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penicillin G benzathine (Bicillin LA, Permapen)

 

Classes: Penicillins, Natural

Dosing and uses of Bicillin LA, Permapen (penicillin G benzathine)

 

Adult dosage forms and strengths

injectable suspension

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

 

Group A Streptococcal Respiratory Infections

1.2 million units IM x1

 

Rheumatic Fever Prophylaxis

1.2 million units IM monthly following acute attack, Or

600,000 units IM q2Weeks

 

Syphilis

Primary or secondary (CDC Guidelines 2006)

  • 2.4 million units IM x1
  • If pregnant: Some specialists recommend 2.4 million units IM qWeek x2
  • If HIV+: Some specialists recommend 2.4 million units IM qWeek x 3

Early Latent: 2.4 million units IM x1

Neurosyphilis: 2.4 million units IM qWeek x 3

 

Yaw, Bejel, & Pinta

1.2 million units 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

 

Pediatric dosage forms and 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 unit IM x1 (AHA guidelines 2009)

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

 

Rheumatic Fever, Prophylaxis

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

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

 

Syphilis

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

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

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

 

Renal Impairment

Not defined in children; see adult recommendations

 

Bicillin LA, Permapen (penicillin G benzathine) adverse (side) 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

 

Warnings

Black box warnings

Not for IV use

Do not inject IV or admix with other IV solutions

Reports of inadvertent IV administration associated with cardiorespiratory arrest and death

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

Pseudomembranous colitis reported with antibacterial agents, including penicillin g

 

Pregnancy and 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.

 

Pharmacology of Bicillin LA, Permapen (penicillin G benzathine)

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

 

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