norethisterone 🐶 Veterinary Use | 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 |
|---|---|---|---|---|---|---|
| Vaginal haemorrhage | 118.83 | 19.22 | 56 | 5298 | 24495 | 50575275 |
| Hepatic adenoma | 103.60 | 19.22 | 19 | 5335 | 265 | 50599505 |
| Endometriosis | 53.39 | 19.22 | 19 | 5335 | 4056 | 50595714 |
| Pelvic pain | 49.41 | 19.22 | 24 | 5330 | 11189 | 50588581 |
| Purpura | 49.12 | 19.22 | 23 | 5331 | 9888 | 50589882 |
| Heavy menstrual bleeding | 42.04 | 19.22 | 24 | 5330 | 15513 | 50584257 |
| Pregnancy on oral contraceptive | 40.67 | 19.22 | 11 | 5343 | 947 | 50598823 |
| Intermenstrual bleeding | 40.67 | 19.22 | 18 | 5336 | 6796 | 50592974 |
| Exposure to allergen | 39.75 | 19.22 | 8 | 5346 | 186 | 50599584 |
| Rash erythematous | 32.51 | 19.22 | 28 | 5326 | 34824 | 50564946 |
| Rash maculo-papular | 32.43 | 19.22 | 25 | 5329 | 26616 | 50573154 |
| Ovarian atrophy | 32.36 | 19.22 | 6 | 5348 | 89 | 50599681 |
| Uterine perforation | 32.13 | 19.22 | 15 | 5339 | 6400 | 50593370 |
| Drug-induced liver injury | 29.14 | 19.22 | 24 | 5330 | 28071 | 50571699 |
| Aplastic anaemia | 26.64 | 19.22 | 14 | 5340 | 7689 | 50592081 |
| Cerebral venous sinus thrombosis | 26.57 | 19.22 | 9 | 5345 | 1659 | 50598111 |
| Genital burning sensation | 26.55 | 19.22 | 6 | 5348 | 245 | 50599525 |
| Hereditary angioedema | 25.03 | 19.22 | 12 | 5342 | 5430 | 50594340 |
| Superior sagittal sinus thrombosis | 24.85 | 19.22 | 7 | 5347 | 700 | 50599070 |
| Rectal haemorrhage | 24.44 | 19.22 | 25 | 5329 | 38533 | 50561237 |
| Vaginal ulceration | 24.24 | 19.22 | 6 | 5348 | 364 | 50599406 |
| Haemorrhage | 24.12 | 19.22 | 29 | 5325 | 53412 | 50546358 |
| Hot flush | 23.34 | 19.22 | 26 | 5328 | 44143 | 50555627 |
| Injury | 22.82 | 19.22 | 27 | 5327 | 48898 | 50550872 |
| Lip exfoliation | 22.29 | 19.22 | 6 | 5348 | 507 | 50599263 |
| Migraine | 21.93 | 19.22 | 33 | 5321 | 75247 | 50524523 |
| Melaena | 21.89 | 19.22 | 20 | 5334 | 26844 | 50572926 |
| Pruritus genital | 21.11 | 19.22 | 6 | 5348 | 620 | 50599150 |
| Dilatation intrahepatic duct acquired | 20.93 | 19.22 | 6 | 5348 | 639 | 50599131 |
| Transfusion | 19.97 | 19.22 | 14 | 5340 | 12891 | 50586879 |
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
| 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 |
|---|---|---|---|---|---|---|
| Vaginal haemorrhage | 132.44 | 20.58 | 49 | 4106 | 19295 | 64475282 |
| Hepatic adenoma | 92.26 | 20.58 | 16 | 4139 | 271 | 64494306 |
| Heavy menstrual bleeding | 45.76 | 20.58 | 20 | 4135 | 12057 | 64482520 |
| Purpura | 44.85 | 20.58 | 22 | 4133 | 17224 | 64477353 |
| Pelvic pain | 44.39 | 20.58 | 19 | 4136 | 10891 | 64483686 |
| Exposure to allergen | 43.59 | 20.58 | 8 | 4147 | 189 | 64494388 |
| Pregnancy on oral contraceptive | 43.11 | 20.58 | 10 | 4145 | 761 | 64493816 |
| Uterine perforation | 37.08 | 20.58 | 14 | 4141 | 5806 | 64488771 |
| Ovarian atrophy | 35.53 | 20.58 | 6 | 4149 | 86 | 64494491 |
| Intermenstrual bleeding | 35.10 | 20.58 | 13 | 4142 | 5112 | 64489465 |
| Endometriosis | 34.44 | 20.58 | 11 | 4144 | 2781 | 64491796 |
| Rash erythematous | 30.11 | 20.58 | 25 | 4130 | 48608 | 64445969 |
| Vaginal ulceration | 29.79 | 20.58 | 6 | 4149 | 234 | 64494343 |
| Genital burning sensation | 28.82 | 20.58 | 6 | 4149 | 276 | 64494301 |
