Composition : Bortezomib
Strength availability : 1mg vial
Form : injection
Pack : 1mg containing vial in a carton
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Bortezomib is a drug sold under the brand name of Velcade 1mg which belongs to anti-neoplastic medicine, which is available in the form of lyophilized powder.
Velcade 1mgis a prime benign proteasome inhibitor; proteasome is a biological structure that clefts the proteins
Pharmacological grouped as: anti-neoplastic agent or proteasome inhibitor
The drug is a prescription drug given under the supervision of pharmacist.
Velcade 1mg is majorly indicated for the treatment for patients suffering by following disease.
Mantle cell lymphoma.
Previously untreated multiple myeloma in the therapy:
Velcade dose 1.3mg/m2 should be given as 3 to 5 seconds via IV bolus or subcutaneous by interacting with tablet melphalan and prednisolone for nine 6 weeks treatment cycles
Velcade is taken for two times weekly, (day 1, 4, 8, 11, 22, 25, 29 and 32) for Cycles 1 over 4
Velcade is taken once a week (day 1, 8, 22, and 29) for Cycles 5 over 9
Duration of Velcade is 72 hours
In Relapse stage: Theusual dose of Velcade is 1.3mg/m2 should be given via IV bolus or subcutaneous as two times for two weeks (day1, 4, 8, and 11) followed by a ten-day rest course (day 12 through 21)
Schedule of Treatment increased 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)
Important points: Velcade administrated alone or combination with dexamethasone
therapy cycle requires of Three-week course
Mantle cell lymphoma:
The usual dose of Velcade for untreated mantle cell lymphoma is;
Velcade 1.3mg/m2 given as IV bolus given as two times weekly by concomitant with rituximab, cyclophosphamide, doxorubicin and tablet prednisolone for 2 weeks (day I, IV, VIII & XI) followed by rest period of 10 day (day II through 21).
In Relapse stage:
The regular dose of Velcade is 1.3mg/m2 administered as IV bolus or subcutaneous 2 times for two weeks (day I, IV, VIII & XI) followed by 10-day rest period (day II through 21)
The treatment followed for above 8 cycles may be taken for once weekly for 4 weeks (day 1, 8, 15 & 22), followed by rest of 13 day (days 23 through 35)
Lyophilized powder form is Velcade; which is reconstituted by using 0.9% normal saline (NS) NaCl.
Reconstituted the Velcade 1mg in 2ml of 0.9% NS
The route of administration is IV bolus
Intrathecal not use for administration.
The drug Velcade isa type of chymotrypsin like activity which is in form of unstable prohibitor of the 26S proteasome in human cells. The 26S proteasome is a group of protein that reduces the agglutinated proteins
The various proteins are weakening by proteasome enzymes that make difficult to tumor cells persistence like cyclins, tumor suppressors, BCL-2 & cyclin dependent kinase inhibitors
The functioning site of proteasome has :
Post glutamyl peptide hydrolysis activity
Prevention of these degenerations sensitizes cells to apoptosis and cell arrest and leads to cell lysis.
The Bortezomib peak plasma level occurs as 509ng/ml
The Bortezomibhas nearly 83% of human plasma protein binding.
Primarily metabolic pathway of Velcade 1mg is occurs by deboronation to form 2-deboronated metabolites which are inactive as 26S proteasome inhibitors.
In liver Velcade 1mg is metabolized with the help of cytochrome P 450 enzymes 3A4, 2C19, & 1A2 by oxidation
The half-life period of Velcade 1mg occurs at 9 to 15 hours In single dose IV;
While taking Velcade 1mg some adverse effects occurs care should be taken in the conditions like
Cardiac toxicity :
Pulmonary toxicity like Acute Respiratory Distress Syndrome, pneumonitis, interstitial pneumonia, lung infiltration.
Posterior reversible encephalopathy syndrome-stop the Velcade 1mg therapy
Velcade 1mg 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
Gastrointestinal toxicity-fluid or electrolyte replacements have to take
Thrombocytopenia and neutropenia
Tumor lysis syndrome
Embryo fetal toxicity.
Velcade 1mg vial should be stored at 20℃ to 25℃ (68℉ to 77℉ ); excursion between 15℃ to 30℃ (59℉ to 86℉ )
Keep away from light and heat
Velcade 1mg is not a normal medicine used as anti-cancer drug; it is not to be self-medicated
If a dose failed to take should consult with medical oncologist and followed the dosing schedules
Follow the advice given by physician and do not missed the cycles for course of therapy
Avoid interaction with st.Johns wort to decrease the exposure of Velcade 1mg
while concomitant with CYP3A4 inhibitors: there is a chance of getting Velcade 1mg toxicity; so, to reduce the dose of Velcade 1mg
Interaction with Strong CYP3A4 inducers: decrease the exposure of Velcade 1mg
while concomitant with melphalan-prednisone or dexamethasone alone No clinical effect on Velcade 1mg exposure.
Velcade 1mg is administer through IV bolus or subcutaneous; whereas intrathecal administration is contraindicated to the patients who are receiving Bortezomib
Hypersensitivity reaction occurs in patients who are contraindicated to Velcade 1mg, boron, boric acid or glycine.
Most common side effects occurred after administration of Velcade 1mg includes;
Burning, crawling, itching, numbness, prickling; Chest pain ; Black tarry stools; Bleeding gums ; Blood in urine ; Blurred vision ; Body aches, dizziness, faintness, nerve pain, painful urination, pale skin, runny nose, sore throat, stuffy nose, swollen glands, sunken eyes, ulcer, dry mouth, Cough producing mucus, ear congestion, loss of voice
Less common side effects:
Belching, bone pain, difficulty with moving & bowel movements, cold and shivering, loss of appetite, loss of taste, muscle cramps, muscle pain, stomach discomfort. Vomiting, loss of weight discomfort, increased sensitivity of pain & touch, irregular breathing, heart beats, swelling of peripheral organs, thickening of bronchial secretions.