Product code: SK-00 1
Approval number: National Medicine Zhunzi H20030357
Product introduction:
Properties This product is a white or yellowish lump.
Pharmacology and toxicology
Pharmacological action:
This product is a cytotoxic antineoplastic drug, which can promote the assembly of microtubule dimer and prevent it from depolymerization. It can also lead to the abnormal arrangement of microtubules in the whole cell cycle and the formation of microtubule stellate during cell division, thus preventing cell division and inhibiting tumor growth.
Toxicological research:
Genotoxicity: In vitro (human lymphocyte chromosome aberration test) and in vivo (mouse micronucleus test) tests showed that paclitaxel was a mutagen, but it was not mutagenic in Ames test and CHO/HGPRT gene mutation test.
Reproductive toxicity: Taxol given to rats before and during mating at a dose of 65,438+0 mg/kg/day or above (about 0.04 times the maximum dose recommended by clinical day) can cause damage to the fertility of female and male rats. At this dose, this product can cause the fertility and reproductive index to decrease and the embryo toxicity to increase. Paclitaxel (3mg/kg/ day, converted by body surface area, about 0.2 times of the maximum dose recommended by clinical day) can cause intrauterine death, increase fetal and fetal toxicity, and also show maternal toxicity. When the dose was 1mg/kg/ day (converted from body surface area, it was about115 of the maximum recommended dose in clinical days), no teratogenic effect was observed. At higher doses, it is impossible to evaluate the teratogenic effect of this product because of a large number of fetal deaths. There is no sufficient and strictly controlled clinical research data of pregnant women. If patients use this product during pregnancy or become pregnant during the use of this product, they should be informed of the potential harm of this product to the fetus. Women of childbearing age who receive this product should avoid pregnancy.
It is not clear whether the product is excreted from breast milk. On the 9th-10 day after delivery, rats were injected with paclitaxel labeled with carbon-14 intravenously, which showed that the radiation concentration in milk was higher than that in plasma, and decreased in parallel with the plasma concentration. In view of the fact that many drugs can be excreted from breast milk, and this product may bring serious adverse reactions to nursing babies, it is recommended to stop breastfeeding when accepting this product.
pharmacokinetics
According to the literature, the drug in the plasma of tumor patients is biphasic elimination after infusion of paclitaxel, and the average elimination half-life is 5.3- 17.4 hours. 89%-98% of drugs bind to plasma protein, and plasma Cmax is related to dosage and infusion time, and only a small amount of original drugs are excreted through urine.
adapt to
This product can be used for the first-line chemotherapy of ovarian cancer and the treatment of metastatic ovarian cancer in the future. As a first-line chemotherapy, this product can also be used in combination with cisplatin.
The product can also be used for the follow-up treatment of breast cancer patients using standard chemotherapy containing adriamycin or for the treatment of recurrent patients.
This product can be used in combination with cisplatin for first-line chemotherapy in patients with non-small cell lung cancer who cannot be operated or irradiated.
dosage
The usual dosage is135-175mg/m2. Before use, add 10 ml of 5% glucose solution into the bottle, put it in a special oscillator for liposomes (oscillation frequency is 20Hz, amplitude: 7cm in X axis direction, 7cm in Y axis direction and 4cm in Z axis direction), and oscillate for 5 minutes. After complete dissolution, inject 25438+00 ml. In order to prevent the possible allergic reaction of paclitaxel, please carry out the following pretreatment 30 minutes before using this product: intravenous injection of dexamethasone 5-10 mg; Intramuscular injection of diphenhydramine 50mg；; Intravenous cimetidine 300 mg.
counteraction
1. allergic reaction: manifested as blushing, rash, dyspnea, hypotension and tachycardia. If there is a serious allergic reaction, the drug should be stopped. Allergic patients should not use this product again.
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 neutropenia is 47%, severe thrombocytopenia is 5%, and 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: Hypotension and short-term asymptomatic bradycardia, muscle and joint pain can occur, with an incidence rate of 55%, which is mainly in limbs and joints, 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.
taboo
1, paclitaxel drug allergy is prohibited.
2. Neutrophils below 1500 /mm3 are prohibited.
Matters needing attention
1. Peripheral blood picture and liver function should be checked regularly during medication.
2. This product can only be dissolved and diluted with 5% glucose injection, not with normal saline or other solutions to avoid liposome aggregation. This product is stable within 24 hours at room temperature (25℃) and indoor illumination after being dissolved in 5% glucose injection.
3, abnormal liver function with caution.
Medication for pregnant and lactating women
There is no systematic study on pregnant women. If it is used for pregnant women or the patient is pregnant during the use of this product, the patient should be informed of the potential danger immediately. If lactating women use this product, they must stop breastfeeding.
There is no relevant experiment and no reliable reference for drug use in the elderly.
drug interaction
Pharmacokinetic data showed that the clearance rate of cisplatin was reduced by about 30%. Bone marrow toxicity is 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.
Specification 30mg/bottle
Store in a closed place at 2-8℃ away from light.
The packaging is made of white cardboard boxes with a white background, with 8 boxes per box 1 bottle.