Dosing and uses of Penicillin G procaine
Adult dosage forms and strengths
injectable suspension
- 600,000 units/1mL syringe
- 1.2 million units/2mL syringe
Pneumonia
Indicated for moderately severe uncomplicated pneumococcal pneumonia
600,000-1,000,000 units IM qDay
Streptococcal Infections (Group A)
Indicated for moderately severe-to-severe tonsillitis, erysipelas, scarlet fever, upper respiratory tract, skin and soft tissue infections
600,000-1,000,000 units IM qDay for at least 10 days
Staphylococcal Infections
600,000-1,000,000 units IM qDay
Bacterial Endocarditis
Indicated only for treatment of extremely sensitive infections; not indicated for prophylaxis
600,000 -1,000,000 units IM qDay
Syphilis
Primary, secondary, and latent: 600,000 units IM qDay for 8 days
Late (tertiary and latent syphilis with positive spinal fluid): 600,000 units IM qDay for 10-15 days (total 6-9 million units)
Neurosyphilis: 2.4 million units IM qDay x10-14 days; administer with probenecid 500 mg PO QID (penicillin G aqueous preferred)
Anthrax
Cutaneous: 600,000-1,000,000 units IM qDay
Inhaled (post-exposure): 1.2 million units IM q12hr for up to 2 weeks, THEN switch to PO treatment (total treatment 60 days)
Diphtheria
Adjunct with antitoxin: 300,000-600,000 units IM qDay
Carrier state: 300,000 units IM qDay
Vincent’s Infection (fusospirochetosis)
600,000-1,000,000 units IM qDay
Erysipeloid
600,000-1,000,000 units IM qDay
Rat-Bite Fever
Indicated for Streptobacillus moniliformis and Spirillum minus (rat-bite fever)
600,000-1,000,000 units IM qDay
Whipple’s disease
1.2 million units IM qDay for 10-14 days; coadminister with streptomycin, THEn
Trimethoprim/sulfamethoxazole or doxycycline PO for 1 yr
Renal Impairment
CrCl 10-50 mL/min: Decrease dose by 25%
CrCl <10 mL/min: Decrease dose by 50-70%
Hemodialysis: Removed by hemodialysis; administer after dialysis
Other Indications & Uses
Indicated for susceptible microorganisms that respond to low and persistent penicillin G serum levels (if high, sustained serum levels required, use aqueous penicillin G IV/IM)
Streptococci Groups A, C, G, H, L, and M are sensitive (Group D, ie, enterococcus is resistant); aqueous penicillin G recommended for streptococcal bacteremia
Moderate/severe respiratory tracts infection caused by pneumococci (use aqueous penicillin G for acute stage of severe pneumonia, empyema, bacteremia, pericarditis, meningitis, peritonitis, or arthritis)
Moderate/severe skin infections caused by susceptible staphylococci
Susceptible fusiform bacilli and spirochetes (fusospirochetosis)
Syphilis (all stages) caused by susceptible Treponema pallidum
Yaws, Bejel, Pinta
C diphtheriae carrier stage
Anthrax
Rat-bite fever caused by Streptobacillus moniliformis and Spirillum minus
Erysipeloid caused by Erysipelothrix rhusiopathiae
Subacute bacterial endocarditis, only in extremely sensitive infections caused by susceptible Group A streptococci
Pediatric dosage forms and strengths
injectable suspension
- 600,000 units/1mL syringe
- 1.2 million units/2mL syringe
General Dosing for Infections
Infants/children: 25,000-50,000 units/kg/day Im
Avoid use in neonates; higher risk of abscess and procaine toxicity
Pneumonia
Indicated for pneumonia caused by streptococcal Group A and staphylococcal infections
<60 pounds: 300,000 units IM qDay
60 pounds or greater: As adults; 600,000 units IM qDay
Syphilis
Congenital Syphilis: <70 pounds: 50,000 units/kg IM qDay for 10 days
Primary, secondary, and latent (aged 12 years or older): As adults; 600,000 units IM qDay for 8 days
Anthrax
Inhaled (post-exposure): 25,000 units/kg IM q12hr for up to 2 weeks; not to exceed 1.2 million units q12hr, THEN switch to PO treatment (total treatment 60 days)
Renal Impairment
Not defined in children; see adult recommendations
Other Indications & Uses
Indicated for susceptible microorganisms that respond to low and persistent penicillin G serum levels (if high, sustained serum levels required, use aqueous penicillin G IV/IM)
Streptococci Groups A, C, G, H, L, and M are sensitive (Group D, ie, enterococcus is resistant); aqueous penicillin G recommended for streptococcal bacteremia
Moderate/severe respiratory tracts infection caused by pneumococci (use aqueous penicillin G for acute stage of severe pneumonia, empyema, bacteremia, pericarditis, meningitis, peritonitis, or arthritis)
Moderate/severe skin infections caused by susceptible staphylococci
Susceptible fusiform bacilli and spirochetes (fusospirochetosis)
Syphilis (all stages) caused by susceptible Treponema pallidum
Yaws, Bejel, Pinta C diphtheriae carrier stage
Anthrax
Rat-bite fever caused by Streptobacillus moniliformis and Spirillum minus
Penicillin G procaine adverse (side) effects
Frequency not defined
Skin rashes including maculopapular eruptions and exfoliative dermatitis
Urticaria
Serum-sicknesslike reactions (eg, chills, fever, edema, arthralgia, prostration)
Jarisch-Herxheimer reaction reported when treating syphilis
Pseudomembranous colitis
Warnings
Black box warnings
Prior to administration, carefully read the warnings, adverse reactions, and dosage and administration sections of the labeling
Contraindications
Hypersensitivity; serious and occasionally fatal reactions have been reported
Cautions
For deep IM administration only; do not administer IV, SC, or It
Do not inject near nerve or artery
No longer indicated for gonorrhea; should not be used for beta-lactamase producing organisms which include most strains of Neisseria gonorrhea
Pseudomembranous colitis reported with antibacterial agents, including penicillin g
Procaine reactions: Immediate toxic reactions to procaine reported, particularly when a large single dose is administered (4.8 million units); reaction manifested by mental disturbances including anxiety, confusion, agitation, depression, weakness, seizures, hallucinations, combativeness, and fear
Avoid use in neonates; increased risk for sterile abscess development and procaine toxicity
Pregnancy and lactation
Pregnancy category: B
Lactation: Excreted into breast milk, caution advised
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Penicillin G procaine
Half-Life: 20-30 minutes
Absorption: IM, slow absorption for up to 24 hr
Vd: 0.3-0.47 L/kg
Peak Plasma Time: 2-4 hr
Peak Plasma Concentration: 1.5 units/mL
Protein Bound: 60%
Metabolism: ~30% in liver
Excretion: urine (60-90% within 24-36 hr)
Mechanism of action
Interferes with cell wall mucopeptide synthesis during active multiplication, resulting in bactericidal activity against susceptible microorganisms
Administration
IM Administration
Do not inject near artery or nerve (may result in permanent neurologic damage)
Neonates, infants, small children: Midlateral aspect of thigh preferable
Older children and adults: Deep IM injection in upper outer quadrant of buttock
Because of high concentration of suspended matter, needle may be blocked if injection is not made at slow, steady rate
Storage
Store refrigerated at 2-8 degrees C (36-46 degrees F)
Do not freeze
