norethisterone Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| steroids, progestogens | 1962 | 68-22-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A synthetic progestational hormone with actions similar to those of PROGESTERONE but functioning as a more potent inhibitor of ovulation. It has weak estrogenic and androgenic properties. The hormone has been used in treating amenorrhea, functional uterine bleeding, endometriosis, and for CONTRACEPTION.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 2.50 | mg | P |
| 5 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.01 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 2 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.02 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 64 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| May 21, 1962 | FDA | ORTHO MCNEIL PHARM |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Dilatation intrahepatic duct acquired | 230.26 | 47.86 | 26 | 252 | 62 | 2357745 |
| Vaginal haemorrhage | 155.25 | 47.86 | 31 | 247 | 4949 | 2352858 |
| Purpura | 131.22 | 47.86 | 23 | 255 | 1787 | 2356020 |
| Hepatotoxicity | 128.48 | 47.86 | 25 | 253 | 3456 | 2354351 |
| Venoocclusive liver disease | 125.34 | 47.86 | 19 | 259 | 589 | 2357218 |
| Rash maculo-papular | 117.53 | 47.86 | 24 | 254 | 4228 | 2353579 |
| Rectal haemorrhage | 104.28 | 47.86 | 23 | 255 | 5833 | 2351974 |
| Rash erythematous | 103.81 | 47.86 | 23 | 255 | 5953 | 2351854 |
| Melaena | 100.66 | 47.86 | 21 | 257 | 4085 | 2353722 |
| Haemorrhage | 94.73 | 47.86 | 24 | 254 | 11015 | 2346792 |
| Hepatic adenoma | 88.56 | 47.86 | 11 | 267 | 70 | 2357737 |
| Cholestasis of pregnancy | 83.79 | 47.86 | 11 | 267 | 114 | 2357693 |
| Liver function test abnormal | 82.88 | 47.86 | 20 | 258 | 7470 | 2350337 |
| Alanine aminotransferase increased | 79.62 | 47.86 | 22 | 256 | 14010 | 2343797 |
| Haemoglobin decreased | 74.02 | 47.86 | 22 | 256 | 18129 | 2339678 |
| Platelet count increased | 57.89 | 47.86 | 12 | 266 | 2225 | 2355582 |
| Cerebral venous thrombosis | 48.32 | 47.86 | 8 | 270 | 430 | 2357377 |
| Ovarian atrophy | 48.01 | 47.86 | 6 | 272 | 40 | 2357767 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | G03AC01 | GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE Progestogens |
| ATC | G03DC02 | GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM PROGESTOGENS Estren derivatives |
| ATC | G03AA05 | GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE Progestogens and estrogens, fixed combinations |
| ATC | G03AB04 | GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE Progestogens and estrogens, sequential preparations |
| ATC | G03FA01 | GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM PROGESTOGENS AND ESTROGENS IN COMBINATION Progestogens and estrogens, fixed combinations |
| ATC | G03FB05 | GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM PROGESTOGENS AND ESTROGENS IN COMBINATION Progestogens and estrogens, sequential preparations |
| FDA Chemical/Ingredient | N0000011301 | Progesterone Congeners |
| FDA EPC | N0000175602 | Progestin |
| CHEBI has role | CHEBI:49326 | synthetic oral contraceptive |
| MeSH PA | D003270 | Contraceptive Agents |
| MeSH PA | D003271 | Contraceptive Agents, Female |
| MeSH PA | D000080066 | Contraceptive Agents, Hormonal |
| MeSH PA | D003278 | Contraceptives, Oral, Hormonal |
| MeSH PA | D003280 | Contraceptives, Oral, Synthetic |
| MeSH PA | D012102 | Reproductive Control Agents |
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Contraception | indication | 13197004 | |
| Female hypogonadism syndrome | indication | 16041008 | |
| Dysfunctional uterine bleeding | indication | 19155002 | |
| Atrophic vaginitis | indication | 52441000 | |
| Primary ovarian failure | indication | 65846009 | |
| Secondary physiologic amenorrhea | indication | 86030004 | |
| Acne vulgaris | indication | 88616000 | |
| Postmenopausal osteoporosis | indication | 102447009 | |
| Endometriosis | indication | 129103003 | |
| Menopausal flushing | indication | 198436008 | |
| Atrophic vulva | indication | 248861000 | DOID:14275 |
| Menorrhagia | indication | 386692008 | |
| Amenorrhea | off-label use | 14302001 | DOID:13938 |
| Polycystic ovaries | off-label use | 69878008 | |
| Dysmenorrhea | off-label use | 266599000 | |
