drospirenone Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| aldosterone antagonists, spironolactone derivates | 968 | 67392-87-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
a progestational compound with antimineralocorticoid and antiandrogenic activity; structure given in first source. It is used in combination with estetrol (nextstellis) as oral contraceptive.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0.10 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.12 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 76 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| May 11, 2001 | FDA |
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 |
|---|---|---|---|---|---|---|
| Pulmonary embolism | 740.83 | 19.96 | 393 | 9806 | 108192 | 46567671 |
| Injury | 697.61 | 19.96 | 286 | 9913 | 43741 | 46632122 |
| Deep vein thrombosis | 630.32 | 19.96 | 319 | 9880 | 79454 | 46596409 |
| Embolism arterial | 415.52 | 19.96 | 86 | 10113 | 1077 | 46674786 |
| Emotional distress | 364.95 | 19.96 | 163 | 10036 | 30544 | 46645319 |
| Cerebrovascular accident | 192.02 | 19.96 | 166 | 10033 | 100873 | 46574990 |
| Pregnancy on oral contraceptive | 167.14 | 19.96 | 42 | 10157 | 1292 | 46674571 |
| Anxiety | 144.96 | 19.96 | 188 | 10011 | 181769 | 46494094 |
| Pelvic venous thrombosis | 131.33 | 19.96 | 36 | 10163 | 1561 | 46674302 |
| Pain | 129.89 | 19.96 | 306 | 9893 | 476642 | 46199221 |
| Thrombosis | 118.41 | 19.96 | 98 | 10101 | 55971 | 46619892 |
| Anhedonia | 110.36 | 19.96 | 51 | 10148 | 10284 | 46665579 |
| Cerebral venous sinus thrombosis | 104.41 | 19.96 | 31 | 10168 | 1794 | 46674069 |
| Thrombophlebitis superficial | 98.01 | 19.96 | 38 | 10161 | 4965 | 46670898 |
| General physical health deterioration | 89.46 | 19.96 | 118 | 10081 | 115651 | 46560212 |
| Transverse sinus thrombosis | 83.15 | 19.96 | 21 | 10178 | 659 | 46675204 |
| Superior sagittal sinus thrombosis | 55.35 | 19.96 | 16 | 10183 | 842 | 46675021 |
| Death | 55.11 | 19.96 | 5 | 10194 | 335543 | 46340320 |
| Cerebral infarction | 51.69 | 19.96 | 42 | 10157 | 23324 | 46652539 |
| Fear of disease | 51.54 | 19.96 | 16 | 10183 | 1076 | 46674787 |
| Withdrawal bleed | 49.06 | 19.96 | 10 | 10189 | 115 | 46675748 |
| Vena cava thrombosis | 47.88 | 19.96 | 18 | 10181 | 2161 | 46673702 |
| Acne | 44.47 | 19.96 | 36 | 10163 | 19883 | 46655980 |
| Abnormal withdrawal bleeding | 43.30 | 19.96 | 10 | 10189 | 213 | 46675650 |
| Pulmonary infarction | 40.92 | 19.96 | 17 | 10182 | 2654 | 46673209 |
| Hemiparesis | 38.04 | 19.96 | 33 | 10166 | 20036 | 46655827 |
| Cerebral thrombosis | 37.17 | 19.96 | 14 | 10185 | 1689 | 46674174 |
| Hypoaesthesia | 33.89 | 19.96 | 78 | 10121 | 118791 | 46557072 |
| Ischaemic stroke | 32.71 | 19.96 | 28 | 10171 | 16694 | 46659169 |
| Cerebral venous thrombosis | 30.78 | 19.96 | 13 | 10186 | 2114 | 46673749 |
| Fall | 30.53 | 19.96 | 17 | 10182 | 329080 | 46346783 |
| Mesenteric vein thrombosis | 30.31 | 19.96 | 10 | 10189 | 818 | 46675045 |
| Rheumatoid arthritis | 29.53 | 19.96 | 8 | 10191 | 240207 | 46435656 |
| Polyarteritis nodosa | 29.28 | 19.96 | 8 | 10191 | 342 | 46675521 |
| Menstruation irregular | 29.05 | 19.96 | 18 | 10181 | 6521 | 46669342 |
