Faslodex Astra injection treatment for progressive breast cancer (2 tubes x 5 ml)

Dosage form Box of 2 tubes x 10ml
Specifications Flvestrant

Ingredient

Composition informationContent
Flvestrant50mg/ml

Uses

Indications

Faslodex are indicated for treatment of women after menopause with advanced breast cancer on the spot or metastases with positive estrogen receptors, recurrence in or after supplementary estrogen resistance treatment, or progressive while being anti -estrogen treatment.

Pharmacokology

Treatment group: endocrine, anti -estrogen, ATC code: L02BA03.

The mechanism of impact and pharmacological impact of Flvestrant is a competitive substance with the estrogen receptor (ER), with an affinity equivalent to estradiol. Flvestrant prevents the vegetative activity of estrogen without a partial co -action (similar to estrogen). The mechanism of action is associated with the regulation of ER-Protein levels. Clinical trials in postmenopausal women with Tien Phat Breast cancer show that FluLien is a significantly reduced ER-Protein air conditioner in tumors with a positive estrogen receptor compared to placebo. The progesterone receptor expression is also significantly reduced, corresponding to the lack of internal estrogen -manual impact. Flvestrant 500 mg has also been shown to reduce ER and fertility markers (Proliferation Marker) KI67 at a greater level of 250 mg greater than fullant in breast tumors on postmenopausal women in the context of supplementary supplementary.

The endometrial effect on the postmenopausal

Precaessing data does not show the irritation effect of fullant on endometrium after menopause. A 2 -week study in healthy menopausal women volunteered to treat with ethinylestradiol 20 mcg/day for teachers to treat first with Faslodex 250 mg for a significant reduction in postmenopausal irritation compared to the previous treatment with placebo, when assessed by ultrasound technique of endometrial thickness.

Additional treatment for breast cancer patients

In 2 short -term studies (1 and 12 weeks) on menopausal patients with benign gynecological diseases, ultrasound does not see a significant difference in the endometrial thickness between the group using fullant and placebo.

Effects on bone

There is no long -term research data on the effects of fullant on bones. Additional treatment for patients with breast cancer

Children

Faslodex is not indicated for children.

A phase II study, open label, assessment of safety, effectiveness and pharmacokinetics of Flvestrant in 30 girls from 1 to 8 years old with puberty early progress (Progressive Precerty) related to McCune Albright (MAS) syndrome. These children are used in intramuscular fullant at a dose of 4 mg/kg monthly. This 12 -month research has evaluated a group of MAS criteria and replaced a vaginal bleeding frequency and reduced the rate of SOM bone maturity. The steady-state-staule concentration (Steady-State-based of Flvestrant in children in this study is compatible with this concentration in adults. There are no new concerns about safety arising from this small level of research, although there is no 5 -year data.

Pharmacokinetics

absorption

After the endual intramuscular faslodex, Flvestrant is absorbed slowly and the maximum concentration in plasma (CMAX) is achieved after about 5 days. Using faslodex 500 mg dose of contact concentration at or near the dose level at a stable state within the first month ([CV] average = AUC 475 [33.4%] Ng's day/ml, cmax = 25.1 [35.3%] ng/ml, cmin = 16.3 [25.9%] ng/mL corresponding). In a stable state, the plasma fullant concentration is maintained in a narrow range, with a top concentration of the bottom concentration of up to 3 times. After intramuscular injection, the contact concentration is proportional to the dose in the dose of 50 - 500 mg.

Distribution

Flvestrant is distributed quickly and widely. The large appointed distribution volume in a stable state (VDSS) is about 3-5 l/kg, showing a large distribution of external circuit. Flvestrant is highly connected to plasma proteins (99%). Lipoprotein molecules are very low density (VLDL), low density lipoprotein (LDL) and high density lipoprotein (HDL) are the main components. There is no study on protein interaction. The role of Globulin connects sex hormones (SHBG) has not been determined.

Metabolism

The metabolism of Flvestrant has not been fully evaluated, but is related to the combination of some biological transformations similar to endogenous steroids. The metabolites are determined (including 17-ketone metabolites, sulphone, 3-sulphate, 3-and 17-glucuronide) are substances that are less active or have similar activity of fullant about anti-estrogen effects. Studies using liver preparations and recombinant enzymes in humans show that CYP3A4 is the only ISOENZE P450 is related to the oxidation process of Flvestrant, however, on Vivo, non -P450 metabolic lines are more dominant. In-Vitro data shows that Flvestrant does not inhibit isenzyme CYP450.

Elimination

Flvestrant is excreted mainly in the form of metabolism. The main excretion of the stool, with less than 1% is excreted through the urine. Flvestrant has a high clearance, 11 ± 1.7 ml/min/kg, showing the high rate of excretion through the liver. The sale time after intramuscular injection is dominated by the absorption rate and estimates of 50 days.

Special subjects

Dynamic pharmacokinetic analysis data from phase III studies shows that there is no difference in fullant's dynamic specialties at all ages (from 33-89 years old), needing heavy (40-127 kg) or race.

kidney failure

Mild and moderate renal function does not affect the pharmacokinetics of Flvestrant at clinical significance.

Hepatic failure

A clinical test of a single dose has been conducted to evaluate the pharmacokinetic properties of Flvestrant in patients with mild and medium liver impairment (Child-Pugh degrees A and B). Intramuscular injection in high doses in a short time. The area under the curve (AUC) in patients with liver failure increased by a maximum of 2.5 times compared to a healthy Nguyen lover. In patients using Faslodex, the increase in concentration and time of exposure to the drug is expected to be well tolerated. Patients with severe liver failure (C-Pul) have not been evaluated.

