Peringatan Keamanan

The oral LD50 of drospirenone in rats is >2000 mg/kg.L7994

Overdose information
An overdose of drospirenone, like other oral contraceptives, may lead to cause nausea or withdrawal bleeding. For drospirenone in particular, as an analog of spironolactone, may affect the levels of serum sodium and potassium. Their concentrations should be monitored in cases of overdose in addition to monitoring from metabolic acidosis and hyperkalemia, which may also result.A182600,L7973

Drospirenone

DB01395

small molecule approved

Deskripsi

Drospirenone is a synthetic progestin commonly found in the popular oral contraceptive, Yaz in combination with Ethinyl estradiol.L7973 Most recently, it was approved by both Health Canada and the FDA in combination with Estetrol as an oral contraceptive therapy.L33199,L33174 Aside from its contraceptive effects, drospirenone is used with estrogens to control acne and premenstrual dysphoric disorder (PMDD).

Drospirenone has been the subject of widespread safety concern due to the possibility of an increased risk of venous thromboembolism associated with its use.A182543,A182552 In 2012, however, a safety statement by the FDA concluded that the increase in the risk of thromboembolism resulting from the use of drospirenone remains unclear, as studies regarding this risk are conflicting. Some studies have demonstrated a significantly increased risk and some demonstrating no risk of thromboembolic events. In its statement, the FDA has mentioned that increased risk of venous thromboembolism with oral contraceptives such as drospirenone exists but remains lower than the risk of this condition during pregnancy and during the postpartum period, and this should be considered when assessing potential risks of hormonal contraceptive use.L7979

Struktur Molekul 2D

Berat 366.4932
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The serum half-life of drospirenone is estimated to be 30 hours.[A182591] The half-life of drospirenone metabolite excretion in the urine and feces is approximately 40 hours.[L7997]
Volume Distribusi The volume of distribution of drospirenone is estimated to be 4 L/kg, according to the FDA label for Yaz.[L7973] Prescribing information from a combination of estradiol and drospirenone estimates the volume of distribution to range from 3.7- 4.2 L/kg.[L7997]
Klirens (Clearance) Drospirenone is rapidly cleared, typically within 2-3 days of administration of the last active tablet.[A182597] The rate of clearance of drospirenone calculated in the serum ranges from 1.2-1.5 ml/min/kg, however, this value can vary by up to 25% according to the patient.[L7997]

Absorpsi

The absolute bioavailability of drospirenone is approximately 76% due to first-pass effects.A182591,L7973 The maximum plasma concentration of drospirenone occurs within 1 to 2 hours after oral administration and is estimated to range between 60 and 87 ng/mL.A2439 A European prescribing monograph for the combination product of estradiol and drospirenone indicates that drospirenone is both completely and rapidly absorbed. It reports a Cmax of 21.9 ng/ml, achieved approximately 1-hour post-administration. The absolute bioavailability is reported to range between 76 to 85%.L7997

Metabolisme

Drospirenone is heavily metabolized. The two major inactive metabolites identified are the acid form of drospirenone produced by the opening of its lactone ring, known as M11, and the 4,5-dihydro-drospirenone-3-sulfate (M14).A2439,A182591 Drospirenone also undergoes oxidative metabolism via the hepatic cytochrome enzyme CYP3A4.A183044,A35775,L7997

Rute Eliminasi

Various metabolites of drospirenone are measured in the urine and feces. Drospirenone elimination from the body is almost after 10 days post-administrationA2439 when negligible amounts of drospirenone are found unchanged in both the urine and feces.L7997 Between 38% to 47% of the metabolites are identified as glucuronide and sulfate conjugates in the urine. In the feces, approximately 17% to 20% of identifiable metabolites are found to be excreted as glucuronides and sulfates.A2439

