Penicillin G Procaine

Penicillin G Procaine should only be prescribed for the indications listed in this insert.

NOTE: This drug is no longer indicated in the treatment of gonorrhea.

Anaphylaxis

SERIOUS AND OCCASIONALLY FATAL HYPERSENSITIVITY (ANAPHYLACTIC) REACTIONS HAVE BEEN REPORTED IN PATIENTS ON PENICILLIN THERAPY. THESE REACTIONS ARE MORE LIKELY TO OCCUR IN INDIVIDUALS WITH A HISTORY OF PENICILLIN HYPERSENSITIVITY AND/OR A HISTORY OF SENSITIVITY TO MULTIPLE ALLERGENS. THERE HAVE BEEN REPORTS OF INDIVIDUALS WITH A HISTORY OF PENICILLIN HYPERSENSITIVITY WHO HAVE EXPERIENCED SEVERE REACTIONS WHEN TREATED WITH CEPHALOSPORINS. BEFORE INITIATING THERAPY WITH ANY PENICILLIN, CAREFUL INQUIRY SHOULD BE MADE CONCERNING PREVIOUS HYPERSENSITIVITY REACTIONS TO PENICILLINS, CEPHALOSPORINS, OR OTHER ALLERGENS. IF AN ALLERGIC REACTION OCCURS, THE DRUG SHOULD BE DISCONTINUED AND APPROPRIATE THERAPY INSTITUTED. SERIOUS ANAPHYLACTIC REACTIONS REQUIRE IMMEDIATE EMERGENCY TREATMENT WITH EPINEPHRINE. OXYGEN, INTRAVENOUS STEROIDS, AND AIRWAY MANAGEMENT, INCLUDING INTUBATION, SHOULD ALSO BE ADMINISTERED AS INDICATED.

Pseudomembranous Colitis

Pseudomembranous colitis has been reported with nearly all antibacterial agents, including penicillin G, and may range in severity from mild to life-threatening. Therefore, it is important to consider this diagnosis in patients who present with diarrhea subsequent to the administration of antibacterial agents.

Treatment with antibacterial agents alters the normal flora of the colon and may permit overgrowth of clostridium. Studies indicate that a toxin produced by Clostridium difficile is one primary cause of "antibiotic-associated colitis."

After the diagnosis of pseudomembranous colitis has been established, therapeutic measures should be initiated. Mild cases of pseudomembranous colitis usually respond to drug discontinuation alone. In moderate to severe cases, consideration should be given to management of fluids and electrolytes, protein supplementation and treatment with an antibacterial drug clinically effective against C. difficile colitis.

Procaine Reactions

Immediate toxic reactions to procaine may occur in some individuals, particularly when a large single dose is administered (4.8 million units). These reactions may be manifested by mental disturbances, including anxiety, confusion, agitation, depression, weakness, seizures, hallucinations, combativeness, and expressed "fear of impending death." The reactions noted in carefully controlled studies occurred in approximately one in 500 patients who received large doses of Penicillin G Procaine. Reactions are transient, lasting from 15 to 30 minutes.

Method of Administration

Do not inject into or near an artery or nerve.

Injection into or near a nerve may result in permanent neurological damage.

Inadvertent intravascular administration, including inadvertent direct intra-arterial injection or injection immediately adjacent to arteries, of Penicillin G Procaine Injectable Suspension and other penicillin preparations has resulted in severe neurovascular damage, including transverse myelitis with permanent paralysis, gangrene requiring amputation of digits and more proximal portions of extremities, and necrosis and sloughing at and surrounding the injection site. Such severe effects have been reported following injections into the buttock, thigh, and deltoid areas. Other serious complications of suspected intravascular administration which have been reported include immediate pallor, mottling, or cyanosis of the extremity, both distal and proximal to the injection site, followed by bleb formation; severe edema requiring anterior and/or posterior compartment fasciotomy in the lower extremity. The above-described severe effects and complications have most often occurred in infants and small children. Prompt consultation with an appropriate specialist is indicated if any evidence of compromise of the blood supply occurs at, proximal to, or distal to the site of injection.1–9 (See PRECAUTIONS, and  DOSAGE AND ADMINISTRATION.)

Quadriceps femoris fibrosis and atrophy have been reported following repeated intramuscular injections of penicillin preparations into the anterolateral thigh.

Do not inject into or near an artery or nerve. Injection into or near a nerve may result in permanent neurologic damage (see WARNINGS).

Penicillin G Procaine (aqueous) is for intramuscular injection only.

Administer by DEEP INTRAMUSCULAR INJECTION in the upper, outer quadrant of the buttock. In neonates, infants and small children, the midlateral aspect of the thigh may be preferable. When doses are repeated, vary the injection site.

Because of the high concentration of suspended material in this product, the needle may be blocked if the injection is not made at a slow, steady rate.

Pneumonia (pneumococcal), moderately severe (uncomplicated): 600,000 to 1,000,000 units daily.

Streptococcal infections (Group A), moderately severe to severe tonsillitis, erysipelas, scarlet fever, upper respiratory tract, skin and soft tissue: 600,000 to 1,000,000 units daily for 10-day minimum.

Staphylococcal infections, moderately severe to severe: 600,000 to 1,000,000 units daily.

In pneumonia, streptococcal (Group A) and staphylococcal infections in pediatric patients under 60 pounds: 300,000 units daily.

Bacterial endocarditis (Group A streptococci) only in extremely sensitive infections: 600,000 to 1,000,000 units daily.

