ceftriaxone

REMS

Treatment of:
- Skin and skin structure infections,
- Bone and joint infections,
- Complicated and uncomplicated urinary tract infections,
- Uncomplicated gynecological infections including gonorrhea,
- Lower respiratory tract infections,
- Intra-abdominal infections,
- Septicemia,
- Meningitis,
- Otitis media.
Perioperative prophylaxis.

Action ⬆ ⬇

Binds to the bacterial cell wall membrane, causing cell death.

Therapeutic effects:

Bactericidal action against susceptible bacteria.

Spectrum:

Similar to that of second-generation cephalosporins, but activity against staphylococci is less, while activity against gram-negative pathogens is greater, even for organisms resistant to first- and second-generation agents.
Notable is increased action against:
- Acinetobacter,
- Enterobacter,
- Haemophilus influenzae (including β-lactamase-producing strains),
- Haemophilus parainfluenzae,
- Escherichia coli,
- Klebsiella pneumoniae,
- Morganella morganii,
- Neisseria,
- Proteus,
- Providencia,
- Serratia,
- Moraxella catarrhalis.
Has some activity against anaerobes, includingBacteroides fragilis.
Not active against methicillin-resistant staphylococci or enterococci.

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed following IM administration; IV administration results in complete bioavailability.

Distribution: Widely distributed. CSF penetration better than with first- and second-generation agents. Crosses the placenta; enters breast milk in low concentrations.

Protein Binding: ≥90%.

Metabolism/Excretion: 33–67% excreted in urine as unchanged drug; remainder excreted in feces.

Half-Life: 6–9 hr.

Time/Action Profile ⬆ ⬇

ROUTE	ONSET	PEAK	DURATION
IM	rapid	1–2 hr	12–24 hr
IV	rapid	end of infusion	12–24 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity to cephalosporins;
Serious hypersensitivity to penicillins;
Pedi: Premature neonates up to a postmenstrual age of 41 wk;
Pedi: Hyperbilirubinemic neonates (may lead to bilirubin encephalopathy)
Pedi: Neonates 28 days requiring calcium-containing IV solutions ( risk of precipitation formation).

Use Cautiously in:

Combined severe hepatic and renal impairment (↑ risk of neurological adverse reactions) (dose ↓/↑ dosing interval recommended);
History of GI disease, especially colitis;
Pedi: risk of urolithiasis and acute renal failure

Adv. Reactions/Side Effects ⬆ ⬇

Derm: rash, urticaria

GI: CLOSTRIDIODES DIFFICILE-ASSOCIATED DIARRHEA (CDAD), cholelithiasis, diarrhea, gallbladder sludging, pancreatitis

GU: acute renal failure, urolithiasis

Hemat: bleeding, eosinophilia, hemolytic anemia, leukopenia, thrombocytosis

Local: pain at IM site, phlebitis at IV site

Neuro: encephalopathy, SEIZURES (HIGH DOSES)

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS) , superinfection

Interactions ⬆ ⬇

Drug-drug:

Should not be administered concomitantly with any calcium-containing solutions.
May ↑ risk of bleeding with warfarin.

Route/Dosage ⬆ ⬇

IM IV (Adults ): Most infections: 1–2 g every 12–24 hr Gonorrhea: 500 mg IM (single dose). Meningitis: 2 g every 12 hr.Perioperative prophylaxis: 1 g 0.5–2 hr before surgery (single dose).
IM IV (Children ): Most infections: 50–75 mg/kg/day (not to exceed 2 g/day) divided every 12–24 hr. Meningitis: 100 mg/kg/day (not to exceed 4 g/day) divided every 12–24 hr or Uncomplicated gonorrhea: 125 mg IM (single dose).Acute otitis media: 50 mg/kg (not to exceed 1 g) IM single dose.
IM IV (Adults ): Hepatic impairment with significant renal impairment: Not to exceed 2 g/day.

Availability ⬆ ⬇

(Generic available)

Powder for injection: 250 mg/vial; 500 mg/vial; 1 g/vial; 2 g/vial; 10 g/vial; 100 g/vial
Premixed infusion: 1 g/50 mL; 2 g/50 mL

Assessment ⬆ ⬇

Assess for infection (vital signs; appearance of wound, sputum, urine, and stool; WBC) at beginning of and throughout therapy.
Before initiating therapy, obtain a history to determine previous use of and reactions to penicillins or cephalosporins. Persons with a negative history of penicillin sensitivity may still have an allergic response.
Obtain specimens for culture and sensitivity before initiating therapy. First dose may be given before receiving results.
Pedi: Assess newborns for jaundice and hyperbilirubinemia; can increase bilirubinemia and should not be administered to jaundiced neonates, especially premature neonates.
Observe patient for signs and symptoms of anaphylaxis (rash, pruritus, laryngeal edema, wheezing). Discontinue the drug and notify health care professional immediately if these symptoms occur. Keep epinephrine, an antihistamine, and resuscitation equipment close by in the event of an anaphylactic reaction.
Monitor bowel function. Diarrhea, abdominal cramping, fever, and bloody stools should be reported to health care professional promptly as a sign of Clostridioides difficile-associated colitis. May begin up to several wk following cessation of therapy.

Lab Test Considerations:

May cause positive results for Coombs' test.
- May cause increased AST, ALT, alkaline phosphatase, bilirubin, LDH, BUN, and serum creatinine.
- May rarely cause leukopenia, neutropenia, agranulocytosis, thrombocytopenia, eosinophilia, lymphocytosis, and thrombocytosis.

Implementation ⬆ ⬇

Do not confuse ceftriaxone with cefazolin, cefoxitin, cefotetan, or ceftazidime.
IM: Reconstitute IM doses with sterile water for injection, or 0.9% NaCl for injection. May be diluted with lidocaine to minimize injection discomfort. Do not administer lidocaine-containing ceftriaxone IV.
- Inject deep into a well-developed muscle mass; massage well.

IV Administration:

IV: Monitor injection site frequently for phlebitis (pain, redness, swelling). Change sites every 48–72 hr to prevent phlebitis.
- If aminoglycosides are administered concurrently, administer in separate sites, if possible, at least 1 hr apart. If second site is unavailable, flush lines between medications.
Intermittent Infusion: Reconstitution: Reconstitute each 250-mg vial with 2.4 mL, each 500-mg vial with 4.8 mL, each 1-g vial with 9.6 mL, and each 2-g vial with 19.2 mL of sterile water for injection, 0.9% NaCl, or D5W for a concentration of 100 mg/mL. Diluent: Solution should be further diluted in 50–100 mL of 0.9% NaCl, D5W, D10W, D5/0.45% NaCl, or D5/0.9% NaCl. Solution may appear light yellow to amber. Solution is stable for 3 days at room temperature .
Rate: Infuse over 30 min.

Patient/Family Teaching ⬆ ⬇

Advise patient to report signs of superinfection (furry overgrowth on the tongue, vaginal itching or discharge, loose or foul-smelling stools) and allergy.
Instruct patient to notify health care professional if fever and diarrhea develop, especially if diarrhea contains blood, mucus, or pus. Advise patient not to treat diarrhea without consulting health care professional.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