Procaine Benzylpenicillin

These indications are based on manufacturer information for both originator and generic products. For product specific registered indications, please refer to product specific manufacturer information

Registered South African indications:

• Pneumococcal infections  of the middle ear
• Pneumococcal pneumonia
• Pneumococcal pharyngitis
• Pneumococcal endocarditis sensitive to penicillin
• Early primary, secondary or latent syphilis and prophylaxis of syphilis contacts

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients

Cautions

• Breastfeeding
• Severe renal impairment
• Seizure disorders
• Prolonged use

Forms avail. in SA and covered in this monograph: inj

Dosages below include:

• General dosing range
• South African registered indications and dosages
• Indications and dosages registered in other jurisdictions

Infections caused by: Most Gram-positive and Gram-negative aerobic cocci (excluding Enterococcus); Gram-positive anaerobic organisms; Some Gram-positive and Gram-negative bacilli (including C. diptheria, B. anthracis, Listeria spp., E. coli and P. mirabilis); Other, including: B. burgdorferi, T. pallidum and Leptospirae

General dosing range

• IM: 300 000 - 600 000U (three hundred thousand to six hundred thousand units), dly in divided doses

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Should be administered by deep intramuscular injection. Should NOT be given intravenously

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Specific doses based on individual indications

Please note that the dosages below should be used in combination with regional guidelines, taking into account local antibiotic sensitivities

South African registered indications and dosages

Penicillin sensitive streptococcal endocarditis

• IM: 1 200 000U (one million two hundred thousand units), 6hrly

Early syphilis
Prophylaxis of syphilis contacts

• IM: 2 400 000U (two million four hundred thousand units), dly

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Indications and dosages registered in other jurisdictions

Anthrax
- Post-exposure prophylaxis for inhalation

• IM: 1 200 000U (one million two hundred thousand units), 12hrly

Anthrax
- Treatment for cutaneous exposure

• IM: 600 000 - 1 000 000U (six hundred thousand to one million units), dly

Diphtheria
- Adjunctive therapy with antitoxin

•  IM: 300 000 - 600 000U (three hundred thousand to six hundred thousand units), dly; Treatment duration: 14 days

- Carrier state

• IM: 300 000U (three hundred thousand units), dly; Treatment duration: 10 days

Neurosyphilis

• IM: 600 000U (six hundred thousand units), dly; Treatment duration: 10-15 days 

Pneumococcal pneumonia
- Uncomplicated, moderately severe

• IM: 600 000 - 1 000 000U (six hundred thousand to one million units), dly

Streptococcal infections
- Group A, moderately severe to severe

• IM: 600 000 - 1 000 000U (six hundred thousand to one million units), dly; Treatment duration: 10 days

Yaws

• IM: 600 000U (six hundred thousand units), dly

Paed. forms avail. in SA and covered in this monograph: inj

Dosages below include:

• General dosing range
• South African Standard Treatment Guidelines indications and dosages
• Indications and dosages registered in other jurisdictions

Infections caused by: Most Gram-positive and Gram-negative aerobic cocci (excluding Enterococcus); Gram-positive anaerobic organisms; Some Gram-positive and Gram-negative bacilli (including C. diptheria, B. anthracis, Listeria spp., E. coli and P. mirabilis); Other, including: B. burgdorferi, T. pallidum and Leptospirae

General dosing range

• IM: 20 000 - 25 000U/kg (twenty thousand to twenty five thousand units per kilogram), dly in divided doses

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Should be administered by deep intramuscular injection. Should NOT be given intravenously

---

Specific doses based on individual indications

Please note that the dosages below should be used in combination with regional guidelines, taking into account local antibiotic sensitivities

South African Standard Treatment Guidelines indications and dosages

Early congenital syphilis
- Symptomatic baby

• IM: 50 000U/kg (fifty thousand units per kilogram), dly; Treatment duration: 10 days
  (STG, Paed. 2017)

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Indications and dosages registered in other jurisdictions

Diphtheria
- Adjunctive therapy with antitoxin

•  IM: 300 000 - 600 000U (three hundred thousand to six hundred thousand units), dly; Treatment duration: 14 days

- Carrier state

• IM: 300 000U (three hundred thousand units), dly; Treatment duration: 10 days

Pregnancy

• Safe; no evidence of risk in studies
• In animal reproduction studies, adverse events were not observed. Adverse effects on the foetus have not been observed following the administration of penicillin G procaine during pregnancy, although it crosses the placenta. Syphilis and Bacillus anthracis during pregnancy may be treated with penicillin G procaine, however, for the latter other agents are preferred during pregnancy

Breastfeeding

• Caution
• Penicillin G procaine is detectable in breast milk, therefore caution is recommended when administered to breastfeeding women. Modification of bowel flora and allergic sensitization are undesirable effects that may affect the nursing infant

Renal Impairment

• eGFR ≥11-89ml/min: No dose adjustment recommended
• eGFR <10ml/min: Caution; no dose adjustment recommended
  Only contraindicated in patients with a history of epilepsy and seizures
  Continued therapy for longer than 2 weeks may incur additional serious adverse reactions. Switch to an effective alternative treatment when >2 weeks of antimicrobial therapy is required

Hepatic Impairment

• No dose adjustment recommended

Elderly

• No dose adjustment recommended

Porphyria Information

• Not yet classified (NC)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Central nervous system stimulation
• Confusion
• Drowsiness
• Myoclonus
• Seizure 

Cardiovascular Disorders

• Cardiac conduction disturbance
• Cardiac insufficiency
• Thrombophlebitis
• Vasodilatation
• Vasculitis

Gastrointestinal Disorders

• Diarrhoea
• Nausea
• Heartburn
• Sore mouth
• Sore tongue
• Hairy tongue

Hepatobiliary Disorders

• Increase in hepatic enzymes

Genitourinary Disorders

•  Interstitial nephritis

Musculoskeletal Disorders

• Joint pains

Skin and Subcutaneous Tissue Disorders

• Exfoliative dermatitis
• Rash
• Urticaria
• Pain at injection site
• Sterile abscess at injection site

Immune, Blood and Lymphatic System Disorders

• Hemolytic anaemia
• Neutropenia
• Positive direct Coombs' test
• Anaphylactoid reaction
• Hypersensitivity reaction
• Serum sickness
• Jarisch-Herxheimer reaction
• Fever
• Eosinophilia

• Bacille Calmette-Guérin (BCG) immunotherapy
• Cholera vaccine
• Probenecid
• Sodium picosulfate
• Tetracycline deriviatives
• Typhoid vaccine

Specific cases may require

• Renal function
• Full blood count

Procaine benzylpenicillin disrupts bacterial cell wall synthesis by inhibiting the transpeptidation enzyme that crosslinks the peptide chains attached to the backbone of the peptidoglycan. Bacterial lysis then occurs due to the action of cell wall autolytic enzymes.

Spectrum of activity: Most Gram-positive and Gram-negative aerobic cocci (excluding Enterococcus); Gram-positive anaerobic organisms; Some Gram-positive and Gram-negative bacilli (including C. diptheria, B. anthracis, Listeria spp., E. coli and P. mirabilis); Other, including: B. burgdorferi, T. pallidum and Leptospirae

Injection (per ml) 300mg (300 000 units)

• Bio-Cillin (Biotech) 
• Procillin (Caps Pharma)