DescriptionSources: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=f7848550-086a-43d8-8ae5-047f4b9e4382Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/17107221 | http://adisinsight.springer.com/drugs/800013168
Sources: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=f7848550-086a-43d8-8ae5-047f4b9e4382
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/17107221 | http://adisinsight.springer.com/drugs/800013168
Norelgestromin, the progestin, is the active metabolite of norgestimate and is structurally related to 19-nortestosterone. Norgestimate and norelgestromin mimic the physiologic effects of progesterone at the progesterone receptor. Johnson & Johnson developed an adhesive female contraceptive patch that contains ethinylestradiol (0.75mg) and the progestogen norelgestromin (6mg). his product is a combination contraceptive acting via the inhibition gonadotropins. Its primary mechanism of action involves the suppression of ovulation, including changes in the cervical mucus and endometrium. The patch delivers a continuous flow of hormones through the skin and into the bloodstream. The contraceptive patch is available in countries worldwide.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Preventing | ORTHO EVRA Approved UseORTHO EVRA® is indicated for the prevention of pregnancy in women who elect to
use a transdermal patch as a method of contraception. Launch Date2001 |
|||
Preventing | XULANE Approved UseXulane is indicated for the prevention of pregnancy in women who elect to use a transdermal patch as a method of contraception. Launch Date2014 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
987 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31935382 |
6 mg 1 times / day steady-state, transdermal dose: 6 mg route of administration: Transdermal experiment type: STEADY-STATE co-administered: ETHINYL ESTRADIOL |
NORELGESTROMIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
156702 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31935382 |
6 mg 1 times / day steady-state, transdermal dose: 6 mg route of administration: Transdermal experiment type: STEADY-STATE co-administered: ETHINYL ESTRADIOL |
NORELGESTROMIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
27.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31935382 |
6 mg 1 times / day steady-state, transdermal dose: 6 mg route of administration: Transdermal experiment type: STEADY-STATE co-administered: ETHINYL ESTRADIOL |
NORELGESTROMIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3% |
NORELGESTROMIN serum | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
150 ug 1 times / day multiple, transdermal Recommended Dose: 150 ug, 1 times / day Route: transdermal Route: multiple Dose: 150 ug, 1 times / day Co-administed with:: ethinyl estradiol, transdermal(20 ug/day) Sources: Page: p.803 |
healthy, 28.7 n = 1672 Health Status: healthy Condition: Pregnancy prevention Age Group: 28.7 Sex: F Population Size: 1672 Sources: Page: p.803 |
Disc. AE: Application site reaction, Nausea... AEs leading to discontinuation/dose reduction: Application site reaction (1.9%) Sources: Page: p.803Nausea (1.8%) Emotional lability (1.5%) Headache (1.1%) Breast discomfort (1%) Menorrhagia (serious, 0.06%) |
6 mg 1 times / week multiple, transdermal Recommended Dose: 6 mg, 1 times / week Route: transdermal Route: multiple Dose: 6 mg, 1 times / week Co-administed with:: ethinyl estradiol, transdermal(0.75 mg/week) Sources: Page: p.1 |
healthy Health Status: healthy Condition: Pregnancy prevention Sex: F Sources: Page: p.1 |
Disc. AE: Cardiovascular risk, Venous thromboembolism... AEs leading to discontinuation/dose reduction: Cardiovascular risk (serious) Sources: Page: p.1Venous thromboembolism |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Breast discomfort | 1% Disc. AE |
150 ug 1 times / day multiple, transdermal Recommended Dose: 150 ug, 1 times / day Route: transdermal Route: multiple Dose: 150 ug, 1 times / day Co-administed with:: ethinyl estradiol, transdermal(20 ug/day) Sources: Page: p.803 |
healthy, 28.7 n = 1672 Health Status: healthy Condition: Pregnancy prevention Age Group: 28.7 Sex: F Population Size: 1672 Sources: Page: p.803 |
Headache | 1.1% Disc. AE |
150 ug 1 times / day multiple, transdermal Recommended Dose: 150 ug, 1 times / day Route: transdermal Route: multiple Dose: 150 ug, 1 times / day Co-administed with:: ethinyl estradiol, transdermal(20 ug/day) Sources: Page: p.803 |
healthy, 28.7 n = 1672 Health Status: healthy Condition: Pregnancy prevention Age Group: 28.7 Sex: F Population Size: 1672 Sources: Page: p.803 |
Emotional lability | 1.5% Disc. AE |
150 ug 1 times / day multiple, transdermal Recommended Dose: 150 ug, 1 times / day Route: transdermal Route: multiple Dose: 150 ug, 1 times / day Co-administed with:: ethinyl estradiol, transdermal(20 ug/day) Sources: Page: p.803 |
healthy, 28.7 n = 1672 Health Status: healthy Condition: Pregnancy prevention Age Group: 28.7 Sex: F Population Size: 1672 Sources: Page: p.803 |
Nausea | 1.8% Disc. AE |
150 ug 1 times / day multiple, transdermal Recommended Dose: 150 ug, 1 times / day Route: transdermal Route: multiple Dose: 150 ug, 1 times / day Co-administed with:: ethinyl estradiol, transdermal(20 ug/day) Sources: Page: p.803 |
healthy, 28.7 n = 1672 Health Status: healthy Condition: Pregnancy prevention Age Group: 28.7 Sex: F Population Size: 1672 Sources: Page: p.803 |
Application site reaction | 1.9% Disc. AE |
150 ug 1 times / day multiple, transdermal Recommended Dose: 150 ug, 1 times / day Route: transdermal Route: multiple Dose: 150 ug, 1 times / day Co-administed with:: ethinyl estradiol, transdermal(20 ug/day) Sources: Page: p.803 |
healthy, 28.7 n = 1672 Health Status: healthy Condition: Pregnancy prevention Age Group: 28.7 Sex: F Population Size: 1672 Sources: Page: p.803 |
