(British Approved Name, US Adopted Name, rINN)
INNs in other languages (French, Latin, and Spanish): Dihydrospinenone; Drospinenon; Drospirenona; Drospirenone; Drospirenoni; Drospirenonum; SH-470; ZK-30595.
C24H30O3 = 366.5.
CAS — 67392-87-4.
Pharmacopoeias. In US.
The United States Pharmacopeia 31, 2008 (Drospirenone). A white to off-white powder. Practically insoluble in water and in hexane sparingly soluble in alcohol and in ethyl acetate soluble in methyl alcohol and in acetone freely soluble in dichloromethane. Store in airtight containers at a temperature of 20° to 25°, excursions permitted between 15° and 30°.
Adverse Effects and Precautions
As for progestogens in general (see Progesterone). See also under Hormonal Contraceptives, p.2059. Drospirenone has antimineralocorticoid activity and therefore should not be used in patients at risk of hyperkalaemia, such as those with renal or hepatic impairment or adrenal insufficiency.
Effects on the cardiovascular system. As with combined oral contraceptives containing other progestogens, there are reports of thrombotic and ischaemic events in patients taking a preparation of ethinylestradiol and drospirenone. The extent of risk associated with hormonal contraceptives that contain drospirenone is mentioned under Venous Thromboembolism.
Renal impairment. US licensed product information for preparations containing drospirenone contra-indicates its use in renal impairment, and in the UK it is contra-indicated in severe impairment. A study of women with renal impairment that was mild (creatinine clearance 50 to 80 mL/minute) or moderate (30 to 50 mL/min) found a trend toward increasing drospirenone exposure with decreasing creatinine clearance. Serum-potassium concentrations were not significantly altered by drospirenone, despite the concomitant use of other drugs that can also potentially increase potassium concentrations including beta blockers and ACE inhibitors.
As for progestogens in general (see Progesterone). See also under Hormonal Contraceptives, and Hormone Replacement Therapy. Because drospirenone has antimineralocorticoid activity, it may potentially exacerbate the effects of drugs that can increase serum-potassium, such as ACE inhibitors, angiotensin II receptor antagonists, aldosterone antagonists, potassium-sparing diuretics, or NSAIDs. Drospirenone may also reduce blood pressure, such that antihypertensive treatment may require adjustment.
Diuretics. The pharmacokinetics of hydrochlorothiazide were not affected by the addition of drospirenone and estradiol in a placebo-controlled study of 36 hypertensive postmenopausal women. However, those given the combination in this study developed lower blood pressure and higher serum-potassium concentrations, which was attributed to the antimineralocorticoid effect of drospirenone. Nontheless, there were no cases of hyperkalaemia. It has been suggested that these potential antihypertensive and potassium-sparing effects might be beneficial in women requiring treatment for both menopausal symptoms and hypertension (see also Menopausal Disorders).
NSAIDs. Drospirenone has the potential to exacerbate the effects of other drugs, such as NSAIDs, that can increase serum potassium. Licensed product information suggests that a clinical effect is unlikely in practice, although the use of a number of such drugs together or the presence of renal impairment may increase the risk. In a small study of healthy postmenopausal women, there was no evidence that potassium concentrations were any higher during concomitant use of indometacin with a combination of drospirenone plus estradiol compared with indometacin alone.
After oral doses, drospirenone is rapidly absorbed with a bioavailability of about 76%. It is about 97% bound to plasma proteins, though it does not bind to sex hormone binding globulin or corticosteroid binding globulin. It is extensively metabolised with a terminal half-life of about 30 to 40 hours. The metabolites are excreted in the urine and faeces.
Uses and Administration
Drospirenone is a structural analogue of spironolactone it has the effects of a progestogen (see Progesterone) with antimineralocorticoid and anti-androgenic activity. It is used as the progestogenic component of combined oral contraceptives, usually in a dose of 3 mg daily with ethi-nylestradiol 30 micrograms, for 21 days of each 28-day cycle. A combination of drospirenone 3 mg with ethinylestradiol 20 micrograms, given daily for 24 days of each 28-day cycle, may also be used for contraception and for the management of premenstrual dys-phoric disorder or moderate acne in women who also require an oral contraceptive. Drospirenone is also used as the progestogenic component of menopausal HRT in a continuous dosage regimen of 0.5 or 2 mg daily.
Menopausal disorders. Drospirenone is used as the progestogenic component of menopausal HRT. The antimineralocorticoid effect of drospirenone has also been investigated and found to lower blood pressure in postmenopausal women with treated and untreated hypertension.
Premenstrual syndrome. The combination of drospirenone with ethinylestradiol has been studied in the management of premenstrual syndrome. A systematic review of 5 studies found some evidence that the combination may be useful in the treatment of premenstrual dysphoric disorder. However, it was not known whether the effect lasted beyond 3 cycles of treatment, whether the combination was effective for less severe symptoms, or whether combinations using drospirenone were any better than combined contraceptives containing other progestogens.
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