General Information of Drug (ID: DM1DP7T)

Drug Name
Levonorgestrel
Synonyms
norgestrel; 797-63-7; D-Norgestrel; (-)-Norgestrel; Microval; Levonova; Postinor; Mirena; Ovrette; Neogest; Jadelle; Plan B; NORPLANT; Norplant 2; Microlution; Follistrel; Trivora; Monovar; Triciclor; Microgyn; Ovranette; Triagynon; Microlut; Nordet; Trigoa; 18-Methylnorethisterone; Levonorgestrelum; Microgynon CD; Microgest ED; Norplant II; Ovral-Lo; Logynon ED; Levlen ED; Trinordiol 28; Trinordiol 21; Microgynon 28; Microgynon 21; d(-)-Norgestrel; Neogynon 21; Monofeme 28; Nordette 28; Minivlar 30; Stediril 30; Nordette 21; Trifeme; Capronor; DNorgestrel; Levlen; Levonelle; Methylnorethindrone; Microluton; NorLevo; Norgeston; Norgestrel; Norgestrelum; Preven; Tetragynon; LD norgestrel [French]; Ld norgestrel; Levonorgestrel implants; Norgestrel [Progestins]; Norplant System in Plastic Container; Triquilar ED; Microgynon 30 ED; SH 70850; SH 850; Trifeme 28; Triphasil 21; Triphasil 28; Wy 3707; Alpha-Norgestrel; Component of Lo/ovral; Dl-Norgestrel; FH 122-A; LO/Ovral; Levonorgestrelum [INN-Latin]; Levora-21; Levora-28; Mirena (TN); Norgestrelum [INN-Latin]; Norplant (TN); Norplant-2; Ovoplex 30-150; Ovrette (TN); Postinor-2; Rigevidon 21+7; SOH-075; Tri-Levlen 21; Wy-3707; Wy-5104; E-Gen-C; Levonorgestrel [USAN:INN:BAN]; D(-)-Norgestrel; Levonorgestrel (JAN/USP/INN); Norgestrel (JP15/USP/INN); Norgestrel [USAN:BAN:INN:JAN]; Norgestrel [USAN:INN:BAN:JAN]; D-(-)-Norgestrel; Levonelle, D-Norgestrel, Levonova, Levonorgestrel; Norgestrel-(-)-D; Dl-13-beta-Ethyl-17-alpha-ethynyl-19-nortestosterone; 13-BETA-ETHYL-17-ALPHA-ETHYNYL-17-BETA-HYDROXYGON-4-EN-3-ONE; 13-Ehyl-17alpha-ethynyl-17-hydroxygon-4-en-3-one; 13-Ethyl-17-alpha-ethynyl-17-beta-hydroxy-4-gonen-3-one; 13-Ethyl-17-alpha-ethynylgon-4-en-17-beta-ol-3-one; 13-Ethyl-17alpha-ethynylgon-4-en-17beta-ol-3-one; 13-beta-Ethyl-17alpha-ethynyl-17beta-hydroxygon-4-en-3-one; 13beta-Ethyl-17alpha-ethynyl-17beta-hydroxygon-4-en-3-one; 17-Ethynyl-18-methyl-19-nortestosterone; 17-alpha-Ethynyl-13-ethyl-19-nortestosterone; 17alpha-Ethynyl-13-ethyl-19-nortestosterone; 17alpha-Ethynyl-13beta-ethyl-3-oxo-4-estren-17beta-ol; 17alpha-Ethynyl-17-hydroxy-18-methylestr-4-en-3-one; 17alpha-Ethynyl-18-homo-19-nor-testosterone; 17alpha-Ethynyl-18-homo-19-nortestosterone; 17alpha-ethynyl-17beta-hydroxy-18a-homoestr-4-en-3-one; 18,19-Dinor-4-pregnen-20-yn-3-one; 18-Methyl-17-alpha-ethynyl-19-nortestosterone; 72-HOURS
Indication
Disease Entry ICD 11 Status REF
Atypical endometrial hyperplasia N.A. Approved [1]
Contraception QA21 Approved [2]
Hot flushes GA30 Approved [1]
Menorrhagia GA20.50 Approved [1]
Therapeutic Class
Contraceptive Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 312.4
Logarithm of the Partition Coefficient (xlogp) 3.3
Rotatable Bond Count (rotbonds) 2
Hydrogen Bond Donor Count (hbonddonor) 1
Hydrogen Bond Acceptor Count (hbondacc) 2
ADMET Property
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 2-3 days [3]
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 4: low solubility and low permeability [4]
Bioavailability
94% of drug becomes completely available to its intended biological destination(s) [5]
Clearance
The clearance of drug is 4.8 L/h in healthy female volunteers [6]
Elimination
Approximately 45% of an oral levonorgestrel dose and its conjugated or sulfate metabolites are found to be excreted in the urine [7]
Half-life
The concentration or amount of drug in body reduced by one-half in 20 - 60 hours [8]
Metabolism
The drug is metabolized via plasma [9]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 0.03245 micromolar/kg/day [10]
Unbound Fraction
The unbound fraction of drug in plasma is 0.025% [11]
Vd
The volume of distribution (Vd) of drug is 162.2 L [6]
Water Solubility
