What happens if I overdose Arinib?
Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately.
Proper storage of Arinib:
Store Arinib at room temperature, between 68 and 77 degrees F (20 and 25 degrees C), in a tightly closed container. Store away from heat, moisture, and light. Do not store in the bathroom. Keep Arinib out of the reach of children and away from pets.
Overdose of Arinib in details
There is limited clinical experience of overdose of Arinib. There are no reports where a patient has taken a dose excessing 60 mg. No toxicity was observed and no clinically relevant adverse effects have been seen.
Acute toxicity was seen in animals at a dose greater than 45 mg/kg (equivalent to 2.7 g). Clinical trials have been conducted with various dosages of Arinib, up to 60 mg in a single dose given to healthy male volunteers and up to 10 mg daily given to postmenopausal women with advanced breast cancer; these dosages were well tolerated. A single dose of Arinib that results in life threatening symptoms has not been established.
There is no specific antidote to over dosage and treatment must be symptomatic. In the management of an overdose, consideration should be given to the possibility that multiple agents may have been taken. Vomiting may be induced if the patient is alert. Dialysis may be helpful because Arinib is not highly protein bound. General supportive care, including frequent monitoring of vital signs and close observation of the patient, is indicated.
What should I avoid while taking Arinib?
Arinib can pass into body fluids (urine, feces, vomit). Caregivers should wear rubber gloves while cleaning up a patient's body fluids, handling contaminated trash or laundry or changing diapers. Wash hands before and after removing gloves. Wash soiled clothing and linens separately from other laundry.
This medication may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.
Arinib warnings
Ischemic Cardiovascular Events
In women with pre-existing ischemic heart disease, an increased incidence of ischemic cardiovascular events was observed with Arinib in the ATAC trial (17% of patients on Arinib and 10% of patients on tamoxifen). Consider risk and benefits of Arinib therapy in patients with pre-existing ischemic heart disease.
Bone Effects
Results from the ATAC trial bone substudy at 12 and 24 months demonstrated that patients receiving Arinib had a mean decrease in both lumbar spine and total hip bone mineral density (BMD) compared to baseline. Patients receiving tamoxifen had a mean increase in both lumbar spine and total hip BMD compared to baseline.
Cholesterol
During the ATAC trial, more patients receiving Arinib were reported to have elevated serum cholesterol compared to patients receiving tamoxifen (9% versus 3.5%, respectively).
Pregnancy
Patients should be advised that Arinib may cause fetal harm. They should also be advised that Arinib is not for use in premenopausal women; therefore, if they become pregnant they should stop taking Arinib and immediately contact their doctor.
Allergic (Hypersensitivity) Reactions:
Patients should be informed of the possibility of serious allergic reactions with swelling of the face, lips, tongue and/or throat (angioedema) which may cause difficulty in swallowing and/or breathing and to immediately report this to their doctor.
Ischemic Cardiovascular Events
Patients with pre-existing ischemic heart disease should be informed that an increased incidence of cardiovascular events has been observed with Arinib use compared to tamoxifen use.
Bone Effects
Patients should be informed that Arinib lowers the level of estrogen. This may lead to a loss of the mineral content of bones, which might decrease bone strength. A possible consequence of decreased mineral content of bones is an increase in the risk of fractures.
Cholesterol
Patients should be informed that an increased level of cholesterol might be seen while receiving Arinib.
Tamoxifen
Patients should be advised not to take Arinib with Tamoxifen.
Nonclinical Toxicology
Carcinogenesis, Mutagenesis, Impairment of Fertility
A conventional carcinogenesis study in rats at doses of 1.0 to 25 mg/kg/day (about 10 to 243 times the daily maximum recommended human dose on a mg/m2 basis) administered by oral gavage for up to 2 years revealed an increase in the incidence of hepatocellular adenoma and carcinoma and uterine stromal polyps in females and thyroid adenoma in males at the high dose. A dose related increase was observed in the incidence of ovarian and uterine hyperplasia in females. At 25 mg/kg/day, plasma AUC0-24 hr levels in rats were 110 to 125 times higher than the level exhibited in postmenopausal volunteers at the recommended dose. A separate carcinogenicity study in mice at oral doses of 5 to 50 mg/kg/day (about 24 to 243 times the daily maximum recommended human dose on a mg/m2 basis) for up to 2 years produced an increase in the incidence of benign ovarian stromal, epithelial and granulosa cell tumors at all dose levels. A dose related increase in the incidence of ovarian hyperplasia was also observed in female mice. These ovarian changes are considered to be rodent-specific effects of aromatase inhibition and are of questionable significance to humans. The incidence of lymphosarcoma was increased in males and females at the high dose. At 50 mg/kg/day, plasma AUC levels in mice were 35 to 40 times higher than the level exhibited in postmenopausal volunteers at the recommended dose.
Arinib has not been shown to be mutagenic in in vitro tests (Ames and E. coli bacterial tests, CHO-K1 gene mutation assay) or clastogenic either in vitro (chromosome aberrations in human lymphocytes) or in vivo (micronucleus test in rats).
