What Are Oxaliplatin Side Effects?

The chemical name of this product is: trans-l-1,2-cyclohexanediamine oxalate platinum, and its structural formula is:

Oxaliplatin injection is indicated for patients with metastatic colorectal cancer who have failed fluorouracil therapy and can be used alone or in combination with fluorouracil.

Drug Name

Oxaliplatin injection

Drug type

Prescription drugs, medicines for medical workers' injuries

Use classification

Cytotoxic drugs

Oxaliplatin injection ingredients

The chemical name of this product is: trans-l-1,2-cyclohexanediamine oxalate platinum, and its structural formula is:

Molecular formula: C ₈ H ₁₄ N ₂ O ₄ Pt
Molecular weight: 397.30

Characteristics of Oxaliplatin Injection

This product is a colorless or almost colorless clear liquid.

Indications of oxaliplatin injection

Can be used alone or in combination with fluorouracil in patients with metastatic colorectal cancer who have failed fluorouracil therapy.

Oxaliplatin injection specifications

20ml: 40mg.

Oxaliplatin injection dosage

When used alone or in combination, the recommended dose is 130 mg / m [sup] 2 [/ sup] once per body surface area, added to 250 ~ 500ml 5% glucose solution for 2-6 hours. When no major toxicity occurs, the drug is administered every 3 weeks (21 days). Adjusting the dose is based on safety, especially neurological safety.

Adverse reactions of oxaliplatin injection

1. Hematopoietic system: This product has a certain blood toxicity. When used alone, it can cause the following adverse reactions: anemia, leukopenia, granulocytopenia, thrombocytopenia, sometimes grade 3 or 4. When combined with 5-fluorouracil, hematological toxicity such as neutropenia and thrombocytopenia increases;
2. Digestive system: This product alone can cause nausea, vomiting and diarrhea. These symptoms are sometimes severe. These side effects are significantly increased when used in combination with 5-fluorouracil. Prophylactic and / or therapeutic antiemetics are recommended;
3. Nervous system: Peripheral sensory neuropathy characterized by peripheral neuritis. Sometimes accompanied by spasms and sensory disturbances around the mouth, upper respiratory tract and upper digestive tract. Even similar to the clinical manifestations of laryngospasm without anatomical basis. Can recover on its own without sequelae. These symptoms are often triggered or exacerbated by a cold. Paresthesia can be relieved during treatment breaks, but when the cumulative dose is greater than 800 mg / m [sup] 2 [/ sup] (6 cycles), it may cause permanent paresthesia and dysfunction. Within months of treatment termination, neurotoxicity can be reduced or eliminated in more than three-quarters of patients. When reversible paresthesia occurs, there is no need to adjust the next dose of this product. The dose adjustment should be based on the duration and severity of the observed neurological symptoms. When paresthesia persists between the two courses, and painful paresthesia and / or dysfunction begin to appear, the dose of this product should be reduced by 25% (or 100mg / m [sup] 2 [/ sup]). Symptoms persist or worsen after dose adjustment and treatment should be discontinued. After the symptoms have completely or partially disappeared, it is still possible to use them in full or in reduced amounts, and a decision should be made based on the judgment of the physician.

Oxaliplatin injection contraindications

1. Those who are allergic to platinum derivatives are prohibited;
2. Banned during pregnancy and lactation.

Precautions for oxaliplatin injection

1. This product should be used under the supervision of a physician with experience in anti-cancer chemotherapy. Especially when combined with drugs with potential neurotoxicity, their neurological safety should be closely monitored;
2. Due to the toxicity of this product in the digestive system, such as nausea and vomiting, prophylactic or therapeutic antiemetic drugs should be given;
3. When hematological toxicity occurs (leukocytes <2000 / mm [sup] 3 [/ sup] or platelets <50000 / mm [sup] 3 [/ sup]>), the next cycle of medication should be postponed until recovery;
4. Hematological counting and classification should be performed before each treatment, and neurological examination should also be performed, and it should be performed regularly afterwards.
5. When patients have painful paresthesia or / and dysfunction between two courses, the dosage of this product should be reduced by 25%. If symptoms persist or worsen after dose adjustment, the drug should be discontinued.
6. Do not use aluminum-containing needles or injection equipment when preparing and infusion of this product.
7. Low temperature can cause laryngospasm when using this product, so do not use cold food or gargle with ice water.

Oxaliplatin injection for pregnant and lactating women

May be toxic to fetus. This product is banned during pregnancy. Studies through milk excretion have not been conducted and are contraindicated during lactation.

Oxaliplatin injection for children

There is no sufficient data on the safety of medications for children.

Oxaliplatin injection drug interactions

Due to incompatibility with sodium chloride and alkaline solutions (especially 5-fluorouracil), this product should not be mixed with the above preparations or administered simultaneously through the same vein. In vitro studies have shown that in the presence of compounds such as erythromycin, salicylate, paclitaxel and sodium valproate, the protein binding of this product has not changed significantly. In vivo studies in animals and humans have shown synergistic effects when combined with 5-fluorouracil.
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Oxaliplatin injection overdose

No antidote is available. When overdose, the adverse reactions will be exacerbated, hematological monitoring should be carried out, and symptomatic treatment for their toxic reactions should be performed.

Oxaliplatin injection pharmacology and toxicology

This product shows general toxicity of platinum compounds and species-specific cardiotoxicity. This product does not show renal toxicity of cisplatin, nor bone marrow toxicity of carboplatin. This product is a new platinum derivative. This product acts on DNA by generating alkylated conjugates to form intra-chain and inter-chain cross-links, thereby inhibiting DNA synthesis and replication. This product binds quickly to DNA, which takes up to 15 minutes. The combination of cisplatin and DNA is divided into two phases, including a delayed phase after 48 hours. One hour after administration in humans, the presence of leukocytes can be shown by measuring their adduct. DNA synthesis during replication, subsequent isolation of DNA, and synthesis of RNA and cellular proteins are inhibited. This treatment is effective for certain cell lines that are resistant to cisplatin.

Pharmacokinetics of Oxaliplatin Injection

Continuous instillation at a dose of 130 mg / m [sup] 2 [/ sup] for 2 hours, the total plasma platinum reached a peak of 5.1 ± 0.8 mg / ml / h, and the area under the simulated curve was 189 ± 45 mg / ml / h. When the infusion is complete, 50% of the platinum binds to the red blood cells, while the other 50% is present in the plasma. 25% of plasma platinum is free, and 75% of plasma platinum is bound to proteins. The protein-bound platinum gradually increased and stabilized at a level of 95% after the fifth day of administration. The elimination of the drug is divided into two phases, and the elimination phase half-life is about 40 hours. Up to 50% of the drug is excreted in the urine within 48 hours of administration (55% of the drug is cleared after 6 days). Fecal doses are limited (only 5% are excreted in the feces after 11 days of administration). In patients with renal failure, only the elimination of filterable platinum is not accompanied by an increase in toxicity, so there is no need to adjust the dosage.

The clearance of platinum bound to red blood cells is slow. On day 22 after dosing, the level of erythrocyte-bound platinum was 56% of the peak plasma level, and by this time most of the total plasma platinum had been cleared. In the subsequent dosing cycles, the total or non-centrifuged plasma platinum level did not increase significantly; and the red blood cells bound platinum showed a significant early accumulation phenomenon.

Oxaliplatin injection storage

Shaded and sealed.

Oxaliplatin injection packaging

One vial in ampoules.

Validity of Oxaliplatin Injection

Tentatively set for two years.