Ceftizoxime

Ceftizoxime belongs to the pharmacological class of Third-generation cephalosporin antibiotics.

Ceftizoxime has been approved to relieve symptoms and also for the treatment and maintenance of Lower respiratory tract infections, Urinary tract infections, Gynecologic infections, Intra-abdominal infections, Skin and skin structure infections, Bone as well as joint infections, Septicemia, Meningitis, Gonorrhea.

Ceftizoxime is linear and dose-proportional pharmacokinetics within the recommended dosage range. The drug has a half-life of approximately 1.2 hours and is eliminated primarily by the kidneys via glomerular filtration and tubular secretion. The recommended dosing regimen for adults with normal renal function is 1 to 2 grams every 8 hours, with dose adjustments recommended for patients with impaired renal function. Ceftizoxime is highly protein-bound (approximately 70%) and is distributed widely throughout the body, including the respiratory tract, bone, and bile.

The common side effects involved in using Ceftizoxime are Diarrhea, Nausea, Vomiting, Abdominal pain, Headache, Dizziness, Rash, Itching, Elevated liver enzymes

Ceftizoxime is available in the form of Intramuscular and Intravenous Solutions

Ceftizoxime is approved in Germany, Japan, Malaysia, India, U.K.,U.S, and China.

Ceftizoxime belongs to the pharmacological class of Third-generation cephalosporin antibiotics.

Ceftizoxime is a cephalosporin antibiotic that possesses an extended spectrum of activity against many nosocomially acquired, gram-negative pathogens. Its beta-lactamase stability is exceptional, and it exhibits good in vitro activity against Haemophilus influenzae, Neisseria gonorrhoeae, and Klebsiella pneumoniae. Ceftizoxime, similar to penicillins, belongs to the beta-lactam antibiotic class. It works by binding to particular penicillin-binding proteins (PBPs) located inside the bacterial cell wall. This mechanism blocks the third and final stage of bacterial cell wall synthesis. Bacterial cell wall autolytic enzymes, such as autolysins, mediate cell lysis. Ceftizoxime may interfere with an autolysin inhibitor.

Ceftizoxime has been approved to relieve symptoms and also for the treatment and maintenance of Lower respiratory tract infections, Urinary tract infections, Gynecologic infections, Intra-abdominal infections, Skin and skin structure infections, Bone and joint infections, Septicemia, Meningitis, Gonorrhea.

The Tmax (time to reach maximum concentration) for intravenous (IV) administration of ceftizoxime is approximately 30 minutes. The onset of action of ceftizoxime is rapid, with bactericidal activity occurring within 30 minutes of administration. The elimination half-life of ceftizoxime is approximately 1.5 hours. The duration of action of ceftizoxime is approximately 8 hours, although this may vary depending on the type and severity of infection being treated.

Ceftizoxime is found to be available in the form of Intramuscular and Intravenous Solutions.

Ceftizoxime can be used in the following treatment:

• Lower respiratory tract infections
• Urinary tract infections
• Gynecologic infections
• Intra-abdominal infections
• Skin and skin structure infections
• Bone and joint infections
• Septicemia
• Meningitis
• Gonorrhea

Ceftizoxime can help to relieve symptoms and also for the treatment and maintenance of Lower respiratory tract infections, Urinary tract infections, Gynecologic infections, Intra-abdominal infections, Skin and skin structure infections, Bone and joint infections, Septicemia, Meningitis, Gonorrhea.

Ceftizoxime is approved for use in the following clinical indications:

• Lower respiratory tract infections
• Urinary tract infections
• Gynecologic infections
• Intra-abdominal infections
• Skin and skin structure infections
• Bone and joint infections
• Septicemia
• Meningitis
• Gonorrhea

Lower respiratory tract infections: The recommended dose for lower respiratory tract infections is 1 to 2 grams every 8 hours, depending on the severity of the infection.

Urinary tract infections: The recommended dose for uncomplicated urinary tract infections is 500 mg to 1 gram every 12 hours. For complicated urinary tract infections, the recommended dose is 1 gram every 8 hours.

Gynecologic infections: The recommended dose for gynecologic infections is 1 gram every 8 hours.

Intra-abdominal infections: The recommended dose for intra-abdominal infections is 1 to 2 grams every 6 to 8 hours, depending on the severity of the infection.

Skin and skin structure infections: The recommended dose for skin and skin structure infections is 500 mg to 1 gram every 12 hours.

Bone and joint infections: The recommended dose for bone and joint infections is 1 to 2 grams every 8 hours.

Septicemia: The recommended dose for septicemia is 2 grams every 8 hours.

