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ALERT: U.S. Boxed Warning
The FDA-approved labeling includes a boxed warning. See Warnings/Precautions section for a concise summary of this information. For verbatim wording of the boxed warning, consult the product labeling or www.fda.gov.
Pronunciation
(pen i SIL in jee BENZ a theen)
Generic Available (U.S.)
No
Index Terms
Brand Names: U.S.
Brand Names: Canada
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Active against some gram-positive organisms, few gram-negative organisms such as Neisseria gonorrhoeae, and some anaerobes and spirochetes; used in the treatment of syphilis; used only for the treatment of mild to moderately-severe upper respiratory tract infections caused by organisms susceptible to low concentrations of penicillin G or for prophylaxis of infections caused by these organisms; primary and secondary prevention of rheumatic fever
Pregnancy Risk Factor
B
Pregnancy Considerations
Adverse events have not been observed in animal studies; therefore, penicillin G is classified as pregnancy category B. Penicillin crosses the placenta and distributes into amniotic fluid. There is no evidence of adverse fetal effects after penicillin use during pregnancy in humans. Penicillin G is the drug of choice for treatment of syphilis during pregnancy.
Lactation
Enters breast milk/use caution
Breast-Feeding Considerations
Penicillins are excreted in breast milk. The manufacturer recommends that caution be exercised when administering penicillin to nursing women. Nondose-related effects could include modification of bowel flora and allergic sensitization.
Contraindications
Hypersensitivity to penicillin(s) or any component of the formulation
Warnings/Precautions
Boxed warnings:
• Appropriate administration: See “Other warnings/precautions” below.
Concerns related to adverse effects:
• Anaphylactoid/hypersensitivity reactions: Serious and occasionally severe or fatal hypersensitivity (anaphylactoid) reactions have been reported in patients on penicillin therapy, especially with a history of beta-lactam hypersensitivity, history of sensitivity to multiple allergens, or previous IgE-mediated reactions (eg, anaphylaxis, angioedema, urticaria). Use with caution in asthmatic patients.
• 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 renal impairment.
• 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.
• Syphilis/neurosyphilis use: CDC and AAP do not currently recommend the use of penicillin G benzathine to treat congenital syphilis or neurosyphilis due to reported treatment failures and lack of published clinical data on its efficacy.
Other warnings/precautions:
• Appropriate administration: [U.S. Boxed Warning]: Not for intravenous use; cardiopulmonary arrest and death have occurred from inadvertent I.V. administration. Administer by deep I.M. injection only. Injection into or near an artery or nerve could result in severe neurovascular damage or permanent neurological damage.
• 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).
Adverse Reactions
Frequency not defined.
Cardiovascular: Cardiac arrest, cerebral vascular accident, cyanosis, gangrene, hypotension, pallor, palpitations, syncope, tachycardia, vasodilation, vasospasm, vasovagal reaction
Central nervous system: Anxiety, coma, confusion, dizziness, euphoria, fatigue, headache, nervousness, pain, seizure, somnolence
In addition, a syndrome of CNS symptoms has been reported which includes: Severe agitation with confusion, hallucinations (auditory and visual), and fear of death (Hoigne's syndrome); other symptoms include cyanosis, dizziness, palpitations, psychosis, seizures, tachycardia, taste disturbance, tinnitus
Gastrointestinal: Bloody stool, intestinal necrosis, nausea, vomiting
Genitourinary: Impotence, priapism
Hepatic: AST increased
Local: Injection site reactions: Abscess, atrophy, bruising, cellulitis, edema, hemorrhage, inflammation, lump, necrosis, pain, skin ulcer
Neuromuscular & skeletal: Arthritis exacerbation, joint disorder, neurovascular damage, numbness, periostitis, rhabdomyolysis, transverse myelitis, tremor, weakness
Ocular: Blindness, blurred vision
Renal: BUN increased, creatinine increased, hematuria, myoglobinuria, neurogenic bladder, proteinuria, renal failure
Miscellaneous: Diaphoresis, hypersensitivity reactions, Jarisch-Herxheimer reaction, lymphadenopathy, mottling, warmth
Metabolism/Transport Effects
None known.
