Ceftriaxone

CLINICAL USE

Antibacterial agent

DOSE IN NORMAL RENAL FUNCTION

1 g daily (severe infections: 2–4 g daily)Gonorrhoea: single dose 250 mg IM

PHARMACOKINETICS

Molecular weight :661.6 (as sodium salt)

%Protein binding :85–95

%Excreted unchanged in urine : 40–60

Volume of distribution (L/kg) :0.12–0.18

half-life – normal/ESRD (hrs) :6–9/14.7

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 : Dose as in normal renal function

10 to 20 : Dose as in normal renal function

<10 : Dose as in normal renal function Maximum 2 g daily

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD :Not dialysed. Dose as in GFR <10 mL/min

HD :Not dialysed. Dose as in GFR <10 mL/min

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

CAV/VVHD :Unknown dialysability. 2 g every 12–24 hours1CVVhd/HDFLikely dialysability. 2 g every 12–24 hours1

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Anticoagulants: effects of coumarins may be enhanced

Ciclosporin: may cause increased ciclosporin levels

ADMINISTRATION

Reconstition

Bolus 250 mg: IV – 5mL water for injection; IM – 1 mL 1% lidocaine hydrochloride

Bolus 1 g: IV – 10 mL water for injection; IM – 3.5 mL 1% lidocaine hydrochloride

Infusion: 2 g in 40 mL of calcium-free solution, e.g. sodium chloride 0.9%, glucose 5%

Incompatible with calcium containing solutions, e.g. Hartmann’s, Ringer’s

Route

IV, IM, SC

Rate of Administration

Bolus: over 2–4 minutes Infusion: over at least 30 minutes

Comments

Doses of 50 mg/kg or over should be given by slow IV infusion

For IM injection: doses greater than 1 g should be divided and injected at more than one site

OTHER INFORMATION

Calcium ceftriaxone has appeared as a precipitate in urine, or been mistaken as gallstones in patients receiving higher than recommended doses

Contains 3.6 mmol sodium per gram of ceftriaxone

Information from the company shows that the bioavailability of SC administration is equivalent to IV. The maximum amount able to be given in a single SC injection is 500 mg dissolved in 2 mL lidocaine 1%. Administration was said to be tolerable

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