Procaine benzylpenicillin

Intramuscular
Bejel, Pinta, Syphilis, Yaws

Intramuscular
Neurosyphilis

Intramuscular
Congenital syphilis

Intramuscular
Fusospirochetosis (Vincent's infection) of the oropharynx, Invasive Group A beta-hemolytic streptococcal disease, Pneumococcal pneumonia, Staphylococcal infections

Intramuscular
Pneumococcal pneumonia

Intramuscular
Uncomplicated gonorrhoea

Intramuscular
Diphtheria

Intramuscular
Treatment and postexposure prophylaxis of inhalation anthrax

Intramuscular
Cutaneous anthrax

Hypersensitivity to penicillin.

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.

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

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.

Decreased effect with tetracycline.

False-positive urinary glucose test using cupric sulfate.

Description:
Mechanism of Action: 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).

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)

Store between 2-8°C. Do not freeze.

Penicillins

J01CE09 - procaine benzylpenicillin ; Belongs to the class of beta-lactamase sensitive penicillins. Used in the systemic treatment of infections.

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.