Opioids Library

ISO 17025–ACCREDITED LABORATORY ENVIRONMENT

Opioids DMPK and Bioanalytical Services

Opioid bioanalysis is defined by metabolic diversity unmatched by any other class in this library. Codeine is a CYP2D6 prodrug — its active metabolite, morphine, is a separate compound in this same drug index. Morphine itself is metabolized not by CYP but by UGT2B7 Phase II glucuronidation. Tramadol straddles both prodrug activation and Phase I metabolism. Buprenorphine spans CYP3A4 Phase I and UGT Phase II simultaneously. The remaining five opioids follow CYP3A4/CYP2D6 Phase I metabolism. No single cofactor, no single enzyme panel, and no single incubation protocol serves all nine compounds — because the metabolite of one opioid is the parent drug of another.

Creative Proteomics provides CYP2D6 prodrug activation monitoring, CYP Phase I metabolic profiling, UGT Phase II glucuronidation analysis, dual-cofactor Phase I+II profiling, and custom multi-opioid panels with mechanism-matched incubation arms.

Prodrug Activation: Codeine & TramadolCodeine (CYP2D6→morphine) and tramadol (CYP2D6→active metabolite) require prodrug activation monitoring with NADPH cofactor.
Phase II GlucuronidationMorphine (UGT2B7) and buprenorphine (UGT) require UDPGA cofactor. Morphine needs no NADPH at all.
Metabolite = Next CompoundCodeine CYP2D6 metabolism produces morphine — a separate entry in this index. Sequential pathway, dual-compound readout.
Opioid Metabolic Diversity DMPK Strategy Map
Prodrug Activation (NADPH)Codeine (CYP2D6→morphine), tramadol (CYP2D6→active metabolite). Prodrug activation monitoring — simultaneous parent-prodrug and active metabolite quantification.
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CYP Phase I Metabolism (NADPH)Fentanyl (CYP3A4), pethidine (CYP3A4/2B6), oxycodone/hydrocodone (CYP3A4/2D6), methadone (CYP3A4/2B6/2C19) — multi-isoform incubation.
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Phase II Glucuronidation (UDPGA)Morphine (UGT2B7, UDPGA-only, no NADPH). Buprenorphine (UGT+CYP3A4, both cofactors). Two distinct Phase II strategies.
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Sequential Pathway AnalyticsCodeine→morphine via CYP2D6, morphine→glucuronide via UGT2B7. One compound's metabolite is another's parent — two linked assays in sequence.
Opioid mechanism mapping before method development.Creative Proteomics classifies each opioid as CYP prodrug, CYP Phase I substrate, UGT Phase II substrate, or dual Phase I+II — because codeine's metabolite IS morphine, and a NADPH-only incubation misses both the prodrug activation step and the downstream UGT2B7 glucuronidation.
Opioid Drug Index

Find the Opioid Compound Behind the Study

Opioid studies split across four mechanisms: CYP prodrug activation, CYP Phase I metabolism, UGT Phase II glucuronidation, and dual Phase I+II — with codeine producing morphine as its active metabolite. Use the index to classify the mechanism before method development.

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9 entries · Page 1 of 5
Analytical Pain Points

What Drives Assay Failure in Opioid Studies?

Opioid assays fail when four mechanisms — prodrug activation, CYP Phase I, UGT Phase II, and dual Phase I+II — are forced into one protocol. Codeine needs NADPH to become morphine. Morphine needs UDPGA to become glucuronide. The same incubation that activates codeine will miss morphine glucuronidation entirely.

Codeine Is a Prodrug — Morphine Is Its Metabolite

Codeine requires CYP2D6 NADPH-supplemented incubation to monitor codeine→morphine conversion. Morphine, the product of this reaction, is a separate compound in this index with its own UGT2B7 Phase II metabolism.

Our responseSimultaneous codeine-prodrug and morphine-product quantification with CYP2D6-genotyped incubation and NADPH cofactor.
Simultaneous Parent-Metabolite Panels →

Morphine: Phase II Glucuronidation, No CYP

Morphine is metabolized by UGT2B7 via Phase II glucuronidation. UDPGA is the required cofactor. Adding NADPH adds nothing; omitting UDPGA produces zero morphine-3/6-glucuronide data.

