penicillin G benzathine (Rx)

Brand and Other Names:Bicillin LA, Permapen
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Dosing & Uses

AdultPediatric

Dosing Form & Strengths

injectable suspension

  • 600,000 units/1mL
  • 1.2 million units/2mL
  • 2.4 million units/4mL

Group A Streptococcal Respiratory Infections

1.2 million U IM x1

Rheumatic Fever Prophylaxis

Acute attack: 1.2 million U IM monthly, OR

600,000 U IM q2Weeks

Syphilis

Primary or secondary (CDC Guidelines 2006)

  • 2.4 million U IM x1
  • If pregnant: 2.4 million U IM qWeek x2, recommended
  • If HIV+: 2.4 million U IM qWeek x 3, recommended

Early Latent: 2.4 million U IM x1

Neurosyphilis: 2.4 million U IM qWeek x 3

Yaw, Bejel, & Pinta

1.2 million U IM x1

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

Dosing Form & Strengths

injectable suspension

  • 600,000 units/1mL syringe
  • 1.2 million units/2mL syringe
  • 2.4 million units/4mL syringe

Group A Streptococcal Infections

<27 kg: 600,000 U IM x1 (AHA guidelines 2009)

27 kg or greater: 1.2 million U IM x1 (AHA guidelines 2009)

Rheumatic Fever, Prophylaxis

<27 kg: 600,000 U IM q4Weeks; high-risk patients q3Weeks (AHA guidelines 2009)

27 kg or greater: 1.2 million U IM q4Weeks; high-risk patients q3Weeks (AHA guidelines 2009)

Syphilis

Congenital (<2 years old): 50,000 U/kg IM x 1 dose

Early: 50,000 U/kg IM x 1 dose; not to exceed 2.4 million units/dose

>1 year duration: 50,000 U/kg qWeek x3 weeks; not to exceed 2.5 million units/dose

Renal Impairment

Not defined in children; see adult recommendations

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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

Not for IV use

Do not inject IV or admix with other IV solutions

Inadvertent intravenous administration, which has been associated with cardiorespiratory arrest and death reported; do not inject drug intravenously or admix with other intravenous solutions

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

Severe cutaneous adverse reactions (SCAR), such as Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), drug reaction with eosinophilia and systemic symptoms (DRESS), and acute generalized exanthematous pustulosis (AGEP) reported in patients taking beta-lactam antibiotics; discontinue therapy when SCAR suspected; consider an alternative treatment

Pseudomembranous colitis reported with antibacterial agents, including penicillin G

Administer by deep intramuscular injection only in the upper, outer quadrant of buttock (dorsogluteal) or ventrogluteal site; quadriceps femoris fibrosis and atrophy reported following repeated intramuscular injections of penicillin preparations into anterolateral thigh and is not recommended

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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 after hydrolysis to penicillin G

Absorption: IM, slow

Peak Plasma Concentration: 0.03-0.05 units/mL; levels persist for 5-14 days depending on dose

Protein Bound: 60%

Metabolism: ~30% in liver

Excretion: urine (60-90%)

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

BRAND FORM. UNIT PRICE PILL IMAGE
Bicillin L-A intramuscular
-
2,400,000 unit/4 mL solution
Bicillin L-A intramuscular
-
1,200,000 unit/2 mL solution
Bicillin L-A intramuscular
-
600,000 unit/mL solution
Bicillin L-A intramuscular
-
600,000 unit/mL solution
Bicillin L-A intramuscular
-
1,200,000 unit/2 mL solution
Bicillin L-A intramuscular
-
2,400,000 unit/4 mL solution

Copyright © 2010 First DataBank, Inc.

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Patient Handout

Patient Education
penicillin G benzathine intramuscular

PENICILLIN G BENZATHINE - INJECTION

(PEN-i-SIL-in BEN-za-theen)

COMMON BRAND NAME(S): Bicillin L-A

WARNING: This medication must not be injected into a vein or mixed with solutions that will be injected into a vein because serious (possibly fatal) side effects can occur.