Meningitis: The recommended dose for meningitis is 2 grams every 6 to 8 hours.

Gonorrhea: The recommended dose for gonorrhea is a single dose of 1 gram, either intramuscularly or intravenously.

● Powder for injection: 500 mg, 1 g, and 2 g

● Premixed solution for injection: 1 g and 2 g

Intramuscular and Intravenous Solutions.

• Dosage Adjustments in Kidney Patients:

For patients with creatinine clearance (CrCl) greater than 50 mL/min, the usual adult dose of 1 to 2 grams every 6 to 8 hours may be given.

For patients with CrCl between 30 and 50 mL/min, the usual adult dose of 1 to 2 grams should be given every 12 hours.

For patients with CrCl less than 30 mL/min, the usual adult dose of 1 to 2 grams should be given every 24 hours.

• Dosage Adjustments in Pediatric Patients:

The dosage of ceftizoxime in pediatric patients should be based on the child's age, weight, and renal function. The recommended dosage for children is 50-180 mg/kg/day, divided into 2-4 doses, not to exceed the adult dose. For infants under 1 month of age, the recommended dosage is 30-100 mg/kg/day, divided into 2-4 doses.

In pediatric patients with impaired renal function, dosage adjustments should be made based on the degree of impairment. In children with creatinine clearance (CrCl) greater than or equal to 70 mL/min/1.73 m², the usual recommended dose can be used. For children with CrCl of 30-69 mL/min/1.73 m², the dose should be reduced to 50% of the usual recommended dose. In children with CrCl less than 30 mL/min/1.73 m², the dose should be reduced to 25% of the usual recommended dose.

Dosage adjustments may also be necessary for pediatric patients with hepatic impairment, although there are no specific recommendations for dosage adjustment in this population.

There are no specific dietary restrictions related to the use of ceftizoxime. However, it is generally recommended to take the medication on an empty stomach, at least 30 minutes before or 2 hours after a meal, to ensure proper absorption. It is also important to avoid consuming alcohol while taking ceftizoxime, as it may increase the risk of side effects such as dizziness or drowsiness.

Ceftizoxime may be contraindicated under the following conditions:

• In patients with known hypersensitivity to ceftizoxime, cephalosporins, penicillins, or any component of the formulation.
• In patients with a history of severe hypersensitivity reactions (e.g., anaphylaxis) to any other beta-lactam antibiotic.
• In neonates and infants with hyperbilirubinemia because it can displace bilirubin from albumin binding sites, leading to an increased risk of kernicterus.
• In patients with a history of pseudomembranous colitis or ulcerative colitis.
• Ceftizoxime should be used cautiously in patients with a history of gastrointestinal disease, particularly colitis.

The physician should closely monitor the patients and keep pharmacovigilance as follows:

Hypersensitivity Reactions and Cross-Sensitivity

• Prior Inquiry Necessary
• Caution for Penicillin-Sensitive Patients
• Discontinue Drug if Allergic Reaction Occurs
• Emergency Measures for Serious Acute Hypersensitivity Reactions

Pseudomembranous Colitis and Antibiotic-Associated Colitis

• Reported with nearly all antibacterial agents, including ceftizoxime
• Diagnosis Consideration for Patients with Diarrhea
• Appropriate Therapeutic Measures for Established Diagnosis
• Management for Mild, Moderate, and Severe Cases

Precautions

• Caution in Patients with a History of Gastrointestinal Disease, Particularly Colitis
• Renal Status Evaluation
• Careful Observation for Overgrowth of Nonsusceptible Organisms
• Fall in Prothrombin Activity Associated with Cephalosporins
• Monitoring and Vitamin K Administration for Patients at Risk
• Prescribing Ceftizoxime without Proven or Strongly Suspected Bacterial Infection or Prophylactic Indication

There is no known interaction between Ceftizoxime and alcohol, and the USFDA does not have an alcohol warning for this medication. However, it is always advisable to consult with a healthcare provider regarding the consumption of alcohol while taking any medication. This is especially important for patients with pre-existing liver conditions, as alcohol consumption can worsen liver function and affect the metabolism of medications.

Ceftizoxime is excreted in low concentrations in human milk, and caution is recommended when administering Ceftizoxime to a nursing woman.

Pregnancy Category B

Reproduction studies in animals have not shown any harm to the fetus or impaired fertility caused by Ceftizoxime. However, no adequate and well-controlled studies have been conducted on pregnant women. Thus, Ceftizoxime should be used during pregnancy only if the benefits clearly outweigh the potential risks.

There are no specific food warnings associated with the use of Ceftizoxime.

