Ceftizoxime Sodium

(BANM, USAN, rINNM)
Synonyms: Ceftizoxima sódica; Ceftizoxime Sodique; Ceftizoximnatrium; Ceftizoximum Natricum; FK-749; FR-13749; Keftitsoksiiminatrium; Natrii Ceftizoximum; Seftizoksim Sodyum; SKF-88373-Z. Sodium (Z)-7-[2-(2-aminothiazol-4-yl)-2-methoxyiminoacetamido]-3-cephem-4-carboxylate.
Cyrillic synonym: Натрий Цефтизоксим.

💊 Chemical information

Chemical formula: C13H12N5NaO5S2 = 405.4.
CAS — 68401-81-0 (ceftizoxime); 68401-82-1 (ceftizoxime sodium).
ATC — J01DD07.
ATC Vet — QJ01DD07.

Pharmacopoeias.

In Jpn and US.

USP 31

(Ceftizoxime Sodium). A white to pale yellow crystalline powder. Freely soluble in water. pH of a 10% solution in water is between 6.0 and 8.0. Store in airtight containers.

Stability.

References. 1. Lesko AB, et al. Ceftizoxime stability in iv solutions. DICP Ann Pharmacother 1989; 23: 615–18.

💊 Adverse Effects and Precautions

Sodium content.

Each g of ceftizoxime sodium contains about 2.5 mmol of sodium.

💊 Interactions

Probenecid reduces the renal clearance of ceftizoxime.

💊 Antimicrobial Action

As for Cefotaxime Sodium, although ceftizoxime has no active metabolite.

💊 Pharmacokinetics

After intramuscular injection of 0.5 and 1 g of ceftizoxime, mean peak plasma concentrations of about 14 and 39 micrograms/mL respectively have been reported after 1 hour. The plasma half-life of ceftizoxime is about 1.7 hours and is prolonged in neonates and in renal impairment. Ceftizoxime is 30% bound to plasma proteins. Ceftizoxime is widely distributed in body tissues and fluids; therapeutic concentrations are achieved in the CSF when the meninges are inflamed. It crosses the placenta and low concentrations have been detected in breast milk. Nearly all of a dose is excreted unchanged in the urine within 24 hours of dosage, thus achieving high urinary concentrations. Ceftizoxime is excreted by tubular secretion as well as glomerular filtration and giving it with probenecid results in higher and more prolonged plasma concentrations. Some ceftizoxime is removed by haemodialysis.

Neonates.

References.
1. Fujii R. Investigation of half-life and clinical effects of ceftizoxime in premature and newborn infants. Drug Invest 1990; 2: 143–9
2. Reed MD, et al. Ceftizoxime disposition in neonates and infants during the first six months of life. DICP Ann Pharmacother 1991; 25: 344–7.

💊 Uses and Administration

Ceftizoxime is a third-generation cephalosporin antibacterial used similarly to cefotaxime for the treatment of susceptible infections. It is given as the sodium salt by deep intramuscular injection, or intravenously as a slow injection over 3 to 5 minutes or as a continuous or intermittent infusion. If 2 g of ceftizoxime is injected intramuscularly the dose should be divided between sites. Doses are expressed in terms of the equivalent amount of ceftizoxime; 1.06 g of ceftizoxime sodium is equivalent to about 1 g of ceftizoxime. It is usually given in an adult dose of 1 to 2 g every 8 to 12 hours. In severe infections 2 to 4 g may be given intravenously every 8 hours; doses up to 2 g every 4 hours have been given in life-threatening infections. Children over 6 months of age may be given 50 mg/kg every 6 to 8 hours. For the treatment of uncomplicated urinary-tract infections, a dose of 500 mg every 12 hours is used. For details of reduced doses in patients with renal impairment, see below. A single intramuscular dose of 1 g has been given in uncomplicated gonorrhoea.
1. Richards DM, Heel RC. Ceftizoxime: a review of its antibacterial activity, pharmacokinetic properties and therapeutic use. Drugs 1985; 29: 281–329.

Administration in renal impairment.

Doses of ceftizoxime should be modified in renal impairment; after a loading dose of 0.5 to 1 g, the maintenance dosage should be adjusted according to creatinine clearance (CC) and the severity of the infection:
CC 50 to 79 mL/minute: 0.5 to 1.5 g every 8 hours
CC 5 to 49 mL/minute: 0.25 to 1 g every 12 hours
CC less than 5 mL/minute: 250 to 500 mg every 24 hours or 0.5 to 1 g every 48 hours, after dialysis.

💊 Preparations

USP 31: Ceftizoxime for Injection; Ceftizoxime Injection.

Proprietary Preparations

Arg.: Ceftix†; Ceftizon†; Canad.: Cefizox; Cz.: Cefizox†; Fr.: Cefizox†; India: Cefizox; Indon.: Cefizox; Tizos; Ital.: Eposerin; Jpn: Epocelin†; Mex.: Cefizox†; Neth.: Cefizox; Philipp.: Tergecin; Unizox; Port.: Cefizox; Turk. : Cefizox; USA: Cefizox.
Published January 15, 2019.