Menorrhagia | serious, 0.06% Disc. AE |
150 ug 1 times / day multiple, transdermal Recommended Dose: 150 ug, 1 times / day Route: transdermal Route: multiple Dose: 150 ug, 1 times / day Co-administed with:: ethinyl estradiol, transdermal(20 ug/day) Sources: Page: p.803 |
healthy, 28.7 n = 1672 Health Status: healthy Condition: Pregnancy prevention Age Group: 28.7 Sex: F Population Size: 1672 Sources: Page: p.803 |
Venous thromboembolism | Disc. AE | 6 mg 1 times / week multiple, transdermal Recommended Dose: 6 mg, 1 times / week Route: transdermal Route: multiple Dose: 6 mg, 1 times / week Co-administed with:: ethinyl estradiol, transdermal(0.75 mg/week) Sources: Page: p.1 |
healthy Health Status: healthy Condition: Pregnancy prevention Sex: F Sources: Page: p.1 |
Cardiovascular risk | serious Disc. AE |
6 mg 1 times / week multiple, transdermal Recommended Dose: 6 mg, 1 times / week Route: transdermal Route: multiple Dose: 6 mg, 1 times / week Co-administed with:: ethinyl estradiol, transdermal(0.75 mg/week) Sources: Page: p.1 |
healthy Health Status: healthy Condition: Pregnancy prevention Sex: F Sources: Page: p.1 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://pubmed.ncbi.nlm.nih.gov/28283499/ Page: - |
inconclusive | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/28283499/ Page: - |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/28283499/ Page: - |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/28283499/ Page: - |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/28283499/ Page: - |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/28283499/ Page: - |
yes | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/28283499/ Page: - |
yes | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/28283499/ Page: - |
yes | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/28283499/ Page: - |
yes | yes (co-administration study) Comment: compounds that inhibit or induce CYP3A4 such as cobicistat, LPR/RTV combination, RTV/ATV combination and EFZ significantly altered the exposure and PK of NGMN (Vogler et al., 2010; Polina German, 2011; Sevinsky et al., 2011; Zhang et al., 2011). A fixed dose combination ofelvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate increased NGMN’s exposure by greater than 2-fold which is consistent with cobicistat’s irreversible CYP3A4 inhibition properties (Polina German, 2011). Sources: https://pubmed.ncbi.nlm.nih.gov/28283499/ Page: - |
Sample Use Guides
Transdermal system: 150 mcg/day norelgestromin and 35 mcg/day ethinyl estradiol.
Route of Administration:
Transdermal
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/12711003
After 24h incubation of physiological concentrations of estrone sulfate 5 nM the inhibitory effect of norelgestromin (NGMN) (a metabolite of norgestimate) at concentrations of 5 nM, 0.5 uM and 50 uM was 43, 74 and 97%, respectively, in T-47D cells; 25, 57 and 96 respectively, in MCF-7 cells. Comparative studies using medroxyprogesterone acetate (MPA) showed that this progestin also has an inhibitory effect on sulfatase activity, but significantly less intense than that of NGMN. The inhibition for MPA at concentrations of 5 nM, 0.5 uM and 50 uM was 31, 47 and 61, respectively, for T-47D cells; 6, 20 and 63, respectively, for MCF-7 cells.
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Classification Tree | Code System | Code | ||
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EMA ASSESSMENT REPORTS |
EVRA (AUTHORIZED: CONTRACEPTION)
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WHO-ATC |
G03AA13
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LIVERTOX |
695
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WHO-VATC |
QG03AA13
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NDF-RT |
N0000175602
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NDF-RT |
N0000011301
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NCI_THESAURUS |
C776
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Code System | Code | Type | Description | ||
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100000092089
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m8053
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PRIMARY | Merck Index | ||
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1959
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DB06713
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R0TAY3X631
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7939
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SUB20476
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1468454
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ALTERNATIVE | |||
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1471958
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PRIMARY | |||
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C449219
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PRIMARY | |||
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NORELGESTROMIN
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C511292
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R0TAY3X631
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326374
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PRIMARY | RxNorm | ||
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C66243
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KK-83
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53016-31-2
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DTXSID9046788
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62930
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CHEMBL1200807
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PRIMARY |
All of the following components must be present:
ACTIVE MOIETY
METABOLITE ACTIVE (PARENT)