Ceftriaxone
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)       :0.12–0.18half-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/minHDF/high flux   :Unknown dialysability. Dose as in GFR <10 mL/minCAV/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 drugsAnticoagulants: effects of coumarins may be enhancedCiclosporin: may cause increased ciclosporin levels ADMINISTRATION
Reconstition
Bolus 250 mg: IV – 5mL water for injection; IM – 1 mL 1% lidocaine hydrochlorideBolus 1 g: IV – 10 mL water for injection; IM – 3.5 mL 1% lidocaine hydrochlorideInfusion: 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 dosesContains 3.6 mmol sodium per gram of ceftriaxoneInformation 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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