Ilosone: Potent Macrolide Antibiotic for Bacterial Infection Resolution
Ilosone
| Product dosage: 250 mg | |||
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| Product dosage: 500 mg | |||
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Synonyms | |||
Ilosone (erythromycin estolate) is a cornerstone macrolide antibiotic medication with a well-established efficacy profile against a wide spectrum of Gram-positive and some Gram-negative bacteria. It functions by inhibiting bacterial protein synthesis, effectively halting the growth and proliferation of susceptible organisms. This makes it a trusted choice for healthcare professionals in treating various respiratory, skin, and soft tissue infections. Its formulation is designed for reliable systemic absorption, ensuring therapeutic drug levels are achieved to combat bacterial pathogens effectively.
Features
- Active Ingredient: Erythromycin estolate.
- Drug Class: Macrolide antibiotic.
- Available Formulations: Oral capsules (250 mg, 500 mg), oral suspension (125 mg/5 mL, 250 mg/5 mL), and chewable tablets.
- Mechanism of Action: Binds to the 50S subunit of the bacterial ribosome, inhibiting protein synthesis.
- Spectrum of Activity: Effective against Streptococcus pyogenes, Streptococcus pneumoniae, Staphylococcus aureus (methicillin-susceptible), Corynebacterium diphtheriae, Bordetella pertussis, Legionella pneumophila, Mycoplasma pneumoniae, and Chlamydia trachomatis.
Benefits
- Broad-Spectrum Efficacy: Provides reliable treatment for a diverse range of common bacterial infections, reducing diagnostic uncertainty.
- Proven Clinical History: Decades of use have solidified its safety and effectiveness profile, making it a predictable and trusted therapeutic option.
- Alternative for Penicillin Allergy: Serves as a first-line alternative for patients with hypersensitivity to penicillin, expanding treatment possibilities.
- Convenient Oral Administration: Available in multiple formulations, including a pleasant-tasting suspension, facilitating adherence in both adult and pediatric populations.
- Bacteriostatic Action: Halts bacterial growth, allowing the host’s immune system to effectively clear the infection.
Common use
Ilosone is indicated for the treatment of infections caused by susceptible strains of microorganisms. Common uses include:
- Upper and lower respiratory tract infections (e.g., pharyngitis, tonsillitis, bronchitis, pneumonia, including atypical pneumonia caused by Mycoplasma pneumoniae).
- Skin and skin structure infections of mild to moderate severity (e.g., impetigo, erysipelas, cellulitis).
- Pertussis (whooping cough), as a prophylaxis for exposed individuals and as treatment for the disease.
- Diphtheria, as an adjunct to antitoxin to prevent carriers and eradicate the organism.
- Erythrasma, intestinal amebiasis, and Legionnaires’ disease.
- As an alternative agent for the treatment of primary syphilis in penicillin-allergic patients.
Dosage and direction
Dosage must be individualized based on the severity of the infection and the patient’s age, weight, and renal function. It is typically administered orally.
- Adults: The usual dose ranges from 250 mg to 500 mg every 6 hours, or 500 mg to 1 g every 12 hours. For more severe infections, doses up to 4 grams per day may be required.
- Children: The usual dosage is 30 to 50 mg/kg/day in divided doses every 6 hours. For more severe infections, this may be doubled.
- Administration: Should be taken on an empty stomach (1 hour before or 2 hours after meals) for optimal absorption, unless significant gastrointestinal upset occurs, in which case it may be taken with food (note: this may slightly decrease absorption). The suspension and chewable tablets must not be crushed or chewed, respectively, if meant to be swallowed whole. The suspension should be shaken vigorously before each use.
Precautions
- Hepatotoxicity: Erythromycin estolate has been associated with drug-induced cholestatic hepatitis. Liver function tests should be monitored in patients receiving prolonged therapy (over 10-14 days) or high doses. Therapy should be discontinued if symptoms such as malaise, nausea, vomiting, abdominal colic, or fever occur, followed by jaundice.
