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Erythromycin, Systemic
Pronunciation
U.S. Brand Names
Generic Available
Canadian Brand Names
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Stability
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Test Interactions
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(er ith roe MYE sin)

U.S. Brand Names
E.E.S.® Oral; E-Mycin® Oral; Eryc® Oral; EryPed® Oral; Ery-Tab® Oral; Erythrocin® Oral; Ilosone® Oral; PCE® Oral

Generic Available

Yes


Canadian Brand Names
Apo®-Erythro E-C; Diomycin; Erybid™; Erythro-Base®; Novo-Rythro Encap; PMS-Erythromycin

Synonyms
Erythromycin Base; Erythromycin Estolate; Erythromycin Ethylsuccinate; Erythromycin Gluceptate; Erythromycin Lactobionate; Erythromycin Stearate

Pharmacological Index

Antibiotic, Macrolide


Use

Dental: An alternative to penicillin VK for treating orofacial infections

Medical: Treatment of susceptible bacterial infections including S. pyogenes, some S. pneumoniae, some S. aureus, M. pneumoniae, Legionella pneumophila, diphtheria, pertussis, chancroid, Chlamydia, erythrasma, N. gonorrhoeae, E. histolytica, syphilis and nongonococcal urethritis, and Campylobacter gastroenteritis; used in conjunction with neomycin for decontaminating the bowel; treatment of gastroparesis


Pregnancy Risk Factor

B


Contraindications

Hepatic impairment, known hypersensitivity to erythromycin or its components; pre-existing liver disease (erythromycin estolate); concomitant use with pimozide, terfenadine, astemizole, or cisapride


Warnings/Precautions

Hepatic impairment with or without jaundice has occurred, it may be accompanied by malaise, nausea, vomiting, abdominal colic, and fever; discontinue use if these occur; avoid using erythromycin lactobionate in neonates since formulations may contain benzyl alcohol which is associated with toxicity in neonates; observe for superinfections


Adverse Reactions

>10%: Gastrointestinal: Abdominal pain, cramping, nausea, vomiting

1% to 10%:

Gastrointestinal: Oral candidiasis

Hepatic: Cholestatic jaundice

Local: Phlebitis at the injection site

Miscellaneous: Hypersensitivity reactions

<1%: Ventricular arrhythmias, fever, rash, hypertrophic pyloric stenosis, diarrhea, pseudomembranous colitis, eosinophilia, cholestatic jaundice (most common with estolate), thrombophlebitis, allergic reactions


Overdosage/Toxicology

Symptoms of overdose include nausea, vomiting, and diarrhea

General and supportive care only


Drug Interactions

CYP3A3/4 enzyme substrate; CYP1A2 and 3A3/4 enzyme inhibitor

Protease inhibitor like amprenavir and ritonavir may increase erythromycin's serum concentration.

Erythromycin decreases clearance of carbamazepine, cyclosporine, and triazolam, alfentanil, bromocriptine, digoxin (~10% of patients), disopyramide, ergot alkaloids, methylprednisolone; may decrease clearance of protease inhibitors

Erythromycin may decrease theophylline clearance and increase theophylline's half-life by up to 60% (patients on high-dose theophylline and erythromycin or who have received erythromycin for >5 days may be at higher risk)

Decreases metabolism of terfenadine, cisapride, and astemizole resulting in an increase in Q-T interval and potential heart failure

Inhibits felodipine (and other dihydropyridine calcium antagonist) metabolism in the liver resulting in a twofold increase in levels and consequent toxicity

Death has been reported by potentiation of pimozide's cardiotoxicity when given concurrently with erythromycin. Use contraindicated.