| Drug-induced liver injury | 28.48 | 20.58 | 24 | 4131 | 47619 | 64446958 |
| Rash maculo-papular | 26.70 | 20.58 | 23 | 4132 | 47003 | 64447574 |
| Superior sagittal sinus thrombosis | 26.06 | 20.58 | 7 | 4148 | 969 | 64493608 |
| Cerebral venous sinus thrombosis | 25.76 | 20.58 | 8 | 4147 | 1847 | 64492730 |
| Injury | 25.14 | 20.58 | 24 | 4131 | 55968 | 64438609 |
| Ovarian failure | 24.89 | 20.58 | 6 | 4149 | 539 | 64494038 |
| Lip exfoliation | 24.71 | 20.58 | 6 | 4149 | 555 | 64494022 |
| Migraine | 24.67 | 20.58 | 25 | 4130 | 62652 | 64431925 |
| Maternal exposure during pregnancy | 23.66 | 20.58 | 30 | 4125 | 95854 | 64398723 |
| Dilatation intrahepatic duct acquired | 23.45 | 20.58 | 6 | 4149 | 688 | 64493889 |
| Rectal haemorrhage | 23.14 | 20.58 | 24 | 4131 | 61793 | 64432784 |
| Aplastic anaemia | 22.68 | 20.58 | 13 | 4142 | 13907 | 64480670 |
| Transfusion | 22.06 | 20.58 | 14 | 4141 | 17980 | 64476597 |
| Pruritus genital | 21.09 | 20.58 | 6 | 4149 | 1026 | 64493551 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| 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 | 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 | 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 |
| ATC | H01CC54 | SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES HYPOTHALAMIC HORMONES Anti-gonadotropin-releasing hormones |
| FDA CS | M0447349 | Progesterone Congeners |
| FDA EPC | N0000175602 | Progestin |
| FDA Chemical/Ingredient | N0000011301 | Progesterone Congeners |
| 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 |
| CHEBI has role | CHEBI:49326 | synthetic oral contraceptives |
| CHEBI has role | CHEBI:59826 | progestins |
Drug Use | Suggest Off label Use Form| |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 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
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 | |||
| Glucocorticoid receptor | Nuclear hormone receptor | Ki | 6.71 | DRUG MATRIX | |||||
| Estrogen receptor | Nuclear hormone receptor | Ki | 6.64 | DRUG MATRIX | |||||
| Androgen receptor | Nuclear hormone receptor | IC50 | 7.12 | WOMBAT-PK | |||||
| Sex hormone-binding globulin | Secreted | Kd | 7.97 | CHEMBL | |||||
| Sodium-dependent serotonin transporter | Transporter | Ki | 5.62 | DRUG MATRIX | |||||
| Androgen receptor | Transcription factor | IC50 | 6.92 | CHEMBL | |||||
| Progesterone receptor | Transcription factor | Ki | 8.91 | DRUG MATRIX | |||||
| Estrogen receptor | Transcription factor | Kd | 9.20 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4018496 | VUID |
| N0000146818 | NUI |
| D00182 | KEGG_DRUG |
| 4018496 | VANDF |
| C0028356 | UMLSCUI |
| CHEBI:7627 | CHEBI |
| NDR | PDB_CHEM_ID |
| CHEMBL1162 | ChEMBL_ID |
| DB00717 | DRUGBANK_ID |
| 2880 | IUPHAR_LIGAND_ID |
| T18F433X4S | UNII |
| 6230 | PUBCHEM_CID |
| 7514 | RXNORM |
| 182290 | MMSL |
| 5187 | MMSL |
| d00555 | MMSL |
| 001298 | NDDF |
| 001326 | NDDF |
| 126102009 | SNOMEDCT_US |
| 63758001 | SNOMEDCT_US |
| D009640 | MESH_DESCRIPTOR_UI |
| 687 | INN_ID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Norethindrone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-7272 | TABLET | 0.35 mg | ORAL | ANDA | 14 sections |
| Norethindrone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-7272 | TABLET | 0.35 mg | ORAL | ANDA | 14 sections |
