FEDRA ® is a drug based on ethinyl estradiol + gestodene
THERAPEUTIC GROUP: Systemic hormonal contraceptives - Progestin and estrogens, fixed combination
IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects
Indications FEDRA ® - Contraceptive Pill
FEDRA ® is used as an oral contraceptive.
Action mechanism FEDRA ® - Contraceptive Pill
The advent of third-generation oral contraceptives such as FEDRA ® characterized by the presence of a synthetic progestogen such as Gestodene, has made it possible to significantly reduce some of the most complained of side effects by patients who consume combined oral contraceptives such as weight gain, water retention, hypertension and skin diseases like acne.
Despite the reduction of these events, the mechanism underlying the contraceptive action of drugs like FEDRA ® remains almost unchanged compared to its predecessors, exerting both an inhibitory action on the release of gonadotropins, then on the subsequent ovulation process that a change in the chemical characteristics -physics of uterine mucus and endometrium such as to counteract the spermatozoa rising towards the salpingi and the eventual embryo nesting.
Taken orally, both active ingredients reach maximum plasma concentration in about 2 hours, and bound to plasma proteins such as SHBG and albumin to a small extent, reaching target tissues exerting their biological effect.
Following an estimated half-life of around 24 hours and an important hepatic metabolism, both ethinylestradiol and gestodene are eliminated as active metabolites through feces and urine.
Studies carried out and clinical efficacy
1. THIRD GENERATION AND HEART RATE ACCOUNTS
Given the risk of occurrence of embolic and cardiovascular thrombus episodes associated with the use of oral contraceptives, the effects of ethinylestradiol / gestodene on heart rate were evaluated in 55 women within 26 years. The study demonstrated the absence of changes in heart rate.
2. GESTODENE AND TROMBOEMBOLISMO
Countercurrent study that evaluates the effects of gestodene on the risk of occurrence of embolic thrombus events, after more than 10 years from the placing on the market. This work demonstrates how the administration of gestodene does not correlate with a significant increase in the risk of embolic thrombus, justifying the previous results obtained by other studies as a normal variability determined by the choice of enrolled populations.
3. THIRD GENERATION CONTRACTS AND C REACTIVE PROTEIN
C-reactive protein is an independent cardiovascular risk factor, very correlated to the incidence of serious diseases. The administration of third-generation oral contraceptives proved to be able to increase the concentrations of this protein, thus increasing the risk of developing cardiac and vascular events.
Method of use and dosage
FEDRA ® 20 mcg coated tablets of ethinyl estradiol and 75 mcg of gestodene:
the contraceptive action of combined oral contraceptives is guaranteed by the daily intake of a tablet always at the same time.
The recruitment scheme in these cases includes 21-day cycles, to be initiated the first time, on the first day of menstruation, interspersed with 7-day withdrawal periods, useful for ensuring the endometrial detachment, therefore a suspension bleeding similar to physiological menstruation.
Medical supervision is essential in the initial phase of treatment and after having forgotten about taking one tablet for one or more days, in case of a previous or imminent pregnancy, in case of variation of the contraceptive used and in case of all those pathological conditions or predisposed described in the following paragraph.
It is useful to remember that the maximum contraceptive coverage tends to decrease as early as 36 hours after taking the last tablet, until normal hormonal control is resumed, which is generally achieved after 7 days of suspension.
FEDRA ® warnings - Contraceptive Pill
The biological complexity of the action of combined oral contraceptives and the presence of even serious side effects such as thromboembolic events require careful medical examination, aimed at assessing the therapeutic appropriateness and the possible presence of predisposing factors, before undertaking the taking these drugs.
The presence of existing or previous cardiovascular and neoplastic diseases, liver and kidney diseases, neurological and psychiatric disorders, metabolic pathologies such as diabetes and risk factors for cardiovascular diseases such as obesity or smoking, should push the doctor towards a more accurate assessment of the cost / benefit ratio, considering the need for periodic checks on ongoing therapy.
To further reduce the appearance of clinically relevant side effects it is useful that the patient knows how to recognize the first signs of the morbid states related to the therapy so that he can promptly resort to useful remedies under the guidance of his doctor.
FEDRA ® contains lactose so that its intake in patients with lactase enzyme deficiency, glucose / galactose malabsorption or lactose intolerance, could be associated with severe gastrointestinal disorders.
PREGNANCY AND BREASTFEEDING
Although the scientific literature has not observed any side effects on fetuses accidentally exposed to estrogen-progestins, FEDRA ® intake is contraindicated during the entire pregnancy period.
Furthermore, given the ability of ethinylestradiol and gestodene to pass through the breast filter and concentrate in breast milk, the aforementioned contraindication also extends to the subsequent breastfeeding phase.
Interactions
Given the hepatic metabolism to which ethinylestradiol and gestodene present in FEDRA ® are subjected, it is important to remember that active ingredients modulating the activity of cytochromial enzymes can significantly alter their pharmacokinetic characteristics, reducing the contraceptive capacity of the drug.
Rifampicin, phenytoin, barbiturates, antiretrovirals, antibiotics, herbal remedies such as St. John's wort are just some of the cytochrome p450 inducing drugs.
At the same time, taking FEDRA ® could alter the therapeutic activity of numerous drugs, so that any concurrent administration of other active ingredients should be preceded by medical advice.
Contraindications FEDRA ® - Contraceptive Pill
FEDRA ® is contraindicated in case of current or previous venous thrombosis, stroke, hypertension, metabolic disorders such as diabetes mellitus, hypertension and dyslipidemia, liver and kidney function changes, malignant pathologies, neuro-psychiatric disorders, motor disorders, undiagnosed gynecological disorders and in case of hypersensitivity to the active ingredient or to one of its excipients.
Undesirable effects - Side effects
Although third-generation oral contraceptives have significantly decreased the incidence of some side effects of classic contraceptives such as acne, weight gain and water retention, studies show a slight increase in the incidence of thromboembolic episodes estimated at around 20/30 cases per 100, 000 users .
Fortunately, serious side effects such as the one just described tend to occur especially in predisposed individuals, whereas FEDRA ® has been associated more frequently with headache, depression, nausea, vomiting, abdominal pain, rash, urticaria, increased breast tension and associated pain.
All the above reactions, however, present a transitory character, tending to regress spontaneously once therapy is suspended.
Note
FEDRA ® can be sold only under medical prescription.