May potentiate anticoagulant effect of warfarin and decrease metabolism of vinblastine

Concurrent use of erythromycin and lovastatin and simvastatin may result in significantly increased levels and rhabdomyolysis


Stability

Erythromycin lactobionate should be reconstituted with sterile water for injection without preservatives to avoid gel formation; the reconstituted solution is stable for 2 weeks when refrigerated for 24 hours at room temperature

Erythromycin I.V. infusion solution is stable at pH 6-8. Stability of lactobionate is pH dependent; I.V. form has the longest stability in 0.9% sodium chloride (NS) and should be prepared in this base solution whenever possible. Do not use D5W as a diluent unless sodium bicarbonate is added to solution. If I.V. must be prepared in D5W, 0.5 mL of the 8.4% sodium bicarbonate solution should be added per each 100 mL of D5W.

Stability of parenteral admixture at room temperature (25°C) and at refrigeration temperature (4°C): 24 hours

Standard diluent: 500 mg/250 mL D5W/NS; 750 mg/250 mL D5W/NS; 1 g/250 mL D5W/NS

Refrigerate oral suspension


Mechanism of Action

Inhibits RNA-dependent protein synthesis at the chain elongation step; binds to the 50S ribosomal subunit resulting in blockage of transpeptidation


Pharmacodynamics/Kinetics

Absorption: Variable but better with salt forms than with base form; 18% to 45% absorbed orally, ethylsuccinate may be better absorbed with food

Distribution: Crosses the placenta; appears in breast milk

Relative diffusion of antimicrobial agents from blood into cerebrospinal fluid (CSF): Minimal even with inflammation

Ratio of CSF to blood level (%): Normal meninges: 1-12; Inflamed meninges: 7-25

Protein binding: 75% to 90%

Metabolism: In the liver by demethylation

Half-life: 1.5-2 hours (peak)

End-stage renal disease: 5-6 hours

Time to peak serum concentration: 4 hours for the base, 30 minutes to 2.5 hours for the ethylsuccinate; delayed in the presence of food; due to differences in absorption

Elimination: 2% to 15% excreted as unchanged drug in urine and major excretion in feces (via bile)


Usual Dosage

Infants and Children (Note: 400 mg ethylsuccinate = 250 mg base, stearate, or estolate salts):

Oral: 30-50 mg/kg/day divided every 6-8 hours; may double doses in severe infections

Preop bowel preparation: 20 mg/kg erythromycin base at 1, 2, and 11 PM on the day before surgery combined with mechanical cleansing of the large intestine and oral neomycin

I.V.: Lactobionate: 20-40 mg/kg/day divided every 6 hours

Adults:

Oral:

Base: 250-500 mg every 6-12 hours

Ethylsuccinate: 400-800 mg every 6-12 hours

Preop bowel preparation: Oral: 1 g erythromycin base at 1, 2, and 11 PM on the day before surgery combined with mechanical cleansing of the large intestine and oral neomycin

I.V.: Lactobionate: 15-20 mg/kg/day divided every 6 hours or 500 mg to 1 g every 6 hours, or given as a continuous infusion over 24 hours (maximum: 4 g/24 hours)

Children and Adults: Ophthalmic: Instill 1/2 " (1.25 cm) 2-8 times/day depending on the severity of the infection

Dialysis: Slightly dialyzable (5% to 20%); no supplemental dosage necessary in hemo or peritoneal dialysis or in continuous arteriovenous or venovenous hemofiltration (CAVH/CAVHD)

Erythromycin has been used as a prokinetic agent to improve gastric emptying time and intestinal motility. In adults, 200 mg was infused I.V. initially followed by 250 mg orally 3 times/day 30 minutes before meals. In children, erythromycin 3 mg/kg I.V. has been infused over 60 minutes initially followed by 20 mg/kg/day orally in 3-4 divided doses before meals or before meals and at bedtime


Dietary Considerations

Food: Increased drug absorption with meals. Drug may cause GI upset; may take with food.


