ceftriaxone sodium powder for injection
- Pregnancy Category B1
- Low concentrations of ceftriaxone are excreted in human milk.
- Liver impairment: no dosage adjustment necessary.
- Severe renal impairment: Serum levels should not exceed 280 μg/mL.
- Ceftriaxone-AFT contains ≅ 83 mg (3.6 mEq) of sodium per gram of ceftriaxone activity.
For front-line care, you might use ceftriaxone for a CAP or pre-hospital first dose meningitis treatment (or cover for someone with a possible viral meningitis). Ceftriaxone is also used in the treatment of gonococcus (not jut meningococcus). Another possibility might be that biliary colic which you suspect might progress, but the person is nonetheless keen to stay at home.
Contraindications
- cephalosporin allergy (or major allergy to penicillin: anaphylaxis, angioneurotic oedema, urticaria)
- lignocaine hypersensitivity (lignocaine is used as the diluent for I.M. administration)
- preterms and hyperbilirubinaemic newborns (ceftriaxone displaces bilirubin from its binding to serum albumin, leading to a possible risk of bilirubin encephalopathy).
- incompatible drugs / solutions
- calcium containing I.V. solutions such as TPN (risk of precipitation)
- Ringer’s or Hartmann’s solutions
- amsacrine, vancomycin, fluconazole and aminoglycosides
Precautions
- C. difficile associated diarrhoea (CDAD)
- Repeated lignocaine use in those with liver impairment
Dosage
- Adults: 1-2 g IMI or IVI daily
- Children: 50 mg / kg (not > 2 g) IMI or IVI daily or divided in between two daily doses
Solutions retain their efficacy for 6 hours at room temperature or 24 hours when stored in the refrigerator (2-8 ºC). Ceftriaxone sodium is a white to yellowish-orange crystalline powder which is readily soluble in water. The pH of a 5% aqueous solution is approximately 6-8 and its colour ranges from light yellow to amber, depending on the length of storage, concentration and diluent used.
Intramuscular Administration
- Dissolve 1 g Ceftriaxone-AFT in 3.5 mL of 1% lignocaine solution.
- Administer by deep intragluteal injection (using the opposite buttock for a further 1 g if necessary).
Intravenous Injection: give over 2-4 minutes
- Dissolve 500 mg in 5 mL or 1 g in 10 mL sterile water for injection and
- administer by direct I.V. injection given over a period of 2-4 minutes.
Intravenous Infusion: given over at least 30 minutes
- Dissolve 2 g Ceftriaxone-AFT in approximately 40 mL of one of the following infusion solutions:
- Sodium chloride 0.9
- Sodium chloride 0.45% + glucose 2.5%
- Glucose 5%
- Glucose 10%
Generally ceftriaxone therapy should be continued for at least 2 days after the signs and symptoms of the infection have disappeared. However, prolonged therapy results in a higher incidence of adverse effects especially diarrhoea, rash, eosinophilia, elevated liver enzymes and to a lesser extent neutropenia.
Overdosage: supportive treatment (drug concentration would not be reduced by
haemodialysis or peritoneal dialysis and there is no specific antidote)
Contact the Poisons Information Centre (Phone 13 11 26, in Australia), or equivalent in your country, for advice on the management of overdosage.
Activity: beta-lactamase stable inhibition of cell-wall synthesis (susceptible to type IV beta-lactamases)
Gram Negative (not reliable anti-pseudomonal cover)
- Enterobacteriacae
- E. coli
- Haemophilus influenzae (including ampicillin-resistant strains),
- Klebsiella species (including K. pneumoniae).
- Neisseria gonorrhoeae (including penicillinase and non-penicillinase producing strains)
- Neisseria meningitidis
- Proteus mirabilis, and Proteus vulgaris
- Morganella morganii
- Serratia marcescens
Gram Positive
- Staphylococcus aureus (including penicillinase producing strains)
- Staphylococcus epidermidis (except methicillin-resistant staphylococci)
- Streptococcus pyogenes (Group A beta-haemolytic streptococci)
- Streptococcus agalactiae (Group B streptococci)
- Streptococcus pneumoniae Group G streptococci
- Streptococcus viridans and Streptococcus species (most species of Group D streptococci including Streptococcus faecalis and Streptococcus faecium are resistant).
Peak plasma concentrations after IM administration are reached after 2 hours:
About 85-95% of ceftriaxone is reversibly bound to human plasma proteins. Elimination half-life ranges from about 6 to 9 hours with an apparent volume of distribution between 6 and to 13 L.One- to two-thirds of the drug is excreted unchanged in urine while significant amounts are eliminated via bile.
- Plasma clearance: 0.58 to 1.45 L/hr
- Renal clearance: 0.32 to 0.73 L/hr.
In some patients with severely impaired renal function the t½ of
ceftriaxone may be prolonged (37-52 hours) and dosage adjustment should be
considered to maintain peak serum concentrations below 280 μg/mL.
Adverse Reactions (uncommon but incidence slightly higher in children with higher doses)
- Rash infrequently. Less frequently, pruritus, fever or chills, severe dermatitis including exfoliative erythroderma, anaphylaxis, erythema multiforme, urticaria, exanthema and allergic dermatitis.
- Immune Mediated Haemolytic Anaemia
- Gall bladder concretions / precipitates and pancreatitis
- Renal Toxicity (no impairment of renal function has been observed, however, with concurrent use of diuretics e.g. frusemide)
- Altered Clotting Time (Vitamin K 10 mg weekly if PT prolonged)
- Alteration in haematological laboratory parameters after prolonged (i.e. 10 days or more) high doses: eosinophilia, leucopenia, granulocytopenia,
haemolytic anemia, thrombocytopenia, isolated cases of agranulocytosis - local reactions: pain/induration/tenderness worse if water (WFI) rather than lignocaine is used as diluent
Reference
Ceftriaxone-AFT Product Information (AFT Pharmaceuticals Pty. Ltd), August 2015.
