Roxithromycin: Advanced Macrolide Antibiotic for Respiratory Infections
Roxithromycin
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Synonyms
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Roxithromycin is a semi-synthetic macrolide antibiotic derived from erythromycin, specifically engineered to enhance stability, bioavailability, and tolerability. It exerts its antibacterial effect by binding to the 50S ribosomal subunit of susceptible bacteria, inhibiting protein synthesis and leading to bacteriostatic action against a broad spectrum of Gram-positive and some Gram-negative pathogens. Its improved pharmacokinetic profile allows for convenient once- or twice-daily dosing, making it a preferred choice in outpatient management of community-acquired infections, particularly those affecting the upper and lower respiratory tracts. Clinicians value roxithromycin for its reliable efficacy, favorable safety profile, and reduced potential for gastrointestinal side effects compared to earlier macrolides.
Features
- Chemical structure: 14-membered lactone ring with oxime modification enhancing acid stability
- Mechanism: Binds to 50S ribosomal subunit, inhibiting bacterial protein synthesis
- Spectrum: Active against Streptococcus pneumoniae, Streptococcus pyogenes, Staphylococcus aureus, Moraxella catarrhalis, Legionella pneumophila, Chlamydia pneumoniae, and Mycoplasma pneumoniae
- Pharmacokinetics: Rapid oral absorption with 50-60% bioavailability; not significantly affected by food
- Half-life: Approximately 12 hours, enabling once-daily dosing
- Metabolism: Primarily hepatic via cytochrome P450 system
- Excretion: Mainly fecal (53-65%), with renal excretion accounting for 7-15%
- Protein binding: Approximately 90-96%
- Formulations: 150 mg and 300 mg tablets; granules for oral suspension
Benefits
- Effective against atypical pathogens including Mycoplasma, Chlamydia, and Legionella species
- Convenient dosing regimen improves patient compliance compared to multiple-daily antibiotics
- Superior gastric acid stability reduces incidence of gastrointestinal adverse effects
- Favorable tissue penetration, particularly in respiratory tissues and phagocytes
- Lower potential for drug interactions than erythromycin due to reduced cytochrome P450 inhibition
- Well-tolerated profile suitable for extended duration therapy when indicated
Common use
Roxithromycin is primarily indicated for the treatment of mild to moderate community-acquired respiratory infections. Its spectrum of activity makes it particularly valuable for upper respiratory tract infections including pharyngitis, tonsillitis, sinusitis, and otitis media caused by susceptible Streptococcus species. In lower respiratory tract infections, it demonstrates efficacy against bronchitis, community-acquired pneumonia, and exacerbations of chronic bronchitis. Beyond respiratory applications, it is employed in skin and soft tissue infections such as erysipelas, impetigo, and secondary infected dermatoses when caused by susceptible staphylococcal and streptococcal organisms. Some guidelines also support its use in genital infections caused by Chlamydia trachomatis and as prophylaxis against endocarditis in high-risk patients undergoing dental procedures, though this varies by regional recommendations.
Dosage and direction
The standard adult dosage is 300 mg daily, administered either as a single dose or divided as 150 mg twice daily. For more severe infections, the dose may be increased to 300 mg twice daily, not to exceed 600 mg daily. Pediatric dosing is typically 5-8 mg/kg/day divided into two doses, with maximum daily dose not exceeding 10 mg/kg. Administration should occur at least 15 minutes before meals or on an empty stomach to optimize absorption, though food does not significantly affect bioavailability. The usual treatment duration ranges from 5 to 10 days depending on infection severity and clinical response. In renal impairment with creatinine clearance below 30 mL/min, dosage reduction to 150 mg once daily is recommended. Hepatic impairment requires careful monitoring rather than specific dose adjustment. For streptococcal infections, a minimum 10-day course is recommended to prevent rheumatic fever or glomerulonephritis.
Precautions
Roxithromycin should be used with caution in patients with pre-existing liver disease, as hepatic enzyme elevations may occur. Periodic liver function tests are advisable during extended therapy beyond two weeks. QT interval prolongation, though less common than with other macrolides, warrants caution in patients with known cardiac arrhythmias, particularly ventricular tachycardia, or those taking other QT-prolonging medications. Electrolyte imbalances, especially hypokalemia and hypomagnesemia, should be corrected before initiation. The potential for Clostridium difficile-associated diarrhea exists, requiring vigilance for watery or bloody diarrhea during and after treatment. Cross-resistance with other macrolides, lincosamides, and streptogramins should be considered when selecting therapy. Use during pregnancy (Category B) should be reserved for cases where benefits outweigh risks, and breastfeeding mothers should consider alternative feeding options due to excretion in breast milk.
Contraindications
Roxithromycin is contraindicated in patients with known hypersensitivity to macrolide antibiotics or any component of the formulation. Concomitant administration with ergot derivatives (ergotamine, dihydroergotamine) is absolutely contraindicated due to risk of severe vasoconstriction and ergotism. It should not be used with terfenadine, astemizole, or cisapride due to potential for serious cardiac arrhythmias from QT prolongation. Patients with history of hepatitis or jaundice associated with previous macrolide use should avoid roxithromycin. Severe hepatic impairment (Child-Pugh Class C) represents a contraindication due to impaired metabolism and elimination. The combination with pimozide is contraindicated because of increased risk of ventricular arrhythmias.
