Mechanism of Action
Erythromycin and other macrolide antibiotics inhibit protein synthesis by binding to the 23S rRNA molecule (in the 50S subunit) of the bacterial ribosome blocking the exit of the growing peptide chain of sensitive microorganism
Mechanism of Resistance
The major route of resistance is modification of the 23S rNA in the 50S ribosomal subunit to insensitivity while efflux can also be significant.
Interactions with Other Antibiotics
Antagonism exists in vitro between erythromycin and clindamycin, lincomycin, and chloramphenicol.
Erythromycin has been shown to be active against most isolates of the following bacteria both in vitro and in clinical infections as described in the INDICATIONS AND USAGE section.
Gram-positive Bacteria
Corynebacterium diphtheriae
Corynebacterium minutissimum
Listeria monocytogenes
Staphylococcus aureus (resistant organisms may emerge during treatment)
Streptococcus pneumoniae
Streptococcus pyogenes
Gram-negative Bacteria
Bordetella pertussis
Haemophilus influenzae
Legionella pneumophila
Neisseria gonorrhoeae
Other Microorganisms
Chlamydia trachomatis
Entamoeba histolytica
Mycoplasma pneumoniae
Treponema pallidum
Ureaplasma urealyticum
Asomycin, Astra Lifecare
Biotrocin, Biodeal Laboratories Ltd.
Elocin , Elys Chemical Industries Ltd
Erilide, Plethico
Erocin, Laboratory & Allied Ltd
Erocos, Cosmos Limited
Erocos-ST, Cosmos
Eromycin, Square Pharmaceuticals Ltd.
Erythromed , Medisel Kenya Limited
Erythrolite, Skylight Chemical Industries
Erythromycin, Shelys
Erycin, Flamingo
Erygyl , Harleys Limited
Erymed, Medipharm
Erythro, National Pharmacy Ltd
Erythromax, Mac’s
Erythromycin , Medopharm
Erythromycin, Macleods Pharmaceuticals Limited
Erythroriv, Riva
Erythrox, Dawa Limited
Erythrozen, Zenufa
Erythyl, Regal Pharmaceuticals Limited
Ethro, Universal Corporation Limited
Etocin, Cadila Pharmaceuticals (EA) Ltd
Indo, Indoco Remedies Limited
Labcin, Laborate pharmaceuticals India Limited
Medithrocin, Medivet
Rythro, Medreich
Rythrocin, Gesto
Throcin, Zest pharma
INDICATIONS AND DOSAGE
In most patients, Erythromycin are well absorbed and may be dosed orally without regard to meals. However, optimal blood levels are obtained when Erythromycin tablets are given in the fasting state (at least 1/2 hour after and preferably 2 hours before meals).
Adults
The usual dose is 250 mg four times daily in equally spaced doses. The 333 mg tablet is recommended if the dosage is desired every 8 hours. If twice-a-day dosage is desired, the recommended dose is 500 mg every 12 hours. Dosage may be increased up to 4 g per day according to the severity of the infection. However, twice-a-day dosing is not recommended when doses larger than 1 g daily are administered.
Children
Age, weight, and severity of the infection are important factors in determining the proper dosage. The usual dosage is 30 to 50 mg/kg/day, in equally divided doses. For more severe infections, this dose may be doubled but should not exceed 4 g per day.
In the treatment of streptococcal infections of the upper respiratory tract (e.g., tonsillitis or pharyngitis), the therapeutic dosage of erythromycin should be administered for at least ten days.
The American Heart Association suggests a dosage of 250 mg of erythromycin orally, twice a day in long-term prophylaxis of streptococcal upper respiratory tract infections for the prevention of recurring attacks of rheumatic fever in patients allergic to penicillin and sulfonamides.4
- Conjunctivitis of the Newborn Caused by Chlamydia trachomatis
Oral erythromycin suspension 50 mg/kg/day in 4 divided doses for at least 2 weeks.
- Pneumonia of Infancy Caused by Chlamydia trachomatis
Although the optimal duration of therapy has not been established, the recommended therapy is oral erythromycin suspension 50 mg/kg/day in 4 divided doses for at least 3 weeks.
