Penicillin G benzathine

Penicillin G benzathine is a slow-onset antibiotic that fights bacteria in your body.

Penicillin G benzathine is used to treat many different types of severe infections, including strep infections, rheumatic fever, and syphilis.

Penicillin G benzathine may also be used for purposes not listed in this medication guide.

You should not receive this medication if you are allergic to penicillin. Tell your doctor if you have ever had an allergic reaction to a cephalosporin antibiotic such as Ceftin, Cefzil, Omnicef, Keflex, and others.

Before you receive penicillin G benzathine, tell your doctor if you have asthma or a history of allergies, liver disease, kidney disease, or heart disease.

Be sure to receive all doses your doctor has prescribed. Your symptoms may get better before the infection is completely cleared.

After you have finished your treatment with penicillin G benzathine, your doctor may want to do tests to make sure your infection has completely cleared up.

You should not receive this medication if you are allergic to penicillin. Tell your doctor if you have ever had an allergic reaction to a cephalosporin antibiotic such as cefdinir (Omnicef), cefprozil (Cefzil), cefuroxime (Ceftin), cephalexin (Keflex), and others.

To make sure penicillin G benzathine is safe for you, tell your doctor if you have:

• asthma or a history of allergies;
• liver disease;
• kidney disease; or
• heart disease.

FDA pregnancy category B. This medication is not expected to be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment.

Penicillin G benzathine can pass into breast milk and may harm a nursing baby. Tell your doctor if you are breast-feeding a baby.

Penicillin G benzathine is a prescription medication used to treat bacteria that cause infections of the upper airways, heart valves, joints, skin, brain, and the genital areas. Penicillin G benzathine belongs to a group of drugs called penicillin antibiotics, which help stop the growth of bacteria.

This medication is available in an injectable form to be given directly into a muscle (IM) by a healthcare professional.

Common side effects include an allergic reaction, pain at the site of injection, and upset stomach.

WARNING: NOT FOR INTRAVENOUS USE. DO NOT INJECT INTRAVENOUSLY OR ADMIX WITH OTHER INTRAVENOUS SOLUTIONS. THERE HAVE BEEN REPORTS OF INADVERTENT INTRAVENOUS ADMINISTRATION OF PENICILLIN G BENZATHINE, WHICH HAS BEEN ASSOCIATED WITH CARDIORESPIRATORY ARREST AND DEATH.

Tell your doctor about all medicines you use, and those you start or stop using during your treatment with penicillin G benzathine, especially:

• methotrexate;

• probenecid;

• birth control pills;

• a blood thinner such as warfarin (Coumadin, Jantoven); or

• a blood thinner such as warfarin, Coumadin; or

• a tetracycline antibiotic--doxycycline, minocycline, tetracycline.

This list is not complete. Other drugs may interact with penicillin G benzathine, including prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide.

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
• Any unexplained bruising or bleeding.
• Redness or swelling where the shot is given.
• It is common to have diarrhea when taking penicillin G benzathine. Rarely, a very bad form of diarrhea called Clostridium difficile (C diff)–associated diarrhea (CDAD) may occur. Sometimes, this has led to a deadly bowel problem (colitis). CDAD may happen while you are taking this medicine or within a few months after you stop taking it. Call your doctor right away if you have stomach pain or cramps, very loose or watery stools, or bloody stools. Do not try to treat loose stools without first checking with your doctor.

• Benzathine Benzylpenicillin
• Benzathine Penicillin G
• Benzylpenicillin Benzathine

Interferes with bacterial cell wall synthesis during active multiplication, causing cell wall death and resultant bactericidal activity against susceptible bacteria

Absorption

IM: Slow

Distribution

Minimal concentrations attained in CSF with inflamed or uninflamed meninges; highest levels in the kidney; lesser amounts in liver, skin, intestines

Excretion

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

Acute glomerulonephritis: Prophylaxis (secondary) in patients with a history of acute glomerulonephritis

Respiratory tract infections: Treatment of mild to moderate upper respiratory tract infections 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

Usual dosage range: IM: 1.2 to 2.4 million units as a single dose

Upper respiratory infection, group A streptococci: IM: 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 to 4 weeks or 600,000 units twice monthly (Gerber, 2009)