| NORETHINDRONE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-7292 | TABLET | 0.35 mg | ORAL | ANDA | 14 sections |
| Nortrel21 Day | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0555-9009 | TABLET | 1 mg | ORAL | ANDA | 21 sections |
| LYZA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50102-100 | TABLET | 0.35 mg | ORAL | ANDA | 13 sections |
| Tulana | Human Prescription Drug Label | 1 | 50102-200 | TABLET | 0.35 mg | ORAL | ANDA | 14 sections |
| Lyleq | Human Prescription Drug Label | 1 | 50102-300 | TABLET | 0.35 mg | ORAL | ANDA | 14 sections |
| Ortho Micronor | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50458-194 | TABLET | 0.35 mg | ORAL | NDA | 24 sections |
| NORLYROC | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51660-127 | TABLET, FILM COATED | 0.35 mg | ORAL | ANDA | 12 sections |
| CAMILA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51862-884 | TABLET | 0.35 mg | ORAL | ANDA | 25 sections |
| ERRIN | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51862-886 | TABLET | 0.35 mg | ORAL | ANDA | 26 sections |
| ERRIN | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51862-886 | TABLET | 0.35 mg | ORAL | ANDA | 26 sections |
| Nora BE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52544-629 | TABLET | 0.35 mg | ORAL | NDA authorized generic | 19 sections |
| Jolivette | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52544-892 | TABLET | 0.35 mg | ORAL | NDA | 27 sections |
| Lyleq | Human Prescription Drug Label | 1 | 53002-1793 | TABLET | 0.35 mg | ORAL | ANDA | 14 sections |
| Tulana | Human Prescription Drug Label | 1 | 53002-2687 | TABLET | 0.35 mg | ORAL | ANDA | 14 sections |
| MICRONOR | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-4369 | TABLET | 0.35 mg | ORAL | NDA | 14 sections |
| Camila | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-4814 | TABLET | 0.35 mg | ORAL | ANDA | 15 sections |
| NORETHINDRONE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 57297-876 | TABLET | 0.35 mg | ORAL | ANDA | 13 sections |
| Jencycla | HUMAN PRESCRIPTION DRUG LABEL | 1 | 57297-877 | TABLET | 0.35 mg | ORAL | ANDA | 14 sections |
| Norethindrone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63187-748 | TABLET | 0.35 mg | ORAL | ANDA | 24 sections |
| Incassia | Human Prescription Drug Label | 1 | 65862-925 | TABLET | 0.35 mg | ORAL | ANDA | 14 sections |
| AMABELZ | HUMAN PRESCRIPTION DRUG LABEL | 2 | 68180-829 | TABLET | 0.10 mg | ORAL | ANDA | 30 sections |
| AMABELZ | HUMAN PRESCRIPTION DRUG LABEL | 2 | 68180-829 | TABLET | 0.10 mg | ORAL | ANDA | 30 sections |
| AMABELZ | HUMAN PRESCRIPTION DRUG LABEL | 2 | 68180-830 | TABLET | 0.50 mg | ORAL | ANDA | 30 sections |
| AMABELZ | HUMAN PRESCRIPTION DRUG LABEL | 2 | 68180-830 | TABLET | 0.50 mg | ORAL | ANDA | 30 sections |
| NORETHINDRONE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68180-876 | TABLET | 0.35 mg | ORAL | ANDA | 13 sections |
| NORETHINDRONE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68180-876 | TABLET | 0.35 mg | ORAL | ANDA | 13 sections |
| Jencycla | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68180-877 | TABLET | 0.35 mg | ORAL | ANDA | 14 sections |
| Jencycla | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68180-877 | TABLET | 0.35 mg | ORAL | ANDA | 14 sections |