Version May 2024
Note: Penicillin G Procaine is no longer available in the United States.
Usual dosage range: IM: 600,000 to 1 million units daily; higher doses may be needed for some indications (eg, diphtheria, neurosyphilis).
Anthrax, cutaneous (without systemic involvement), treatment: Note: Consult public health officials for event-specific recommendations. A high index of suspicion for emergent beta-lactam resistance during therapy is warranted (Ref).
IM: 800,000 to 1 million units every 12 to 24 hours (Ref); duration is 7 to 10 days after naturally acquired infection and 60 days following biological weapon–related event (Ref). Note: Patients with extensive edema or cutaneous lesions of the head or neck should be treated with an IV regimen recommended for systemic infection (Ref).
Diphtheria, adjunctive therapy with antitoxin: IM: Patients >10 kg: 600,000 units every 12 hours for 14 days (including oral step-down therapy) (Ref).
Neurosyphilis (including ocular and otosyphilis) (alternative agent):
Note: Reserve for patients who are unable to receive IV therapy (Ref).
IM: 2.4 million units once daily with concomitant probenecid for 10 to 14 days; for late neurosyphilis (syphilis exposure >1 year ago), may consider administration of penicillin G benzathine following initial penicillin G procaine therapy to provide a comparable total duration of therapy for late syphilis (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no dosage adjustments provided in the manufacturer's labeling, however, excretion is delayed with impaired renal function and dosage adjustments may be necessary. Use with caution.
There are no dosage adjustments provided in the manufacturer's labeling.
Refer to adult dosing.
(For additional information see "Penicillin G procaine (intermediate-acting intramuscular) (United States: Not available): Pediatric drug information")
Note: Penicillin G Procaine is no longer available in the United States. Although FDA approved for some indications, dosing is not provided in some instances if current guidelines do not recommend use (eg, streptococcal or staphylococcal pneumonia and pharyngitis) (Ref).
General dosing (non-CNS infections): Infants, Children, and Adolescents: IM: 50,000 units/kg/day in divided doses every 12 to 24 hours; maximum daily dose: 1.2 million units/day (Ref).
Anthrax, inhalational (postexposure prophylaxis): Note: Although FDA approved, penicillin G procaine is not included in current guidelines (Ref).
Infants, Children, and Adolescents: IM: 25,000 units/kg/dose every 12 hours; maximum dose: 1.2 million units/dose. Overall treatment duration should be 60 days. Available safety data suggest continued administration of penicillin G procaine for longer than 2 weeks may incur additional risk for adverse reactions. Clinicians may consider switching to effective alternative treatment for completion of therapy beyond 2 weeks (Ref).
Diphtheria infection, adjunctive therapy with antitoxin (Ref):
Infants, Children, and Adolescents:
Patients ≤10 kg: IM: 300,000 units every 12 hours. Treat for 14 days total, including oral step-down therapy.
Patients >10 kg: IM: 600,000 units every 12 hours. Treat for 14 days total, including oral step-down therapy.
Syphilis (alternative agent): Note: Aqueous penicillin G is preferred due to better CNS penetration (Ref).
Congenital:
Infants and Children: IM: 50,000 units/kg/dose once daily for 10 days; maximum daily dose: 2.4 million units/day; if >1 day of therapy is missed, the entire course should be restarted (Ref).
Neurosyphilis (including ocular or otic syphilis): HIV-exposed/-infected:
Adolescents: IM: 2.4 million units once daily for 10 to 14 days in combination with probenecid (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no dosage adjustments provided in the manufacturer's labeling; however, excretion is delayed with impaired renal function and dosage adjustments may be necessary. Use with caution.
There are no dosage adjustments provided in the manufacturer's labeling.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Frequency not defined.
<1%, postmarketing, and/or case reports: Anaphylaxis, central nervous system toxicity, Clostridioides difficile colitis, exfoliative dermatitis, hypersensitivity reaction, Jarisch-Herxheimer reaction, maculopapular rash, serum sickness-like reaction, skin rash, urticaria
Hypersensitivity to any penicillin or any component of the formulation.
Concerns related to adverse effects:
• Anaphylactic/hypersensitivity reactions: Serious and occasionally severe or fatal hypersensitivity (anaphylactic) reactions have been reported in patients on penicillin therapy, especially with a history of beta-lactam hypersensitivity, and/or history of sensitivity to multiple allergens. Use with caution in asthmatic patients. If an allergic reaction occurs, discontinue therapy and institute appropriate supportive measures.
