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Identification
NameDrospirenone
Accession NumberDB01395
TypeSmall Molecule
GroupsApproved
DescriptionDrospirenone is a synthetic progestin that is an analog to spironolactone. It is found in a number of birth control formulations. Drospirenone differs from other synthetic progestins in that its pharmacological profile in preclinical studies shows it to be closer to the natural progesterone. As such it has anti-mineralocorticoid properties, counteracts the estrogen-stimulated activity of the renin-angiotensin-aldosterone system, and is not androgenic. It was shown in animal studies that drospirenone exhibits antiandrogenic activity judging from accessory sex gland growth in castrated, androgen-treated, juvenile rats.
Structure
Thumb
Synonyms
1,2-Dihydrospirorenone
6beta,7Beta;15beta,16beta-dimethylene-3-oxo-17alpha-pregn-4-ene-21,17-carbolactone
6β,7β,15β,16β-dimethylene-3-oxo-17α-pregn-4-ene-21,17 carbolactone
Dehydrospirorenone
Drospirenona
Drospirenonum
DRSP
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixtures
NameLabellerIngredients
AngeliqBayer Health Care Pharmaceuticals Inc.
Drospirenone and Ethinyl EstradiolMylan Pharmaceuticals Inc.
Drospirenone and Ethinyl Estradiol Tablets USP (21-day Regimen)Glenmark Pharmaceuticals Canada Inc.
Drospirenone and Ethinyl Estradiol Tablets USP (28-day Regimen)Glenmark Pharmaceuticals Canada Inc.
GianviPhysicians Total Care, Inc.
LorynaSandoz Inc
MyaApotex Inc
NikkiLupin Pharmaceuticals, Inc.
OcellaBarr Laboratories, Inc.
Qismette 21LUPIN LIMITED
Qismette 28LUPIN LIMITED
RajaniActavis Pharma, Inc.
SyedaSandoz Inc
VesturaWatson Pharma, Inc.
YasminBayer Health Care Pharmaceuticals Inc.
Yasmin 21Bayer Inc
Yasmin 28Bayer Inc
Yasmin PlusBayer Inc
YazBayer Health Care Pharmaceuticals Inc.
Yaz PlusBayer Inc
Zamine 21Apotex Inc
Zamine 28Apotex Inc
ZarahWatson Pharma, Inc.
Zarah 21Cobalt Pharmaceuticals Company
Zarah 28Cobalt Pharmaceuticals Company
SaltsNot Available
Categories
UNIIN295J34A25
CAS number67392-87-4
WeightAverage: 366.4932
Monoisotopic: 366.219494826
Chemical FormulaC24H30O3
InChI KeyMETQSPRSQINEEU-HXCATZOESA-N
InChI
InChI=1S/C24H30O3/c1-22-6-3-12(25)9-17(22)13-10-14(13)20-16(22)4-7-23(2)21(20)15-11-18(15)24(23)8-5-19(26)27-24/h9,13-16,18,20-21H,3-8,10-11H2,1-2H3/t13-,14+,15-,16+,18+,20-,21+,22-,23+,24+/m1/s1
IUPAC Name
(1R,2R,4R,10R,11S,14S,15S,16S,18S,19S)-10,14-dimethylspiro[hexacyclo[9.8.0.0²,⁴.0⁵,¹⁰.0¹⁴,¹⁹.0¹⁶,¹⁸]nonadecane-15,2'-oxolan]-5-ene-5',7-dione
SMILES
[H][C@@]12C[C@]1([H])[C@@]1([H])[C@]3([H])[C@]4([H])C[C@]4([H])[C@@]4(CCC(=O)O4)[C@@]3(C)CC[C@]1([H])[C@@]1(C)CCC(=O)C=C21
Pharmacology
IndicationFor the prevention of pregnancy in women who elect an oral contraceptive.
Structured Indications
PharmacodynamicsDrospirenone differs from other synthetic progestins in that its pharmacological profile in preclinical studies shows it to be closer to the natural progesterone. As such it has anti-mineralocorticoid properties, counteracts the estrogen-stimulated activity of the renin-angiotensin-aldosterone system, and is not androgenic.
Mechanism of actionProgestins such as drospirenone diffuse freely into target cells in the female reproductive tract, mammary gland, hypothalamus, and the pituitary and bind to the progesterone receptor. Once bound to the receptor, progestins slow the frequency of release of gonadotropin releasing hormone (GnRH) from the hypothalamus and blunt the pre-ovulatory LH surge.
TargetKindPharmacological actionActionsOrganismUniProt ID
Progesterone receptorProteinyes
agonist
HumanP06401 details
Mineralocorticoid receptorProteinyes
antagonist
HumanP08235 details
Androgen receptorProteinyes
antagonist
HumanP10275 details
Related Articles
AbsorptionOral bioavailability is approximately 76%.
Volume of distributionNot Available
Protein binding95-97%
Metabolism

Extensively metabolized following oral or intravenous administration. The two major metabolites are inactive and are formed independent of the CYP450 enzyme system. The metabolites are the acid form of drospirenone formed by opening of the lactone ring and the 4,5-dihydro-drospirenone-3-sulfate.

