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Methylergonovine powder is a compound that is an alkylation product of LSA (Lysergic acid amide) derivative. Is a solid substance that usually occurs as a powder or crystals. It can be white, yellowish or brownish in color and has a certain smell. Poor solubility in water, difficult to dissolve completely. In acidic or alkaline solutions, it has poor stability and is easy to decompose, and has high solubility in ethanol and methanol. It is a drug with a structure similar to lysergic acid and is mainly used to treat gynecological diseases such as mastitis, uterine cramping and bleeding. Because of its remarkable therapeutic effect, it has been widely used in medical practice.
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Chemical Formula |
C20H25N3O2 |
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Exact Mass |
339 |
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Molecular Weight |
339 |
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m/z |
339 (100.0%), 340 (21.6%), 341 (2.2%), 340 (1.1%) |
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Elemental Analysis |
C, 70.77; H, 7.42; N, 12.38; O, 9.43 |
Methylergonovine powder is a derivative of ergot alkaloids with unique pharmacological effects. Its core use revolves around uterine contraction function, and it also involves anti-tumor adjuvant therapy, intervention in neurological diseases, and special medical applications.
Obstetrics and Gynecology: Core Regulation of Uterine Contraction Function
The application in obstetrics and gynecology is based on strong uterine contraction, which directly activates serotonin receptors and alpha adrenergic receptors on uterine smooth muscle cells, causing an increase in intracellular calcium ion concentration while inhibiting phosphodiesterase activity to enhance contractile protein sensitivity. Its strength of action is about 10-20 times that of oxytocin, with a duration of 3-6 hours, and its contraction effect on the cervix is more significant.
Prevention and treatment of postpartum hemorrhage
Postpartum bleeding is a serious complication during childbirth, which reduces the risk of bleeding by promoting uterine contractions. The conventional administration regimen is intramuscular injection of 0.2mg, with repeated administration every 2-4 hours if necessary, and a total dose not exceeding 1mg within 24 hours. In severe bleeding, intravenous injection can be used, but blood pressure changes need to be closely monitored. During cesarean section, 0.2mg of medication can be directly injected into the uterine muscle layer to achieve strong local contractions.
Intervention for incomplete uterine involution
After childbirth, the uterus needs to be restored to its pre pregnancy state through contraction. Poor restoration may lead to sustained bleeding or infection. Oral administration of 0.2-0.4mg, 3-4 times a day, with a course of treatment generally not exceeding 7 days, can significantly improve the process of uterine involution.
Control of uterine bleeding after miscarriage
After natural or induced abortion, weak uterine contractions may cause bleeding, which can be accelerated by enhancing uterine contractions to stop bleeding. After intramuscular injection of 0.2mg, the drug takes effect within 2-5 minutes and lasts for about 3 hours, providing an effective means for managing bleeding after abortion.
Regulation of excessive menstruation
For menstrual bleeding caused by functional uterine bleeding, abnormal bleeding can be reduced by regulating endometrial contractions and mucus dissolution. Clinically, it is necessary to strictly follow medical advice to control the dosage and avoid excessive contractions that may cause pain.
The potential value of adjuvant therapy in the field of anti-tumor treatment
The anti-tumor effect of ergometrine is derived from its weak male hormone activity and regulation of specific signaling pathways. Currently, it is mainly used as an adjuvant therapy for hormone dependent tumors and malignant lymphomas.
Adjuvant therapy for prostate cancer
The occurrence of prostate cancer is closely related to the level of androgen, which inhibits tumor cell proliferation by regulating the expression of androgen receptors. Clinically, it is often used in combination with other anti androgen drugs to enhance the therapeutic effect.
Intervention of breast cancer
Some breast cancer cells express androgen receptors, which can inhibit tumor growth by blocking androgen signaling pathways. Its combination with chemotherapy drugs can reduce the risk of recurrence and prolong survival.
Exploratory application of hepatocellular carcinoma
Early studies have shown that it has a growth inhibitory effect on hepatocellular carcinoma cell lines, and its mechanism may be related to inducing cell apoptosis or inhibiting angiogenesis. At present, it is still in the preclinical research stage and further validation of its effectiveness and safety is needed.
Adjuvant therapy for malignant lymphoma
The immunomodulatory effect may have a synergistic effect on the treatment of malignant lymphoma. Clinical observations have found that its combination with chemotherapy drugs can improve patient prognosis, but the specific mechanism still needs to be further explored.
The dual role of migraine and wakefulness in the field of nervous system
As a 5-HT receptor antagonist (pA2 value 9.6), methylergonovine powder has unique value in the treatment of neurological diseases, especially in the prevention of migraine and the promotion of coma awakening.
Preventive treatment of migraine
The onset of migraine is related to an imbalance of 5-HT neurotransmitters, which stabilizes 5-HT receptor activity and reduces the frequency of migraine attacks. Clinical studies have shown that long-term regular medication can reduce the incidence rate by more than 50%, but attention should be paid to the risk of drug dependence.