The ability of drug to dissolve in water is measured as 0.0014 mg/mL [4]
Chemical Identifiers
Formula
C21H28O2
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
Canonical SMILES
CC[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@]2(C#C)O)CCC4=CC(=O)CC[C@H]34
InChI
InChI=1S/C21H28O2/c1-3-20-11-9-17-16-8-6-15(22)13-14(16)5-7-18(17)19(20)10-12-21(20,23)4-2/h2,13,16-19,23H,3,5-12H2,1H3/t16-,17+,18+,19-,20-,21-/m0/s1
InChIKey
WWYNJERNGUHSAO-XUDSTZEESA-N
Cross-matching ID
PubChem CID
13109
ChEBI ID
CHEBI:6443
CAS Number
797-63-7
DrugBank ID
DB00367
TTD ID
D0BA9U
VARIDT ID
DR01186
ACDINA ID
D00363
Combinatorial Drugs (CBD) Click to Jump to the Detailed CBD Information of This Drug
Repurposed Drugs (RPD) Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Progesterone receptor (PGR) TTUV8G9 PRGR_HUMAN Binder [12]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Aldo-keto reductase family 1 member C3 (AKR1C3) OTU2SXBA AK1C3_HUMAN Gene/Protein Processing [13]
Apoptosis regulator Bcl-2 (BCL2) OT9DVHC0 BCL2_HUMAN Gene/Protein Processing [14]
ATP-dependent translocase ABCB1 (ABCB1) OTEJROBO MDR1_HUMAN Gene/Protein Processing [15]
Low-density lipoprotein receptor (LDLR) OTH559LU LDLR_HUMAN Gene/Protein Processing [16]
Lutropin subunit beta (LHB) OT5GBOVJ LSHB_HUMAN Protein Interaction/Cellular Processes [17]
Proliferation marker protein Ki-67 (MKI67) OTA8N1QI KI67_HUMAN Gene/Protein Processing [14]
Prostate-specific antigen (KLK3) OTFGSBFJ KLK3_HUMAN Gene/Protein Processing [18]
Sex hormone-binding globulin (SHBG) OTPWU5IW SHBG_HUMAN Protein Interaction/Cellular Processes [19]
Tumor necrosis factor ligand superfamily member 11 (TNFSF11) OTJEPKEQ TNF11_HUMAN Gene/Protein Processing [20]
Tumor necrosis factor receptor superfamily member 11B (TNFRSF11B) OTQ4W7MT TR11B_HUMAN Gene/Protein Processing [20]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Atypical endometrial hyperplasia
ICD Disease Classification
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Progesterone receptor (PGR) DTT PGR 3.26E-38 -3.79 -2.5
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Levonorgestrel (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Metreleptin DM1NOEK Moderate Decreased metabolism of Levonorgestrel caused by Metreleptin mediated inhibition of CYP450 enzyme. Acute diabete complication [5A2Y] [21]
Pioglitazone DMKJ485 Minor Increased metabolism of Levonorgestrel caused by Pioglitazone mediated induction of CYP450 enzyme. Acute diabete complication [5A2Y] [22]
Ivosidenib DM8S6T7 Moderate Increased metabolism of Levonorgestrel caused by Ivosidenib mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [23]
Arn-509 DMT81LZ Moderate Increased metabolism of Levonorgestrel caused by Arn-509 mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [24]
Emapalumab DMZG5WL Moderate Altered metabolism of Levonorgestrel due to Emapalumab alters the formation of CYP450 enzymes. Adaptive immunity immunodeficiency [4A01] [25]
Mitotane DMU1GX0 Moderate Increased metabolism of Levonorgestrel caused by Mitotane mediated induction of CYP450 enzyme. Adrenal cancer [2D11] [24]
Siltuximab DMGEATB Moderate Altered metabolism of Levonorgestrel due to Siltuximab alters the formation of CYP450 enzymes. Anemia [3A00-3A9Z] [25]
Dronedarone DMA8FS5 Moderate Decreased metabolism of Levonorgestrel caused by Dronedarone mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [26]
Methylphenobarbital DMDSWAG Moderate Increased metabolism of Levonorgestrel caused by Methylphenobarbital mediated induction of CYP450 enzyme. Anxiety disorder [6B00-6B0Z] [27]
Voriconazole DMAOL2S Moderate Decreased metabolism of Levonorgestrel caused by Voriconazole mediated inhibition of CYP450 enzyme. Aspergillosis [1F20] [28]
