Procaine benzylpenicillin

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Procaine benzylpenicillin
Combination of
Benzylpenicillin antibiotic
Procaine anaesthetic
Clinical data
Trade names Bicillin C-R,[1] other
AHFS/Drugs.com FDA Professional Drug Information
Pregnancy
category
  • US: B (No risk in non-human studies) [1]
Routes of
administration
IM
ATC code
Legal status
Legal status
Identifiers
Synonyms penicillin G procaine, procaine penicillin G, procaine penicillin
CAS Number
ChEMBL
E number E707 (antibiotics)
ECHA InfoCard 100.000.187
 NYesY (what is this?)  (verify)

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.[2]

Side effects include pain at the site of injection, blood clotting problems, seizures, and allergic reactions including anaphylaxis. When used to treat syphilis a reaction known as Jarisch-Herxheimer may occur.[2] It is not recommended in those with a history of penicillin allergy or procaine allergy. Use during pregnancy and breastfeeding is relatively safe.[1][2] Procaine benzylpenicillin is in the penicillin and beta lactam family of medications.[2] It works via benzylpenicillin and results in bacterial death.[2][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, the most effective and safe medicines needed in a health system.[5] The wholesale cost in the developing world is about 0.09 to 0.18 USD per day.[6] In the United States a course of treatment costs 100 to 200 USD.[1]

Medical uses[edit]

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[edit]

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

Mechanism[edit]

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[edit]

References[edit]

  1. ^ a b c d Hamilton, Richart (2015). Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. p. 95. ISBN 9781284057560. 
  2. ^ a b c d e WHO Model Formulary 2008 (PDF). World Health Organization. 2009. p. 113, 607, 618. ISBN 9789241547659. Retrieved 8 December 2016. 
  3. ^ a b "Penicillin G Procaine - FDA prescribing information, side effects and uses". www.drugs.com. Retrieved 10 December 2016. 
  4. ^ Ebadi, Manuchair (2007). Desk Reference of Clinical Pharmacology, Second Edition. CRC Press. p. 555. ISBN 9781420047448. 
  5. ^ "WHO Model List of Essential Medicines (19th List)" (PDF). World Health Organization. April 2015. Retrieved 8 December 2016. 
  6. ^ "Penicillin, Procaine Benzyl". International Drug Price Indicator Guide. Retrieved 8 December 2016. 
  7. ^ Rossi S, editor, ed. (2006). Australian Medicines Handbook. Adelaide: Australian Medicines Handbook. ISBN 0-9757919-2-3. 
  8. ^ 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. 
  9. ^ 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.
  10. ^ 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. 
  11. ^ British Pharmacopoeia Commission Secretariat. "Index (BP 2009)" (PDF). Retrieved 26 March 2010.