Children

FuluDrant's

pharmacokinetics was evaluated in a clinical trial on 30 girls who were puberty early in progress related to McCune Albright syndrome. Pediatric patients aged 1-8 are used in intramuscular fullant at a dose of 4mg/kg/month. Average multiplication (standard deviation - SD) of the bottom concentration in a stable state (cmin, ss) and the area under the curve (AUCSS) is estimated to be 4.2 (0.9) ng/ml and 3680 (1020) ng*hour/ml. Although the data collected is limited, the bottom concentration in the stable state of Flvestrant in children is compatible with this concentration in adults.

Before taking Faslodex Astra injection treatment for progressive breast cancer (2 tubes x 5 ml)

How to use

Faslodex medicine is used in injection, which should be done by professional health workers.

Faslodex is indicated with 2 continuous 5 ml injections, slow intramuscular injection (1-2 minutes/time), 1 injection in each buttock.

Details on how to use, see more in manuals.

Dosage

Adults (including the elderly)

The recommended dose is 500 mg/time/month, adding 500 mg after 2 weeks of treatment with the starting dose.

Special subjects

kidney failure

No dose adjustment for patients with mild and medium renal failure (creatinine clearance ≥ 30 ml/min). Safety and effectiveness have not been evaluated in patients with severe renal impairment (creatinine clearance Hepatic failure

No dose adjustment for patients with mild and medium liver failure. However, because the concentration and time of Flvestrant exposure may increase, it is advisable to use Faslodex carefully for these patients.

Children

Safety and effectiveness of Faslodex in children from birth to 18 years of age has not been determined. The existing data is presented in the pharmacological and pharmacokinetic characteristics section but does not recommend the dose.

What do

do when using overdose? Animal studies have not proved any effects other than the direct or indirect effects on estrogen -resistant activity with high doses of Flvestrant. If an overdose occurs, symptomatic treatment should be treated and supported.

What to do when forgetting a dose?

Side Effects

This item includes information about all the adverse drug reactions of the drug are reported based on clinical trials, reports after circulation of drugs on the market or spontaneous reports. Adultery reactions are often recorded as a reaction at the injection site, weakness, nausea and increased liver enzymes (ALT, AST, ALP).

The following frequency of adultery reaction frequency is calculated based on the Faslodex 500 mg treatment group, in the combination of the safety of the Confirm research (D6997C00002), Finder 1 (D6997C00004), Finder 2 (research D6997C00006) and Newest (Research D6997C00003), are comparison of studies Faslodex 500 mg with Faslodex 250 mg. The following frequency of the following is based on all the adverse reactions of the drug recorded and arrested by the researcher of the cause and effect.

The following adultery reactions are classified by frequency and organ systems (Soc). Frequency is divided according to the following convention: Very common (> = 1/10), common (> = 1/100 = 1/1,000 -

harmful reactions classified by organ and frequency Man Loiia, flushed with face ALP) A

Common Bilirubin increases with rising Drugs are very common , reactions at the injection site hidden.

b reacts at the injection site without bleeding and hematoma at the injection site.

C events are not recorded in the main clinical studies (Confirm, Finder 1, Finder2, Newest). The frequency of occurrence is estimated by the upper limit of 95%trust range, 3/563 (of which 563 is the number of patients in the clinical studies), corresponding to the "rare" frequency classification.

Warnings

Before using the drug you need to read the instructions carefully and refer to the information below.

Contraindicated

Hypersensitivity to active ingredients or any other excipients.

Pregnant and lactating women.

Severe liver failure.

Be cautious when using

Precautions when using Faslodex in patients with mild to moderate liver failure.

Be cautious when using faslodex in patients with severe renal impairment (creatinine clearance

Due to intramuscularly used, cautious use when using Faslodex for patients with atopic bleeding, thrombocytopenia or treating anticoagulants.

thrombosis is often recorded in breast cancer women and is also recorded in clinical studies with Faslodex. This should be considered when indicating Faslodex for patients at risk.

There is no long -term research data on the impact of fullant on bones. Due to the mechanism of action of Flvestrant, there is a risk of osteoporosis when used.

Children

Faslodex does not recommend for children and adolescents because of safety and effectiveness have not been determined in this patient group.

The effect of the drug on driving and operating machinery

Faslodex does not affect or negligible on the ability to drive or operate machinery. However, because weakness is often recorded when using Faslodex, patients with adverse effects should be cautious when driving or operating machinery.

Using drugs for women during pregnancy and lactation

Women are likely to be pregnant

Patients who are likely to get pregnant should take effective contraception when treated.

Pregnant women

Faslodex is contraindicated for pregnant women. If pregnant while taking Faslodex, patients should be notified of the possibility of danger to the fetus and the risk of miscarriage.

breastfeeding women

Must stop breastfeeding when treated with faslodex. Flvestrant is excreted in milk in breastfeeding mice. It is unclear whether Flvestrant will excrete in breast milk.

Contraindicated drug use during breastfeeding due to the risk of serious adverse effects caused by fullant on breastfed babies.

Reproduction

The impact of faslodex on human fertility has not been studied.

Drug interaction

A clinical study on interactive with Midazolam (the substrate of CYP3A4) shows that Flvestrant does not inhibit CYP3A4. Clinical studies interact with rifampicin (CYP3A4 induction) and ketoconazole (CYP3A4 inhibitors) show that there are no clinical changes related to Flvestrant clearance. Therefore, do not need to adjust the dose in patients using Flvestrant simultaneously with CYP3A4 inhibitors or induction drugs.

Cavalry

Because there is no study on similarity, this drug is not mixed with other drugs.

Storage

Store at a temperature of 2 ° C - 8 ° C (in the refrigerator). Preserving the injecting pump containing drugs in the original packaging to avoid light.

Other drugs

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