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