat surgery and in the emergency department where numbing of the surface is needed rapidly, especially when children have been injured in the eye, ear, or other sensitive locations.[8]

Mechanism

In biomedical research, tetracaine is used to alter the function of calcium release channels (ryanodine receptors) that control the release of calcium from intracellular stores. Tetracaine is an allosteric blocker of channel function. At low concentrations, tetracaine causes an initial inhibition of spontaneous calcium release events, while at high concentrations, tetracaine blocks release completely.[9]

References

1. ^{{cite book|title=British national formulary : BNF 69|date=2015|publisher=British Medical Association|isbn=9780857111562|pages=769, 897|edition=69}}
2. ^{{cite web|title=Tetracaine|url=https://www.drugs.com/monograph/tetracaine.html|publisher=The American Society of Health-System Pharmacists|accessdate=8 December 2016|deadurl=no|archiveurl=https://web.archive.org/web/20161228195913/https://www.drugs.com/monograph/tetracaine.html|archivedate=28 December 2016|df=}}
3. ^{{cite book|title=WHO Model Formulary 2008|date=2009|publisher=World Health Organization|isbn=9789241547659|page=437|url=http://apps.who.int/medicinedocs/documents/s16879e/s16879e.pdf|accessdate=8 December 2016|deadurl=no|archiveurl=https://web.archive.org/web/20161213060118/http://apps.who.int/medicinedocs/documents/s16879e/s16879e.pdf|archivedate=13 December 2016|df=}}
4. ^{{cite book|last1=Fischer|first1=Janos|last2=Ganellin|first2=C. Robin|title=Analogue-based Drug Discovery|date=2006|publisher=John Wiley & Sons|isbn=9783527607495|page=475|url=https://books.google.ca/books?id=FjKfqkaKkAAC&pg=PA475|language=en|deadurl=no|archiveurl=https://web.archive.org/web/20161229100237/https://books.google.ca/books?id=FjKfqkaKkAAC&pg=PA475|archivedate=2016-12-29|df=}}
5. ^{{cite web|title=WHO Model List of Essential Medicines (19th List)|url=http://www.who.int/medicines/publications/essentialmedicines/EML_2015_FINAL_amended_NOV2015.pdf?ua=1|work=World Health Organization|accessdate=8 December 2016|date=April 2015|deadurl=no|archiveurl=https://web.archive.org/web/20161213052708/http://www.who.int/medicines/publications/essentialmedicines/EML_2015_FINAL_amended_NOV2015.pdf?ua=1|archivedate=13 December 2016|df=}}
6. ^{{cite web|title=Tetracaine|url=http://mshpriceguide.org/en/single-drug-information/?DMFId=754&searchYear=2014|website=International Drug Price Indicator Guide|accessdate=8 December 2016}}
7. ^{{cite journal|last=Pywell|first=A|author2=Xyrichis, A |title=Does topical Amethocaine cream increase first-time successful cannulation in children compared with a eutectic mixture of local anaesthetics (EMLA) cream? A systematic review and meta-analysis of randomised controlled trials|publisher=Emerg Med J|volume=0|issue=0|year=2014|pages=1–5|doi=10.1136/emermed-2014-204066}}
8. ^Appleton's Nursing Manual - "Cocaine"
9. ^{{cite journal|last=Györke|first=S|author2=Lukyanenko, V|title=Dual effects of tetracaine on spontaneous sodium release in rat ventricular myocytes|publisher=J Physiol|volume=500|issue=2|year=1997|pages=297–309|display-authors=etal}}
{{Vasoprotectives}}{{Local anesthetics}}{{portal bar|Pharmacy and pharmacology|Medicine}}

4 : Local anesthetics|Ethyl esters|World Health Organization essential medicines|RTT

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