Possible side effect
The most commonly reported adverse effects involve the gastrointestinal system (approximately 4-6% of patients), including nausea, abdominal pain, diarrhea, vomiting, and dyspepsia. Dermatological reactions such as rash, urticaria, and pruritus occur in approximately 1-2% of patients. Headache and dizziness have been reported in less than 2% of cases. Hepatic effects including transient elevations in liver enzymes, cholestatic hepatitis, and rarely, hepatocellular damage may occur. Cardiac effects including QT prolongation, palpitations, and rare cases of torsades de pointes have been documented. Other infrequent reactions include taste disturbances, stomatitis, glossitis, and transient hearing loss at high doses. Pseudomembranous colitis may develop during or after treatment.
Drug interaction
Roxithromycin demonstrates moderate inhibition of cytochrome P450 3A4, though less potent than erythromycin. Significant interactions occur with CYP3A4 substrates including statins (increased risk of myopathy with simvastatin, lovastatin), benzodiazepines (increased sedation with midazolam, triazolam), and sildenafil (increased plasma concentrations). Anticoagulant effects of warfarin may be enhanced, requiring frequent INR monitoring. Concomitant use with theophylline may increase theophylline concentrations, necessitating level monitoring and potential dose reduction. Digoxin bioavailability may increase due to gut flora alteration. Colchicine toxicity risk increases when co-administered. HIV protease inhibitors and non-nucleoside reverse transcriptase inhibitors may have altered pharmacokinetics. Calcium channel blockers may have enhanced effects requiring blood pressure monitoring.
Missed dose
If a dose is missed, it should be taken as soon as remembered unless it is nearly time for the next scheduled dose. In that case, the missed dose should be skipped and the regular dosing schedule resumed. Doubling the dose to make up for a missed dose is not recommended as it may increase the risk of adverse effects. Patients should be advised to maintain consistent timing of doses to ensure stable antibiotic concentrations. If multiple doses are missed, patients should contact their healthcare provider for guidance on whether to extend the treatment duration. For once-daily dosing regimens, a missed dose taken within 12 hours of the scheduled time can generally be taken and the next dose at the regular time the following day.
Overdose
Symptoms of overdose may include severe nausea, vomiting, diarrhea, and abdominal pain. In massive overdoses, hearing loss, QT prolongation, and ventricular arrhythmias may occur. Management is primarily supportive with gastric lavage if presentation is within one hour of ingestion. Activated charcoal may be administered if no contraindications exist. Cardiac monitoring is essential for 24-48 hours to detect QT prolongation or arrhythmias. Electrolyte abnormalities should be corrected promptly. Hemodialysis is not effective due to high protein binding and extensive tissue distribution. Specific antidotes are not available. Serum levels are not routinely measured as they do not guide management. Patients should receive symptomatic treatment for gastrointestinal distress and adequate hydration. Medical toxicology consultation is recommended for significant ingestions.
Storage
Store at controlled room temperature between 15-30°C (59-86°F) in the original container. Protect from light, moisture, and excessive heat. Keep the container tightly closed to prevent degradation. Do not store in bathroom or kitchen where humidity and temperature fluctuations may occur. Keep out of reach of children and pets. Do not use after the expiration date printed on packaging. For oral suspension, reconstituted product should be stored in refrigerator at 2-8°C (36-46°F) and discarded after 10 days. Tablets should not be removed from blister packaging until immediately before use to maintain stability. Do not freeze any formulation.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Roxithromycin is a prescription medication that should only be used under the supervision of a qualified healthcare professional. The prescribing physician should be consulted for specific diagnostic and treatment decisions. Individual patient factors including allergies, comorbidities, concomitant medications, and renal/hepatic function must be considered before initiation. Healthcare providers should reference official prescribing information and current clinical guidelines. The manufacturer’s package insert contains complete safety and efficacy information. Antibiotic use should be based on confirmed or suspected bacterial infection to avoid contributing to antimicrobial resistance.
Reviews
Clinical studies demonstrate roxithromycin’s efficacy with clinical success rates of 85-92% in respiratory tract infections. A meta-analysis of 15 randomized controlled trials showed equivalent efficacy to amoxicillin-clavulanate with better gastrointestinal tolerability. Pediatric studies indicate similar efficacy to other macrolides with acceptance of once-daily dosing. Post-marketing surveillance data from over 25 million treatments confirms the favorable safety profile, with serious adverse events reported in less than 0.1% of patients. Comparative studies show fewer drug interactions than erythromycin while maintaining clinical effectiveness. Patient satisfaction surveys indicate preference for once-daily dosing compared to multiple-daily regimens, particularly in working adults and elderly populations. Long-term follow-up studies demonstrate minimal impact on normal gut flora compared to broader-spectrum antibiotics.