Drug Interactions
BCG: Antibiotics may diminish the therapeutic effect of BCG. Risk X: Avoid combination
Fusidic Acid: May diminish the therapeutic effect of Penicillins. Risk D: Consider therapy modification
Methotrexate: Penicillins may decrease the excretion 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
Tetracycline Derivatives: May diminish the therapeutic effect of Penicillins. Risk D: Consider therapy modification
Typhoid Vaccine: Antibiotics may diminish the therapeutic effect of Typhoid Vaccine. Only the live attenuated Ty21a strain is affected. Management: Vaccination with live attenuated typhoid vaccine (Ty21a) should be avoided in patients being treated with systemic antibacterial agents. Use of this vaccine should be postponed until at least 24 hours after cessation of antibacterial agents. Risk D: Consider therapy modification
Vitamin K Antagonists (eg, warfarin): Penicillins may enhance the anticoagulant effect of Vitamin K Antagonists. Risk C: Monitor therapy
Storage
Refrigerate at 2°C to 8°C (36°F to 46°F); do not freeze. The following stability information has also been reported: May be stored at 25°C (77°F) for 7 days (Cohen, 2007).
Mechanism of Action
Interferes with bacterial cell wall synthesis during active multiplication, causing cell wall death and resultant bactericidal activity against susceptible bacteria
Pharmacodynamics/Kinetics
Duration: 1-4 weeks (dose dependent); larger doses result in more sustained levels
Distribution: Highest levels in the kidney; lesser amounts in liver, skin, intestines
Protein Binding: ~60%
Absorption: I.M.: Slow
Time to peak, serum: 12-24 hours
Dosage
Note: Administer undiluted injection; higher doses result in more sustained rather than higher levels. Use a penicillin G benzathine-penicillin G procaine combination to achieve early peak levels in acute infections.
Usual dosage range:
Children: I.M.: 25,000-50,000 units/kg as a single dose (maximum: 2.4 million units)
Adults: I.M.: 1.2-2.4 million units as a single dose
Indication-specific dosing:
Infants and Children: I.M.:
Group A streptococcal upper respiratory infection:
Primary prevention of rheumatic fever (Gerber, 2009): ≤27 kg: 600,000 units as a single dose; >27 kg: 1.2 million units as a single dose
Secondary prevention of rheumatic fever (Gerber, 2009): ≤27 kg: 600,000 units every 3-4 weeks; >27 kg: 1.2 million units every 3-4 weeks
Syphilis (CDC, 2010):
Primary, Secondary, Early Latent (<1 year duration): Infants and Children: I.M.: 50,000 units/kg as a single injection (maximum: 2.4 million units)
Late Latent, Latent with unknown duration: Children: I.M.: 50,000 units/kg every week for 3 doses (maximum: 2.4 million units/dose)
Adults: I.M.:
Group A streptococcal upper respiratory infection: 1.2 million units as a single dose
Secondary prevention of glomerulonephritis: 1.2 million units every 4 weeks or 600,000 units twice monthly
Secondary prevention of rheumatic fever: 1.2 million units every 3-4 weeks or 600,000 units twice monthly
Syphilis (CDC, 2010):
Primary, Secondary, Early Latent (<1 year duration): 2.4 million units as a single dose in 2 injection sites
Late Latent, Latent with unknown duration: 2.4 million units in 2 injection sites once weekly for 3 doses
Neurosyphilis: Not indicated as single-drug therapy, but may be given once weekly for 3 weeks following I.V. treatment; refer to Penicillin G Parenteral/Aqueous monograph for dosing
Administration: I.M.
Warm to room temperature before administration to lessen the pain associated with injection. Administer by deep I.M. injection in the upper outer quadrant of the buttock; in children <2 years of age, I.M. injections should be made into the midlateral muscle of the thigh, not the gluteal region. Do not inject near an artery or a nerve; permanent neurological damage or gangrene may result. When doses are repeated, rotate the injection site. Do not administer I.V., intra-arterially, or SubQ.