Posaconazole DMUL5EW Moderate Decreased metabolism of Levonorgestrel caused by Posaconazole mediated inhibition of CYP450 enzyme. Aspergillosis [1F20] [28]
Aminophylline DML2NIB Moderate Decreased metabolism of Levonorgestrel caused by Aminophylline. Asthma [CA23] [29]
Clarithromycin DM4M1SG Moderate Decreased metabolism of Levonorgestrel caused by Clarithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [30]
Telithromycin DMZ4P3A Moderate Decreased metabolism of Levonorgestrel caused by Telithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [31]
Ag-221 DMS0ZBI Moderate Decreased metabolism of Levonorgestrel caused by Ag-221 mediated inhibition of CYP450 enzyme. BCR-ABL1-negative chronic myeloid leukaemia [2A41] [32]
Pexidartinib DMS2J0Z Major Increased metabolism of Levonorgestrel caused by Pexidartinib mediated induction of CYP450 enzyme. Bone/articular cartilage neoplasm [2F7B] [33]
Lapatinib DM3BH1Y Moderate Decreased metabolism of Levonorgestrel caused by Lapatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [34]
Atorvastatin DMF28YC Minor Decreased metabolism of Levonorgestrel caused by Atorvastatin mediated inhibition of CYP450 enzyme. Cardiovascular disease [BA00-BE2Z] [35]
Secobarbital DM14RF5 Moderate Increased metabolism of Levonorgestrel caused by Secobarbital mediated induction of CYP450 enzyme. Chronic insomnia [7A00] [24]
Phenylbutazone DMAYL0T Moderate Increased metabolism of Levonorgestrel caused by Phenylbutazone mediated induction of CYP450 enzyme. Chronic pain [MG30] [36]
Oxtriphylline DMLHSE3 Moderate Decreased metabolism of Levonorgestrel caused by Oxtriphylline. Cough [MD12] [29]
Lumacaftor DMCLWDJ Major Increased metabolism of Levonorgestrel caused by Lumacaftor mediated induction of CYP450 enzyme. Cystic fibrosis [CA25] [25]
Ivacaftor DMZC1HS Moderate Decreased metabolism of Levonorgestrel caused by Ivacaftor mediated inhibition of CYP450 enzyme. Cystic fibrosis [CA25] [37]
Ethanol DMDRQZU Minor Decreased metabolism of Levonorgestrel caused by Ethanol. Cystitis [GC00] [38]
MK-8228 DMOB58Q Moderate Decreased metabolism of Levonorgestrel caused by MK-8228 mediated inhibition of CYP450 enzyme. Cytomegaloviral disease [1D82] [30]
Aprepitant DM053KT Moderate Increased metabolism of Levonorgestrel caused by Aprepitant mediated induction of CYP450 enzyme. Depression [6A70-6A7Z] [36]
Nefazodone DM4ZS8M Moderate Decreased metabolism of Levonorgestrel caused by Nefazodone mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [39]
Selegiline DM6034S Moderate Decreased metabolism of Levonorgestrel caused by Selegiline mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [40]
Griseofulvin DMK54YG Major Increased metabolism of Levonorgestrel caused by Griseofulvin mediated induction of CYP450 enzyme. Dermatophytosis [1F28] [41]
Primidone DM0WX6I Major Increased metabolism of Levonorgestrel caused by Primidone mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [24]
Felbamate DM1V5ZS Major Increased metabolism of Levonorgestrel caused by Felbamate mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [24]
Oxcarbazepine DM5PU6O Major Increased metabolism of Levonorgestrel caused by Oxcarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [24]
Cenobamate DM8KLU9 Moderate Increased metabolism of Levonorgestrel caused by Cenobamate mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [24]
Stiripentol DMMSDOY Moderate Decreased metabolism of Levonorgestrel caused by Stiripentol mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [42]
Fosphenytoin DMOX3LB Major Increased metabolism of Levonorgestrel caused by Fosphenytoin mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [24]
Brivaracetam DMSEPK8 Minor Increased metabolism of Levonorgestrel caused by Brivaracetam mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [25]
