Procaine benzylpenicillin


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : IM Syphilis; Bejel; Pinta; Yaws Early stage: 600 mg once daily for 10 days. Late stage: 600 mg once daily for 17 days. Neurosyphilis Combined with probenecid: 1.8-2.4 g once daily for 17 days. Invasive Group A beta-hemolytic streptococcal disease; Staphylococcal infections; Fusospirochetosis (Vincent’s infection) of the oropharynx; Pneumococcal pneumonia Moderately severe to severe cases: 1.5 g daily for 2-5 days. Uncomplicated gonorrhoea 1 g once daily for 7-14 days. Alternatively, up to 4.8 g as a single dose combined with probenecid. Diphtheria As adjunctive therapy with antitoxin: 300-600 mg once daily. Carrier state: 300 mg once daily for 10 days. Treatment and postexposure prophylaxis of inhalation anthrax 1.2 g every 12 hours for 60 days. Cutaneous anthrax 0.6-1 g once daily.
Dosage Details
Intramuscular
Bejel, Pinta, Syphilis, Yaws
Adult: For early stage: 600 mg once daily via deep injection for 10 days. For late stage: 600 mg once daily via deep injection for 17 days.

Intramuscular
Neurosyphilis
Adult: In combination with probenecid: 1.8-2.4 g once daily via deep injection for 17 days.

Intramuscular
Congenital syphilis
Child: For early stage and patient with abnormal CSF: ≤2 years 50 mg/kg once daily via deep injection for 10 days.

Intramuscular
Fusospirochetosis (Vincent's infection) of the oropharynx, Invasive Group A beta-hemolytic streptococcal disease, Pneumococcal pneumonia, Staphylococcal infections
Adult: For moderately severe to severe cases: 1.5 g daily via deep injection for 2-5 days. The 4th and 5th doses are dependent on the severity of infection.

Intramuscular
Pneumococcal pneumonia
Child: 50 mg/kg once daily via deep injection for 10 days.

Intramuscular
Uncomplicated gonorrhoea
Adult: 1 g once daily via deep injection for 7-14 days. Alternatively, up to 4.8 g as a single dose in combination with probenecid.

Intramuscular
Diphtheria
Adult: As adjunctive therapy with antitoxin: 300-600 mg once daily via deep injection. Carrier state: 300 mg once daily for 10 days.
Child: Carrier state: 300 mg once daily via deep injection for 10 days.

Intramuscular
Treatment and postexposure prophylaxis of inhalation anthrax
Adult: 1.2 g via deep injection every 12 hours for 60 days.
Child: 25 mg/kg every 12 hours for 60 days via deep injection. Max: 1.2 g/dose.

Intramuscular
Cutaneous anthrax
Adult: 0.6-1 g once daily via deep injection.
Contraindications
Hypersensitivity to penicillin.
Special Precautions
Patient with hypersensitivity to cephalosporins, procaine (known or suspected) or to other allergens, asthma, Brugada syndrome, cardiac conduction abnormalities. Renal impairment. Children. Pregnancy and lactation. Not intended for injection into or near a blood vessel or nerve or for intravascular administration.
Adverse Reactions
Significant: Increased risk of neutropenia and of serum sickness-like reactions (prolonged treatment), superinfection. Rarely, procaine-related reactions manifested as transient mental disturbances (e.g. weakness, anxiety, agitation, combativeness, confusion, depression, hallucinations, seizures, sensation of impending death); quadriceps femoris fibrosis and atrophy (after repeated intramuscular administration into the anterolateral thigh).
Gastrointestinal disorders: Nausea, vomiting, diarrhoea.
Immune system disorders: Jarisch-Herxheimer reaction (for syphilis).
Respiratory, thoracic and mediastinal disorders: Dyspnoea.
Skin and subcutaneous tissue disorders: Rashes.
Potentially Fatal: Rarely, anaphylactic reactions (e.g. maculopapular eruptions, exfoliative dermatitis, urticaria, laryngeal oedema, serum sickness-like reactions), pseudomembranous colitis.
IM/Parenteral: B
MonitoringParameters
Perform susceptibility tests especially for staphylococcal infections prior to treatment. Periodically monitor CBC and renal function if prolonged treatment. Perform monthly serological test for at least 4 months and dark-field examination if syphilis is suspected.
Drug Interactions
Decreased effect with tetracycline.
Lab Interference
False-positive urinary glucose test using cupric sulfate.
Action
Description: Procaine benzylpenicillin is an equimolecular compound of procaine and benzylpenicillin. After IM administration, it is gradually hydrolysed into benzylpenicillin; thus, prolonging its action. Benzylpenicillin is a long-acting penicillin antibacterial which is active against a variety of susceptible gram-positive and gram-negative organisms. It binds to penicillin-binding proteins (PBPs) which inhibits transpeptidation step of peptidoglycan synthesis in bacterial cell wall thus arresting assembly.
Synonym: benzylpenicillin novocaine, penicillin G procaine, procaine penicillin, procaine penicillin G.
Duration: 15-24 hours.
Pharmacokinetics:
Absorption: Slowly absorbed after IM administration. Highly distributed in kidneys, lesser amount in liver, skin and intestines. Time to peak plasma concentration: 1-4 hours.
Distribution: Enters breastmilk. Plasma protein binding: Approx 60%.
Excretion: Mainly via urine (60-90%, as unchanged drug).
Chemical Structure

Chemical Structure Image
Procaine benzylpenicillin

Source: National Center for Biotechnology Information. PubChem Database. Procaine penicillin G, CID=5903, https://pubchem.ncbi.nlm.nih.gov/compound/Procaine-penicillin-G (accessed on Jan. 23, 2020)

Storage
Store between 2-8°C. Do not freeze.
MIMS Class
ATC Classification
J01CE09 - procaine benzylpenicillin ; Belongs to the class of beta-lactamase sensitive penicillins. Used in the systemic treatment of infections.
References
Anon. Penicillin G Procaine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 06/06/2018.

Anon. Penicillin G Procaine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 06/06/2018.

Buckingham R (ed). Procaine Benzylpenicillin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/06/2018.

Buckingham R (ed). Syphilis (Antibacterials-Sexually Transmitted Diseases). Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 20/06/2018.

Penicillin G Procaine Injection, Suspension (Pfizer Laboratories Div Pfizer Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 06/06/2018.

Pharmacy Retailing (NZ) Limited. Cilicaine Syringe data sheet 1 June 2017. Medsafe. http://www.medsafe.govt.nz/. Accessed 06/06/2018.

Disclaimer: This information is independently developed by MIMS based on Procaine benzylpenicillin from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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