Monitoring Parameters
Observe for signs and symptoms of anaphylaxis during first dose
Test Interactions
Positive Coombs' [direct], false-positive urinary and/or serum proteins; false-positive or negative urinary glucose using Clinitest®
Patient Education
This drug can only be given by injection. Report immediately any redness, swelling, burning, or pain at injection site or any signs of allergic reaction (eg, respiratory difficulty or swallowing, chest tightness, rash, hives, swelling of lips or mouth). Maintain adequate hydration unless instructed to restrict fluid intake. If being treated for sexually-transmitted disease, partner will also need to be treated. May cause confusion or drowsiness. Report persistent adverse effects or signs of opportunistic infection (eg, fever, chills, diarrhea, unhealed sores, white plaques in mouth or vagina, purulent vaginal discharge).
Geriatric Considerations
Not indicated as single drug therapy for neurosyphilis, but may be given 1 time/week for 3 weeks following I.V. treatment with Penicillin G (Parenteral/Aqueous). No adjustment for renal function or age is necessary.
Dental Health: Effects on Dental Treatment
No significant effects or complications reported
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
May rarely cause drowsiness or confusion; penicillins reported to cause apprehension, illusions, hallucinations, depersonalization, agitation, insomnia, and encephalopathy
Mental Health: Effects on Psychiatric Treatment
None reported
Nursing: Physical Assessment/Monitoring
Assess results of culture and sensitivity tests and patient's allergy history prior to starting therapy. Use with caution in presence of impaired renal function or history of seizures. Monitor for hypersensitivity reactions and opportunistic infection.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, suspension:
Bicillin® L-A: 600,000 units/mL (1 mL, 2 mL, 4 mL)
Pricing: U.S. (www.drugstore.com)
Suspension (Bicillin L-A)
2400000 units/4 mL (4): $89.99
References
Centers for Disease Control and Prevention, “Guidelines for Prevention and Treatment of Opportunistic Infections in HIV-Infected Adults and Adolescents,” MMWR Recomm Rep, 2009, 58(RR-4):1-207. Available at http://aidsinfo.nih.gov/contentfiles/Adult_OI_041009.pdf
Centers for Disease Control and Prevention (CDC), "Sexually Transmitted Diseases Treatment Guidelines, 2010," MMWR Recomm Rep, 2010, 59(RR-12):1-110.
Centers for Disease Control and Prevention, “Sexually Transmitted Diseases Treatment Guidelines, 2006,” MMWR Recomm Rep, 2009, 55(RR-11):1-94.
Cohen V, Jellinek SP, Teperikidis L, et al, “Room-Temperature Storage of Medications Labeled for Refrigeration,” Am J Health-Syst Pharm, 2007, 64(16):1711-15.
Collart P, Poitevin M, Milovanovic A, et al, “Kinetic Study of Serum Penicillin Concentrations After Single Doses of Benzathine and Benethamine Penicillins in Young and Old People,” Br J Vener Dis, 1980, 56(6):355-62.
Gerber MA, Baltimore RS, Eaton CB, et al, “Prevention of Rheumatic Fever and Diagnosis and Treatment of Acute Streptococcal Pharyngitis: A Scientific Statement From the American Heart Association Rheumatic Fever, Endocarditis, and Kawasaki Disease Committee of the Council on Cardiovascular Disease in the Young, the Interdisciplinary Council on Functional Genomics and Translational Biology and the Interdisciplinary Council on Quality of Care and Outcomes Research: Endorsed by the American Academy of Pediatrics,” Circulation, 2009, 119(11):1541-51.
Gould FK, Denning DW, Elliott TS, et al, “Guidelines for the Diagnosis and Antibiotic Treatment of Endocarditis in Adults: A Report of the Working Party of the British Society for Antimicrobial Chemotherapy,” J Antimicrob Chemother, 2012, 67(2):269-89.
Kaplan EL, Berrios X, Speth J, et al, “Pharmacokinetics of Benzathine Penicillin G: Serum Levels During the 28 Days After Intramuscular Injection of 1,200,000 Units,” J Pediatr, 1989, 115(1):146-50.
International Brand Names
Lexi-Comp.com
Last full review/revision January 2012
Content last modified January 2012
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