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penicillin G procaine (Rx)Brand and Other Names:

 
 
 

Dosing & Uses

AdultPediatric

Dosing Form & 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

Dosing Form & 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

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Adverse 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

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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

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Pregnancy & 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.

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Pharmacology

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

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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

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Images

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Formulary

FormularyPatient Discounts

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The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

Tier Description
1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
NC NOT COVERED – Drugs that are not covered by the plan.
Code Definition
PA Prior Authorization
Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
QL Quantity Limits
Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
ST Step Therapy
Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
OR Other Restrictions
Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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