Page last updated: 2024-11-06

norelgestromin

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

norelgestromin: transdermal hormonal contraceptive [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID13752005
MeSH IDM0417269

Synonyms (3)

Synonym
norelgestromin
15-ethyl-14-ethynyl-5-(hydroxyimino)tetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-en-14-ol
(3z)-13-ethyl-17-ethynyl-3-hydroxyimino-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-17-ol

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Adverse events were typical of hormonal contraception, and most were mild-to-moderate in severity and not treatment limiting."( Efficacy and safety of a transdermal contraceptive system.
Creasy, GW; Fisher, AC; Lenihan, JP; Meador, ML; Shangold, GA; Smallwood, GH, 2001
)
0.31
"2%) participants experienced a serious adverse event classified as possibly, probably, or likely related to the patch."( A comparative and pooled analysis of the safety and tolerability of the contraceptive patch (Ortho Evra/Evra).
Creasy, GW; Fisher, AC; Meador, ML; Odlind, V; Shangold, GA; Sibai, BM, 2002
)
0.31
"Overall, the contraceptive patch is well tolerated and has a side effect profile similar to an established oral contraceptive."( A comparative and pooled analysis of the safety and tolerability of the contraceptive patch (Ortho Evra/Evra).
Creasy, GW; Fisher, AC; Meador, ML; Odlind, V; Shangold, GA; Sibai, BM, 2002
)
0.31
"evaluation of the frequency of adverse events during the therapy with a transdermal contraceptive system (TCS) in comparison to an oral contraceptive."( [Safety evaluation of a transdermal contraceptive system with an oral contraceptive].
Radowicki, S; Skórzewska, K; Szlendak, K, 2005
)
0.33
" Safety evaluation was based on the frequency of adverse effects, changes in physical and gynecological examinations."( [Safety evaluation of a transdermal contraceptive system with an oral contraceptive].
Radowicki, S; Skórzewska, K; Szlendak, K, 2005
)
0.33
"The incidence of most adverse effects was similar between the transdermal and oral contraceptive therapies, except of a higher incidence of breast pain, dysmenorrhoea and application site reactions in the patch group."( [Safety evaluation of a transdermal contraceptive system with an oral contraceptive].
Radowicki, S; Skórzewska, K; Szlendak, K, 2005
)
0.33
"The study suggests that a transdermal contraceptive system is a safe and well tolerated therapy."( [Safety evaluation of a transdermal contraceptive system with an oral contraceptive].
Radowicki, S; Skórzewska, K; Szlendak, K, 2005
)
0.33

Pharmacokinetics

The study looked at the pharmacokinetic profile of norelgestromin (NGMN) and ethinyloestradiol (EE) following application of the contraceptive patch, Evra/Ortho Evra.

ExcerptReferenceRelevance
"Biotransformation, pharmacologic, and pharmacokinetic studies of norgestimate and its metabolites indicate that 17-deacetyl norgestimate, along with the parent drug, contributes to the biologic response."( Pharmacologic and pharmacokinetic characteristics of norgestimate and its metabolites.
Flor, S; Hahn, DW; Kafrissen, ME; McGuire, JL; Phillips, A; Tolman, EL, 1990
)
0.28
" This overview summarizes the relevant pharmacokinetic data for the contraceptive patch."( Pharmacokinetic overview of Ortho Evra/Evra.
Abrams, LS; Natarajan, J; Skee, D; Wong, FA, 2002
)
0.31
"The contraceptive patch exhibits an excellent pharmacokinetic profile, maintaining efficacious serum hormone concentrations under varying conditions."( Pharmacokinetic overview of Ortho Evra/Evra.
Abrams, LS; Natarajan, J; Skee, D; Wong, FA, 2002
)
0.31
"To determine the pharmacokinetic profile of norelgestromin (NGMN) and ethinyloestradiol (EE) following application of the contraceptive patch, Evra/Ortho Evra, at each of four anatomic sites (abdomen, buttock, arm, and torso)."( Pharmacokinetics of a contraceptive patch (Evra/Ortho Evra) containing norelgestromin and ethinyloestradiol at four application sites.
Abrams, LS; Anderson, GD; Natarajan, J; Skee, DM; Wong, FA, 2002
)
0.31
" Comparable systemic exposure of EE and 17-DNE in the presence and absence of dexloxiglumide suggests that dexloxiglumide treatment is unlikely to interfere with the safety and efficacy of oral contraceptives based on the analysis of the resulting pharmacokinetic profile."( Effect of multiple-dose dexloxiglumide on the pharmacokinetics of oral contraceptives in healthy women.
Abramowitz, W; Jakate, AS; Kapil, R; Patel, A; Persiani, S; Roy, P; Wangsa, J, 2005
)
0.33
" The clinical significance of the differences in pharmacokinetic and pharmacodynamic profiles between the patch and oral contraceptive is not fully known."( Pharmacokinetics and pharmacodynamics of a transdermal contraceptive patch and an oral contraceptive.
Devineni, D; Janssens, L; LaGuardia, KD; Leung, AT; Massarella, J; Skee, D; Vaccaro, N, 2007
)
0.34
"5, 2, 3, 4, 6, 8, 12, and 24 hours postdose on day 21 of each cycle for determination of AUC0-24 h and Cmax of ethinyl estradiol and norelgestromin."( Influence of taranabant, an orally active, highly selective, potent cannabinoid-1 receptor (CB1R) inverse agonist, on ethinyl estradiol and norelgestromin plasma pharmacokinetics.
Dunbar, S; Johnson-Levonas, AO; Lasseter, KC; Li, S; Miller, DL; Rosko, K; Schwartz, JI; Wagner, JA; Yuan, J, 2009
)
0.35
" The method has been successfully applied to a pharmacokinetic study of the ORTHO EVRA patch in rabbits."( Determination of norelgestromin in rabbit plasma by LC-MS/MS and its application to the pharmacokinetic study of ORTHO EVRA.
Ding, C; Ge, Q; Liu, X; Zhi, X; Zhou, Z, 2009
)
0.35

