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Pronunciation |
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(er
ith roe MYE
sin) |
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U.S. Brand
Names |
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E.E.S.® Oral; E-Mycin® Oral;
Eryc® Oral; EryPed® Oral; Ery-Tab® Oral;
Erythrocin® Oral; Ilosone® Oral; PCE®
Oral |
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Generic
Available |
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Yes |
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Canadian Brand
Names |
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Apo®-Erythro E-C; Diomycin;
Erybid™; Erythro-Base®; Novo-Rythro Encap;
PMS-Erythromycin |
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Synonyms |
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Erythromycin Base; Erythromycin Estolate; Erythromycin Ethylsuccinate;
Erythromycin Gluceptate; Erythromycin Lactobionate; Erythromycin
Stearate |
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Pharmacological Index |
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Antibiotic, Macrolide |
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Use |
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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 |
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Pregnancy Risk
Factor |
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B |
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Contraindications |
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Hepatic impairment, known hypersensitivity to erythromycin or its components;
pre-existing liver disease (erythromycin estolate); concomitant use with
pimozide, terfenadine, astemizole, or cisapride |
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Warnings/Precautions |
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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 |
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Adverse
Reactions |
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>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
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Overdosage/Toxicology |
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Symptoms of overdose include nausea, vomiting, and diarrhea
General and supportive care only |
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Drug
Interactions |
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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 |
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Stability |
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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 |
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Mechanism of
Action |
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Inhibits RNA-dependent protein synthesis at the chain elongation step; binds
to the 50S ribosomal subunit resulting in blockage of
transpeptidation |
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Pharmacodynamics/Kinetics |
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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) |
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Usual Dosage |
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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 |
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Dietary
Considerations |
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Food: Increased drug absorption with meals. Drug may cause GI upset; may take
with food. |
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Test
Interactions |
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False-positive urinary catecholamines |
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Mental Health: Effects
on Mental Status |
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Macrolides have been reported to cause nightmares, confusion, anxiety, and
mood lability |
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Mental Health:
Effects on Psychiatric
Treatment |
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Contraindicated with pimozide; may increase concentration of bromocriptine,
carbamazepine, and triazolam |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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1% to 10% of patients experience oral candidiasis |
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Patient
Information |
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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. |
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Nursing
Implications |
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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 |
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Dosage Forms |
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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 |
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References |
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