the package insert of the medicine is Evista. Active principles hydrochloride raloxifene.
EVISTA is indicated for the prevention and treatment of osteoporosis in women after menopause and also to reduce the risk of breast cancer in post-menopausal women with osteoporosis. The occurrence of the number of fractures, vertebral size was reduced. Although the reduction in the incidence of other fractures is not significant, the risk of these fractures decreases with the use of EVISTA. At the time of choosing between treatment with EVISTA or other therapies for women after menopause, one should take into account the symptoms of the menopause and the effects on the breasts and the uterus.
When should I not use?
EVISTA is contraindicated in women who are or may become pregnant. Treatment with EVISTA during pregnancy increases the risk of problems in the development of the fetus. EVISTA is contraindicated in patients who have or have had thrombosis (blood clot in the vein) with or without embolism (obstruction of the vein), patients with allergy to raloxifene or to any ingredient of the tablet. EVISTA should not be used in men or children, as well as in women who are pre-menopausal. The use of EVISTA is not recommended in patients with hepatic insufficiency (a malfunction of the liver) or who are breastfeeding. Care should be taken when prescribing EVISTA to patients in post-menopause with a history of stroke, or other factors a significant risk of stroke.
How to use?
The recommended dose is one tablet of 60 mg of EVISTA, administered once a day, orally, may be taken at any time of day, independent of meals. It is not necessary to adjust dose for patients at an advanced age. Due to the nature of the illness, it is expected that
EVISTA is used as a treatment in the long term. In women with a diet low in calcium and vitamin D, it is recommended to administer add-ins
these substances. Follow the guidance of your doctor, always respecting the schedules, doses and duration of treatment. Do not stop treatment without the knowledge of your doctor.
What are the evils that can cause me?
The majority of adverse reactions was mild and not required discontinuation of treatment. Thus, the adverse reactions during clinical studies with EVISTA were: hot flashes (flushes, hot flashes, or heat waves), cramp in the legs, peripheral edema (swelling of the hands, feet and legs), superficial thrombophlebitis [a disease characterized by thrombosis (blood clot) within the vein surface, with inflammatory reaction of the vein wall and the neighboring tissues],
muscle spasms and cholelithiasis (presence of gallstones in the gall bladder). In the follow-up after the launch of EVISTA, the following adverse events have been reported: gastrointestinal symptoms such as nausea, vomiting, abdominal pain, upset stomach (dyspepsia), skin rash, rise in blood pressure, headache including migraines, mild symptoms of the breast such as pain, enlargement and tenderness to palpation, decreased blood platelets
(thrombocytopenia), arterial occlusion (severe acute thromboembolic disease blood), swelling (peripheral edema) and the blood clot inside the deep veins (thromboembolic disease venous).
Warnings and Precautions
what should I know before using?
-Accident vascular cerebral (avc): the balance risk/benefit on the use of raloxifene in post-menopausal women with a history of cerebral vascular accident (stroke) or other significant risk factors of stroke, such as transitory ischemic events or atrial fibrillation, should be considered when raloxifene is prescribed. In a study of women post-post-menopausal making use of raloxifene with a history of coronary heart disease or with high risk of coronary events, the incidence of stroke, myocardial infarction, hospitalization for acute coronary syndrome (acs), cardiovascular mortality, or all mortality were compared with placebo. however, there was an increase in mortality due to stroke. the incidence of mortality from stroke was 1.5/1,000 women per year for the group receiving placebo versus 2.2/1,000 women per year for the group receiving raloxifene. Venous thromboembolic events: raloxifene is associated with a
greater risk of developing episode thromboembolic, which is similar to the risk related to hormone replacement therapy. You must take into account the risk/benefit in all patients with risk of venous thromboembolic events of any aetiology. Treatment with evista should be discontinued in case of disease or condition that can lead to a prolonged period of immobilization. The interruption of treatment should be made as soon as possible in case of illness or 3 days prior to the immobilization occur. the therapy should not be restarted until the initial condition has resolved and the patient is fully mobile.
-Hepatic impairment: raloxifene is metabolized primarily in the liver. the effectiveness of raloxifene has not been studied in patients with hepatic insufficiency. Raloxifene was studied in a single dose in patients with cirrhosis (child pugh class a), with serum bilirubin ranging in the range of 0.6 to 2.0 mg/dl. plasma concentrations of raloxifene were approximately 2.5 times higher than in the control group, and related to the total concentration of bilirubin. Until safety and efficacy have been evaluated in patients with hepatic insufficiency, the use of evista is not recommended in this population of patients. serum bilirubin total, gamma-glutamyl transferase, alkaline phosphatase, sgot and sgpt should be monitored during treatment if observed high values. Use in pre-Menopause: there is no indication for use of evista in pre-menopause (see contraindications).
