Description

Simple

A medication used in birth control pills.

Clinical

A progestin used in oral contraceptive pills for the prevention of pregnancy and other conditions.

Overview

Drospirenone is a synthetic progestin commonly found in the popular oral contraceptive, Yaz in combination with [Ethinyl estradiol].[19] 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.[4,7] 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.... Read more

Pharmacology

Indication

Drospirenone, in combination with ethinyl estradiol, is indicated as an oral contraceptive for the prevention of pregnancy. In addition to its use for contraceptive effects, this combination is used to treat moderate acne vulgaris and the symptoms of premenstrual dysphoric disorder.[ Read more

Pharmacodynamic

Drospirenone inhibits the maturation of follicles and inhibits ovulation, preventing pregnancy. It has antiandrogen effects, improving acne and hirsutism. When combined with ethinyl estradiol, it has been shown to have favorable effects on the plasma lipid profile.[ Read more

Mechanism of action

Drospirenone and ethinyl estradiol in combination suppress the release of follicle stimulating hormone (FSH) and luteinizing hormone (LH), preventing ovulation. Other changes induced by this drug which may aid in the prevention of pregnancy include alterations in cervical mucus consistency, hinderin... Read more

Absorption

The absolute bioavailability of drospirenone is approximately 76% due to first-pass effects.[13, Read more

Protein binding

Drospirenone is about 95% to 97% bound to serum plasma protein, likely to albumin.[1] During in vitro studies, d... Read more

Volume of distribution

The volume of distribution of drospirenone is estimated to be 4 L/kg, according to the FDA label for Yaz.[19] Prescribing information from a combination of estradiol and drospirenone estimates the volume of distribution to ra... Read more

Clearance

Drospirenone is rapidly cleared, typically within 2-3 days of administration of the last active tablet.[ Read more

Half life

The serum half-life of drospirenone is estimated to be 30 hours.[13] The half-life of drospirenone meta... Read more

Route of elimination

Various metabolites of drospirenone are measured in the urine and feces. Drospirenone elimination from the body is almost after 10 days post-administration[ Read more

Toxicity

The oral LD50 of drospirenone in rats is >2000 mg/kg.[22]

Overdose information
An overdose of drospirenone, like other oral contraceptives, may lead to cause nausea or withdrawal bleeding. For dros... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Breast discomfort US
  • adult
  • Kind: experimental
    • Percent: 18%
  • Clinical Trial
    Breast Pain US
    • adult
  • Kind: experimental
    • Percent: 18%
  • Clinical Trial
    Female genital tract bleeding US
    • adult
  • Kind: experimental
    • Percent: 14%
  • Clinical Trial
    Abdominal Pain US
    • adult
  • Kind: experimental
    • Percent: 7%
  • Clinical Trial
    Gastrointestinal pain US
    • adult
  • Kind: experimental
    • Percent: 7%
  • Clinical Trial
    Gastrointestinal pain US
    • adult
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Abdominal Pain US
    • adult
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Headache US
    • adult
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Vulvovaginal fungal infections US
    • adult
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Breast discomfort US
    • adult
  • Kind: experimental
    • Percent: 6%
  • Clinical Trial
    Breast Pain US
    • adult
  • Kind: experimental
    • Percent: 6%
  • Clinical Trial
    Abdominal Pain US
    • adult
  • Kind: experimental
    • Percent: 4%
  • Clinical Trial
    Gastrointestinal pain US
    • adult
  • Kind: experimental
    • Percent: 4%
  • Clinical Trial
    Acne US
  • Kind: experimental
    • Percent: 3.8
  • Clinical Trial
    Breast Pain US
    • adult
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Nausea US
    • adult
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Female genital tract bleeding US
    • adult
  • Kind: experimental
    • Percent: 3%
  • Clinical Trial
    Metrorrhagia US
  • Kind: experimental
    • Percent: 2.8
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 2.7
  • Clinical Trial
    Breast Pain US
  • Kind: experimental
    • Percent: 2.2
  • Clinical Trial
    Diarrhea US
    • adult
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Peripheral Edema US
    • adult
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Dysmenorrhea US
  • Kind: experimental
    • Percent: 1.9
  • Clinical Trial
    Weight increased US
  • Kind: experimental
    • Percent: 1.9
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 1.8
  • Clinical Trial
    Vaginal hemorrhage US
  • Kind: experimental
    • Percent: 1.7
  • Clinical Trial
    Libido decreased US
  • Kind: experimental
    • Percent: 1.3
  • Clinical Trial
    Menstruation irregular US
  • Kind: experimental
    • Percent: 1.2
  • Clinical Trial
    Breast tenderness US
  • Kind: experimental
    • Percent: 1.2
  • Clinical Trial
    Migraine US
    • adult
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Emotional Lability US
    • adult
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Cervical polyp US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Cervical polyp US
    • adult
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Migraine US
    • adult
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Emotional Lability US
    • adult
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Breast Cancer US
    Post Marketing
    Urticaria US
    Post Marketing
    Pruritus US
    Post Marketing
    Rash US
    Post Marketing
    Hypersensitivity reactions US
    Post Marketing
    Myocardial infarction/ cerebral infarction US
    Post Marketing
    Stroke US
    Post Marketing
    Thrombosis US
    Post Marketing
    Embolism and infarction US
    Post Marketing
    Embolism US
    Post Marketing
    Pulmonary vascular occlusion US
    Post Marketing
    Peripheral deep venous occlusion US
    Post Marketing
    Thrombosis US
    Post Marketing
    Venous thromboembolic events US
    Post Marketing
    Arterial Thromboembolic Events US
    Post Marketing

    Contraindications

    • Regions: US
    • Patient Conditions:
        • Name: Estrogen-dependent neoplasia
        • Drugbank Id: DBCOND0107558
    • With Drugs:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977
    • Regions: US
    • Patient Conditions:
        • Name: Loss of Vision
        • Drugbank Id: DBCOND0076879
    • Patient Conditions Associated With:
        • Name: Ophthalmic vascular disease
        • Drugbank Id: DBCOND0107904
    • With Drugs:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977
    • Regions: US
    • Patient Conditions:
        • Name: Lactation
        • Drugbank Id: DBCOND0032213
    • With Drugs Coadmin:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977
    • Regions: US
    • Patient Conditions:
        • Name: Suspected pregnancy
        • Drugbank Id: DBCOND0107509
    • With Drugs:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977
    • Regions: US
    • Patient Conditions:
        • Name: Classic Migraine
        • Drugbank Id: DBCOND0032742
    • With Drugs:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977
    • Regions: US
    • Patient Conditions:
        • Name: Adrenal insuffiency
        • Drugbank Id: DBCOND0100193
    • With Drugs:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977
    • Regions: US
    • Patient Conditions:
        • Name: High risk of venous thrombotic disease
        • Drugbank Id: DBCOND0108457
    • Regions: US
    • Patient Conditions:
        • Name: High risk of arterial thrombotic disease
        • Drugbank Id: DBCOND0108456
    • With Drugs:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977
    • Regions: US
    • Patient Conditions:
        • Name: Undiagnosed abnormal uterine bleeding
        • Drugbank Id: DBCOND0107577
    • With Drugs:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977
    • Regions: US
    • Patient Conditions:
        • Name: Liver Tumors
        • Drugbank Id: DBCOND0040731
    • With Drugs:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977
    • Regions: US
    • Patient Conditions:
        • Name: Progestin-sensitive cancer
        • Drugbank Id: DBCOND0107569
    • With Drugs:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977
    • Regions: US
    • Patient Conditions:
        • Name: Renal Impairment
        • Drugbank Id: DBCOND0031781
    • With Drugs:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977
    • Regions: US
    • Patient Conditions:
        • Name: Pregnancy
        • Drugbank Id: DBCOND0018394
    • With Drugs:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977
    • Regions: EU
    • Patient Conditions:
        • Name: Porphyria
        • Drugbank Id: DBCOND0008396
    • With Drugs:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977
    • Regions: EU
    • Patient Conditions Associated With:
        • Name: Renal Failure, Chronic Renal Failure
        • Drugbank Id: DBCOND0035136
    • With Drugs:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977
    • Regions: EU
    • Patient Conditions:
        • Name: Acute Renal Insufficiency
        • Drugbank Id: DBCOND0042690
        • Modification Of:
          • Base:
            • Name: Renal Insufficiency
            • Drugbank Id: DBCOND0031387
          • Severity:
            • Includes:
              • acute
    • With Drugs:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977
    • Regions: EU
    • Patient Conditions:
        • Name: Thrombophilic disorders
        • Drugbank Id: DBCOND0107564
    • With Drugs:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977
    • Regions: EU
    • Patient Conditions:
        • Name: Abnormal liver function
        • Drugbank Id: DBCOND0094513
    • With Drugs:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977
    • Regions: EU
    • Patient Conditions:
        • Name: Acute liver disease
        • Drugbank Id: DBCOND0107479
        • Modification Of:
          • Base:
            • Name: Liver Disease
            • Drugbank Id: DBCOND0028338
          • Severity:
            • Includes:
              • acute
    • With Drugs:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977
    • Regions: EU
    • Patient Conditions:
        • Name: Recent thromboembolic event
        • Drugbank Id: DBCOND0121968
    • With Drugs:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977
    • Regions: EU
    • Patient Conditions:
        • Name: Active thromboembolic disease
        • Drugbank Id: DBCOND0107589
        • Modification Of:
          • Condition Status: active
          • Base:
            • Name: Thromboembolic Disease
            • Drugbank Id: DBCOND0039495
    • With Drugs:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977
    • Regions: EU
    • Patient Conditions:
        • Name: Venous Thromboembolism
        • Drugbank Id: DBCOND0000676
    • With Drugs:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977
    • Regions: EU
    • Patient Conditions:
        • Name: Untreated endometrial hyperplasia
        • Drugbank Id: DBCOND0121967
    • With Drugs:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977
    • Regions: EU
    • Patient Conditions:
        • Name: Suspected estrogen-dependent neoplasia
        • Drugbank Id: DBCOND0108036
    • With Drugs:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977
    • Regions: EU
    • Patient Conditions:
        • Name: Estrogen-dependent neoplasia
        • Drugbank Id: DBCOND0107558
    • With Drugs:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977
    • Regions: EU
    • Patient Conditions:
        • Name: Suspected breast cancer
        • Drugbank Id: DBCOND0108615
    • With Drugs:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977
    • Regions: EU
    • Patient Conditions:
        • Name: History of breast cancer
        • Drugbank Id: DBCOND0102794
    • With Drugs:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977
    • Regions: US
    • Patient Conditions:
        • Name: Patients above 35 years
        • Drugbank Id: DBCOND0121966
        • Name: Smoking
        • Drugbank Id: DBCOND0027935
    • With Drugs:
        • Name: Ethinylestradiol
        • Drugbank Id: DB00977

    Food Interactions

    Avoid St. John's Wort.

    Take at the same time every day.

    Take with or without food.