Test Interactions

False-positive urinary catecholamines


Mental Health: Effects on Mental Status

Macrolides have been reported to cause nightmares, confusion, anxiety, and mood lability


Mental Health: Effects on Psychiatric Treatment

Contraindicated with pimozide; may increase concentration of bromocriptine, carbamazepine, and triazolam


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

1% to 10% of patients experience oral candidiasis


Patient Information

Take as directed, around-the-clock, with a full glass of water (not juice or milk), preferably on an empty stomach (1 hour before or 2 hours after meals). Take complete prescription even if you are feeling better. You may experience nausea, vomiting, or mouth sores (small frequent meals, frequent mouth care may help). Report skin rash or itching; easy bruising or bleeding; unhealed sores of mouth; itching or vaginal discharge; watery or bloody diarrhea; unresolved vomiting; yellowing of skin or eyes; easy fatigue; pale stool or dark urine; skin rash or itching; white plaques, sores, or fuzziness in mouth; or any change in hearing.


Nursing Implications

Some formulations may contain benzyl alcohol as a preservative; use with extreme care in neonates; do not crush enteric coated drug product; GI upset, including diarrhea, is common; I.V. infusion may be very irritating to the vein; if phlebitis/pain occurs with used dilution, consider diluting further (eg, 1:5) and administer over greater than or equal to 20-60 minutes, if fluid status of the patient will tolerate, or consider administering in larger available vein


Dosage Forms

Erythromycin base:

Capsule, delayed release: 250 mg

Capsule, delayed release, enteric coated pellets (Eryc®): 250 mg

Ointment, ophthalmic: 0.55 mg (3.5 g)

Tablet, delayed release: 333 mg

Tablet, enteric coated (E-Mycin®, Ery-Tab®, E-Base®): 250 mg, 333 mg, 500 mg

Tablet, film coated: 250 mg, 500 mg

Tablet, polymer coated particles (PCE®): 333 mg, 500 mg

Erythromycin estolate:

Capsule (Ilosone® Pulvules®): 250 mg

Suspension, oral (Ilosone®): 125 mg/5 mL (480 mL); 250 mg/5 mL (480 mL)

Tablet (Ilosone®): 500 mg

Erythromycin ethylsuccinate:

Granules for oral suspension (EryPed®): 400 mg/5 mL (60 mL, 100 mL, 200 mL)

Powder for oral suspension (E.E.S.®): 200 mg/5 mL (100 mL, 200 mL)

Suspension, oral (E.E.S.®, EryPed®): 200 mg/5 mL (5 mL, 100 mL, 200 mL, 480 mL); 400 mg/5 mL (5 mL, 60 mL, 100 mL, 200 mL, 480 mL)

Suspension, oral [drops] (EryPed®): 100 mg/2.5 mL (50 mL)

Tablet (E.E.S.®): 400 mg

Tablet, chewable (EryPed®): 200 mg

Erythromycin gluceptate: Injection: 1000 mg (30 mL)

Erythromycin lactobionate: Powder for injection: 500 mg, 1000 mg

Erythromycin stearate: Tablet, film coated (Eramycin®, Erythrocin®): 250 mg, 500 mg


References

Amsden GW, "Erythromycin, Clarithromycin, and Azithromycin: Are the Differences Real?" Clin Ther, 1996, 18(1):56-72.

Boyd I, "Erythromycin-Induced Hearing Loss," Lancet, 1991, 337(8733):113.

Catnach SM and Fairclough PD, "Erythromycin and the Gut," Gut, 1992, 33(3):397-401.

Council on Dental Therapeutics, American Heart Association, "Preventing Bacterial Endocarditis," J Am Dent Assoc, 1991, 122(2):87-92.

Dajani AS, Bisno AL, Chung KJ, et al, "Prevention of Bacterial Endocarditis. Recommendations by the American Heart Association," JAMA, 1990, 264(22):2919-22.

Di Lorenzo C, Lachman R, and Hyman PE, "Intravenous Erythromycin for Postpyloric Intubation," J Pediatr Gastroenterol Nutr, 1990, 11(1):45-7.

Furlan V, Perello L, Jacquemin E, et al, "Interactions Between FK506 and Rifampicin or Erythromycin in Pediatric Liver Recipients," Transplantation, 1995, 59(8):1217-8.

Gholson CF and Warren GH, "Fulminant Hepatic Failure Associated With Intravenous Erythromycin Lactobionate," Arch Intern Med, 1990, 150(1):215-6.