| Abnormal uterine bleeding unrelated to menstrual cycle | off-label use | 312984006 | |
| Heart valve disorder | contraindication | 368009 | DOID:4079 |
| Hyperlipoproteinemia | contraindication | 3744001 | DOID:1168 |
| Hypocalcemia | contraindication | 5291005 | |
| Hypercholesterolemia | contraindication | 13644009 | |
| Myocardial infarction | contraindication | 22298006 | DOID:5844 |
| Depressive disorder | contraindication | 35489007 | |
| Chloasma | contraindication | 36209000 | |
| Migraine | contraindication | 37796009 | DOID:6364 |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Disorder of gallbladder | contraindication | 39621005 | DOID:0060262 |
| Hypothyroidism | contraindication | 40930008 | DOID:1459 |
| Body fluid retention | contraindication | 43498006 | |
| Thrombosis of retinal vein | contraindication | 46085004 | |
| Humoral hypercalcemia of malignancy | contraindication | 47709007 | |
| Chronic heart failure | contraindication | 48447003 | |
| Dementia | contraindication | 52448006 | |
| Hepatic porphyria | contraindication | 55056006 | DOID:3133 |
| Systemic lupus erythematosus | contraindication | 55464009 | DOID:9074 |
| Hyperlipidemia | contraindication | 55822004 | DOID:1168 |
| Benign mammary dysplasia | contraindication | 57993004 | |
| Obstructive hyperbilirubinemia | contraindication | 59848001 | |
| Thrombophlebitis | contraindication | 64156001 | DOID:3875 |
| Intermenstrual bleeding - irregular | contraindication | 64996003 | |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Hyperglycemia | contraindication | 80394007 | DOID:4195 |
| Epilepsy | contraindication | 84757009 | DOID:1826 |
| Breast lump | contraindication | 89164003 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Malignant neoplasm of liver | contraindication | 93870000 | DOID:3571 |
| Uterine leiomyoma | contraindication | 95315005 | DOID:13223 |
| Deep venous thrombosis | contraindication | 128053003 | |
| Liver function tests abnormal | contraindication | 166603001 | |
| Mammography abnormal | contraindication | 168750009 | |
| Angina pectoris | contraindication | 194828000 | |
| Asthma | contraindication | 195967001 | DOID:2841 |
| Cerebrovascular accident | contraindication | 230690007 | |
| Pulmonary thromboembolism | contraindication | 233935004 | |
| Thrombophilia | contraindication | 234467004 | DOID:2452 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Cholestasis of pregnancy | contraindication | 235888006 | |
| Endometrial carcinoma | contraindication | 254878006 | DOID:2871 |
| Chorea | contraindication | 271700006 | |
| Pregnancy, function | contraindication | 289908002 | |
| Hypertriglyceridemia | contraindication | 302870006 | |
| Functional visual loss | contraindication | 313165001 | |
| Malignant tumor of cervix | contraindication | 363354003 | DOID:4362 |
| Malignant tumor of ovary | contraindication | 363443007 | DOID:2394 |
| Thromboembolic disorder | contraindication | 371039008 | |
| Cardiovascular event risk | contraindication | 395112001 | |
| Disorder of coronary artery | contraindication | 414024009 | |
| Obesity | contraindication | 414916001 | DOID:9970 |
| Estrogen receptor positive tumor | contraindication | 416053008 | |
| Porphyria | contraindication | 418470004 | |
| Optic disc edema | contraindication | 423341008 | DOID:146 |
| Family history of malignant neoplasm of breast | contraindication | 429740004 | |
| Hypertensive urgency | contraindication | 443482000 | |
| Carcinoma of female breast | contraindication | 447782002 | |
| Smokes tobacco daily | contraindication | 449868002 | |
| Nonspecific Abnormal Papanicolaou Smear of Cervix | contraindication | ||
| Major Surgery with Prolonged Post-Operative Immobilization | contraindication |
Acid dissociation constants calculated using MoKa v3.0.0
None
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Progesterone receptor | Nuclear hormone receptor | AGONIST | ED50 | 11.26 | WOMBAT-PK | CHEMBL | |||
| Sodium-dependent serotonin transporter | Transporter | Ki | 5.62 | DRUG MATRIX | |||||
| Glucocorticoid receptor | Nuclear hormone receptor | Ki | 6.71 | DRUG MATRIX | |||||
| Estrogen receptor | Nuclear hormone receptor | Ki | 6.64 | DRUG MATRIX | |||||
| Sex hormone-binding globulin | Secreted | Kd | 7.97 | CHEMBL | |||||
