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Penicillin類抗生素

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

Distribution: Poor penetration across blood-brain barrier, despite inflamed meninges
Half-life elimination:
Neonates: <6 days of age: 3.1 hours; ?14 days of age: 1.4 hours
Adults: Normal renal function: 31 to 50 minutes
End-stage renal disease (ESRD): 6 to 20 hours (Aronoff 2007)
Excretion: Urine (58% to 85% as unchanged drug)(UTD)

History of penicillin hypersensitivity.

B (FDA) A (AUS)

Infant risk cannot be ruled out.(MDX)

Serious:
Cardiovascular: Congestive heart failure.
Endocrine metabolic: Electrolyte imbalance.
Immunologic: Anaphylaxis, Hypersensitivity reaction.
Neurologic: Coma, Seizure

Usual dosage range: IM, IV: 12 to 24 million units/day in divided doses every 4 to 6 hours
Diphtheria (adjunctive therapy to antitoxin and for prevention of carrier state): IV: 2 to 3 million units/day in divided doses every 4 to 6 hours for 10 to 12 days
Endocarditis, treatment: IV:
Enterococcus, native or prosthetic valve (off-label dose): 18 to 30 million units/day as continuous infusion or in divided doses every 4 hours with concomitant streptomycin. Duration of therapy: 4 weeks (native valve and symptoms present <3 months); ?6 weeks (native valve and symptoms present ?3 months or prosthetic valve) .
Erysipelothrix rhusiopathiae: 12 to 20 million units/day in divided doses every 4 to 6 hours for 4 to 6 weeks Listeria monocytogenes: 15 to 20 million units/day in divided doses every 4 to 6 hours for 4 weeks
Viridans group streptococcus (VGS) and S. bovis (off-label dose) :
Native valve: Highly penicillin-susceptible (MIC ?0.12 mcg/mL): 12 to 18 million units/day as continuous infusion or in divided doses every 4 or 6 hours for 4 weeks or 12 to 18 million units/day as continuous infusion or in divided doses every 6 hours for 2 weeks with concomitant gentamicin
Native valve: Relatively penicillin-resistant (MIC >0.12 to <0.5 mcg/mL): 24 million units/day as continuous infusion or in divided doses every 4 or 6 hours for 4 weeks with concomitant gentamicin for the first 2 weeks
Prosthetic valve: Highly penicillin-susceptible (MIC ?0.12 mcg/mL): 24 million units/day as continuous infusion or in divided doses every 4 or 6 hours for 6 weeks (with or without concomitant gentamicin for the first 2 weeks)
Prosthetic valve: Relatively or fully penicillin-resistant (MIC >0.12 mcg/mL): 24 million units/day as continuous infusion or in divided doses every 4 or 6 hours with concomitant gentamicin for 6 weeks
Meningitis: IV:
Listeria: 15 to 20 million units/day in divided doses every 4 to 6 hours for 2 weeks
Meningococcus: 24 million units/day in divided doses every 2 hours
Neurosyphilis: IV:
2 to 4 million units every 4 hours for 10 to 14 days; after completion, additional therapy with benzathine penicillin G may be warranted
Streptococcus infections: IV:
Group B streptococcus, maternal dose (neonatal prophylaxis) (off-label use): 5 million units x 1 dose, then 2.5 to 3.0 million units every 4 hours until delivery
Streptococcal pneumonia: IV: 12 to 24 million unit/day in divided doses every 4 to 6 hours. Note: Only recommended for S. pneumoniae when MIC is <2 mcg/mL .(UTD)

Community-acquired pneumonia (CAP) (off-label dose) :
Infants >3 months, Children, and Adolescents:
Empiric treatment or S. pneumoniae (moderate-to-severe; MICs to penicillin ?2.0 mcg/mL) :
200,000 to 250,000 units/kg/day in divided doses every 4 to 6 hours
Group A Streptococcus (moderate-to-severe) :
100,000 to 250,000 units/kg/day in divided doses every 4 to 6 hours
Diphtheria (adjunctive therapy to antitoxin and for prevention of carrier state): IV: 150,000 to 250,000 units/kg/day in divided doses every 6 hours for 7 to 10 days.
Lyme neuroborreliosis (off-label use): IV: 200,000 to 400,000 units/kg/day in divided doses every 4 hours
Meningitis:
Group B streptococcus: Infants: 450,000 to 500,000 units/kg/day divided every 6 hours
S. pneumoniae: Infants, Children, and Adolescents: 250,000 to 400,000 units/kg/day divided every 4 to 6 hours
Other susceptible organisms: Infants, Children, and Adolescents: 300,000 units/kg/day divided every 4 to 6 hours; maximum daily dose: 24 million units/day
Meningococcal disease:
300,000 units/kg/day in divided doses every 4 to 6 hours; maximum daily dose: 12 million units/day
Neurosyphilis:
200,000 to 300,000 units/kg/day divided every 4 to 6 hours for 10 to 14 days (maximum dose: 24 million units/day)
Syphilis (congenital):
50,000 units/kg/dose every 4 to 6 hours for 10 to 14 days
Alternate recommendations (off-label dose) :
Neonates: 50,000 units/kg/dose every 12 hours for first 7 days of life, then every 8 hours for a total of 10 days. If more than one day of therapy is missed, the entire course needs to be restarted.
Infants ?30 days and Children: 50,000 units/kg/dose every 4 to 6 hours for 10 days.(UTD)

Uremic patients with CrCl >10 mL/minute/1.73 m2: Administer a usual recommended dose followed by 50% of the usual recommended dose every 4 to 5 hours.
CrCl <10 mL/minute/1.73 m2: Administer a normal dose followed by 50% of the normal dose every 8 to 10 hours(UTD).

No dosage adjustment provided in manufacturer's labeling.