-Concomitant use with hormone therapy systemic: safety information on the concomitant use of raloxifene and hormone therapy systemic (estrogen with or without progestin) is limited and, consequently, the concomitant use of raloxifene with estrogen systemic is not recommended.
-Endometrial cancer: raloxifene is not related with proliferation endometrial. any uterine bleeding/vaginal unexpected during therapy with evista should be well-researched.
-Hypertriglyceridemia-induced estrogen: in patients with a history of hypertriglyceridemia induced by oral estrogen (> 5,6 mmol/l), raloxifene may be associated with an increase in triglycerides, serum. patients with this medical history should be monitored as to the triglycerides serum when they are using raloxifene.
-Vasodilation: raloxifene is not effective in reducing manifestations vasomotoras (flushing, hot flashes, or heat waves) associated with deficiency of estrogen.
the use of raloxifene is not indicated in male patients.
-Carcinogenesis, mutagênese, damage to fertility: in carcinogenicity study for 2 years in rats, it was observed an increase in the incidence of tumors of ovarian origin in cells in the teak-grit faced females who received 279 mg/kg/day of raloxifene. the exposure systemic (area under the curve – auc) of raloxifene in this group was approximately 400 times larger than the women post-post-menopausal who have received a dose of 60 mg. in a carcinogenicity study of 21 months in mice, there was an increase in the incidence of tumours of the interstitial cells testicular, adenomas and adenocarcinomas prostáticos in males that were given 41 or 210 mg/kg, and leiomioblastoma prostate in males that received 210 mg/kg. in female rats given 9 to 242 mg/kg (0.3 to 32 times the auc in humans), there has been an increase in the incidence of tumors ovarian benign and malignant derivatives of the cells in the teak-grit faced and benign tumors originating in epithelial cells. rodents females in these studies were treated during their reproductive cycle when the ovaries were active and highly responsive to hormonal stimulation. unlike ovaries highly responsive in this model, rodents, ovarian human after menopause is relatively non-responsive to the stimulation of hormones for breeding. raloxifene was not genotoxic in any of the conventional tests of routine in vivo or in vitro.
there were no pregnancies when raloxifene (≥ 5 mg/kg) was administered to male and female rats before and during mating. in female rats, at doses of 0.1 to 10 mg/kg/day, raloxifene disrupted the cio (cycle of estrus) during the treatment, but the mating fertile were not delayed after the end of treatment, although there have been reduction in marginal in litter size, increase in the duration of gestation and the change in timing of neonatal development. the treatment during the period of pre-deployment female rats acasaladas slowed and/or stopped the deployment embryo, resulting in pregnancy prolonged and a reduction in litter size, but development of offspring to weaning was not affected. these reproductive effects are consistent with the profile of pharmacological of raloxifene (see contraindications). Studies were performed of teratology in rabbits and rats. in rabbits were observed abortions and a low rate of ventricular septal defects (≥ 0.1 mg/kg) and hydrocephalus (≥ 10 mg/kg). in rats, there occurred delay in fetal development, changes in the walls and cavities of the kidney (≥ 1 mg/kg). Raloxifene is a potent anti-estrogen in the uterus of rats and prevents the growth of breast tumours is estrogen-dependent in mice or female rats.
Use during pregnancy and lactation: pregnancy category x: evista should be used only in women post-post-menopausal. should not be taken by women with the potential to become pregnant. raloxifene may cause fetal harm when administered to a pregnant woman. if this drug is used during pregnancy or if the patient becomes pregnant while taking this drug, the patient should be informed of the potential damage to the fetus. Evista should not be used by lactating women (see contraindications). it is not known whether raloxifene is excreted in human milk (evista can affect fetal development).
Use in the elderly, children and other risk groups evista should not be used in children. their use is not indicated for men or women in pre-menopause. there is no need of dose adjustment for the elderly. it is not recommended the use of evista in patients with liver failure.
what to do if someone use a larger amount than is recommended?
In clinical studies, have not been reported superdose with raloxifene. Not have been reported fatalities associated with the superdose. In adults, symptoms reported by patients who took more than 120 mg how to intake only included cramping in legs and dizziness. In some cases, were not reported adverse events as results of the superdose. In superdose accidental in children 2 years of age, the maximum dose reported was 180 mg. In children, the symptoms reported include: ataxia (lack of motor coordination), dizziness, vomiting, skin rash, diarrhea, tremor, and redness, as well as, the elevation of an enzyme of the blood, alkaline phosphatase. There is no specific antidote for raloxifene. In the case of a suspected superdose, immediately seek the service of the nearest health. Do not try to give any medicine to the patient intoxicated, as this can worsen the picture.