Peringatan Keamanan

LD50

The oral LD50 of erythromycin in rats is 9272 mg/kg.L7279

Overdose information

Symptoms of overdose may include diarrhea, nausea, stomach cramps, and vomiting. Erythromycin should immediately be discontinued in cases of overdose. Rapid elimination of unabsorbed drug should be attempted. Supportive measures should be initiated. Erythromycin is not adequately removed by peritoneal dialysis or hemodialysis.L7261

Erythromycin

DB00199

small molecule approved investigational vet_approved

Deskripsi

Erythromycin is a bacteriostatic antibiotic drug produced by a strain of Saccharopolyspora erythraea (formerly Streptomyces erythraeus) and belongs to the macrolide group of antibiotics which consists of Azithromycin, Clarithromycin, Spiramycin and others. It was originally discovered in 1952.L5245 Erythromycin is widely used for treating a variety of infections, including those caused by gram-positive and gram-negative bacteria.L5245,L7261 It is available for administration in various forms, including intravenous, topical, and eye drop preparations.L5245

Struktur Molekul 2D

Berat 733.9268
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of oral erythromycin was 3.5 hours according to one study[A174451] and ranged between 2.4-3.1 hours in another study.[A180598] Repetitive dosing of erythromycin leads to increased elimination half-life.[A180601]
Volume Distribusi Erythromycin is found in most body fluids and accumulates in leucocytes and inflammatory liquid.[L7261,A174448,A180607] Spinal fluid concentrations of erythromycin are low, however, the diffusion of erythromycin through the blood-brain barrier increases in meningitis, likely due to the presence of inflamed tissues which are easily penetrated.[L7270] Erythromycin crosses the placenta.[L7261]
Klirens (Clearance) The clearance of erythromycin in healthy subjects was 0.53 ± 0.13 l/h/kg after a 125mg intravenous dose.[A174457] In a clinical study of healthy patients and patients with liver cirrhosis, clearance of erythromycin was significantly reduced in those with severe liver cirrhosis.[A180604] The clearance in cirrhotic patients was 42.2 ± 10.1 l h–1 versus 113.2 ± 44.2 l h-1 in healthy patients.[A180604]

Absorpsi

Orally administered erythromycin is readily absorbed. Food intake does not appear to exert effects on serum concentrations of erythromycin.L7261 Some interindividual variation exists in terms of erythromycin absorption, which may impact absorption to varying degrees.L7261 The Cmax of erythromycin is 1.8 mcg/LA180598 and the Tmax is 1.2 hours.A180607 The serum AUC of erythromycin after the administration of a 500mg oral dose was 7.3±3.9 mg.h/l in one pharmacokinetic study.A180607 Erythromycin is well known for a bioavailability that is variable (18-45%) A174451,A180595 after oral administration and its susceptibility to broken down under acidic conditions.A174448

Metabolisme

Hepatic first-pass metabolism contributes significantly to erythromycin metabolism after an oral dose.A174457 Erythromycin is partially metabolized by CYP3A4 enzyme to N-desmethylerythromycin.L7261,A174175 Erythromycin is also hydrolyzed to anhydro forms (anhydroerythromycin AHE and other metabolites), and this process is promoted by acidic conditions.A174448 AHE is inactive against microbes but inhibits hepatic drug oxidation and is therefore considered to be an important contributor to erythromycin drug-drug interactions.A174448

Rute Eliminasi

In patients with normal liver function, erythromycin concentrates in the liver and is then excreted in the bile.L7270Under 5% of the orally administered dose of erythromycin is found excreted in the urine.L7270,A180607 A high percentage of absorbed erythromycin is not accounted for, but is likely metabolized.L7270

Interaksi Makanan

3 Data
  • 1. Avoid grapefruit products.
  • 2. Take on an empty stomach. Allow approximately 30 minutes to 2 hours before meals, as this increases erythromycin absorption.
  • 3. Take with a full glass of water.

