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It is a form of penicillin which is a combination of benzylpenicillin and the local anaesthetic agent procaine. 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.
This combination is aimed at reducing the pain and discomfort associated with a large intramuscular injection of penicillin. It is widely used in veterinary settings.
It is on the World Health Organization's List of Essential Medicines, a list of the most important medication needed in a basic health system.
Specific indications for procaine penicillin include:
- 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. 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.
- 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.
At high doses procaine penicillin can cause seizures and CNS abnormalities due to procaine present in it.
- "WHO Model List of EssentialMedicines" (PDF). World Health Organization. October 2013. Retrieved 22 April 2014.
- Rossi S, editor, ed. (2006). Australian Medicines Handbook. Adelaide: Australian Medicines Handbook. ISBN 0-9757919-2-3.
- 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.
- 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.
- British Pharmacopoeia Commission Secretariat. "Index (BP 2009)" (PDF). Retrieved 26 March 2010.