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erythromycin (Eryc, Eryctte, E-mycin, Ilotycin, AK-Mycin, A/T/S, T-stat)

Tradename: Eryc, E-mycin, Erycette (topical), Ilotycin, AK-Mycin (ophthalmic) Indications: - treatment of non life threatening bacterial infections - skin or soft tissue infection - ecthyma, erysipeloid, erysepelas, erythrasma - moderate-severe inflammatory acne [6] - respiratory tract infection - pertussis - pneumonia - gastrointestinal infection - proctitis - urogenital infection - urethritis - syphilis, trachoma, gonorrhea, chancroid, lymphogranuloma venereum, donovanosis - acute otitis media - rheumatic fever - Lyme disease, borreliosis - anthrax, cutaneous anthrax, inhalation anthrax [15] - listeriosis, diptheria, actinomycosis, Legionnaire's disease, - prophylaxis before bowel surgery, upper GI endoscopy - stimulate intestinal motility - GERD, gastroparesis, bowel preparation - topical: treatment of acne, rosacea [10]: - eye infections - blepharoconjunctivitis - ophthalmia neonatorum - eyelid disease - meibomitis Contraindications: Caution: avoid in infants < 2 weeks of age [8,9] Dosage: 1) systemic - 250-500 mg PO QID. - 333 mg PO TID. - 500 mg PO BID. - 10-20 mg/kg/day IV divided every 6 hours, max 4 g/day. - Legionella dose: 1 g IV every 6 hours 2) topical: apply BID after cleansing 3) ophthalmic - apply BID-QID - Chlamydia: 1 strip BID for 2 months, or BID for the 1st 5 days of the month for 6 months Tabs: 250, 333, 500 mg. Injection: IV form: erythromycin lactobionate. Solution: 60 mL Ointment: 0.5% Dosage adjustment in renal failure: creatinine clearance dosage 10-50 mL/min 100% < 10 mL/min 50-75% dosing hemodialysis no post-hemodialysis dosing Pharmacokinetics: 1) oral dose absorbed primarily in the duodenum 2) oral bioavailability 18-45% 3) well distributed to most tissues a) does not penetrate CSF well b) crosses placenta 4) protein-binding 75-90% 5) metabolized by demethylation in the liver by cyt P450 3A4 6) eliminated in the bile 7) 1/2life is 1-2 hours (5-6 hours ESRD) Antimicrobial activity: Gram positive - Streptococcus - Streptococcus group A - Streptococcus group B - Streptococcus group C - Streptococcus group G - Streptococcus pneumonia - Staphylococcus aureus (MSSA) (+/-) - Staphylococcus epidermidis (+/-) - Corynebacterium diphtheriae Gram negative - Neisseria gonorrhoeae - Moraxella catarrhalis - Haemophilus influenzae (+/-) - Legionella - Haemophilus ducreyi - Bordetella pertussis [15] - Chlamydophila pneumoniae [15] - Campylobacter [15] Atypical bacteria - Chlamydia species - Mycoplasma pneumonia - Rickettsia (+/-) - Ureaplasma Anaerobes - Actinomyces - Clostridium species (+/-) Adverse effects: 1) common & less common (> 1%) - nausea/vomiting - diarrhea, cramps* - increased aspartate transaminase (AST) - cholestatic jaundice - phlebitis at injection site & thrombophlebitis - oral candidiasis 2) uncommon (< 1%) - hypertrophic pyloric stenosis#, ventricular arrhythmias, fever, skin rash, diarrhea, eosinophilia, hypersensitivity reaction (rare) 3) other - increased PT & INR - ototoxicity (tinnitus, transient deafness) - high doses IV, i.e. 4 g/day - generally reversible - QT prolongation, torsades de pointes 4) as topical agent - local dryness - erythema - tenderness - burning - irritation - hypersensitivity (rare) * GI intolerance due to hepatic reduction to ketal analogous to motilin. # Incidence of hypertrophic pyloric stenosis 1-2.6% in infants given erythromycin within 1st 2 weeks of life [8,9] Drug interactions: 1) QT prolongation associated with concurrent administration of cyt P450 3A4 inhibitors: [11,12] a) astemizole b) terfenadine c) cisapride d) ketoconazole e) itraconazole f) nefazodone g) antiretroviral protease inhibitors 2) erythromycin inhibits metabolism of: a) theophylline b) carbamazepine c) warfarin d) cyclosporine e) benzodiazepines f) phenytoin g) triazolam h) diltiazem i) verapamil 3) do NOT administer in combination with clindamycin 4) any drug that inhibits cyt P450 3A4 may increase levels of erythromycin 5) any drug that induces cyt P450 3A4 may diminish levels of erythromycin 6) erythromycin inhibits cyt P450 1A2 & cyt P450 3A4 a) inhibits its own metabolism & metabolism of other cyt P450 3A4 substrates b) inhibits metabolism of cyt P450 1A2 substrates 7) inhibits P-glycoprotein - increases intracellular concentration of drugs pumped out of cells by P-glycoprotein [13] 8) erythromycin in combination with calcium channel blocker may increase risk of hypotension & acute renal failure [16] Mechanism of action: 1) bacteriostatic 2) binds to 50S ribosomal subunits 3) inhibits bacterial protein synthesis 4) may have anti-inflammatory properties [14] 5) enhances GI motility, peristalsis