SubstrateEnzymesProduct
Drospirenone
Not Available
4,5-dihydro-drospirenone-3-sulfateDetails
Route of eliminationNot Available
Half life30 hours
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AbciximabThe therapeutic efficacy of Abciximab can be decreased when used in combination with Drospirenone.Approved
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Drospirenone.Approved, Investigational
AceclofenacAceclofenac may increase the hyperkalemic activities of Drospirenone.Approved
AcenocoumarolDrospirenone may decrease the anticoagulant activities of Acenocoumarol.Approved
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Drospirenone.Withdrawn
AcetovanilloneAcetovanillone may increase the hyperkalemic activities of Drospirenone.Investigational
Acetylsalicylic acidAcetylsalicylic acid may increase the hyperkalemic activities of Drospirenone.Approved, Vet Approved
AcitretinThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Acitretin.Approved
AdapaleneAdapalene may increase the hyperkalemic activities of Drospirenone.Approved
AicarThe therapeutic efficacy of Aicar can be decreased when used in combination with Drospirenone.Experimental
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Drospirenone.Approved, Illicit
AliskirenDrospirenone may increase the hyperkalemic activities of Aliskiren.Approved, Investigational
AlitretinoinThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Alitretinoin.Approved, Investigational
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Drospirenone.Approved
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Alphacetylmethadol is combined with Drospirenone.Experimental, Illicit
AmilorideDrospirenone may increase the hyperkalemic activities of Amiloride.Approved
AmiodaroneThe serum concentration of Drospirenone can be increased when it is combined with Amiodarone.Approved, Investigational
AmobarbitalThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Amobarbital.Approved, Illicit
AncrodThe therapeutic efficacy of Ancrod can be decreased when used in combination with Drospirenone.Investigational
AnisodamineAnisodamine may increase the hyperkalemic activities of Drospirenone.Investigational
AntipyrineAntipyrine may increase the hyperkalemic activities of Drospirenone.Approved
Antithrombin III humanThe therapeutic efficacy of Antithrombin III human can be decreased when used in combination with Drospirenone.Approved
ApixabanThe therapeutic efficacy of Apixaban can be decreased when used in combination with Drospirenone.Approved
ApremilastApremilast may increase the hyperkalemic activities of Drospirenone.Approved, Investigational
AprepitantThe serum concentration of Drospirenone can be decreased when it is combined with Aprepitant.Approved, Investigational
ArdeparinThe therapeutic efficacy of Ardeparin can be decreased when used in combination with Drospirenone.Approved, Withdrawn
ArgatrobanThe therapeutic efficacy of Argatroban can be decreased when used in combination with Drospirenone.Approved, Investigational
ArtemetherThe serum concentration of Drospirenone can be decreased when it is combined with Artemether.Approved
AtazanavirThe serum concentration of Drospirenone can be increased when it is combined with Atazanavir.Approved, Investigational
AzapropazoneAzapropazone may increase the hyperkalemic activities of Drospirenone.Withdrawn
AzelastineAzelastine may increase the hyperkalemic activities of Drospirenone.Approved
Azilsartan medoxomilAzilsartan medoxomil may increase the hyperkalemic activities of Drospirenone.Approved
BalaglitazoneThe therapeutic efficacy of Balaglitazone can be decreased when used in combination with Drospirenone.Investigational
BalsalazideBalsalazide may increase the hyperkalemic activities of Drospirenone.Approved, Investigational
BarbexacloneThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Barbexaclone.Experimental
BarbitalThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Barbital.Illicit
BecaplerminThe therapeutic efficacy of Becaplermin can be decreased when used in combination with Drospirenone.Approved, Investigational
BenazeprilBenazepril may increase the hyperkalemic activities of Drospirenone.Approved, Investigational
BenoxaprofenBenoxaprofen may increase the hyperkalemic activities of Drospirenone.Withdrawn
Betulinic AcidBetulinic Acid may increase the hyperkalemic activities of Drospirenone.Investigational
BexaroteneThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Bexarotene.Approved, Investigational
BexaroteneThe serum concentration of Drospirenone can be decreased when it is combined with Bexarotene.Approved, Investigational
BezitramideThe risk or severity of adverse effects can be increased when Bezitramide is combined with Drospirenone.Experimental, Illicit, Withdrawn
BivalirudinThe therapeutic efficacy of Bivalirudin can be decreased when used in combination with Drospirenone.Approved, Investigational
BoceprevirThe serum concentration of Drospirenone can be increased when it is combined with Boceprevir.Approved
BosentanThe serum concentration of Drospirenone can be decreased when it is combined with Bosentan.Approved, Investigational
BromfenacBromfenac may increase the hyperkalemic activities of Drospirenone.Approved
BucillamineBucillamine may increase the hyperkalemic activities of Drospirenone.Investigational
BuforminThe therapeutic efficacy of Buformin can be decreased when used in combination with Drospirenone.Withdrawn
BuprenorphineThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Drospirenone.Approved, Illicit, Investigational, Vet Approved
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Drospirenone.Approved, Illicit, Vet Approved
C1 Esterase Inhibitor (Human)Drospirenone may increase the thrombogenic activities of C1 Esterase Inhibitor (Human).Approved
C1 Esterase Inhibitor (Recombinant)Drospirenone may increase the thrombogenic activities of C1 Esterase Inhibitor (Recombinant).Approved
CanagliflozinThe therapeutic efficacy of Canagliflozin can be decreased when used in combination with Drospirenone.Approved
CandesartanCandesartan may increase the hyperkalemic activities of Drospirenone.Approved
CandoxatrilCandoxatril may increase the hyperkalemic activities of Drospirenone.Experimental
CaptoprilCaptopril may increase the hyperkalemic activities of Drospirenone.Approved
CarbamazepineThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Carbamazepine.Approved, Investigational
CarfentanilThe risk or severity of adverse effects can be increased when Carfentanil is combined with Drospirenone.Illicit, Vet Approved
CarprofenCarprofen may increase the hyperkalemic activities of Drospirenone.Approved, Vet Approved, Withdrawn
