Benzylpenicillin

CLINICAL USE

Antibacterial agent

DOSE IN NORMAL RENAL FUNCTION

2.4–14.4 g daily in 4–6 divided doses

PHARMACOKINETICS

Molecular weight :334.4

%Protein binding :60

%Excreted unchanged in urine : 60–90

Volume of distribution (L/kg) :0.3–0.42

half-life – normal/ESRD (hrs) :0.5/10

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 : Dose as in normal renal function

10 to 20 : 600 mg – 2.4 g every 6 hours depending on severity of infection

<10 : 600 mg – 1.2 g every 6 hours depending on severity of infection

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD :Dialysed. Dose as in GFR <10 mL/min

HD :Dialysed. Dose as in GFR <10 mL/min

HDF/high flux :Dialysed. Dose as in GFR <10 mL/min

CAV/VVHD :Dialysed. Dose as in GFR 10 to 20 mL/min

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugsReduced excretion of methotrexate

ADMINISTRATION

Reconstition

IV Bolus: 600 mg in 5 mL water for injectionIV Infusion: 600 mg in at least 10 mL sodium chloride 0.9%

IM: 600 mg in 1.6 mL water for injection 600 mg displaces 0.4 mL

Route

IV Bolus, IV Infusion, IM

Rate of Administration

IV bolus: over 3–4 minutes

IV infusion

: over 30–60 minutes

Comments

IV doses in excess of 1.2 g must be given slowly at minimum rate of 300 mg/minute

OTHER INFORMATION

Dose in normal renal function: meningitis up to 14.4 g daily; bacterial endocarditis 4.8 g daily

Maximum dose in severe renal impairment: 4.8 g per day600 mg of benzylpenicillin sodium (1 mega unit) contains 1.68 mmol of sodium600 mg of benzylpenicillin potassium contains 1.7 mmol potassium

Increased incidence of neurotoxicity in renal impairment (seizures)

False positive urinary protein reactions may be caused by benzylpenicillin therapy

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