Rufinamide DMWE60C Moderate Increased metabolism of Levonorgestrel caused by Rufinamide mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [30]
Phenobarbital DMXZOCG Major Increased metabolism of Levonorgestrel caused by Phenobarbital mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [24]
Carbamazepine DMZOLBI Major Increased metabolism of Levonorgestrel caused by Carbamazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [24]
Eslicarbazepine DMZREFQ Major Increased metabolism of Levonorgestrel caused by Eslicarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [24]
Tazemetostat DMWP1BH Moderate Increased metabolism of Levonorgestrel caused by Tazemetostat mediated induction of CYP450 enzyme. Follicular lymphoma [2A80] [43]
Miconazole DMPMYE8 Moderate Decreased metabolism of Levonorgestrel caused by Miconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [28]
Ketoconazole DMPZI3Q Moderate Decreased metabolism of Levonorgestrel caused by Ketoconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [28]
Sulfinpyrazone DMEV954 Moderate Increased metabolism of Levonorgestrel caused by Sulfinpyrazone mediated induction of CYP450 enzyme. Gout [FA25] [24]
Boceprevir DMBSHMF Major Increased metabolism of Levonorgestrel caused by Boceprevir mediated induction of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [36]
Telaprevir DMMRV29 Major Increased metabolism of Levonorgestrel caused by Telaprevir mediated induction of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [36]
Rifampin DMA8J1G Major Increased metabolism of Levonorgestrel caused by Rifampin mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [44]
Rifapentine DMCHV4I Major Increased metabolism of Levonorgestrel caused by Rifapentine mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [45]
Delavirdine DM3NF5G Minor Decreased metabolism of Levonorgestrel caused by Delavirdine mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [46]
Efavirenz DMC0GSJ Moderate Increased metabolism of Levonorgestrel caused by Efavirenz mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [25]
Saquinavir DMG814N Moderate Decreased metabolism of Levonorgestrel caused by Saquinavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [47]
Darunavir DMN3GCH Moderate Decreased metabolism of Levonorgestrel caused by Darunavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [48]
Atazanavir DMSYRBX Moderate Decreased metabolism of Levonorgestrel caused by Atazanavir mediated inhibition of UGT. Human immunodeficiency virus disease [1C60-1C62] [49]
BMS-201038 DMQTAGO Moderate Decreased metabolism of Levonorgestrel caused by BMS-201038 mediated inhibition of CYP450 enzyme. Hyper-lipoproteinaemia [5C80] [50]
Conivaptan DM1V329 Moderate Decreased metabolism of Levonorgestrel caused by Conivaptan mediated inhibition of CYP450 enzyme. Hypo-osmolality/hyponatraemia [5C72] [51]
Lesinurad DMUR64T Moderate Increased metabolism of Levonorgestrel caused by Lesinurad mediated induction of CYP450 enzyme. Inborn purine/pyrimidine/nucleotide metabolism error [5C55] [52]
Berotralstat DMWA2DZ Moderate Decreased metabolism of Levonorgestrel caused by Berotralstat mediated inhibition of CYP450 enzyme. Innate/adaptive immunodeficiency [4A00] [53]
Amobarbital DM0GQ8N Moderate Increased metabolism of Levonorgestrel caused by Amobarbital mediated induction of CYP450 enzyme. Insomnia [7A00-7A0Z] [24]
Linaclotide DM4EGV0 Moderate Altered absorption of Levonorgestrel caused by Linaclotide. Irritable bowel syndrome [DD91] [25]
R0-93877 DMM4U9G Moderate Altered absorption of Levonorgestrel caused by R0-93877. Irritable bowel syndrome [DD91] [30]
Miltefosine DMND304 Moderate Altered absorption of Levonorgestrel caused by Miltefosine. Leishmaniasis [1F54] [54]
