testosterone enanthate

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After intramuscular injection, fulvestrant is slowly absorbed, reaching maximum concentration after about 7 days in plasma. Absorption continues for more than one month, so if monthly injections occurs approximately 2-fold accumulation of the drug. Equilibrium concentration in plasma is established after about 6 monthly injections, with the major part of the accumulation achieved after 3-4 injections.  In the equilibrium state plasma fulvestrant content varies within relatively narrow boundaries – the maximum and minimum values differ by approximately 2-3 times. After intramuscular injection is approximately proportional to exposure dose administered (at a dosage range from 50 to 250 mg). Fulvestrant is characterized by a rapid and extensive distribution . Large apparent volume of distribution  at the equilibrium concentration involves predominantly extravascular distribution. Connection with the plasma protein -99%. The main components include binding fraction of very low density lipoproteins testosterone enanthate, low density lipoproteins and high density lipoproteins.

The role of sex hormone binding globulin has not been established. Metaboh edited fulvestrant include a combination of multiple potential pathways for biotransformation, similar mechanisms of metabolism of endogenous steroids (includes 17-ketone metabolites, sulphone, 3-sulphate, 3- and 17-glucuronide). Identified active metabolites or less equal in activity Fulvestrant is the only  isoenzyme family  that is involved in the oxidation of fulvestrant. However, it appears that in vivo biotransformation prevail . Fulvestrant mainly excreted in feces, urine output of less than 1% of the substance. Specific populations: The pharmacokinetic profile of fulvestrant is independent of age (range 33 -89 years), weight ( 40 -. 127 kg) or race impaired renal function mild to moderate renal impairment did not have a clinically meaningful effect on the pharmacokinetics of fulvestrant.violations of the liver Research pharmacokinetics of fulvestrant in patients with impaired hepatic function have not been conducted.

Indications for use of
locally advanced or disseminated breast cancer testosterone enanthate with positive estrogen receptors in postmenopausal women with the progression after or on a background of anti-estrogen therapy.

Contraindications .


  • hypersensitivity to fulvestrant or to any other component of the drug;
  • expressed human liver;
  • Pregnancy and lactationPrecautions : in disorders of the kidneys and liverDosage and administration by intramuscular injection, by slow injection. Adult female patients (including old age). The recommended dose -. 250 mg 1 time per month . Children and adolescents Safety Data and effectiveness in children and adolescents is not. Patients with impaired renal function . In cases of mild or moderate renal impairment (creatinine clearance> 30 ml / min) dose adjustment is required. Safety and efficacy in patients with severe renal impairment (creatinine clearance <30 mL / min) have not been established. Patients with impaired hepatic function Use of Fazlodeksa in patients with mild or moderate hepatic impairment requires caution. Safety and efficacy in patients with hepatic impairment have not been established.


    Side effects
    The observed adverse reactions are presented below. The definition of the frequency of adverse reactions: very common (> 10%); common (> 1 – ≤10%); rare (> 0.1 – ≤1%); the part of the digestive system:often – nausea, vomiting, diarrhea, anorexia, Cardio-vascular system: very often – heat sensation ( “hot flushes”); often – thromboembolism. Skin and skin appendages: often – a rash. Local reactions: often – transient pain, inflammatory reactions With the genitourinary system: often – urinary tract infection; rarely – vaginal bleeding, vaginal candidiasis. Other: often – headache, asthenia, back pain; rarely – galactorrhea, hypersensitivity reactions (edema, urticaria).


    Cases of overdose in humans is unknown. In animal studies, when administered at high doses of fulvestrant only observed effects are directly or indirectly associated with the antiestrogenic activity. In cases of overdose symptomatic therapy is recommended.

    Interaction with other drugs and other forms of interaction .
    The study of clinical interaction with midazolam fulvestrant does not inhibit the activity . In vitro data suggest that fulvestrant does not affect the activity of testosterone enanthate. The ability to suppress the activity  has not been evaluated.
    The study of clinical interaction with rifampicin and ketoconazole  is not revealed clinically significant changes in fulvestrant clearance. Therefore, the appointment of fulvestrant in combination with inducers or inhibitors  adjustment is required.

    Fazlodeksom Treatment should only be carried out under the supervision of a physician who has experience with anticancer drugs.
    It is recommended to exercise caution when using Fazlodeksa patients with mild or moderate hepatic impairment. We recommend caution when using Fazlodeksa in patients with severe renal impairment (creatinine clearance <30 mL / min).
    Given the way the drug is recommended to be careful when using Fazlodeksa in patients with a tendency to bleeding, thrombocytopenia or patients taking anticoagulants.
    Thromboembolism breast observed frequently in patients with advanced cancer of women. It must be taken into account when appointing Fazlodeksa patients at risk of thromboembolic events.
    Long-term use effects of fulvestrant on bone are not established.
    Given the mechanism of action of fulvestrant, we can not exclude the potential risk of osteoporosis.
    Fazlodeks should not be mixed with other drugs.
    The effect of Fazlodeksa on ability to drive and other mechanisms slightly. Patients with symptoms of fatigue must be careful when driving or other mechanisms.

    For instructions on handling and use
    of the syringe Remove the glass body of the blisters and inspected for damage.
    Breaking the outer packaging of the safety needle (SafetyGlide). Remove the needle case strictly according to its direction to prevent damage to the needle tip. Touch the needle during use can not be.
    Break jumper white plastic syringe tip cap and remove the cap from the tip attached rubber plug (see. Figure 1). Rotational motion to secure the needle tip of the syringe. Remove the holder from the needle.Visually assess the state of a solution for parenteral administration for the absence of particles and discoloration before use.
    Remove the extra gas bubbles from the syringe (small bubbles may remain). Slowly introduce the solution into the gluteal muscle.
    After removing the needle from the gluteal muscles immediately activate the safety needle device, pushing the lever to transfer it to the forward position as long as the tip of the needle is not fully closed (see. Figure 2). For the convenience of the plane “skew” the tip of the needle is aligned with the lever of the safety device, as shown in Figure 3. When the activation of the protective mechanism may be minimal splatter of fluid that may remain on the needle after injection. Visually testosterone enanthate confirm that the lever is moved to the extreme position and the needle tip is fully closed. If you are unable to activate the safety device needle, immediately place the needle into the standard container for needles.
    For maximum safety, use a one-handed manipulation and follow at a distance from himself and others.


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