Interaksi Makanan

3 Data
  • 1. Avoid St. John's Wort.
  • 2. Take at the same time every day.
  • 3. Take with or without food.

Interaksi Obat

1539 Data
Phenytoin The metabolism of Drospirenone can be increased when combined with Phenytoin.
Fosphenytoin The metabolism of Drospirenone can be increased when combined with Fosphenytoin.
Valsartan The risk or severity of hyperkalemia can be increased when Valsartan is combined with Drospirenone.
Olmesartan The risk or severity of hyperkalemia can be increased when Olmesartan is combined with Drospirenone.
Losartan The risk or severity of hyperkalemia can be increased when Losartan is combined with Drospirenone.
Candesartan cilexetil The risk or severity of hyperkalemia can be increased when Candesartan cilexetil is combined with Drospirenone.
Eprosartan The risk or severity of hyperkalemia can be increased when Eprosartan is combined with Drospirenone.
Telmisartan The risk or severity of hyperkalemia can be increased when Telmisartan is combined with Drospirenone.
Irbesartan The risk or severity of hyperkalemia can be increased when Irbesartan is combined with Drospirenone.
Forasartan The risk or severity of hyperkalemia can be increased when Forasartan is combined with Drospirenone.
Saprisartan The risk or severity of hyperkalemia can be increased when Saprisartan is combined with Drospirenone.
Tasosartan The risk or severity of hyperkalemia can be increased when Tasosartan is combined with Drospirenone.
Saralasin The risk or severity of hyperkalemia can be increased when Saralasin is combined with Drospirenone.
Azilsartan medoxomil The risk or severity of hyperkalemia can be increased when Azilsartan medoxomil is combined with Drospirenone.
Fimasartan The risk or severity of hyperkalemia can be increased when Fimasartan is combined with Drospirenone.
Candesartan The risk or severity of hyperkalemia can be increased when Candesartan is combined with Drospirenone.
Ramipril Ramipril may increase the hyperkalemic activities of Drospirenone.
Fosinopril Fosinopril may increase the hyperkalemic activities of Drospirenone.
Trandolapril Trandolapril may increase the hyperkalemic activities of Drospirenone.
Benazepril Benazepril may increase the hyperkalemic activities of Drospirenone.
Enalapril Enalapril may increase the hyperkalemic activities of Drospirenone.
Moexipril Moexipril may increase the hyperkalemic activities of Drospirenone.
Lisinopril Lisinopril may increase the hyperkalemic activities of Drospirenone.
Perindopril Perindopril may increase the hyperkalemic activities of Drospirenone.
Quinapril Quinapril may increase the hyperkalemic activities of Drospirenone.
Omapatrilat Omapatrilat may increase the hyperkalemic activities of Drospirenone.
Rescinnamine Rescinnamine may increase the hyperkalemic activities of Drospirenone.
Captopril Captopril may increase the hyperkalemic activities of Drospirenone.
Cilazapril Cilazapril may increase the hyperkalemic activities of Drospirenone.
Spirapril Spirapril may increase the hyperkalemic activities of Drospirenone.
Temocapril Temocapril may increase the hyperkalemic activities of Drospirenone.
Imidapril Imidapril may increase the hyperkalemic activities of Drospirenone.
Zofenopril Zofenopril may increase the hyperkalemic activities of Drospirenone.
Delapril Delapril may increase the hyperkalemic activities of Drospirenone.
Benazeprilat Benazeprilat may increase the hyperkalemic activities of Drospirenone.
Fosinoprilat Fosinoprilat may increase the hyperkalemic activities of Drospirenone.
Ramiprilat Ramiprilat may increase the hyperkalemic activities of Drospirenone.
Trandolaprilat Trandolaprilat may increase the hyperkalemic activities of Drospirenone.
Moexiprilat Moexiprilat may increase the hyperkalemic activities of Drospirenone.
Perindoprilat Perindoprilat may increase the hyperkalemic activities of Drospirenone.
Quinaprilat Quinaprilat may increase the hyperkalemic activities of Drospirenone.
Cilazaprilat Cilazaprilat may increase the hyperkalemic activities of Drospirenone.
Acitretin The therapeutic efficacy of Drospirenone can be decreased when used in combination with Acitretin.
Atazanavir The serum concentration of Drospirenone can be increased when it is combined with Atazanavir.
Boceprevir The serum concentration of Drospirenone can be increased when it is combined with Boceprevir.
Prucalopride The serum concentration of Drospirenone can be decreased when it is combined with Prucalopride.
Sugammadex The serum concentration of Drospirenone can be decreased when it is combined with Sugammadex.
Thalidomide Drospirenone may increase the thrombogenic activities of Thalidomide.
Ulipristal The therapeutic efficacy of Drospirenone can be decreased when used in combination with Ulipristal.
Icosapent The risk or severity of hyperkalemia can be increased when Icosapent is combined with Drospirenone.
Mesalazine The risk or severity of hyperkalemia can be increased when Mesalazine is combined with Drospirenone.
Nabumetone The risk or severity of hyperkalemia can be increased when Nabumetone is combined with Drospirenone.
Ketorolac The risk or severity of hyperkalemia can be increased when Ketorolac is combined with Drospirenone.
Tenoxicam The risk or severity of hyperkalemia can be increased when Tenoxicam is combined with Drospirenone.