Awakening therapy after cerebrovascular accident
For comatose patients caused by traumatic brain injury or stroke, low-dose administration can stimulate the cerebral cortex and promote consciousness recovery after the condition stabilizes.
The mechanism may be related to enhancing dopaminergic nerve conduction, but the timing and dosage of medication need to be strictly controlled.
Improvement of Blurred State of Consciousness
Patients who are not awake during postoperative anesthesia, elderly dementia, or delirium can improve their clarity of consciousness by regulating neurotransmitter balance. Clinically, it is often used in combination with other awakening drugs to enhance therapeutic efficacy.
Exploration of Induced Abortion and Luteal Function Regulation in Special Medical Scenarios
Although its core use is focused on uterine contractions, its application in special medical scenarios is also worthy of attention, but strict adherence to contraindication management is necessary.
Cautious Application of Selective Induced Abortion
When there is no indication of cesarean section during full-term pregnancy, uterine contractions can be induced to initiate delivery. However, it may cause uterine rigidity contractions leading to fetal distress, so it should only be used with caution when other methods are ineffective, and fetal heart rate should be monitored throughout the entire process.
Regulation of luteal insufficiency
For infertility caused by insufficient luteal function, ergometrine can improve ovulation function by regulating the secretion of luteinizing hormone. Clinically, it is often used in combination with ovulation inducing drugs to improve the success rate of pregnancy, but organic lesions such as tubal obstruction need to be ruled out.
Intervention for Postpartum Placental Retention
Postpartum placental retention may cause massive bleeding, promoting placental abruption by enhancing uterine contractions. After intramuscular injection of 0.2mg, the drug quickly takes effect, providing an option for emergency treatment of placental retention.
Adjuvant therapy for bleeding related to coagulation disorders
For postpartum hemorrhage caused by coagulation dysfunction, mechanical uterine contractions can be used to reduce the amount of bleeding and buy time for coagulation factor replacement therapy. However, it should be noted that medication may mask the true extent of coagulation abnormalities, and a comprehensive assessment of medication risks is necessary.
synthesis method
Methylergonovine powder is a synthetic drug, a semi-synthetic derivative. It is a semi-synthetic plant ingredient, originally extracted from lysergic acid and now mainly prepared by chemical synthesis.
- Preparation of 8-bromo-1-methyl-6-methylergoline. 5-methyl-8-bromo-1H-indole-3-acetic acid and 1-methyl acetate were reacted for more than 4 hours, and the reaction solution was added to acetone. For the protection of the 6-position of the produced 6-bromo-8-methylergolin, where an acetyl group is added, a polystyrene resin having an affinity for acetone was used. After the reaction, the reactant was purified by adsorption-type silica gel column chromatography to obtain 8-bromo-1-methyl-6-methylergoline.
- Preparation of Methylergonovine. 8-Bromo-1-methyl-6-methylergoline was reacted with cyanobenzoate. Adding dibenzoyl chloride (DPC) to the reaction can form a cyanobenzoate intermediate. This intermediate is then hydrogenated (using aluminum trihydride) and esterified (using dipropyl malonate) to give Methylergonovine. Finally, Methylergonovine is purified by methods such as crystallization or column chromatography.
Chemical properties
Methylergonovine is more stable than ergotamine and can be stored at room temperature for a long time. It is not easily affected by air, water and light, and is not affected by slight acids or alkalis. The ultraviolet absorption spectrum of it has a certain absorption peak at 220nm, and the absorption intensity is the strongest at this time. Which can be hydrolyzed under alkaline conditions, and its product is ergoline. Under physiological conditions, the hydrolysis rate of Methylergonovine is relatively slow, so it has a longer duration of drug effect. And has a strong electron cloud and strong nucleophilicity, and can undergo nucleophilic addition reactions with other chemical substances. For example, it can undergo nucleophilic addition reactions with phenols to produce phenol-like products. There may be residual organic solvents in the preparation of Methylergonovine, such as ethanol, n-butanol, etc. These organic solvents may affect the quality of Methylergonovine powder, so proper purification and detection must be carried out.
FAQ
What is the drug methylergonovine used for?
Methylergonovine belongs to a class of drugs called ergot alkaloids. Methylergonovine is used to prevent or treat bleeding from the uterus that can happen after childbirth or an abortion.
What is the mechanism of action of methylergonovine in pregnancy?
Methergine (methylergonovine maleate) acts directly on the smooth muscle of the uterus and increases the tone, rate, and amplitude of rhythmic contractions. Thus, it induces a rapid and sustained tetanic uterotonic effect which shortens the third stage of labor and reduces blood loss.
Does methylergonovine raise blood pressure?
Increased Blood Pressure (Hypertension). Methylergonovine may increase your blood pressure or worsen it if you have a history of high blood pressure.
What should I avoid while taking methylergonovine?
Notes for Consumers: Taking grapefruit juice with Methylergonovine might increase the risk of chest pain, high blood pressure, nausea, palpitations, or other serious side effects, like pain, numbness or reduced circulation to the hands, feet or legs.
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