Glycerol phenylbutyrate DMDGRQO Moderate Increased metabolism of Levonorgestrel caused by Glycerol phenylbutyrate mediated induction of CYP450 enzyme. Liver disease [DB90-DB9Z] [25]
Brigatinib DM7W94S Major Increased metabolism of Levonorgestrel caused by Brigatinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [55]
PF-06463922 DMKM7EW Moderate Increased metabolism of Levonorgestrel caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [24]
Selpercatinib DMZR15V Moderate Decreased metabolism of Levonorgestrel caused by Selpercatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [25]
Artemether DM48QOT Moderate Increased metabolism of Levonorgestrel caused by Artemether mediated induction of CYP450 enzyme. Malaria [1F40-1F45] [56]
Calaspargase pegol DMQZBXI Moderate Decreased metabolism of Levonorgestrel caused by Calaspargase pegol mediated hepatotoxicity. Malignant haematopoietic neoplasm [2B33] [30]
IPI-145 DMWA24P Moderate Decreased metabolism of Levonorgestrel caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [57]
Vemurafenib DM62UG5 Moderate Increased metabolism of Levonorgestrel caused by Vemurafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [24]
LGX818 DMNQXV8 Major Increased metabolism of Levonorgestrel caused by LGX818 mediated induction of CYP450 enzyme. Melanoma [2C30] [58]
Dabrafenib DMX6OE3 Major Increased metabolism of Levonorgestrel caused by Dabrafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [36]
Exjade DMHPRWG Moderate Increased metabolism of Levonorgestrel caused by Exjade mediated induction of CYP450 enzyme. Mineral absorption/transport disorder [5C64] [59]
Carfilzomib DM48K0X Major Additive thrombogenic effects by the combination of Levonorgestrel and Carfilzomib. Multiple myeloma [2A83] [25]
Rifabutin DM1YBHK Major Increased metabolism of Levonorgestrel caused by Rifabutin mediated induction of CYP450 enzyme. Mycobacterium infection [1B10-1B21] [45]
Fedratinib DM4ZBK6 Moderate Decreased metabolism of Levonorgestrel caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [25]
Nilotinib DM7HXWT Moderate Decreased metabolism of Levonorgestrel caused by Nilotinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [60]
Dasatinib DMJV2EK Moderate Decreased metabolism of Levonorgestrel caused by Dasatinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [61]
Modafinil DMYILBE Moderate Increased metabolism of Levonorgestrel caused by Modafinil mediated induction of CYP450 enzyme. Narcolepsy [7A20] [30]
E-2007 DMJDYNQ Moderate Increased metabolism of Levonorgestrel caused by E-2007 mediated induction of CYP450 enzyme. Neuropathy [8C0Z] [30]
Olaparib DM8QB1D Moderate Increased metabolism of Levonorgestrel caused by Olaparib mediated induction of CYP450 enzyme. Ovarian cancer [2C73] [25]
Rucaparib DM9PVX8 Moderate Decreased metabolism of Levonorgestrel caused by Rucaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [62]
Abametapir DM2RX0I Moderate Decreased metabolism of Levonorgestrel caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [63]
Lefamulin DME6G97 Moderate Decreased metabolism of Levonorgestrel caused by Lefamulin mediated inhibition of CYP450 enzyme. Pneumonia [CA40] [64]
Lonafarnib DMGM2Z6 Moderate Decreased metabolism of Levonorgestrel caused by Lonafarnib mediated inhibition of CYP450 enzyme. Premature ageing appearance [LD2B] [65]
Enzalutamide DMGL19D Moderate Increased metabolism of Levonorgestrel caused by Enzalutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [24]
Ustekinumab DMHTYK3 Moderate Altered metabolism of Levonorgestrel due to Ustekinumab alters the formation of CYP450 enzymes. Psoriasis [EA90] [25]
Ixekizumab DMXW92T Moderate Altered metabolism of Levonorgestrel due to Ixekizumab alters the formation of CYP450 enzymes. Psoriasis [EA90] [25]
