Usage
Cefditoren, a third-generation cephalosporin antibiotic, is prescribed for the treatment of various bacterial infections. These include:
- Acute bacterial exacerbation of chronic bronchitis: Caused by susceptible strains of Haemophilus influenzae, Haemophilus parainfluenzae, Streptococcus pneumoniae, and Moraxella catarrhalis.
- Community-acquired pneumonia: Caused by susceptible strains of Streptococcus pneumoniae, Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, Klebsiella pneumoniae, and Staphylococcus aureus (methicillin-susceptible strains).
- Pharyngitis/Tonsillitis: Caused by susceptible strains of Streptococcus pyogenes.
- Uncomplicated Skin and Skin Structure Infections: Caused by susceptible strains of Staphylococcus aureus (methicillin-susceptible strains) and Streptococcus pyogenes.
Pharmacological Classification: Cefditoren is classified as a third-generation cephalosporin antibiotic.
Mechanism of Action: Cefditoren inhibits bacterial cell wall synthesis by binding to and inactivating penicillin-binding proteins (PBPs). This leads to bacterial cell lysis and death.
Alternate Names
Cefditoren is also known as cefditoren pivoxil (the prodrug form). Brand names include Spectracef, Meiact, and Zostom.
How It Works
Pharmacodynamics: Cefditoren exerts its bactericidal effect by disrupting bacterial cell wall synthesis. It binds to penicillin-binding proteins (PBPs), which are essential enzymes for the final steps of peptidoglycan synthesis. This binding inhibits PBP cross-linking activity, leading to cell wall instability, lysis, and bacterial death.
Pharmacokinetics: Cefditoren pivoxil, the orally administered prodrug, is well-absorbed from the gastrointestinal tract and rapidly hydrolyzed to the active cefditoren by esterases. Food enhances absorption. It reaches peak plasma concentrations within 2 to 3 hours. Cefditoren has a volume of distribution of approximately 0.25 L/kg and is about 88% bound to plasma proteins. Metabolism is minimal. Cefditoren is primarily excreted unchanged in the urine, with a half-life of 1.6 hours. Renal excretion involves both glomerular filtration and active tubular secretion.
Elimination Pathways: Primarily renal excretion.
Dosage
Standard Dosage
Adults:
- Chronic Bronchitis: 400 mg orally every 12 hours for 10 days.
- Community-Acquired Pneumonia: 400 mg orally every 12 hours for 14 days.
- Pharyngitis/Tonsillitis, Uncomplicated Skin and Skin Structure Infections: 200 mg orally every 12 hours for 10 days.
Children:
- Children under 12 years: Not generally recommended. Some regional variations exist for granule formulations in specific infections like pneumonia or rhinosinusitis at dosages adjusted for weight, with a maximum daily dosage limit. These pediatric dosages should be based on local guidelines.
- Children 12 years and older: Same as adult dosing.
Special Cases:
- Elderly Patients: No dose adjustment is necessary with normal renal function.
- Patients with Renal Impairment:
- CrCl 30-49 mL/minute/1.73 m²: Maximum 200 mg every 12 hours.
- CrCl <30 mL/minute/1.73 m²: Maximum 200 mg once daily.
- End-stage renal disease: Dosage not established.
- Patients with Hepatic Dysfunction: No dose adjustment is necessary for mild to moderate impairment. Use with caution in severe hepatic impairment.
- Patients with Comorbid Conditions: Caution should be exercised in patients with a history of penicillin allergy, gastrointestinal disease (especially colitis), seizure disorders, and those at risk for decreased prothrombin activity.
Clinical Use Cases
Cefditoren is generally not indicated for use in clinical settings such as intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. Its primary use is for oral treatment of the specific infections mentioned previously.
Dosage Adjustments
Dose adjustments are primarily based on renal function (see above).
Side Effects
Common Side Effects
Diarrhea, headache, nausea, vomiting, abdominal pain, constipation, vaginal itching or discharge, rash.
