Ximeprox

Approved Indications:

• Respiratory Tract Infections:
• Community-acquired pneumonia (mild to moderate)
• Acute exacerbation of chronic bronchitis
• Acute maxillary sinusitis
• Pharyngitis and tonsillitis
• Skin and Skin Structure Infections:
• Uncomplicated skin and soft tissue infections
• Urinary Tract Infections:
• Uncomplicated cystitis
• Sexually Transmitted Infections:
• Uncomplicated gonorrhea (cervical, urethral, rectal)
• Otitis Media:
• Acute otitis media in children
• Pediatric Bacterial Infections:
• Age-appropriate acute infections caused by susceptible organisms

Clinically Accepted Off-label Uses:

• Prophylaxis in urologic procedures (limited evidence)
• Mild diabetic foot infections (when culture-guided)
• Treatment of typhoid fever (in regions with known susceptibility)

General Administration:

• Route: Oral (administered with food to enhance absorption)
• Dosage Forms: Tablets (100 mg, 200 mg), oral suspension (50 mg/5 mL, 100 mg/5 mL)

Adults:

• Community-acquired pneumonia: 200 mg twice daily for 10–14 days
• Acute exacerbation of chronic bronchitis: 200 mg twice daily for 10 days
• Pharyngitis/Tonsillitis: 100 mg twice daily for 5–10 days
• Acute maxillary sinusitis: 200 mg twice daily for 10 days
• Uncomplicated urinary tract infections: 100 mg twice daily for 7 days
• Uncomplicated gonorrhea: 200 mg single dose

Pediatrics:

• Acute otitis media & other infections: 10 mg/kg/day divided every 12 hours
• Max dose: 200 mg/day
• Duration: 5–10 days depending on severity and site

Elderly:

• Dose as in adults unless renal function is impaired.

Renal Impairment:

• Creatinine clearance <30 mL/min: Dose adjustment required
• E.g., 100–200 mg once daily

Hepatic Impairment:

• No dosage adjustment typically required.

Cefpodoxime Proxetil is an oral third-generation cephalosporin prodrug that, upon absorption, is hydrolyzed to its active form, cefpodoxime. It acts by inhibiting bacterial cell wall synthesis through binding to penicillin-binding proteins (PBPs), which interferes with the final transpeptidation step of peptidoglycan synthesis. This results in weakened bacterial cell walls and cell lysis. Its bactericidal activity covers a broad range of Gram-positive and Gram-negative organisms.

• Absorption: ~50% bioavailability when taken with food
• Peak Plasma Concentration: 2–3 hours post-dose
• Distribution: Widely distributed; moderate protein binding (~22–33%)
• Metabolism: Minimal hepatic metabolism
• Excretion: Primarily renal (over 80% unchanged in urine)
• Half-life: ~2–3 hours (prolonged in renal impairment)

• Pregnancy: Not assigned a formal FDA pregnancy category; animal studies show no teratogenicity. Use only if clearly needed during pregnancy.
• Lactation: Excreted in breast milk in low amounts. Generally considered safe during breastfeeding; monitor infant for gastrointestinal disturbances (e.g., diarrhea or thrush).
• Caution: Limited human data; avoid in neonates <2 months due to immature renal function.

• Primary Class: Third-generation cephalosporin antibiotic
• Subclass: Oral cephalosporin
• Spectrum: Broad-spectrum (Gram-positive & Gram-negative coverage)

• Known hypersensitivity to cefpodoxime, cephalosporins, or any component of the formulation
• History of severe hypersensitivity reactions (e.g., anaphylaxis) to penicillins or other beta-lactams
• Neonates under 2 months (due to immature renal function)

• Hypersensitivity Reactions: Risk of cross-reactivity in penicillin-allergic patients
• Clostridium difficile–associated diarrhea (CDAD): Can range from mild diarrhea to fatal colitis
• Renal Impairment: Dose adjustment required; monitor renal function in long-term use
• Seizures: Rare, but can occur with high doses, especially in renal dysfunction
• Prolonged Use: May lead to superinfections, including fungal overgrowth
• Laboratory Monitoring: Periodic renal and hepatic function tests during prolonged therapy

Common:

• Gastrointestinal: Diarrhea, nausea, abdominal pain, vomiting
• CNS: Headache, dizziness
• Skin: Rash, pruritus
• Others: Vaginal candidiasis

Serious:

• Hypersensitivity: Anaphylaxis, angioedema
• Hematologic: Thrombocytopenia, eosinophilia, leukopenia
• Renal: Interstitial nephritis (rare)
• GI: Pseudomembranous colitis

Timing & Severity:

• Onset: Usually within first few days of therapy
• Dose-dependent: Some GI effects more likely with higher doses

• Antacids/H2-blockers: Decrease absorption of cefpodoxime; separate dosing by ≥2 hours
• Probenecid: Increases serum levels by reducing renal excretion
• Live bacterial vaccines (e.g., typhoid): Antibiotic may reduce vaccine effectiveness
• Loop diuretics/aminoglycosides: Increased risk of nephrotoxicity (caution advised)

Enzyme Systems:

• Not a substrate or inhibitor of CYP450 enzymes

• WHO/IDSA Guidelines (latest): Cefpodoxime is no longer first-line for gonorrhea due to emerging resistance; ceftriaxone preferred
• Emerging Resistance Trends: Resistance in E. coli and Klebsiella species rising in Asia-Pacific regions; use based on susceptibility testing
• Pediatric Dosing Update: Weight-based dosing emphasized over age-only criteria in children

• Tablets: Store below 25°C; protect from moisture and light
• Oral Suspension (dry powder):
• Store at or below 25°C before reconstitution
• After reconstitution: refrigerate at 2°C–8°C; use within 14 days
• Shake well before each use
• Handling Precautions: Keep out of reach of children; do not freeze suspension