• Fibrosis and atrophy: Quadriceps femoris fibrosis and atrophy have been reported following repeated IM injections of penicillins into the anterolateral thigh.
• Methemoglobinemia: Has been reported with local anesthetics, including procaine; clinically significant methemoglobinemia requires immediate treatment along with discontinuation of the anesthetic and other oxidizing agents. Onset may be immediate or delayed (hours) after anesthetic exposure. Patients with G6PD deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, exposure to oxidizing agents or their metabolites, or infants <6 months of age are more susceptible and should be closely monitored for signs and symptoms of methemoglobinemia (eg, cyanosis, headache, rapid pulse, shortness of breath, lightheadedness, fatigue).
• Neurovascular damage: Avoid IV, intravascular, or intra-arterial administration since severe and/or permanent neurovascular damage (eg, transverse myelitis with permanent paralysis, gangrene requiring digit or proximal extremity amputation, necrosis and sloughing at and surrounding the injection site) may occur. These reactions have occurred following injection into the deltoid, thigh, or buttock areas. Other serious complications of suspected intravascular administration (eg, immediate distal and proximal pallor, mottling or cyanosis of the extremity around the injection site followed by bleb formation or severe edema requiring anterior and/or posterior compartment fasciotomy in the lower extremity) occur most often in infants and small children. If any evidence of blood supply compromise is noted, consult appropriate specialists promptly.
• Procaine neuropsychiatric reactions: Immediate toxic reactions (eg anxiety, confusion, agitation, depression, weakness, seizures, hallucinations, combativeness and expressed “fear of impending death”) have been reported. Mental disturbance reactions are more common in patients receiving a large single dose (eg 4.8 million units). Reactions are transient and last 15 to 30 minutes.
• Procaine sensitivity: If there is a history of hypersensitivity to procaine, test with 0.1 mL of 1% or 2% procaine solution. If erythema, wheal, flare, or eruption occurs, patient may be sensitive to procaine; do not use penicillin G procaine in these patients. Treat sensitivity with supportive measures, including antihistamines.
• Superinfection: Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea (CDAD) and pseudomembranous colitis; CDAD has been observed >2 months postantibiotic treatment.
Disease-related concerns:
• Renal impairment: Use with caution in patients with severe renal impairment; dosage adjustment may be necessary.
• Seizure disorders: Use with caution in patients with a history of seizure disorder; high levels, particularly in the presence of renal impairment, may increase risk of seizures.
Other warnings/precautions:
• Appropriate use: Do not use for the treatment of gonorrhea.
• Choice of preparation: Penicillin G procaine is not the same preparation as penicillin G benzathine-penicillin G procaine (eg, Bicillin C-R). Dispensing errors have occurred (CDC 2005).
• Prolonged use: Extended duration of therapy or use associated with high serum concentrations (eg, in renal insufficiency) may be associated with an increased risk for some adverse reactions (neutropenia, hemolytic anemia, serum sickness).
Avoid repeated IM injections into the anterolateral thigh since quadriceps femoris fibrosis and atrophy may occur.
Penicillin G Procaine is no longer available in the United States.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Suspension, Intramuscular:
Generic: 600,000 units/mL (1 mL [DSC], 2 mL [DSC])
Yes
Suspension (Penicillin G Procaine Intramuscular)
600000 units/mL (per mL): $55.14
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IM: Procaine suspension for deep IM injection only; rotate the injection site; do not administer IV, intravascularly, or intra-arterially since severe and/or permanent neurovascular damage may occur
IM: Procaine suspension is for deep IM injection only. Do not administer IV, intravascularly, intra-arterially, SUBQ, or near an artery or nerve; severe and/or permanent neurovascular damage has been reported. For neonates, infants, and small children, administer IM into the midlateral muscles of the thigh; quadriceps femoris and atrophy have been reported following repeated IM injections into the anterolateral thigh; for older pediatric patients and adolescents, administer into the upper outer quadrant of the buttocks. Inject at a slow, steady rate to avoid needle blockage; rotate injection sites.
Note: When high, sustained serum levels are required, use aqueous penicillin G, either IM or IV.
