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词条 Glucagon (medication)
释义

  1. Medical uses

      Low blood sugar    Beta blocker overdose    Anaphylaxis    Impacted food bolus    Endoscopic retrograde cholangiopancreatography  

  2. Adverse effects

      Contraindications  

  3. Mechanism of action

  4. History

  5. References

{{About|the medication|the natural hormone|Glucagon}}{{drugbox
| Verifiedfields = changed
| Watchedfields = changed
| verifiedrevid = 461121086
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 76LA80IG2G
| drug_name = Glucagon
| IUPAC_name = Glucagon
| image = Glucagon stereo animation.gif
| caption = Glucagon ball and stick model, with the carboxyl terminus above and the amino terminus below
| tradename = GlucaGen, others
| Drugs.com = {{Drugs.com|monograph|glucagon}}
| MedlinePlus =
| C=153 | H=225 | N=43 | O=49 | S=1
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 17288942
| smiles = C[C@H]([C@@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccc(cc2)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc3ccc(cc3)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc4ccccc4)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](Cc5c[nH]c6c5cccc6)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H]([C@@H](C)O)C(=O)O)NC(=O)CNC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CO)NC(=O)[C@H](Cc7cnc[nH]7)N)O
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 1S/C153H225N43O49S/c1-72(2)52-97(133(226)176-96(47-51-246-11)132(225)184-104(60-115(159)209)143(236)196-123(78(10)203)151(244)245)179-137(230)103(58-83-64-167-89-29-19-18-28-87(83)89)183-131(224)95(43-46-114(158)208)177-148(241)120(74(5)6)194-141(234)101(54-79-24-14-12-15-25-79)182-138(231)105(61-117(211)212)185-130(223)94(42-45-113(157)207)171-124(217)75(7)170-127(220)91(31-22-49-165-152(160)161)172-128(221)92(32-23-50-166-153(162)163)174-146(239)110(69-199)191-140(233)107(63-119(215)216)186-134(227)98(53-73(3)4)178-135(228)99(56-81-33-37-85(204)38-34-81)180-129(222)90(30-20-21-48-154)173-145(238)109(68-198)190-136(229)100(57-82-35-39-86(205)40-36-82)181-139(232)106(62-118(213)214)187-147(240)111(70-200)192-150(243)122(77(9)202)195-142(235)102(55-80-26-16-13-17-27-80)188-149(242)121(76(8)201)193-116(210)66-168-126(219)93(41-44-112(156)206)175-144(237)108(67-197)189-125(218)88(155)59-84-65-164-71-169-84/h12-19,24-29,33-40,64-65,71-78,88,90-111,120-123,167,197-205H,20-23,30-32,41-63,66-70,154-155H2,1-11H3,(H2,156,206)(H2,157,207)(H2,158,208)(H2,159,209)(H,164,169)(H,168,219)(H,170,220)(H,171,217)(H,172,221)(H,173,238)(H,174,239)(H,175,237)(H,176,226)(H,177,241)(H,178,228)(H,179,230)(H,180,222)(H,181,232)(H,182,231)(H,183,224)(H,184,225)(H,185,223)(H,186,227)(H,187,240)(H,188,242)(H,189,218)(H,190,229)(H,191,233)(H,192,243)(H,193,210)(H,194,234)(H,195,235)(H,196,236)(H,211,212)(H,213,214)(H,215,216)(H,244,245)(H4,160,161,165)(H4,162,163,166)/t75-,76+,77+,78+,88-,90-,91-,92-,93-,94-,95-,96-,97-,98-,99-,100-,101-,102-,103-,104-,105-,106-,107-,108-,109-,110-,111-,120-,121-,122-,123-/m0/s1
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| CAS_number = 16941-32-5
| ATCvet =
| ATC_prefix = H04
| ATC_suffix = AA01
| PubChem = 16132283
| IUPHAR_ligand = 1136
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank =
| ChEMBL_Ref = {{ebicite|changed|EBI}}
| ChEMBL = 266481
| molecular_weight = 3482.747314 g/mol
| bioavailability =
| protein_bound =
| metabolism =
| elimination_half-life =
| excretion =
| pregnancy_AU =
| pregnancy_US = B
| pregnancy_category=
| legal_AU =
| legal_CA =
| legal_UK =
| legal_US =
| legal_status =
| routes_of_administration = IV, IM, subQ
}}Glucagon is a medication and hormone.[1] As a medication it is used to treat low blood sugar, beta blocker overdose, calcium channel blocker overdose, and those with anaphylaxis who do not improve with epinephrine.[2] It is given by injection into a vein, muscle, or under the skin.[2]

