Drug information of Drospirenone

Drospirenone

Drug group: Hormone

Drospirenone is a progestin-only birth control pill that is used to prevent pregnancy.

Mechanism of effect

Spironolactone analogue with antimineralocorticoid and antiandrogenic activity; suppresses luteinizing hormone and ovulation by binding to the progesterone receptor; also alters cervical mucus, causing unfavorable sperm penetration; changes to the endometrial lining may decrease implantation

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. Due to its similarity to naturally occurring progesterone, drospirenone is thought to be associated with a lower incidence of progesterone contraceptive related adverse effects, such as breast tenderness and mood swings.

Pharmacokinetics

Peak plasma time: 2-6 hr

Peak plasma concentration: 27 ng/mL (single ingestion); 41 ng/mL (steady state [~10 days])

Vd: 4 L/kg

Protein bound: 95-97% (albumin)

Metabolism:Extensively metabolized

Nonactive metabolites: Acid form of drospirenone (formed by opening of lactone ring) and 4,5-dihydrodrospirenone (formed by reduction and subsequent sulfation)

Drospirenone is also subject to oxidative metabolism catalyzed by CYP3A4

Half-life: ~30 hr

Excretion: Nearly complete after ~10 days; amounts excreted in feces slightly higher compared with urine

 

Drug indications

Contraception

Contraception: Prevention of pregnancy in females of reproductive potential

Dosage

1 tablet qDay for 28 consecutive days; 1 white active tablet/day during the first 24 days and 1 green inert tablet/day during the 4 following days

Drug contraindications

liver failure , Abnormal uterine bleeding , adrenal dysfunction

-Renal impairment

-Adrenal insufficiency

-Presence or history of cervical cancer or progestin-sensitive cancers

-Liver tumors, benign or malignant, or hepatic impairment

-Undiagnosed abnormal uterine bleeding

Side effects

Acne , Headache , nausea , Weight increase , decreased libido , breast pain , Dysmenorrhea

Breakthrough bleeding-Unscheduled bleeding, cycle 1 -Unscheduled bleeding, cycle 13 -Acne -Metrorrhagia -Headache -Breast pain -Weight increased -Dysmenorrhea .-Nausea -Vaginal hemorrhage -Libido decreased -Breast tenderness -Menstruation irregular -Decreased plasma estradiol concentration-Hyperkalemia

Interactions

Spironolactone , Triamterene-H , Atenolol , Epinephrine , Ephedrine , Enalapril , Ibuprofen , Indomethacin , dopexamine , imidapril , Siltuximab , xipamide , cyclopenthiazide , Avapritinib , carbenoxolone , choline magnesium trisalicylate , Methyclothiazide , tolvaptan , magnesium citrate , Potassium iodide , lemborexant , tazemetostat , etodolac , flucloxacillin , Ruxolitinib , magnesium chloride , quinapril , Sulfamethoxazole , Levalbuterol , SULFISOXAZOLE , Lornoxicam , Meclofenamate , Nabumetone , Oxaprozin , Pirbuterol , Forskolin , Fedratinib , Pivmecillinam , Flibanserin , Moexipril , Olmesartan , Arformoterol , Albiglutide , Bendroflumethiazide , temocillin , Nadolol , Benazepril , Maraviroc , Candesartan , Nebivolol , Exenatide , Irbesartan , Esmolol , Aceclofenac , Celecoxib , Acemetacin , Sulindac , Agrimony , Penbutolol , Perindopril , Parecoxib , Chlorthalidone , Telmisartan , Sacubitril and valsartan , Ketoprofen , Celiprolol , Salsalate , Diflunisal , Tolfenamic Acid , Trandolapril , Magnesium hydroxide , Bumetanide , Ivacaftor , Torsemide , Triamterene , Eprosartan , Calcium chloride , Calcium citrate , Pindolol , Indapamide , Epoprostenol , flurbiprofen , Norepinephrine , Axitinib , ISOPROTERENOL , Aldesleukin , Mifepristone , Calcium acetate , Trimethoprim , Aspirin , Chlorothiazide , Metaproterenol , Acebutolol , Lomitapide , formoterol , Bisoprolol , Atazanavir , Darunavir , Ticarcillin , ethacrynic acid , Carvedilol , Ketorolac , Calcium Gloconate , Calcium carbonate , Clobazam , Liraglutide , Magnesium oxide , Magnesium sulfate , Midazolam , Hydrochlorothiazide , Valsartan , Captopril , Lisinopril , Minoxidil , Metoprolol , Metolazone , Mefenamic acid , Meloxicam , Sulfasalazine , Succinylcholine , Cyclosporine , Furosemide , Labetalol , Losartan , Disopyramide , Digoxin , Diclofenac , Salmeterol , Sotalol , Sulfadiazine , Tolmetin , Tizanidine , Timolol , Tinidazole , Gentamicin , Dobutamine , Betaxolol , Brimonidine , Potassium chloride , Propranolol , Piroxicam , Terbutaline , eplerenone , Amiloride , potassium citrate , Fosinopril , fenoprofen , Ramipril , Canagliflozin , Potassium Phosphate , Treprostinil , Lopinavir and Ritonavir , Troleandomycin
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Alerts