Celecoxib The risk or severity of hyperkalemia can be increased when Celecoxib is combined with Drospirenone.
Tolmetin The risk or severity of hyperkalemia can be increased when Tolmetin is combined with Drospirenone.
Rofecoxib The risk or severity of hyperkalemia can be increased when Rofecoxib is combined with Drospirenone.
Piroxicam The risk or severity of hyperkalemia can be increased when Piroxicam is combined with Drospirenone.
Fenoprofen The risk or severity of hyperkalemia can be increased when Fenoprofen is combined with Drospirenone.
Valdecoxib The risk or severity of hyperkalemia can be increased when Valdecoxib is combined with Drospirenone.
Diclofenac The risk or severity of hyperkalemia can be increased when Diclofenac is combined with Drospirenone.
Sulindac The risk or severity of hyperkalemia can be increased when Sulindac is combined with Drospirenone.
Flurbiprofen The risk or severity of hyperkalemia can be increased when Flurbiprofen is combined with Drospirenone.
Etodolac The risk or severity of hyperkalemia can be increased when Etodolac is combined with Drospirenone.
Mefenamic acid The risk or severity of hyperkalemia can be increased when Mefenamic acid is combined with Drospirenone.
Naproxen The risk or severity of hyperkalemia can be increased when Naproxen is combined with Drospirenone.
Sulfasalazine The risk or severity of hyperkalemia can be increased when Sulfasalazine is combined with Drospirenone.
Phenylbutazone The risk or severity of hyperkalemia can be increased when Phenylbutazone is combined with Drospirenone.
Meloxicam The risk or severity of hyperkalemia can be increased when Meloxicam is combined with Drospirenone.
Carprofen The risk or severity of hyperkalemia can be increased when Carprofen is combined with Drospirenone.
Diflunisal The risk or severity of hyperkalemia can be increased when Diflunisal is combined with Drospirenone.
Salicylic acid The risk or severity of hyperkalemia can be increased when Salicylic acid is combined with Drospirenone.
Meclofenamic acid The risk or severity of hyperkalemia can be increased when Meclofenamic acid is combined with Drospirenone.
Oxaprozin The risk or severity of hyperkalemia can be increased when Oxaprozin is combined with Drospirenone.
Ketoprofen The risk or severity of hyperkalemia can be increased when Ketoprofen is combined with Drospirenone.
Balsalazide The risk or severity of hyperkalemia can be increased when Balsalazide is combined with Drospirenone.
Ibuprofen The risk or severity of hyperkalemia can be increased when Ibuprofen is combined with Drospirenone.
Lumiracoxib The risk or severity of hyperkalemia can be increased when Lumiracoxib is combined with Drospirenone.
Magnesium salicylate The risk or severity of hyperkalemia can be increased when Magnesium salicylate is combined with Drospirenone.
Salsalate The risk or severity of hyperkalemia can be increased when Salsalate is combined with Drospirenone.
Choline magnesium trisalicylate The risk or severity of hyperkalemia can be increased when Choline magnesium trisalicylate is combined with Drospirenone.
Antrafenine The risk or severity of hyperkalemia can be increased when Antrafenine is combined with Drospirenone.
Aminophenazone The risk or severity of hyperkalemia can be increased when Aminophenazone is combined with Drospirenone.
Antipyrine The risk or severity of hyperkalemia can be increased when Antipyrine is combined with Drospirenone.
Tiaprofenic acid The risk or severity of hyperkalemia can be increased when Tiaprofenic acid is combined with Drospirenone.
Etoricoxib The risk or severity of hyperkalemia can be increased when Etoricoxib is combined with Drospirenone.
Taxifolin The risk or severity of hyperkalemia can be increased when Taxifolin is combined with Drospirenone.
Oxyphenbutazone The risk or severity of hyperkalemia can be increased when Oxyphenbutazone is combined with Drospirenone.
Licofelone The risk or severity of hyperkalemia can be increased when Licofelone is combined with Drospirenone.
Nimesulide The risk or severity of hyperkalemia can be increased when Nimesulide is combined with Drospirenone.
Benoxaprofen The risk or severity of hyperkalemia can be increased when Benoxaprofen is combined with Drospirenone.
Metamizole The risk or severity of hyperkalemia can be increased when Drospirenone is combined with Metamizole.
Zomepirac The risk or severity of hyperkalemia can be increased when Zomepirac is combined with Drospirenone.
Cimicoxib The risk or severity of hyperkalemia can be increased when Cimicoxib is combined with Drospirenone.
Lornoxicam The risk or severity of hyperkalemia can be increased when Lornoxicam is combined with Drospirenone.
Aceclofenac The risk or severity of hyperkalemia can be increased when Aceclofenac is combined with Drospirenone.
Zaltoprofen The risk or severity of hyperkalemia can be increased when Zaltoprofen is combined with Drospirenone.
Azapropazone The risk or severity of hyperkalemia can be increased when Azapropazone is combined with Drospirenone.
Parecoxib The risk or severity of hyperkalemia can be increased when Parecoxib is combined with Drospirenone.
Salicylamide The risk or severity of hyperkalemia can be increased when Salicylamide is combined with Drospirenone.

Target Protein

Mineralocorticoid receptor NR3C2
Androgen receptor AR
Progesterone receptor PGR
Glucocorticoid receptor NR3C1

Referensi & Sumber

Synthesis reference: DOI: 10.1002/cjoc.201201147
Artikel (PubMed)
  • PMID: 11024226
    Krattenmacher R: Drospirenone: pharmacology and pharmacokinetics of a unique progestogen. Contraception. 2000 Jul;62(1):29-38.
  • PMID: 23577032
    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.
  • PMID: 28276140
    Larivee N, Suissa S, Khosrow-Khavar F, Tagalakis V, Filion KB: Drospirenone-containing oral contraceptive pills and the risk of venous thromboembolism: a systematic review of observational studies. BJOG. 2017 Sep;124(10):1490-1499. doi: 10.1111/1471-0528.14623. Epub 2017 May 5.
  • PMID: 29573722
    Oedingen C, Scholz S, Razum O: Systematic review and meta-analysis of the association of combined oral contraceptives on the risk of venous thromboembolism: The role of the progestogen type and estrogen dose. Thromb Res. 2018 May;165:68-78. doi: 10.1016/j.thromres.2018.03.005. Epub 2018 Mar 15.
  • PMID: 27923166
    Li J, Ren J, Sun W: A comparative systematic review of Yasmin (drospirenone pill) versus standard treatment options for symptoms of polycystic ovary syndrome. Eur J Obstet Gynecol Reprod Biol. 2017 Mar;210:13-21. doi: 10.1016/j.ejogrb.2016.11.013. Epub 2016 Nov 16.
  • PMID: 22336820
    Lopez LM, Kaptein AA, Helmerhorst FM: Oral contraceptives containing drospirenone for premenstrual syndrome. Cochrane Database Syst Rev. 2012 Feb 15;(2):CD006586. doi: 10.1002/14651858.CD006586.pub4.
  • PMID: 23090561
    Authors unspecified: ACOG Committee Opinion Number 540: Risk of venous thromboembolism among users of drospirenone-containing oral contraceptive pills. Obstet Gynecol. 2012 Nov;120(5):1239-42. doi: http://10.1097/AOG.0b013e318277c93b.
  • PMID: 27593335
    Kluft C, Zimmerman Y, Mawet M, Klipping C, Duijkers IJ, Neuteboom J, Foidart JM, Bennink HC: Reduced hemostatic effects with drospirenone-based oral contraceptives containing estetrol vs. ethinyl estradiol. Contraception. 2017 Feb;95(2):140-147. doi: 10.1016/j.contraception.2016.08.018. Epub 2016 Sep 1.
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