ANGELIQ ® - Estradiol + Drospirenone

ANGELIQ ® a drug based on estradiol hemihydrate + drospirenone

THERAPEUTIC GROUP: Female sexual hormones - Progestin and estrogen, fixed combination

IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects

Indications ANGELIQ ® - Estradiol + Drospirenone

ANGELIQ® used as a substitution therapy in postmenopausal women or in case of estrogen deficiency.

The presence of fixed combination estrogens and progestins also allows their use in the prevention of pathologies associated with menopause such as osteoporosis.

Mechanism of action ANGELIQ ® - Estradiol + Drospirenone

ANGELIQ ® a drug based on estradiol and drospirenone, both sex hormones very important in maintaining the overall health status of women.

The presence of estradiol, makes it possible to compensate for the physiological deficiencies typical of the post-climacteric period, which are often accompanied by vasomotor, neurological and serious pathologies such as osteoporosis which significantly reduce the quality of life of these women.

In this case, replacement therapy becomes necessary to reduce the severity of the symptoms described above and to prevent the onset of highly disabling diseases such as osteoporosis.

The presence of drospirenone, a synthetic progestin with antimineralocorticoid activity useful for reducing the accumulation of sodium and water and associated pathologies, is instead justified by the direct action on the endometrium, useful for controlling the growth of endometrial cells induced by estradiol, potentially dangerous for the development of neoplastic diseases.

The simultaneous presence of the two active ingredients is therefore useful for controlling post-climacteric symptoms, while reducing the risks associated with this therapy and preventing the appearance of more serious conditions such as osteoporosis and cardiovascular diseases.

Studies carried out and clinical efficacy

1. EFFECTIVENESS AND SAFETY OF THE REPLACEMENT ORMONAL THERAPY WITH ESTRADIOLO and DROSPIRENONE

A study conducted on around 250 healthy postmenopausal Chinese women, which demonstrates that estradiol + drospirenone can be taken for 16 weeks without interruption, can guarantee a marked improvement in symptoms without the appearance of clinically significant side effects.

2. THE METABOLIC EFFECTS OF ESTRADIOLO / DROSPIRENONE

All-Italian clinical work demonstrating that the intake of ethinyl estradiol / drospirenone in healthy women in the post-menopausal age does not induce any type of deterioration on the glucose metabolism, indeed it is able to improve the lipidemic profile and vascular reactivity.

3. ANGELIQ AND VASCULAR HEALTH

The daily intake of Angeliq has proved effective in reducing the intima-media thickness of the carotid artery, reducing some related symptoms such as dizziness and dizziness. This action could be associated with Angeliq's antriandrogenic and anti-mineralocorticoid activity.

Method of use and dosage

ANGELIQ ® 1 mg estradiol coated tablets and 2 mg drospirenone:

given the half-life of the two active ingredients, estimated by pharmacokinetic studies around 24 hours, the recommended dosage is one tablet per day, taken every day at the same time.

Warnings ANGELIQ ® - Estradiol + Drospirenone

The potential side effects of hormone replacement therapy, even when associated with the progestogenic one, encourage the doctor to pay particular attention to the patient's overall health.

More precisely, the intake of ANGELIQ ® must be preceded by a careful medical examination useful for evaluating the presence of conditions predisposing to neoplastic or thromboembolic diseases such as:

leiomyomas (uterine fibroids) or endometriosis, history of thromboembolic disorders, risk factors for estrogen-dependent tumors, e.g. hereditary predisposition (1st degree relatives with breast cancer), hypertension, liver disease, diabetes mellitus with or without vascular involvement, cholelithiasis, migraine or headache (severe), systemic lupus erythematosus, history of endometrial hyperplasia, epilepsy, and osteosclerosis.

In the aforementioned cases it is advisable for the doctor to carefully evaluate the cost / benefit ratio by carefully informing the patient of the potential side effects and the symptoms that precede them.

In the event that you opt for hormone replacement therapy, the doctor should establish a schedule of periodic checks to assess the health status of the patient and the tolerability of the therapy.

ANGELIQ ® contains lactose so that its intake in patients with lactase enzyme deficiency, poor glucose / galactose absorption or lactose intolerance, could be associated with severe gastrointestinal disorders.

PREGNANCY AND BREASTFEEDING

The absence of clinical trials able to characterize the safety profile of ANGELIQ ® and the presence of experimental studies showing potentially dangerous side effects of estrogen on the fetus, contraindicate the use of this medicine throughout the pregnancy.

Furthermore, given the ability of both active ingredients and related metabolites to permeate the breast filter, concentrating in breast milk, the aforementioned contraindication also extends to the subsequent breastfeeding period.

Interactions

Given the hepatic metabolism of estradiol and drospirenone, both supported by enzymes belonging to the family of cytochromes, it is evident that the simultaneous intake of active ingredients inducing such enzymes as primidone, phenytoin, barbiturates, carbamazepine (used for the treatment of epilepsy), rifampicin (used to treat tuberculosis), ampicillin, tetracycline, griseofulvin (antibiotics used for the treatment of infectious diseases), ritonavir, modafinil and sometimes St. John's wort (hypericum perforatum) could cause a decrease in the effects therapeutic products of ANGELIQ ®

Furthermore, in light of the antimineralocorticoid effect of drospirenone, it is possible to predict a modest drop in blood pressure in hypertensive women, especially if already treated pharmacologically.

Contraindications ANGELIQ ® - Estradiol + Drospirenone

ANGELIQ ® contraindicated in case of hypersensitivity to the active ingredient or to one of its excipients, in case of vaginal bleeding of unknown origin, breast cancer or estrogen-progestin dependent tumors, changes in liver and kidney function, existing or previous thromboembolic processes

Undesirable effects - Side effects

Careful post-marketing monitoring and different clinical trials have shown that taking ANGELIQ ® may be associated with side effects:

Frequent such as: headache, depression, changes in mood, abdominal pain, nausea, abdominal swelling, asthenia and localized edema;
Uncommon: weight gain and changes in appetite, sleep disturbances, paraesthesia and dizziness, palpitations, thrombo-embolic events, migraine, skin diseases, urinary tract infections, breast and endometrial carcinomas;
Rare such as: myalgia, cholelithiasis, dizziness and anemia.

However, in spite of the frequency, the side effects that are of major concern from the clinical point of view are those relating to estrogen-dependent tumor transformations and to embolic thrombus events of an acute nature, whose frequency appears to be correlated to the length of the treatment period.