CastanospermineCastanospermine may increase the hyperkalemic activities of Drospirenone.Experimental
CelecoxibCelecoxib may increase the hyperkalemic activities of Drospirenone.Approved, Investigational
CeritinibThe serum concentration of Drospirenone can be increased when it is combined with Ceritinib.Approved
CertoparinThe therapeutic efficacy of Certoparin can be decreased when used in combination with Drospirenone.Approved
ChloroquineChloroquine may increase the hyperkalemic activities of Drospirenone.Approved, Vet Approved
ChlorpropamideThe therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Drospirenone.Approved
CholestyramineThe serum concentration of Drospirenone can be decreased when it is combined with Cholestyramine.Approved
CiglitazoneThe therapeutic efficacy of Ciglitazone can be decreased when used in combination with Drospirenone.Experimental
CilazaprilCilazapril may increase the hyperkalemic activities of Drospirenone.Approved
Citric AcidThe therapeutic efficacy of Citric Acid can be decreased when used in combination with Drospirenone.Nutraceutical, Vet Approved
ClarithromycinThe serum concentration of Drospirenone can be increased when it is combined with Clarithromycin.Approved
ClobazamThe serum concentration of Drospirenone can be decreased when it is combined with Clobazam.Approved, Illicit
ClonixinClonixin may increase the hyperkalemic activities of Drospirenone.Approved
CobicistatThe serum concentration of Drospirenone can be increased when it is combined with Cobicistat.Approved
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Drospirenone.Approved, Illicit
ColesevelamThe serum concentration of Drospirenone can be decreased when it is combined with Colesevelam.Approved
ColestipolThe serum concentration of Drospirenone can be decreased when it is combined with Colestipol.Approved
CurcuminCurcumin may increase the hyperkalemic activities of Drospirenone.Investigational
D-LimoneneD-Limonene may increase the hyperkalemic activities of Drospirenone.Investigational
Dabigatran etexilateThe therapeutic efficacy of Dabigatran etexilate can be decreased when used in combination with Drospirenone.Approved
DabrafenibThe serum concentration of Drospirenone can be decreased when it is combined with Dabrafenib.Approved
DalteparinThe therapeutic efficacy of Dalteparin can be decreased when used in combination with Drospirenone.Approved
DanaparoidThe therapeutic efficacy of Danaparoid can be decreased when used in combination with Drospirenone.Approved, Withdrawn
DarunavirThe serum concentration of Drospirenone can be decreased when it is combined with Darunavir.Approved
DeoxyspergualinThe therapeutic efficacy of Deoxyspergualin can be decreased when used in combination with Drospirenone.Investigational
DesirudinThe therapeutic efficacy of Desirudin can be decreased when used in combination with Drospirenone.Approved
DextranThe therapeutic efficacy of Dextran can be decreased when used in combination with Drospirenone.Approved, Vet Approved
Dextran 40The therapeutic efficacy of Dextran 40 can be decreased when used in combination with Drospirenone.Approved
Dextran 70The therapeutic efficacy of Dextran 70 can be decreased when used in combination with Drospirenone.Approved
Dextran 75The therapeutic efficacy of Dextran 75 can be decreased when used in combination with Drospirenone.Approved
DextromoramideThe risk or severity of adverse effects can be increased when Dextromoramide is combined with Drospirenone.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Drospirenone.Approved, Illicit, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Dezocine is combined with Drospirenone.Approved
DiclofenacDiclofenac may increase the hyperkalemic activities of Drospirenone.Approved, Vet Approved
DicoumarolDrospirenone may decrease the anticoagulant activities of Dicoumarol.Approved
DiflunisalDiflunisal may increase the hyperkalemic activities of Drospirenone.Approved
DihydrocodeineThe risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Drospirenone.Approved, Illicit
DihydroetorphineThe risk or severity of adverse effects can be increased when Dihydroetorphine is combined with Drospirenone.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Dihydromorphine is combined with Drospirenone.Experimental, Illicit
DiphenoxylateThe risk or severity of adverse effects can be increased when Diphenoxylate is combined with Drospirenone.Approved, Illicit
DPDPEThe risk or severity of adverse effects can be increased when DPDPE is combined with Drospirenone.Investigational
DroxicamDroxicam may increase the hyperkalemic activities of Drospirenone.Approved
DulaglutideThe therapeutic efficacy of Dulaglutide can be decreased when used in combination with Drospirenone.Approved
DuvelisibDuvelisib may increase the hyperkalemic activities of Drospirenone.Investigational
E6201E6201 may increase the hyperkalemic activities of Drospirenone.Investigational
EbselenEbselen may increase the hyperkalemic activities of Drospirenone.Investigational
Edetic AcidThe therapeutic efficacy of Edetic Acid can be decreased when used in combination with Drospirenone.Approved, Vet Approved
EdoxabanThe therapeutic efficacy of Edoxaban can be decreased when used in combination with Drospirenone.Approved
EfavirenzThe serum concentration of Drospirenone can be decreased when it is combined with Efavirenz.Approved, Investigational
EmpagliflozinThe therapeutic efficacy of Empagliflozin can be decreased when used in combination with Drospirenone.Approved
EnalaprilEnalapril may increase the hyperkalemic activities of Drospirenone.Approved, Vet Approved
EnalaprilatEnalaprilat may increase the hyperkalemic activities of Drospirenone.Approved
EnoxaparinThe therapeutic efficacy of Enoxaparin can be decreased when used in combination with Drospirenone.Approved
EpirizoleEpirizole may increase the hyperkalemic activities of Drospirenone.Approved
EplerenoneDrospirenone may increase the hyperkalemic activities of Eplerenone.Approved
EprosartanEprosartan may increase the hyperkalemic activities of Drospirenone.Approved
Eslicarbazepine acetateThe serum concentration of Drospirenone can be decreased when it is combined with Eslicarbazepine acetate.Approved
EtanerceptEtanercept may increase the hyperkalemic activities of Drospirenone.Approved, Investigational
Ethyl biscoumacetateDrospirenone may decrease the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
EthylmorphineThe risk or severity of adverse effects can be increased when Ethylmorphine is combined with Drospirenone.Approved, Illicit
EtodolacEtodolac may increase the hyperkalemic activities of Drospirenone.Approved, Investigational, Vet Approved
EtofenamateEtofenamate may increase the hyperkalemic activities of Drospirenone.Approved
EtoricoxibEtoricoxib may increase the hyperkalemic activities of Drospirenone.Approved, Investigational
EtorphineThe risk or severity of adverse effects can be increased when Etorphine is combined with Drospirenone.Illicit, Vet Approved
Evening primrose oilEvening primrose oil may increase the hyperkalemic activities of Drospirenone.Approved
ExenatideThe serum concentration of Drospirenone can be decreased when it is combined with Exenatide.Approved, Investigational
exisulindexisulind may increase the hyperkalemic activities of Drospirenone.Investigational
FelbamateThe serum concentration of Drospirenone can be decreased when it is combined with Felbamate.Approved
FenbufenFenbufen may increase the hyperkalemic activities of Drospirenone.Approved
FenoprofenFenoprofen may increase the hyperkalemic activities of Drospirenone.Approved
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Drospirenone.Approved, Illicit, Investigational, Vet Approved
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Drospirenone.Approved
FloctafenineFloctafenine may increase the hyperkalemic activities of Drospirenone.Approved, Withdrawn
FluindioneDrospirenone may decrease the anticoagulant activities of Fluindione.Investigational
FlunixinFlunixin may increase the hyperkalemic activities of Drospirenone.Vet Approved
FlurbiprofenFlurbiprofen may increase the hyperkalemic activities of Drospirenone.Approved, Investigational
FondaparinuxThe therapeutic efficacy of Fondaparinux can be decreased when used in combination with Drospirenone.Investigational
Fondaparinux sodiumThe therapeutic efficacy of Fondaparinux sodium can be decreased when used in combination with Drospirenone.Approved, Investigational
ForasartanForasartan may increase the hyperkalemic activities of Drospirenone.Experimental
FosamprenavirThe serum concentration of the active metabolites of Fosamprenavir can be reduced when Fosamprenavir is used in combination with Drospirenone resulting in a loss in efficacy.Approved
FosaprepitantThe serum concentration of Drospirenone can be decreased when it is combined with Fosaprepitant.Approved
FosinoprilFosinopril may increase the hyperkalemic activities of Drospirenone.Approved
FosphenytoinThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Fosphenytoin.Approved
GabexateThe therapeutic efficacy of Gabexate can be decreased when used in combination with Drospirenone.Investigational
GlibornurideThe therapeutic efficacy of Glibornuride can be decreased when used in combination with Drospirenone.Withdrawn
GliclazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Drospirenone.Approved
GlimepirideThe therapeutic efficacy of Glimepiride can be decreased when used in combination with Drospirenone.Approved
GlipizideThe therapeutic efficacy of Glipizide can be decreased when used in combination with Drospirenone.Approved
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Drospirenone.Approved
GlyburideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Drospirenone.Approved
GriseofulvinThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Griseofulvin.Approved, Vet Approved
GusperimusThe therapeutic efficacy of Gusperimus can be decreased when used in combination with Drospirenone.Investigational
HeparinThe therapeutic efficacy of Heparin can be decreased when used in combination with Drospirenone.Approved, Investigational
HeroinThe risk or severity of adverse effects can be increased when Heroin is combined with Drospirenone.Approved, Illicit
HexobarbitalThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Hexobarbital.Approved
HigenamineHigenamine may increase the hyperkalemic activities of Drospirenone.Investigational
HirulogThe therapeutic efficacy of Hirulog can be decreased when used in combination with Drospirenone.Experimental
HMPL-004HMPL-004 may increase the hyperkalemic activities of Drospirenone.Investigational
HydrocodoneThe serum concentration of Hydrocodone can be decreased when it is combined with Drospirenone.Approved, Illicit
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Drospirenone.Approved, Illicit
IbuprofenIbuprofen may increase the hyperkalemic activities of Drospirenone.Approved
IbuproxamIbuproxam may increase the hyperkalemic activities of Drospirenone.Withdrawn
IcatibantIcatibant may increase the hyperkalemic activities of Drospirenone.Approved
IdelalisibThe serum concentration of Drospirenone can be increased when it is combined with Idelalisib.Approved
idraparinuxThe therapeutic efficacy of idraparinux can be decreased when used in combination with Drospirenone.Investigational
ImidaprilImidapril may increase the hyperkalemic activities of Drospirenone.Investigational
IndinavirThe serum concentration of Drospirenone can be increased when it is combined with Indinavir.Approved
IndomethacinIndomethacin may increase the hyperkalemic activities of Drospirenone.Approved, Investigational
IndoprofenIndoprofen may increase the hyperkalemic activities of Drospirenone.Withdrawn
Insulin AspartThe therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Drospirenone.Approved
Insulin DetemirThe therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Drospirenone.Approved
Insulin GlargineThe therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Drospirenone.Approved
Insulin GlulisineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Drospirenone.Approved
Insulin LisproThe therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Drospirenone.Approved
Insulin PorkThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Drospirenone.Approved
IrbesartanIrbesartan may increase the hyperkalemic activities of Drospirenone.Approved, Investigational
IsotretinoinThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Isotretinoin.Approved
IsoxicamIsoxicam may increase the hyperkalemic activities of Drospirenone.Withdrawn
ItraconazoleThe serum concentration of Drospirenone can be increased when it is combined with Itraconazole.Approved, Investigational
KebuzoneKebuzone may increase the hyperkalemic activities of Drospirenone.Experimental
KetobemidoneThe risk or severity of adverse effects can be increased when Ketobemidone is combined with Drospirenone.Approved
KetoconazoleThe serum concentration of Drospirenone can be increased when it is combined with Ketoconazole.Approved, Investigational
KetoprofenKetoprofen may increase the hyperkalemic activities of Drospirenone.Approved, Vet Approved
KetorolacKetorolac may increase the hyperkalemic activities of Drospirenone.Approved
LamotrigineThe serum concentration of Drospirenone can be decreased when it is combined with Lamotrigine.Approved, Investigational
