Erimycin For Suspension

Each 5 mL contains Erythromycin ethylsuccinate 234.913 mg is equivalent to Erythromycin 200 mg.

Pharmacology: Pharmacodynamics: Erythromycin is a macrolide antibacterial with a broad and essentially bacteriostatic action against many Gram-positive and to a lesser extent some Gram-negative bacteria. Erythromycin binds to the 50S ribosomal subunit of susceptible organisms, resulting in inhibition of protein synthesis and hence inhibition of cell growth.
Erythromycin is active against: Gram-positive such as Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumoniae, Viridans group streptococci, Listeria monocytogenes, Corynebacterium diphtheriae and Corynebacterium minutissimum.
Gram-negative organism including Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Legionella pneumophila and Neisseria gonorrhoeae.
Some strains of Chlamydia trachomatis, Mycoplasma pneumoniae, Treponema pallidum, Ureaplasma urealyticum, Entamoeba histolytica and Clostridium tetani.
Pharmacokinetics: Absorption: Erythromycin base is an unstable in gastric acid and absorption is variable and unreliable. The bioavailability is 18-45%. Erythromycin ethylsuccinate is an ester of Erythromycin suitable for oral administration. The ester is generally more reliably and quickly absorbed. Erythromycin ethylsuccinate is partially dissociated in the intestine where both erythromycin and the undissociated ester are absorbed. In the blood, the ester is partially hydrolyzed to release free erythromycin. Peak serum concentrations given orally in 4 doses daily are higher than single dose. Oral administration of 400 mg of Erythromycin ethylsuccinate 4 times daily maintains antibacterial serum concentrations of 0.1-2 mcg/mL. Time to peak serum of Erythromycin ethylsuccinate is 1-2 hours.
Erythromycin ethylsuccinate may be administered without regard to meals.
Distribution: Erythromycin is widely distributed throughout body tissue and fluids. Although it does not cross the blood-brain barrier well and low concentrations (2-13% of serum concentrations) are distributed into CSF. Erythromycin base is 73-81% bound to serum proteins.
Metabolism: Erythromycin is partly metabolized in the liver by the cytochrome P450 isoenzyme CYP3A4 by N-demethylation to inactive, unidentified metabolites.
Elimination: Erythromycin is mainly excreted unchanged via bile and undergoes intestinal reabsorption. About 2-15% of an oral dose is excreted unchanged in the urine. Only small amounts of erythromycin are removed by hemodialysis. The half-life of Erythromycin is about 1.5 to 2.5 hours. In patients with renal impairment may be prolonged half-life and has been reported to be between 4 to 7 hours.

Erythromycin is indicated for the treatment of infections caused by susceptible strains in the following diseases: 1. Respiratory tract infection: Upper respiratory tract infection of mild to moderate degree caused by Streptococcus pyogenes, Streptococcus pneumoniae, or Haemophilus influenzae (when used concomitantly with adequate doses of sulfonamides). Lower respiratory tract infection of mild to moderate severity caused by Streptococcus pneumoniae or Streptococcus pyogenes. Moreover, respiratory tract infection due to Mycoplasma pneumoniae.
2. Skin infection: Mild to moderate severity caused by Streptococcus pyogenes or Staphylococcus aureus.
3. Erythrasma caused by Corynebacterium minutissimum.
4. Prevention of initial attacks of rheumatic fever and prevention of recurrent attacks of rheumatic fever: As an alternative treatment in penicillin-allergic patients.
5. Acute pelvic inflammatory disease caused by Neisseria gonorrhoeae: As an alternative treatment in penicillin-allergic patients.
6. Nongonococcal urethritis: As an alternative to azithromycin or doxycycline for the treatment of nongonococcal urethritis that caused by Ureaplasma urealyticum.
7. Chlamydial infections: As an alternative to azithromycin or tetracyclines for the treatment of uncomplicated urethral, endocervical or rectal infections that caused by Chlamydia trachomatis. Moreover, the treatment of chlamydial urogenital infections during pregnancy and the treatment of pneumonia or ophthalmic neonatorum in infants caused by C. trachomatis are used.
8. Diphtheria caused by Corynebacterium diphtheriae, as an adjunct to antitoxin, to prevent establishment of carriers and to eradicate the organism in carriers.
9. Pertussis caused by Bordetella pertussis.
10. Legionnaire disease caused by Legionella pneumophila.
11. Intestinal amebiasis caused by Entamoeba histolytica.

Mode of Administration: ERIMYCIN FOR SUSPENSION administered by orally, may be administered without regard to meals or may be administered with food to decrease GI upset. Do not give with milk or acidic beverages.
How supplied ERIMYCIN FOR SUSPENION: To make up to volume, add 2/3 marked volume of water, shake the bottle well and then add water to the marked line. The reconstituted suspension should be stored in a refrigerator (2-8°C), and used within 7 days. Shake well before taking each dose.
Dosage: Due to differences in absorption, 400 mg of Erythromycin ethylsuccinate provide 250 mg of Erythromycin activity as the stearate, bases or estolate.
Usual dosage in children: The usual oral dosage of Erythromycin ethylsuccinate in children is 30-50 mg/kg daily in 4 equally divided doses every 6 hours. Maximum dose 3.2 g daily. Erythromycin ethylsuccinate should be administered for at least 10 days for Streptococcal infections.
Indication-specific dosing: See Table 1.

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Usual dosage in adult: The usual adult oral dosage of Erythromycin ethylsuccinate is 400 mg every 6 hours. Dosage may be increased up to 4 g daily according to the severity of the infection. Maximum dose 4 g daily.
Erythromycin ethylsuccinate should be administered for at least 10 days for Streptococcal infections.
Indication-specific dosing: See Table 2.

