证据内容以英文维护。

Vancomycin 的理想化结构描述

Idealised conformer generated from PubChem SMILES via RDKit ETKDG; not an experimental or predicted structure. A single computed low-energy conformer does not represent conformational ensembles or the receptor-bound (bioactive) conformation.

速览

ENTRY TYPE
approved drug
IDENTITY
Sequence verified

No structure asset recorded

TOP EVIDENCE
Grade A — MRSA bacteremia
MAJOR STATUS
Jurisdiction-specific — see status table
SPORT
Prohibited — as of 2026-08-06
VERIFIED
2026-08-06

Bottom line

Vancomycin is a tricyclic glycopeptide antibiotic with bactericidal activity against Gram-positive bacteria through inhibition of cell wall synthesis. It remains the standard of care for serious MRSA infections. Oral vancomycin is a first-line therapy for C. difficile infection; per IDSA/SHEA 2021 guidelines, fidaxomicin is conditionally preferred over vancomycin for initial CDI episodes when available. Therapeutic drug monitoring is standard practice due to variable and nephrotoxicity risk.

Identity and composition

FieldVerified information
Preferred nameVancomycin
Key aliasesVancomycin hydrochloride, Vancocin, Vancoled
Molecular/sequence identityTricyclic glycopeptide (heptapeptide backbone); C66H75Cl2N9O24 (base); molecular weight 1,449.3 Da (base), 1,485.7 Da (HCl salt). Produced by Amycolatopsis orientalis (formerly Nocardia orientalis).
Modifications/formHydrochloride salt; powder for infusion after ; oral capsules and oral solution for C. difficile. Contains a disaccharide moiety and a unique tricyclic structure not found in typical linear peptides.
Stable identifiers: 14969 (vancomycin); DrugBank: DB00512; ChEBI: CHEBI:28001; CAS: 1404-90-6 (base)
Identity caveatsVancomycin is a glycopeptide (macrocyclic peptide with sugar moieties) rather than a linear peptide or lipopeptide. Distinguish from telavancin, dalbavancin, oritavancin — the "lipoglycopeptides."

Development and approval status

JurisdictionStatus and indicationProduct/sourceAs of
USA (FDA)Approved (1958) — : septicemia, endocarditis, skin/bone/LRT infections (MRSA); Oral: C. difficile and staphylococcal enterocolitisMultiple generic manufacturers; Vancocin1958 (original NDA)
EU (EMA)Approved — same indicationsMultiple productsNational approvals
WHOListed on WHO Essential Medicines ListCurrent
Status is multi-axis
Vancomycin authorization and sport-status profileFour medicine-authorization axes reproduce only documented status rows; sport status is shown separately.UNITED STATESApproved (1958) — IV:septicemia, endocarditis,SOURCE / AS OFROW 1 / 1958 (original NDA)EU/EEAApproved — same indicationsSOURCE / AS OFROW 2 / National approvalsUNITED KINGDOMSOURCE ROW OMITTEDSEE AUDIT REASONSOURCE / AS OFNOT PRESENT / NOT RECORDEDOTHER DOCUMENTEDListed on WHO EssentialMedicines ListSOURCE / AS OFROW 3 / CurrentSPORT STATUS — SEPARATE FROM MEDICINE AUTHORIZATIONWADA status: not prohibited. No US federal CSA scheduling was identified as of 2026-08-06;state law and other jurisdictions were not assessed. Generic and formulation availability is
Authorization belongs to the named product, use, place, and date; sport status is independent.
文字说明
UNITED STATES
USA (FDA): Approved (1958) — IV: septicemia, endocarditis, skin/bone/LRT infections (MRSA); Oral: C. difficile and staphylococcal enterocolitis
EU/EEA
EU (EMA): Approved — same indications
UNITED KINGDOM
No UNITED KINGDOM row is present in the source status table
OTHER DOCUMENTED
WHO: Listed on WHO Essential Medicines List

Sport status: WADA status: not prohibited. No US federal CSA scheduling was identified as of 2026-08-06; state law and other jurisdictions were not assessed. Generic and formulation availability is product- and jurisdiction-specific.

