Fine cisplatin powder is a platinum-containing anticancer drug. It is a brownish-yellow powder, slightly soluble in water and easily soluble in dimethylformamide. It can be gradually converted into a trans-form and hydrolyzed in an aqueous solution. Its density is 3.7.
Melting point: 270°C, water solubility: < 0.1 g/100 mL at 19°C, which belongs to cell cycle nonspecific drug, and has a therapeutic effect on sarcoma, malignant epithelial tumor, lymphoma, and germ cell tumor. It is the first synthetic platinum anticancer drug, with a simple structure and clear mechanism, and it has led to an upsurge of research on platinum drugs, including carboplatin, oxaliplatin, and nedaplatin.
The chemical structure of cisplatin is a simple plane square, with bivalent platinum as the center, two amino groups as ligands, and two chlorine groups as leaving groups. The activity of cisplatin mainly depends on the concentration of chloride ions. The physiological chloride ion concentration in blood or extracellular tissue fluid is about 100mmol/L, so its activity is low. When the concentration of chloride ions in cells decreases to several mmol/L, a large number of nucleophilic groups (such as oxygen, nitrogen, sulfhydryl, etc.) in cells can replace chloride ions in cisplatin to form new complexes, which can occur on the side chains of amino acids, the important components of purine bases of DNA and RNA, etc.
What is cisplatin?
Fine cisplatin powder is a heavy metal complex with bivalent platinum combined with two chlorine atoms and two ammonia molecules, which is similar to the bifunctional alkylating agent and can inhibit the DNA replication process. It is a cell cycle nonspecific drug with cytotoxicity, which can inhibit the DNA replication process of cancer cells and damage the structure of their cell membranes, and has a strong broad-spectrum anti-cancer effect.
Fine Cisplatin Powder is a chemotherapy drug that damages DNA, and it is used in the standard treatment of lung cancer, head and neck cancer, ovarian cancer, and testicular cancer. Its structure is very simple. After entering the body, platinum element crosses with two points or double strands in DNA single-strand, resulting in connection. Although it can treat many cancers, in some cases, cancer cells will also develop drug resistance.
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Real shot pictures of cisplatin raw powder | cisplatin structure diagram |
How does Cisplatin work?
Platinum anticancer drugs belong to cell cycle nonspecific drugs, which enter the body and act on cell DNA, including four processes:
① transmembrane movement into cells;
(2) dissociation reaction occurs in cells to generate hydrated coordination ions;
③ migrate to the target DNA;
④ Coordinate with DNA to form Pt-DNA adduct, which hinders the synthesis of DNA.
What are the adverse reactions of Cisplatin?
1. Nephrotoxicity: After a single medium and large dose of medication, slight and reversible renal dysfunction may occasionally occur, which may lead to microhematuria. Repeated administration of high doses and the short term will lead to irreversible renal dysfunction. In severe cases, renal tubular necrosis will lead to anuria and uremia.
2. Digestive system: including nausea, vomiting, loss of appetite, diarrhea, etc. The reaction often occurs within 1 ~ 6 hours after administration, and the longest time is no more than 24 ~ 48 hours. Occasionally, liver dysfunction and an increase in serum transaminase can be recovered after drug withdrawal.
3. Hematopoietic system: It is characterized by the decrease of white blood cells and (or) platelets, which is generally related to the dosage of drugs. Bone marrow suppression generally reaches its peak in about 3 weeks, and it recovers in 4 ~ 6 weeks.
4. Otototoxicity: Tinnitus and high-frequency hearing loss may occur, which are mostly reversible and do not require special treatment.
5. Neurotoxicity: It is more common in patients whose total amount exceeds 300mg/m2, and peripheral nerve injuries are more common, which are manifested as dyskinesia, myalgia, paresthesia of upper and lower limbs, etc. A few patients may have brain dysfunction, epilepsy, and retrobulbar optic neuritis.
6. Allergic reactions: such as increased heart rate, decreased blood pressure, dyspnea, facial edema, allergic fever, etc., may occur.
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