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Renal impairment: Since renal excretion is not a major route of elimination of Erythromycin and prolongation of serum half-life of the drug is not clinically important. No supplemental dosage necessary in hemo- or peritoneal dialysis or in continuous arteriovenous or venovenous hemofiltration.
Hepatic impairment: No dosage adjustment; use with caution.

Overdose and Treatment: In case of overdosage, Erythromycin should be discontinued. Overdosage should be handles with the prompt elimination of unabsorbed drug and all other appropriate measures should be instituted. Erythromycin is not removed by peritoneal dialysis or hemodialysis.

1.Hypersensitivity to Erythromycin, any macrolide antibiotics, or any component of the formulation.
2. Concomitant use with pimozide, cisapride, ergotamine or dihydroergotamine, terfenadine, astemizole, lovastatin, or simvastatin.

1. It is contraindicated in patients with Erythromycin hypersensitivity.
2. Erythromycin may cause hepatotoxicity.

Hepatic function impairment including increased liver enzymes, and hepatocellular and/or cholestatic hepatitis, with or without jaundice has occurred in patients receiving oral Erythromycin. Use caution with hepatic impairment with or without jaundice.
Macrolides have been associated with rare QTc prolongation and ventricular arrhythmias, including torsade de pointes. Avoid use in patients with prolonged QT interval, uncorrected hypokalemia or hypomagnesemia, clinically significant bradycardia or concurrent use of Class IA (i.e. quinidine, procainamide) or Class III (i.e. amiodarone, dofetilide, sotalol) antiarrhythmic agents.
Prolonged use may result in fungal or bacterial superinfection including Clostridium difficile-associated diarrhea (CDAD) and pseudomembranous colitis; CDAD has been observed > 2 months post-antibiotic treatment.
Erythromycin may aggravate muscle weakness in patients with myasthenia gravis.
Use in Children: Use in infants has been associated with infantile hypertrophic pyloric stenosis (IHPS).

Pregnancy: Pregnancy category B.
Erythromycin crosses the placenta and low concentrations are found in the fetal serum. Serum concentrations of Erythromycin may be variable in pregnant women.
The patients with acute infections during pregnancy, Erythromycin may be given if an antibiotic is required and appropriate based on bacterial sensitivity.
Lactation: Erythromycin is excreted in breast milk. Caution should be exercised when administrating Erythromycin to breast-feeding or nursing women.

Erythromycin and its esters (Erythromycin ethylsuccinate) are generally well tolerated and serious adverse effects are rare. The adverse effect was shown in the table as follows. (See Table 3.)

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1. Antifungal agent: Concomitant use of Erythromycin with these drugs that inhibit CYP3A isoenzyme (i.e., fluconazole, ketoconazole, itraconazole) increases Erythromycin plasma concentration. The result of this effect increases risk of QT prolongation (a dose-associated effect of Erythromycin) and serious ventricular arrhythmias. Should be avoid this combination.
2. Astemizole and Terfenadine: Erythromycin may interaction with astemizole and terfenadine, resulting in potentially serious adverse cardiovascular effects (prolongation of the QT interval, ventricular tachycardia, torsades de pointes). Coadministration is contraindication.
3. Calcium-channel blocking agents: Concomitant use with diltiazem or verapamil; presumably increased serum concentrations of both drugs resulting in an increased risk of QT prolongation (a dose-associated effect of Erythromycin) and serious ventricular arrhythmias or cardiotoxicity and hypotension. Should be avoid this combination.
4. Cisapride: Erythromycin inhibits cytochrome P450 enzymes that metabolize cisapride (CYP3A4) and increase plasma cisapride concentrations, which may increase the potential for serious adverse effects (e.g., life-threatening cardiac arrhythmias). Coadministration is contraindication.
5. Digoxin: Concomitant use of Erythromycin and digoxin has resulted in increased serum concentration of digoxin; toxicity may occur. Monitor digoxin levels and adjust dose as needed.
6. Carbamazepine: Concomitant use of Erythromycin and carbamazepine has resulted in increased serum concentration of carbamazepine and subsequent signs of carbamazepine toxicity (e.g. ataxia, dizziness, drowsiness, and vomiting). Should be avoid this combination.
7. Cyclosporine: Concomitant use of Erythromycin and cyclosporine has resulted in increased serum concentration of cyclosporine subsequent signs of cyclosporine toxicity (e.g. nephrotoxicity, neurotoxicity). Monitor cyclosporine levels and serum creatinine; adjust dose as needed.
8. Ergot alkaloids: Concomitant use of Erythromycin and ergotamine may induce ischemic reactions, peripheral vasospasm and dysesthesia. Coadministration is contraindication.
9. Benzodiazepines (i.e. alprazolam, diazepam, midazolam, triazolam): Coadministration may decrease the metabolism of certain benzodiazepines resulting in increased CNS depression and prolonged sedation. Use with caution.
10. Theophylline: Concomitant use of Erythromycin and theophylline may decrease clearance of theophylline, elevate serum concentrations of theophylline, and a prolong serum half-life of the bronchodilator. Monitor theophylline levels.
11. Warfarin: Concomitant use of Erythromycin and warfarin may increase the anticoagulant effect of warfarin. Bleeding has occurred. Increased anticoagulant effect may be more pronounced in geriatric patients. Monitor anticoagulant parameters and adjust the warfarin dose as needed.

Store below 30°C.
The reconstituted suspension should be stored in a refrigerator (2-8°C), and used within 7 days.

Macrolides

J01FA01 - erythromycin ; Belongs to the class of macrolides. Used in the systemic treatment of infections.

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