Our responseUDPGA-supplemented UGT2B7 glucuronidation incubation with morphine-3-glucuronide and morphine-6-glucuronide quantification.
Phase I & II Metabolite Characterization →

Tramadol: Prodrug + Phase I in One Compound

Tramadol is both a CYP2D6 prodrug (activation to O-desmethyltramadol) and a CYP Phase I substrate. Two analytical dimensions in one compound — prodrug activation monitoring and Phase I metabolite profiling.

Our responseDual-readout tramadol workflow: prodrug activation quantification (CYP2D6→active metabolite) and Phase I depletion kinetics in parallel.
Metabolite Identification →

Buprenorphine: Phase I + II Dual-Cofactor

Buprenorphine undergoes CYP3A4 Phase I (NADPH) and UGT Phase II (UDPGA). Both cofactors must be present. NADPH-only or UDPGA-only captures half the clearance pathway.

Our responseDual-cofactor (NADPH+UDPGA) incubation with CYP3A4 Phase I and UGT Phase II metabolite profiling in one incubation.
Phase I & II Metabolite Characterization →

Multi-Opioid Panels: Four Mechanisms, One Study

CYP prodrug activation (codeine, tramadol), CYP Phase I (fentanyl, pethidine, oxycodone, hydrocodone, methadone), UGT Phase II (morphine), and dual Phase I+II (buprenorphine) — four distinct analytical strategies, not one pooled method.

Our responseMechanism-matched panels with prodrug activation, CYP Phase I, UGT Phase II, and dual-cofactor arms in one validated study.
Custom Panels →
Focused Service Paths

Four Practical Routes for Opioid Studies

Opioid workflows should be selected by mechanism: CYP2D6 prodrug activation for codeine and tramadol; CYP Phase I metabolism for fentanyl, pethidine, oxycodone, hydrocodone, and methadone; UGT Phase II for morphine; dual Phase I+II for buprenorphine; or mechanism-matched panels for mixed studies.

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CYP Prodrug Activation & Monitoring

For codeine and tramadol — CYP2D6-mediated prodrug-to-active metabolite conversion monitoring with NADPH cofactor.

  • Codeine→morphine CYP2D6 activation
  • Tramadol→active metabolite activation
  • Simultaneous prodrug-product quantification
Simultaneous Parent-Metabolite Panels →
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CYP Phase I Metabolism & MetID

For fentanyl, pethidine, oxycodone, hydrocodone, and methadone — multi-CYP Phase I metabolism in microsome/hepatocyte models.

  • Multi-CYP incubation (CYP3A4/2D6/2B6/2C19)
  • Phase I metabolite profiling
  • Isoform-specific depletion kinetics
Metabolite Identification →
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UGT Phase II Glucuronidation

For morphine (UGT2B7, UDPGA-only) and buprenorphine (UGT+CYP3A4, dual-cofactor) — Phase II glucuronidation profiling.

  • Morphine: UGT2B7 UDPGA-only incubation
  • Buprenorphine: UGT+CYP3A4 dual-cofactor
  • Glucuronide metabolite identification
Phase I & II Metabolite Characterization →
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Custom Multi-Opioid Panel Development

For studies spanning prodrug activation, CYP Phase I, UGT Phase II, and dual-cofactor mechanisms in one validated panel.

  • Prodrug activation arm (codeine, tramadol)
  • CYP Phase I arm (fentanyl, pethidine, etc.)
  • UGT Phase II + dual-cofactor arms
Custom Multi-Analyte Drug Panels →
Project Inquiry

Need Support for a Novel or Unlisted Opioid?

If your opioid has a specific mechanism — prodrug activation, Phase I, Phase II, or dual Phase I+II — not covered by standard protocols, Creative Proteomics maps the metabolic pathway before method development.

Creative Proteomics classifies the compound as CYP prodrug, CYP Phase I, UGT Phase II, or dual-cofactor — then selects enzyme system, cofactor, and incubation conditions accordingly.

Target opioid
Prodrug / Phase I / Phase II / dual
CYP isoform or UGT specificity
Cofactor requirement
Sequential pathway context
Panel requirements

Ready to Quantify Your Lead Compound or Metabolite?

Share your matrix type, sample count, and expected range—feasibility routing will confirm whether direct quantification is fit-for-purpose or method development is recommended.

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