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Bortezomib information from DrugsUpdate  

See Available Brands of Bortezomib in India

P - Contraindicated in Pregnancy
L - Contraindicated in Lactation

Bortezomib is the first therapeutic proteasome inhibitor to be tested in humans. It is approved in the U.S. for treating relapsed multiple myeloma and mantle cell lymphoma. 

Pharmacodynamics

Bortezomib is a reversible inhibitor of the chymotrypsin-like activity of the 26-S proteasome. It prevents targeted proteolysis that affects multiple signaling cascades responsible for normal homeostatic functions within the cell, leading to cell death.

Pharmacokinetics

Distribution: Protein binding: >80%.


Metabolism: Mainly metabolised via the cytochrome P450 isoenzymes CYP3A4, CYP2C19 and CYP1A2.

Bortezomib Indications / Bortezomib Uses

In Multiple myeloma.

Bortezomib Adverse Reactions / Bortezomib Side Effects

Asthenic conditions; pyrexia; GI disturbances, anorexia; dehydration; peripheral neuropathy; thrombocytopenia, neutropenia, anaemia; hypotension; cardiac disorders; bone and body pain; cough, dyspnoea; rash, oedema; hypersensitivity reactions; painful or difficult urination.


Potentially Fatal: Pneumonia, pyrexia, diarrhoea, vomiting, dehydration and nausea.

Precautions

Information Not Available

Special Precautions

Hepatic or renal impairment; history of syncope, orthostatic hypotension; dehydration. Impairs ability to drive or operate machinery. Monitor for symptoms of peripheral neuropathy. Monitor closely the blood glucose levels in patients receiving oral antidiabetic agents.

Other Drug Interactions

Concurrent use of amiodarone, antivirals, isoniazid, nitrofurantoin, statins may increase the chance of peripheral neuropathy. Concurrent use of antihypertensives increases the chance of hypotension.

Other Interactions

Information Not Available

Dosage

Intravenous


Multiple myeloma


Adult: Patients without symptoms or with Grade 1 peripheral neuropathy symptoms: 1.3 mg/m2 as IV bolus over 3-5 sec on days 1, 4, 8 and 11 of a 21-day cycle, followed by a 10-day rest period (days 12-21). At least 72 hr should elapse between consecutive doses.


Special Populations: Onset of any Grade 3 non-haematological or Grade 4 haematological toxicities excluding neuropathy: Withhold therapy until toxicities symptoms resolved, then reinitiate at 25% reduced dose. Grade 1 with pain or Grade 2 peripheral neuropathy symptoms: 1 mg/m2 2x wkly for 2 wk (days 1, 4, 8, 11), then a 10-day rest period (days 12-21). At least 72 hrs elapse between consecutive dose. Grade 2 with pain or Grade 3 peripheral neuropathy symptoms: Withhold therapy until toxicity resolves, then reduce dose to 0.7 mg/m2 weekly. Grade 4 peripheral neuropathy symptoms: Discontinue.


Overdosage: Symptoms include hypotension and thrombocytopenia. Monitor vital signs and admin appropriate supportive care.

Food(before/after)

Information Not Available

List of Contraindications

Bortezomib and Pregnancy

Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).

Bortezomib and Lactation

Contraindicated in Lactation

Bortezomib and Children

Information Not Available

Bortezomib and Geriatic

Information Not Available

Bortezomib and Other Contraindications

Hypersensitivity. Child. Pregnancy and lactation

Storage

Information Not Available

Lab interference

Information Not Available

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