The treatment of gynecological disorders and prostate cancer.
This is a combined oral contraceptive tablet containing the synthetic progestogen, drospirenone and the synthetic estrogen, ethinylestradiol. The contraceptive effect of this tablet is based on the interaction of various factors, the most important of which are seen as the inhibition of ovulation and the changes in cervical secretion. When this tablet is taken according to instructions, the egg cells are prevented from maturing to the point at which they can be fertilized, the cervical mucus remains thick so as to constitute a barrier to sperm and the endometrium is rendered unreceptive to implantation. As well as protection against pregnancy, estrogen/progestogen combinations have several positive properties which, next to the negative properties, can be useful in deciding on the method of birth control. The cycle is more regular and the menstruation is often less painful and bleeding is lighter.
Drospirenone has antimineralocorticoid activity, counteracting estrogen related sodium retention. In combination with ethinylestradiol, drospirenone displays a favourable lipid profile with an increase in high-density lipoprotein HDL. Drospirenone exerts antiandrogenic activity and does not counteract the ethinylestradiol-related sex hormone binding globulin (SHBG) increase which is useful for binding and inactivating the endogenous androgens. Drospirenone is devoid of any androgenic, estrogenic, glucocorticoid and antiglucocorticoid activity. This in combination with the antimineralocorticoid and antiandrogenic properties, gives drospirenone a biochemical and pharmacological profile closely resembling the natural hormone progesterone.
ORAL Menopausal hormone replacement therapy: Adult: In menopausal women: 10-20 mcg daily in conjunction w/ a progestogen in women w/ uterus. Female hypogonadism: Adult: 10-50 mcg daily in a cyclical regimen. As part of combined oral contraceptive: Adult: As the oestrogenic component of combined oral contraceptive: 20-40 mcg/ day.
Interactions between ethinylestradiol and other drugs may lead to decreased or increased ethinylestradiol concentrations, respectively. Decreased ethinylestradiol serum concentrations may cause an increased incidence of breakthrough bleeding and menstrual irregularities and may possibly reduce efficacy of the oral contraceptive. Example of substances that may decrease serum ethinylestradiol concentrations include rifampicin, phenytoin, primidone, rifabutin, dexamethasone, griseofulvin, topiramate, some protease inhibitors, modafinil, ritonavir and barbiturates. Certain antibiotics including ampicillin, other penicillins and tetracyclines may reduce the efficacy of oral contraceptives. During concomitant use of this tablet & other drugs that may lead to decreased ethinylestradiol serum concentrations, it is recommended that a non hormonal back-up method of contraception to be used in addition to the regular intake of this tablet.
Uterine, liver & mammary carcinoma, thromboembolic disorders. Pregnancy, lactation, untreated endometriosis, jaundice, undiagnosed vag bleeding. Asthma; epilepsy; migraine; DM; cardiac or renal dysfunction; hepatic disease; familial defects of lipoprotein metabolism. Increased risk of endometrial cancer in unopposed oestrogen therapy. Increased risk of gallbladder disease in women on postmenopausal oestrogens. Large doses may increase CV risk, BP, risk of thrombophlebitis & pulmonary embolism.
Oedema, hypertension; dizziness; headache; thromboembolism; cholestatic jaundice; nausea, vomiting; disturbance of menstrual cycle; fluid retention, discomfort in breast, wt gain/loss; increased appetite, increased tendency for vag candidiasis; mental depression; alteration In libido; rashes; alopoecia, hirsutism; gynaecomastia & Impotence. Endometrial cancer (prolonged use).
Use is contraindicated during pregnancy. Breastfeeding is not recommended during use of this drug.
Symptoms of oral contraceptive overdose may include nausea, vomiting, breast tenderness, dizziness, abdominal pain, drowsiness/fatigue; withdrawal bleeding may occur in females. There is no specific antidote and further treatment of overdose, if necessary, is directed to the symptoms.
Store below 30°C. Store all drugs properly and keep them out of reach of children.
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