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Identification
NameDrospirenone
Accession NumberDB01395
TypeSmall Molecule
GroupsApproved
Description

Drospirenone 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 21Famy Care Ltd
Drospirenone and Ethinyl Estradiol Tablets 28Famy Care Ltd
Drospirenone and Ethinyl Estradiol Tablets USP (21-day Regimen)Glenmark Generics Canada Inc
Drospirenone and Ethinyl Estradiol Tablets USP (28-day Regimen)Glenmark Generics Canada Inc
GianviTeva Pharmaceuticals USA Inc
LorynaSandoz Inc
MyaApotex Inc
NikkiLupin Pharmaceuticals, Inc.
OcellaBarr Laboratories, Inc.
Qismette 21LUPIN LIMITED
Qismette 28LUPIN LIMITED
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 KeyInChIKey=METQSPRSQINEEU-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
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
Pharmacology
IndicationFor the prevention of pregnancy in women who elect an oral contraceptive.
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.
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
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)
SpectraNot Available
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 CodesG03AA12G03AC10G03FA17
AHFS Codes
  • 68:12
PDB EntriesNot Available
FDA labelDownload (292 KB)
MSDSDownload (567 KB)
Interactions
Drug Interactions
Drug
AbciximabDrospirenone may decrease the anticoagulant activities of Abciximab.
AcenocoumarolDrospirenone may decrease the anticoagulant activities of Acenocoumarol.
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Drospirenone.
AliskirenDrospirenone may increase the hyperkalemic activities of Aliskiren.
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Drospirenone.
AmilorideDrospirenone may increase the hyperkalemic activities of Amiloride.
Anthrax immune globulinDrospirenone may increase the thrombogenic activities of Anthrax immune globulin.
Azilsartan medoxomilAzilsartan medoxomil may increase the hyperkalemic activities of Drospirenone.
BenazeprilBenazepril may increase the hyperkalemic activities of Drospirenone.
BexaroteneThe serum concentration of Drospirenone can be decreased when it is combined with Bexarotene.
BoceprevirThe serum concentration of Drospirenone can be increased when it is combined with Boceprevir.
ButabarbitalThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Butabarbital.
ButethalThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Butethal.
C1 Esterase Inhibitor (Human)Drospirenone may increase the thrombogenic activities of C1 Esterase Inhibitor (Human).
CanagliflozinThe therapeutic efficacy of Canagliflozin can be decreased when used in combination with Drospirenone.
CandesartanCandesartan may increase the hyperkalemic activities of Drospirenone.
CapromabDrospirenone may decrease effectiveness of Capromab as a diagnostic agent.
CaptoprilCaptopril may increase the hyperkalemic activities of Drospirenone.
CarbamazepineThe metabolism of Drospirenone can be increased when combined with Carbamazepine.
CelecoxibCelecoxib may increase the hyperkalemic activities of Drospirenone.
CeritinibThe serum concentration of Drospirenone can be increased when it is combined with Ceritinib.
ChlorpropamideThe therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Drospirenone.
CilazaprilCilazapril may increase the hyperkalemic activities of Drospirenone.
Citric AcidDrospirenone may decrease the anticoagulant activities of Citric Acid.
ClarithromycinThe serum concentration of Drospirenone can be increased when it is combined with Clarithromycin.
ColesevelamThe serum concentration of Drospirenone can be decreased when it is combined with Colesevelam.
Cyproterone acetateThe serum concentration of Drospirenone can be decreased when it is combined with Cyproterone acetate.
DalteparinDrospirenone may decrease the anticoagulant activities of Dalteparin.
DiclofenacDiclofenac may increase the hyperkalemic activities of Drospirenone.
DicoumarolDrospirenone may decrease the anticoagulant activities of Dicoumarol.
DiflunisalDiflunisal may increase the hyperkalemic activities of Drospirenone.
Edetic AcidDrospirenone may decrease the anticoagulant activities of Edetic Acid.
EnalaprilEnalapril may increase the hyperkalemic activities of Drospirenone.
EnalaprilatEnalaprilat may increase the hyperkalemic activities of Drospirenone.
EnoxaparinDrospirenone may decrease the anticoagulant activities of Enoxaparin.
EplerenoneDrospirenone may increase the hyperkalemic activities of Eplerenone.
EprosartanEprosartan may increase the hyperkalemic activities of Drospirenone.
Eslicarbazepine acetateThe serum concentration of Drospirenone can be decreased when it is combined with Eslicarbazepine acetate.
Ethyl biscoumacetateDrospirenone may decrease the anticoagulant activities of Ethyl biscoumacetate.
EtodolacEtodolac may increase the hyperkalemic activities of Drospirenone.
FenoprofenFenoprofen may increase the hyperkalemic activities of Drospirenone.
FloctafenineFloctafenine may increase the hyperkalemic activities of Drospirenone.
FludrocortisoneThe serum concentration of Fludrocortisone can be increased when it is combined with Drospirenone.
FlurbiprofenFlurbiprofen may increase the hyperkalemic activities of Drospirenone.
Fondaparinux sodiumDrospirenone may decrease the anticoagulant activities of Fondaparinux sodium.
FosinoprilFosinopril may increase the hyperkalemic activities of Drospirenone.
GliclazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Drospirenone.
GlimepirideThe therapeutic efficacy of Glimepiride can be decreased when used in combination with Drospirenone.
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Drospirenone.
GlyburideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Drospirenone.
HeparinDrospirenone may decrease the anticoagulant activities of Heparin.
HeptabarbitalThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Heptabarbital.
HexobarbitalThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Hexobarbital.
IbuprofenIbuprofen may increase the hyperkalemic activities of Drospirenone.
IdelalisibThe serum concentration of Drospirenone can be increased when it is combined with Idelalisib.
IndinavirThe serum concentration of Drospirenone can be increased when it is combined with Indinavir.
IndomethacinIndomethacin may increase the hyperkalemic activities of Drospirenone.
InfliximabInfliximab may increase the hyperkalemic activities of Drospirenone.
Insulin AspartThe therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Drospirenone.
Insulin DetemirThe therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Drospirenone.
Insulin GlargineThe therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Drospirenone.
Insulin GlulisineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Drospirenone.
Insulin HumanThe therapeutic efficacy of Insulin Regular can be decreased when used in combination with Drospirenone.
Insulin LisproThe therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Drospirenone.
IrbesartanIrbesartan may increase the hyperkalemic activities of Drospirenone.
ItraconazoleThe serum concentration of Drospirenone can be increased when it is combined with Itraconazole.
KetoconazoleThe serum concentration of Drospirenone can be increased when it is combined with Ketoconazole.
KetoprofenKetoprofen may increase the hyperkalemic activities of Drospirenone.
KetorolacKetorolac may increase the hyperkalemic activities of Drospirenone.
LinagliptinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Drospirenone.
LiothyronineThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Drospirenone.
LisinoprilLisinopril may increase the hyperkalemic activities of Drospirenone.
LosartanLosartan may increase the hyperkalemic activities of Drospirenone.
LumacaftorThe serum concentration of Drospirenone can be decreased when it is combined with Lumacaftor.
Mefenamic acidMefenamic acid may increase the hyperkalemic activities of Drospirenone.
MeloxicamMeloxicam may increase the hyperkalemic activities of Drospirenone.
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Drospirenone.
MethohexitalThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Methohexital.
MoexiprilMoexipril may increase the hyperkalemic activities of Drospirenone.
NabumetoneNabumetone may increase the hyperkalemic activities of Drospirenone.
NaproxenNaproxen may increase the hyperkalemic activities of Drospirenone.
NefazodoneThe serum concentration of Drospirenone can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Drospirenone can be increased when it is combined with Nelfinavir.
OlmesartanOlmesartan may increase the hyperkalemic activities of Drospirenone.
OxaprozinOxaprozin may increase the hyperkalemic activities of Drospirenone.
PentobarbitalThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Pentobarbital.
PerindoprilPerindopril may increase the hyperkalemic activities of Drospirenone.
PhenindioneDrospirenone may decrease the anticoagulant activities of Phenindione.
PhenprocoumonDrospirenone may decrease the anticoagulant activities of Phenprocoumon.
PhenytoinThe metabolism of Drospirenone can be increased when combined with Phenytoin.
PiroxicamPiroxicam may increase the hyperkalemic activities of Drospirenone.
PosaconazoleThe serum concentration of Drospirenone can be increased when it is combined with Posaconazole.
PrimidoneThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Primidone.
QuinaprilQuinapril may increase the hyperkalemic activities of Drospirenone.
RamiprilRamipril may increase the hyperkalemic activities of Drospirenone.
RepaglinideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Drospirenone.
RifabutinThe serum concentration of Drospirenone can be decreased when it is combined with Rifabutin.
RitonavirThe serum concentration of Drospirenone can be increased when it is combined with Ritonavir.
SaquinavirThe serum concentration of Drospirenone can be increased when it is combined with Saquinavir.
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Drospirenone.
SecobarbitalThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Secobarbital.
SpironolactoneDrospirenone may increase the hyperkalemic activities of Spironolactone.
St. John's WortThe therapeutic efficacy of Drospirenone can be decreased when used in combination with St. John's Wort.
SulindacSulindac may increase the hyperkalemic activities of Drospirenone.
SulodexideDrospirenone may decrease the anticoagulant activities of Sulodexide.
TelithromycinThe serum concentration of Drospirenone can be increased when it is combined with Telithromycin.
TelmisartanTelmisartan may increase the hyperkalemic activities of Drospirenone.
TesmilifeneThe serum concentration of Drospirenone can be decreased when it is combined with Tesmilifene.
TheophyllineThe serum concentration of Theophylline can be increased when it is combined with Drospirenone.
Tiaprofenic acidTiaprofenic acid may increase the hyperkalemic activities of Drospirenone.
TolbutamideThe therapeutic efficacy of Tolbutamide can be decreased when used in combination with Drospirenone.
TolmetinTolmetin may increase the hyperkalemic activities of Drospirenone.
TrandolaprilTrandolapril may increase the hyperkalemic activities of Drospirenone.
TreprostinilDrospirenone may decrease the anticoagulant activities of Treprostinil.
TriamtereneDrospirenone may increase the hyperkalemic activities of Triamterene.
ValsartanValsartan may increase the hyperkalemic activities of Drospirenone.
VerapamilThe serum concentration of Drospirenone can be increased when it is combined with Verapamil.
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Drospirenone.
Vitamin CThe serum concentration of Drospirenone can be increased when it is combined with Vitamin C.
VoriconazoleThe serum concentration of Drospirenone can be increased when it is combined with Voriconazole.
WarfarinDrospirenone may decrease the anticoagulant activities of Warfarin.
Food Interactions
  • Food reduces the rate of absorption, but not the extent of absorption.

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 July 24, 2016 01:52