Bortezomib is sold under the brand name Bortecad which is a type of anti-cancer medicine, which is in the form of lyophilized powder A first beneficial proteasome inhibitor is known as Bortecad ; proteasome is a cellular structure which breaks the proteins.
Bortecad injection will helps to prevent from multiple myeloma in patients with or without before treatment history and mantle cell lymphoma.
Bortecad is indicated to treat the patients suffering from multiple myeloma. Mantle cell lymphoma Bortecad is indicated to treat the disease mantle cell lymphoma which the patients have received at least 1 prior therapy.
MECHANISM OF ACTION
Bortecad 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.
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.
human serum plasma concentration is >80%
Bortecad injection metabolized mainly through cytochrome P450 isoenzymes CYP3A4, CYP2C19 & CYP1A2.
The excretion pathways of Bortecad 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.
BORTECAD DOSAGE AND ADMINISTRATION
Bortecad 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 Bortecad. Bortecad (lyophilized powder form) is reconstituted by using 0.9% sodium chloride (NS) Bortecad 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 Bortecad recommended dose for untreated mantle cell lymphoma is;1.3mg/m2 of Bortecad 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 Bortecad 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)
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, Bortecad is administrated for two times weekly, (day 1, 4, 8, 11, 22, 25, 29 and 32) Cycles 5 over 9, Bortecad is administrated once a week (day 1, 8, 22, and 29)
Moderately, 72 hours should be passing between following doses of Bortecad
IN RELAPSE STAGE
The usual dose of Bortecad 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)
While taking Bortecad some adverse effects occurs care should be taken in the conditions like Bortecad 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 Bortecad therapy Gastrointestinal toxicity-fluid or electrolyte replacements have to take Thrombocytopenia and neutropenia Tumor lysis syndrome Hepatic toxicity Embryo fetal toxicity
BORTECAD 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
Interaction with Strong CYP3A4 inhibitors then there is a chance of getting Bortecad toxicity; so to reduce the dose of Bortecad while concomitant with CYP3A4 inhibitors Strong CYP3A4 inducers: decrease the exposure of Bortecad Do not use combination with st. Johns wort to lowers the exposure of Bortecad While concomitant with melphalan-prednisone or dexamethasone alone has no clinical effect on Bortecad exposure
Bortecad is not recommended in pregnancy condition, it causes harm to fetus Breast feeding is not recommended.
The drug excreted into human milk is unknown and effects in the new born baby are unknown
Hence use is contraindicated
Bortecad vial should be stored at 20°C to 25°C (68°F to 77°F) excursion between 15°C to 30°C (59°F to 86°F). Keep away from light and heat.
If a single dose missed then administer the dose as you remember, If it is near to next dose then skip the missed dose and follow the regular schedule. Do not take extra dose at a time. Consult with the doctor for further changes in dose.