Penicillin G Benzathine
Medically reviewed by Drugs.com. Last updated on Nov 19, 2018.
(pen i SIL in jee BENZ a theen)
- Benzathine Benzylpenicillin
- Benzathine Penicillin G
- Benzylpenicillin Benzathine
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Bicillin L-A: 600,000 units/mL (1 mL); 1,200,000 units/2 mL (2 mL); 2,400,000 units/4 mL (4 mL) [contains methylparaben, propylparaben]
Brand Names: U.S.
- Bicillin L-A
- Antibiotic, Penicillin
Interferes with bacterial cell wall synthesis during active multiplication, causing cell wall death and resultant bactericidal activity against susceptible bacteria
Minimal concentrations attained in CSF with inflamed or uninflamed meninges; highest levels in the kidney; lesser amounts in liver, skin, intestines
Excreted by renal tubular excretion; penicillin G is detected in urine for up to 12 weeks after a single IM injection; renal clearance is delayed in neonates, young infants, and patients with impaired renal function
Time to Peak
Serum: Within 12 to 24 hours; serum levels are usually detectable for 1 to 4 weeks depending on the dose; larger doses result in more sustained levels rather than higher levels
Duration of Action
Dose dependent: 1 to 4 weeks; larger doses result in more sustained levels
Use: Labeled Indications
Acute glomerulonephritis: Prophylaxis (secondary) in patients with a history of acute glomerulonephritis
Respiratory tract infections: Treatment of mild to moderate upper respiratory tract infections (including pharyngitis) caused by streptococci susceptible to low, prolonged serum concentrations of penicillin G
Rheumatic fever and chorea: Prophylaxis (secondary) of rheumatic fever and/or chorea
Rheumatic heart disease: Prophylaxis (secondary) in patients with rheumatic heart disease
Syphilis and other venereal diseases: Treatment of syphilis, yaws, bejel, and pinta
Off Label Uses
Streptococcal (group A) chronic carriage
Based on the IDSA guidelines for diagnosis and management of group A streptococcal pharyngitis, penicillin G benzathine, in combination with rifampin, is an effective and recommended agent for the treatment of chronic group A streptococcus carriage.
Hypersensitivity to penicillin(s) or any component of the formulation
Usual dosage range: IM: 1.2 to 2.4 million units as a single dose
Streptococcus (group A):
Pharyngitis, acute treatment: IM: 1.2 million units as a single dose (AHA [Gerber 2009]; IDSA [Shulman 2012])
Secondary prophylaxis for rheumatic fever (prevention of recurrent attacks): IM: 1.2 million units once every 21 to 28 days. Duration depends on risk factors and presence of valvular heart disease (AHA [Gerber 2009]).
Manufacturer's labeling: Dosing in the prescribing information may not reflect current clinical practice. IM: 600,000 units every 2 weeks
Secondary prophylaxis of glomerulonephritis: IM: 1.2 million units every 4 weeks or 600,000 units twice monthly
Chronic carriage (off-label use): IM: 1.2 million units as a single dose in combination with oral rifampin. Note: Most individuals with chronic carriage do not require antibiotics (IDSA [Shulman 2012]).
Syphilis (CDC [Workowski 2015]):
Primary, Secondary, Early Latent (<1 year duration): IM: 2.4 million units as a single dose
Late Latent, Latent with unknown duration, or Tertiary Syphilis (with normal CSF examination): IM: 2.4 million units once weekly for 3 doses
Neurosyphilis (including Ocular Syphilis): Not indicated for initial treatment; aqueous penicillin G IV is preferred initial therapy (refer to Penicillin G Parenteral/Aqueous monograph for dosing). Following penicillin G IV initial treatment, may consider administration of penicillin G benzathine 2.4 million units IM once weekly for 3 weeks to provide a comparable total duration of therapy as for latent syphilis.
Yaws, bejel, and pinta: IM: 1.2 million units as a single dose
Refer to adult dosing.
Group A streptococcal upper respiratory infection (Gerber, 2009): Infants, Children, and Adolescents: IM:
Rheumatic fever, primary prevention:
≤27 kg: 600,000 units as a single dose
>27 kg: 1.2 million units as a single dose
Rheumatic fever, secondary prevention: Note: Duration of secondary rheumatic fever prophylaxis varies: Rheumatic fever with carditis and residual heart disease: 10 years or until 40 years of age (whichever is longer), sometimes lifelong prophylaxis; rheumatic fever with carditis but no residual heart disease: 10 years or until 21 years of age (whichever is longer); rheumatic fever without carditis: 5 years or until 21 years of age (whichever is longer)
≤27 kg: 600,000 units every 3-4 weeks
>27 kg: 1.2 million units every 3-4 weeks
Syphilis: (CDC, 2010; Red Book, 2012): Infants, Children, and Adolescents: IM
Primary, Secondary, or Early Latent (<1 year duration): 50,000 units/kg once; maximum dose: 2.4 million units
Late Latent or Latent with unknown duration: 50,000 units/kg once weekly for 3 doses; maximum dose: 2.4 million units
IM: Warm to room temperature before administration to lessen the pain associated with injection. Administer by deep IM injection in the upper outer quadrant of the buttock. 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 IV, intra-arterially, or SubQ.
Store 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).
