Dosing & Uses
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
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
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
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
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.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
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
Images
Patient Handout
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