Compound-Compound Interactions

ExcerptReferenceRelevance
" This 2-period crossover study was conducted to evaluate the potential for drug-drug interaction between DMF (240 mg twice daily) and a combined oral contraceptive (OC; norgestimate 250 μg, ethinyl estradiol 35 μg)."( Evaluation of Potential Drug-Drug Interaction Between Delayed-Release Dimethyl Fumarate and a Commonly Used Oral Contraceptive (Norgestimate/Ethinyl Estradiol) in Healthy Women.
Kam, J; Leahy, M; Meka, V; Nestorov, I; Sheikh, SI; Zhao, G; Zhu, B, 2017
)
0.46

Bioavailability

ExcerptReferenceRelevance
" The very poor solubility and wettability of these drugs, along with their high potency (adsorption issues), give rise to difficulties in designing intravenous (IV) formulations to assess absolute bioavailability of products containing both drugs."( Norelgestromin/ethinyl estradiol intravenous infusion formulation optimization, stability and compatibility testing: A case study to overcome polysorbate 80 interference in chromatographic analysis.
Abdallah, IA; Hammell, DC; Hassan, HE; Stinchcomb, AL, 2016
)
0.43

Dosage Studied

Norelgestromin and ethinyl estradiol were superimposable following OC alone and OC coadministered with DMF.

