Procaine Penicillin G is intermediate-acting insulin indicated for the treatment of moderately severe to severe infections in infections caused by susceptible organisms.

Indications of Penicillin G Procaine:

• Prophylaxis of Anthrax:

  • It is used to reduce the incidence of anthrax following exposure to aerosolized Bacillus anthracis.

• Treatment of Anthrax:

  • It is indicated for the treatment of anthrax, including post-exposure inhalational disease due to aerosolized B. anthracis.

• Diphtheria:

  • It is used in combination with antitoxin for the prevention of the carrier stage of diphtheria caused by susceptible Corynebacterium diphtheriae.

• Subacute endocarditis:

  • Penicillin G is prescribed for treating subacute bacterial endocarditis, only in extremely sensitive infections, caused by susceptible group A streptococci.

• Erysipeloid:

  • It is used for the treatment of erysipeloid caused by susceptible Erysipelothrix rhusiopathiae.

• Fusospirochetosis:

  • Penicillin G is effective for treating fusospirochetosis (Vincent gingivitis and pharyngitis) in conjunction with dental care, and moderately severe infections of the oropharynx caused by susceptible fusiform bacilli and spirochetes.

• Pneumococcal infection:

  • Respiratory tract infections caused by susceptible pneumococci can be treated by penicillin G.
  • Limitations of use: Aqueous penicillin G is preferred for severe pneumonia, empyema, bacteremia, pericarditis, meningitis, peritonitis, and arthritis of pneumococcal etiology.

• Rat-bite fever:

  • It is prescribed for the treatment of rat-bite fever caused by susceptible Streptobacillus moniliformis and Spirillum minus organisms.

• Skin and soft tissue infection:

  • Moderately/severe infections of the skin and soft tissues caused by susceptible staphylococci can be treated by it.

• Streptococcal infections:

  • Treatment of moderately severe to severe infections of the upper respiratory tract, skin and soft tissue infections, scarlet fever, and erysipelas caused by susceptible streptococci (group A, without bacteremia).
  • Limitations of use: Some streptococcal groups, including group D (enterococcus), are resistant. Aqueous penicillin is recommended for streptococcal infections with bacteremia.

• Syphilis:

  • It is effective against all stages of syphilis caused by susceptible Treponema pallidum.

• Yaws, bejel, and pinta:

  • Treatment of yaws, bejel, and pinta caused by susceptible organisms.
  • Limitations of use: When high, sustained serum levels are required, use aqueous penicillin G, either intramuscularly (IM) or intravenously (IV).
  • Do not use in the treatment of beta-lactamase producing organisms, which includes most strains of Neisseria gonorrhea.

Procaine Penicillin G dose in Adults

Procaine Penicillin G dose in the treatment of Anthrax:

• Inhalational (post-exposure prophylaxis):

  • 1,200,000 intramuscular units every 12 hours

Note:

Not a preferred regimen. The overall treatment duration should be 60 days. Therapy more than 14 days can increase the risk of adverse events therefore it is better to switch to alternate agents in case of prolonged use.

• Treatment of Cutaneous anthrax:

  • 600,000 to 1,000,000 units intramuscular daily

Procaine Penicillin G dose for the treatment of Diphtheria as adjunctive therapy with antitoxin: 

• Patients >10 kg:

  • 600,000 units intramuscular daily for 14 days.

• Manufacturer's labeling:

  • Dosing in the prescribing information may not reflect current clinical practice.
  • 300,000 to 600,000 units IM daily.

Procaine Penicillin G dose for the carrier state of Diphtheria:

• 300,000 units IM once daily for 10 days.
• Note: Penicillin G benzathine is preferred.

Procaine Penicillin G dose for the treatment of Neurosyphilis (including ocular syphilis):

• 2.4 million units  IM once daily with concomitant probenecid for 10 to 14 days
• Note: Aqueous penicillin G IV monotherapy is the preferred initial treatment.

Procaine Penicillin G dose for the treatment of uncomplicated, moderately severe, Pneumococcal pneumonia:

• 600,000 to 1,000,000 units IM daily.

Dose in the treatment of moderately severe to severe Staphylococcal infections:

• 600,000 to 1,000,000 units  IM daily.

Dose in the treatment of moderately severe to severe Group A Streptococcal infections:

• 600,000 to 1,000,000 units  IM daily for a minimum of 10 days.

Procaine Penicillin G dose in the treatment of Yaws:

• 600,000 units IM daily.

Note: Duration dependent upon the stage of disease, azithromycin is preferred.

Procaine Penicillin G dose in Childrens

Procaine Penicillin G dose in children:

Note:

Although FDA approved for some indications, dosing may not be provided if current guidelines do not recommend use (eg, streptococcal or staphylococcal pneumonia or pharyngitis.

Procaine Penicillin G General dosing in mild to moderate susceptible infections:

• 50,000 units/kg/day IM in divided doses every 12 to 24 hours.
• The maximum daily dose: 1.2 million units/day.

Dose for the postexposure prophylaxis of inhalational Anthrax:

Note: Although FDA approved, penicillin G procaine is not a preferred regimen.

• 25,000 units/kg/dose IM b.i.d.
• The maximum dose: 1.2 million units/dose.

Procaine Penicillin G dose for the treatment of Diphtheria as adjunctive therapy with antitoxin:

• Patients ≤10 kg:

  • 300,000 units IM daily for 14 days.

• Patients >10 kg:

  • 600,000 units IM daily for 14 days.

Procaine Penicillin G dose for the treatment of Syphilis:

• Congenital:

  • 50,000 units/kg/day  IM once daily for 10 days.
  • The maximum daily dose: 2.4 million units/day.
  • The entire course should be restarted in case of a single missed day if more than 1 day of therapy is missed.
  • Penicillin G procaine is not the preferred therapy in HIV positive patients due to poor CNS penetration.