| Androgen receptor | Nuclear hormone receptor | IC50 | 7.12 | WOMBAT-PK | |||||
| Progesterone receptor | Transcription factor | Ki | 8.91 | DRUG MATRIX | |||||
| Estrogen receptor | Transcription factor | Kd | 9.20 | CHEMBL | |||||
| Androgen receptor | Transcription factor | IC50 | 6.92 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4018496 | VUID |
| N0000146818 | NUI |
| C0028356 | UMLSCUI |
| D00182 | KEGG_DRUG |
| 63758001 | SNOMEDCT_US |
| 4018496 | VANDF |
| 7514 | RXNORM |
| 126102009 | SNOMEDCT_US |
| 5187 | MMSL |
| d00555 | MMSL |
| 182290 | MMSL |
| 001298 | NDDF |
| 001326 | NDDF |
| CHEBI:7627 | CHEBI |
| CHEMBL1162 | ChEMBL_ID |
| DB00717 | DRUGBANK_ID |
| T18F433X4S | UNII |
| 687 | INN_ID |
| 6230 | PUBCHEM_CID |
| D009640 | MESH_DESCRIPTOR_UI |
| 2880 | IUPHAR_LIGAND_ID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| GENERESS Fe | HUMAN PRESCRIPTION DRUG LABEL | 3 | 0023-6030 | KIT | 0.80 mg | ORAL | NDA | 19 sections |
| Norethindrone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-7272 | TABLET | 0.35 mg | ORAL | ANDA | 13 sections |
| NORETHINDRONE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-7292 | TABLET | 0.35 mg | ORAL | ANDA | 13 sections |
| NORETHINDRONE AND ETHINYL ESTRADIOL AND FERROUS FUMARATE | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0378-7297 | KIT | 0.40 mg | None | ANDA | 19 sections |
| NORETHINDRONE AND ETHINYL ESTRADIOL AND FERROUS FUMARATE | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0378-7308 | KIT | 0.80 mg | None | ANDA | 19 sections |
| Nortrel | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0555-9008 | KIT | 0.50 mg | None | ANDA | 14 sections |
| Nortrel | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0555-9009 | TABLET | 1 mg | ORAL | ANDA | 14 sections |
| Nortrel | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0555-9010 | KIT | 1 mg | None | ANDA | 14 sections |
| Nortrel 7/7/7 | HUMAN PRESCRIPTION DRUG LABEL | 6 | 0555-9012 | KIT | 0.75 mg | None | ANDA | 15 sections |
| Nortrel 7/7/7 | HUMAN PRESCRIPTION DRUG LABEL | 6 | 0555-9012 | KIT | 1 mg | None | ANDA | 15 sections |
| Nortrel 7/7/7 | HUMAN PRESCRIPTION DRUG LABEL | 6 | 0555-9012 | KIT | 0.50 mg | None | ANDA | 15 sections |
| Balziva | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0555-9034 | KIT | 0.40 mg | None | ANDA | 14 sections |
| Aranelle | HUMAN PRESCRIPTION DRUG LABEL | 4 | 0555-9066 | KIT | 1 mg | None | ANDA | 14 sections |
| Aranelle | HUMAN PRESCRIPTION DRUG LABEL | 4 | 0555-9066 | KIT | 0.50 mg | None | ANDA | 14 sections |
| Cyclafem 1/35 | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0603-7521 | KIT | 1 mg | None | ANDA | 16 sections |
| Cyclafem 7/7/7 | HUMAN PRESCRIPTION DRUG LABEL | 6 | 0603-7525 | KIT | 1 mg | None | ANDA | 16 sections |
| Cyclafem 7/7/7 | HUMAN PRESCRIPTION DRUG LABEL | 6 | 0603-7525 | KIT | 0.75 mg | None | ANDA | 16 sections |
| Cyclafem 7/7/7 | HUMAN PRESCRIPTION DRUG LABEL | 6 | 0603-7525 | KIT | 0.50 mg | None | ANDA | 16 sections |
| Dasetta 7/7/7 | HUMAN PRESCRIPTION DRUG LABEL | 6 | 16714-346 | KIT | 1 mg | ORAL | ANDA | 15 sections |
| Dasetta 7/7/7 | HUMAN PRESCRIPTION DRUG LABEL | 6 | 16714-346 | KIT | 0.50 mg | ORAL | ANDA | 15 sections |
| Dasetta 7/7/7 | HUMAN PRESCRIPTION DRUG LABEL | 6 | 16714-346 | KIT | 0.75 mg | ORAL | ANDA | 15 sections |
| Philith | HUMAN PRESCRIPTION DRUG LABEL | 2 | 16714-347 | KIT | 0.40 mg | ORAL | ANDA | 13 sections |
| Dasetta 1/35 | HUMAN PRESCRIPTION DRUG LABEL | 2 | 16714-348 | KIT | 1 mg | ORAL | ANDA | 14 sections |
| Wera | HUMAN PRESCRIPTION DRUG LABEL | 2 | 16714-370 | KIT | 0.50 mg | ORAL | ANDA | 15 sections |
| DEBLITANE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16714-440 | KIT | 0.35 mg | None | ANDA | 14 sections |
| SHAROBEL | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16714-441 | KIT | 0.35 mg | None | ANDA | 14 sections |
| Necon | HUMAN PRESCRIPTION DRUG LABEL | 2 | 21695-857 | KIT | 1 mg | None | ANDA | 13 sections |
| Necon 0.5/35 | HUMAN PRESCRIPTION DRUG LABEL | 2 | 42254-287 | KIT | 0.50 mg | None | ANDA | 14 sections |
| ALYACEN 1/35 | HUMAN PRESCRIPTION DRUG LABEL | 2 | 50090-1477 | KIT | 1 mg | None | ANDA | 12 sections |
| ALYACEN 7/7/7 | HUMAN PRESCRIPTION DRUG LABEL | 2 | 50090-1478 | KIT | 0.50 mg | None | ANDA | 12 sections |