Mentholase for Injection for the treatment of a variety of acute leukemia Below is my compilation of Mentholase for Injection instructions, welcome to read.
Mentholase for Injection
General name: Mentholase for Injection
Manufacturer: Guangzhou Baiyunshan Mingxing Pharmaceutical Co.
Approval number: State Pharmaceutical License No. H19993914
Drug specifications: 10,000 units
Drug price: ￥ 187
Mentholase for Injection InstructionDrug Name
Common Name: Mendonuclease for Injection
English Name: Asparaginase for Injection
Chinese Pinyin: Zhusheyong Mendongxian?anmei
Main Ingredients The main ingredients of Mendonuclease for Injection are: Mendonuclease, Mendonuclease, Mendonuclease, Mendonuclease, Mendonuclease, Mendonuclease, Mendonuclease and Mendonuclease.
Characteristics Mendonuclease for injection is a white lyophilized mass.
Pharmacology and toxicology
Mentholase for Injection is an enzyme antitumor drug taken from Escherichia coli, which can hydrolyze serum Mentholatum to Mentholatum and Ammonia, which is an essential amino acid for cellular protein synthesis and proliferation.
Normal cells have the function of synthesizing asparagine on their own, while tumor cells such as acute leukemia cells do not have this function. Therefore, when injectable asparagine enzyme is used to make the asparagine shortage, the tumor cells can not get enough asparagine from the blood, and can not synthesize it on their own, so that their protein synthesis is impeded, and their proliferation is inhibited, and the cells are destroyed in large quantities, and they can't grow and survive.
Injectable mentholase can also interfere with cellular DNA and RNA synthesis, and may play a role in the cellular G1 proliferation cycle, inhibiting cell division in this phase of the cell cycle-specific drugs.
Pharmacokinetics
Mentholase for Injection is absorbed by the intramuscular or intravenous route, with a plasma protein binding rate of approximately 30%, and can be measured in the lymph fluid after absorption, but the concentration in the cerebrospinal fluid is very low. After injection of menthionase, the concentration of menthionine in the blood decreased almost immediately to a level that could not be measured, indicating that menthionase injection begins to act soon after entering the body.
Plasma t1/2 was 39 to 49 hours for intramuscular injection and 8 to 30 hours for sedation. Peak time after intramuscular injection is 12 to 24 hours, but 23 to 33 days after discontinuation of injectable menthylase, menthylase is still measurable in plasma, and excretion of injectable menthylase appears to be biphasic, with only trace amounts presented in the urine.
Indications
It is indicated for the treatment of acute lymphoblastic leukemia (referred to as acute), acute granulocytic leukemia, acute monocytic leukemia, chronic lymphocytic leukemia, Hodgkin's disease and non-Hodgkin's disease lymphomas, and melanoma.
Mentholase injection has an inhibitory effect on the proliferation of the above kinds of tumor cells, which has good efficacy in the induction of remission in children with acute gonorrhea, and sometimes may be effective in some patients with relapse after remission of commonly used chemotherapeutic drugs, but the remission period is shorter when applied alone, and it is easy to produce drug resistance, so it is often applied with other chemotherapeutic drugs to form a joint program to improve the therapeutic efficacy.
Dosage
Depending on the type of disease and the treatment plan, the dosage of Mentholase for Injection varies greatly.
Take the induced remission regimen for acute gonorrhea as an example: the dosage can be based on the body surface area, the daily dose of 500 units/m2, or 1000 units/m2, and as high as 2000 units/m2; with a course of treatment of 10 to 20 days.
Adverse effects
Seem to be more common in adults than in children.
(1) the more common are allergic reactions, liver damage, pancreatitis, loss of appetite, coagulation factors V, VII, VIII, IX and fibrinogen reduction, etc., the main manifestations of allergic reactions for the sudden onset of respiratory distress, arthralgia, skin rash, skin itching, facial edema, severe respiratory distress, shock and even death.
In advanced childhood leukemia with intramuscular administration, although the incidence of mild allergic reactions is higher, the incidence of severe allergic reactions has been reported to be lower than that of static administration. Allergic reactions are generally more likely to occur with multiple repeated injections, but have occurred in patients with negative intradermal sensitization tests (referred to as skin tests).
In other allergic individuals, anaphylactic reactions have occasionally occurred even when injecting skin-test doses of Mentholase.
Liver damage usually occurs within 2 weeks of the start of treatment, and a variety of hepatic abnormalities may occur, including elevated serum alanine aminotransferase [ALT (SGpT)], aminotransferase mentholatum [AST (SGOT)], and bilirubin, and lowered serum albumin. If the patient feels severe epigastric pain accompanied by nausea and vomiting, acute pancreatitis should be suspected, of which fulminant pancreatitis is very serious and may even be fatal. Other symptoms include nausea, vomiting and diarrhea.