Mechanism and pharmacology

Vancomycin inhibits bacterial cell wall biosynthesis by binding with high affinity to the D-alanyl-D-alanine (D-Ala-D-Ala) terminus of the lipid II–linked peptidoglycan precursor, preventing transpeptidation (cross-linking) and transglycosylation (polymerization). It also alters bacterial cell membrane permeability and RNA synthesis. Bactericidal against most Gram-positive organisms.

: administration; poor oral absorption (oral use limited to GI infections); ~4-8 h (normal renal); >90% excreted unchanged in urine; Vd 0.4-1 L/kg; 30-55% protein-bound. AUC24/MIC is the best PK/PD correlate for efficacy.

Resistance mechanisms

  • VanA: high-level vancomycin resistance (VRE, VRSA) — D-Ala-D-Ala replaced by D-Ala-D-Lac (vancomycin affinity reduced ~1000-fold).

  • VanB: moderate-level resistance (inducible; D-Ala-D-Lac, still susceptible to teicoplanin).

  • VanC: intrinsic, constitutively expressed low-level resistance (D-Ala-D-Ser). Characteristic of E. gallinarum and E. casseliflavus.

  • VISA/hVISA: vancomycin-intermediate S. aureus (MIC 4-8 mcg/mL) due to cell wall thickening.

  • VRSA: vancomycin-resistant S. aureus (MIC ≥16 mcg/mL) — rare, VanA acquisition.

Evidence by claim

Claim/indicationStageGradeBest human evidenceMain resultImportant limitations
MRSA bacteremiaApprovedAMultiple and meta-analyses; vancomycin is the historical reference comparator in MRSA trialsClinical success rates typically 45-65% for MRSA bacteremiaInferior to daptomycin and ceftaroline in some retrospective analyses at higher MICs (≥1.5 mcg/mL)
C. difficile infectionApprovedAMultiple RCTs (fidaxomicin non-inferiority trials; vancomycin as active comparator)Clinical cure 81-97% for initial episodeOral metronidazole no longer first-line (superiority of vancomycin in severe CDI per IDSA/SHEA guidelines)
MRSA pneumoniaApprovedARCTs and retrospective cohortsClinical response 50-75%Debate around optimal dosing (AUC-guided) to reach lung penetration targets
证据等级
  • AA级:已确定特定标签用途
  • BB级:中等人体证据
  • CC级:初步人体证据
  • DD级:仅临床前
  • EE级:轶事/营销声明
  • XX级:证据与该声明相矛盾或不支持该声明
了解有关证据分级的更多信息
Claim-evidence profile
Vancomycin claim-evidence profileA: 3 claims; B: 0 claims; C: 0 claims; D: 0 claims; E: 0 claims; X: 0 claimsCONTRADICTORY / NON-SUPPORTIVEA — Established for a specific labeled useGrade A: Established for a specific labeled use — current approval plus adequate controlled trials and post-market context.3 claimsMRSA bacteremiaC. difficile infection+1 moreB — Moderate human evidenceGrade B: Moderate human evidence — multiple controlled studies or a strong pivotal study, but no current approval for the claim.0 claimsC — Preliminary human evidenceGrade C: Preliminary human evidence — small, uncontrolled, surrogate-endpoint, or early-phase studies.0 claimsD — Preclinical onlyGrade D: Preclinical only — in vitro or animal evidence with no adequate human efficacy evidence.0 claimsE — Anecdotal/marketing claimGrade E: Anecdotal/marketing claim — testimonials, extrapolation, or vendor claims without adequate scientific support.0 claimsX — Evidence contradicts or does not support the claimGrade X: Evidence contradicts or does not support the claim — adequate negative evidence, failed program, or claim inconsistent with the studied material.0 claims
This counts the page's claim rows; it does not average them into a score. All claims: MRSA bacteremia; C. difficile infection; MRSA pneumonia.
文字说明