Anthrax: Treatment of anthrax due to Bacillus anthracis, including inhalational anthrax (post-exposure) to reduce the incidence or progression of the disease following exposure to aerosolized B. anthracis.
Diphtheria: As an adjunct to antitoxin for prevention of the carrier stage of diphtheria caused by susceptible Corynebacterium diphtheriae.
Endocarditis: Treatment of subacute bacterial endocarditis, only in extremely sensitive infections, due to susceptible Group A streptococci. Note: Penicillin G procaine is not included as an option in the American Heart Association infective endocarditis treatment guidelines (AHA [Baddour 2015]).
Erysipeloid: Treatment of erysipeloid caused by susceptible Erysipelothrix rhusiopathiae.
Fusospirochetosis: Treatment of 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: Treatment of moderately severe infections of the respiratory tract caused by susceptible pneumococci.
Limitations of use: Severe pneumonia, empyema, bacteremia, pericarditis, meningitis, peritonitis, and arthritis of pneumococcal etiology are better treated with aqueous penicillin G during the acute stage.
Rat bite fever: Treatment of rat bite fever caused by susceptible Streptobacillus moniliformis and Spirillum minus organisms.
Staphylococcal infections: Treatment of moderately severe infections of the skin and soft tissue due to susceptible staphylococci (penicillin G susceptible). Note: Because of increased staphylococcal resistance, determine susceptibility prior to use. Clinical practice guidelines also do not include penicillin G procaine as a treatment option for skin and soft tissue infection due to staphylococci (IDSA [Stevens 2014]).
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: Treatment of syphilis caused by susceptible Treponema pallidum. Note: Centers for Disease Control and Prevention guidelines only recommend penicillin G procaine, in combination with probenecid, as an alternative treatment for neurosyphilis (including ocular and otosyphilis) (CDC [Workowski 2021]).
Yaws, bejel, and pinta: Treatment of yaws, bejel, and pinta caused by susceptible organisms.
Penicillin may be confused with penicillAMINE
Penicillin G procaine may be confused with penicillin G benzathine, penicillin G (parenteral/aqueous), penicillin G procaine, penicillin V potassium
Wycillin may be confused with Bicillin
Substrate of OAT1/3
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Acemetacin: May increase the serum concentration of Penicillins. Risk C: Monitor therapy
Aminoglycosides: Penicillins may decrease the serum concentration of Aminoglycosides. Primarily associated with extended spectrum penicillins, and patients with renal dysfunction. Risk C: Monitor therapy
Bacillus clausii: Antibiotics may diminish the therapeutic effect of Bacillus clausii. Management: Bacillus clausii should be taken in between antibiotic doses during concomitant therapy. Risk D: Consider therapy modification
BCG (Intravesical): Antibiotics may diminish the therapeutic effect of BCG (Intravesical). Risk X: Avoid combination
BCG Vaccine (Immunization): Antibiotics may diminish the therapeutic effect of BCG Vaccine (Immunization). Risk C: Monitor therapy
Cholera Vaccine: Antibiotics may diminish the therapeutic effect of Cholera Vaccine. Management: Avoid cholera vaccine in patients receiving systemic antibiotics, and within 14 days following the use of oral or parenteral antibiotics. Risk X: Avoid combination
Dichlorphenamide: Penicillins may enhance the hypokalemic effect of Dichlorphenamide. Risk C: Monitor therapy
Fecal Microbiota (Live) (Oral): May diminish the therapeutic effect of Antibiotics. Risk X: Avoid combination
Fecal Microbiota (Live) (Rectal): Antibiotics may diminish the therapeutic effect of Fecal Microbiota (Live) (Rectal). Risk X: Avoid combination
Immune Checkpoint Inhibitors (Anti-PD-1, -PD-L1, and -CTLA4 Therapies): Antibiotics may diminish the therapeutic effect of Immune Checkpoint Inhibitors (Anti-PD-1, -PD-L1, and -CTLA4 Therapies). Risk C: Monitor therapy
Lactobacillus and Estriol: Antibiotics may diminish the therapeutic effect of Lactobacillus and Estriol. Risk C: Monitor therapy
Methotrexate: Penicillins may increase the serum concentration of Methotrexate. Risk C: Monitor therapy
Mycophenolate: Penicillins may decrease serum concentrations of the active metabolite(s) of Mycophenolate. This effect appears to be the result of impaired enterohepatic recirculation. Risk C: Monitor therapy
Probenecid: May increase the serum concentration of Penicillins. Risk C: Monitor therapy
Sodium Benzoate: Penicillins may diminish the therapeutic effect of Sodium Benzoate. Risk C: Monitor therapy
Sodium Picosulfate: Antibiotics may diminish the therapeutic effect of Sodium Picosulfate. Management: Consider using an alternative product for bowel cleansing prior to a colonoscopy in patients who have recently used or are concurrently using an antibiotic. Risk D: Consider therapy modification
Tetracyclines: May diminish the therapeutic effect of Penicillins. Risk C: Monitor therapy
Typhoid Vaccine: Antibiotics may diminish the therapeutic effect of Typhoid Vaccine. Only the live attenuated Ty21a strain is affected. Management: Avoid use of live attenuated typhoid vaccine (Ty21a) in patients being treated with systemic antibacterial agents. Postpone vaccination until 3 days after cessation of antibiotics and avoid starting antibiotics within 3 days of last vaccine dose. Risk D: Consider therapy modification
Vitamin K Antagonists (eg, warfarin): Penicillins may enhance the anticoagulant effect of Vitamin K Antagonists. Risk C: Monitor therapy
Penicillin G crosses the placenta.