LeflunomideLeflunomide may increase the hyperkalemic activities of Drospirenone.Approved, Investigational
LepirudinThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Drospirenone.Approved
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Levomethadyl Acetate is combined with Drospirenone.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with Drospirenone.Approved
LinagliptinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Drospirenone.Approved
LiraglutideThe therapeutic efficacy of Liraglutide can be decreased when used in combination with Drospirenone.Approved
LisinoprilLisinopril may increase the hyperkalemic activities of Drospirenone.Approved, Investigational
LisofyllineLisofylline may increase the hyperkalemic activities of Drospirenone.Investigational
LofentanilThe risk or severity of adverse effects can be increased when Lofentanil is combined with Drospirenone.Illicit
LopinavirThe serum concentration of Drospirenone can be decreased when it is combined with Lopinavir.Approved
LornoxicamLornoxicam may increase the hyperkalemic activities of Drospirenone.Approved
LosartanLosartan may increase the hyperkalemic activities of Drospirenone.Approved
LoxoprofenLoxoprofen may increase the hyperkalemic activities of Drospirenone.Approved
LumacaftorThe serum concentration of Drospirenone can be decreased when it is combined with Lumacaftor.Approved
LumiracoxibLumiracoxib may increase the hyperkalemic activities of Drospirenone.Approved, Investigational
Magnesium salicylateMagnesium salicylate may increase the hyperkalemic activities of Drospirenone.Approved
MasoprocolMasoprocol may increase the hyperkalemic activities of Drospirenone.Approved
Meclofenamic acidMeclofenamic acid may increase the hyperkalemic activities of Drospirenone.Approved, Vet Approved
Mefenamic acidMefenamic acid may increase the hyperkalemic activities of Drospirenone.Approved
MeloxicamMeloxicam may increase the hyperkalemic activities of Drospirenone.Approved, Vet Approved
MesalazineMesalazine may increase the hyperkalemic activities of Drospirenone.Approved
MetamizoleMetamizole may increase the hyperkalemic activities of Drospirenone.Withdrawn
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Drospirenone.Approved
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Drospirenone.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Methadyl Acetate is combined with Drospirenone.Approved, Illicit
MethohexitalThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Methohexital.Approved
MethylphenobarbitalThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Methylphenobarbital.Approved
MetreleptinThe serum concentration of Drospirenone can be decreased when it is combined with Metreleptin.Approved
MifepristoneThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Mifepristone.Approved, Investigational
MiglitolThe therapeutic efficacy of Miglitol can be decreased when used in combination with Drospirenone.Approved
MiglustatThe therapeutic efficacy of Miglustat can be decreased when used in combination with Drospirenone.Approved
MitiglinideThe therapeutic efficacy of Mitiglinide can be decreased when used in combination with Drospirenone.Approved, Investigational
MizoribineMizoribine may increase the hyperkalemic activities of Drospirenone.Investigational
MoexiprilMoexipril may increase the hyperkalemic activities of Drospirenone.Approved
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Drospirenone.Approved, Investigational
Mycophenolate mofetilMycophenolate mofetil may increase the hyperkalemic activities of Drospirenone.Approved, Investigational
Mycophenolic acidThe serum concentration of Drospirenone can be decreased when it is combined with Mycophenolic acid.Approved
NabumetoneNabumetone may increase the hyperkalemic activities of Drospirenone.Approved
NadroparinThe therapeutic efficacy of Nadroparin can be decreased when used in combination with Drospirenone.Approved
NafamostatNafamostat may increase the hyperkalemic activities of Drospirenone.Investigational
NaftifineNaftifine may increase the hyperkalemic activities of Drospirenone.Approved
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with Drospirenone.Approved
NaproxenNaproxen may increase the hyperkalemic activities of Drospirenone.Approved, Vet Approved
NateglinideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Drospirenone.Approved, Investigational
NCX 4016NCX 4016 may increase the hyperkalemic activities of Drospirenone.Investigational
NefazodoneThe serum concentration of Drospirenone can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Drospirenone can be decreased when it is combined with Nelfinavir.Approved
NepafenacNepafenac may increase the hyperkalemic activities of Drospirenone.Approved
NevirapineThe serum concentration of Drospirenone can be decreased when it is combined with Nevirapine.Approved
Niflumic AcidNiflumic Acid may increase the hyperkalemic activities of Drospirenone.Approved
NimesulideNimesulide may increase the hyperkalemic activities of Drospirenone.Approved, Withdrawn
NimodipineThe serum concentration of Nimodipine can be decreased when it is combined with Drospirenone.Approved
NitroaspirinNitroaspirin may increase the hyperkalemic activities of Drospirenone.Investigational
NormethadoneThe risk or severity of adverse effects can be increased when Normethadone is combined with Drospirenone.Approved, Illicit
OlmesartanOlmesartan may increase the hyperkalemic activities of Drospirenone.Approved, Investigational
OlopatadineOlopatadine may increase the hyperkalemic activities of Drospirenone.Approved
OlsalazineOlsalazine may increase the hyperkalemic activities of Drospirenone.Approved
OmapatrilatOmapatrilat may increase the hyperkalemic activities of Drospirenone.Investigational
OpiumThe risk or severity of adverse effects can be increased when Opium is combined with Drospirenone.Approved, Illicit
OrgoteinOrgotein may increase the hyperkalemic activities of Drospirenone.Vet Approved
OtamixabanThe therapeutic efficacy of Otamixaban can be decreased when used in combination with Drospirenone.Investigational
OxaprozinOxaprozin may increase the hyperkalemic activities of Drospirenone.Approved
OxcarbazepineThe serum concentration of Drospirenone can be decreased when it is combined with Oxcarbazepine.Approved
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Drospirenone.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Drospirenone.Approved, Investigational, Vet Approved
OxyphenbutazoneOxyphenbutazone may increase the hyperkalemic activities of Drospirenone.Withdrawn
ParecoxibParecoxib may increase the hyperkalemic activities of Drospirenone.Approved
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Drospirenone.Approved, Vet Approved
PentobarbitalThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Pentobarbital.Approved, Vet Approved
Pentosan PolysulfateThe therapeutic efficacy of Pentosan Polysulfate can be decreased when used in combination with Drospirenone.Approved
PerampanelThe serum concentration of Drospirenone can be decreased when it is combined with Perampanel.Approved
PerindoprilPerindopril may increase the hyperkalemic activities of Drospirenone.Approved
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Drospirenone.Approved
PhenforminThe therapeutic efficacy of Phenformin can be decreased when used in combination with Drospirenone.Approved, Withdrawn
PhenindioneDrospirenone may decrease the anticoagulant activities of Phenindione.Approved
PhenobarbitalThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Phenobarbital.Approved
PhenprocoumonDrospirenone may decrease the anticoagulant activities of Phenprocoumon.Approved
PhenylbutazonePhenylbutazone may increase the hyperkalemic activities of Drospirenone.Approved, Vet Approved
PhenytoinThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Phenytoin.Approved, Vet Approved
PimecrolimusPimecrolimus may increase the hyperkalemic activities of Drospirenone.Approved, Investigational
PioglitazoneThe therapeutic efficacy of Pioglitazone can be decreased when used in combination with Drospirenone.Approved, Investigational
PirfenidonePirfenidone may increase the hyperkalemic activities of Drospirenone.Investigational
PiritramideThe risk or severity of adverse effects can be increased when Piritramide is combined with Drospirenone.Investigational
PiroxicamPiroxicam may increase the hyperkalemic activities of Drospirenone.Approved, Investigational
PosaconazoleThe serum concentration of Drospirenone can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PramlintideThe therapeutic efficacy of Pramlintide can be decreased when used in combination with Drospirenone.Approved, Investigational
PrimidoneThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Primidone.Approved, Vet Approved
PropacetamolPropacetamol may increase the hyperkalemic activities of Drospirenone.Approved
Protein CThe therapeutic efficacy of Protein C can be decreased when used in combination with Drospirenone.Approved
Protein S humanThe therapeutic efficacy of Protein S human can be decreased when used in combination with Drospirenone.Approved
ProtocatechualdehydeThe therapeutic efficacy of Protocatechualdehyde can be decreased when used in combination with Drospirenone.Approved
PrucaloprideThe serum concentration of Drospirenone can be decreased when it is combined with Prucalopride.Approved
PTC299PTC299 may increase the hyperkalemic activities of Drospirenone.Investigational
QuinaprilQuinapril may increase the hyperkalemic activities of Drospirenone.Approved, Investigational
RamiprilRamipril may increase the hyperkalemic activities of Drospirenone.Approved
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Drospirenone.Approved
RepaglinideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Drospirenone.Approved, Investigational
RescinnamineRescinnamine may increase the hyperkalemic activities of Drospirenone.Approved
ResveratrolResveratrol may increase the hyperkalemic activities of Drospirenone.Experimental, Investigational
ReviparinThe therapeutic efficacy of Reviparin can be decreased when used in combination with Drospirenone.Approved
RifabutinThe serum concentration of Drospirenone can be decreased when it is combined with Rifabutin.Approved
RifampicinThe serum concentration of Drospirenone can be decreased when it is combined with Rifampicin.Approved
RifapentineThe serum concentration of Drospirenone can be decreased when it is combined with Rifapentine.Approved
RitonavirThe serum concentration of Drospirenone can be increased when it is combined with Ritonavir.Approved, Investigational
RivaroxabanThe therapeutic efficacy of Rivaroxaban can be decreased when used in combination with Drospirenone.Approved
RofecoxibRofecoxib may increase the hyperkalemic activities of Drospirenone.Investigational, Withdrawn
RosiglitazoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Drospirenone.Approved, Investigational
SacubitrilSacubitril may increase the hyperkalemic activities of Drospirenone.Approved
SalicylamideSalicylamide may increase the hyperkalemic activities of Drospirenone.Approved
Salicylic acidSalicylic acid may increase the hyperkalemic activities of Drospirenone.Approved, Vet Approved
SalsalateSalsalate may increase the hyperkalemic activities of Drospirenone.Approved
SaprisartanSaprisartan may increase the hyperkalemic activities of Drospirenone.Experimental
SaquinavirThe serum concentration of Drospirenone can be decreased when it is combined with Saquinavir.Approved, Investigational
SaralasinSaralasin may increase the hyperkalemic activities of Drospirenone.Investigational
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Drospirenone.Approved
SecobarbitalThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Secobarbital.Approved, Vet Approved
SelegilineThe serum concentration of Selegiline can be increased when it is combined with Drospirenone.Approved, Investigational, Vet Approved
SeratrodastSeratrodast may increase the hyperkalemic activities of Drospirenone.Approved, Investigational
SitagliptinThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Drospirenone.Approved, Investigational
SpiraprilSpirapril may increase the hyperkalemic activities of Drospirenone.Approved
SpironolactoneDrospirenone may increase the hyperkalemic activities of Spironolactone.Approved
SRT501SRT501 may increase the hyperkalemic activities of Drospirenone.Investigational
St. John's WortThe therapeutic efficacy of Drospirenone can be decreased when used in combination with St. John's Wort.Nutraceutical
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Drospirenone.Approved, Investigational
SugammadexThe serum concentration of Drospirenone can be decreased when it is combined with Sugammadex.Approved
SulfasalazineSulfasalazine may increase the hyperkalemic activities of Drospirenone.Approved
SulindacSulindac may increase the hyperkalemic activities of Drospirenone.Approved
SulodexideThe therapeutic efficacy of Sulodexide can be decreased when used in combination with Drospirenone.Approved, Investigational
SuprofenSuprofen may increase the hyperkalemic activities of Drospirenone.Approved, Withdrawn
TapentadolThe risk or severity of adverse effects can be increased when Tapentadol is combined with Drospirenone.Approved
TasosartanTasosartan may increase the hyperkalemic activities of Drospirenone.Approved