| Genital haemorrhage | 28.98 | 19.96 | 18 | 10181 | 6548 | 46669315 |
| Ectopic pregnancy under hormonal contraception | 28.54 | 19.96 | 5 | 10194 | 23 | 46675840 |
| Migraine | 28.23 | 19.96 | 53 | 10146 | 69973 | 46605890 |
| Psychological trauma | 27.46 | 19.96 | 10 | 10189 | 1098 | 46674765 |
| Mood swings | 27.37 | 19.96 | 25 | 10174 | 16227 | 46659636 |
| Hemianaesthesia | 27.26 | 19.96 | 8 | 10191 | 444 | 46675419 |
| Embolic stroke | 26.96 | 19.96 | 14 | 10185 | 3625 | 46672238 |
| Headache | 26.66 | 19.96 | 187 | 10012 | 478165 | 46197698 |
| Cerebral artery occlusion | 25.10 | 19.96 | 9 | 10190 | 945 | 46674918 |
| Speech disorder | 23.55 | 19.96 | 34 | 10165 | 36133 | 46639730 |
| Product substitution issue | 23.15 | 19.96 | 22 | 10177 | 15009 | 46660854 |
| Peripheral artery thrombosis | 22.71 | 19.96 | 10 | 10189 | 1799 | 46674064 |
| Libido decreased | 22.15 | 19.96 | 11 | 10188 | 2594 | 46673269 |
| Drug hypersensitivity | 22.01 | 19.96 | 13 | 10186 | 243812 | 46432051 |
| Aphasia | 21.82 | 19.96 | 29 | 10170 | 28538 | 46647325 |
| Depression | 21.78 | 19.96 | 84 | 10115 | 170020 | 46505843 |
| Product use in unapproved indication | 21.19 | 19.96 | 55 | 10144 | 90218 | 46585645 |
| Venous thrombosis limb | 21.17 | 19.96 | 11 | 10188 | 2852 | 46673011 |
| Vaginal haemorrhage | 21.12 | 19.96 | 27 | 10172 | 25577 | 46650286 |
| Hemiplegia | 20.91 | 19.96 | 15 | 10184 | 6923 | 46668940 |
| Acute kidney injury | 20.70 | 19.96 | 13 | 10186 | 235842 | 46440021 |
| Porphyria non-acute | 20.48 | 19.96 | 6 | 10193 | 331 | 46675532 |
| Transient ischaemic attack | 20.13 | 19.96 | 31 | 10168 | 34872 | 46640991 |
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 | G03AA12 | 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 | G03AA18 | 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 | G03AC10 | GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE Progestogens |
| ATC | G03FA17 | GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM PROGESTOGENS AND ESTROGENS IN COMBINATION Progestogens and estrogens, fixed combinations |
| FDA CS | M0447349 | Progesterone Congeners |
| FDA EPC | N0000175602 | Progestin |
| MeSH PA | D004232 | Diuretics |
| MeSH PA | D006727 | Hormone Antagonists |
| MeSH PA | D000451 | Mineralocorticoid Receptor Antagonists |
| MeSH PA | D045283 | Natriuretic Agents |
| CHEBI has role | CHEBI:49323 | contraceptive agent |
| CHEBI has role | CHEBI:59826 | progestins |
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Premenstrual dysphoric disorder | indication | 596004 | |
| Contraception | indication | 13197004 | |
| Atrophic vaginitis | indication | 52441000 | |
| Acne vulgaris | indication | 88616000 | |
| Menopausal flushing | indication | 198436008 | |
| Atrophic vulva | indication | 248861000 | DOID:14275 |
| Polycystic ovaries | off-label use | 69878008 | |
| Hyperlipoproteinemia | contraindication | 3744001 | DOID:1168 |
| Hypocalcemia | contraindication | 5291005 | |
| Hypercholesterolemia | contraindication | 13644009 | |
| Hyperkalemia | contraindication | 14140009 | |
| Myocardial infarction | contraindication | 22298006 | DOID:5844 |