Maternal use of penicillins has generally not resulted in an increased risk of adverse fetal effects.
Penicillin is widely used in pregnant women. Based on available data, penicillin is generally considered compatible for use during pregnancy (Ailes 2016; Bookstaver 2015; Crider 2009; Damkier 2019; Heinonen 1977; Lamont 2014; Muanda 2017a; Muanda 2017b).
Penicillin G procaine may be used in the treatment of syphilis during pregnancy (CDC [Workowski 2021]). Untreated maternal syphilis can cause congenital syphilis, which is associated with bone deformities, neurologic impairment, stillbirth, or neonatal death (USPSTF 2018). Symptoms of congenital syphilis may include hepatosplenomegaly, jaundice, nonimmune hydrops, pseudoparalysis of an extremity, rhinitis, or skin rash. The Centers for Disease Control and Prevention sexually transmitted diseases treatment guidelines provide recommendations for the treatment of syphilis in pregnant patients. The penicillin regimen (dose, duration, and preparation) for the treatment of pregnant patients is the same as for a nonpregnant patient and depends on the stage of syphilis; however, procaine penicillin is not a recommended agent in any of the penicillin regimens based on syphilis staging. Parenteral penicillin G is the only agent with documented efficacy in pregnancy. Patients who are allergic to penicillin should be desensitized and treated with penicillin. Pregnant patients being treated for latent syphilis must repeat the full course of therapy if any doses are missed. A Jarisch-Herxheimer reaction may occur in any patient within the first 24 hours of therapy, including pregnant patients. This reaction may induce early labor, fetal distress, or stillbirth (rare); however, it is not a reason to prevent or delay maternal therapy (CDC [Workowski 2021]).
Penicillin G procaine is also approved for the management of Bacillus anthracis; however, other agents are preferred for use in pregnant patients (Meaney-Delman 2014).
Penicillins are present in breast milk.
Concentrations of penicillin class antibiotics in breast milk are limited (Nau 1987). In general, antibiotics that are present in breast milk may cause nondose-related modification of bowel flora. Monitor infants for GI disturbances, such as thrush or diarrhea (WHO 2002).
Although the manufacturer recommends that caution be exercised when administering penicillin G procaine to breastfeeding patients, penicillin G procaine is considered compatible with breastfeeding when used in usual recommended doses (WHO 2002).
Hypersensitivity reactions with first dose, injection site reactions, mental status post injection, periodic renal and hematologic function tests with prolonged therapy.
Inhibits bacterial cell wall synthesis by binding to one or more of the penicillin-binding proteins (PBPs); which in turn inhibits the final transpeptidation step of peptidoglycan synthesis in bacterial cell walls, thus inhibiting cell wall biosynthesis. Bacteria eventually lyse due to ongoing activity of cell wall autolytic enzymes (autolysins and murein hydrolases) while cell wall assembly is arrested.
Duration: Therapeutic: 15 to 24 hours
Absorption: IM: Slow
Distribution: High distribution in kidneys, lesser amounts in liver, skin and intestines. Very small levels found in CSF.
Protein binding: 60%
Time to peak, serum: 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
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