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Norgestimate

Hormonal Contraceptiveprescriptionoral · inferred

Third-generation prodrug progestin rapidly deacetylated to the primary active metabolite norelgestromin (also the transdermal-patch active) and secondarily to levonorgestrel (~20% conversion). Parent norgestimate is essentially undetectable in plasma due to near-complete first-pass hydrolysis, so PK is described for norelgestromin (t1/2 ~28 h). Lower androgenic activity than older 19-nor progestins, making it skin/lipid-profile friendly. Component of Ortho Tri-Cyclen, Sprintec, Tri-Sprintec.

Projected serum levels — 250 mcg (≈ 0.25 mg), once daily

Norgestimate (precursor)Norelgestromin
Norgestimate modeled serum levels, 250 mcg (≈ 0.25 mg) once daily over 15 days Population-based pharmacokinetic estimate. Steady state reached after approximately 1 days. 0 0.25 0.50 0.75 1 Day 0 Day 4 Day 8 Day 11 Day 15 Time on a regular schedule ≈ steady state · day 1

Maintenance schedule: 250 mcg (≈ 0.25 mg) once daily (oral).

Modeled steady state after ~1 days: peak ≈ 0.12 mg, trough ≈ 0.000 mg body load. Population-based estimate over 15 days for a reference dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.

Key facts

Category
Hormonal Contraceptive
Route modeled
Oral
Model confidence
inferred
Half-life
28 h
Common dose
250 mcg (≈ 0.25 mg)
Suggested maximum
250 mcg/day
Reference dose range
125–250 mcg (single dose)
Suggested cadence
once daily
Validated against
0.25 mg oral — Cmax 0.002 mg/L at 1.5 h

Documented interactions

  • danger
    7-Hydroxymitragynine (7-OH) + Norgestimate CYP inhibition

    Norgestimate reversible_inhibitor of CYP3A4 predicted to change 7-Hydroxymitragynine (7-OH) AUC by ~2.20x

  • danger
    Alfuzosin (Uroxatral) + Norgestimate CYP inhibition

    Norgestimate reversible_inhibitor of CYP3A4 predicted to change Alfuzosin (Uroxatral) AUC by ~3.33x

  • danger
    Alprazolam (Xanax) + Norgestimate CYP inhibition

    Norgestimate reversible_inhibitor of CYP3A4 predicted to change Alprazolam (Xanax) AUC by ~3.33x

  • danger
    Amlodipine (Norvasc) + Norgestimate CYP inhibition

    Norgestimate reversible_inhibitor of CYP3A4 predicted to change Amlodipine (Norvasc) AUC by ~3.33x

  • danger
    Anastrozole (Arimidex) + Norgestimate CYP inhibition

    Norgestimate reversible_inhibitor of CYP3A4 predicted to change Anastrozole (Arimidex) AUC by ~2.68x

  • danger
    Astaxanthin + Norgestimate CYP inhibition

    Norgestimate reversible_inhibitor of CYP3A4 predicted to change Astaxanthin AUC by ~3.33x

Serum checks 450 modeled interaction pairings for norgestimate across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.

Research behind this entry

  1. Pharmacokinetics of norgestimate and ethinyl estradiol in women after single- and multiple-dose administration of oral contraceptives Wiesinger H et al. · Contraception, 1998 DOI

    PK characterization establishing that norgestimate is undetectable in plasma (rapid presystemic hydrolysis) and norelgestromin is the operative PK species with terminal t1/2 ~28 h.

  2. Pharmacokinetics of a contraceptive patch (Evra/Ortho Evra) containing norelgestromin and ethinyl estradiol at four application sites Abrams LS et al. · American Journal of Obstetrics and Gynecology, 2001 DOI

    Comprehensive PK study of transdermal norelgestromin delivery with detailed clearance, half-life, and protein binding parameters.

  3. Norgestimate and ethinyl estradiol pharmacokinetics: a review Phillips A et al. · Contraception, 1992 DOI

    Foundational review establishing the norgestimate -> norelgestromin -> 3-keto-LNG metabolic cascade and pharmacokinetic implications.

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