Home › Compound Library › Midazolam (Versed)

Midazolam (Versed)

Benzodiazepineprescriptionoral · predicted

Ultra-short-acting benzodiazepine used for anxiolysis, sedation, and amnesia in procedural and perioperative settings. Available for IV, oral, intranasal, and intramuscular administration. Rapidly metabolized by CYP3A4/5 to active metabolite 1-OH-midazolam. Widely used as in vivo probe substrate to assess CYP3A4 activity. Respiratory depression risk with opioids (black box warning).

Projected serum levels — 7.5 mg, as needed (shown daily)

Midazolam (Versed)
Midazolam (Versed) modeled serum levels, 7.5 mg as needed (shown daily) over 15 days Population-based pharmacokinetic estimate. Steady state reached after approximately 1 days. 0 0.63 1.3 1.9 2.5 Day 0 Day 4 Day 8 Day 11 Day 15 Time on a regular schedule ≈ steady state · day 1

Maintenance schedule: 7.5 mg as needed (shown daily) (oral).

Modeled steady state after ~1 days: peak ≈ 2.3 mg, trough ≈ 0.009 mg body load. Population-based estimate over 15 days for a 7.5 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.

Key facts

Category
Benzodiazepine
Route modeled
Oral
Model confidence
predicted
Half-life
3 h
Common dose
7.5 mg
Suggested maximum
20 mg/day
Reference dose range
1–20 mg (single dose)
Suggested cadence
as needed (shown daily)
Validated against
7.5 mg oral — Cmax 0.055 mg/L at 0.75 h

Documented interactions

  • contraindicated
    Clarithromycin (Biaxin) + Midazolam (Versed) CYP inhibition

    Clarithromycin (Biaxin) mechanism_based of CYP3A4 predicted to change Midazolam (Versed) AUC by ~6.79x

  • contraindicated
    Diltiazem + Midazolam (Versed) CYP inhibition

    Diltiazem mechanism_based of CYP3A4 predicted to change Midazolam (Versed) AUC by ~6.79x

  • contraindicated
    Efavirenz (Sustiva) + Midazolam (Versed) CYP induction

    Efavirenz (Sustiva) inducer of CYP3A4 predicted to change Midazolam (Versed) AUC by ~0.13x

  • contraindicated
    Grapefruit (whole fruit) + Midazolam (Versed) CYP inhibition

    Grapefruit (whole fruit) mechanism_based of CYP3A4 predicted to change Midazolam (Versed) AUC by ~6.79x

  • contraindicated
    Grapefruit Juice + Midazolam (Versed) CYP inhibition

    Grapefruit Juice mechanism_based of CYP3A4 predicted to change Midazolam (Versed) AUC by ~6.79x

  • contraindicated
    Paxlovid (Nirmatrelvir/Ritonavir) + Midazolam (Versed) CYP inhibition

    Paxlovid (Nirmatrelvir/Ritonavir) mechanism_based of CYP3A4 predicted to change Midazolam (Versed) AUC by ~6.79x

Serum checks 221 modeled interaction pairings for midazolam (versed) across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.

Research behind this entry

  1. Midazolam as a Probe for Drug-Drug Interactions Mediated by CYP3A4: Homotropic Allosteric Mechanism of Site-Specific Hydroxylation Wandel C et al. · Drug Metabolism and Disposition, 2004 DOI

    Establishment of midazolam as preferred CYP3A4 probe substrate, demonstrating regiospecific 1-OH and 4-OH hydroxylation via allosteric effects.

  2. Structural basis for regiospecific midazolam oxidation by human cytochrome P450 3A4 Sevrioukova IF et al. · Proceedings of the National Academy of Sciences, 2017 DOI

    Crystal structure revealing how CYP3A4 catalyzes site-specific midazolam hydroxylation and allosteric modulation mechanism.

  3. Pharmacokinetics of the CYP3A Substrate Midazolam After Steady-state Dosing of Delafloxacin Gotfried MH et al. · Clinical Therapeutics, 2018 DOI

    Clinical CYP3A4 DDI study using midazolam as probe to assess drug-drug interactions with fluoroquinolones.

3 published studies referenced in the app, each with a plain-language summary.