Norgestrel
JFDA label: PROGYLUTON Tab
Mechanism of Action
Agonist of Progesterone receptor — Progesterone receptor agonist
| Target | Action | Gene / class |
|---|---|---|
| Progesterone receptor efficacy | AGONIST | PGR |
Indications
Approved
- Hemorrhage — hemorrhage
Off-label
- Endometrial Neoplasms
Dosing
Source: openFDA
Warnings & Precautions
Source: openFDA
Warnings & Precautions
Warnings Allergy alert: Do not use if you are allergic to this product or any of its ingredients, such as FD&C yellow No. 5 (tartrazine). People allergic to aspirin often have a tartrazine allergy too. Symptoms may include hives, facial swelling, asthma (wheezing), shock, skin reddening, rash, blisters. If an allergic reaction occurs, stop use and seek medical help right away. Sexually transmitted diseases (STDs) alert: This product does not protect against HIV/AIDS or other STDs. Do not use • if you have or ever had breast cancer • if you are already pregnant or think you may be pregnant • together with another birth control pill, vaginal ring, patch, implant, injection or an IUD (intra-uterine device) • as an emergency contraceptive (morning after pill). This product does not prevent pregnancy when used after unprotected sex • if you are male Ask a doctor before use if • you currently have vaginal bleeding between your periods and you have not already talked to a doctor • you have liver problems • you have or ever had any cancer Ask doctor or pharmacist before use if • you are taking a prescription drug for seizures, tuberculosis, HIV/AIDS, pulmonary hypertension • you are taking a supplement containing St John’s Wort (an herbal ingredient) • if you have taken ulipristal acetate (an emergency contraceptive, or morning after pill) in the past 5 days See the enclosed leaflet for a detailed list of medicines that may interact with this product. When using this product • you are likely to experience changes in your menstrual periods, such as irregular periods, spotting or bleeding between your periods, or you may stop having periods. To prevent pregnancy, keep taking the product. • you may experience headaches, dizziness, nausea, increased appetite, abdominal pain, cramps or bloating • talk to a doctor (but continue taking every day) if • you have repeated vaginal bleeding brought on by sex • you start having periods that last more than 8 days or are unusually heavy • you start having migraines with aura (headaches that start with changes in vision) or your migraine headaches get worse • take a pregnancy test or talk to a doctor if • your period is late after missing any tablets in the last month • you have not had a period for 2 months or think you may be pregnant Seek medical help right away if • you have sudden or severe persistent pain in your lower belly mostly on one side (you could have an ectopic pregnancy) • you develop yellowing of your skin or whi
Pregnancy & Lactation
Lactation
This record contains information specific to the levonorgestrel implant, which is not available in the United States.
Chemistry & Properties
| Formula | C21H28O2 |
|---|---|
| Molecular weight | 312.45 g/mol |
| IUPAC name | (8R,9S,10R,13S,14S,17R)-13-ethyl-17-ethynyl-17-hydroxy-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-one |
| CAS | 797-63-7 |
| PubChem CID | 13109 |
| InChIKey | WWYNJERNGUHSAO-CULCCENASA-N |
| logP | 3.88 (XLogP 3.3) |
| Polar surface area | 37.3 Ų |
| H-bond acceptors / donors | 2 / 1 |
| Drug-likeness (QED) | 0.75 |
| Lipinski violations | 0 |
SMILES
C#CC1(O)CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@@H]4[C@H]3CC[C@@]21CCBiology & Pharmacokinetics
Pharmacokinetics
| BBB penetrant | No |
|---|
Enzyme interactions
| Enzyme | Role | Detail |
|---|---|---|
| CYP1A2 | Substrate | — |
| CYP2B6 | Inhibitor | — |
| CYP2C19 | Inhibitor | — |
| CYP2C19 | Substrate | — |
| CYP2C8 | Inhibitor | — |
| CYP3A4 | Substrate | — |
Transporters
BCRP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)
Drug–drug interactions (100+, DDInter)
| Interacting drug | Severity | Management |
|---|---|---|
| Acitretin | major | |
| Bexarotene | major | |
| Brigatinib | major | |
| Carfilzomib | major | |
| Dabrafenib | major | |
| Encorafenib | major | |
| Griseofulvin | major | |
| Lumacaftor | major | |
| Mycophenolic acid | major | |
| Sugammadex | major | |
| Tranexamic acid | major | |
| Acarbose | moderate | |
| Adalimumab | moderate | |
| Albiglutide | moderate | |
| Alefacept | moderate | |
| Alogliptin | moderate | |
| Aminophylline | moderate | |
| Anakinra | moderate | |
| Apalutamide | moderate | |
| Aprepitant | moderate | |
| Artemether | moderate | |
| Asparaginase Escherichia coli | moderate | |
| Canagliflozin | moderate | |
| Canakinumab | moderate | |
| Certolizumab pegol | moderate | |
| Chlorpropamide | moderate | |
| Cladribine | moderate | |
| Clarithromycin | moderate | |
| Clotrimazole | moderate | |
| Cobicistat | moderate | |
| Cyclosporine | moderate | |
| Dapagliflozin | moderate | |
| Dasatinib | moderate | |
| Deferasirox | moderate | |
| Dulaglutide | moderate | |
| Elagolix | moderate | |
| Emapalumab | moderate | |
| Empagliflozin | moderate | |
| Enasidenib | moderate | |
| Entrectinib | moderate |
Showing 40 of 100+.
Registered Products (2)
| Brand | Form / strength | Pack | Agent | Citizen (JOD) |
|---|---|---|---|---|
| OVRAL TABS | Tablet 50 mcg, 500 mcg | 21 tab | Arab Company for Medical & Agricultural Products | 1.290 |
| PROGYLUTON Tab | Tablet 0.5 mg, 2 mg | 21 tab | The Jordan Drugstore Co | 1.520 |