GRACIAL ® is a drug based on ethinylestradiol + desogestrel
THERAPEUTIC GROUP: Systemic biphasic hormonal contraceptives based on progestogens and estrogens
Indications GRACIAL® - Contraceptive Pill
GRACIAL ® is used as an oral contraceptive.
Mechanism of action GRACIAL® - Contraceptive Pill
GRACIAL ® is a biphasic oral contraceptive due to the presence of ethinylestradiol and desogestrel at different concentrations between the various tablets.
The rationale of the biphasic formulation consists in administering estrogens and progestogens in such ratios as to mirror those physiologically present during the menstrual cycle, thus ensuring better control of the cycle, a reduction in associated pains 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 hypothalamus-pituitary axis which leads to a significant decrease in the endogenous concentrations of gonadotropins necessary for both correct follicular maturation and subsequent ovulation.
In addition to the hormonal effects, the ethinyl estradiol / desogestrel combination allows to induce substantial changes at the uterine level, both on the chemical-physical composition of the cervical mucus and on the endometrial one, such as to make it more difficult for the spermatozoa to rise in the female genital tract. embryonic nesting.
Studies carried out and clinical efficacy
1. BIPHASIC ORAL CONTRACEPTIVES AND METABOLIC PARAMETERS
Eur J Contracept Reprod Health Care. 1997 Sep; 2: 173-80.
A randomized cross-over study comparing pharmacodynamic and metabolic variables of a new combiphasic and a well-established triphasic oral contraceptive.
van den Ende A, Geurts TB, Kloosterboer HJ.
Interesting study that demonstrates 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 CONTRACEPTIVES IN CLINICAL PRACTICE
Eur J Contracept Reprod Health Care. 2001 Jun; 6: 108-14.
A large observational clinical evaluation of a desogestrel-containingcombiphasic oral contraceptive in Germany.
Vree ML, Schmidt J.
Large clinical study conducted on over 2200 patients which demonstrated how switching to biphasic oral contraceptives containing ethinylestradiol and desogestrel can improve contraception tolerability while improving cycle control and skin disorders such as acne.
3. BIPHASIC ORAL CONTRACEPTIVES AND HEMOSTASIS
Adv Contracept. 1995 Sep; 11: 227-37.
The effects of two phasic oral contraceptives on hemostasis and platelet function.
Weinges KF, Wenzel E, Hellstern P, Geurts TB, Dieben TO.
Work that demonstrates how the assumption of biphasic oral contraceptives based on ethinylestradiol 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 light blue coated tablets of 40 mcg ethinyl estradiol and 25 mcg desogestrel;
15 white coated tablets of 30 mcg ethinyl estradiol and 125 mcg desogestrel;
the seven blue tablets must be taken every day, possibly at the same time, during the first week and immediately followed by the white ones for the next 15 days.
The cycles of intake of 21 days must therefore be interspersed with a week of suspension, in which the appearance of a withdrawal bleeding linked to the histological changes induced on the endometrium is physiological.
The beginning of the normal cycle of intake, which normally coincides with the first day of menstruation, could undergo variations in the case of recent pregnancies or abortions or if it came from an alternative method of contraception.
In the aforementioned cases and following a forgetfulness it would be necessary to consult your doctor and strictly follow his instructions.
Warnings GRACIAL® - Contraceptive Pill
The administration of GRACIAL ® must be preceded by a "careful medical-gynecological examination aimed at evaluating the prescribing appropriateness and the possible presence of conditions predisposing to the development of adverse reactions, even serious ones.
The greater cardiovascular risk, the disorders affecting the endocrine-metabolic and psychiatric system to which patients undergoing therapy with hormonal oral contraceptives are subjected, requires a "careful evaluation of their state of health and in particular for those suffering from diabetes; overweight ; hypertension; heart valve defects or certain heart rhythm disturbances; 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 family members of breast cancer liver or gallbladder disease Crohn's disease or ulcerative colitis (chronic inflammatory bowel disease); systemic lupus erythematosus (disease affecting the skin of the whole body); hemolytic-uremic syndrome (blood clotting disorder causing kidney failure); sickle cell anemia; porphyria; Chloasma, present or previous (patches on the skin with yellowish-brown pigmentation, particularly on the face.
In the aforementioned cases, the doctor should carefully inform the patient of all the potential side effects related to taking GRACIAL ® and opt for this contraceptive system only after carefully evaluating the risk / benefit ratio and setting up a series of periodic medical checks. .
GRACIAL ® contains lactose so its intake in patients with lactase enzyme deficiency, glucose / galactose malabsorption or lactose intolerance, could be associated with even serious gastrointestinal disorders.
PREGNANCY AND BREASTFEEDING
The use of estrogen-progestogen oral contraceptives such as GRACIAL ® is contraindicated during pregnancy, given the absence of studies capable of characterizing the safety profile of the drug for the health of the fetus.
Furthermore, the ability of ethinylestradiol and desogestrel to cross the breast filter and concentrate in breast milk extends the aforementioned contraindication also to the subsequent period of breastfeeding.
Interactions
Ethinylestradiol and desogestrel are two active ingredients metabolized in the liver by citrochromial enzymes, an enzyme 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 for the treatment of tuberculosis), ampicillin, tetracyclines, griseofulvin (antibiotics used for the treatment of infectious diseases), ritonavir, modafinil and sometimes St. John's wort (hypericum perforatum), could increase the hepatic estrogen-progestogen metabolism, thus reducing the contraceptive efficacy of GRACIAL ®
In these cases it could be useful to use alternative methods of contraception, able to increase the coverage.
The use of oral contraceptives has often been associated with the variation of some laboratory parameters, with significant alterations in the markers of hepatic, thyroid, adrenal and renal function.
Contraindications GRACIAL® - Contraceptive Pill
GRACIAL ® is contraindicated in case of current or previous venous thrombosis, stroke, hypertension, metabolic diseases such as diabetes mellitus, hypertension and dyslipidemia, impaired liver and kidney function, malignant diseases, neuro-psychiatric disorders, motor disorders, undiagnosed gynecological diseases and in case of hypersensitivity to the active substance 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.
Alteration of mood, headache, nausea and abdominal pain, increased breast tenderness and tenderness, weight gain, vomiting and diarrhea, migraine and skin diseases are in fact the disorders most commonly associated with the use of estrogen-progestogen oral contraceptives such as GRACIAL ®
Fortunately, cases of hypersensitivity, arterial and venous thromboembolic disorders, hypertension and coronary heart disease, biliary lithiasis, liver tumors and breast carcinomas have been rarer, for which immediate suspension of treatment is necessary.
Note
GRACIAL ® can only be sold under medical prescription.
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