DrospirenoneDrospirenoneDrospirenone is a synthetic progestin that is a spironolactone analogue with antimineralocorticoid
activity.
drospirenone has no androgenic, estrogenic, glucocorticoid, or antiglucocorticoid activity. drospirenone has antiandrogenic activity. Its molecular weight is 366.5 and its molecular formula is C24H30O3.
It has a unique pharmacologic profile that is similar to that of natural progesterone. The drug is metabolized mainly in liver by Cytochrome P450 3A4 (CYP3A4). The half life of the drug is 30 hours.
Uses: 1) Contraception : Oral contraceptives with drospirenone reportedly produce fewer side effects. Its antimineralocorticoid effects may prevent estrogen-related bloating and weight gain secondary to water retention. It may decrease blood pressure. And its antiandrogenic effects have the potential to reduce the severity of acne, seborrhea, and related skin conditions.
Preparations available generally contains: 3mg of drospirenone in
combination with 20or30mcg of ethynyl estradiol
2) Premenstrual dysphoric disorder (PMDD) a low-dose OC that contains drospirenone 3 mg plus EE 20 mcg administered for 24 days in a 28-day cycle, i.e., a 24/4 regimen
has been shown to be effective in reducing mood, behavioral, and physical symptoms in women with PMDD, who also are seeking contraception, and it is comparable to sertraline Recently, the US Food and Drug Administration approved the use of a COC containing drospirenone for treating PMDD (FDA-2006).
3) Acne Vulgaris: The combination is also indicated for the treatment of moderate acne vulgaris in women at least 14 years of age, who have no known contraindications to oral contraceptive therapy and have achieved menarche. However, this combination should be used for the treatment of acne only if the patient desires an oral contraceptive.
4) Menopause: drospirenone in combination with estradiol (0.5 mg Drospirenone and 1 mg estradiol) may provide a safer and more beneficial HRT It reduces hot flushes. a greater improvement in other menopausal symptoms – including sweating episodes, sleep problems, vaginal dryness, and nocturia moderate to severe vulvar and vaginal atrophy associated with menopause . favorable effects on lipids and on blood pressure. Estradiol on its own lowers total cholesterol by lowering LDL, but raises triglycerides and has a positive, but slight, effect on HDL. In combination with drospirenone, there is a much more significant (17-18%) reduction in total cholesterol, not only due to a more profound effect on LDL cholesterol, but also a reduction in triglycerides. It also appears to lower blood pressure in women, an effect that “may well be due to its antimineralocorticoid effect.” Drospirenone/ EE has all the features of a good HRT with inhibition of hot flushes, inhibition of hyperplasia, amenorrhea, a good lipid profile, and positive effects on blood pressure
Adverse drug effects:The most frequent adverse events reported with the use of Drospirenone-EE combination in the contraception clinical trials, which may or not be drug related, included headache, breast pain, vaginal moniliasis, leucorrhea, diarrhea, nausea, vomiting, vaginitis, abdominal pain, dysmenorrhea, accidental injury, cystitis, tooth disorder ,emotional liability, migraine, suspicious Papanicolaou smear, dyspepsia, skin disorder, inter-menstrual bleeding, decreased libido, weight gain, pain, depression, increased cough, dizziness, menstrual disorder, pain in extremity, pelvic pain, and asthenia.
Drospirenone- EE combination should not be used in patients with conditions that predispose to hyperkalemia (i.e. renal insufficiency, hepatic dysfunction and adrenal insufficiency). Women receiving daily, long-term treatment for chronic conditions or diseases with medications that may increase serum potassium (ACE inhibitors, Angiotensin II receptor antagonists,potassium sparing diuretics, potassium supplementation, heparin, aldosterone antagonists and NSAIDS) should get the serum potassium levels checked in the first cycle of treatment.