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MYEZOM 2mg mechanism of action


Myezom 2mg injection used in mammalian cells is a reversible inhibitor of the chymotrypsin-like activity of the 26-S proteasome. The drug prohibits targeted proteolysis that affects multiple signaling cascades responsible for normal homeostatic functions within the cell, leading to cell death.

PHARMACOKINETIC

Absorption

The peak plasma concentration after 1st dose is 57 and 112ng/mL, If administrated two times a week, Cmax observed for 1mg/m2dose is 67 to 106ng/mL, for 1.3mg/m2 is 89 to 720ng/mL.

Distribution

human serum plasma concentration is >80%

Metabolism

Myezom 2mg injection metabolized mainly through cytochrome P450 isoenzymes CYP3A4, CYP2C19 & CYP1A2.

Elimination

The excretion pathways of Myezom have not been characterized. The terminal elimination of half life after the 1mg/m2 dose is 40hrs - 193hrs, after dose 1.3mg/m2 is 76hrs - 108hrs.



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Brand : Myezom
Ingredients : Bortezomib
Strength : 2mg vial
Manufactured : Dr. Reddy’s Laboratory
Pack : 2mg Bortezomib containing vial in a carton

MYEZOM 2MG DOSAGE AND ADMINISTRATION

Myezom is administrated alone or combination with dexamethasone Three week course is considered as therapy cycle Atleast 72 hours must slip away between constant doses of Myezom Myezom (lyophilized powder form) is reconstituted by using 0.9% sodium chloride (NS) Myezom should be reconstituted in 3.5ml NS The route of administration is IV bolus Intrathecal not use for administration In adults:

Mantle cell lymphoma

The Myezom recommended dose for untreated mantle cell lymphoma is;1.3mg/m2 of Myezom administered as IV bolus given as two times weekly by combining with rituximab, cyclophospahmide, doxorubicin and tablet prednisolone for two weeks (day I, IV, VIII & XI) followed rest period of 10 days (day II through 21). In Relapse stage: The normal dose of Myezom is 1.3mg/m2 administered as IV bolus or subcutaneous two times for two weeks (day I, IV, VIII & XI) followed by 10 day rest period (day II through 21) The therapy should followed for above 8 cycles may be given for once weekly for 4 weeks (day 1, 8, 15 & 22), followed by 13 day rest (days 23 through 35)

Multiple myeloma

In the therapy of previously untreated multiple myeloma:1.3mg/m2 of dose must be given as 3 to 5 seconds through IV bolus or subcutaneous by concomitant use with tablet melphalan and prednisolone for nine 6 weeks therapy cycles Cycles 1 over 4, Myezom is administrated for two times weekly, (day 1, 4, 8, 11, 22, 25, 29 and 32) Cycles 5 over 9, Myezom is administrated once a week (day 1, 8, 22, and 29)

Key points

Moderately, 72 hours should be passing between following doses of Myezom 2mg

In Relapse stage

The usual dose of Myezom is 1.3mg/m2 should be administered through IV bolus or subcutaneous as two times for two weeks (day1, 4, 8, and 11) continued by a ten day of rest course (day 12 through 21) The schedule of the treatment has been raised above 8 cycles may be taken once weekly for 4 weeks (day 1, 8, 15, and 22), followed by 13 day rest (day 23 over 35)

MYEZOM 2MG SIDE EFFECTS

Most common side effects

Black tarry stools ; Bleeding gums ; Blood in urine ; Blurred vision ; Body aches ; Burning, crawling, itching, numbness, prickling ;Chest pain ; Cough producing mucus, dizziness, faintness, nerve pain, painful urination, pale skin, runny nose, sore throat, stuffy nose, swollen glands, sunken eyes, ulcer, dry mouth, ear congestion, loss of voice

Less common side effects

loss of appetite, Muscle cramps Belching, bone pain, difficulty with moving & bowel movements, cold and shivering, loss of taste, , muscle pain, stomach discomfort. Vomiting, loss of weight ; irregular breathing , Swelling of peripheral organs ,Dilated veins, discomfort, increased sensitivity of pain & touch, , heart beats, , thickening of bronchial secretions



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MYEZOM 2MG DRUG INTERACTION

Interaction with Strong CYP3A4 inhibitors then there is a chance of getting Myezom 2mg toxicity; so to reduce the dose of Myezom 2mg while concomitant with CYP3A4 inhibitors Strong CYP3A4 inducers: decrease the exposure of Myezom 2mg Do not use combination with st. Johns wort to lowers the exposure of Myezom 2mg While concomitant with melphalan-prednisone or dexamethasone alone has no clinical effect on Myezom 2mg exposure

PRECAUTION & WARNING

While taking Myezom 2mg some adverse effects occurs care should be taken in the conditions like Myezom 2mg leads to peripheral neuropathy like burning sensation, hyperesthesia, hypoesthesia, paresthesia, neuropathic pain Manage postural Hypotension by altering the antihypertensive agents, hydration, and administration of mineralocorticoids or sympathomimetics Cardiac toxicity Pulmonary toxicity like Acute Respiratory Distress Syndrome, pneumonitis, interstitial pneumonia, lung infiltration Posterior reversible encephalopathy syndrome-stop the Myezom 2mg therapy Gastrointestinal toxicity-fluid or electrolyte replacements have to take Thrombocytopenia and neutropenia Tumor lysis syndrome Hepatic toxicity Embryo fetal toxicity






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