Rare but Serious Side Effects
- Clostridium difficile-associated diarrhea, Stevens-Johnson Syndrome, Seizures, Anaphylaxis, Pseudomembranous colitis, Hepatic dysfunction, Renal dysfunction, Blood dyscrasias.
Long-Term Effects
Carnitine deficiency may occur with prolonged use.
Adverse Drug Reactions (ADR)
Anaphylaxis, severe skin reactions (Stevens-Johnson Syndrome, toxic epidermal necrolysis), Clostridium difficile-associated diarrhea, Hepatitis, Acute renal failure, Agranulocytosis, Thrombocytopenia.
Contraindications
- Hypersensitivity to cefditoren or other cephalosporins.
- Carnitine deficiency or inborn errors of metabolism leading to carnitine deficiency.
- Milk protein hypersensitivity (due to the presence of sodium caseinate in some formulations).
Drug Interactions
- Antacids (aluminum or magnesium-containing): Reduced cefditoren absorption. Administer at least 2 hours apart.
- H2-receptor antagonists (e.g., famotidine): Reduced cefditoren absorption.
- Probenecid: Increases cefditoren plasma concentration.
- Anticoagulants: May potentiate anticoagulant effects.
- Bacteriostatic antibiotics: May antagonize cefditoren’s bactericidal activity.
- Oral contraceptives: Potential for reduced contraceptive efficacy (though not definitively established).
Pregnancy and Breastfeeding
- Pregnancy: Pregnancy Category B. Use only if clearly needed.
- Breastfeeding: Cefditoren is excreted in rat milk. Caution is advised in human breastfeeding.
Drug Profile Summary
- Mechanism of Action: Inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins.
- Side Effects: Diarrhea, headache, nausea, vomiting, abdominal pain, rare but serious effects include C. difficile infection, Stevens-Johnson syndrome, seizures.
- Contraindications: Cephalosporin allergy, carnitine deficiency, milk protein hypersensitivity.
- Drug Interactions: Antacids, H2-receptor antagonists, probenecid, anticoagulants.
- Pregnancy & Breastfeeding: Use with caution if benefits outweigh risks.
- Dosage: Refer to detailed dosage section above.
- Monitoring Parameters: Renal function, signs of superinfection (e.g., thrush, vaginal yeast infection), signs of allergic reaction.
Popular Combinations
Cefditoren is not typically used in combination with other antibiotics.
Precautions
- History of penicillin allergy.
- Renal/hepatic impairment.
- Gastrointestinal disease (colitis).
- Seizure disorders.
- Monitor for signs of superinfection.
- Concomitant use of anticoagulants.
FAQs
Q1: What is the recommended dosage for Cefditoren?
A: See detailed dosage section above for adult, pediatric, and special population dosing.
Q2: What are the most common side effects?
A: The most common side effects are diarrhea, headache, nausea, and vomiting.
Q3: Is Cefditoren safe in pregnancy?
A: Cefditoren is Pregnancy Category B. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Q4: Can Cefditoren be used in patients with renal impairment?
A: Yes, but dosage adjustments are often necessary depending on the degree of impairment. See the detailed dosage guidelines above.
Q5: What are the contraindications to Cefditoren use?
A: Hypersensitivity to cefditoren or other cephalosporins, carnitine deficiency, and milk protein hypersensitivity.
Q6: Does Cefditoren interact with other medications?
A: Yes, cefditoren can interact with antacids, H2-receptor antagonists, probenecid, and anticoagulants among others.
Q7: What is the mechanism of action of Cefditoren?
A: Cefditoren inhibits bacterial cell wall synthesis by binding to and inactivating penicillin-binding proteins (PBPs).
Q8: How is Cefditoren eliminated from the body?
A: Primarily through renal excretion.
Q9: What type of antibiotic is Cefditoren?
A: It is a third-generation cephalosporin antibiotic.
Q10: What infections is Cefditoren commonly used to treat?
A: Cefditoren is used to treat community-acquired pneumonia, acute bacterial exacerbations of chronic bronchitis, pharyngitis/tonsillitis, and uncomplicated skin and skin structure infections.