Temsirolimus DMS104F Moderate Increased plasma concentrations of Levonorgestrel and Temsirolimus due to competitive inhibition of the same metabolic pathway. Renal cell carcinoma [2C90] [66]
Tocilizumab DM7J6OR Moderate Altered metabolism of Levonorgestrel due to Tocilizumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [25]
Canakinumab DM8HLO5 Moderate Altered metabolism of Levonorgestrel due to Canakinumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [25]
Rilonacept DMGLUQS Moderate Altered metabolism of Levonorgestrel due to Rilonacept alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [25]
Golimumab DMHZV7X Moderate Altered metabolism of Levonorgestrel due to Golimumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [25]
Nafcillin DMN9RPO Moderate Increased metabolism of Levonorgestrel caused by Nafcillin mediated induction of CYP450 enzyme. Rheumatoid arthritis [FA20] [24]
Sarilumab DMOGNXY Moderate Altered metabolism of Levonorgestrel due to Sarilumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [25]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Levonorgestrel caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [25]
Larotrectinib DM26CQR Moderate Decreased metabolism of Levonorgestrel caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [30]
Armodafinil DMGB035 Moderate Increased metabolism of Levonorgestrel caused by Armodafinil mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [30]
Pitolisant DM8RFNJ Moderate Increased metabolism of Levonorgestrel caused by Pitolisant mediated induction of CYP450 enzyme. Somnolence [MG42] [25]
Fostamatinib DM6AUHV Moderate Decreased metabolism of Levonorgestrel caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [67]
Tizanidine DMR2IQ4 Major Decreased metabolism of Levonorgestrel caused by Tizanidine mediated inhibition of CYP450 enzyme. Tonus and reflex abnormality [MB47] [68]
Sirolimus DMGW1ID Moderate Increased plasma concentrations of Levonorgestrel and Sirolimus due to competitive inhibition of the same metabolic pathway. Transplant rejection [NE84] [66]
Tacrolimus DMZ7XNQ Moderate Increased plasma concentrations of Levonorgestrel and Tacrolimus due to competitive inhibition of the same metabolic pathway. Transplant rejection [NE84] [66]
Elagolix DMB2C0E Moderate Increased metabolism of Levonorgestrel caused by Elagolix mediated induction of CYP450 enzyme. Uterine fibroid [2E86] [24]
⏷ Show the Full List of 103 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Sunset yellow FCF E00255 17730 Colorant
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Povidone E00667 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Talc E00520 16211421 Anticaking agent; Diluent; Glidant; lubricant
Vinylpyrrolidone E00668 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
⏷ Show the Full List of 7 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Levonorgestrel 1.5 mg tablet 1.5 mg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 Levonorgestrel FDA Label
2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2881).
3 Norplant FDA label
4 BDDCS applied to over 900 drugs
5 Critical Evaluation of Human Oral Bioavailability for Pharmaceutical Drugs by Using Various Cheminformatics Approaches
6 Natavio M, Stanczyk FZ, Molins EAG, Nelson A, Jusko WJ: Pharmacokinetics of the 1.5 mg levonorgestrel emergency contraceptive in women with normal, obese and extremely obese body mass index. Contraception. 2019 May;99(5):306-311. doi: 10.1016/j.contraception.2019.01.003. Epub 2019 Jan 28.
7 Levonorgestrel FDA label
8 Mechanism of action of levonorgestrel emergency contraception. Linacre Q. 2015 Feb;82(1):18-33. doi: 10.1179/2050854914Y.0000000026.
9 Hammer HF, Hammer J, Gasche C: [Polyethylene glycol (Macrogol)--an overview of its use in diagnosis and therapy of gastrointestinal diseases]. Wien Klin Wochenschr. 2000 Jan 28;112(2):53-60.
