BORTEZOMIB 1MG


Description


Velcade 1mg belongs to class of anti-cancer medicine, which is in the form of lyophilized powder
A first beneficial proteasome inhibitor is known as Velcade 1mg; proteasome is a cellular structure which breaks the proteins


Indication

Velcade 1mg is mainly indicated for the treatment of
Multiple myeloma
Mantle cell lymphoma






Dosage and administration


Velcade (lyophilized powder form) is reconstituted by using 0.9% sodium chloride (NS)
Velcade 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 Velcade recommended dose for untreated mantle cell lymphoma is;
1.3mg/m2 of Velcade administered as IV bolus given as two times weekly by combining with rituximab, cyclophosphamide, 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 usual dose of Velcade 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 treatment continued for above 8 cycles may be taken 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 should be administered as 3 to 5 seconds through IV bolus or subcutaneous by combining with tablet melphalan and prednisolone for nine 6 weeks therapy cycles
Cycles 1 over 4, Velcade is taken for two times weekly, (day 1, 4, 8, 11, 22, 25, 29 and 32)
Cycles 5 over 9, Velcade is taken once a week (day 1, 8, 22, and 29)
Key points:
Partially, 72 hours should be passing between following doses of Velcade
In Relapse stage:
The usual dose of Velcade is 1.3mg/m2 should be administered through 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)
Treatment schedule 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 should be used alone or combination with dexamethasone
Three-week course is considered as therapy cycle
A minimum 72 hours should slip away between constant doses of Velcade

Mechanism Of Action


Pharmacological category: anti-neoplastic agent or proteasome inhibitor
Velcade 1mg is a type of chymotrypsin like activity unpredictable inhibitor of the 26S proteasome in human cells. The 26S proteasome is a big protein multiplex which degraded the accompany proteins
The functioning site of proteasome has :
Chymotrypsin like
Trypsin like
Post glutamyl peptide hydrolysis activity
The 26S proteasome enzyme recede assorted proteins which demanding to tumor cells survival like cyclins, tumor suppressors, BCL-2 & cyclin dependent kinase inhibitors
Prevention of these degenerations sensitizes cells to apoptosis and cell arrest

ADME


Absorption:
Velcade has good absorption The Velcade has peak plasma level occurs as 509ng/ml
Distribution:
The Velcade has human plasma protein binding occurs as nearly 83%
Metabolism:
Hepatically Velcade 1mg is metabolized with the help of cytochrome P 450 enzymes 3A4, 2C19, & 1A2 by oxidation Major metabolic pathway: deboronation to form 2-deboronated metabolites which are inactive as 26S proteasome inhibitors.
Elimination:
The half-life period occurs at 9 to 15 hours for single dose IV dosing: 40 to 193 hours for Multiple 1mg/m2 dosing: 76 to 108 hours for Multiple 1.3mg/m2

Precautions


While taking Velcade 1mg some adverse effects occurs care should be taken in the conditions like
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
Cardiac toxicity
Pulmonary toxicity like Acute Respiratory Distress Syndrome, pneumonitis, interstitial pneumonia, lung infiltration
Posterior reversible encephalopathy syndrome-stop the Velcade 1mg therapy
Gastrointestinal toxicity-fluid or electrolyte replacements have to take
Thrombocytopenia and neutropenia
Tumor lysis syndrome
Hepatic toxicity
Embryo fetal toxicity

Drug Interaction


Strong CYP3A4 inhibitors: there is a chance of getting Velcade 1mg toxicity; so, to reduce the dose of Velcade 1mg while concomitant with CYP3A4 inhibitors
Strong CYP3A4 inducers: decrease the exposure of Velcade 1mg
Avoid concomitant with st. John’s wort to decrease the exposure of Velcade 1mg
No clinical effect on Velcade 1mg exposure while concomitant with melphalan-prednisone or dexamethasone alone

Side Effects


Most common side effects occurred after administration of Velcade includes;
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:
irregular breathing, Swelling of peripheral organs ,Dilated veins, discomfort, increased sensitivity of pain & touch, , heart beats, , thickening of bronchial secretions
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

Pregnancy & Lactation


Velcade 1mg is not recommended in pregnancy condition, it causes harm to fetus
Breast feeding is not recommended

Storage


Velcade 1mg vial should be stored at 20oC to 25oC (68oF to 77oF); excursion between 15oC to 30oC (59oF to 86oF) Keep away from light and heat



Missed Dose


Velcade 1mg is not a normal medicine used as anti-cancer drug; it is not to be self-medicated
Please consult with physician and do not missed the cycles for course of therapy


Missed Dose


If patient fail to take the dose of Velcade 1mg, must consult with medical oncologist and followed the dosing schedules
Do not self administered


Contraindication


Hypersensitivity reaction occurs in patients who are contraindicated to Velcade 1mg, boron, boric acid or glycine
Velcade 1mg is given through IV bolus or subcutaneous; whereas intrathecal administration is contraindicated to the patients who are receiving Velcade 1mg


Connect With Us

Prescription Medication Policy


1. Anti-Cancer-Drugs.com, a fully licensed and regulated pharmacy, takes all precautions to strictly abide by the laws and regulations set forth in the dispensing of prescription medications. By placing the order for your prescription medicines, you acknowledge and accept the following terms regarding the purchase of any prescription medicines.
2. Anti-Cancer-Drugs.com will not dispense any prescription medication without a valid prescription from a licensed physician.
3. If you are ordering prescription medication(s), you hereby confirm that you will send us a scanned copy of your valid prescription(s) via email, fax, Whatsapp, or by post, and this prescription shall then be subject to the scrutiny of and approval by our qualified Pharmacists.
4. The drug information provided in the Anti-Cancer-Drugs.com is for informative purposes only and this Website is not intended to provide diagnosis, treatment or medical advice. We are not liable for any adverse effects or harm to you as a result of your reliance on the information in the Website.
5. Anti-Cancer-Drugs.com requires either the User or Customer or the Caregiver to confirm he/she is completely aware of the indications, side effects, drug interactions, effects of missed dose or overdose of the medicines he/she orders from us. It is imperative to seek professional advice from your physician before purchasing or consuming any medicine from Anti-Cancer-Drugs.com
6. At Anti-Cancer-Drugs.com, a Caregiver can order prescription medicines on your behalf.