ILOTYCIN GLUCEPTATE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ILOTYCIN GLUCEPTATE (ILOTYCIN GLUCEPTATE).
Erythromycin gluceptate is a macrolide antibiotic that inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit, blocking peptide chain elongation.
| Metabolism | Primarily hepatic via CYP3A4; erythromycin is a substrate and inhibitor of CYP3A4. Excretion mainly in bile, with some renal elimination. |
| Excretion | Primarily hepatic metabolism and biliary excretion; about 10-15% excreted unchanged in urine; some fecal elimination due to biliary excretion. |
| Half-life | Terminal elimination half-life is approximately 1.5-2 hours in adults with normal renal function; may be prolonged in hepatic impairment (up to 5-6 hours). |
| Protein binding | Erythromycin is approximately 70-80% bound to plasma proteins, primarily alpha-1-acid glycoprotein. |
| Volume of Distribution | Approximately 0.5-0.7 L/kg, indicating distribution into total body water and moderate tissue penetration. |
| Bioavailability | Intravenous: 100%; intramuscular: approximately 30-40% due to poor absorption; oral (erythromycin base/stearate/estolate): variable 30-65% due to acid instability and first-pass metabolism. |
| Onset of Action | Intravenous: rapid, within 30 minutes after infusion; intramuscular: variable, but clinical effect observed within 1-2 hours. |
| Duration of Action | Intravenous: approximately 6 hours following a single dose; intramuscular: up to 8-12 hours for susceptible organisms. |
| Molecular Weight | 733.93 |
Erythromycin gluceptate (Ilotycin Gluceptate) is administered intravenously at a dose of 250-500 mg every 6 hours for adults. Maximum daily dose: 4 g.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustment is recommended for renal impairment. However, caution is advised in severe renal dysfunction (CrCl <10 mL/min) due to potential accumulation, and monitoring for adverse effects is recommended. |
| Liver impairment | Contraindicated in patients with pre-existing liver disease or hepatic impairment. Avoid use. If necessary, dose reduction may be considered, but no specific guidelines exist. |
| Pediatric use | Intravenous dose: 15-50 mg/kg/day divided every 6 hours. Maximum daily dose: 50 mg/kg, not to exceed 4 g/day. |
| Geriatric use | No specific dose adjustment is required. However, elderly patients may have reduced renal function and increased risk of QT prolongation; use with caution and monitor ECG. |
| 1st trimester | Erythromycin gluceptate crosses the placenta. Use only if clearly needed due to limited safety data. No evidence of major teratogenicity in humans, but risk of cardiovascular malformations reported with some erythromycin formulations. |
| 2nd trimester | Generally considered safe when indicated. Monitor for gastrointestinal effects and QT prolongation. |
| 3rd trimester | Use with caution near term due to risk of infantile hypertrophic pyloric stenosis (IHPS) if used after 32 weeks. |
Clinical note
Comprehensive clinical and safety monograph for ILOTYCIN GLUCEPTATE (ILOTYCIN GLUCEPTATE).
| Placental transfer | Erythromycin gluceptate crosses the placenta. Fetal serum concentrations are approximately 5-20% of maternal serum levels. Placental transfer is limited due to high protein binding and low lipid solubility. |
| Breastfeeding | Erythromycin gluceptate is excreted into breast milk in small amounts. The American Academy of Pediatrics considers erythromycin compatible with breastfeeding, but monitor for possible gastrointestinal disturbances and potential development of resistant bacteria in the infant. Avoid use if maternal QT prolongation risk. |
■ FDA Black Box Warning
Not available
| Serious Effects |
Hypersensitivity to erythromycin or any macrolide antibioticUse with drugs that prolong QT interval and increase risk of torsades de pointes (e.g., pimozide, cisapride, terfenadine, astemizole)Hepatic dysfunction (especially when used with drugs metabolized by CYP3A4)Known QT interval prolongation or history of torsades de pointes
| Precautions | QT prolongation and risk of cardiac arrhythmias (especially torsades de pointes) due to K+ channel blockade; increased risk in elderly, patients with electrolyte disturbances, bradycardia, or concurrent use of other QT-prolonging drugs. Hepatotoxicity; hypersensitivity reactions including anaphylaxis; pseudomembranous colitis; exacerbation of myasthenia gravis; use caution in renal and hepatic impairment. |
| Food/Dietary | Grapefruit and grapefruit juice inhibit CYP3A4 metabolism of erythromycin, increasing risk of QT prolongation and cardiotoxicity. Avoid consumption during therapy. Alcohol may increase gastrointestinal side effects. |
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| Lactation Rating | L2 (Possibly Safe) |
| Teratogenic Risk | Category B: Animal studies have not demonstrated fetal risk, and there are no adequate controlled studies in pregnant women. Erythromycin, including Ilotycin Gluceptate, is generally considered safe in all trimesters when used as indicated. No known teratogenic effects in first trimester; risk of infantile hypertrophic pyloric stenosis (IHPS) if used after second trimester, especially in neonates exposed late in pregnancy or during lactation. |
| Fetal Monitoring | No specific maternal-fetal monitoring required beyond routine obstetric care. Monitor for maternal GI intolerance (nausea, vomiting, abdominal cramps) and signs of hepatitis. In neonate, observe for symptoms of IHPS (projectile vomiting) if exposed late in pregnancy. |
| Fertility Effects | No evidence of adverse effects on human fertility. Animal studies have not shown impaired fertility. |
| Clinical Pearls | Ilotycin Gluceptate (erythromycin gluceptate) is a parenteral macrolide antibiotic indicated for serious infections. Administer IV slowly over 20-60 minutes to reduce thrombophlebitis. Monitor for QTc prolongation, especially with concurrent use of other QT-prolonging drugs. Note potential drug interactions with CYP3A4 substrates (e.g., statins, warfarin). Reduces gastric motility; consider for gastroparesis. |
| Patient Advice | This medication is an antibiotic given through your vein to treat bacterial infections. · You may experience pain or redness at the injection site; report if severe. · Avoid grapefruit and grapefruit juice during treatment as it may increase side effects. · Complete the full course even if you feel better. · Contact your doctor immediately if you experience irregular heartbeat, fainting, or severe diarrhea. |