Interaksi Obat

1322 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Erythromycin.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Erythromycin.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Erythromycin.
Glycochenodeoxycholic Acid Erythromycin may decrease the excretion rate of Glycochenodeoxycholic Acid which could result in a higher serum level.
Glimepiride Erythromycin may decrease the excretion rate of Glimepiride which could result in a higher serum level.
Olmesartan Olmesartan may decrease the excretion rate of Erythromycin which could result in a higher serum level.
Flucloxacillin Erythromycin may decrease the excretion rate of Flucloxacillin which could result in a higher serum level.
Atenolol Erythromycin may decrease the excretion rate of Atenolol which could result in a higher serum level.
Rosiglitazone The serum concentration of Rosiglitazone can be increased when it is combined with Erythromycin.
Fluorescein Erythromycin may decrease the excretion rate of Fluorescein which could result in a higher serum level.
Nitrofurantoin Erythromycin may decrease the excretion rate of Nitrofurantoin which could result in a higher serum level.
Naproxen Erythromycin may decrease the excretion rate of Naproxen which could result in a higher serum level.
Disulfiram The serum concentration of Disulfiram can be increased when it is combined with Erythromycin.
Cefaclor Erythromycin may decrease the excretion rate of Cefaclor which could result in a higher serum level.
Tinidazole The serum concentration of Tinidazole can be increased when it is combined with Erythromycin.
Glipizide Erythromycin may decrease the excretion rate of Glipizide which could result in a higher serum level.
Sulfinpyrazone The serum concentration of Sulfinpyrazone can be increased when it is combined with Erythromycin.
Indocyanine green acid form Erythromycin may decrease the excretion rate of Indocyanine green acid form which could result in a higher serum level.
Benzbromarone Erythromycin may decrease the excretion rate of Benzbromarone which could result in a higher serum level.
Glycyrrhizic acid Erythromycin may decrease the excretion rate of Glycyrrhizic acid which could result in a higher serum level.
Ezetimibe Erythromycin may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Diethylstilbestrol The serum concentration of Diethylstilbestrol can be increased when it is combined with Erythromycin.
Indomethacin Erythromycin may decrease the excretion rate of Indomethacin which could result in a higher serum level.
Diclofenac The serum concentration of Diclofenac can be increased when it is combined with Erythromycin.
Fluvoxamine The serum concentration of Fluvoxamine can be increased when it is combined with Erythromycin.
Loratadine The serum concentration of Loratadine can be increased when it is combined with Erythromycin.
Losartan The serum concentration of Losartan can be increased when it is combined with Erythromycin.
Telmisartan Erythromycin may decrease the excretion rate of Telmisartan which could result in a higher serum level.
Fenofibrate The serum concentration of Fenofibrate can be increased when it is combined with Erythromycin.
Belantamab mafodotin Erythromycin may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Cerivastatin The serum concentration of Cerivastatin can be increased when it is combined with Erythromycin.
Prasterone sulfate Erythromycin may decrease the excretion rate of Prasterone sulfate which could result in a higher serum level.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Erythromycin.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Erythromycin.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Erythromycin.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Erythromycin.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Erythromycin.
Silodosin The excretion of Silodosin can be decreased when combined with Erythromycin.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Erythromycin.
Brexpiprazole The metabolism of Brexpiprazole can be decreased when combined with Erythromycin.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Erythromycin.
Everolimus The metabolism of Everolimus can be decreased when combined with Erythromycin.
Flibanserin The metabolism of Flibanserin can be decreased when combined with Erythromycin.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Erythromycin.
Ivabradine The metabolism of Ivabradine can be decreased when combined with Erythromycin.
Ivacaftor The metabolism of Ivacaftor can be decreased when combined with Erythromycin.
Lurasidone The metabolism of Lurasidone can be decreased when combined with Erythromycin.
Olaparib The metabolism of Olaparib can be decreased when combined with Erythromycin.
Sonidegib The metabolism of Sonidegib can be decreased when combined with Erythromycin.
Alfentanil The serum concentration of Alfentanil can be increased when it is combined with Erythromycin.
Atorvastatin The serum concentration of Atorvastatin can be increased when it is combined with Erythromycin.
Avanafil The metabolism of Avanafil can be decreased when combined with Erythromycin.
Carbamazepine The metabolism of Carbamazepine can be decreased when combined with Erythromycin.
Cisapride The serum concentration of Cisapride can be increased when it is combined with Erythromycin.
Disopyramide Erythromycin may increase the QTc-prolonging activities of Disopyramide.
Eplerenone The metabolism of Eplerenone can be decreased when combined with Erythromycin.
Estazolam The serum concentration of Estazolam can be increased when it is combined with Erythromycin.
Fexofenadine Erythromycin can cause an increase in the absorption of Fexofenadine resulting in an increased serum concentration and potentially a worsening of adverse effects.
Fluconazole Fluconazole may increase the QTc-prolonging and arrhythmogenic activities of Erythromycin.
Lovastatin The serum concentration of Lovastatin can be increased when it is combined with Erythromycin.
Mequitazine The risk or severity of ventricular arrhythmias and torsade de pointes can be increased when Erythromycin is combined with Mequitazine.
Pimozide The risk or severity of QTc prolongation and ventricular arrhythmias can be increased when Erythromycin is combined with Pimozide.
Pitavastatin The serum concentration of Pitavastatin can be increased when it is combined with Erythromycin.
Pravastatin The risk or severity of myopathy and rhabdomyolysis can be increased when Erythromycin is combined with Pravastatin.
Quinine The risk or severity of QTc prolongation can be increased when Erythromycin is combined with Quinine.
Quinidine The risk or severity of QTc prolongation can be increased when Erythromycin is combined with Quinidine.
Repaglinide The serum concentration of Repaglinide can be increased when it is combined with Erythromycin.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Erythromycin.
Rilpivirine The serum concentration of Rilpivirine can be increased when it is combined with Erythromycin.
Sildenafil The metabolism of Sildenafil can be decreased when combined with Erythromycin.
Simvastatin The serum concentration of Simvastatin can be increased when it is combined with Erythromycin.
Sirolimus The serum concentration of Sirolimus can be increased when it is combined with Erythromycin.
Temsirolimus The serum concentration of Temsirolimus can be increased when it is combined with Erythromycin.
Terfenadine The serum concentration of Terfenadine can be increased when it is combined with Erythromycin.
Triazolam The serum concentration of Triazolam can be increased when it is combined with Erythromycin.
Zafirlukast The serum concentration of Zafirlukast can be decreased when it is combined with Erythromycin.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Erythromycin.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Erythromycin.
Fentanyl The serum concentration of Fentanyl can be increased when it is combined with Erythromycin.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Erythromycin.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Erythromycin.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Erythromycin.
Eszopiclone The serum concentration of Eszopiclone can be increased when it is combined with Erythromycin.
Zopiclone The serum concentration of Zopiclone can be increased when it is combined with Erythromycin.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Erythromycin.
Alprazolam The serum concentration of Alprazolam can be increased when it is combined with Erythromycin.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Erythromycin.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Erythromycin.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Erythromycin.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Erythromycin.
Telaprevir The serum concentration of Telaprevir can be increased when it is combined with Erythromycin.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Erythromycin.
Picosulfuric acid The therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Erythromycin.
Vincristine The serum concentration of Vincristine can be increased when it is combined with Erythromycin.
Vintafolide The serum concentration of Vintafolide can be increased when it is combined with Erythromycin.
Vincamine The serum concentration of Vincamine can be increased when it is combined with Erythromycin.
Acetyldigitoxin The serum concentration of Acetyldigitoxin can be increased when it is combined with Erythromycin.
Deslanoside The serum concentration of Deslanoside can be increased when it is combined with Erythromycin.
Ouabain The serum concentration of Ouabain can be increased when it is combined with Erythromycin.
Oleandrin The serum concentration of Oleandrin can be increased when it is combined with Erythromycin.