- Prolonged Use: May result in the overgrowth of non-susceptible bacteria or fungi. If a superinfection occurs during therapy, appropriate measures should be taken.
- Clostridium difficile-Associated Diarrhea (CDAD): Antibiotic use can cause colitis, which may range in severity from mild to life-threatening. This diagnosis should be considered in patients who present with diarrhea subsequent to antibiotic administration.
- QT Prolongation: Erythromycin has been associated with prolongation of the QT interval and rare cases of arrhythmias, including torsades de pointes. Use with caution in patients with known QT prolongation, electrolyte imbalances, or those taking other drugs that prolong the QT interval.
- Myasthenia Gravis: May exacerbate muscle weakness in patients with myasthenia gravis.
Contraindications
Ilosone is contraindicated in patients with:
- Known hypersensitivity to erythromycin or any other macrolide antibiotic.
- Pre-existing liver disease or a history of previous hepatotoxicity with this drug.
- Concomitant administration with drugs that are potent CYP3A4 substrates and known to prolong the QT interval (e.g., astemizole, cisapride, pimozide, terfenadine), due to the risk of serious cardiac arrhythmias.
Possible side effect
Side effects are generally dose-related and often gastrointestinal in nature.
- Common: Nausea, vomiting, abdominal pain, cramping, diarrhea, and anorexia.
- Less Common: Mild skin rashes, urticaria, and other allergic reactions.
- Rare but Serious: Cholestatic hepatitis (characterized by jaundice), pseudomembranous colitis, QT interval prolongation, ventricular arrhythmias, and reversible hearing loss (usually with high doses in patients with renal impairment).
Drug interaction
Erythromycin is a potent inhibitor of the cytochrome P450 enzyme system (CYP3A4). Concomitant use can lead to increased plasma concentrations of other drugs metabolized by this pathway, potentially leading to serious adverse effects.
- Significant Interactions: Carbamazepine, cyclosporine, digoxin, disopyramide, ergot alkaloids, lovastatin, simvastatin, phenytoin, theophylline, triazolam, valproate, warfarin, and verapamil.
- QT Prolonging Drugs: Concomitant use with other drugs known to prolong the QT interval (e.g., certain antiarrhythmics, antipsychotics, antidepressants, fluoroquinolones) is not recommended due to additive effects.
- Other Antibiotics: May antagonize the bactericidal effects of penicillins or other beta-lactam antibiotics; concurrent use is not recommended.
Missed dose
If a dose is missed, it should be taken as soon as it is remembered. However, if it is almost time for the next scheduled dose, the missed dose should be skipped, and the regular dosing schedule resumed. Do not double the dose to make up for the missed one.
Overdose
Symptoms of overdose are primarily an extension of the drug’s known adverse effects, including severe nausea, vomiting, diarrhea, and abdominal pain. Reversible hearing loss may occur. The drug is not removed by peritoneal dialysis or hemodialysis. Treatment should be supportive and symptomatic. Gastric lavage may be considered if ingestion was recent.
Storage
- Store at room temperature (20°-25°C or 68°-77°F) in a tight, light-resistant container.
- Keep the bottle tightly closed and protect from excessive moisture.
- Do not freeze the oral suspension.
- Keep all medications out of the reach of children and pets.
Disclaimer
This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or before starting any new treatment. Never disregard professional medical advice or delay in seeking it because of something you have read here.
Reviews
(Compilation of expert clinical consensus and pharmacologic reviews) Ilosone (erythromycin estolate) remains a valuable agent in the antimicrobial arsenal. Its broad spectrum of activity and utility as a penicillin alternative are its primary strengths. Clinical reviews consistently highlight its efficacy in treating respiratory tract infections, skin/soft tissue infections, and pertussis. The main drawbacks noted in the literature are its gastrointestinal side effect profile and the potential for hepatotoxicity with the estolate salt, particularly in adults receiving therapy for longer than two weeks. Its significant drug interaction potential mandates careful review of a patient’s concomitant medications. Overall, when used appropriately with attention to its contraindications and precautions, it is considered a safe and effective antibiotic.