Common side effects include vomiting.[2] Other side effects include low blood potassium and low blood pressure.[1] It is not recommended in people who have a pheochromocytoma or insulinoma.[2] Use in pregnancy has not be found to be harmful to the baby.[1] Glucagon is in the glycogenolytic family of medications.[2] It works by causing the liver to break down glycogen into glucose.[2]

Glucagon was approved for medical use in the United States in 1960.[2] It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.[3] The wholesale cost in the developing world is about {{US$}}25.75 a dose.[4] In the United Kingdom that dose costs the NHS about £11.52.[5] In the United States the wholesale cost of a dose is {{US$}}247.32.[6] It is a manufactured form of the glucagon hormone.[2]

Medical uses

Low blood sugar

An injectable form of glucagon may be part of first aid in cases of low blood sugar when the person is unconscious or for other reasons cannot take glucose orally or by intravenous. The glucagon is given by intramuscular, intravenous or subcutaneous injection, and quickly raises blood glucose levels. To use the injectable form, it must be reconstituted prior to use, a step that requires a sterile diluent to be injected into a vial containing powdered glucagon, because the hormone is highly unstable when dissolved in solution. When dissolved in a fluid state, glucagon can form amyloid fibrils, or tightly woven chains of proteins made up of the individual glucagon peptides, and once glucagon begins to fibrilize, it becomes useless when injected, as the glucagon cannot be absorbed and used by the body. The reconstitution process makes using glucagon cumbersome, although there are a number of products now in development from a number of companies that aim to make the product easier to use.

Beta blocker overdose

Anecdotal evidence suggests a benefit of higher doses of glucagon in the treatment of overdose with beta blockers; the likely mechanism of action is the increase of cAMP in the myocardium, in effect bypassing the β-adrenergic second messenger system.[7]