TelaprevirThe serum concentration of Drospirenone can be decreased when it is combined with Telaprevir.Approved
TelithromycinThe serum concentration of Drospirenone can be increased when it is combined with Telithromycin.Approved
TelmisartanTelmisartan may increase the hyperkalemic activities of Drospirenone.Approved, Investigational
TemocaprilTemocapril may increase the hyperkalemic activities of Drospirenone.Experimental, Investigational
TenoxicamTenoxicam may increase the hyperkalemic activities of Drospirenone.Approved
TepoxalinTepoxalin may increase the hyperkalemic activities of Drospirenone.Vet Approved
TeriflunomideTeriflunomide may increase the hyperkalemic activities of Drospirenone.Approved
ThalidomideDrospirenone may increase the thrombogenic activities of Thalidomide.Approved, Investigational, Withdrawn
ThiamylalThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Thiamylal.Approved, Vet Approved
ThiazolidinedioneThe therapeutic efficacy of Thiazolidinedione can be decreased when used in combination with Drospirenone.Investigational
ThiopentalThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Thiopental.Approved, Vet Approved
Tiaprofenic acidTiaprofenic acid may increase the hyperkalemic activities of Drospirenone.Approved
TinoridineTinoridine may increase the hyperkalemic activities of Drospirenone.Investigational
TipranavirThe serum concentration of Drospirenone can be increased when it is combined with Tipranavir.Approved, Investigational
TolazamideThe therapeutic efficacy of Tolazamide can be decreased when used in combination with Drospirenone.Approved
TolbutamideThe therapeutic efficacy of Tolbutamide can be decreased when used in combination with Drospirenone.Approved
Tolfenamic AcidTolfenamic Acid may increase the hyperkalemic activities of Drospirenone.Approved
TolmetinTolmetin may increase the hyperkalemic activities of Drospirenone.Approved
TopiramateThe serum concentration of Drospirenone can be decreased when it is combined with Topiramate.Approved
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Drospirenone.Approved, Investigational
TrandolaprilTrandolapril may increase the hyperkalemic activities of Drospirenone.Approved
Tranexamic AcidDrospirenone may increase the thrombogenic activities of Tranexamic Acid.Approved
TranilastTranilast may increase the hyperkalemic activities of Drospirenone.Approved, Investigational
TretinoinThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Tretinoin.Approved, Investigational, Nutraceutical
TriamtereneDrospirenone may increase the hyperkalemic activities of Triamterene.Approved
Trisalicylate-cholineTrisalicylate-choline may increase the hyperkalemic activities of Drospirenone.Approved
TroglitazoneThe therapeutic efficacy of Troglitazone can be decreased when used in combination with Drospirenone.Withdrawn
UlipristalThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Ulipristal.Approved
ValdecoxibValdecoxib may increase the hyperkalemic activities of Drospirenone.Investigational, Withdrawn
ValsartanValsartan may increase the hyperkalemic activities of Drospirenone.Approved, Investigational
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Drospirenone.Approved, Investigational
VogliboseThe therapeutic efficacy of Voglibose can be decreased when used in combination with Drospirenone.Approved, Investigational
VoriconazoleThe serum concentration of Drospirenone can be increased when it is combined with Voriconazole.Approved, Investigational
WarfarinDrospirenone may decrease the anticoagulant activities of Warfarin.Approved
XimelagatranThe therapeutic efficacy of Ximelagatran can be decreased when used in combination with Drospirenone.Approved, Investigational, Withdrawn
Ym150The therapeutic efficacy of Ym150 can be decreased when used in combination with Drospirenone.Investigational
ZaltoprofenZaltoprofen may increase the hyperkalemic activities of Drospirenone.Approved
ZileutonZileuton may increase the hyperkalemic activities of Drospirenone.Approved, Investigational, Withdrawn
ZomepiracZomepirac may increase the hyperkalemic activities of Drospirenone.Withdrawn
Food Interactions
  • Food reduces the rate of absorption, but not the extent of absorption.
References
Synthesis Reference

DOI: 10.1002/cjoc.201201147

General References
  1. Krattenmacher R: Drospirenone: pharmacology and pharmacokinetics of a unique progestogen. Contraception. 2000 Jul;62(1):29-38. [PubMed:11024226 ]
  2. Wichianpitaya J, Taneepanichskul S: A comparative efficacy of low-dose combined oral contraceptives containing desogestrel and drospirenone in premenstrual symptoms. Obstet Gynecol Int. 2013;2013:487143. doi: 10.1155/2013/487143. Epub 2013 Feb 20. [PubMed:23577032 ]
External Links
ATC CodesG03FA17G03AC10G03AA12
AHFS Codes
  • 68:12
PDB EntriesNot Available
FDA labelDownload (292 KB)
MSDSDownload (567 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9383
Caco-2 permeable+0.6376
P-glycoprotein substrateSubstrate0.6524
P-glycoprotein inhibitor IInhibitor0.6171
P-glycoprotein inhibitor IINon-inhibitor0.6726
Renal organic cation transporterNon-inhibitor0.7005
CYP450 2C9 substrateNon-substrate0.796
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.6964
CYP450 1A2 substrateNon-inhibitor0.5534
CYP450 2C9 inhibitorNon-inhibitor0.8665
CYP450 2D6 inhibitorNon-inhibitor0.9336
CYP450 2C19 inhibitorNon-inhibitor0.7754
CYP450 3A4 inhibitorNon-inhibitor0.8355
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8541
Ames testNon AMES toxic0.9163
CarcinogenicityNon-carcinogens0.9505
BiodegradationNot ready biodegradable0.9757
Rat acute toxicity1.9430 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9393
hERG inhibition (predictor II)Non-inhibitor0.8215
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tablet, film coatedOral
Kit
TabletOral
KitOral
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5798338 No1995-07-102015-07-10Us
US6441168 No2002-07-302022-07-30Us
US6787531 No2000-08-312020-08-31Us
US6933395 No1997-08-112017-08-11Us
US6958326 No2001-12-202021-12-20Us
US6987101 No1997-12-222017-12-22Us
US7163931 No2001-12-202021-12-20Us
US8617597 No2010-02-082030-02-08Us
US8906890 No2011-10-222031-10-22Us
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.00225 mg/mLALOGPS
logP2.36ALOGPS
logP3.37ChemAxon
logS-5.2ALOGPS
pKa (Strongest Basic)-5ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area43.37 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity101.68 m3·mol-1ChemAxon
Polarizability41.81 Å3ChemAxon
Number of Rings7ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (37.1 KB)
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as spironolactones and derivatives. These are steroid lactones with a structure based on the spironolactone skeleton.
