ceftriaxone

Ceftriaxone is a broad spectrum third generation cephalosporin antibiotic used to treat a wide range of bacterial infections. Ceftriaxone is administered as an intramuscular (IM) or intravenous (IV) injection. Ceftriaxone is highly effective against gram-negative bacteria, and gram-positive bacteria that are resistant to the first two generations of cephalosporins.

Gram-negative bacteria are structurally different from gram-positive bacteria, and the types are identified by whether the bacteria get dyed or not in the Gram stain lab test. Ceftriaxone kills bacteria by inhibiting the synthesis of peptidoglycan, a vital constituent that provides stability to the bacterial cell wall.

The brand Rocephin has been discontinued in the U.S., however, generic ceftriaxone is available.

Ceftriaxone is used to treat the following bacterial infections:

Adult:

• Complicated, mild-to-moderate, community-acquired intra-abdominal infections, in combination with metronidazole
• Acute bacterial otitis media (middle ear infection)
• Pelvic inflammatory disease, with doxycycline, with or without metronidazole
• Prosthetic joint infection
• Meningitis
• Acute uncomplicated pyelonephritis
• Surgical prophylaxis
• Uncomplicated gonococcal infections of pharynx, cervix, urethra or rectum

Off-label uses include:

• Septic/toxic shock
• Acute epididymitis
• Skin and soft tissue necrotizing infection
• Severe acute bacterial rhinosinusitis
• Other gonococcal infections including:
  • Gonococcal conjunctivitis
  • Disseminated gonococcal infection
  • Gonococcal endocarditis
  • Gonococcal meningitis

Pediatric:

• Acute bacterial otitis media
• Meningitis
• Serious infections other than meningitis
• Skin and skin structure infections
• Gonococcal infections
• Epiglottitis (off-label)

Organisms susceptible to ceftriaxone include:

• Anaerobic cocci, Bacteroides fragilis, Borrelia burgdorferi, Clostridium spp, Enterobacter spp, Escherichia coli, Haemophilus influenzae, Klebsiella spp, Morganella morganii, Neisseria gonorrhoeae, Neisseria meningitides, Proteus mirabilis, Providencia rettgeri, Pseudomonas spp, Serratia spp, Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes

• Do not treat hyperbilirubinemic (high blood level of bilirubin) neonates, especially if premature, with ceftriaxone.
• Do not dilute ceftriaxone with solutions containing calcium. Concomitant calcium-ceftriaxone administration has a risk of fatal precipitant formation in lungs and kidneys of full term and preterm neonates.
• Do not administer any calcium-containing IV drugs or products to infants under 28 days within 48 hours of ceftriaxone (within 5 days if the neonate is under 10 days).
• Do not administer ceftriaxone simultaneously with calcium-containing IV solutions to infants above 28 days. Ceftriaxone and calcium may be given sequentially after thoroughly flushing the infusion lines between the infusions with a compatible fluid.
• Do not administer ceftriaxone to patients with known hypersensitivity to cephalosporin class of antibiotics or any other ingredient of the drug.
• Ceftriaxone must be administered with caution in patients with hypersensitivity to penicillins or any other drugs.

Common side effects of ceftriaxone include:

• Injection site reactions (swelling, redness, pain, a hard lump, or soreness)
• Increase in eosinophils, type of white blood cells (eosinophilia)
• Increased blood platelets (thrombocytosis)
• Diarrhea
• Elevated liver transaminases
• Low white blood cell count (leukopenia)
• Rash
• Increased blood urea nitrogen (BUN)
• Pain

Less common side effects of ceftriaxone include:

• Low level of granulocytes, type of white blood cells (agranulocytosis)
• Low level of red blood cells (anemia)
• Increase basophils, type of white blood cells (basophilia)
• Blood in urine
• Bronchospasm
• Changes in taste
• Chills
• Dizziness
• Excess sweating
• Flushing
• Gallstones
• Headache
• Hemolytic anemia (anemia caused by red blood cell destruction)
• Increase in lymphocytes in the blood (lymphocytosis)
• Increase in monocytes in the blood (monocytosis)
• Increase in leukocytes, type of white blood cells (leukocytosis)
• Increased alkaline phosphatase or bilirubin
• Increased creatinine
• Itching
• Loss of appetite
• Low levels of lymphocytes in the blood (lymphopenia)
• Low platelet count (thrombocytopenia)
• Low neutrophil white blood cell count (neutropenia)
• Nausea
• Overactive reflexes
• Pain or swelling in your tongue
• Inflammation of a vein (phlebitis)
• Prolonged or decreased prothrombin time (PT)
• Renal stones
• Serum sickness
• Severe allergic reaction (anaphylaxis)
• Sugar in the urine
• Upset stomach
• Urinary casts
• Vaginal itching or discharge (vaginitis)
• Vomiting
• Yeast infection (candidiasis)
• Yellowing skin and eyes (jaundice)