Anaphylaxis

Some people who have anaphylaxis and are on beta blockers are resistant to epinephrine. In this situation glucagon intravenously may be useful to treat their low blood pressure.{{cite journal | vauthors = Tang AW | title = A practical guide to anaphylaxis | journal = American Family Physician | volume = 68 | issue = 7 | pages = 1325–32 | date = Oct 2003 | pmid = 14567487 | doi = }}
9. ^{{cite journal | vauthors = Ko HH, Enns R | title = Review of food bolus management | journal = Canadian Journal of Gastroenterology | volume = 22 | issue = 10 | pages = 805–8 | date = Oct 2008 | pmid = 18925301 | pmc = 2661297 }}
10. ^{{cite journal | vauthors = Arora S, Galich P | title = Myth: glucagon is an effective first-line therapy for esophageal foreign body impaction | journal = Canadian Journal of Emergency Medicine| volume = 11 | issue = 2 | pages = 169–71 | date = Mar 2009 | pmid = 19272219 }}
11. ^{{cite journal | vauthors = Leopard D, Fishpool S, Winter S | title = The management of oesophageal soft food bolus obstruction: a systematic review | journal = Annals of the Royal College of Surgeons of England | volume = 93 | issue = 6 | pages = 441–4 | date = Sep 2011 | pmid = 21929913 | pmc = 3369328 | doi = 10.1308/003588411X588090 }}
12. ^{{cite journal | vauthors = Weant KA, Weant MP | title = Safety and efficacy of glucagon for the relief of acute esophageal food impaction | journal = American Journal of Health-System Pharmacy | volume = 69 | issue = 7 | pages = 573–7 | date = Apr 2012 | pmid = 22441787 | doi = 10.2146/ajhp100587 }}
13. ^{{cite journal | vauthors = Ikenberry SO, Jue TL, Anderson MA, Appalaneni V, Banerjee S, Ben-Menachem T, Decker GA, Fanelli RD, Fisher LR, Fukami N, Harrison ME, Jain R, Khan KM, Krinsky ML, Maple JT, Sharaf R, Strohmeyer L, Dominitz JA | title = Management of ingested foreign bodies and food impactions | journal = Gastrointestinal Endoscopy | volume = 73 | issue = 6 | pages = 1085–1091 | date = Jun 2011 | pmid = 21628009 | doi = 10.1016/j.gie.2010.11.010 | url = http://www.asge.org/uploadedFiles/Publications_and_Products/Practice_Guidelines/Management%20of%20ingested%20foreign%20bodies%20and%20food%20impactions.pdf | deadurl = no | archiveurl = https://web.archive.org/web/20130808035202/http://www.asge.org/uploadedFiles/Publications_and_Products/Practice_Guidelines/Management%20of%20ingested%20foreign%20bodies%20and%20food%20impactions.pdf | archivedate = 2013-08-08 | df = }}
14. ^{{cite journal | vauthors = Chauvin A, Viala J, Marteau P, Hermann P, Dray X | title = Management and endoscopic techniques for digestive foreign body and food bolus impaction | journal = Digestive and Liver Disease | volume = 45 | issue = 7 | pages = 529–42 | date = Jul 2013 | pmid = 23266207 | doi = 10.1016/j.dld.2012.11.002 }}
15. ^{{cite journal | vauthors = Koch-Weser J | title = Potentiation by glucagon of the hypoprothrombinemic action of warfarin | journal = Annals of Internal Medicine | volume = 72 | issue = 3 | pages = 331–5 | date = Mar 1970 | pmid = 5415418 | doi = 10.7326/0003-4819-72-3-331 }}
16. ^{{cite web| url =http://pi.lilly.com/us/rglucagon-pi.pdf| title =Information for the Physician: Glucagon for Injection (rDNA origin)| format =| website =| publisher =Eli Lilly and Company| accessdate =2016-10-12| deadurl =no| archiveurl =https://web.archive.org/web/20161120012906/http://pi.lilly.com/us/rglucagon-pi.pdf| archivedate =2016-11-20| df =}}
17. ^{{cite journal | vauthors = Hue L, Rider MH | title = Role of fructose 2,6-bisphosphate in the control of glycolysis in mammalian tissues | journal = The Biochemical Journal | volume = 245 | issue = 2 | pages = 313–24 | date = Jul 1987 | pmid = 2822019 | pmc = 1148124 | doi = }}
18. ^{{cite book | vauthors = Claus TH, El-Maghrabi MR, Regen DM, Stewart HB, McGrane M, Kountz PD, Nyfeler F, Pilkis J, Pilkis SJ | title = The role of fructose 2,6-bisphosphate in the regulation of carbohydrate metabolism | journal = Current Topics in Cellular Regulation | volume = 23 | issue = | pages = 57–86 | year = 1984 | pmid = 6327193 | doi = 10.1016/b978-0-12-152823-2.50006-4| isbn = 9780121528232 }}
19. ^{{cite journal | vauthors = Feliú JE, Hue L, Hers HG | title = Hormonal control of pyruvate kinase activity and of gluconeogenesis in isolated hepatocytes | journal = Proceedings of the National Academy of Sciences of the United States of America | volume = 73 | issue = 8 | pages = 2762–6 | date = Aug 1976 | pmid = 183209 | pmc = 430732 | doi = 10.1073/pnas.73.8.2762 | bibcode = 1976PNAS...73.2762F }}
20. ^{{cite journal | vauthors = Kimball C, Murlin J | title = Aqueous extracts of pancreas III. Some precipitation reactions of insulin | journal = J. Biol. Chem. | year = 1923 | volume = 58 | pages = 337–348 | url = http://www.jbc.org/cgi/reprint/58/1/337 | issue = 1 | deadurl = no | archiveurl = https://web.archive.org/web/20070929090405/http://www.jbc.org/cgi/reprint/58/1/337 | archivedate = 2007-09-29 | df = }}
21. ^{{cite journal | vauthors = Bromer W, Winn L, Behrens O | title = The amino acid sequence of glucagon V. Location of amide groups, acid degradation studies and summary of sequential evidence | journal = J. Am. Chem. Soc. | year = 1957 | volume = 79 | issue = 11 | pages = 2807–2810|doi=10.1021/ja01568a038 }}
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3 : World Health Organization essential medicines|Drugs_acting_on_the_cardiovascular_system|RTT

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