Trade name(s): Rocephin Drug Class: Antibacterial
Theraputic use: Used as an antibacterial that attach to penicillin binding protein to cause bacterial cell death.
Pharmacological action: Cephalosporins are antibacterials that attach to penicillin binding proteins to interrupt cell wall biosynthesis, leading to bacterial cell lysis and death.
Pharmacokinetics:
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Absorption Ceftriaxone is poorly absorbed from the gastrointestinal tract.
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Distribution maximum concentrations occur 2-3 hours post dosing, accumulation is great with IM doses in 12-24 hour dose intervals
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Metabolism Metabolism of ceftriaxone is negligible
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Excretion 33 – 67% of a ceftriaxone dose is excreted in the urine as the unchanged drug. Substantial amounts are secreted in the bile and eventually found in the faeces as microbiologically inactive compounds.
Indications: Infections due to gram positive and gram negative bacteria. Suspected meningococcal infection, endocarditism early syphilis, uncomplicated gonorrhoea prophylaxis of surgery and neisseria meningitidis
Contraindications: cephalosporin hypersensetivity, neonates less than 41 wks gestational age, full term neonates with jaundice, hyperalbuminaemia, acidosis, conjugated hyperbilirubinaemia, impaired bilirubin binding.
Precautions: sensitivity ot betalactam antibacterialsm false positive urinary glucose
Adverse reactions: diarhoea, nauseam vomiting, abdominal discomfort, headache, allergic reactions, disturbances in liver enzymes, transient hepatitis, haundice
Interactions:
- live cholera and typhoid vaccines
- coumarins can interact with cephalosporins to increase bleeding
- warfarin
- voclosporin nephrotoxicity could compound.
Dosing/Current guidelines: do not administer with calcium
For infections due to sensitive gram positive and gram negative bacteria Adult 1g daily and 2-4 in severe infections (IV, or deep IM)
Suspected meningococcal infection Bacterial meningitis Adult 4 g once daily or 2 g every 12 hours (IV injection or infusion) Endocarditis Adult 2-4 g daily (IV injection or infusion) Early syphilis Adult 500 mg daily for 10 days (deep IM injeciton) Uncomplicated gonorrhoea (incombination with azithromycin) Adult 500 mg daily for 10 days (deep IM injeciton) Surgical prophylaxis Adult 1 g up to 30 minutes before the procedure (IV injeciton) Colorectal prophylaxis Adult 2 g up to 30 minutes before the procedure (IV infusion injection or deep IM injection) Prophylaxis of neisseria meningitis infection Adult 250 mg as a single dose (deep IM injection)
Overdose: no specific antidote and treatment should be symptomatic
Pregnancy
subsidisation ceftriaxone-AFT is fully subsudised for 500mg vial and 1g vial
What to tell patients:
Comments/Observations/notes: Ceftriaxone-AFT is a single dose and any extra should be discarded Use freshly prepared solutions as fast as possible for best effects The solution is yellowish and slightly opalescent Ceftriaxone forms a calium precipitate on contact with calcium. do not mix it with calcium and do not administer in conjunction with ceftriaxone
Ceftriaxone should not be mixed with any other antimicrobial solution. specifically, amsacrine, vancomysin, fluconazole, and aminoglycosides
IM admin dissolve 500 mg of ceftriaxone-AFT in 2 mL or 1 g in 3.2ml lignocaine solution. it should be administered by deep gluteal injection, it should never be given intravenously,
Intravenous admin
injection dissolve 500 mg in 5 ml or 1 g in 10 ml sterile eater for injection and administer by direct IV injection given over a period of 2-4 mins
infusion dissolve 2 g ceftriaxone in approx 40 ml of a sodium glucose levulose or dextran 70 solution.