desogestrel 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| steroids, progestogens | 818 | 54024-22-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents (ORAL CONTRACEPTIVES, COMBINED).
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.32 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.01 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 5 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 10, 1992 | FDA | ORGANON USA INC |
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 |
|---|---|---|---|---|---|---|
| Pregnancy on oral contraceptive | 72.79 | 19.90 | 17 | 4579 | 941 | 50599587 |
| Hepatocellular injury | 51.33 | 19.90 | 31 | 4565 | 25916 | 50574612 |
| Lip swelling | 39.97 | 19.90 | 26 | 4570 | 24710 | 50575818 |
| Essential tremor | 33.49 | 19.90 | 9 | 4587 | 882 | 50599646 |
| Folliculitis | 31.31 | 19.90 | 27 | 4569 | 39198 | 50561330 |
| Pruritus | 31.19 | 19.90 | 75 | 4521 | 283493 | 50317035 |
| Irritable bowel syndrome | 30.53 | 19.90 | 30 | 4566 | 51411 | 50549117 |
| Maculopathy | 30.40 | 19.90 | 10 | 4586 | 1964 | 50598564 |
| Polymenorrhagia | 30.03 | 19.90 | 5 | 4591 | 45 | 50600483 |
| Blister | 28.65 | 19.90 | 37 | 4559 | 85381 | 50515147 |
| Lower respiratory tract infection | 27.00 | 19.90 | 38 | 4558 | 95163 | 50505365 |
| Reversible cerebral vasoconstriction syndrome | 25.81 | 19.90 | 9 | 4587 | 2110 | 50598418 |
| Cell death | 25.42 | 19.90 | 9 | 4587 | 2206 | 50598322 |
| Gastrointestinal disorder | 24.29 | 19.90 | 36 | 4560 | 94420 | 50506108 |
| Peripheral swelling | 24.27 | 19.90 | 56 | 4540 | 205880 | 50394648 |
| Rash | 23.60 | 19.90 | 90 | 4506 | 437381 | 50163147 |
| Swollen tongue | 23.44 | 19.90 | 20 | 4576 | 28610 | 50571918 |
| Drug interaction | 23.21 | 19.90 | 54 | 4542 | 199567 | 50400961 |
| Swelling face | 22.88 | 19.90 | 26 | 4570 | 52569 | 50547959 |
| Nasal mucosal erosion | 21.56 | 19.90 | 4 | 4592 | 70 | 50600458 |
| Meningioma | 21.54 | 19.90 | 9 | 4587 | 3440 | 50597088 |
| Impaired healing | 21.50 | 19.90 | 29 | 4567 | 69757 | 50530771 |
| Muscle injury | 20.82 | 19.90 | 21 | 4575 | 37090 | 50563438 |
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 |
|---|---|---|---|---|---|---|
| Pregnancy on oral contraceptive | 77.10 | 23.38 | 16 | 3981 | 755 | 64493980 |
| Hepatocellular injury | 46.40 | 23.38 | 31 | 3966 | 45204 | 64449531 |
| Lip swelling | 43.04 | 23.38 | 26 | 3971 | 31881 | 64462854 |
| Essential tremor | 33.41 | 23.38 | 9 | 3988 | 1310 | 64493425 |
| Polymenorrhagia | 32.04 | 23.38 | 5 | 3992 | 44 | 64494691 |
| Maculopathy | 31.86 | 23.38 | 10 | 3987 | 2486 | 64492249 |
| Pruritus | 29.75 | 23.38 | 62 | 3935 | 312338 | 64182397 |
| Rash | 28.47 | 23.38 | 77 | 3920 | 458472 | 64036263 |
| Reversible cerebral vasoconstriction syndrome | 28.30 | 23.38 | 9 | 3988 | 2333 | 64492402 |
| Swelling face | 26.71 | 23.38 | 25 | 3972 | 59141 | 64435594 |
| Irritable bowel syndrome | 25.48 | 23.38 | 20 | 3977 | 37349 | 64457386 |
| Blister | 25.22 | 23.38 | 28 | 3969 | 80939 | 64413796 |
| Swollen tongue | 24.46 | 23.38 | 19 | 3978 | 34935 | 64459800 |
| Cell death | 23.47 | 23.38 | 9 | 3988 | 4045 | 64490690 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | G03AA09 | 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 | G03AB05 | 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 | G03AC09 | GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE Progestogens |
| ATC | G03FB10 | 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 CS | M0447349 | Progesterone Congeners |
| FDA EPC | N0000175602 | Progestin |
| CHEBI has role | CHEBI:49323 | contraceptive drugs |
| CHEBI has role | CHEBI:49326 | synthetic oral contraceptives |
| CHEBI has role | CHEBI:59826 | progestins |
| 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 | D006728 | Hormones |
| MeSH PA | D011372 | Progestins |
| MeSH PA | D012102 | Reproductive Control Agents |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Contraception | indication | 13197004 | |
| Amenorrhea | off-label use | 14302001 | DOID:13938 |
| Female hypogonadism syndrome | off-label use | 16041008 | |
| Polycystic ovaries | off-label use | 69878008 | |
| Dysmenorrhea | off-label use | 266599000 | |
| Abnormal uterine bleeding unrelated to menstrual cycle | off-label use | 312984006 | |
| Menorrhagia | off-label use | 386692008 | |
| 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 | |
| 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 | |
| Malignant neoplasm of liver | contraindication | 93870000 | DOID:3571 |
| Uterine leiomyoma | contraindication | 95315005 | DOID:13223 |
| Deep venous thrombosis | contraindication | 128053003 | |
| Endometriosis | contraindication | 129103003 | |
| 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 | |
| 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
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 13.93 | acidic |
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 | WOMBAT-PK | CHEMBL | |||||
| Sex hormone-binding globulin | Secreted | Kd | 6.60 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4020568 | VUID |
| N0000148270 | NUI |
| D02367 | KEGG_DRUG |
| 22656 | RXNORM |
| 4020568 | VANDF |
| C0057558 | UMLSCUI |
| CHEBI:4453 | CHEBI |
| CHEMBL1533 | ChEMBL_ID |
| DB00304 | DRUGBANK_ID |
| D017135 | MESH_DESCRIPTOR_UI |
| 40973 | PUBCHEM_CID |
| 7065 | IUPHAR_LIGAND_ID |
| 4384 | INN_ID |
| 81K9V7M3A3 | UNII |
| 4549 | MMSL |
| d03780 | MMSL |
| 003956 | NDDF |
| 116074007 | SNOMEDCT_US |
| 126108008 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| MERCILON | HUMAN OTC DRUG LABEL | 2 | 72689-0020 | TABLET | 0.15 mg | ORAL | unapproved drug other | 7 sections |