• Neurosyphilis (including ocular or otic syphilis):

  • HIV-exposed/-positive:

    • Adolescents:
      • 2.4 million units  IM once daily for 10 to 14 days in combination with probenecid.

Pregnancy Risk Category: B

• Studies on animal reproduction did not show any adverse results.
• Penicillin G crosses the placenta but its use during pregnancy has not been shown to increase the chance of adverse fetal effects.
• For the treatment of syphilis and bacillus aureus, penicillin G procaine is approved for use during pregnancy.

Penicillin G procaine use during breastfeeding:

• Breast milk is known to contain penicillins.
• The manufacturer suggests that nursing mothers be cautious when using penicillin.
• It can cause bowel flora modifications and allergic sensitization.

Dose adjustment in renal disease:

There are no dosage adjustments provided in the manufacturer's labeling, however, dose reduction is required in impaired renal function due to delayed excretion.

Procaine Penicillin Dose adjustment in liver disease:

There are no dosage adjustments provided in the manufacturer's labeling.

Side effects of Procaine Penicillin:

• Cardiovascular:

  • Conduction disturbances,
  • myocardial depression,
  • vasodilation

• Central nervous system:

  • CNS stimulation,
  • confusion,
  • drowsiness,
  • myoclonus,
  • seizure

• Hematologic:

  • Hemolytic anemia,
  • neutropenia,
  • positive Coombs' reaction

• Local:

  • Pain at the injection site,
  • sterile abscess at the injection site,
  • thrombophlebitis

• Renal:

  • Interstitial nephritis

• Miscellaneous:

  • Hypersensitivity reactions,
  • Jarisch-Herxheimer reaction,
  • pseudoanaphylactic reactions,
  • serum sickness

Contraindications to Penicillin G procaine:

• Hypersensitivity to penicillin or any other component of the formula

Warnings and precautions

• Anaphylactic and hypersensitivity reactions

  • It can cause life-threatening anaphylactic reactions that require immediate discontinuation and supportive therapy.
  • Asthmatic patients should use it with caution.

• Fibrosis, atrophy and other:

  • After repeated penicillin injections into the anterolateral thigh, quadriceps femoris fibrosis is seen and atrophy.

• Methemoglobinemia:

  • It is often treated with local anesthetics, including procaine.
  • The onset of symptoms can be delayed or immediate (hours) following anesthesia exposure.
  • Risk factors include heart or pulmonary disease and G6PD deficiency.
  • Methemoglobinemia symptoms such as headaches, weakness, cyanosis headaches, dyspnoea, dyspnoea and tachycardia must be recognized.

• Neurovascular damage:

  • Penicillin G can cause severe or permanent neurovascular damage (e.g. transverse myelitis, necrosis, and gangrene that requires amputation), if it is administered to the buttock, thigh, and deltoid areas.
  • If intravascular, especially for children, it can cause cyanosis and bleb formation around the injection site.
  • Consult the appropriate specialists immediately if you notice any signs of a blood supply problem.

• Procaine neuropsychiatric reactions:

  • With higher doses (4.8 million units), immediate toxic reactions may occur. These include weakness, confusion anxiety/depression and hallucinations.
  • Reactions last half an hour and are temporary.

• Sensitivity to Procaine:

  • Test with 0.01 mL of 1%/2% procaine solution if you have a history or hypersensitivity to it.
  • If erythema or wheal, flare up, or eruption occur, it should be avoided.
  • Antihistamines can be used to manage sensitive skin.

• Superinfection

  • Fungal or bacterial superinfection such as C.difficile-associated diarrhea (CDAD) and pseudomembranous colitis can be seen with long term therapy.

• Renal impairment

  • Patients with severe renal impairment should be cautious. A dosage reduction may be required.

• Seizure disorders:

  • Patients with seizure disorders should be cautious.
  • Higher levels of renal impairment can increase the risk of seizures.

Monitoring parameters:

• Hypersensitivity reactions with the first dose
• Injection site reactions
• mental status post injection
• Monthly hematological and renal function tests with prolonged therapy.

How to administer Procaine Penicillin G?

• Procaine suspension is for deep IM injection only.
• Rotate the injection site.
• It should not be administered via any other route due to the risk of permanent neuro-vascular damage.

Mechanism of action of Procaine Penicillin:

• Penicillin G procaine is a penicillin that binds to one or more penicillin-binding protein (PBPs).
• This inhibits the final transpeptidation step in peptidoglycan synthesis in bacterial cell walls and thus, inhibits cell wall biosynthesis.
• This causes cell-wall assembly to be stopped and bacterial lysis due to the activity of cell wall selflytic enzymes (autolysins or murein hydrolases).

Duration: Therapeutic: 15 to 24 hours

Absorption after Intramuscular administration is Slow

Distribution: High distribution in kidneys, lesser amounts in the liver, skin, and intestines. Very small levels found in CSF.

Protein binding: 60%

The time to peak serum concentration: Within 1 to 4 hours and can persist within the therapeutic range for 15 to 24 hours

Excretion: Urine (60% to 90% as unchanged drug); renal clearance is delayed in neonates, young infants, and patients with impaired renal function

International Brands of Procaine Penicillin:

• Penpro
• Aquacaine
• Benzetacil
• Cilicaine Syringe
• Hidrociclina
• Intrasept
• Jenacillin O
• Mudapenil
• Pam
• Penicillinum procainicum
• Procain-Penicillin Streuli
• Procaine Penicillin. G
• Procapen
• Retardillin
• Servipen-G Forte

Procaine penicillin Brands in Pakistan: