Drug General Information (ID: DDI8C6NYT2)
  Drug Name Ulipristal Drug Info Norgestrel Drug Info
  Drug Type Small molecule Small molecule
  Therapeutic Class Progesterone Receptor Modulators Contraceptive Agents
  Structure

 Mechanism of Ulipristal-Norgestrel Interaction (Severity Level: Moderate)
     Attenuated pharmacological effects (Unspecific) Click to Show/Hide Mechanism Graph
      Drug Name Ulipristal Norgestrel
      Mechanism Post-coital contraceptive
Progesterone receptor  Modulator
Hormonal contraceptives
Progesterone receptor  Agonist
      Key Mechanism Factor 1
Factor Name Progesterone receptor
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Structure Sequence
MTELKAKGPRAPHVAGGPPSPEVGSPLLCRPAAGPFPGSQTSDTLPEVSAIPISLDGLLFPRPCQGQDPSDEKTQDQQSLSDVEGAYSRAEATRGAGGSSSSPPEKDSGLLDSVLDTLLAPSGPGQSQPSPPACEVTSSWCLFGPELPEDPPAAPATQRVLSPLMSRSGCKVGDSSGTAAAHKVLPRGLSPARQLLLPASESPHWSGAPVKPSPQAAAVEVEEEDGSESEESAGPLLKGKPRALGGAAAGGGAAAVPPGAAAGGVALVPKEDSRFSAPRVALVEQDAPMAPGRSPLATTVMDFIHVPILPLNHALLAARTRQLLEDESYDGGAGAASAFAPPRSSPCASSTPVAVGDFPDCAYPPDAEPKDDAYPLYSDFQPPALKIKEEEEGAEASARSPRSYLVAGANPAAFPDFPLGPPPPLPPRATPSRPGEAAVTAAPASASVSSASSSGSTLECILYKAEGAPPQQGPFAPPPCKAPGASGCLLPRDGLPSTSASAAAAGAAPALYPALGLNGLPQLGYQAAVLKEGLPQVYPPYLNYLRPDSEASQSPQYSFESLPQKICLICGDEASGCHYGVLTCGSCKVFFKRAMEGQHNYLCAGRNDCIVDKIRRKNCPACRLRKCCQAGMVLGGRKFKKFNKVRVVRALDAVALPQPVGVPNESQALSQRFTFSPGQDIQLIPPLINLLMSIEPDVIYAGHDNTKPDTSSSLLTSLNQLGERQLLSVVKWSKSLPGFRNLHIDDQITLIQYSWMSLMVFGLGWRSYKHVSGQMLYFAPDLILNEQRMKESSFYSLCLTMWQIPQEFVKLQVSQEEFLCMKVLLLLNTIPLEGLRSQTQFEEMRSSYIRELIKAIGLRQKGVVSSSQRFYQLTKLLDNLHDLVKQLHLYCLNTFIQSRALSVEFPEMMSEVIAAQLPKILAGMVKPLLFHKK
Gene Name PGR NR3C3
Uniprot ID PRGR_HUMAN
KEGG Pathway hsa:5241
Protein Family Nuclear hormone receptor family, NR3 subfamily
Protein Function
The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Depending on the isoform, progesterone receptor functions as transcriptional activator or repressor.; FUNCTION: [Isoform A]: Ligand-dependent transdominant repressor of steroid hormone receptor transcriptional activity including repression of its isoform B, MR and ER. Transrepressional activity may involve recruitment of corepressor NCOR2. ; FUNCTION: [Isoform B]: Transcriptional activator of several progesteron-dependent promoters in a variety of cell types. Involved in activation of SRC-dependent MAPK signaling on hormone stimulation. ; FUNCTION: [Isoform 4]: Increases mitochondrial membrane potential and cellular respiration upon stimulation by progesterone.
    Click to Show/Hide
      Mechanism Description
  • Attenuated pharmacological effects of  Ulipristal when combined with Norgestrel 

Recommended Action
      Management Concomitant use of ulipristal with combination hormonal contraceptives should be avoided. After emergency contraception with ulipristal, routine contraception should be continued or initiated as soon as possible to ensure ongoing prevention of pregnancy. Patients who wish to use progestogen-containing contraceptives should do so no sooner than 5 days after taking ulipristal, and they should use a reliable barrier method of contraception until their next menstrual period.

References
1 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
2 Product Information. ella (ulipristal). Afaxys Inc., Charleston, SC.
3 Schubert W, Eriksson U, Edgar B, Cullberg G, Hedner T "Flavonoids in grapefruit juice inhibit the in vitro hepatic metabolism of 17B-estradiol." Eur J Drug Metab Pharmacokinet 20 (1995): 219-24. [PMID: 8751044]