Acemetacin: May increase the serum concentration of Penicillins. Monitor therapy
BCG (Intravesical): Antibiotics may diminish the therapeutic effect of BCG (Intravesical). Avoid combination
BCG Vaccine (Immunization): Antibiotics may diminish the therapeutic effect of BCG Vaccine (Immunization). 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. Avoid combination
Lactobacillus and Estriol: Antibiotics may diminish the therapeutic effect of Lactobacillus and Estriol. Monitor therapy
Methotrexate: Penicillins may increase the serum concentration of Methotrexate. 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. Monitor therapy
Probenecid: May increase the serum concentration of Penicillins. Management: Avoid the routine use of penicillins and probenecid, but this combination may be used advantageously in select cases with careful monitoring. Monitor for toxic effects of penicillins if probenecid is initiated or the dose is increased. Consider therapy modification
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. Consider therapy modification
Teriflunomide: May increase the serum concentration of OAT3 Substrates. Monitor therapy
Tetracyclines: May diminish the therapeutic effect of Penicillins. Consider therapy modification
Tolvaptan: May increase the serum concentration of OAT3 Substrates. 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 3 days after cessation of antibacterial agents. Consider therapy modification
Vitamin K Antagonists (eg, warfarin): Penicillins may enhance the anticoagulant effect of Vitamin K Antagonists. Monitor therapy
Positive Coombs' [direct], false-positive urinary and/or serum proteins; false-positive or negative urinary glucose using Clinitest®
Frequency not defined:
Cardiovascular: Cerebrovascular accident, hypotension, palpitations, syncope, tachycardia, vasodilatation, vasospasm, vasodepressor syncope
Central nervous system: Anxiety, coma, confusion, dizziness, drowsiness, euphoria, fatigue, headache, localized warm feeling, nervousness, neurologic abnormality (neurogenic bladder), numbness, pain, seizure, transverse myelitis
Dermatologic: Diaphoresis, gangrene of skin or other tissue, pallor, skin mottling, skin ulceration at injection site
Gastrointestinal: Bloody stools, intestinal necrosis, nausea, vomiting
Genitourinary: Hematuria, impotence, priapism, proteinuria
Hematologic & oncologic: Local hemorrhage (at injection site), lymphadenopathy
Hepatic: Increased serum AST
Hypersensitivity: Hypersensitivity reaction
Immunologic: Jarisch-Herxheimer reaction
Local: Abscess at injection site, atrophy at injection site, bruising at injection site, cellulitis at injection site, localized edema (at injection site), inflammation at injection site, injection site reaction (neurovascular damage), pain at injection site, residual mass at injection site, tissue necrosis at injection site
Neuromuscular & skeletal: Arthropathy, exacerbation of arthritis, periosteal disease (periostitis), rhabdomyolysis, tremor, weakness
Ophthalmic: Blindness, blurred vision
Renal: Increased blood urea nitrogen, increased serum creatinine, myoglobinuria, renal failure
Concerns related to adverse effects:
• 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 (including cephalosporins), history of sensitivity to multiple allergens, or previous IgE-mediated reactions (eg, anaphylaxis, angioedema, urticaria). Serious anaphylactic reactions require immediate emergency treatment with epinephrine, oxygen, intravenous steroids and airway management (including intubation) as indicated.
• 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.
• 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 for the initial treatment regimen for congenital syphilis or neurosyphilis due to reported treatment failures and lack of published clinical data on its efficacy (CDC [Workowski 2015]).
• Appropriate administration: [US Boxed Warning]: Not for intravenous use; cardiopulmonary arrest and death have occurred from inadvertent IV administration. Administer by deep IM injection only. Quadriceps femoris fibrosis and atrophy have been reported after repeated IM injections of penicillin preparations into the anterolateral thigh. Injection into or near an artery or nerve could result in severe neurovascular damage or permanent neurological damage.
• Appropriate use: Use only for treatment of infections due to penicillin G sensitive gram positive organisms, few gram-negative organisms such as Neisseria gonorrhoeae, and some anaerobes and spirochetes. Use only for infections susceptible to the low and very prolonged serum concentrations of benzathine penicillin G.
• 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).
Observe for signs and symptoms of anaphylaxis during first dose
Adverse events have not been observed in animal reproduction studies. Penicillin G benzathine crosses the placenta (Nathan 1993; Weeks 1997). Maternal use of penicillins has generally not resulted in an increased risk of adverse fetal effects. Penicillin G is the drug of choice for treatment of syphilis during pregnancy (CDC [Workowski 2015]).
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience headache, nausea, vomiting, tremors, fatigue, or diarrhea. Have patient report immediately to prescriber signs of kidney problems (urinary retention, hematuria, change in amount of urine passed, or weight gain); chills; edema; joint pain; severe dizziness; passing out; severe loss of strength and energy; bruising; bleeding; angina; tachycardia; abnormal heartbeat; shortness of breath; signs of severe cerebrovascular disease (change in strength on one side is greater than the other, difficulty speaking or thinking, change in balance, or vision changes); black, tarry, or bloody stools; severe abdominal pain; swollen glands; confusion; anxiety; seizures; sweating a lot; vision changes; sexual dysfunction; priapism; injection site lump, scab, hardness, or irritation; numbness; tingling; weakness; or signs of Clostridium difficile (C. diff)-associated diarrhea (abdominal pain or cramps, severe diarrhea or watery stools, or bloody stools) (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
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- Drug class: natural penicillins