Penicillin G Procaine is not recommended for prophylaxis against bacterial endocarditis. For prophylaxis against bacterial endocarditis in patients with congenital heart disease or rheumatic or other acquired valvular heart disease when undergoing dental procedures or surgical procedures of the upper respiratory tract, use penicillin V. For patients unable to take oral medications, aqueous penicillin G is recommended.

Syphilis

Primary, secondary, and latent with a negative spinal fluid in adults and pediatric patients over 12 years of age: 600,000 units daily for 8 days-total 4,800,000 units.

Late (tertiary, neurosyphilis, and latent syphilis with positive spinal-fluid examination or no spinal-fluid examination): 600,000 units daily for 10 to 15 days-total 6 to 9 million units.

Congenital syphilis under 70-lb. body weight: 50,000 units/kg/day for 10 days.

Yaws, Bejel, and Pinta: Treatment as for syphilis in corresponding stage of disease.

Diphtheria-adjunctive therapy with antitoxin: 300,000 to 600,000 units daily.

Diphtheria carrier state: 300,000 units daily for 10 days.

Anthrax-cutaneous: 600,000 to 1,000,000 units/day.

Anthrax-inhalational (post-exposure): 1,200,000 units every 12 hours in adults, 25,000 units per kilogram of body weight (maximum 1,200,000 unit) every 12 hours in children. The available safety data for Penicillin G Procaine at this dose would best support a duration of therapy of 2 weeks or less. Treatment for inhalational anthrax (post-exposure) must be continued for a total of 60 days. Physicians must consider the risks and benefits of continuing administration of Penicillin G Procaine for more than 2 weeks or switching to an effective alternative treatment.

Vincent's infection (fusospirochetosis): 600,000 to 1,000,000 units/day.

Erysipeloid: 600,000 to 1,000,000 units/day.

Streptobacillus moniliformis and Spirillum minus (rat-bite fever): 600,000 to 1,000,000 units/day.

Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.

NDC 60793-131-10
Contains 10 of NDC 60793-131-01

Ten Syringes (2 mL size)

Penicillin G Procaine
Injectable Suspension

1,200,000 units per 2 mL

FOR DEEP IM INJECTION ONLY

WARNING: NOT FOR INTRAVENOUS USE
BEFORE INJECTING, SEE PACKAGE INSERT FOR ADMINISTRATION INSTRUCTIONS.

Pfizer Injectables
Rx only

• APPG
• Aqueous Procaine Penicillin G
• Procaine Benzylpenicillin
• Procaine Penicillin G
• Wycillin

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.

Absorption

IM: Slow

Distribution

High distribution in kidneys, lesser amounts in liver, skin and intestines. Very small levels found in CSF.

Excretion

Urine (60% to 90% as unchanged drug); renal clearance is delayed in neonates, young infants, and patients with impaired renal function

Time to Peak

Serum: Within 1 to 4 hours and can persist within the therapeutic range for 15 to 24 hours

Therapeutic: 15 to 24 hours

Protein Binding

60%

Frequency not defined.

Cardiovascular: Cardiac conduction disturbance, cardiac insufficiency, thrombophlebitis, vasodilatation

Central nervous system: Central nervous system stimulation, confusion, drowsiness, myoclonus, seizure

Hematologic & oncologic: Hemolytic anemia, neutropenia, positive direct Coombs test

Hypersensitivity: Anaphylactoid reaction, hypersensitivity reaction, serum sickness

Immunologic: Jarisch-Herxheimer reaction

Local: Pain at injection site, sterile abscess at injection site

Renal: Interstitial nephritis

Hypersensitivity reactions with first dose, injection site reactions, mental status post injection, periodic renal and hematologic function tests with prolonged therapy.

Adverse events have not been observed in animal reproduction studies. Penicillin G crosses the placenta. Maternal use of penicillins has generally not resulted in an increased risk of adverse fetal effects. Penicillin G procaine may be used in the treatment of syphilis during pregnancy (consult current guidelines) (CDC [Workowski 2015]). Penicillin G procaine is also approved for the management of Bacillus anthracis, however other agents are preferred for use in pregnant women (Meaney-Delman 2014).

Procaine penicillin has been assigned to pregnancy category B by the FDA. Animal studies failed to reveal evidence of fetotoxicity or teratogenicity. Adverse effects have not been reported during human use; however, there are no controlled data in human pregnancies. Procaine penicillin is only recommended for use during pregnancy when benefit outweighs risk.

Penicillin is excreted into human milk. The manufacturer recommends that caution be used when administering penicillin to nursing women.

Allergic Reactions

Penicillin is a substance of low toxicity but does possess a significant index of sensitization. The following hypersensitivity reactions associated with use of penicillin have been reported: Skin rashes, ranging from maculopapular eruptions to exfoliative dermatitis; urticaria; serum-sicknesslike reactions, including chills, fever, edema, arthralgia, and prostration. Severe and often fatal anaphylaxis has been reported (see WARNINGS). As with other treatments for syphilis, the Jarisch-Herxheimer reaction has been reported.

Procaine toxicity manifestations and hypersensitivity reactions have been reported (see WARNINGS and PRECAUTIONS).

Gastrointestinal

Pseudomembranous colitis has been reported with the use of penicillin G. Onset of pseudomembranous colitis symptoms may occur during or after antibiotic treatment (see WARNINGS).

• Comvax
• Emtriva
• Epivir

• Grifulvin V
• Truvada
• Viread

© Penicillin G Procaine Patient Information is supplied by Cerner Multum, Inc. and Penicillin G Procaine Consumer information is supplied by First Databank, Inc., used under license and subject to their respective copyrights.