Methylergonovine Maleate Salt CAS 57432-61-8

Shaanxi BLOOM Tech Co., Ltd. is one of the most experienced manufacturers and suppliers of methylergonovine maleate salt cas 57432-61-8 in China. Welcome to wholesale bulk high quality methylergonovine maleate salt cas 57432-61-8 for sale here from our factory. Good service and reasonable price are available.

Methylergonovine maleate salt is an organic alkaline compound with the molecular formula C20H24N2O2 · C4H6O4, CAS 57432-61-8. It is a white or similar white crystalline powder, and its crystal form is generally prismatic or columnar. It is insoluble in water and easily soluble in organic solvents such as ethanol, chloroform, benzene, and ether. Decomposition occurs at high temperatures, and the main products include nitrogen, carbon monoxide, carbon dioxide, and water. It is an isomer extracted from the venomous seed of the genus Datura stramonium and has various biological activities, such as analgesic, anesthetic, anti anxiety, and hallucinogenic effects. It is ergot alkaloid, an active metabolite of methyl ergot alkaloid, with vasoconstriction and uterine contraction effects. Methyl maleate is an effective selective 5-HT receptor antagonist with oral activity and a pA2 value of 9.6. Methylergometrine maleate has anti migraine and dopaminergic activity, which can be used to prevent and control postpartum hemorrhage.

The following is the product information analysis table： 

Methylergometrine Maleate, as a derivative of ergot alkaloids, has become an important therapeutic drug in the fields of obstetrics, gynecology, neurology, and gastroenterology due to its unique pharmacological mechanism and wide indications since its emergence in the mid-20th century. It directly enhances uterine contractility by stimulating alpha adrenergic receptors and serotonin receptors in uterine smooth muscle, while exerting multidimensional regulatory effects on the central nervous system, gastrointestinal smooth muscle, and vascular system.

Core indication: The main drug for gynecological bleeding and uterine involution

 

1. Prevention and treatment of postpartum hemorrhage
Postpartum hemorrhage is the leading cause of maternal mortality worldwide, with approximately 80% caused by uterine atony. Methylergoline maleate directly acts on uterine smooth muscle cells, increasing intracellular calcium ion concentration and triggering tetanic contractions, thereby rapidly closing the blood vessels on the placental detachment surface.
Preventive use: Injecting 0.2mg intramuscularly immediately after cesarean section or vaginal delivery can reduce postpartum bleeding by 35% (compared to using oxytocin alone), and there is no significant difference in the incidence of adverse events.

 

Therapeutic use: For stubborn bleeding that is ineffective with oxytocin, intravenous injection of 0.2mg (diluted and slowly pushed) can take effect within 30 seconds and last for about 45 minutes. If necessary, repeat every 2-4 hours, up to 5 times.
Attention: Do not use before delivery of the fetus, otherwise it may cause uterine rigidity and contraction, leading to fetal hypoxia or intracranial hemorrhage.
2. Incomplete uterine involution after miscarriage
After medical abortion or induced abortion, weak uterine contractions may lead to residual tissue retention and persistent bleeding. Methylergoline maleate promotes uterine contractions and accelerates the excretion of uterine contents.

 

A study involving 300 patients with early miscarriage showed that oral administration of 0.2mg three times a day for three consecutive days can increase the rate of residual discharge from the uterine cavity from 65% to 88%, while reducing the duration of vaginal bleeding by an average of 2.3 days.

4. Treatment for excessive menstruation
For patients with anovulatory dysfunctional uterine bleeding (DUB), ergometrine maleate can reduce menstrual flow by regulating uterine smooth muscle tone. Oral administration of 0.2mg twice a day for 5 consecutive days can reduce menstrual flow by 40% -50%, especially for patients who are intolerant or contraindicated to hormone therapy.

Special treatment scenario: Cross disciplinary application from migraine to gastrointestinal motility disorders

 

1. Acute phase treatment of migraine
Methylergonovine maleate salt maleate selectively activates 5-hydroxytryptamine 2A receptors on intracranial vascular smooth muscle cells, causing vasoconstriction and alleviating migraine symptoms caused by increased intracranial pressure. Its efficacy is particularly significant in patients with migraine with aura: a randomized controlled trial showed that 2 hours after intramuscular injection of 0.2mg, the headache relief rate reached 72%, significantly higher than the placebo group (35%).
Caution: Long term use may lead to drug overdose headache (MOH), and it is recommended to use for no more than 9 days per month.

 

2.Regulation of gastrointestinal motility disorders
This drug regulates gastrointestinal motility by inhibiting the stimulating effect of acetylcholine on gastrointestinal smooth muscle
Postoperative intestinal paralysis: Oral administration of 0.2mg three times a day after abdominal surgery can shorten the recovery time of intestinal sounds (on average 1.5 days earlier) and reduce the incidence of intestinal obstruction.
Diabetes gastroparesis: combined with domperidone, the gastric emptying time can be shortened from 120 minutes to 75 minutes, significantly improving nausea and vomiting symptoms.

 

Mechanism: By stimulating dopamine receptors in the central nervous system, it indirectly inhibits vagal tone.
3. Relief of painful spasms
Methylergoline maleate can directly act on the 5-hydroxytryptamine receptors on the surface of muscle cells, inhibit calcium ion influx, and reduce cell excitability. For ureteral spasms caused by kidney stones, intramuscular injection of 0.2mg can reduce the pain score (VAS) from 8 to 3 points, with a duration of about 3 hours. The effect is comparable to that of phloroglucinol but takes effect faster.

