Erythromycin


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intravenous
Prophylaxis of surgical infections, Respiratory tract infections, Skin and soft tissue infections, Susceptible Gram-negative infections, Susceptible Gram-positive infections
Adult: As erythromycin lactobionate: 1-2 g daily equivalent to 25 mg/kg daily given in 2-4 divided doses, up to 4 g daily equivalent to 50 mg/kg daily in severe infections. Doses may be given as continuous or via intermittent infusion over 20-60 minutes every 6 hours. Replace with oral erythromycin after 2-7 days.
Child: 15-20 mg/kg daily divided every 6 hours. Max: 4 g daily.

Ophthalmic
Prophylaxis of neonatal conjunctivitis
Child: As 0.5% oint: Instill approx 1 cm in length into each of the lower conjunctival sac.

Ophthalmic
Superficial ocular infections
Adult: As 0.5% oint: Apply approx 1 cm length to the affected eye(s) up to 6 times daily depending on the severity of the infection.
Child: Same as adult dose.

Oral
Prophylaxis of surgical infections, Respiratory tract infections, Skin and soft tissue infections, Susceptible Gram-negative infections, Susceptible Gram-positive infections
Adult: 1-2 g daily in 2-4 divided doses; may be increased up to 4 g daily for severe infections. Doses >1 g should be given in more than 2 divided doses.
Child: 30-50 mg/kg daily in 2-4 divided doses; may be doubled in severe infections.

Topical/Cutaneous
Acne vulgaris
Adult: As 2 or 4% gel/pad/soln: Apply onto affected areas 1-2 times daily. Discontinue treatment if condition worsens or if there is no improvement after 6-8 weeks.
Cách dùng
Should be taken on an empty stomach. Best taken on an empty stomach at least 30 min & preferably 2 hr before meals.
Hướng dẫn pha thuốc
Oral: Add enough water to make 100 mL susp, shake vigorously. IV: Add 20 mL sterile water for inj to a vial labelled as containing 1 g to prepare a concentration of 50 mg/mL; further dilute with ≥100 mL of suitable diluent to a final concentration of 1-5 mg/mL.
Chống chỉ định
Hypersensitivity. Prolonged QT interval, uncorrected hypokalaemia or hypomagnesaemia, clinically significant bradycardia. Concomitant use with astemizole, terfenadine, cisapride, pimozide, tolterodine, mizolastine, amisulpride, ergotamine or dihydroergotamine, lovastatin, simvastatin, Class 1A or III antiarrhythmic agents.
Thận trọng
Patient with risk factors for prolonged cardiac repolarisation, coronary artery disease, myasthenia gravis. Hepatic impairment. Children. Pregnancy and lactation.
Phản ứng phụ
Significant: Fungal or bacterial superinfection (e.g. C. difficile-associated diarrhoea [CDAD]); myasthenia gravis; infantile hypertrophic pyloric stenosis; hepatotoxicity.
Blood and lymphatic system disorders: Eosinophilia.
Cardiac disorders: Chest pain, palpitations.
Ear and labyrinth disorders: Deafness, tinnitus.
Eye disorders: Mitochondrial optic neuropathy.
Gastrointestinal disorders: Nausea, vomiting, abdominal pain, diarrhoea, pancreatitis.
General disorders and administration site conditions: Fever, malaise.
Hepatobiliary disorders: Cholestatic hepatitis, jaundice, hepatic dysfunction, hepatomegaly, hepatic failure, hepatocellular hepatitis.
Immune system disorders: Allergic reactions, anaphylaxis.
Investigations: Increased liver enzymes.
Metabolism and nutrition disorders: Anorexia.
Nervous system disorders: Convulsions, vertigo.
Psychiatric disorders: Hallucinations, confusion.
Renal and urinary disorders: Interstitial nephritis.
Skin and subcutaneous tissue disorders: Pruritus, urticaria, exanthema, angioedema, Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme. Topical: burning, peeling, drying, reddening, oiliness and pruritus at the application site.
Vascular disorders: Hypotension.
Potentially Fatal: QT prolongation, ventricular arrhythmias including torsades de pointes, pseudomembranous colitis.
IV/Ophth/Parenteral/PO/Topical: B
Tương tác
Increased risk of hypotension with Ca channel blockers that are metabolised by CYP3A4 (e.g. verapamil, amlodipine, diltiazem). May cause a significant increase in the plasma concentration of colchicine. Decreased serum concentration with CYP3A4 inducers (e.g. rifampicin, phenytoin). May decrease the effectiveness of contraceptives. May increase the effect of oral anticoagulants (e.g. warfarin). May increase plasma concentration of benzodiazepines (e.g. midazolam). May increase the pharmacodynamic effects of zopiclone. Increased plasma concentration with cimetidine.
Potentially Fatal: Increased risk of rhabdomyolysis with simvastatin and lovastatin. May increase serum concentration and enhance QT prolongation, ventricular tachycardia or fibrillation and torsades de pointes with Class IA (e.g. procainamide, quinidine) or Class III (e.g. amiodarone, sotalol, dofetilide) antiarrhythmics, cisapride. Increased risk of serious CV events with astemizole, terfenadine, pimozide, tolterodine, mizolastine, amisulpride. Increased risk of acute ergot toxicity with ergotamine or dihydroergotamine.
Food Interaction
Decreased serum concentration with St John's wort.
Lab Interference
May give a false-positive result for urinary catecholamines, 17-hydroxycorticosteroids and 17-ketosteroids. May interfere with colorimetric assays resulting in falsely elevated AST and ALT concentrations.
Tác dụng
Description: Erythromycin inhibits protein synthesis by binding to the 50S ribosomal subunit of susceptible organisms resulting in blockage of transpeptidation.
Pharmacokinetics:
Absorption: Variable and unreliable due to instability in gastric acid. Time to peak plasma concentration: 1-4 hours.
Distribution: Widely distributed throughout the body tissues and fluids; diffused into CSF (minimal). Crosses the placenta and enters breast milk. Volume of distribution: 0.64 L/kg. Plasma protein binding: 70-75% (as the base), 95% (as the propionate ester).
Metabolism: Partly metabolised in the liver via N-demethylation by CYP3A4 into inactive, unidentified metabolites.
Excretion: Mainly via faeces; urine (2-15% as unchanged drug). Elimination half-life: 1.5-2.5 hours.
Đặc tính