(2) Rarely, there are elevated blood glucose, hyperuricemia, high fever, mental and neurotoxicity. Patients with hyperglycemia have symptoms of polyuria, polydipsia, and thirst, and their plasma osmolality may be elevated while their blood ketone content is normal. Hyperglycemia can be reduced or eliminated by discontinuing injectable mentholase, or by giving appropriate amounts of insulin and rehydration, but a few severe cases can be fatal.
Hyperuricemia often occurs at the beginning of treatment, due to the rapid destruction of a large number of tumor cells, resulting in the release of nucleic acid decomposition of uric acid increased, severe can cause uric acid nephropathy, renal failure.
Psychotoxicity and neurotoxicity are characterized by drowsiness, mental inhibition, confusion, agitation, hallucinations, and occasionally Parkinson's syndrome. Others include leukopenia, immunosuppression, stomatitis, and so on.
(3) Rarely, there are bleeding due to hypofibrinogenemia and coagulation factor reduction, hypolipidemia, intracranial hemorrhage or thrombosis, lower extremity venous thrombosis and bone marrow suppression. Decreased coagulation factors are associated with inhibition of protein synthesis by injectable menthase.
(4) Other: there are also high blood ammonia, alopecia, thrombocytopenia, anemia and so on.
We should pay attention to the emergence of adverse reactions, its nature should be carefully analyzed, where there is a possibility of causing serious consequences, should be immediately discontinued with the injection of Mentholase, and combined with the specific performance to give the appropriate therapeutic measures, and the critical need to be actively resuscitated.
Contraindications
The following conditions are contraindicated:
① history of hypersensitivity to injectable menthyl aminidase or a positive skin test;
② history of pancreatitis or currently suffering from pancreatitis;
③ currently suffering from severe infections such as chickenpox and widespread herpes zoster.
Precautions
(1) Occasional cross-sensitization between Mentholase derived from Escherichia coli and Mentholase derived from Erwinia carotora.
(2) Interference with diagnosis:
(1) Thyroid function test, within 2 days of the first injection of menthionase, the concentration of thyroid-binding protein in the serum of the patient decreased, and the concentration did not return to normal until 4 weeks after the subsequent injection of menthionase;
(2) Due to the decomposition of menthionase, the concentration of blood ammonia and urea nitrogen may increase;
(3) Blood ammonia and urea nitrogen concentration may increase;
(4) The concentration of blood glucose and urine nitrogen may increase. p>
③ Blood glucose, blood uric acid, and urinary uric acid may increase;
④ During the first 3 weeks of treatment, partial thromboplastin time, prothrombin time, and prothrombin time may be prolonged, and platelet counts may be increased;
⑤ Due to the inhibition of plasma protein synthesis by injectable menthyl aminotransferase, the concentrations of plasma fibrinogen, antithrombin, fibrinolytic enzyme, and serum albumin may be decreased;
The concentrations of plasma fibrinogen and fibrinolysis may be decreased. albumin concentrations may be reduced;
⑥ If there are liver function abnormalities suggestive of hepatotoxicity, signs of liver damage;
⑦ Serum calcium may be reduced.
(3) Use with caution in the following cases:
① Diabetes mellitus;
② History of gout or renal urate stones;
③ Hepatic insufficiency, infections, etc.;
④ Patients with previous cytotoxicity or radiation therapy.
(4) Follow-up of the following tests before and during the start of treatment: peripheral blood picture, plasma coagulation factors, blood glucose, serum amylase, blood uric acid, liver function, renal function, classification of bone marrow smears, serum calcium, and central nervous system function.
(5) Because injectable menthyl amidase can further inhibit the patient's immune mechanism and increase the proliferative capacity, toxicity, and adverse reactions of the inoculated virus, it is not advisable to receive live virus vaccination within 3 months of receiving injectable menthyl amidase treatment, and the oral polio vaccine schedule for close contacts of the patient should be delayed.
(6) instructions for the administration of drugs:
① The patient must be hospitalized, under the guidance of a doctor experienced in tumor chemotherapy, each injection must be prepared before the anti-allergic drugs (including epinephrine, antihistamines, intravenous steroids such as dexamethasone, and so on), and resuscitation equipment.
② the first time the use of injectable menthase or injectable menthase has been used but has been discontinued for a week or more, the injection of menthase before the skin test.
