Flutastad tablets

Flutastad

  • Active Ingredient: Flutamide
  • 250 mg
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What is Flutastad?

The active ingredient of Flutastad brand is flutamide. Flutamide is an antiandrogen. It works in the body to prevent the actions of androgens (male hormones). C11H11F3N2O3 M.W. 276.21 Flutamide is a buff to yellow powder. Each capsule, for oral administration, contains 125 mg Flutamide and has the following inactive ingredients: black iron oxide, corn starch, D&C yellow #10 aluminum lake, FD&C blue #1 aluminum lake, FD&C blue #2 aluminum lake, FD&C red #40 aluminum lake, gelatin, lactose monohydrate, magnesium stearate, red iron oxide, sodium lauryl sulfate, titanium dioxide and yellow iron oxide.

Used for

Flutastad is used to treat diseases such as: Hirsutism, Prostate Cancer.

Side Effect

Possible side effects of Flutastad include: sores, ulcers, or white spots on the lips or in the mouth; swelling of the breasts or breast soreness in both females and males; continuing diarrhea; Depression; light-colored stools.

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Administration

Flutastad is taken as a 250 mg oral capsule given every 8 hours.

For stage B2-C prostatic carcinoma, it is advised that patients take Flutastad in combination with a gonadotropin-releasing hormone analog that is started eight weeks before the initiation of radiation therapy and continued throughout the course of radiation treatment.

For stage D2 metastatic carcinoma of the prostate, it is advised that the patient take Flutastad in combination with a gonadotropin-releasing hormone analog.

Can Flutastad cause problems?

Along with their useful effects, most medicines can cause unwanted side-effects although not everyone experiences them. The table below contains some of the most common ones associated with Flutastad. You will find a full list in the manufacturer's information leaflet supplied with your medicine. The unwanted effects often improve as your body adjusts to the new medicine, but speak with your doctor or pharmacist if any of the following continue or become troublesome.

More About Flutam >Definition from the NCI Drug Dictionary - Detailed scientific definition and other names for this drug.

MedlinePlus Information on Flutastad - A lay language summary of important information about this drug that may include the following:

  • warnings about this drug,
  • what this drug is used for and how it is used,
  • what you should tell your doctor before using this drug,
  • what you should know about this drug before using it,
  • other drugs that may interact with this drug, and
  • possible s >Drugs are often studied to find out if they can help treat or prevent conditions other than the ones they are approved for. This patient information sheet applies only to approved uses of the drug. However, much of the information may also apply to unapproved uses that are being studied.

Flutastad (FLUT) is an antiandrogen which interferes the binding of androgen to androgen receptor in target organs.

Observational studies

Although Flutastad is effective in treating hirsutism, adverse reactions are very frequent and long-term adherence is poor. In one study over 7 years, of 83 women who took Flutastad 250 mg/day alone or in combination with an oral contraceptive containing ethinylestradiol 20 micrograms and desogestrel 150 micrograms, 34 had one or more adverse reaction during follow-up, 28 had at least one adverse reaction that was possibly related to the study drug, and 20 withdrew because of adverse reactions, hepatotoxicity being the most troublesome; during follow-up, as many as 59% abandoned the study .

Flutam > Flutastad is a synthetic nonsteroidal drug that is a competitive antagonist of the androgen receptor. After oral administration, Flutastad undergoes extensive first-pass metabolism with formation of several oxidized metabolites. Formation of electrophilic metabolites is catalyzed via CYP3A and CYP1A . Experimental studies in rat hepatocytes suggest that toxicity from the electrophilic metabolites occurs through depletion of hepatocyte GSH, which is accompanied by oxidative stress. Toxicity to mitochondria is manifested by depression of mitochondrial respiration and ATP formation, but the study did not report whether mitochondrial toxicity was due to depletion of mitochondrial GSH.

Liver injury presents with marked elevations of bilirubin and a wide range in elevation of serum aminotransferases. The predominant histological feature determined on autopsy is marked-to-massive hepatic necrosis. In a multicenter study of 905 patients treated with Flutastad, liver tests with elevations >4×ULN occurred in 0.8% of patients . According to postmarketing surveillance, severe liver disease due to Flutastad has occurred in 46 patients with 20 fatalities . The rate of serious liver injury is estimated to be 3 per 10,000 Flutastad users, based on the number of prescriptions written.

When you have Flutastad

You might have Flutastad before or during other hormone treatments called LH blockers (such as goserelin, leuprorelin and triptorelin). LH blockers work by lowering the level of testosterone (the male sex hormone). It stops the release of lutenising hormone from the pituitary gland.

You need to take Flutastad before you start some other types of hormone treatment because they can take a few weeks to lower your testosterone. During this time they can make your symptoms worse. This is called tumour flare.

If you are having Flutastad to stop a flare reaction, you take it for a few days before starting the LH blocker, and stay on it for about 4 to 6 weeks.

How Flutastad works

Prostate cancer needs the male hormone testosterone to grow. Testosterone is also called an androgen.

Flutastad is a type of hormone drug called an anti androgen. It stops testosterone from reaching the cancer cells. This can slow the growth of your cancer and may shrink it.

11.09.3 Flutastad

Flutastad (FLUT) is an antiandrogen which interferes the binding of androgen to androgen receptor in target organs. Effects of FLUT on spermatogenesis have recently been summarized by Anahara et al. (2008) . Both neonatal and adult mice showed morphological abnormalities in the testis after subcutaneous injections of FLUT at 0.012 mg kg −1 b.w. for 5 days. FLUT apparently exerts its effects via depolymerization of actin bundles at the apical ES but not basal ES by tyrosine phosphorylation of cortactin ( Anahara et al. 2006a,b ) ( Table 3 ). However, FLUT seems to target cortactin specifically at the apical ES but not at the basal ES. Cortactin is an F-actin binding protein and its tyrosine phosphorylation status is directly correlated to actin bundle remodeling in chinese hamster ovarian (CHO) cells ( Fan et al. 2004 ), as well as centrosome separation during mitosis ( Wang et al. 2008 ). Cortactin was localized to the heads of elongated spermatids when examined by immunohistochemistry. When mice were treated with FLUT at 0.012 mg kg −1 b.w. for 5 days, the protein level of cortactin was significantly reduced at stages VI–IX of the seminiferous epithelial cycle, concomitant with a significant increase in tyrosine phosphorylated cortactin protein in the testis ( Anahara et al. 2006a,b ). Besides its effects on disrupting the association between Sertoli–germ cell at the apical ES, subcutaneous administration of FLUT was shown to perturb the Sertoli–Sertoli cell interaction by downregulating the expression of TJ protein occludin in rat testis ( Gye and Ohsako 2003 ). It is likely that FLUT mediates its effects on cell junctions by blocking androgen action in the testis since testosterone has been shown to upregulate occludin expression in Sertoli cell cultures ( Chung and Cheng 2001 ) and promote junction integrity at the BTB ( Yan et al. 2008a ).

Table 3 . Effects of Flutastad on cell junctions in the testis

Before taking Flutastad

Some medicines are not suitable for people with certain conditions, and sometimes a medicine can only be used if extra care is taken. For these reasons, before you start taking Flutastad it is important that your doctor knows:

  • If you have any problems with the way your liver works.
  • If you have a heart condition.
  • If you have a rare inherited blood disorder called porphyria.
  • If you are taking any other medicines. This includes any medicines which are available to buy without a prescription, as well as herbal and complementary medicines.
  • If you have ever had an allergic reaction to a medicine.

Flutam >

To help prevent diarrhea, avoid dairy products such as milk, cheese, and yogurt. Do not use laxatives while taking Flutastad.

This medicine 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.

Other drugs may interact with Flutastad, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.


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