-Use leads to decreased estradiol serum levels; unknown if clinically relevant loss of bone mineral density may occur

-Some studies suggest Combined oral contraceptive containing progestin and estradiol associated with increased risk of cervical cancer or intraepithelial neoplasia; however, controversy continues about the extent to which such findings may be due to differences in sexual behavior and other factors

-Discontinue if jaundice or acute or chronic disturbances of liver function develop; do not resume until LFTs return to normal and causation identified;

 

-Consider possibility of ectopic pregnancy in women who become pregnant or report lower abdominal pain

-Progestins may decrease insulin sensitivity; patients with diabetes may be at greater risk of hyperglycemia and may require additional medication adjustments or monitoring

-Bleeding irregularities (eg, breakthrough or intracyclic bleeding or spotting) may occur, especially during the first 3 months; may resolve over time or by changing to different contraceptive; if persists, evaluate for causes (eg, pregnancy, malignancy)

-Carefully observe females for history of depression and discontinue drospirenone if depression recurs to a serious degree

-Thromboembolism risk with combined oral contraceptives containing drospirenone and ethinyl estradiol higher than those containing some other progestins plus ethinyl estradiol

-Epidemiological studies have not indicated an association between progestin-only preparations and an increased risk of myocardial infarction, cerebral thromboembolism, or venous thromboembolism

-Discontinue if arterial or venous thromboembolic events occur; consider discontinuing with prolonged immobilization due to surgery or illness

-Drospirenone has antimineralocorticoid activity, including the potential for hyperkalemia in high-risk females, comparable to spironolactone 25 mg

-Contraindicated in females with conditions that predispose to hyperkalemia (eg, renal impairment, hepatic impairment, adrenal insufficiency, long-term coadministration with strong CYP3A4 inhibitor)

-Drugs or herbal products that induce certain enzymes, including CYP3A4, may decrease systemic concentrations of hormonal contraceptives and potentially diminish the effectiveness or increase breakthrough bleeding

-Strong CYP3A4 inhibitors may result in a moderate increase of drospirenone systemic exposure

-Potential for increased serum potassium concentration if drospirenone coadministered with other drugs that increase potassium levels

Points of recommendation

-Take first white active tablet on the first day of menses

-Take subsequent white active tablets qDay at the same time each day for a total of 24 days

-Take 1 green inert tablet daily for 4 days and at the same time of day that active tablets were taken

-Begin each subsequent pack on the same day of the week as the first cycle pack (ie, on the day after taking the last inactive tablet)

-Instruct women to use a nonhormonal backup contraceptive for 28 days after discontinuing the enzyme inducer

-Switching from a different contraceptive:

Oral contraceptive: Start on the same day that a new pack of the previous oral contraceptive would have been taken.

Transdermal patch, vaginal ring, injection: Start on the day the next dose would have been due.

Intrauterine device or implant: Start on the day of removal.

-Missed doses:

If 1 hormonal (active) tablet is missed: Take the missed tablet as soon as possible. Continue taking 1 tablet a day until the pack is finished.

If vomiting or diarrhea occurs within 3 to 4 hours after taking 1 hormonal (active) tablet: Take the next scheduled tablet as soon as possible (preferably within 12 hours of the usual scheduled time).

If ≥2 consecutive hormonal (active) tablets are missed: Take the most recently missed tablet as soon as possible. Continue taking 1 tablet a day until the pack is finished (1 or more missed tablets will remain in the pack). Use additional nonhormonal contraception until hormonal (active) tablets have been taken for 7 consecutive days.

 

Pregnancy level

Forbidden

Based on epidemiologic studies and meta-analyses, there is little or no increased risk of birth defects in the children of females who inadvertently use oral progestins during early pregnancy

Discontinue if pregnancy occurs, as there is no reason to use hormonal contraceptives during pregnancy

Breast feeding warning

Negligible amounts of drospirenone are excreted in the breast milk

At therapeutic doses, no effects on breastfed newborns/infants are anticipated

-No effects on breastfed newborns or infants is expected with progesterone-only contraceptives; no adverse effects on milk production or on the health, growth, or development of the infant have been demonstrated.

Drug forms

Slynd

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