ExcerptRelevanceReference
" The contraceptive patch provided ovulation suppression and cycle control similar to that of oral norgestimate 250 microg/EE 35 microg, significantly decreased mean maximum follicular diameter following a 3-day intentional delayed dosing phase when compared with oral levonorgestrel (LNG) 50/75/125 microg/EE 30/40/30 micorg and oral LNG 100 microg/EE 20 microg, and was as effective as oral LNG 50/75/125 microg/EE 30/40/30 microg and oral desogestrel 150 microg/EE 20 microg in altering cervical mucus composition (i."( Transdermal contraception.
Abrams, LS; Creasy, GW; Fisher, AC, 2001
)
0.31
" A major advantage of this method compared to oral contraceptives is a nearly 90% perfect adherence to the dosing schedule across all age groups."( The transdermal contraceptive patch: a new approach to hormonal contraception.
Burkman, RT,
)
0.13
"To compare the effects of the contraceptive patch to oral contraceptives (OCs) on follicular size and incidence of ovulation in normal cycles and after dosing errors."( Ortho Evra/Evra versus oral contraceptives: follicular development and ovulation in normal cycles and after an intentional dosing error.
Archer, DF; Creasy, GW; Fisher, AC; Moreau, M; Pierson, RA; Shangold, GA, 2003
)
0.32
"Follicular size and incidence of ovulation were significantly reduced among contraceptive patch users compared with women using OCs in normal cycles and after planned dosing errors."( Ortho Evra/Evra versus oral contraceptives: follicular development and ovulation in normal cycles and after an intentional dosing error.
Archer, DF; Creasy, GW; Fisher, AC; Moreau, M; Pierson, RA; Shangold, GA, 2003
)
0.32
" Reduced frequency of dosing has the potential to improve patient compliance."( Transdermal delivery of sex steroids for hormone replacement therapy and contraception. A review of principles and practice.
Henzl, MR; Loomba, PK, 2003
)
0.32
"250 mg per 7-day phase, respectively) for 5 days (days 17-21) concurrently with either 200 mg dexloxiglumide (3 times a day on days 17-20, followed by a single dose on day 21) or matching placebo during 2 consecutive 28-day OC dosing cycles."( Effect of multiple-dose dexloxiglumide on the pharmacokinetics of oral contraceptives in healthy women.
Abramowitz, W; Jakate, AS; Kapil, R; Patel, A; Persiani, S; Roy, P; Wangsa, J, 2005
)
0.33
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (69)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (1.45)18.7374
1990's3 (4.35)18.2507
2000's55 (79.71)29.6817
2010's10 (14.49)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials29 (39.19%)5.53%
Reviews16 (21.62%)6.00%
Case Studies0 (0.00%)4.05%
Observational1 (1.35%)0.25%
Other28 (37.84%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (13)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
The Impact of Different Administration Routes of Hormonal Contraceptives on Androgen Synthesis, Glucose Metabolism and Inflammation. A Prospective Randomized Trial. [NCT01087879]45 participants (Anticipated)Interventional2007-10-31Completed
An Open Label Multicentre Study to Evaluate Patient Satisfaction and Preference for the EVRA Transdermal Contraceptive System Compared to Previously Used Contraceptive Method. [NCT00653016]Phase 4405 participants (Actual)Interventional2002-10-31Completed
A Definitive Bioequivalence Study of ORTHO EVRA Exhibiting Faster Equilibration Profile and Currently Marketed ORTHO EVRA in Healthy Female Volunteers [NCT00775086]Phase 142 participants (Actual)Interventional2004-05-31Completed
Transdermal Contraception Patch: EU Cycle Control Study Versus EVRA [NCT00984789]Phase 3393 participants (Actual)Interventional2009-05-31Completed
The Effects of Oral Contraceptive Pills vs Hormonal Patch on Coagulation Parameters [NCT00554632]24 participants (Actual)Interventional2003-04-30Completed
An Open-label Study to Evaluate Contraceptive Efficacy and Safety of the Transdermal Contraceptive System of 17dNorgestimate and Ethinyl Estradiol With the Oral Contraceptive Mercilon. [NCT00236782]Phase 31,517 participants (Actual)Interventional1997-10-31Completed
An Open-Label, Randomized, Multicenter Trial to Evaluate Continuation Rates, Side Effects and Acceptability of NuvaRing Versus OrthoEvra [NCT00269620]Phase 4500 participants (Actual)Interventional2005-06-30Completed
A Comparative Pharmacokinetic Study of EVRA and CILEST in Healthy Female Volunteers [NCT00254865]Phase 134 participants (Actual)Interventional2002-08-31Completed
An Open-label Study to Evaluate Contraceptive Efficacy and Safety of the Transdermal Contraceptive System of 17deacetyl-norgestimate and Ethinyl Estradiol. [NCT00236769]Phase 31,751 participants (Actual)Interventional1997-11-30Completed
Open-Label, Randomized, Partially Balanced, Incomplete Block Design Study to Evaluate the Hormone Exposure From Commercial EVRA (Manufactured by LOHMANN Therapie-Systeme) and an Oral Contraceptive [NCT00258063]Phase 160 participants (Actual)Interventional2004-05-31Completed
An Open-label Study to Evaluate the Contraceptive Efficacy and Safety of the Transdermal Contraceptive System of 17-deacetylnorgestimate and Ethinyl Estradiol With the Oral Contraceptive Triphasil. [NCT00236795]Phase 31,494 participants (Actual)Interventional1997-01-31Completed
An Open Label, Multicentre Study of the EVRA (Norelgestromin + Ethinyl Estradiol) Transdermal Contraceptive Patch in Europe: Evaluation of Women's Experience With EVRA� and Comparison With Previously Used Methods of Contraception. [NCT00261482]Phase 4778 participants (Actual)Interventional2003-07-31Completed
A Randomized, Open-Label, Multicenter Study Comparing the Bleeding Profile of Ortho Evra (Norelgestromin/Ethinyl Estradiol) Continuous Regimen vs. Ortho Evra Cyclic Regimen [NCT00320580]Phase 2239 participants (Actual)InterventionalCompleted
[information is prepared from clinicaltrials.gov, extracted Sep-2024]