Oral administration of Arinib to female rats (from 2 weeks before mating to pregnancy day 7) produced significant incidence of infertility and reduced numbers of viable pregnancies at 1 mg/kg/day (about 10 times the recommended human dose on a mg/m2 basis and 9 times higher than the AUC0-24 hr found in postmenopausal volunteers at the recommended dose). Pre-implantation loss of ova or fetus was increased at doses equal to or greater than 0.02 mg/kg/day (about one-fifth the recommended human dose on a mg/m2 basis). Recovery of fertility was observed following a 5-week non-dosing period which followed 3 weeks of dosing. It is not known whether these effects observed in female rats are indicative of impaired fertility in humans.
Multiple-dose studies in rats administered Arinib for 6 months at doses equal to or greater than 1 mg/kg/day (which produced plasma Arinib Cssmax and AUC0-24 hr that were 19 and 9 times higher than the respective values found in postmenopausal volunteers at the recommended dose) resulted in hypertrophy of the ovaries and the presence of follicular cysts. In addition, hyperplastic uteri were observed in 6-month studies in female dogs administered doses equal to or greater than 1 mg/kg/day (which produced plasma Arinib Cssmax and AUC0-24 hr that were 22 times and 16 times higher than the respective values found in postmenopausal women at the recommended dose). It is not known whether these effects on the reproductive organs of animals are associated with impaired fertility in premenopausal women.
What should I discuss with my healthcare provider before taking Arinib?
You should not use Arinib if you are allergic to Arinib, if you are breast-feeding a baby, or if you have not yet completed menopause. Arinib is not for use in men or children.
To make sure Arinib is safe for you, tell your doctor if you have:
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heart disease;
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circulation problems;
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a history of stroke or blood clot;
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severe liver disease;
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high cholesterol; or
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osteoporosis or low bone mineral density.
Arinib can decrease bone mineral density, which may increase your risk of developing osteoporosis. Your bone mineral density may need to be tested before and during treatment with Arinib.
Although it is not likely that a postmenopausal woman would be pregnant, Arinib could harm an unborn baby. Do not take this medicine if you are pregnant or may become pregnant. Use effective birth control if you are not past menopause, and tell your doctor right away if you become pregnant during treatment.
It is not known whether Arinib passes into breast milk or if it could harm a nursing baby. You should not breast-feed while you are using Arinib.
You may need to take a pregnancy test before using Arinib, to make sure you are not pregnant.
Arinib precautions
General: Arinib should not be used in premenopausal women. The menopause should be defined biochemically [luteinizing-hormone (LH), follicle stimulating hormone (FSH), and/or estradiol levels] in any patient where there is doubt about menopausal status. There are no data to support the use of Arinib with LHRH analogues.
Co-administration of tamoxifen or estrogen-containing therapies with Arinib should be avoided as this may diminish its pharmacological action.
Effect on Bone Mineral Density: As Arinib lowers circulating estrogen levels it may cause a reduction in bone mineral density with a possible consequent increased risk of fracture.
Women with osteoporosis or at risk of osteoporosis, should have their bone mineral density formally assessed at the commencement of treatment and at regular intervals thereafter. Treatment or prophylaxis for osteoporosis should be initiated as appropriate and carefully monitored.
The use of specific treatments, e.g., bisphosphonates, may stop further bone mineral loss caused by Arinib in postmenopausal women and could be considered.
Hepatic Impairment: Arinib has not been investigated in breast cancer patients with moderate or severe hepatic impairment. Exposure to Arinib can be increased in subjects with hepatic impairment; administration of Arinib in patients with moderate and severe hepatic impairment should be performed with caution. Treatment should be based on a benefit-risk evaluation for the individual patient.
Renal Impairment: Arinib has not been investigated in breast cancer patients with severe renal impairment.
Exposure to Arinib is not increased in subjects with severe renal impairment (GRF <30 mL/min); in patients with severe renal impairment, administration of Arinib should be performed with caution.
Hypersensitivity to Lactose: This product contains lactose. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
Effects on Ability to Drive and Use Machines: Arinib has no or negligible influence on the ability to drive and use machines. However, asthenia and somnolence have been reported with the use of Arinib and caution should be observed when driving or operating machinery while such symptoms persist.
Fertility: The effects of Arinib on fertility in humans have not been studied. Studies in animals have shown reproductive toxicity.
Use in Children: Arinib is not recommended for use in children and adolescents as safety and efficacy have not been established in this group of patients.
Arinib should not be used in boys with growth hormone deficiency in addition to growth hormone treatment. In the pivotal clinical trial, efficacy was not demonstrated and safety was not established. Since Arinib reduces estradiol levels, Arinib must not be used in girls with growth hormone deficiency in addition to growth hormone treatment.
Long-term safety data in children and adolescents are not available.
What happens if I miss a dose of Arinib?
Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.
References
- DailyMed. "ANASTROZOLE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
- DrugBank. "anastrozole". http://www.drugbank.ca/drugs/DB01217 (accessed September 17, 2018).
- MeSH. "Aromatase Inhibitors". https://www.ncbi.nlm.nih.gov/mesh/68... (accessed September 17, 2018).
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Information checked by Dr. Sachin Kumar, MD Pharmacology