10 Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
11 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
12 Met909 plays a key role in the activation of the progesterone receptor and also in the high potency of 13-ethyl progestins. Mol Pharmacol. 2009 Jun;75(6):1317-24.
13 Progestins as inhibitors of the human 20-ketosteroid reductases, AKR1C1 and AKR1C3. Chem Biol Interact. 2011 May 30;191(1-3):227-33.
14 Effect of menstrual cycle and hormonal treatment on ki-67 and bcl-2 expression and adenomyosis. Gynecol Endocrinol. 2005 Mar;20(3):127-31. doi: 10.1080/09513590400021086.
15 P-glycoprotein (P-gp/MDR1)-mediated efflux of sex-steroid hormones and modulation of P-gp expression in vitro. Pharm Res. 2004 Jul;21(7):1284-93.
16 Study of low-density lipoprotein receptor regulation by oral (steroid) contraceptives: desogestrel, levonorgestrel and ethinyl estradiol in JEG-3 cell line and placental tissue. Contraception. 2007 Oct;76(4):297-305. doi: 10.1016/j.contraception.2007.06.011. Epub 2007 Sep 14.
17 Relative progestational and androgenic activity of four progestins used for male hormonal contraception assessed in vitro in relation to their ability to suppress LH secretion in the castrate male rat. Mol Cell Endocrinol. 2010 Oct 26;328(1-2):16-21. doi: 10.1016/j.mce.2010.06.010. Epub 2010 Jun 25.
18 Effects of natural products and nutraceuticals on steroid hormone-regulated gene expression. Clin Chim Acta. 2001 Oct;312(1-2):213-9. doi: 10.1016/s0009-8981(01)00626-x.
19 Serum distribution of the major metabolites of norgestimate in relation to its pharmacological properties. Contraception. 2003 Feb;67(2):93-9. doi: 10.1016/s0010-7824(02)00473-0.
20 [Effect of nylestriol and levonorgestrel on the expression of Opg/OPGL in human osteosarcoma MG-63 cell lines]. Zhong Nan Da Xue Xue Bao Yi Xue Ban. 2004 Dec;29(6):667-70.
21 Product Information. Myalept (metreleptin). Bristol-Myers Squibb, Princeton, NJ.
22 Glazer NB, Cheatham WW "Thiazolidinediones for type 2 diabetes - No evidence exists that pioglitazone induces hepatic cytochrome P450 isoform CYP3A4." Br Med J 322 (2001): 235-6. [PMID: 11159615]
23 Product Information. Tibsovo (ivosidenib). Agios Pharmaceuticals, Cambridge, MA.
24 Baciewicz AM "Oral contraceptive drug interactions." Ther Drug Monit 7 (1985): 26-35. [PMID: 2859674]
25 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
26 Product Information. Multaq (dronedarone). sanofi-aventis , Bridgewater, NJ.
27 Back DJ, Breckenridge AM, Crawford FE, MacIver M, Orne ML, Rowe PH "Interindividual variation and drug interactions with hormonal steroid contraceptives." Drugs 21 (1981): 46-61. [PMID: 7009137]
28 Devenport MH, Crook D, Wynn V, Lees LJ "Metabolic effects of low-dose fluconazole in healthy female users and non-users of oral contraceptives." Br J Clin Pharmacol 27 (1989): 851-9. [PMID: 2547410]
29 Gardner MJ, Tornatore KM, Jusko WJ, Kanarkowski R "Effects of tobacco smoking and oral contraceptive use on theophylline disposition." Br J Clin Pharmacol 16 (1983): 271-80. [PMID: 6626419]
