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erythromycin lactobionate (Erythrocin Lactobionate)

 

Classes: Macrolides

Dosing and uses of Erythrocin Lactobionate (erythromycin lactobionate)

 

Adult dosage forms and strengths

injection

  • 500mg
  • 1g

 

General Dosing Recommendations

15-20 mg/kg/day IV divided q6hr; infuse IV over 1 hr

Up to 4 g/day may be administered for severe infections

Geriatric: Increased risk for hearing loss in elderly patients with 4 g/day or more

 

Acute Pelvic Inflammatory Disease

500 mg IV q6hr for 3 days; follow by 500 mg PO q12hr

 

Legionaire Disease

1-4 g IV in divided doses

 

Streptococcal Infections

250 mg PO q12hr

 

Renal Impairment

CrCl <10 mL/min: Administer 50-75% of usual dose

 

Other Indications & Uses

Group A beta-hemolytic strep, Actinobacillus actinomycetemcomitans, Actinomyces israelii, Actinomyces naeslundii, Actinomyces odontolyticus, Afipia felis, Arachnia propionica, Arcanobacterium (Corynebacterium) haemolyticum, Bacillus anthracis, Bartonella henselae, Bartonella quintana, Bordetella pertussis, Borrelia burgdorferi, Borrelia recurrentis, C. diphtheriae, C. trachomatis, Klebsiella granulomatis, Campylobacter jejuni, Capnocytophaga ochracea, Chlamydia pneumonia (TWAR agent), Chlamydia psittaci, Chlamydia trachomatis, Chryseobacterium meningosepticum, Corynebacterium jeikeium (CDC group JK), Corynebacterium minutissimum, Corynebacterium ulcerans, Coxiella burnetii, E. histolytica, Erysipelothrix rhusiopathiae, H. ducreyi, H. influenzae, Kingella sp., Lactobacillus sp, Legionella pneumophilia, Leptospira interrogans, Leptotrichia buccalis, Leuconostoc species, Listeria, Mycobacterium chelonae, Mycobacterium fortuitum, M. catarrhalis, Mycoplasma pneumoniae, N. gonorrhoeae, Rhodococcus equi, S. aureus, S. pyogenes (group A beta-hemolytic streptococci), S. pneumoniae, Spirillum minus, Streptobacillus moniliformis, Streptococcus (Group C, G), Streptococcus agalactiae (Group B), Streptococcus bovis (Group D), Streptococcus intermedius group (S. anginosus, S intermedius, S. constellatus), Streptococcus pneumoniae (PCN sensitive, MIC <0.1 mcg/mL), Streptococcus pyogenes (Group A), Treponema pallidum, U. urealyticum, Ureaplasma urealyticum, Vibrio cholerae, Viridans streptococci

Off-label: Campylobacter jejuni, Calymmatobacterium granulomatis, Haemophilus ducreyi, prophylaxis in colorectal surgery, anthrax, tetanus, Lyme disease

First line: Afipia felis, Arcanobacterium (Corynebacterium) haemolyticum, Bartonella henselae, Bartonella quintana, Campylobacter jejuni, Capnocytophaga ochracea, Chlamydia pneumonia, Corynebacterium minutissimum, Corynebacterium ulcerans, Haemophilus ducreyi, Mycobacterium fortuitum, Ureaplasma urealyticum (others eg, Haemophilus ducreyi not unanimous)

 

Pediatric dosage forms and strengths

injection

  • 500mg
  • 1g

 

Usual Dosage Range, Infants & Children

15-20 mg/kg/day IV divided q6hr; infuse IV over 1 hr

Higher doses may be administered for severe infection; not to exceed 4 g/day

 

Renal Impairment

CrCl <10 mL/min: Administer 50-75% of usual dose

 

Erythrocin Lactobionate (erythromycin lactobionate) adverse (side) effects

1-10%

Abdominal pain (8%)

Headache (8%)

Nausea (8%)

Diarrhea (7%)

Rash (3%)

Vomiting (3%)

Dyspepsia (2%)

Flatulence (2%)

Pain (2%)

