GRACIAL ® is a drug based on ethinyl estradiol + desogestrel
THERAPEUTIC GROUP: Biphasic systemic hormonal contraceptives based on progestins and estrogens
IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects
Indications GRACIAL® - Contraceptive Pill
GRACIAL ® is used as an oral contraceptive.
GRACIAL® Action Mechanism - Contraceptive Pill
GRACIAL ® is a biphasic oral contraceptive due to the presence of ethinyl estradiol and desogestrel at different concentrations among the various tablets.
The rationale of the biphasic formulation consists in administering estrogens and progestins in ratios that reflect those present physiologically during the menstrual cycle, thus ensuring better control of the cycle, a reduction in associated pain and a decrease in intermenstrual bleeding spotting.
From the contraceptive point of view, on the other hand, GRACIAL ® carries out its activity through an inhibitory action on the hypothalamic-pituitary axis that leads to a significant decrease in endogenous gonadotropin concentrations necessary both for correct follicular maturation and for subsequent ovulation.
In addition to the hormonal effects, the combination ethinyl estradiol / desogestrel, allows to induce substantial changes at the uterine level, both on the chemical-physical composition of the cervical and endometrial mucus, such as to make the ascent of the spermatozoa in the female genital tract more difficult and possible embryonic nesting.
Studies carried out and clinical efficacy
1. BIPHASIC ORAL CONTRACEPTIVES AND METABOLIC PARAMETERS
An interesting study demonstrating how biphasic oral contraceptives such as GRACIAL ® can guarantee the same inhibition of follicular maturation of triphasic contraceptives, while improving some metabolic parameters such as the HDL / LDL ratio
2. BIPHASIC CONTRACTS IN THE CLINICAL PRACTICE
Extensive clinical study conducted on over 2200 patients who demonstrated how switching to biphasic oral contraceptives containing ethinyl estradiol and desogestrel can improve the tolerability of contraception while improving control of the cycle and skin disorders such as acne.
3. BIPHASIC ORAL CONTRACEPTIVES AND HEMOSTASIS
Work that shows how the intake of biphasic oral contraceptives based on ethinyl estradiol and desogestrel does not induce any kind of variation on the blood parameters linked to the haemostatic balance.
Method of use and dosage
GRACIAL ®
7 blue coated tablets of 40 mcg of ethinyl estradiol and 25 mcg of desogestrel;
15 white coated tablets of 30 mcg of ethinyl estradiol and 125 mcg of desogestrel;
the seven blue tablets must be taken every day, preferably always at the same time, during the first week and immediately followed for the next 15 days by white ones.
The 21-day intake cycles must therefore be interspersed with a week of suspension, in which the appearance of suspension bleeding linked to histological changes induced on the endometrium is physiological.
The beginning of the normal intake cycle, which normally coincides with the first day of menstruation, may change in the case of recent pregnancies or abortions or if it came from an alternative contraceptive method.
In the above cases and following forgetfulness it would be necessary to consult your doctor and strictly adhere to his instructions.
GRACIAL® Warnings - Contraceptive Pill
The administration of GRACIAL ® must be preceded by a careful medical-gynecological examination in order to evaluate the prescriptive appropriateness and the possible presence of conditions predisposing to the development of even serious adverse reactions.
The greater cardiovascular risk, the disorders affecting the endocrine-metabolic and psychiatric system to which patients undergoing hormonal oral contraceptives are subjected, requires a careful evaluation of their health status and in particular for those suffering from diabetes; overweight; hypertension; heart valve defects or some heart rhythm disorders; superficial phlebitis (venous inflammation), varicose veins; migraine; depression; epilepsy; high levels of cholesterol and triglycerides in the blood, present or past, even in close family members; breast lumps; previous, in next family members, of breast cancer; liver or gallbladder disease; Crohn's disease or ulcerative colitis (chronic inflammatory bowel disease); systemic lupus erythematosus (pathology that affects the skin of the whole body); hemolytic-uremic syndrome (blood clotting disorder that causes renal failure); sickle cell disease; porphyria; chloasma, present or previous (patches on the skin with yellowish-brown pigmentation, in particular on the face.
In the aforementioned cases the physician should carefully inform the patient of all the potential side effects related to the intake of GRACIAL ® and opt for this contraceptive system only after having carefully evaluated the risk / benefit ratio and set a series of periodic medical checks .
GRACIAL ® 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
The use of oral estro-progestin contraceptives such as GRACIAL ® is contraindicated during pregnancy, given the lack of studies able to characterize the safety profile of the drug for fetal health.
Furthermore, the ability of ethinyl estradiol and desogestrel to pass through the breast filter and concentrate in breast milk also extends the aforementioned contraindication to the subsequent breastfeeding period.
Interactions
Ethinylestradiol and desogestrel are two active ingredients metabolized at the hepatic level by citrochromial enzymes, an enzymatic class particularly subject to induction and inhibition.
More precisely active ingredients such as primidone, phenytoin, barbiturates, carbamazepine, (used for the treatment of epilepsy), rifampicin (used to treat tuberculosis), ampicillin, tetracyclines, griseofulvin (antibiotics used for the treatment of infectious diseases), ritonavir, modafinil and sometimes St. John's wort (hypericum perforatum), could increase hepatic estrogen-progestin metabolism, thus reducing the contraceptive efficacy of GRACIAL ®
In these cases it may be useful to use alternative contraceptive methods that can increase coverage.
The use of oral contraceptives has often been associated with the variation of some laboratory parameters, with significant alterations affecting the markers of hepatic, thyroid, adrenal and renal function.
GRACIAL® Contraindications - Contraceptive Pill
GRACIAL ® is contraindicated in case of current or previous venous thrombosis, stroke, hypertension, metabolic pathologies such as diabetes mellitus, hypertension and dyslipidemia, alterations of liver and kidney function, 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
The presence of innovative progestogens such as desogestrel and the biphasic formulation, such as to reproduce more similarly the physiological hormonal fluctuation, are not able to eliminate some particularly unpleasant side effects.
Mood alteration, headache, nausea and abdominal pain, increased breast tension and tenderness, weight gain, vomiting and diarrhea, migraine and skin diseases are in fact the most common disorders associated with the intake of oral estrogen-progestins such as GRACIAL ®
Fortunately, the cases of hypersensitivity, arterial and venous thromboembolic disorders, hypertension and coronary artery disease, biliary lithiasis, liver tumors and mammary carcinomas for which the immediate suspension of treatment becomes necessary, are rarer.
Note
GRACIAL ® is salable only under medical prescription.