Chemical Structure Image
Erythromycin

Source: National Center for Biotechnology Information. PubChem Database. Erythromycin, CID=12560, https://pubchem.ncbi.nlm.nih.gov/compound/Erythromycin (accessed on Jan. 22, 2020)

Bảo quản
Store between 20-25°C.
Phân loại ATC
S01AA17 - erythromycin ; Belongs to the class of antibiotics. Used in the treatment of eye infections.
D10AF02 - erythromycin ; Belongs to the class of topical antiinfective preparations used in the treatment of acne.
J01FA01 - erythromycin ; Belongs to the class of macrolides. Used in the systemic treatment of infections.
References
Anon. Erythromycin (Ophthalmic). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 13/05/2020.

Anon. Erythromycin (Systemic). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 13/05/2020.

Anon. Erythromycin (Topical). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 13/05/2020.

Buckingham R (ed). Erythromycin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 13/05/2020.

E.E.S. 400 Tablet, Granule for Suspension (Arbor Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 13/05/2020.

Ery Swab (Perrigo New York Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 13/05/2020.

Erygel Gel (Mylan Pharmaceuticals Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 13/05/2020.

Eryhtrodar Tablets 500 mg (Ennogen Pharma Limited). MHRA. https://products.mhra.gov.uk/. Accessed 15/05/2020.

Erythromycin 1 g Powder for Solution for Infusion (Stragen UK Ltd.). MHRA. https://products.mhra.gov.uk/. Accessed 15/05/2020.

Erythromycin Ointment (Akorn, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 15/05/2020.

Erythromycin Solution (Teligent Pharma, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 13/05/2020.

Erythroped SF 250 mg/5mL Suspension (Amdipharm UK Limited). MHRA. https://products.mhra.gov.uk/. Accessed 15/05/2020.

Joint Formulary Committee. Erythromycin. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 13/05/2020.

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