Conception and pharmacodynamic profile of drospirenone

Elger, W.; Beier, S.; Pollow, K.; Garfield, Robert E.; Shi, Shao Qing; Hillisch, Alexander

doi:10.1016/j.steroids.2003.08.008

Cited by 130 publications

(73 citation statements)

References 61 publications

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“…However, endogenous progesterone has low oral bioavailability and a short plasma halflife, rendering the hormone unsuitable for use in HRT preparations [45,46]. Although micronized progesterone is available for use in HRT, and data, for example, from the PEPI trial demonstrated that it is effective [18], most HRT combinations contain a synthetic progestogen, commonly derived from 19-nortestosterone (e.g.…”

Section: Drsp: a Synthetic Progestogen With Added Benefitsmentioning

confidence: 99%

“…Moreover, its binding region and biological activities are closely akin to those of endogenous progesterone (Table 1) [35,36,40]. DRSP and progesterone both exhibit moderate binding affinity to progesterone receptors and high binding affinity to mineralocorticoid receptors (as antagonists) in the uterus and kidney [45]. Both DRSP and progesterone have considerable anti-mineralocorticoid activity in transactivation studies of hormone receptors [35,38].…”

Section: Drsp: a Synthetic Progestogen With Added Benefitsmentioning

confidence: 99%

“…The anti-androgenic potency of DRSP is reported to be 5-10 times greater than that of progesterone and one-third that of cyproterone acetate (CPA). This contrasts with the absence of anti-androgenic activity for MPA [40,45]. Neither DRSP nor natural progesterone display estrogenic, androgenic or glucocorticoid activity [44,45,47].…”

Section: Drsp: a Synthetic Progestogen With Added Benefitsmentioning

confidence: 99%

“…This contrasts with the absence of anti-androgenic activity for MPA [40,45]. Neither DRSP nor natural progesterone display estrogenic, androgenic or glucocorticoid activity [44,45,47]. Unlike other progestogens, DRSP has anti-aldosterone activity.…”

Section: Drsp: a Synthetic Progestogen With Added Benefitsmentioning

confidence: 99%

“…Unlike other progestogens, DRSP has anti-aldosterone activity. The binding affinity of DRSP at the mineralocorticoid receptor is 2.3-to 5-fold higher than that of aldosterone, whereas the affinity of MPA or NETA is only approximately 3% that of aldosterone, and neither display antimineralocorticoid activity [45,47]. In spontaneously hypertensive rats, SBP and DBP were decreased or remained unchanged over 27 days of DRSP administration, whereas blood pressure increased with conventional progestogens, such as CPA [45].…”

Section: Drsp: a Synthetic Progestogen With Added Benefitsmentioning

confidence: 99%

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Advances in hormone replacement therapy with drospirenone, a unique progestogen with aldosterone receptor antagonism

2006

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Unlike other currently available progestogens, drospirenone (DRSP) has a pharmacological profile, which closely mimics that of endogenous progesterone, most notably potent anti-aldosterone and anti-androgenic effects. Consequently, DRSP, when combined with 17β-estradiol (E2) as hormone replacement therapy (HRT), offsets E2-related water and sodium retention by blocking the mineralocorticoid receptor. This review evaluates the potential benefits offered by DRSP as the progestin component of HRT with respect to its anti-aldosterone activity, which translates into positive effects on body weight and blood pressure in clinical trials of continuous, combined E2/DRSP in post-menopausal women. In a 1 -year, large-scale, randomised, controlled trial, E2 1 mg/DRSP 2 mg significantly decreased mean body weight by 1.2 kg versus baseline (P < 0.001), whereas patients receiving E2 1 mg gained weight. E2 1 mg/DRSP 2 mg also significantly lowered mean systolic blood pressure (SBP) by 9.0 mmHg from baseline (P < 0.05) versus 3.7 mmHg in the E2 1 mg group (P = 0.220) in a sub-group of hypertensive women. In addition, E2/DRSP was not associated with hyperkalemia (potassium ≥ 5.5 meq/L) irrespective of concomitant use of ACE inhibitors, angiotensin II receptor antagonists or non-steroidal anti-inflammatory drugs, and co-morbid diabetes mellitus. In summary, as well as effectively treating climacteric symptoms, DRSP 2 mg combined with E2 1 mg has shown positive effects on body weight and blood pressure in clinical trials, most likely due to DRSP's anti-aldosterone properties. This combination may therefore offer an alternative therapeutic option with additional benefits beyond current HRT agents for symptomatic postmenopausal women.

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Section: Drsp: a Synthetic Progestogen With Added Benefitsmentioning

confidence: 99%

Section: Drsp: a Synthetic Progestogen With Added Benefitsmentioning

confidence: 99%

Section: Drsp: a Synthetic Progestogen With Added Benefitsmentioning

confidence: 99%

Section: Drsp: a Synthetic Progestogen With Added Benefitsmentioning

confidence: 99%

Section: Drsp: a Synthetic Progestogen With Added Benefitsmentioning

confidence: 99%

See 3 more Smart Citations

Advances in hormone replacement therapy with drospirenone, a unique progestogen with aldosterone receptor antagonism

2006

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Contraception

Hahn¹,

McGuire²,

Kuhnke³

2011

Ullmann's Encyclopedia of Industrial Chemistry

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The article contains sections titled: 1. Introduction 2. Natural Methods 2.1. Periodic Methods 2.2. Breast Feeding 3. Barrier Methods 3.1. Chemical Vaginal Contraceptives 3.2. Physical Barriers 4. Hormonal Methods 4.1. The Menstrual Cycle 4.1.1. The Regulatory System 4.1.2. Hormonal Effects on the Endometrium 4.1.3. Hormonal Effects on the Cervix 4.1.4. How Hormonal Contraceptives Work 4.2. Historical Survey on Hormonal Contraception and Combined Oral Contraceptives 4.2.1. The Estrogenic Component 4.2.2. The Progestogenic Component 4.2.3. New Regimen for Oral Contraceptives 4.3. Progestogen‐Only Oral Contraceptives 4.4. Long‐Acting Contraceptives – Drug Delivery Systems 4.5. Emergency Contraception 4.6. Benefits and Risks of Hormonal Contra‐ception 4.6.1. Cardiovascular Risks 4.6.2. Cancer 5. Intrauterine Contraception 5.1. Intrauterine Device (IUD) 5.2. Intrauterine System (IUS) 6. Sterilization 6.1. Male Sterilization (Vasectomy) 6.2. Female Sterilization 7. New Approaches 7.1. Hormonal Research 7.2. Nonhormonal Research 7.3. Contraceptive Vaccines 7.4. Male Fertility Control 7.4.1. Nonhormonal Research 7.4.2. Hormonal Research

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