USES: Penicillin G benzathine is used to treat a wide variety of bacterial infections. It may also be used to prevent certain bacterial infections (such as rheumatic fever). This medication is a long-acting penicillin antibiotic. It works by stopping the growth of bacteria.

HOW TO USE: This medication is given by injection into a large muscle as directed by your doctor. The dosage is based on your medical condition and response to treatment. For children, the dosage is also based on age and weight.If you are using this medication at home, learn all preparation and usage instructions from your health care professional. Do not inject into or near an artery, nerve, or vein. See also Warning section. Change the injection site each time to lessen injury to the muscle. Before using, check this product visually for particles or discoloration. If either is present, do not use the liquid. Learn how to store and discard medical supplies safely.For the best effect, follow your doctor's directions for when to receive this antibiotic, and make sure to not miss any doses.Continue to receive this medication for the full time prescribed, even if symptoms disappear after a few days. Stopping the medication too early may result in a return of the infection.Tell your doctor if your condition lasts or gets worse.

SIDE EFFECTS: Pain at the injection site, nausea, or vomiting may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: joint/muscle pain, vision changes, signs of a new infection (such as sore throat that doesn't go away, fever, chills), easy bruising/bleeding, unusual tiredness, mental/mood changes (such as confusion, hallucinations, depression, agitation).This medication may rarely cause a severe intestinal condition due to a bacteria called C. difficile. This condition may occur during treatment or weeks to months after treatment has stopped. Tell your doctor right away if you develop: diarrhea that doesn't stop, abdominal or stomach pain/cramping, blood/mucus in your stool.If you have these symptoms, do not use anti-diarrhea or opioid products because they may make symptoms worse.Use of this medication for prolonged or repeated periods may result in oral thrush or a new yeast infection. Contact your doctor if you notice white patches in your mouth, a change in vaginal discharge, or other new symptoms.When used to treat syphilis and certain other infections, this medication may cause a reaction that occurs several hours after starting treatment and can last up to 24 hours. Tell your doctor right away if you have any of these symptoms: headache, fever/chills, sweating, joint/muscle pain, fast heartbeat, dizziness, worsening of skin sores or other disease symptoms.Get medical help right away if you have any very serious side effects, including: pain/redness/swelling/numbness/weakness of arms/legs, change in skin color near the injection site or on arms/legs, severe pain/peeling skin at the injection site, muscle cramps/weakness around the injection site, inability to move (paralysis), chest pain, swollen lymph nodes, severe stomach/abdominal pain, nausea/vomiting that doesn't stop, yellowing eyes/skin, irregular heartbeat, seizures, pink/bloody/dark urine, signs of kidney problems (such as a change in the amount of urine).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

PRECAUTIONS: Before using this medication, tell your doctor or pharmacist if you are allergic to it; or to other antibiotics (such as other penicillins, cephalosporins); or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: kidney disease.This medication may cause live bacterial vaccines (such as typhoid vaccine) to not work as well. Do not have any immunizations/vaccinations while using this medication unless your doctor tells you to.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.This drug passes into breast milk in small amounts. Consult your doctor before breast-feeding.

DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.One product that may interact with this drug is: methotrexate.This medication may interfere with certain lab tests (including certain urine glucose tests), possibly causing false test results. Make sure lab personnel and all your doctors know you use this drug.

OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: seizures.

NOTES: Do not share this medication with others.Lab and/or medical tests (such as complete blood count, kidney function tests, blood cultures) may be done if you are using this medication for a long time. Keep all medical and lab appointments.

MISSED DOSE: It is important to get each dose of this medication as scheduled. If you miss a dose, ask your doctor or pharmacist right away for a new dosing schedule. Do not double the dose to catch up.

STORAGE: Store in the refrigerator or as directed by your pharmacist. Do not freeze. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

Information last revised August 2021. Copyright(c) 2021 First Databank, Inc.

IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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Formulary

FormularyPatient Discounts

Adding plans allows you to compare formulary status to other drugs in the same class.

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Adding plans allows you to:

  • View the formulary and any restrictions for each plan.
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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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Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.