Oxaliplatin


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intravenous
Metastatic colorectal cancer
Adult: Combination therapy w/ FU/FA: 85 mg/m2 every 2 wk, given via infusion over 2-6 hr for 12 cycles. Dose may be reduced to 65 mg/m2, according to tolerability.

Intravenous
Adjuvant therapy in stage III colon cancer
Adult: Combination therapy w/ fluorouracil (FU)/folinic acid (FA): 85 mg/m2 every 2 wk, given via infusion over 2-6 hr for 12 cycles. Dose may be reduced to 75 mg/m2, according to tolerability.
Suy thận
CrCl (mL/min) Dosage
<30 Contraindicated.
Hướng dẫn pha thuốc
Dilute the required dose w/ 250-500 mL of dextrose 5% in water, to provide a soln containing 0.2-0.7 mg/mL.
Tương kỵ
Incompatible w/ Cl-containing solutions. Alkaline agents or soln (e.g. 5-FU, trometamol) negatively affect the stability. Needles and IV admin sets containing Al can cause degradation of platinum compd.
Chống chỉ định
Hypersensitivity to oxaliplatin and other platinum agents. Myelosuppression, peripheral sensory neuropathy w/ functional impairment, congenital long QT prolongation. Severe renal impairment (CrCl <30 mL/min). Lactation. Concomitant use w/ live vaccines.
Thận trọng
Patient w/ history of or risk for QT prolongation, electrolyte disturbances. Pregnancy.
Tác dụng không mong muốn
Significant: QT prolongation, ventricular arrhythmias, hypersensitivity reactions (e.g. burning sensations, pruritus, erythema, rashes/urticaria, flushing, diaphoresis, diarrhoea, shortness of breath, chest pain, syncope, disorientation; rarely, bronchospasm, hypotension); hepatotoxicity (e.g. peliosis, nodular regenerative hyperplasia or sinusoidal alterations, perisinusoidal fibrosis, veno-occlusive lesions; rarely, hepatitis, hepatic failure, hepatic vascular disorder); peripheral sensory neuropathy; reversible posterior leukoencephalopathy syndrome; neurological toxicity (e.g. acute laryngopharyngeal dysaesthesia); pulmonary symptoms (e.g. non-productive cough, dyspnoea, crackles, radiological pulmonary infiltrates); extravasation; GI toxicity (e.g. nausea, vomiting, severe diarrhoea/emesis, ulcer); haematological toxicity (e.g. neutropenia, thrombocytopenia).
Nervous: Meningism, motor neuritis, depression, insomnia, fatigue, asthenia, rigors, dizziness, headache.
CV: DVT, haemorrhage, peripheral oedema, flushing, thromboembolism, HTN.
GI: Abdominal pain, constipation, anorexia, stomatitis, dyspepsia, flatulence, GERD, GI/rectal haemorrhage, dysgeusia, anorexia, mucositis, dysphagia.
Resp: Coughing, epistaxis, hiccups, pulmonary embolism, rhinitis, URTI.
Hepatic: Increased blood bilirubin, ALT/AST and alkaline phosphatase levels.
Genitourinary: Dysuria, abnormal micturition frequency, haematuria, increased creatinine.
Endocrine: Hyperglycaemia, wt gain/loss, increased blood lactate dehydrogenase.
Haematologic: Anaemia, leukopenia, lymphopenia.
Musculoskeletal: Arthralgia, back pain.
Ophthalmologic: Conjunctivitis, visual disturbance, abnormal lacrimation.
Dermatologic: Skin/nail disorder, alopecia, palmar-plantar erythrodysesthesia, exfoliation, hyperhidrosis.
Immunologic: Infection.
Others: Fever, hypocalcaemia, hypokalaemia, hypernatraemia, dehydration, inj site reactions (e.g. pain, redness, swelling and thrombosis).
Potentially Fatal: Anaphylaxis; bone marrow suppression (e.g. sepsis, neutropenic sepsis, septic shock); torsade de pointes; pulmonary fibrosis, interstitial lung disease; intestinal ischaemia, duodenal ulcer haemorrhage and perforation; haemolytic uraemic syndrome, disseminated intravascular coagulation; rhabdomyolysis.
Thông tin tư vấn bệnh nhân
This drug may cause dizziness, nausea, vomiting, vision abnormalities and other neurological symptoms that affect gait and balance, if affected, do not drive or operate machinery.
Chỉ số theo dõi
Monitor CBC w/ differential, ALT/AST, bilirubin, creatinine, electrolyte, K, Mg levels. Monitor neurological status, QT interval, hypersensitivity, resp effects and toxicity.
Quá liều
Symptoms: Hypersensitivity reaction, myelosuppression, anaemia, neurotoxicity, grade 4 thrombocytopenia, sensory neuropathy (e.g. paraesthesia, dysaesthesia, laryngospasm and facial muscle spasms), GI disorders (e.g. nausea, vomiting, stomatitis, flatulence, enlarged abdomen, grade 4 intestinal obstruction), grade 4 dehydration, dyspnoea, wheezing, chest pain, resp failure, severe bradycardia. Management: Supportive treatment.
Tương tác
May enhance adverse effect of live vaccines.
Potentially Fatal: May diminish the therapeutic effect of vaccines. Increased risk of torsade de pointes w/ QT interval prolonging drugs.
Tác dụng
Description:
Mechanism of Action: Oxaliplatin is a platinum-containing antineoplastic drug which forms several transient reactive complexes including monoaquo and diaquo diaminocyclohexane platinum. These complexes covalently bind to DNA base sequences to form inter and intra-strand cross-links thereby inhibiting replication, transcription and cell division leading to cell death.
Pharmacokinetics:
Distribution: Volume of distribution: 440 L. Plasma protein binding: >90%, mainly to albumin and γ globulin.
Metabolism: Undergoes rapid and extensive nonenzymatic metabolism into inactive and active metabolites.
Excretion: Mainly via urine (approx 54%); faeces (approx 2%). Terminal elimination half-life: 391 hr.
Đặc tính

Chemical Structure Image
Oxaliplatin

Source: National Center for Biotechnology Information. PubChem Database. Eloxatin (TN), CID=9887054, https://pubchem.ncbi.nlm.nih.gov/compound/Eloxatin-_TN (accessed on Jan. 22, 2020)

Bảo quản
Store between 20-25°C. Do not freeze. Protect from light. Reconstituted soln: Store between 2-8°C for up to 24 hr.
This is a cytotoxic drug. Follow applicable procedures for receiving, handling, admin, and disposal. Any unused portions should be disposed of in accordance w/ local requirements.
Phân loại MIMS
Hóa trị gây độc tế bào
Phân loại ATC
L01XA03 - oxaliplatin ; Belongs to the class of platinum-containing antineoplastic agents. Used in the treatment of cancer.
Tài liệu tham khảo
Anon. Oxaliplatin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 31/08/2017.

Buckingham R (ed). Oxaliplatin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 31/08/2017.

Joint Formulary Committee. Oxaliplatin. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 31/08/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Oxaliplatin. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 31/08/2017.

Oxaliplatin Injection (Sun Pharmaceutical Industries, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 31/08/2017.

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