Pruritus (1%)

Pseudomembranous colitis

Hypertrophic pyloric stenosis

Anaphylaxis

Fever

Mild allergic reactions

Urticaria

Skin eruptions

Tinnitus

QT prolongation

Venous irritation

Ventricular arrhythmias

 

<1%

Cholestatic hepatitis

Confusion

Hallucinations

Hearing loss

Hypotension

Nervous system effects including seizures

Torsade de pointes

Ventricular tachycardia

Vertigo

 

Postmarketing reports

Interstitial nephritis

 

Warnings

Contraindications

Documented hypersensitivity

Hepatic impairment

History of hepatitis caused by macrolide

Cholestatic hepatitis

Coadministration with terfenadine (discontinued), astemizole (discontinued), cisapride, or pimozide

Coadministration with ergotamine or dihydroergotamine (postmarketing reports of acute ergot toxicity characterized by vasospasm and ischemia of the extremities and other tissues including the central nervous system)

 

Cautions

Risk of sudden death due to cardiac causes w/ concomitant use of oral erythromycin with drugs that inhibit CYP3A4

Erythromycin is considered a moderate inhibitor of CYP3A4; may increase toxicity of CYP3A4 substrates

Colchicine is a substrate for both CYP3A4 and the efflux transporter P-glycoprotein (P-gp); significant increase in colchicine plasma concentration is anticipated when coadministered with moderate CYP3A4 inhibitors; reduce the starting dose of colchicine and lower maximum colchicine dose

Caution in liver disease; estolate formulation may cause cholestatic jaundice; discontinue use if nausea, vomiting, malaise, abdominal colic, or fever occur

Ventricular arrhythmias

Associated with QT prolongation and infrequent cases of arrhythmia

May increase LFTs in pregnant women

Hepatic impairment

Overgrowth of nonsusceptible bacteria or fungi

 

Pregnancy and lactation

Pregnancy category: B

Lactation: distributed in breast milk, use with caution; AAP categorizes as compatible with breastfeeding

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Erythrocin Lactobionate (erythromycin lactobionate)

Mechanism of action

Inhibits bacterial growth, possibly by blocking dissociation of peptidyl tRNA from ribosomes, causing RNA-dependent protein synthesis to arrest

 

Absorption

Peak Plasma Time: 2 hr (base)

 

Distribution

Protein Bound: 75-80%

Crosses placenta; enters breast milk

Relative diffusion from blood into CSF: minimal even with inflammation

 

Metabolism

Via P450 enzyme CYP3A4

Enzymes inhibited: CYP1A2, CYP3A4

 

Elimination

Half-Life: 1.4 hr

Excretion: primarily feces; urine (2-15% as unchanged drug)

 

Administration

IV Compatibilities

Solution: 0.9% NaCL

Additive: Ampicillin, cimetidine, diphenhydramine, hydrocortisone, lidocaine, penicillin G potassium, pentobarbital, KCl, prochlorperazine, ranitidine, Na bicarb, verapamiL

Y-site (partial list): Acyclovir, amiodarone, diltiazem, esmolol, heparin, hydromorphone, labetalol, lorazepam, meperidine, morphine, tacrolimus, aminB/C, zidovudine

 

IV Incompatibilities

Solution (usually 10-15% decomposition): D5/LR, D5/NS, D5W (?), Normosol M, Normosol R, LR, Ringer's

Additive: Aminophylline, ascorbic acid (may be conc-dependent), heparin, vitamin B/C

Syringe: Ampicillin, heparin

Not spec: Carbenicillin, cefazolin, epinephrine, tetracycline

 

IV Preparation

Infusion: Reconstitute 250 or 500 mg vials with 10 mL SWI without preservatives; 1 g vials with 20 mL

Intermittent infusion: Dilute 250-500 mg in 100-250 mL D5W or 0.9% NaCL

Continuous infusion: Final concentration of 1 g/L

 

IV Administration

Intermittent Infusion: Over 20-60 min

Continuous Infusion: Over 6-24 hr

 

Storage

Store at controlled room temperature