The adverse reactions related to Ceftizoxime can be categorized as follows:

Common

• Diarrhea
• Nausea and vomiting
• Headache
• Dizziness
• Rash or itching
• Pain or swelling at the injection site

Less Common

• Elevated liver enzymes
• Elevated eosinophils

Rare

• Anaphylaxis or severe allergic reactions
• Stevens-Johnson syndrome (a severe skin disorder)
• Hemolytic anemia (destruction of red blood cells)
• Agranulocytosis (low white blood cell count)
• Thrombocytopenia (low platelet count)
• Pseudomembranous colitis

The clinically relevant drug interactions of Ceftizoxime are briefly summarized here:

Aminoglycosides - Concurrent use of aminoglycosides with Ceftizoxime may increase the risk of kidney damage.

Diuretics - Ceftizoxime may reduce the effectiveness of diuretics such as furosemide.

Probenecid - Probenecid can slow the elimination of Ceftizoxime from the body, leading to higher levels of the drug in the blood.

Warfarin - Ceftizoxime can interfere with the metabolism of warfarin, increasing the risk of bleeding.

The following are the side effects involving Ceftizoxime:

● Diarrhea

● Nausea and vomiting

● Headache

● Dizziness

● Rash or itching

● Pain or swelling at the injection site

● Elevated liver enzymes

● Elevated eosinophils

● Pseudomembranous colitis

Pregnancy Category B

Reproduction studies in animals have not shown any harm to the fetus or impaired fertility caused by Ceftizoxime. However, no adequate and well-controlled studies have been conducted on pregnant women. Thus, Ceftizoxime should be used during pregnancy only if the benefits clearly outweigh the potential risks.

Nursing Mothers

Ceftizoxime is excreted in low concentrations in human milk, and caution is recommended when administering Ceftizoxime to a nursing woman.

Pediatric Use

Ceftizoxime's safety and efficacy in pediatric patients aged from birth to six months have not been established. However, in pediatric patients aged six months and above, the treatment with Ceftizoxime has been linked to temporary increases in eosinophils, AST (SGOT), ALT (SGPT), and CPK (creatine phosphokinase) levels. CPK elevation may be linked to intramuscular administration. The possibility of toxic effects in pediatric patients from chemicals leaching from the single-dose IV preparation in plastic has not been determined.

Geriatric Use

Clinical studies of Ceftizoxime did not include adequate numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Nonetheless, reported clinical experience has not identified any differences in responses between elderly and younger patients. Generally, a low dose of Ceftizoxime should be selected for elderly patients, reflecting the higher frequency of decreased hepatic, renal, or cardiac function, and concomitant disease or drug therapy.

Physicians should be knowledgeable and vigilant about the treatment and identification of overdosage of Ceftizoxime.

Overdosage of Ceftizoxime may result in increased adverse reactions, including gastrointestinal disturbances, skin rash, and hypersensitivity reactions. In cases of severe overdose, patients may experience neurological symptoms such as seizures and confusion.

Treatment for Ceftizoxime overdose typically involves supportive measures such as monitoring vital signs, providing oxygen, and administering intravenous fluids. In severe cases, hemodialysis or peritoneal dialysis may be necessary to remove the drug from the body.

There is no specific antidote for Ceftizoxime overdose, and the use of activated charcoal is not recommended due to the drug's high protein binding capacity. Patients with a known history of hypersensitivity to cephalosporin antibiotics may require treatment with epinephrine and other appropriate medications.

Pharmacodynamics

Ceftizoxime exhibits high resistance to a wide range of beta-lactamases and demonstrates activity against both gram-positive and gram-negative organisms, whether they are aerobic or anaerobic. The drug has minimal side effects and is considered safe and effective in aged patients and those suffering from hematologic disorders.

Pharmacokinetics

The administration of Ceftizoxime via intravenous or intramuscular route resulted in a serum half-life of approximately 1.7 hours. Ceftizoxime has a protein binding capacity of 30%, and it is not subject to metabolism, being excreted from the body through the kidneys within 24 hours. This leads to high concentrations of the drug in the urine, with levels exceeding 6000 μg/mL achieved within two hours of administering a 1-gram dose intravenously. Probenecid can be used to further increase serum levels and prolong the duration of measurable serum concentrations by slowing tubular secretion. Ceftizoxime has been found to achieve therapeutic levels in various body fluids and tissues, including cerebrospinal fluid, bile, surgical wound fluid, pleural fluid, aqueous humor, ascitic fluid, peritoneal fluid, prostatic fluid, saliva, heart, gallbladder, bone, biliary, peritoneal, prostatic, and uterine tissues. To date, no disulfiram-like reactions have been observed with Ceftizoxime in clinical experience.

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