Description: On February 3rd, 2006, the State Administration of Pharmaceutical Products issued the instructions for paclitaxel injection in the Notice on Printing and Distributing the Instructions for the First Batch of Chemicals (State Drug Administration Note [20065438+0] No.586). The instructions published by the State Administration of Pharmaceutical Products are reference samples for revising the specifications. In case of doubt, the enterprise may propose amendments. Indications should be consistent with the original approval; Adverse reactions, drug interactions and other contents, the instructions provided by the enterprise can not be less than those listed in the sample draft. For empty or incomplete items in the sample manual, enterprises should be required to fill in according to the actual situation, such as product name and specifications.
Drug name
Generic name: paclitaxel injection
Former name:
Commodity name:
English name: paclitaxel injection
Chinese Pinyin: Zi Shan Chunzhu Yeqing
The chemical name of this product is: 5β, 20 epoxy 1, 2α, 4, 7β, 10β, 13α hexahydroxytaxane1alkenyl ketone 4, 10 diacetate 2 benzoate/.
Its structural formula is:
Molecular formula: C47H5 1NO 14.
Molecular weight: 853.92
Character; Role; letter
This product is a colorless or yellowish clear viscous liquid.
Pharmacology and toxicology
This product is a new anti-microtubule drug, which can inhibit depolymerization, maintain the stability of microtubule protein and inhibit cell mitosis by promoting microtubule protein polymerization. In vitro experiments show that paclitaxel has a significant radiosensitization effect, which may be to stop the cells sensitive to radiotherapy in G2 and M phases.
pharmacokinetics
The plasma concentration of intravenous paclitaxel showed a biphasic curve. The protein binding rate of this product is 89% ~ 98%, and paclitaxel is metabolized in the liver. Taxol is mainly metabolized in the liver, enters the intestine with bile and is excreted through feces (>: 90%). The renal clearance rate only accounts for 1% ~ 8% of the total clearance rate, and the metabolism of paclitaxel in patients with renal insufficiency is still unknown.
indicate
First-line and second-line treatment of ovarian cancer, breast cancer and non-small cell lung cancer. Head and neck cancer, esophageal cancer, seminoma, recurrent non-Hodgkin lymphoma, etc.
dosage
In order to prevent allergic reaction, dexamethasone 10mg was taken orally/2 hours before paclitaxel treatment, and dexamethasone 10mg was taken orally 6 hours before treatment, diphenhydramine 20mg was injected intramuscularly 30 ~ 60 minutes before treatment, and cimetidine 300mg or ranitidine 50mg was injected intravenously. The dosage of single drug is 135 ~ 200mg/m2, and with the support of GCSF, the dosage can reach 250mg/m2. Dilute paclitaxel with normal saline or 5% glucose saline for 3 hours. The combined dosage was 135 ~ 175 mg/m2 for 3 ~ 4 weeks.
counteraction
1. Allergic reaction: the incidence was 39%, and the incidence of severe allergic reaction was 2%. Most of them are allergic reactions of type 1, characterized by bronchospasm, dyspnea, urticaria and hypotension. Almost all the reactions occurred in the first 10 minute after administration.
2. Bone marrow suppression: it is the main dose-limiting toxicity, which is characterized by neutropenia and rare thrombocytopenia, generally occurring 8 ~ 10 days after administration. The incidence of severe neutrophils was 47%, and the incidence of severe thrombocytopenia was 5%. Anemia is more common.
3. Neurotoxicity: The incidence of peripheral neuropathy is 62%, the most common manifestations are mild numbness and sensory abnormality, and the incidence of severe neurotoxicity is 6%.
4, cardiovascular toxicity: there may be hypotension and asymptomatic short-term bradycardia. Muscle and joint pain: the incidence rate is 55%, which occurs at the joints of limbs, and the incidence and severity are dose-dependent.
5. Gastrointestinal reactions: The incidence rates of nausea, vomiting, diarrhea and mucositis were 59%, 43% and 39% respectively, which were generally mild and moderate.
6. Hepatotoxicity: alanine aminotransferase, aspartate aminotransferase and AKP increased.
7. Hair loss: the incidence rate is 80%.
8. Local reaction: local inflammation of vein where drugs are injected and drug extravasation.
Contraindications
Allergic to polyoxyethylene castor oil. Neutrophils below 1500/mm are prohibited.
Matters needing attention
Dexamethasone, diphenhydramine and H2 receptor antagonist were used for pretreatment before treatment. Undiluted concentrated liquid medicine shall not contact PVC plastic instruments or equipment, and shall not be intravenously dripped. The diluted liquid medicine should be stored in bottles or plastic bags and dripped with PVC administration equipment. Attention should be paid to whether there are allergic reactions and changes in life characteristics during medication.
Medication for pregnant and lactating women
Paclitaxel has been proved to affect embryo growth in animal experiments, so it is forbidden for pregnant women. Women of childbearing age should not be pregnant during treatment.
drug interaction
Pharmacokinetic data showed that the clearance rate of cisplatin decreased by about 30%, and the bone marrow toxicity was more serious.
At the same time, ketoconazole affects the metabolism of this product.
excessive
There is no corresponding antidote. The main and predictable complications of overdose include bone marrow suppression, peripheral neurotoxicity and mucositis.
standard
5ml∶30mg
store
Keep away from light, sealed and stored below 25℃.
parcel
term of validity
Registration authentication number
Production enterprise
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