Bortezomib information from DrugsUpdate
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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