Text alternative for the claim-evidence diagram. Each grade is defined below:

AEstablished for a specific labeled use
3 claims: MRSA bacteremia; C. difficile infection; MRSA pneumonia
BModerate human evidence
0 claims
CPreliminary human evidence
0 claims
DPreclinical only
0 claims
EAnecdotal/marketing claim
0 claims
XEvidence contradicts or does not support the claim
0 claims
United StatesApproved (1958) — IV: septicemia, endocarditis, skin/bone/LRT infections (MRSA); Oral: C. difficile and staphylococcal enterocolitis
EU/EEAApproved — same indications
OtherListed on WHO Essential Medicines List

Key studies

StudyDesign/populationExposure studiedEndpoints and resultLimitations
Fowler et al. 2006 (daptomycin vs vancomycin/nafcillin)Phase 3 ; N=246; S. aureus bacteremiaVancomycin 1 g q12h (adjusted) vs daptomycin 6 mg/kg IV QDSuccess 41.8% vs 44.2% (non-inferior)Small; vancomycin arm included gentamicin
Johnson et al. 2014 (fidaxomicin vs vancomycin for CDI)Phase 3 RCT; N=629Vancomycin 125 mg PO QID vs fidaxomicin 200 mg PO BID × 10 dCure rates: vancomycin 81.7% vs fidaxomicin 88.2%Vancomycin efficacy consistent with historical data

Dose and administration evidence

Approved labeled regimen

The label summary below is product-, indication-, and jurisdiction-specific; consult the full current label and a licensed clinician/pharmacist.

dosing (normal renal function): Adults — 2 g/day divided as 500 mg q6h or 1 g q12h. Pediatric (1 mo+): 10 mg/kg q6h. Neonates: 15 mg/kg initially, then 10 mg/kg q12h (first week of life) or q8h (thereafter). Infuse over ≥60 min. Oral (C. difficile): 125 mg PO QID × 10 d. Staphylococcal enterocolitis: 500 mg to 2 g/day PO in 3-4 divided doses × 7-10 d. Dose in renal impairment: reduce based on renal function; TDM strongly recommended.

What is not established

  • Optimal dosing strategy (trough-based historically; evolving to AUC24/MIC 400-600).

  • Vancomycin as monotherapy for enterococcal endocarditis (requires aminoglycoside combination per label).

Safety

Established label risks

  • Nephrotoxicity (especially with prolonged courses, high troughs, concomitant nephrotoxins).

  • Ototoxicity (rare but can be irreversible; more common with aminoglycoside combination).

  • Infusion-related reactions: "Red man syndrome" (histamine release from rapid infusion) — flushing, rash, hypotension. Prevented by slower infusion and pre-treatment with antihistamines.

  • Infusion-site phlebitis/inflammation.

  • Neutropenia (rare, typically after prolonged use).

Human-study signals

  • Vancomycin is among the most commonly used hospital antibiotics worldwide. Safety database is large but post-market in nature (lack of modern pre-market clinical trial-based safety characterization).

Unknowns and product-quality risks

  • MIC creep and the clinical significance of MIC ≥1.5-2 mcg/mL.

  • Optimal dosing in obese patients, burn patients, critically ill patients.

  • Compatibility issues (must not mix with many other drugs).

Interactions and special populations

Increased nephrotoxicity risk with aminoglycosides, contrast dye, amphotericin B, cyclosporine, tacrolimus. No CYP metabolism. Renal impairment: dose reduction essential. Elderly: age-related renal decline increases accumulation risk.

Regulatory, compounding, and sport notes

status: not prohibited. No US federal CSA scheduling was identified as of 2026-08-06; state law and other jurisdictions were not assessed. Generic and formulation availability is product- and jurisdiction-specific.