30 Cerner Multum, Inc. "Australian Product Information.".
31 Product Information. Ketek (telithromycin). Aventis Pharmaceuticals, Bridgewater, NJ.
32 Product Information. Idhifa (enasidenib). Celgene Corporation, Summit, NJ.
33 Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
34 Product Information. Tykerb (lapatinib). Novartis Pharmaceuticals, East Hanover, NJ.
35 Product Information. Lipitor (atorvastatin). Parke-Davis, Morris Plains, NJ.
36 Faculty of Sexual & Reproductive Healthcare "FSRH Clinical Guidance: Drug Interactions with Hormonal Contraception.".
37 Product Information. Kalydeco (ivacaftor). Vertex Pharmaceuticals, Cambridge, MA.
38 Hobbes J, Boutagy J, Shenfield GM "Interactions between ethanol and oral contraceptive steroids." Clin Pharmacol Ther 38 (1985): 371-80. [PMID: 4042520]
39 Product Information. Serzone (nefazodone). Bristol-Myers Squibb, Princeton, NJ.
40 Laine K, Anttila M, Helminen A, Karnani H, Huupponen R "Dose linearity study of selegiline pharmacokinetics after oral administration: evidence for strong drug interaction with female sex steroids." Br J Clin Pharmacol 47 (1999): 249-54. [PMID: 10215747]
41 Back DJ, Grimmer SF, Orme ML, Proudlove D, Mann RD, Breckenridge AM "Evaluation of Committee on Safety of Medicines yellow card reports on oral contraceptive-drug interactions with anticonvulsants and antibiotics." Br J Clin Pharmacol 25 (1988): 527-32. [PMID: 3408633]
42 EMEA. European Medicines Agency "EPARs. European Union Public Assessment Reports.".
43 Product Information. Tazverik (tazemetostat). Epizyme, Inc, Cambridge, MA.
44 Back DJ, Breckenridge AM, Crawford F, et al. "The effect of rifampicin on norethisterone pharmacokinetics." Eur J Clin Pharmacol 15 (1979): 193-7. [PMID: 37091]
45 Archer JS, Archer DF "Oral contraceptive efficacy and antibiotic interaction: A myth debunked." J Am Acad Dermatol 46 (2002): 917-23. [PMID: 12063491]
46 Barry M, Mulcahy F, Merry C, Gibbons S, Back D "Pharmacokinetics and potential interactions amongst antiretroviral agents used to treat patients with HIV infection." Clin Pharmacokinet 36 (1999): 289-304. [PMID: 10320951]
47 Product Information. Fortovase (saquinavir) Roche Laboratories, Nutley, NJ.
48 Product Information. Prezista (darunavir). Ortho Biotech Inc, Bridgewater, NJ.
49 Product Information. Reyataz (atazanavir). Bristol-Myers Squibb, Princeton, NJ.
50 Product Information. Juxtapid (lomitapide). Aegerion Pharmaceuticals Inc, Cambridge, MA.
51 Product Information. Vaprisol (conivaptan). Cumberland Pharmaceuticals Inc, Nashville, TN.
52 Product Information. Zurampic (lesinurad). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
53 Product Information. Orladeyo (berotralstat). BioCryst Pharmaceuticals Inc, Durham, NC.
54 Product Information. Impavido (miltefosine). Paladin Therapeutics Inc, Wilmington, DE.
55 Product Information. Alunbrig (brigatinib). Ariad Pharmaceuticals Inc, Cambridge, MA.
56 Faculty of Sexual & Reproductive Healthcare "FSRH Clinical Guidance: Drug Interactions with Hormonal Contraception.".
57 Product Information. Copiktra (duvelisib). Verastem, Inc., Needham, MA.
58 Product Information. Braftovi (encorafenib). Array BioPharma Inc., Boulder, CO.
59 Product Information. Desferal (deferoxamine). Novartis Pharmaceuticals, East Hanover, NJ.
60 Product Information. Tasigna (nilotinib). Novartis Pharmaceuticals, East Hanover, NJ.
61 Product Information. Sprycel (dasatinib). Bristol-Myers Squibb, Princeton, NJ.
62 EMA. European Medicines Agency. European Union "EMA - List of medicines under additional monitoring.".
63 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
64 Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
65 Product Information. Zokinvy (lonafarnib). Eiger BioPharmaceuticals, Palo Alto, CA.
66 Product Information. Prograf (tacrolimus). Fujisawa, Deerfield, IL.
67 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
68 Granfors MT, Backman JT, Laitila J, Neuvonen PJ "Oral contraceptives containing ethinyl estradiol and gestodene markedly increase plasma concentrations and effects of tizanidine by inhibiting cytochrome P450 1A2." Clin Pharmacol Ther 78 (2005): 400-11. [PMID: 16198659]