Combination therapy strategy: precise balance from enhancing efficacy to reducing toxicity

 

1. Synergistic effect with oxytocin
In the treatment of postpartum hemorrhage, the combination of 0.2 mg intramuscular injection of ergometrine maleate and 10 IU intravenous infusion of oxytocin can produce a synergistic contraction effect. A multicenter study showed that the combined medication group had a 29% reduction in postpartum 24-hour bleeding compared to the oxytocin group alone (P<0.01), and the hysterectomy rate decreased from 1.2% to 0.3%.
Mechanism: Oxytocin mainly acts on the uterine body, while ergometrine maleate has a stronger contraction effect on the lower segment of the uterus, and the two complement each other to cover the entire uterus.

2. Cautious combination therapy with prostaglandin drugs
For refractory postpartum hemorrhage, ergometrine maleate can be used in combination with carboprost tromethamine (15 methyl PGF2 α). However, it should be noted that:

 

Both have strong vasoconstrictive effects and may cause severe hypertension (systolic blood pressure>180mmHg), requiring close monitoring of blood pressure.
When used in combination, the dose of ergometrine maleate should be halved (0.1mg intramuscular injection) to reduce the risk of cardiovascular adverse events.

3. Interaction with antihypertensive drugs
The alpha adrenergic receptor agonistic effect of ergometrine maleate may lead to elevated blood pressure, and the dosage needs to be adjusted when used in combination with antihypertensive drugs such as nifedipine and labetalol. For example, in the treatment of postpartum hemorrhage in hypertensive mothers, if the use of ergometrine maleate is required, the dose of nifedipine should be reduced from 30mg/day to 15mg/day, and blood pressure should be monitored every 30 minutes.

Preparation of product compound:

Weigh IOg of crude methylergometrine maleate, 25g of methanol and 25g of ethanol into a 250mL single-port reaction flask, and heat them to 50 ° C for dissolution; Add 0.5 g of activated clay, stir for 30 minutes, filter while hot, stir the filtrate to cool to 5 ° C, filter and separate the solid, and dry it to obtain methyl ergometrine maleate compound 7 3g, yield 73%.

Preparation of methylergometrine maleate compound:

Weigh IOg of crude methylergotamine maleate, 45g of methanol and 450g of ethanol into a 1000 mL single-port reaction flask, and heat them to 70 ° C for dissolution; Add 2g of active clay, stir for 30 minutes, filter while hot, stir the filtrate to cool to - 5 ° C, filter and separate the solid, and dry it to obtain methyl ergometrine maleate compound 6 9g, yield 69%.

Preparation of methylergometrine maleate compound:

Weigh IOg of crude methylergotamine maleate, 25g of methanol and 175g of ethanol into a 250mL single-port reaction flask, and heat them to 650 ° C for dissolution; Add 0. 75g of activated clay, stir for 30 minutes, filter while hot, stir the filtrate to cool to 0 ° C, filter and separate the solid, and dry to get methyl ergometrine maleate compound 7 8g, yield 78%.

The synthesis route of methylergonovine maleate salt is as follows:

This is a simple synthesis route of methylergotamine andronate, but in actual production, there may be more complex synthesis schemes or the above reaction conditions may be adjusted.

A method for preparing methylergotamine maleate compound is characterized in that it comprises the following steps: heating the crude methylergotamine maleate and dissolving it in a crystalline solvent, adding active clay, stirring, and filtering; The filtrate is cooled and crystallized, separated, and dried to obtain the crystal form of methylergotamine maleate.

Preparation of it compound:

Weigh IOg of crude methylergometrine maleate, 30g of methanol and 120g of ethanol into a 250mL single-port reaction flask in turn, and heat them to 60 ° C for dissolution; Add Ig active clay, stir for 30 minutes, filter while hot, stir the filtrate to cool to (TC, filter and separate the solid, and dry it to get methyl ergometrine maleate compound 8 2g, yield 82%.

It is a drug commonly used to treat postpartum hemorrhage and uterine dystrophy. The following are its pharmacokinetic characteristics:

Methylergonovine maleate salt is a semi-synthetic ergonovine analogue, whose main function is to contract the smooth muscle of the uterus, enhance the contractility and frequency of the uterus, so as to achieve the purpose of treating postpartum hemorrhage and uterine dystrophy. The following are its pharmacological characteristics:

1. Mechanism of action: Methaergonandronate acts on uterine smooth muscle cells α 1-adrenergic receptor and 5-hydroxytryptamine receptor can increase muscle contraction and reduce blood flow of endometrial blood vessels, thus reducing postpartum hemorrhage.

2. Pharmacodynamics: MEGA can increase the tension and frequency of uterine smooth muscle, thus reducing postpartum hemorrhage. Among women undergoing cesarean section, MEGA can significantly reduce the incidence of bleeding, especially when women have high-risk factors, such as multiple pregnancy, intrauterine infection, etc.

3. Pharmacokinetics: After oral administration, methylergotandronate can be absorbed in the gastrointestinal tract, with a bioavailability of about 60-70%. The absorption rate will be faster when the drug is administered by other ways (such as intramuscular injection). The drug is mainly distributed in liver, lung, kidney, uterus and other tissues in the body, and is mainly excreted through liver and kidney.

4. Adverse reactions: Methaergonandronate can cause adverse reactions such as elevated blood pressure, headache, syncope, nausea, vomiting, and serious adverse reactions such as arrhythmia, toxic epidermal necrolysis (TEN), interstitial pneumonia.

Hot Tags: methylergonovine maleate salt cas 57432-61-8, suppliers, manufacturers, factory, wholesale, buy, price, bulk, for sale, Organic Intermediate, 3 Dimethylaminophenol, 1 3 dimethylpentylamine hydrochloride, eriodictyol powder, Loperamide Hydrochloride Powder CAS 34552 83 5, API Researching Only