Procaine benzylpenicillin explained

Procaine benzylpenicillin also known as penicillin G procaine, is an antibiotic useful for the treatment of a number of bacterial infections. Specifically it is used for syphilis, anthrax, mouth infections, pneumonia, diphtheria, cellulitis, and animal bites. 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.^{[2] [1]} Use during pregnancy and breastfeeding is relatively safe.^{[2] [1]} Procaine benzylpenicillin is in the penicillin and beta lactam family of medications.^[1] It works via benzylpenicillin and results in bacterial death.^{[1] [3]} Procaine makes the combination long acting.^[4]

Procaine benzylpenicillin was introduced for medical use in 1948.^[3] It is on the World Health Organization's List of Essential Medicines.^[5]

Medical uses

Specific indications for procaine penicillin include:^[6]

• 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.^[7] 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.^[8]
• 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 also: 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.^[9] 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^[10]

See also

• Benzathine benzylpenicillin/procaine benzylpenicillin

External links

• Web site: Penicillin G Procaine . U.S. National Library of Medicine . Drug Information Portal .

Notes and References

1. Book: WHO Model Formulary 2008 . 2009 . 9789241547659 . ((World Health Organization)) . Stuart MC, Kouimtzi M, Hill SR . 10665/44053 . World Health Organization . World Health Organization . free . 113, 607, 618 .
2. Book: Hamilton. Richart. Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. 2015. Jones & Bartlett Learning. 9781284057560. 95.
3. Web site: Penicillin G Procaine - FDA prescribing information, side effects and uses. www.drugs.com. 10 December 2016. live. https://web.archive.org/web/20161220230645/https://www.drugs.com/pro/penicillin-g-procaine.html. 20 December 2016.
4. Book: Ebadi. Manuchair. Desk Reference of Clinical Pharmacology, Second Edition. 2007. CRC Press. 9781420047448. 555. en. live. https://web.archive.org/web/20161220152414/https://books.google.ca/books?id=ihxyHbnj3qYC&pg=PA555. 2016-12-20.
5. Book: ((World Health Organization)) . World Health Organization model list of essential medicines: 21st list 2019 . 2019 . 10665/325771 . World Health Organization . World Health Organization . Geneva . WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO . free .
6. Book: Rossi S . . 2006 . Adelaide . Australian Medicines Handbook . 0-9757919-2-3.
7. Inadvertent use of Bicillin C-R to treat syphilis infection—Los Angeles, California, 1999–2004 . MMWR Morb. Mortal. Wkly. Rep. . 54 . 9 . 217–9 . 2005 . 15758893 . Centers for Disease Control and Prevention (CDC). 6820132 .
8. United States Food & Drug Administration. "FDA Strengthens Labels of Two Specific Types of Antibiotics to Ensure Proper Use." Published December 1, 2004. Last accessed June 18, 2007.
9. Book: 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. 1999. Food & Agriculture Org.. 9789251042809. 96. en.
10. Web site: British Pharmacopoeia Commission Secretariat. Index (BP 2009). 26 March 2010. dead. https://web.archive.org/web/20090411071437/http://www.pharmacopoeia.co.uk/pdf/2009_index.pdf. 11 April 2009.