Postmarketing side effects of ceftriaxone reported include:

• Pancreatitis, stomatitis and swollen tongue
• Urinating less than usual, ureteric obstruction, post-renal acute renal failure
• Hypersensitive reactions such as:
  • Exanthema
  • Allergic dermatitis
  • Hives
  • Swelling (edema)
  • Acute generalized exanthematous pustulosis (AGEP)
  • Isolated cases of severe cutaneous adverse reactions (erythema multiforme, Stevens-Johnson syndrome or Lyell's syndrome/toxic epidermal necrolysis)
• Convulsions

This is not a complete list of all side effects or adverse reactions that may occur from the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may also report side effects or health problems to the FDA at 1-800-FDA-1088.

Adult and Pediatric Dosage Forms and Strengths

Injectable solution

• 1 g/50 mL
• 2 g/50mL

Powder for injection

• 250 mg
• 500 mg
• 1 g
• 2 g
• 10 g (adult only)
• 100 g (adult only)

Inform your doctor of all medications you are currently taking, who can advise you on any possible drug interactions. Never begin taking, suddenly discontinue, or change the dosage of any medication without your doctor’s recommendation.

Severe interactions of ceftriaxone include:

• calcium acetate
• calcium carbonate
• calcium chloride
• calcium citrate
• calcium gluconate

Serious interactions of ceftriaxone include:

• argatroban
• BCG vaccine live
• bivalirudin
• cholera vaccine
• dalteparin
• enoxaparin
• fondaparinux
• heparin
• lepirudin
• tinzaparin
• typhoid vaccine live
• warfarin

Moderate interactions of ceftriaxone include:

• bazedoxifene/conjugated estrogens
• chloramphenicol
• demeclocycline
• dienogest/estradiol valerate
• doxycycline
• erythromycin base
• erythromycin ethylsuccinate
• erythromycin lactobionate
• erythromycin stearate
• minocycline
• probenecid
• sodium picosulfate/magnesium oxide/anhydrous citric acid
• tetracycline
• warfarin
• Mild interactions of ceftriaxone include:
• choline magnesium trisalicylate
• furosemide
• rose hips
• willow bark

The drug interactions listed above are not all of the possible interactions or adverse effects. For more information on drug interactions, visit the RxList Drug Interaction Checker.

It is important to always tell your doctor, pharmacist, or health care provider of all prescription and over-the-counter medications you use, as well as the dosage for each, and keep a list of the information. Check with your doctor or health care provider if you have any questions about the medication.

Ceftriaxone is a Pregnancy Category B drug.

• Ceftriaxone may be acceptable for use during pregnancy. Either animal studies show no risk but human studies are not available or animal studies showed minor risks and human studies were done and showed no risk
• Ceftriaxone enters breast milk in low concentrations. Use with caution in breastfeeding women. Ceftriaxone may displace bilirubin from albumin-binding sites, increasing the risk of kernicterus.

Administration

IV Incompatibilities

• Solution: LR (at drug concentrations >10 mg/mL; compatible at 1 mg/mL)
• Additive: Aminophylline, clindamycin, linezolid, theophylline, metronidazole (at metronidazole 15 g/L with ceftriaxone 20 g/L; compatible at metronidazole 7.5 g/L with ceftriaxone 10 g/L)
• Syringe: Lidocaine (variable)
• Y-site: Alatrofloxacin, amphotericin B cholesteryl sulfate, amsacrine, filgrastim, fluconazole, labetalol, pentamidine, vinorelbine, vancomycin
• General: Calcium-containing drugs

IV/IM Preparation

• Dilutions are stable for 24 hours at room temperature

IV

• Reconstitute to ~100 mg/mL, then dilute further to 10-40 mg/mL
• 10 g bulk package: not for direct IV infusion; reconstitute in 95 mL, then use appropriate portions for further dilution
• 10-g bulk package not for direct IV injection; reconstitute in 95 mL, then use appropriate portions for further dilution

IM

• Dilute with compatible fluid (e.g., SWI, NS, D5W) to 250-350 mg/mL

IV/IM Administration

• IV: Infuse intermittently over 30 minutes
• IM: Inject deep into large muscle mass