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词条 Procaine benzylpenicillin
释义

  1. Medical uses

  2. Adverse effects

  3. Mechanism

  4. Compendial status

  5. References

{{Drugbox
| Verifiedfields = changed
| verifiedrevid = 448213645
| type = combo
| component1 = Benzylpenicillin
| class1 = antibiotic
| component2 = Procaine
| class2 = anaesthetic
| synonyms = penicillin G procaine, procaine penicillin G, procaine penicillin
| tradename = Bicillin C-R,[1] other
| Drugs.com = {{drugs.com|pro|penicillin-g-procaine}}
| pregnancy_AU =
| pregnancy_US = B
| pregnancy_US_comment = [1]
| pregnancy_category =
| legal_AU =
| legal_CA =
| legal_UK =
| legal_US = Rx-only
| legal_status =
| routes_of_administration = IM
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 54-35-3
| ATC_prefix = J01
| ATC_suffix = CE09
| ATC_supplemental = {{ATCvet|J51|CE09}}
| PubChem =
| ChEMBL_Ref = {{ebicite|changed|EBI}}
| ChEMBL = 1628385
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank =
}}Procaine benzylpenicillin also known as penicillin G procaine, is an antibiotic useful for the treatment of a number of bacterial infections.[3] Specifically it is used for syphilis, anthrax, mouth infections, pneumonia, diphtheria, cellulitis, and animal bites.[3] It is given by injection into a muscle.[1]

Side effects include pain at the site of injection, blood clotting problems, seizures, and allergic reactions including anaphylaxis.[1] When used to treat syphilis a reaction known as Jarisch-Herxheimer may occur.[1] It is not recommended in those with a history of penicillin allergy or procaine allergy.[1][1] Use during pregnancy and breastfeeding is relatively safe.[1][1] Procaine benzylpenicillin is in the penicillin and beta lactam family of medications.[1] It works via benzylpenicillin and results in bacterial death.[1][2] Procaine makes the combination long acting.[3]

Procaine benzylpenicillin was introduced for medical use in 1948.[2] It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.[4] The wholesale cost in the developing world is about US$0.09–0.18 per day.[5] In the United States a course of treatment costs $100–200.[6]

Medical uses

Specific indications for procaine penicillin include:[7]

  • Syphilis
    • In the United States, Bicillin C-R (a injectable suspension which 1.2 million units of benzathine penicillin and 1.2 million units of procaine penicillin per 4 ml) is not recommended for treating syphilis, since it contains only half the recommended dose of benzathine penicillin. Medication errors have been made due to the confusion between Bicillin L-A & Bicillin C-R.[8] As a result, changes in product packaging have been made; specifically, the statement "Not for the Treatment of Syphilis" has been added in red text to both the Bicillin CR and Billin CR 900/300 syringe labels.[9]
  • Respiratory tract infections where compliance with oral treatment is unlikely
  • Alongside Pen V and Erythromycin, Bicillin C-R is used to treat strep throat, given as one IM injection
  • Cellulitis, erysipelas
  • Procaine penicillin is also used as an adjunct in the treatment of anthrax.

Adverse effects

{{see|Penicillin drug reaction}}

At high doses procaine penicillin can cause seizures and CNS abnormalities due to procaine present in it.

Mechanism

It is a form of penicillin which is a combination of benzylpenicillin and the local anaesthetic agent procaine.[10] Following deep intramuscular injection, it is slowly absorbed into the circulation and hydrolysed to benzylpenicillin — thus it is used where prolonged low concentrations of benzylpenicillin are required.

Compendial status

  • British Pharmacopoeia [11]

References

1. ^1 2 3 4 5 6 7 8 {{cite book|title=WHO Model Formulary 2008|date=2009|publisher=World Health Organization|isbn=9789241547659|pages=113, 607, 618|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=}}
2. ^1 {{cite web|title=Penicillin G Procaine - FDA prescribing information, side effects and uses|url=https://www.drugs.com/pro/penicillin-g-procaine.html|website=www.drugs.com|accessdate=10 December 2016|deadurl=no|archiveurl=https://web.archive.org/web/20161220230645/https://www.drugs.com/pro/penicillin-g-procaine.html|archivedate=20 December 2016|df=}}
3. ^{{cite book|last1=Ebadi|first1=Manuchair|title=Desk Reference of Clinical Pharmacology, Second Edition|date=2007|publisher=CRC Press|isbn=9781420047448|page=555|url=https://books.google.ca/books?id=ihxyHbnj3qYC&pg=PA555|language=en|deadurl=no|archiveurl=https://web.archive.org/web/20161220152414/https://books.google.ca/books?id=ihxyHbnj3qYC&pg=PA555|archivedate=2016-12-20|df=}}
4. ^{{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=}}
5. ^{{cite web|title=Penicillin, Procaine Benzyl|url=http://mshpriceguide.org/en/single-drug-information/?DMFId=P599&searchYear=2014|website=International Drug Price Indicator Guide|accessdate=8 December 2016}}
6. ^1 2 3 4 {{cite book|last1=Hamilton|first1=Richart|title=Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition|date=2015|publisher=Jones & Bartlett Learning|isbn=9781284057560|page=95}}
7. ^{{cite book | editor=Rossi S, editor | title=Australian Medicines Handbook | year=2006 | location=Adelaide | publisher=Australian Medicines Handbook | isbn=0-9757919-2-3}}
8. ^{{cite journal |author= |title=Inadvertent use of Bicillin C-R to treat syphilis infection—Los Angeles, California, 1999–2004 |journal=MMWR Morb. Mortal. Wkly. Rep. |volume=54 |issue=9 |pages=217–9 |year=2005 |pmid=15758893 |doi= |author1= Centers for Disease Control and Prevention (CDC)}}
9. ^United States Food & Drug Administration. "FDA Strengthens Labels of Two Specific Types of Antibiotics to Ensure Proper Use." {{webarchive|url=https://web.archive.org/web/20090114183518/http://www.fda.gov/bbs/topics/ANSWERS/2004/ANS01329.html |date=2009-01-14 }} Published December 1, 2004. Last accessed June 18, 2007.
10. ^{{cite book|title=Residues of Some Veterinary Drugs in Animals and Foods: Monographs Prepared by the Fiftieth Meeting of the Joint FAO/WHO Expert Committee on Food Additives : Rome, 17-26 February 1998|date=1999|publisher=Food & Agriculture Org.|isbn=9789251042809|page=96|url=https://books.google.ca/books?id=jMCHWPfDYf4C&pg=PA96|language=en|deadurl=no|archiveurl=https://web.archive.org/web/20161220085048/https://books.google.ca/books?id=jMCHWPfDYf4C&pg=PA96|archivedate=20 December 2016|df=}}
11. ^{{cite web| last =British Pharmacopoeia Commission Secretariat| first =| authorlink =| coauthors =| title =Index (BP 2009)| work =| publisher =| date =| url =http://www.pharmacopoeia.co.uk/pdf/2009_index.pdf| doi =| accessdate =26 March 2010| deadurl =yes| archiveurl =https://web.archive.org/web/20090411071437/http://www.pharmacopoeia.co.uk/pdf/2009_index.pdf| archivedate =11 April 2009| df =}}
{{PenicillinAntiBiotics}}{{portal bar|Pharmacy and pharmacology|Medicine}}

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