KingdomOrganic compounds
Super ClassLipids and lipid-like molecules
ClassSteroids and steroid derivatives
Sub ClassSteroid lactones
Direct ParentSpironolactones and derivatives
Alternative Parents
Substituents
  • Spironolactone
  • Gamma butyrolactone
  • Oxolane
  • Cyclic ketone
  • Lactone
  • Ketone
  • Carboxylic acid ester
  • Oxacycle
  • Organoheterocyclic compound
  • Monocarboxylic acid or derivatives
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Carbonyl group
  • Aliphatic heteropolycyclic compound
Molecular FrameworkAliphatic heteropolycyclic compounds
External Descriptors

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Zinc ion binding
Specific Function:
The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Progesterone receptor isoform B (PRB) is involved activation of c-SRC/MAPK signaling on hormone stimulation.Isoform A: inactive in stimulating c-Src/MAPK signaling on hormone stimulation.Isoform 4: Increases mitochondrial ...
Gene Name:
PGR
Uniprot ID:
P06401
Molecular Weight:
98979.96 Da
References
  1. Krattenmacher R: Drospirenone: pharmacology and pharmacokinetics of a unique progestogen. Contraception. 2000 Jul;62(1):29-38. [PubMed:11024226 ]
  2. Bray JD, Jelinsky S, Ghatge R, Bray JA, Tunkey C, Saraf K, Jacobsen BM, Richer JK, Brown EL, Winneker RC, Horwitz KB, Lyttle CR: Quantitative analysis of gene regulation by seven clinically relevant progestins suggests a highly similar mechanism of action through progesterone receptors in T47D breast cancer cells. J Steroid Biochem Mol Biol. 2005 Dec;97(4):328-41. Epub 2005 Sep 12. [PubMed:16157482 ]
  3. Fuhrmann U, Krattenmacher R, Slater EP, Fritzemeier KH: The novel progestin drospirenone and its natural counterpart progesterone: biochemical profile and antiandrogenic potential. Contraception. 1996 Oct;54(4):243-51. [PubMed:8922878 ]
  4. Arias-Loza PA, Hu K, Schafer A, Bauersachs J, Quaschning T, Galle J, Jazbutyte V, Neyses L, Ertl G, Fritzemeier KH, Hegele-Hartung C, Pelzer T: Medroxyprogesterone acetate but not drospirenone ablates the protective function of 17 beta-estradiol in aldosterone salt-treated rats. Hypertension. 2006 Nov;48(5):994-1001. Epub 2006 Sep 25. [PubMed:17000933 ]
  5. Sitruk-Ware R: New progestagens for contraceptive use. Hum Reprod Update. 2006 Mar-Apr;12(2):169-78. Epub 2005 Nov 16. [PubMed:16291771 ]
  6. Sitruk-Ware R: New progestogens: a review of their effects in perimenopausal and postmenopausal women. Drugs Aging. 2004;21(13):865-83. [PubMed:15493951 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Zinc ion binding
Specific Function:
Receptor for both mineralocorticoids (MC) such as aldosterone and glucocorticoids (GC) such as corticosterone or cortisol. Binds to mineralocorticoid response elements (MRE) and transactivates target genes. The effect of MC is to increase ion and water transport and thus raise extracellular fluid volume and blood pressure and lower potassium levels.
Gene Name:
NR3C2
Uniprot ID:
P08235
Molecular Weight:
107066.575 Da
References
  1. Krattenmacher R: Drospirenone: pharmacology and pharmacokinetics of a unique progestogen. Contraception. 2000 Jul;62(1):29-38. [PubMed:11024226 ]
  2. Fuhrmann U, Krattenmacher R, Slater EP, Fritzemeier KH: The novel progestin drospirenone and its natural counterpart progesterone: biochemical profile and antiandrogenic potential. Contraception. 1996 Oct;54(4):243-51. [PubMed:8922878 ]
  3. Muhn P, Fuhrmann U, Fritzemeier KH, Krattenmacher R, Schillinger E: Drospirenone: a novel progestogen with antimineralocorticoid and antiandrogenic activity. Ann N Y Acad Sci. 1995 Jun 12;761:311-35. [PubMed:7625729 ]
  4. Oelkers WK: Effects of estrogens and progestogens on the renin-aldosterone system and blood pressure. Steroids. 1996 Apr;61(4):166-71. [PubMed:8732994 ]
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Zinc ion binding
Specific Function:
Steroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Transcription factor activity is modulated by bound coactivator and corepressor proteins. Transcription activation is down-regulated by NR0B2. Activated, but not phosphorylated, by HIPK3 and ZIPK/DAPK3.
Gene Name:
AR
Uniprot ID:
P10275
Molecular Weight:
98987.9 Da
References
  1. Krattenmacher R: Drospirenone: pharmacology and pharmacokinetics of a unique progestogen. Contraception. 2000 Jul;62(1):29-38. [PubMed:11024226 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Prostaglandin-endoperoxide synthase activity
Specific Function:
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Constitutively expressed in some tissues in physiological conditions, such as the endothelium, kidney and brain, and in pathological conditions, such as in cancer. PTGS2 is responsible for production of inflammatory prostaglandins. Up-regulation of PTGS2 is also associated with increased cell adhesion, p...
Gene Name:
PTGS2
Uniprot ID:
P35354
Molecular Weight:
68995.625 Da
References
  1. Maia H Jr, Casoy J, Athayde C, Valente Filho J, Coutinho EM: The effect of a continuous regimen of drospirenone 3 mg/ethinylestradiol 30 microg on Cox-2 and Ki-67 expression in the endometrium. Eur J Contracept Reprod Health Care. 2010 Feb;15(1):35-40. doi: 10.3109/13625180903383928. [PubMed:20063991 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Identical protein binding
Specific Function:
Esterase with broad substrate specificity. Contributes to the inactivation of the neurotransmitter acetylcholine. Can degrade neurotoxic organophosphate esters.
Gene Name:
BCHE
Uniprot ID:
P06276
Molecular Weight:
68417.575 Da
References
  1. Koitka M, Hochel J, Gieschen H, Borchert HH: Improving the ex vivo stability of drug ester compounds in rat and dog serum: inhibition of the specific esterases and implications on their identity. J Pharm Biomed Anal. 2010 Feb 5;51(3):664-78. doi: 10.1016/j.jpba.2009.09.023. Epub 2009 Sep 23. [PubMed:19850433 ]
Comments
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Drug created on July 08, 2007 11:03 / Updated on December 02, 2016 02:43