- Urogenital Infections During Pregnancy Due to Chlamydia trachomatis
Although the optimal dose and duration of therapy have not been established, the suggested treatment is 500 mg of erythromycin by mouth four times a day or two erythromycin 333 mg tablets orally every 8 hours on an empty stomach for at least 7 days. For women who cannot tolerate this regimen, a decreased dose of one erythromycin 500 mg tablet orally every 12 hours, one 333 mg tablet orally every 8 hours or 250 mg by mouth four times a day should be used for at least 14 days.6
- For adults with uncomplicated urethral, endocervical, or rectal infections caused by Chlamydia trachomatis, when tetracycline is contraindicated or not tolerated
500 mg of erythromycin by mouth four times a day or two 333 mg tablets orally every 8 hours for at least 7 days.6
- For patients with nongonococcal urethritis caused by Ureaplasma urealyticum when tetracycline is contraindicated or not tolerated
500 mg of erythromycin by mouth four times a day or two 333 mg tablets orally every 8 hours for at least seven days.6
- Primary Syphilis
30 to 40 g given in divided doses over a period of 10 to 15 days.
- Acute pelvic inflammatory disease caused byN. gonorrhoeae
500 mg Erythrocin Lactobionate-I.V. (erythromycin lactobionate for injection, USP) every 6 hours for 3 days, followed by 500 mg of erythromycin base orally every 12 hours, or 333 mg of erythromycin base orally every 8 hours for 7 days.
- Intestinal Amebiasis
Adults
500 mg every 12 hours, 333 mg every 8 hours or 250 mg every 6 hours for 10 to 14 days.
Children
30 to 50 mg/kg/day in divided doses for 10 to 14 days.
- Pertussis
Although optimal dosage and duration have not been established, doses of erythromycin utilized in reported clinical studies were 40 to 50 mg/kg/day, given in divided doses for 5 to 14 days.
- Legionnaires’ Disease
Although optimal dosage has not been established, doses utilized in reported clinical data were 1 to 4 g daily in divided doses.
- Preoperative Prophylaxis for Elective Colorectal Surgery
Listed below is an example of a recommended bowel preparation regimen.
A proposed surgery time of 8:00 a.m. has been used.
Pre-op Day 3
Minimum residue or clear liquid diet. Bisacodyl, 1 tablet orally at 6:00 p.m.
Pre-op Day 2
Minimum residue or clear liquid diet. Magnesium sulfate, 30 mL, 50% solution (15 g) orally at 10:00 a.m., 2:00 p.m. and 6:00 p.m. Enema at 7:00 p.m. and 8:00 p.m.
Pre-op Day 1
Clear liquid diet. Supplemental (IV) fluids as needed. Magnesium sulfate, 30 mL, 50% solution (15 g) orally at 10:00 a.m. and 2:00 p.m. Neomycin sulfate (1.0 g) and erythromycin base (two 500 mg tablets, three 333 mg tablets or four 250 mg tablets) orally at 1:00 p.m., 2:00 p.m. and 11:00 p.m. No enema.
Day of Operation
Patient evacuates rectum at 6:30 a.m. for scheduled operation at 8:00 a.m.
CONTRAINDICATIONS
Erythromycin is contraindicated in patients with known hypersensitivity to this antibiotic.
Erythromycin is contraindicated in patients taking terfenadine, astemizole, cisapride, pimozide, ergotamine, or dihydroergotamine
DRUG INTERACTIONS
There have been reports of increased anticoagulant effects when erythromycin and oral anticoagulants were used concomitantly. Increased anticoagulation effects due to interactions of erythromycin with oral anticoagulants may be more pronounced in the elderly.
Erythromycin has been reported to decrease the clearance of triazolam and midazolam, and thus, may increase the pharmacologic effect of these Triazolobenzodiazepines.
Erythromycin use in patients who are receiving high doses of theophylline may be associated with an increase in serum theophylline levels and potential theophylline toxicity
Concomitant administration of erythromycin and digoxin has been reported to result in elevated digoxin serum levels.
