Procaine benzylpenicillin

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Procaine benzylpenicillin
Combination of
Benzylpenicillinantibiotic
Procaineanaesthetic
Names
Trade namesBicillin C-R,[1] other
Other namespenicillin G procaine, procaine penicillin G, procaine penicillin
Clinical data
WHO AWaRe
Pregnancy
category
  • US: B (No risk in non-human studies)[1]
Routes of
use		IM
Defined daily dose0.6 grams[2]
External links
AHFS/Drugs.comFDA Professional Drug Information
Legal
Legal status

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.[3]

Side effects include pain at the site of injection, blood clotting problems, seizures, and allergic reactions including anaphylaxis.[3] When used to treat syphilis a reaction known as Jarisch-Herxheimer may occur.[3] It is not recommended in those with a history of penicillin allergy or procaine allergy.[1][3] Use during pregnancy and breastfeeding is relatively safe.[1][3] Procaine benzylpenicillin is in the penicillin and beta lactam family of medications.[3] It works via benzylpenicillin and results in bacterial death.[3][4] Procaine makes the combination long acting.[5]

Procaine benzylpenicillin was introduced for medical use in 1948.[4] It is on the World Health Organization's List of Essential Medicines.[6] The wholesale cost in the developing world is about US$0.09–0.18 per day.[7] In the United States a course of treatment costs $100–200.[1]

Medical uses

Specific indications for procaine penicillin include:[8]

  • Syphilis
    • In the United States, Bicillin C-R (an 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.[9] 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.[10]
  • 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.

Dosage

The defined daily dose is 0.6 grams (parenteral)[2]

Adverse effects

Further information: 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.[11] 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

References

  1. ↑ 1.0 1.1 1.2 1.3 1.4 Hamilton, Richart (2015). Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. p. 95. ISBN 9781284057560.
  2. ↑ 2.0 2.1 "WHOCC - ATC/DDD Index". www.whocc.no. Archived from the original on 1 December 2020. Retrieved 21 September 2020.
  3. ↑ 3.0 3.1 3.2 3.3 3.4 3.5 3.6 3.7 3.8 World Health Organization (2009). Stuart MC, Kouimtzi M, Hill SR (eds.). WHO Model Formulary 2008. World Health Organization. pp. 113, 607, 618. hdl:10665/44053. ISBN 9789241547659.
  4. ↑ 4.0 4.1 "Penicillin G Procaine - FDA prescribing information, side effects and uses". www.drugs.com. Archived from the original on 20 December 2016. Retrieved 10 December 2016.
  5. ↑ Ebadi, Manuchair (2007). Desk Reference of Clinical Pharmacology, Second Edition. CRC Press. p. 555. ISBN 9781420047448. Archived from the original on 2016-12-20.
  6. ↑ World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
  7. ↑ "Penicillin, Procaine Benzyl". International Drug Price Indicator Guide. Archived from the original on 22 January 2018. Retrieved 8 December 2016.
  8. ↑ Rossi S, ed. (2006). Australian Medicines Handbook. Adelaide: Australian Medicines Handbook. ISBN 0-9757919-2-3.
  9. ↑ Centers for Disease Control and Prevention (CDC) (2005). "Inadvertent use of Bicillin C-R to treat syphilis infection—Los Angeles, California, 1999–2004". MMWR Morb. Mortal. Wkly. Rep. 54 (9): 217–9. PMID 15758893.
  10. ↑ United States Food & Drug Administration. "FDA Strengthens Labels of Two Specific Types of Antibiotics to Ensure Proper Use." Archived 2009-01-14 at the Wayback Machine Published December 1, 2004. Last accessed June 18, 2007.
  11. ↑ 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. Food & Agriculture Org. 1999. p. 96. ISBN 9789251042809.
  12. ↑ British Pharmacopoeia Commission Secretariat. "Index (BP 2009)" (PDF). Archived from the original (PDF) on 11 April 2009. Retrieved 26 March 2010.

External links

Identifiers:
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