Vancomycin is a glycopeptide antibiotic — not a simple linear peptide. It is classified as a peptide-derived drug for the purposes of this atlas.

Evidence gaps

  • Optimal AUC24/MIC target for non-MRSA Gram-positive infections.

  • Comparative effectiveness of vancomycin vs newer agents (ceftaroline, dalbavancin, oritavancin) for MRSA bacteremia.

  • Better biomarkers for vancomycin-associated nephrotoxicity beyond serum creatinine.

  • Vancomycin loading doses in critically ill patients.

Search notes

  • Databases and registries: FDA label (accessdata.fda.gov), DailyMed, PubMed, IDSA guidelines

  • Search terms: vancomycin, glycopeptide, MRSA, C. difficile, VRE, therapeutic drug monitoring, nephrotoxicity

  • Last searched: 2026-08-06

  • Inclusion emphasis: FDA labels, IDSA/SHEA guidelines, landmark clinical trials

Sources

  1. FDA prescribing information: Vancomycin hydrochloride for injection. Available at: https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/209481s016lbl.pdf (accessed 2026-08-06).

  2. FDA prescribing information: Vancomycin injection. Available at: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213895s000lbl.pdf (accessed 2026-08-06).

  3. DailyMed: Vancomycin hydrochloride. Available at: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=99e523d8-9bde-43cb-8434-497015e5dcbd (accessed 2026-08-06).

  4. Johnson S, et al. Fidaxomicin versus vancomycin for Clostridium difficile infection: meta-analysis of pivotal randomized controlled trials. Clin Infect Dis. 2014;58(6):e84-92. DOI: 10.1093/cid/cit746.

  5. Liu C, et al. Clinical practice guidelines by the Infectious Diseases Society of America for the treatment of methicillin-resistant Staphylococcus aureus infections in adults and children: executive summary. Clin Infect Dis. 2011;52(3):285-92. DOI: 10.1093/cid/cir034.

专家观点

专家怎么说

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问题

What is vancomycin?

Vancomycin is a tricyclic glycopeptide antibiotic with a heptapeptide backbone, produced by Amycolatopsis orientalis. It is a macrocyclic peptide with sugar moieties, distinct from linear peptides and from the lipoglycopeptides (telavancin, dalbavancin, oritavancin).

Is vancomycin FDA-approved?

Yes, vancomycin has been FDA-approved since 1958 for serious Gram-positive infections including MRSA (IV) and C. difficile infection (oral). Multiple generic manufacturers exist. It is listed on the WHO Essential Medicines List.

What evidence supports vancomycin for MRSA and C. difficile?

Multiple RCTs and meta-analyses support vancomycin as the historical reference comparator for MRSA infections, with clinical success typically 45–65% for MRSA bacteremia. For C. difficile, clinical cure rates of 81–97% have been shown. Grade A evidence is available for approved indications.

What are the main safety concerns with vancomycin?

Nephrotoxicity is the most significant concern, especially with prolonged courses or concomitant nephrotoxins. Ototoxicity is rare but can be irreversible. Red man syndrome (histamine release from rapid delivery) causes flushing, rash, and hypotension. Neutropenia occurs rarely after prolonged use.

Can evidence for lipoglycopeptides be applied to vancomycin?

No. Vancomycin is a glycopeptide, while telavancin, dalbavancin, and oritavancin are lipoglycopeptides with structural differences including a lipophilic side chain. These agents have distinct pharmacokinetics, spectra, and regulatory approvals. Evidence for one class cannot be transferred to the other.

What remains unknown about vancomycin?

The optimal AUC24/MIC target for non-MRSA Gram-positive infections is not established. Comparative effectiveness versus newer agents (ceftaroline, dalbavancin, oritavancin) for MRSA bacteremia needs more data. Better biomarkers for nephrotoxicity beyond serum creatinine and optimal loading doses in critically ill patients remain unclear.

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