Drospirenone: Difference between revisions

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|IUPAC_name = (6''R'',7''R'',8''R'',9''S'',10''R'',13''S'',14''S'',15''S'',16''S'',17''S'')-<br>1,3',4',6,6a,7,8,9,10,11,12,13,14,15,15a,16-<br>hexadecahydro-10,13-dimethylspiro-<br>[17''H''-dicyclopropa-6,7:15,16]cyclopenta<br>[a]phenanthrene-17,2'(5''H'')-furan]-3,5'(2''H'')-dione)
|fdaLIADAdult======Condition1=====
| image=Drospirenone.svg
 
| CAS_number=67392-87-4
* Dosing Information
| ATC_prefix=G03
 
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:* Dosage
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| PubChem=68873
=====Condition2=====
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| C = 24 | H = 30 | O = 3
* Dosing Information
| molecular_weight = 366.493 g/mol
 
| bioavailability= 76%
:* Dosage
| metabolism = [[Liver|Hepatic]], minor ([[CYP3A4]]-mediated)
 
| elimination_half-life= 30 hours
=====Condition3=====
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| excretion = [[Kidney|Renal]] and fecal
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* Strength of Evidence:
 
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{{SI}}
{{PillImage
'''Drospirenone''' is a synthetic [[progestin]] that is an [[analog (chemistry)| analog]] to [[spironolactone]]. Its [[molecular weight]] is  366.5 and its [[molecular formula]] is C<sub>24</sub>H<sub>30</sub>O<sub>3</sub>.
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== Properties and uses ==
The compound is part of certain [[birth control]] [[oral contraceptive formulations|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 system|renin-angiotensin]]-[[aldosterone]] system, and is not [[androgen]]ic. With its activities similar to [[spironolactone]] it may lead to less water retention and breast tenderness and improved skin appearance (less [[Acne vulgaris|acne]]).


Drospirenone is taken orally with about 76% [[bioavailability]]. It is not bound by [[sex hormone binding globulin]] or [[Corticosteroid binding protein|corticosteroid binding globulin]], but by other serum proteins. Metabolites have not been shown to be biologically active, show up in urine and feces, and are essentially completely excreted within 10 days. 
<!--Label Display Image-->


The compound is part of certain newer [[oral contraceptive formulations]]:
* Yasmin® contains 3 mg drospirenone and 30 mcg [[ethinylestradiol]] per tablet. It is indicated for the prevention of pregnancy in women who elect an oral contraceptive.
* Yaz® contains 3 mg drospirenone and 20 mcg ethinylestradiol per tablet and is given for 24/4 days with the same indications.
It has also been formulated in medication to manage [[menopause|menopausal]] symptoms using 0.5 mg drsp and 1 mg [[estradiol]] per day by oral application. This medication was introduced in the USA in 2007 as Angeliq®.


Drospirenone, which can potentially cause [[hyperkalemia]] in high-risk patients, is comparable to a 25mg dose of [[spironolactone]].


The medication is contraindicated in patients with [[liver disease|hepatic dysfunction]], [[renal insufficiency]], [[adrenal insufficiency]], or in whom the use of oral contraceptives is contraindicated, such as smokers and patients with a history of [[DVT]], [[stroke]], or other blood clots. Because of the anti-mineralocorticoid effects care needs to be exercised when other drugs that may increase potassium levels are taken. Such medications include [[ACE inhibitor]]s, angiotensin-II receptor agonists, [[potassium-sparing diuretic]]s, potassium supplementation, [[heparin]], [[aldosterone antagonist]]s, and [[Non-steroidal anti-inflammatory drug|NSAID]]s.
== See also==
* [[Progestins]]
* [[Combined oral contraceptive pill]]
* [[Oral contraceptive formulations]]
* [[Hormone replacement therapy]]


==References==
* {{cite journal | author = Krattenmacher R | title = Drospirenone: pharmacology and pharmacokinetics of a unique progestogen | journal = Contraception | volume = 62 | issue = 1 | pages = 29-38 | year = 2000 | id = PMID 11024226}}
* [http://www.yasmin-us.com/index.htm Yasmin product information]
* [http://www.angeliq.com/html/index.html Angeliq product information]


==External links==
<!--Category-->
* [http://www.nlm.nih.gov/medlineplus/druginfo/uspdi/500299.html Medline information]
* [http://www.createforum.com/yasminsideeffec/viewforum.php?f=1&mforum=yasminsideeffec Yasmin Survivors Forum]


{{Sex hormones}}
[[Category:Drug]]
[[category:Progestagens]]
[[Category:Endocrinology]]
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Revision as of 16:40, 22 January 2015

Drospirenone
Black Box Warning
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1];

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Black Box Warning

ConditionName:
See full prescribing information for complete Boxed Warning.
ConditionName:
  • Content

Overview

Drospirenone is a {{{drugClass}}} that is FDA approved for the {{{indicationType}}} of {{{indication}}}. There is a Black Box Warning for this drug as shown here. Common adverse reactions include .

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Condition1
  • Dosing Information
  • Dosage
Condition2
  • Dosing Information
  • Dosage
Condition3
  • Dosing Information
  • Dosage
Condition4
  • Dosing Information
  • Dosage

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

Condition1
  • Developed by:
  • Class of Recommendation:
  • Strength of Evidence:
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Guideline-Supported Use of Drospirenone in adult patients.

Non–Guideline-Supported Use

Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Non–Guideline-Supported Use of Drospirenone in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding FDA-Labeled Use of Drospirenone in pediatric patients.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

Condition1
  • Developed by:
  • Class of Recommendation:
  • Strength of Evidence:
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Guideline-Supported Use of Drospirenone in pediatric patients.

Non–Guideline-Supported Use

Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Non–Guideline-Supported Use of Drospirenone in pediatric patients.

Contraindications

  • Condition1

Warnings

ConditionName:
See full prescribing information for complete Boxed Warning.
ConditionName:
  • Content
  • Description

Precautions

  • Description

Adverse Reactions

Clinical Trials Experience

There is limited information regarding Clinical Trial Experience of Drospirenone in the drug label.

Body as a Whole
Cardiovascular
Digestive
Endocrine
Hematologic and Lymphatic
Metabolic and Nutritional
Musculoskeletal
Neurologic
Respiratory
Skin and Hypersensitivy Reactions
Special Senses
Urogenital
Miscellaneous

Postmarketing Experience

There is limited information regarding Postmarketing Experience of Drospirenone in the drug label.

Body as a Whole
Cardiovascular
Digestive
Endocrine
Hematologic and Lymphatic
Metabolic and Nutritional
Musculoskeletal
Neurologic
Respiratory
Skin and Hypersensitivy Reactions
Special Senses
Urogenital
Miscellaneous

Drug Interactions

  • Drug
  • Description

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA):

  • Pregnancy Category


Pregnancy Category (AUS):

  • Australian Drug Evaluation Committee (ADEC) Pregnancy Category

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Drospirenone in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Drospirenone during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Drospirenone with respect to nursing mothers.

Pediatric Use

There is no FDA guidance on the use of Drospirenone with respect to pediatric patients.

Geriatic Use

There is no FDA guidance on the use of Drospirenone with respect to geriatric patients.

Gender

There is no FDA guidance on the use of Drospirenone with respect to specific gender populations.

Race

There is no FDA guidance on the use of Drospirenone with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Drospirenone in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Drospirenone in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Drospirenone in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Drospirenone in patients who are immunocompromised.

Administration and Monitoring

Administration

  • Oral
  • Intravenous

Monitoring

There is limited information regarding Monitoring of Drospirenone in the drug label.

  • Description

IV Compatibility

There is limited information regarding IV Compatibility of Drospirenone in the drug label.

Overdosage

Acute Overdose

Signs and Symptoms

  • Description

Management

  • Description

Chronic Overdose

There is limited information regarding Chronic Overdose of Drospirenone in the drug label.

Pharmacology

There is limited information regarding Drospirenone Pharmacology in the drug label.

Mechanism of Action

Structure

File:Drospirenone01.png
This image is provided by the National Library of Medicine.

Pharmacodynamics

There is limited information regarding Pharmacodynamics of Drospirenone in the drug label.

Pharmacokinetics

There is limited information regarding Pharmacokinetics of Drospirenone in the drug label.

Nonclinical Toxicology

There is limited information regarding Nonclinical Toxicology of Drospirenone in the drug label.

Clinical Studies

There is limited information regarding Clinical Studies of Drospirenone in the drug label.

How Supplied

Storage

There is limited information regarding Drospirenone Storage in the drug label.

Images

Drug Images

{{#ask: Page Name::Drospirenone |?Pill Name |?Drug Name |?Pill Ingred |?Pill Imprint |?Pill Dosage |?Pill Color |?Pill Shape |?Pill Size (mm) |?Pill Scoring |?NDC |?Drug Author |format=template |template=DrugPageImages |mainlabel=- |sort=Pill Name }}

Package and Label Display Panel

{{#ask: Label Page::Drospirenone |?Label Name |format=template |template=DrugLabelImages |mainlabel=- |sort=Label Page }}

Patient Counseling Information

There is limited information regarding Patient Counseling Information of Drospirenone in the drug label.

Precautions with Alcohol

  • Alcohol-Drospirenone interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

Look-Alike Drug Names

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

  1. Empty citation (help)
  2. "http://www.ismp.org". External link in |title= (help)

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