Pharyngitis, group A streptococci (IDSA guidelines): IM:

Acute treatment: 1.2 million units as a single dose (Shulman, 2012)

Chronic carrier treatment: 1.2 million units as a single dose in combination with oral rifampin (Shulman, 2012)

Syphilis (CDC [Workowski 2015]): IM:

Primary, Secondary, Early Latent (<1 year duration): 2.4 million units as a single dose

Late Latent, Latent with unknown duration, or Tertiary Syphilis (with normal CSF examination): 2.4 million units once weekly for 3 doses

Neurosyphilis (including Ocular Syphilis): Not indicated for use; aqueous penicillin G IV is preferred initial therapy (refer to Penicillin G Parenteral/Aqueous monograph for dosing) but consideration may be given to administering 2.4 million units IM once weekly for 3 weeks following IV treatment to provide a comparable total duration of therapy as latent syphilis

Yaws, bejel, and pinta: IM: 1.2 million units as a single dose

Usual dosage range: IM: 50,000 units/kg as a single dose (maximum: 2.4 million units)

Upper respiratory infection, group A streptococci (eg, pharyngitis): Infants and Children: IM: Manufacturer's labeling:

<27.3 kg: 300,000 to 600,000 units as a single dose. Manufacturer labeling does not provide specific recommendation for children ≥27.3 kg.

For older children, a dose of 900,000 units as a single dose is recommended.

Primary prevention of rheumatic fever: Infants and Children: IM: ≤27 kg: 600,000 units as a single dose; >27 kg: 1.2 million units as a single dose (Gerber, 2009)

Secondary prevention of rheumatic fever: Infants and Children: IM: ≤27 kg: 600,000 units every 3-4 weeks; >27 kg: 1.2 million units every 3 to 4 weeks (Gerber, 2009)

Pharyngitis, group A streptococci (IDSA guidelines): Infants and Children: IM:

Acute treatment: <27 kg: 600,000 units as a single dose; ≥27 kg: 1.2 million units as a single dose (Shulman, 2012)

Chronic carrier treatment: <27 kg: 600,000 units as a single dose (in combination with oral rifampin); ≥27 kg: 1.2 million units as a single dose (in combination with oral rifampin) (Shulman, 2012)

Syphilis (off-label population; CDC [Workowski 2015]): IM:

Primary, Secondary, and Early Latent (<1 year duration): Infants and Children: 50,000 units/kg/dose as a single injection (maximum: 2.4 million units/dose)

Late Latent: Infants and Children: 50,000 units/kg/dose every week for 3 doses (maximum: 2.4 million units/dose)

Positive Coombs' [direct], false-positive urinary and/or serum proteins; false-positive or negative urinary glucose using Clinitest®

1.2 million units IM as a single dose

Uses: For the treatment of mild to moderate upper respiratory tract infections (URTIs) due to susceptible group A streptococci (e.g., pharyngitis); for the treatment of URTIs (pharyngitis) due to group A streptococci (without bacteremia)

Infectious Diseases Society of America (IDSA) and American Heart Association (AHA) recommendations: 1.2 million units IM as a single dose

Comments:
-Preferred for patients with group A streptococcal pharyngitis who are considered unlikely to complete 10 days of oral therapy
-IDSA: This drug plus 4 days of oral rifampin are recommended for chronic carriers of group A streptococci.
-AHA: Recommended for the treatment of streptococcal tonsillopharyngitis (primary prevention of rheumatic fever)
-Current guidelines should be consulted for additional information.

2.4 million units IM as a single dose

Uses: For the treatment of primary, secondary, and latent syphilis

US CDC recommendations:
-Primary, secondary, and early latent syphilis: 2.4 million units IM as a single dose
-Retreatment of primary or secondary syphilis (without neurosyphilis): 2.4 million units IM once a week for 3 weeks
-Late latent syphilis or latent syphilis of unknown duration: 2.4 million units IM once a week for 3 weeks (total dose: 7.2 million units)

Comments:
-A second dose (2.4 million units IM) can be administered 1 week after the initial dose to pregnant women with primary, secondary, or early latent syphilis.
-The patient's sexual partner(s) should also be evaluated/treated.
-Current guidelines should be consulted for additional information.

1.2 million units IM as a single dose

Data not available