Target Protein

23S ribosomal RNA
Motilin receptor MLNR
Voltage-gated inwardly rectifying potassium channel KCNH2 KCNH2

Referensi & Sumber

Synthesis reference: Takehiro Amano, Masami Goi, Kazuto Sekiuchi, Tomomichi Yoshida, Masahiro Hasegawa, "Process for preparing erythromycin A oxime or a salt thereof." U.S. Patent US5274085, issued October, 1966.
Artikel (PubMed)
  • PMID: 11294369
    Kanazawa S, Ohkubo T, Sugawara K: The effects of grapefruit juice on the pharmacokinetics of erythromycin. Eur J Clin Pharmacol. 2001 Jan-Feb;56(11):799-803.
  • PMID: 12789122
    Ogwal S, Xide TU: Bioavailability and stability of erythromycin delayed release tablets. Afr Health Sci. 2001 Dec;1(2):90-6.
  • PMID: 17585116
    Okudaira T, Kotegawa T, Imai H, Tsutsumi K, Nakano S, Ohashi K: Effect of the treatment period with erythromycin on cytochrome P450 3A activity in humans. J Clin Pharmacol. 2007 Jul;47(7):871-6.
  • PMID: 7429008
    Houin G, Tillement JP, Lhoste F, Rapin M, Soussy CJ, Duval J: Erythromycin pharmacokinetics in man. J Int Med Res. 1980;8 Suppl 2:9-14.
  • PMID: 22083477
    Krasniqi S, Matzneller P, Kinzig M, Sorgel F, Huttner S, Lackner E, Muller M, Zeitlinger M: Blood, tissue, and intracellular concentrations of erythromycin and its metabolite anhydroerythromycin during and after therapy. Antimicrob Agents Chemother. 2012 Feb;56(2):1059-64. doi: 10.1128/AAC.05490-11. Epub 2011 Nov 14.
  • PMID: 8851453
    Amsden GW: Erythromycin, clarithromycin, and azithromycin: are the differences real? Clin Ther. 1996 Jan-Feb;18(1):56-72; discussion 55.
  • PMID: 4714113
    Gordon RC, Regamey C, Kirby WM: Serum protein binding of erythromycin, lincomycin, and clindamycin. J Pharm Sci. 1973 Jul;62(7):1074-7.
  • PMID: 28146011
    Fohner AE, Sparreboom A, Altman RB, Klein TE: PharmGKB summary: Macrolide antibiotic pathway, pharmacokinetics/pharmacodynamics. Pharmacogenet Genomics. 2017 Apr;27(4):164-167. doi: 10.1097/FPC.0000000000000270.
Menampilkan 8 dari 19 artikel.

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