Procaine Indicated for the treatment of moderately severe to severe infections caused by susceptible organisms, penicillin G is an intermediate-acting insulin.

Indications of Penicillin G Procaine:

• Prophylaxis of Anthrax:

  • After exposure to aerosolized Bacillus anthracis, it is used to lower the risk of anthrax.

• Treatment of Anthrax:

  • It can be used to treat anthrax, particularly post-exposure inhalational illness brought on by aerosolized B. anthracis.

• Diphtheria:

  • In order to avoid the carrier stage of diphtheria caused by susceptible Corynebacterium diphtheriae, it is used in conjunction with antitoxin.

• Subacute endocarditis:

  • Only in cases when group A streptococci-susceptible infections are particularly sensitive, penicillin G is given for the treatment of subacute bacterial endocarditis.

• Erysipeloid:

  • It is used to treat erysipeloid brought on by Erysipelothrix rhusiopathiae, a sensitive organism.

• Fusospirochetosis:

  • Penicillin G is useful for treating moderately severe oropharyngeal infections brought on by susceptible fusiform bacilli and spirochetes, as well as fusospirochetosis (Vincent gingivitis and pharyngitis) in conjunction with dental therapy.

• Pneumococcal infection:

  • Penicillin G can be used to treat respiratory tract infections brought on by susceptible pneumococci.
  • Use restrictions: Aqueous penicillin G is favoured for severe pneumococcal arthritis, empyema, bacteremia, pericarditis, meningitis, and peritonitis.

• Rat-bite fever:

  • It is used to treat rat-bite fever brought on by strains of the bacteria Streptobacillus moniliformis and Spirillum minus.

• Skin and soft tissue infection:

  • It can be used to treat moderately to severely severe infections of the skin and soft tissues brought on by susceptible staphylococci.

• Streptococcal infections:

  • Treatment of moderately severe to severe skin and soft tissue infections, erysipelas, scarlet fever, and upper respiratory tract infections brought on by susceptible streptococci (group A, without bacteremia).
  • Restrictions on use: Enterococcal group D is one of the more resistant streptococcal types. Streptococcal infections accompanied by bacteremia should be treated with aqueous penicillin.

• Syphilis:

  • It works well against all syphilis phases brought on by Treponema pallidum.

• Yaws, bejel, and pinta:

  • Treatment for susceptible organisms-caused yaws, bejel, and pinta.
  • Restrictions on use: When high, sustained serum levels are needed, administer aqueous penicillin G intravenously or intramuscularly (IM) (IV).
  • Useless when treating organisms that produce beta-lactamases, such as the majority of Neisseria gonorrhoea strains.

Procaine Penicillin G dose in Adults

Procaine Penicillin G dose in the treatment of Anthrax:

• Inhalational (post-exposure prophylaxis):

  • Every 12 hours, 1,200,000 intramuscular units

Note:

The overall treatment duration should be 60 days as this regime is not preffered. 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:

  • Daily 600,000 to 1,000,000 units intramuscularly

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

• Patients >10 kg:

  • For 2 weeks, 600,000 units intramuscularly on a daily basis

• Manufacturer's labeling:

  • Current clinical practise might not be reflected in the dosing in the prescribed information.
  • 300,000 to 600,000 units IM on daily basis

Procaine Penicillin G dose for the carrier state of Diphtheria:

• For 10 days, 300,000 units IM one time in a day
• Note: Penicillin G benzathine is preferred.

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

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

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

• Daily IM 600,000 to 1,000,000 units 

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

• Daily IM 600,000 to 1,000,000 units 

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

• For 10 days atleast, 600,000 to 1,000,000 units  IM daily 

Procaine Penicillin G dose in the treatment of Yaws:

• Daily IM 600,000 units

Note: Azithromycin is recommended and the recommended duration depends on the disease stage.

Procaine Penicillin G dose in Children

Procaine Penicillin G dose in children:

Note:

Despite being FDA-approved for some indications, dosage may not be offered if current recommendations do not support use, such as in the case of pharyngitis or pneumonia caused by streptococci or staphylococci.

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

• In divided doses IM 50,000 units/kg/day IM in divided doses for 12 to 24 hours.
• 1.2 million units/day is maximum daily dose

Dose for the postexposure prophylaxis of inhalational Anthrax:

Note: Penicillin G procaine is not a recommended regimen despite being FDA authorised.

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

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

• Patients ≤10 kg:

  • For 2 weeks, 300,000 units IM daily .

• Patients >10 kg:

  • For 2 weeks,, 600,000 units IM daily 

Procaine Penicillin G dose for the treatment of Syphilis:

• Congenital:

  • 10,000 days at 50,000 units/kg/day IM once daily.
  • The daily dosage cap is 2.4 million units.
  • In the event that more than one therapy day is missed, the complete course should be resumed.
  • Due to its low CNS penetration, penicillin G procaine is not the chosen treatment for HIV-positive patients.

• Neurosyphilis (including ocular or otic syphilis):

  • HIV-exposed/-positive:

    • Adolescents:
      • For 10 to 14 days, 2.4 million units  IM one time daily in combination with probenecid.

Pregnancy Risk Category: B

• Studies on animal reproduction did not show any adverse results.
• Although penicillin G crosses the placenta, there is no evidence that using it while pregnant increases the risk of unfavourable consequences on the foetus.
• 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:

  • If you have a history of procaine sensitivity or hypersensitivity, test with 0.01 mL of 1%/2% procaine solution.
  • 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
• mental status post injection
• Injection site reactions
• Prolonged therapy. with monthly hematological and renal function tests 

How to administer Procaine Penicillin G?

• Only deep IM injections should use procaine suspension.
• Rotate the area of injection.
• It should not be administered via any other route due to the risk of permanent neuro-vascular damage.

Mechanism of action of Procaine Penicillin:

• A penicillin called penicillin G procaine binds to one or more proteins that are penicillin-binding (PBPs).
• This prevents the last transpeptidation step in the production of peptidoglycans in bacterial cell walls, which prevents the formation of the cell wall.
• Due to the action of cell wall selflytic enzymes, this prevents the construction of the bacterial cell wall and results in bacterial lysis (autolysins or murein hydrolases).

Duration: Therapeutic: 15 to 24 hours

Absorption after Intramuscular administration is Slow

Distribution:Significantly more in the kidneys than in the liver, skin, or intestines. CSF has extremely low amounts.

Protein binding: 60%

The time to peak serum concentration: About 1 to 4 hours, and can last for 15 to 24 hours while staying within the therapeutic range.

Excretion: 60% to 90% of the unmodified medication is excreted in the urine; renal clearance is slowed in newborns, young infants, and people who have compromised 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: