Usage
Drospirenone is a synthetic progestin, a class of hormones similar to progesterone, prescribed for contraception (preventing pregnancy) in women and adolescents. Certain combined oral contraceptives containing drospirenone are also indicated for treating moderate acne vulgaris and the symptoms of premenstrual dysphoric disorder (PMDD) in women who choose oral contraception as their method of birth control. Drospirenone is classified as a hormonal contraceptive. It primarily works by suppressing ovulation. Additional contraceptive effects include thickening cervical mucus to hinder sperm penetration and altering the uterine lining to make implantation less likely.
Alternate Names
Drospirenone is the generic name. Brand names include Slynd (for contraception with drospirenone alone) and Yasmin, Yaz, Ocella, Syeda, Gianvi, Loryna, Vestura, Yaela, and Zarah (for combined oral contraceptives containing drospirenone and ethinyl estradiol).
How It Works
Pharmacodynamics: Drospirenone primarily inhibits ovulation and thickens cervical mucus. It also induces changes in the endometrium, making it less receptive to implantation. It exhibits antimineralocorticoid activity, similar to spironolactone, and has antiandrogenic properties. Drospirenone has no estrogenic, glucocorticoid, or antiglucocorticoid activity.
Pharmacokinetics:
- Absorption: Drospirenone is rapidly and completely absorbed after oral administration, reaching peak plasma concentrations within 1 to 2 hours. Food does not significantly affect absorption.
- Metabolism: It is extensively metabolized in the liver primarily by CYP3A4, forming several inactive metabolites.
- Elimination: Drospirenone is eliminated primarily through renal excretion (about 70%) and fecal excretion (about 19%). The elimination half-life is approximately 30 hours.
Mode of Action: Drospirenone binds to progesterone receptors, exerting its contraceptive effects by suppressing the hypothalamic-pituitary-ovarian axis, thereby inhibiting ovulation. The antimineralocorticoid activity results from competitive binding to the mineralocorticoid receptor.
Dosage
Standard Dosage
Adults:
- Drospirenone alone (Slynd): One 4 mg tablet daily for 28 consecutive days. The pack contains 24 active (white) and 4 inert (green) tablets.
- Drospirenone/Ethinyl Estradiol: Dose depends on the specific product. Most commonly, one active tablet is taken daily for 21 or 24 days, followed by 7 or 4 days of either placebo tablets or no tablets, respectively.
Children:
- Drospirenone alone (Slynd): Use of this product before menarche is not indicated. For postmenarchal adolescents, safety and efficacy are expected to be the same as in adults.
- Drospirenone/Ethinyl Estradiol: Safety and efficacy have not been established in girls younger than 14 years. For those 14 years or older, follow adult dosing depending on the product.
Special Cases:
- Elderly Patients: Drospirenone alone or in combination with ethinyl estradiol is not indicated for use in postmenopausal women.
- Patients with Renal Impairment: Contraindicated in patients with renal impairment or acute renal failure.
- Patients with Hepatic Dysfunction: Contraindicated in patients with hepatic impairment or benign or malignant liver tumors.
- Patients with Comorbid Conditions: Caution is advised in patients with a history of hyperkalemia, adrenal insufficiency, or those taking medications that can increase potassium levels. Close monitoring is recommended for patients with diabetes as progestins may decrease insulin sensitivity.
Clinical Use Cases
Drospirenone is not indicated for use in the specific clinical settings of intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. Its primary indication is contraception.
Dosage Adjustments
Dose adjustments are not recommended for drospirenone. It is contraindicated in the presence of renal or hepatic impairment. For other conditions, such as concomitant use of potassium-sparing medications, careful monitoring of potassium levels is essential.
Side Effects
Common Side Effects:
Acne, irregular menstrual bleeding, headache, breast pain or tenderness, weight gain or loss, menstrual cramps, nausea, vaginal bleeding or spotting, decreased libido, mood changes, abdominal pain.
Rare but Serious Side Effects:
Hyperkalemia (high potassium levels), thromboembolic events (blood clots, including deep vein thrombosis and pulmonary embolism), hepatic adenoma (benign liver tumor), cholestatic jaundice (liver problem), gallbladder disease, elevated blood pressure, hypersensitivity reactions.
Long-Term Effects:
Potential long-term complications primarily relate to the risk of thromboembolic events and the effects of chronic exposure to hormones, though more research is needed in this area.
Adverse Drug Reactions (ADR):
Allergic reactions, angioedema (swelling), severe hyperkalemia, thromboembolic complications, hepatic dysfunction.
Contraindications
- Renal impairment.
- Adrenal insufficiency.
- Presence or history of cervical cancer or other progestin-sensitive cancers.
- Liver tumors (benign or malignant) or hepatic impairment.
- Undiagnosed abnormal uterine bleeding.
- Hypersensitivity to drospirenone or any component of the formulation.
- Concomitant use with Hepatitis C drug combinations containing ombitasvir, paritaprevir/ritonavir, with or without dasabuvir (for combined oral contraceptives containing drospirenone and ethinyl estradiol).
Drug Interactions
- CYP3A4 inducers: May decrease drospirenone concentrations, reducing its effectiveness. Examples include rifampin, phenytoin, St. John’s wort.
- CYP3A4 inhibitors: May increase drospirenone concentrations. Examples include ketoconazole, itraconazole, some HIV protease inhibitors.
- Potassium-sparing drugs: May increase the risk of hyperkalemia. Examples include spironolactone, amiloride, triamterene.
- Other interactions: Some medications, such as certain antibiotics and anticonvulsants, may interfere with the efficacy of combined oral contraceptives.
Pregnancy and Breastfeeding
- Pregnancy: Drospirenone is contraindicated in pregnancy. It should be discontinued if pregnancy occurs.
- Breastfeeding: Small amounts of drospirenone are excreted in breast milk. While no significant adverse effects on the infant are expected with drospirenone-only pills, non-hormonal contraceptive methods are preferred during breastfeeding. Combined oral contraceptives containing drospirenone and ethinyl estradiol may decrease milk quantity and quality and are generally not recommended during breastfeeding.
Drug Profile Summary
- Mechanism of Action: Primarily inhibits ovulation; thickens cervical mucus; alters endometrium; antimineralocorticoid and antiandrogenic activity.
- Side Effects: Acne, irregular bleeding, headache, breast tenderness, weight changes, mood swings, nausea. Rarely: thromboembolism, hyperkalemia.
- Contraindications: Renal/hepatic impairment, adrenal insufficiency, progestin-sensitive cancers, undiagnosed abnormal uterine bleeding, pregnancy.
- Drug Interactions: CYP3A4 inducers/inhibitors, potassium-sparing drugs.
- Pregnancy & Breastfeeding: Contraindicated in pregnancy; use with caution during breastfeeding, especially combined oral contraceptives.
- Dosage: Refer to the detailed dosage section above.
- Monitoring Parameters: Potassium levels (especially with risk factors or interacting medications), blood pressure, liver function tests (if clinically indicated).
Popular Combinations
Drospirenone is most popularly combined with ethinyl estradiol in various oral contraceptives. This combination offers the benefits of combined hormonal contraception with the added potential benefits of the antimineralocorticoid and antiandrogenic activity of drospirenone.
Precautions
- General Precautions: Assess for contraindications, including renal and hepatic function, adrenal insufficiency, and history of progestin-sensitive cancers. Monitor potassium levels if risk factors are present or when co-administered with potassium-increasing drugs. Monitor blood pressure and liver function tests as needed.
- Pregnant Women: Contraindicated.
- Breastfeeding Mothers: Use non-hormonal methods if possible. If hormonal methods are necessary, progestin-only contraceptives like Slynd are preferred, especially in the first few weeks postpartum.
- Children & Elderly: Not indicated before menarche or in postmenopausal women.
- Menstruating Individuals: Irregular bleeding is a common side effect, especially in the first few months. If bleeding persists or is heavy, further evaluation is warranted.
- Lifestyle Considerations: Smoking significantly increases the risk of cardiovascular events with combined oral contraceptives containing drospirenone and ethinyl estradiol.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Drospirenone?
A: It depends on whether drospirenone is used alone or in combination with ethinyl estradiol, and the specific product used. See the detailed Dosage section for specific recommendations.
Q2: How does Drospirenone differ from other progestins used in contraceptives?
A: Drospirenone possesses antimineralocorticoid and antiandrogenic activities, which may offer benefits such as reduced bloating and acne, compared to some other progestins.
Q3: What are the most serious side effects of Drospirenone?
A: The most serious side effects include hyperkalemia, thromboembolic events (blood clots), and hepatic adenoma (benign liver tumor).
Q4: Can Drospirenone be used in patients with kidney disease?
A: No, drospirenone is contraindicated in patients with renal impairment.
Q5: What should be done if a dose of Drospirenone is missed?
A: Consult the package insert for specific instructions, as it varies by product. Generally, the missed pill should be taken as soon as remembered, and additional contraceptive measures may be needed.
Q6: Does Drospirenone interact with any other medications?
A: Yes, drospirenone can interact with certain medications, including CYP3A4 inducers and inhibitors, and potassium-sparing drugs. Consult the Drug Interactions section for more details.
Q7: Can Drospirenone be used during pregnancy or breastfeeding?
A: Drospirenone is contraindicated during pregnancy. While it can be used during breastfeeding, non-hormonal methods or progestin-only pills (Slynd) are preferred.
Q8: How does Drospirenone affect potassium levels?
A: Drospirenone has antimineralocorticoid activity, which can lead to increased potassium levels, especially in patients with renal impairment or those taking potassium-sparing drugs.
Q9: Can Drospirenone help treat acne?
A: Some combined oral contraceptives containing drospirenone and ethinyl estradiol are indicated for treating moderate acne in women who also desire contraception. Drospirenone alone (Slynd) is not indicated for this use.