Interactions

drug interactions drug adverse effects of macrolide(s)

Related

cytochrome p450 1A2 (cytochrome P3-450, phenacetin deethylase, cytochrome p450-4, CYP1A2) cytochrome P450 3A4 (cytochrome P450 C3, nifedipine oxidase, P450-PCN1, NF-25, CYP3A4)

Specific

erythromycin estolate (Ilosone) erythromycin ethyl succinate (EES, Pediamycin) erythromycin lactobionate (Erythrocin) Erythromycin Ophthalmic (Romycin)

General

macrolide (macrolide antibiotic)

Properties

MISC-INFO: elimination route LIVER 1/2life 1-2 HOURS protein-binding 75-90% pregnancy-category B safety in lactation +

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Harrison's Principles of Internal Medicine, 13th ed. Companion Handbook. Isselbacher et al (eds), McGraw-Hill Inc. NY, 1995, pg 164
  3. Sanford Guide to antimicrobial therapy 1997
  4. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  5. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  6. Medical Knowledge Self Assessment Program (MKSAP) 11, 17. American College of Physicians, Philadelphia 1998, 2017.
  7. Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: 220233 (subscription needed) http://www.prescribersletter.com
  8. Journal Watch 21(21):170, 2001 Mahon et al, J Pediatr 139:380, 2001
  9. Journal Watch 22(16):128, 2002 Cooper WO et al Arch Pedatr Adolesc Med 156:647, 2002
  10. Prescriber's Letter 10(4):22 2003
  11. Prescriber's Letter 11(11): 2004 Detail-Document#: 201115 (subscription needed) http://www.prescribersletter.com
  12. Journal Watch 24(20):150, 2004 Ray WA, Murray KT, Meredith S, Narasimhulu SS, Hall K, Stein CM. Oral erythromycin and the risk of sudden death from cardiac causes. N Engl J Med. 2004 Sep 9;351(11):1089-96. PMID: 15356306
  13. Prescriber's Letter 12(9): 2005 Fatal Interaction Between Clarithromycin and Colchicine Detail-Document#: 211004 (subscription needed) http://www.prescribersletter.com
  14. Kunisaki KM and Niewoehner DE Antibiotic prophylaxis for chronic obstructive pulmonary disease: resurrecting an old idea. Am J Respir Crit Care Med. 2008 Dec 1;178(11):1098-9 PMID: 19023036
  15. Deprecated Reference
  16. Paauw DS Dangerous and Deadly Drug Combinations Medscape. June 30, 2016 http://www.medscape.com/features/slideshow/dangerous-drug-combinations

Component-of

benzoyl peroxide/erythromycin (Benzamycin)