Erythromycin has been reported to increase concentrations of HMG-CoA reductase inhibitors (e.g., lovastatin and simvastatin). Rare reports of rhabdomyolysis have been reported in patients taking these drugs concomitantly.
Erythromycin has been reported to increase the systemic exposure (AUC) of sildenafil. Reduction of sildenafil dosage should be considered.
There have been spontaneous or published reports of CYP3A based interactions of erythromycin with cyclosporine, carbamazepine, tacrolimus, alfentanil, disopyramide, rifabutin, quinidine, methylprednisolone, cilostazol, vinblastine, and bromocriptine.
Concomitant administration of erythromycin with cisapride, pimozide, astemizole, or terfenadine is contraindicated
Erythromycin has been reported to significantly alter the metabolism of the nonsedating antihistamines terfenadine and astemizole when taken concomitantly. Rare cases of serious cardiovascular adverse events, including electrocardiographic QT/QTc interval prolongation, cardiac arrest, torsades de pointes, and other ventricular arrhythmias have been observed
Erythromycin is considered a moderate inhibitor of CYP3A4. A significant increase in colchicine plasma concentration is anticipated when co-administered with moderate CYP3A4 inhibitors such as erythromycin.
PRECAUTIONS
Prescribing Erythromycin in the absence of a proven or strongly suspected bacterial infection or a prophylactic indication is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria.
Since erythromycin is principally excreted by the liver, caution should be exercised when erythromycin is administered to patients with impaired hepatic function.
Exacerbation of symptoms of myasthenia gravis and new onset of symptoms of the myasthenic syndrome has been reported in patients receiving erythromycin therapy.
There have been reports of infantile hypertrophic pyloric stenosis (IHPS) occurring in infants following erythromycin therapy
Prolonged or repeated use of erythromycin may result in an overgrowth of nonsusceptible bacteria or fungi. If superinfection occurs, erythromycin should be discontinued and appropriate therapy instituted.
When indicated, incision and drainage or other surgical procedures should be performed in conjunction with antibiotic therapy.
Observational studies in humans have reported cardiovascular malformations after exposure to drug products containing erythromycin during early pregnancy.
WARNINGS
There have been reports of hepatic dysfunction, including increased liver enzymes, and hepatocellular and/or cholestatic hepatitis, with or without jaundice, occurring in patients receiving oral erythromycin products.
Erythromycin has been associated with prolongation of the QT interval and infrequent cases of arrhythmia.
There have been reports suggesting that erythromycin does not reach the fetus in adequate concentration to prevent congenital syphilis. Infants born to women treated during pregnancy with oral erythromycin for early syphilis should be treated with an appropriate penicillin regimen.
Clostridium difficile associated diarrhoea (CDAD) has been reported with the use of nearly all antibacterial agents, including Erythromycin, and may range in severity from mild diarrhoea to fatal colitis. Treatment with antibacterial agents alters the normal flora of the colon leading to overgrowth of C. difficile.
ADVERSE EFFECTS
The most frequent side effects of oral erythromycin preparations are gastrointestinal and are dose-related. They include nausea, vomiting, abdominal pain, diarrhoea and anorexia. Symptoms of hepatitis, hepatic dysfunction and/or abnormal liver function test results may occur
Onset of pseudomembranous colitis symptoms may occur during or after antibacterial treatment
Erythromycin has been associated with QT prolongation and ventricular arrhythmias, including ventricular tachycardia and torsades de pointes
Allergic reactions ranging from urticaria to anaphylaxis have occurred. Skin reactions ranging from mild eruptions to erythema multiforme, Stevens-Johnson syndrome, and toxic epidermal necrolysis have been reported rarely.
There have been reports of interstitial nephritis coincident with erythromycin use.
There have been rare reports of pancreatitis and convulsions.
There have been isolated reports of reversible hearing loss occurring chiefly in patients with renal insufficiency and in patients receiving high doses of erythromycin.
Clinical | Pharmacokinetic data
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References/ Citation:
Erythromycin