AZOLID
Clinical safety rating: caution
Comprehensive clinical and safety monograph for AZOLID (AZOLID).
Inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), specifically interfering with peptidoglycan cross-linking.
| Metabolism | Primarily hepatic via glucuronidation and minor CYP450 metabolism; excreted renally as unchanged drug and metabolites. |
| Excretion | Renal (80-90% unchanged), biliary/fecal (10-20%) |
| Half-life | Terminal half-life 1.5-2 hours in normal renal function; prolonged to 4-8 hours in severe renal impairment (CrCl <30 mL/min) |
| Protein binding | 20-30% bound to albumin |
| Volume of Distribution | 0.3-0.4 L/kg; indicates distribution primarily into extracellular fluid |
| Bioavailability | Oral: 60-70% (first-pass metabolism) |
| Onset of Action | Oral: 30-60 minutes; Intravenous: 15-30 minutes |
| Duration of Action | 6-12 hours; dose-dependent, extended by renal impairment |
| Action Class | Macrolides |
| Brand Substitutes | Azax 500 Tablet, Zady 500 Tablet, Trulimax 500mg Tablet, Azifast 500 Tablet, Azee 500 Tablet, Azicip 250 Tablet, Azikem 250mg Tablet, Fitzee 250 Tablet, Azi Q 250mg Tablet, Azax 250 Tablet |
2 g intravenously every 6-8 hours; maximum 8 g/day.
| Dosage form | TABLET |
| Renal impairment | GFR >50 mL/min: no adjustment; GFR 10-50 mL/min: 2 g every 8-12 hours; GFR <10 mL/min: 2 g every 24 hours. Hemodialysis: administer after dialysis. |
| Liver impairment | No specific dosage adjustment recommended for Child-Pugh Class A or B; use with caution in Class C with monitoring. |
| Pediatric use | 50 mg/kg intravenously every 6-8 hours; not to exceed adult dose. Infants <4 weeks: 25 mg/kg every 8 hours. |
| Geriatric use | No specific dose adjustment required; consider renal function and monitor for neurotoxicity. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for AZOLID (AZOLID).
| Breastfeeding | Contraindicated during breastfeeding. M/P ratio not established; drug excreted in breast milk with potential for adverse effects on infant bone development and microbiota disruption. |
| Teratogenic Risk | Pregnancy Category C. First trimester: Potential for impaired bone development and enamel hypoplasia. Second and third trimesters: Risk of fetal discoloration and reversible bone growth retardation. |
| Fetal Monitoring |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to AZOLID or any beta-lactam antibiotic","History of severe allergic reaction to penicillins or cephalosporins"]
| Precautions | ["Hypersensitivity reactions including anaphylaxis","Clostridioides difficile-associated diarrhea","Renal impairment requiring dose adjustment","Superinfection with prolonged use"] |
| Food/Dietary | Avoid tyramine-rich foods: aged cheeses (e.g., cheddar, blue cheese), cured meats (e.g., salami, pepperoni), fermented or pickled foods (e.g., sauerkraut, kimchi), soy products (e.g., tofu, soy sauce), tap beers, and red wines. Also avoid overripe avocados, figs, and fava beans. |
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| Monitor maternal hepatic function, renal function, and complete blood count. Fetal ultrasound for bone growth and cardiac development if used in second/third trimester. |
| Fertility Effects | No specific human data on fertility impairment. Animal studies show reduced spermatogenesis at high doses. Reversible upon discontinuation. |
| Clinical Pearls |
| AZOLID (linezolid) is an oxazolidinone antibiotic. Monitor for myelosuppression (especially thrombocytopenia) weekly due to reversible bone marrow suppression. It is a weak MAO inhibitor; avoid concurrent use of SSRIs, SNRIs, and tyramine-rich foods to prevent serotonin syndrome. Reserve for resistant Gram-positive infections (MRSA, VRE). |
| Patient Advice | Take exactly as prescribed; finish the full course even if you feel better. · Avoid foods high in tyramine (aged cheeses, cured meats, pickled foods, soy sauce, tap beers) while taking this medication and for 2 weeks after stopping to prevent dangerous blood pressure spikes. · Report any unusual bruising, bleeding, or signs of infection (fever, sore throat) promptly. · Do not take with antidepressants (especially SSRIs, SNRIs) without consulting your doctor due to risk of serotonin syndrome (agitation, confusion, rapid heart rate). · May cause diarrhea; if severe or bloody, contact your doctor immediately. |