Goldman MP and Longworth DL, "The Role of Azithromycin and Clarithromycin in Clinical Practice," Cleve Clin J Med, 1993, 60(5):359-64.

Gumaste VV, "Erythromycin-Induced Pancreatitis," Am J Med, 1989, 86(6 Pt 1):725.

Hanrahan JP, Choo PW, Carlson W, et al, "Terfenadine-Associated Ventricular Arrhythmias and QTc Interval Prolongation. A Retrospective Cohort Comparison With Other Antihistamines Among Members of a Health Maintenance Organization," Ann Epidemiol, 1995, 5(3):201-9.

Hassel B, "Hypothermia From Erythromycin," Ann Intern Med, 1991, 115(1):69-70.

Janssens J, Peeters TL, Vantrappen G, et al, "Improvement of Gastric Emptying in Diabetic Gastroparesis by Erythromycin," N Engl J Med, 1990, 322(15):1028-31.

Lestico MR and Smith AD, "Stevens-Johnson Syndrome Following Erythromycin Administration," Am J Health Syst Pharm, 1995, 52(16):1805-7.

Mogford N, Pallet A, and George C, "Erythromycin Deafness and Cimetidine Treatment," BMJ, 1994, 309(6969):1620.

Orban Z, MacDonald LL, Peters MA, et al, "Erythromycin-Induced Cardiac Toxicity," Am J Cardiol, 1995, 75(12):859-61.

Paris DG, Parente TF, Bruschetta HR, et al, "Torsade de Pointes Induced by Erythromycin and Terfenadine," Am J Emerg Med, 1994, 12(6):636-8.

"Pimozide (Orap) Contraindicated With Clarithromycin (Biaxin) and Other Macrolide Antibiotics," FDA Medical Bulletin, October 1996, 3.

Reid B, DiLorenzo C, Travis L, et al, "Diabetic Gastroparesis Due to Postprandial Antral Hypomotility in Childhood," Pediatrics, 1992, 90(1 Pt 1):43-6.

Smilack JD, Wilson WR, and Cockerill FR 3d, "Tetracyclines, Chloramphenicol, Erythromycin, Clindamycin, and Metronidazole," Mayo Clin Proc, 1991, 66(12):1270-80.

Spinler SA, Cheng JW, Kindwall KE, et al, "Possible Inhibition of Hepatic Metabolism of Quinidine by Erythromycin," Clin Pharmacol Ther, 1995, 57(1):89-94.

Stafstrom CE, Nohria V, Loganbill H, et al, "Erythromycin-induced Carbamazepine Toxicity: A Continuing Problem," Arch Pediatr Adolesc Med, 1995, 149(1):99-101.

Tartaglione TA, "Therapeutic Options for the Management and Prevention of Mycobacterium avium Complex Infection in Patients With the Acquired Immunodeficiency Syndrome," Pharmacotherapy, 1996, 16(2):171-82.

Thoene DE and Johnson CE, "Pharmacotherapy of Otitis Media," Pharmacotherapy, 1991, 11(3):212-21.

Tobe SW, Siu LL, Jamal SA, et al, "Vinblastine and Erythromycin: An Unrecognized Serious Drug Interaction," Cancer Chemother Pharmacol, 1995, 35(3):188-90.

Waites KB, Sims PJ, Crouse DT, et al, "Serum Concentrations of Erythromycin After Intravenous Infusion in Preterm Neonates Treated for Ureaplasma urealyticum Infection," Pediatr Infect Dis J, 1994, 13(4):287-93.

Wynn RL, "Current Concepts of the Erythromycins," Gen Dent, 1991, 39(6):408,10-1.

Wynn RL and Bergman SA, "Antibiotics and Their Use in the Treatment of Orofacial Infections, Part I and Part II," Gen Dent, 1994, 42(5):398-402, 498-502.

Yoshikawa TT, "Antimicrobial Therapy for the Elderly Patient," J Am Geriatr Soc, 1990, 38(12):1353-72.


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