Skin test solution can be prepared in the following way: add 5 ml of sterilized water for injection or sodium chloride injection into the vial shaking, so that the vial of 10,000 units of menthyl aminidase dissolved, extracted 0.1 ml (each 1 ml containing 2000 units), injected into another vial containing 9.9 ml of diluent, to make the concentration of 1 ml containing 20 units of skin test solution.
Use 0.1 ml of skin test solution (about 2.0 units) to do the skin test, and observe for at least 1 hour, if there is erythema or windmill extremely skin test positive reaction. Patients must have a negative skin test in order to receive treatment with injectable mentholase.
③ Should be from the intravenous large amount of fluid supplementation, alkalinization of urine, oral allopurinol, in order to prevent the occurrence of hyperuricemia and uric acid nephropathy in patients with leukemia or lymphoma.
④ Because resistance develops quickly after the use of injectable mentholase, injectable mentholase should not be used as a maintenance regimen after remission in patients with acute gonorrhea and other conditions.
⑤ Mentholase for Injection can be administered by IV, IV, or intramuscular injection. It must be diluted with sterilized water for injection or sodium chloride injection, and the amount of vial dilution is 5 ml per 10,000 units.
When administered by static injection, menthylase for injection should be injected through the side tube of the sodium chloride or dextrose injection that is being infused, and the duration of the static injection should not be shorter than half an hour. For administration by sedation, Mentholase for Injection should be diluted with an isotonic solution such as sodium chloride or 5% dextrose injection first, and then added to sodium chloride or 5% dextrose injection for titration.
③ Intramuscular injection, first in the vial containing 10,000 units of injectable menthyl aminotransferase should be diluted by adding 2 ml of sodium chloride injection, and the amount of each intramuscular injection should not be more than 2 ml for each intramuscular injection site. regardless of whether it is injected through the vein or intramuscular injection, the diluted solution must be made into a clarified solution to be used, and it should be applied within 8 hours after dilution.
Medication for Pregnant and Nursing Women
Since the potential teratogenic, mutagenic and secondary carcinogenic effects of Mentholase for Injection cannot be ruled out, avoid its use in pregnant women within the third trimester of pregnancy. Breastfeeding should be discontinued in breastfeeding mothers receiving treatment during breastfeeding due to consideration of the risk to the infant from Mentholase for Injection.
Drug interactions
(1) Prednisone or corticotropin or vincristine, when used with salbutamol, can enhance the hyperglycemic effect of salbutamol and may increase the risk of neuropathy and erythropoiesis induced by salbutamol, but it has been reported that salbutamol appears to be less toxic if it is used after the previous drugs. However, it has been reported that if the drugs are used first, followed by the use of injectable asparaginase, the toxicity seems to be less than that of the first use of injectable asparaginase or the use of both drugs.
(2) As the injectable mentholase can increase the concentration of blood uric acid, so when used in combination with allopurinol or colchicine, sulfinpyrazone and other anti-gout medications, it is necessary to regulate the dosage of the above anti-gout medications in order to control hyperuricemia and gout. Generally, anti-gout medication is selected from allopurinol, because the drug can block or reverse the hyperuricemia caused by the enzyme meningococcal aminopeptidase.
(3) Diabetic patients with injectable mentholase and after treatment, must pay attention to adjust the dose of oral hypoglycemic drugs or insulin.
(4) When combined with azathioprine, nitrogen mustard phenylbutyrate, cyclophosphamide, cyclosporine, mercaptopurine, monoclonal antibody CD3, or radiation therapy, the efficacy of the treatment can be improved, and therefore a reduction in the dosage of chemotherapeutic agents, immunosuppressants, or radiation therapy should be considered.
(5) When used with methotrexate, injectable mentholase can block the antitumor effect of methotrexate by inhibiting cell replication. Some studies have shown that if Mentholase is applied before 9-10 days of methotrexate administration or within 24 hours after methotrexate administration, it can avoid inhibiting the antitumor effect of methotrexate and reduce the adverse effects of methotrexate on the gastrointestinal tract and blood system.
Specifications 10,000 units
Storage Shade, airtight, stored in a cold place
Approved by the National Drug Administration H19993914
Manufacturer Guangzhou Baiyunshan Mingxing Pharmaceutical Co.
The efficacy of Mentonuclease for injection and the role of injectable Mentonuclease in the treatment of a variety of acute leukemias
Injections Frequently Asked Questions on the Use of MentholaseQ: What are the contraindications for Mentholase for Injection?
A: the following conditions are prohibited:
① a history of allergy to injectable Mentamide enzyme or positive skin test;
② a history of pancreatitis or currently suffering from pancreatitis;