| Diplopia | contraindication | 24982008 | |
| Retinal hemorrhage | contraindication | 28998008 | |
| 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 |
| Acute nephropathy | contraindication | 58574008 | |
| Thrombophlebitis | contraindication | 64156001 | DOID:3875 |
| Intermenstrual bleeding - irregular | contraindication | 64996003 | |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Epilepsy | contraindication | 84757009 | DOID:1826 |
| Breast lump | contraindication | 89164003 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Uterine leiomyoma | contraindication | 95315005 | DOID:13223 |
| Deep venous thrombosis | contraindication | 128053003 | |
| Seizure disorder | contraindication | 128613002 | |
| Endometriosis | contraindication | 129103003 | |
| Bed-ridden | contraindication | 160685001 | |
| Mammography abnormal | contraindication | 168750009 | |
| 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 |
| Endometrial carcinoma | contraindication | 254878006 | DOID:2871 |
| Chorea | contraindication | 271700006 | |
| Pregnancy, function | contraindication | 289908002 | |
| Hypertriglyceridemia | contraindication | 302870006 | |
| Functional visual loss | contraindication | 313165001 | |
| Malignant tumor of ovary | contraindication | 363443007 | DOID:2394 |
| Thromboembolic disorder | contraindication | 371039008 | |
| Adrenal cortical hypofunction | contraindication | 386584007 | DOID:10493 |
| 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 |
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)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 4MG | SLYND | EXELTIS USA INC | N211367 | May 23, 2019 | RX | TABLET | ORAL | May 23, 2022 | NEW PRODUCT |
| 3MG;14.2MG | NEXTSTELLIS | MAYNE PHARMA | N214154 | April 15, 2021 | RX | TABLET | ORAL | April 15, 2026 | NEW CHEMICAL ENTITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Progesterone receptor | Nuclear hormone receptor | AGONIST | EC50 | 10.50 | WOMBAT-PK | CHEMBL | |||
| Mineralocorticoid receptor | Nuclear hormone receptor | ANTAGONIST | IC50 | 10.50 | WOMBAT-PK | CHEMBL | |||
| Androgen receptor | Nuclear hormone receptor | IC50 | 8.50 | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| 4021271 | VUID |
| N0000179010 | NUI |
| D03917 | KEGG_DRUG |
| 4021271 | VANDF |
| C0043822 | UMLSCUI |
| CHEBI:50838 | CHEBI |
| CHEMBL1509 | ChEMBL_ID |
| DB01395 | DRUGBANK_ID |
| C035144 | MESH_SUPPLEMENTAL_RECORD_UI |
| 68873 | PUBCHEM_CID |
| 2874 | IUPHAR_LIGAND_ID |
| 6519 | INN_ID |
| N295J34A25 | UNII |
| 11636 | RXNORM |
| 16073 | MMSL |
| d04759 | MMSL |
| 009133 | NDDF |
| 395275003 | SNOMEDCT_US |
| 410919000 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| SLYND | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0642-7470 | TABLET, FILM COATED | 4 mg | ORAL | NDA | 30 sections |
| Angeliq | HUMAN PRESCRIPTION DRUG LABEL | 2 | 50419-482 | TABLET, FILM COATED | 0.25 mg | ORAL | NDA | 29 sections |
| Angeliq | HUMAN PRESCRIPTION DRUG LABEL | 2 | 50419-483 | TABLET, FILM COATED | 0.50 mg | ORAL | NDA | 29 sections |
| Angeliq | HUMAN PRESCRIPTION DRUG LABEL | 2 | 54868-6184 | TABLET, FILM COATED | 0.50 mg | ORAL | NDA | 24 sections |