AZEL - 40mg


Description


Azel 40mg tablets are containing an active substance known as Enzalutamide, which has anti-tumor activity by exhibiting androgen receptor inhibitory activity. Azel 40mg is a non steroidal anti-androgen drug; by inhibiting the androgen synthesis and expels anti-neoplastic activity against prostate tumor. Azel 40mg is an oral tablet form, which is endorsed by FDA. Enzalutamide is related with a reducing rate of serum enzyme increased during treatment, be that as it may, have not been connected to instances of clinically clear liver damage with jaundice.


Clinical use


The major clinical indication of Azel 40mg is involved in the treatment of long lasting or metastatic castration resistant prostate cancer patients who are not responding with docetaxel therapy.



Dosage management


Generally Azel is available in the strength of 40mg; the usual dose of Enzalutamide is 160mg taken as once a day. Four Azel 40mg tablets should be taken as such at whole. Azel 40mg tablets should be administered with or without food Do not chew, open or crush the capsules.

Dose Alteration

If patient accomplished with toxicities with the grade of III, postpone the therapy using with Azel 40mg capsules until changed to grade II. Then continue with the same dose or dose will be reduced to 120mg or 80mg depending upon the condition of the patients.
In combination with strong CYP2C8 inhibitors, dosage altered as :
Azel 40mg capsules, CYP2C8 inhibitors combination should be avoided if possible. Co administration of Azel 40mg capsules with strong CYP2C8 inhibitors, the dose of Azel should be decreased to 80mg as a single dose. After discontinuation of strong CYP2C8 inhibitors, the dose of Azel 40mg capsules should be used as such before the co administration starts.

Pharmacokinetic


Absorption

The maximum plasma concentration time of Enzalutamide is reaches within 1 hour The Cmax value of Enzalutamide and its metabolite are 16.6ng/ml & 12.7ng/ml respectively The steady state value is achieved in day 28 of Azel therapy.

Distribution

After single dose, the apparent volume of distribution of Enzalutamide is 110L The human plasma protein bounds to Enzalutamide at 97 to 98% Nearly 95% of N-desmethyl Enzalutamide is bounds to human plasma protein.

Metabolism

Enzalutamide undergone hepatic metabolism, The two most important cytochrome isoenzymes like CYP2C8 & CYP3A4 are responsible for metabolism of Enzalutamide; whereas CYP2C8 is involved in the formation of active metabolite of Enzalutamide.

Elimination

The elimination of Enzalutamide is occurs by liver metabolism, whereas 71% excreted through urine; 14% in feces. The clearance value of Enzalutamide after a single dose intake is 0.56L/hr. The mean half life period of Enzalutamide is 5.8 days with approximately 2.8 to 10.2 days.


Mechanism of action


Androgen is a male hormone; testosterone is a one of the hormone secreted from androgen which is responsible for growth of the tumor cells present in the prostate glands. Azel 40 mg tablets are comprises of Enzalutamide which acts by inhibiting the binding of androgen into androgen receptor site. This inhibition leads to interfere with signal transduction of receptors and causes growth retardation. The active metabolite of Enzalutamide is N-desmethyl Enzalutamide which is similar to parent form. Azel exhibits anti-neoplastic effect by reducing the cell proliferation leads to cell death and reduce the tumor cell volume.


Drug interaction


A Azel 40mg capsule combines with strong CYP2C8 inducers or inhibitors; Co administration of Azel with strong CYP2C8 inhibitors causes elevation of Cmax and AUC (plasma concentration) of Enzalutamide, to avoid this problem during this concomitant reduce the dose of Azel to 80mg as a single dose. Co administration of Azel with CYP2C8 inducers causes variation in plasma exposure of Azel. Avoid this combination if required. Concurrent use of Azel tablet with CYP3A4 inhibitors, causes elevating the AUC of Enzalutamide. Concurrent use of Azel with strong CYP3A4 inducers causes decreasing the plasmaexposure of Azel. Avoid concurrent use of Azel with anti-convulsants, anti-mycobacterials, anti-virals, herbal product like st. Johns wort. Enzalutamide is considered as strong CYP3A4 inducer & moderate CYP2C9 & CYP2C19 inducers. Azel diminish the plasma exposure to Midazolam, Omeprazole, and warfarin. Concurrent use of Azel with drugs metabolized by CYP3A4 like cyclosporine, ergotamine, fentanyl, quinidine, sirolimus or Tacrolimus may leads to reduce their exposure. Avoid concomitant use of warfarin with Azel capsules.

Side effects


Peripheral edema, Back pain, Arthralgia, Musculoskeletal pain, Musculoskeletal stiffness, weakness, Diarrhea, Hot flush, Hypertension, Head ache, Dizziness, Mental impairment, Hypoesthesia, Respiratory tract infection, Insomnia, Anxiety, Hematuria, Pollakiuria, Fall associated injuries, Non pathogenic fractures, Pruritus, Dry skin, Epistaxis, Elevation of AST & ALT, Elevation of bilirubin, Sepsis, Hallucination.

Safety measures


The major adverse caused during the Azel capsules therapy is seizures. Due to avoid the severe problem , the Patient must be counsel with the risk of participating in any action where sudden loss of awareness could make genuine damage themselves or others

Pregnancy


The pregnancy category of Enzalutamide X, which means it, may cause fetal harm even to death. Azel 40mg should not be recommended in pregnancy conditions.

Lactation


Breast feeding should not be suggested.

Pediatric


The potency and effectiveness of Azel 40mg capsules should not be evaluated in pediatric patients. In renal & hepatic damaged patients, the dosage adjustment of Azel capsules should not be suggested.



Storage


Azel capsules should be stored at 20oC to 25oC. Kept the drug in dry and cool place. Protect from light.


Overdosage


In over dosage condition, seizure may expose largely in the patients who are suspected with over dose of Azel.


Contraindication


Azel is contraindicated in pregnancy condition, it may cause fetal damage.


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