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Methylergometrine | CAS No: 113-42-8 | GMP-certified suppliers
A medication that prevents and controls excessive bleeding after vaginal childbirth by promoting uterine muscle contractions to reduce postpartum hemorrhage.
Therapeutic categories
Primary indications
- For the prevention and control of excessive bleeding following vaginal childbirth
Product Snapshot
- Methylergometrine is available primarily as injectable solutions and oral tablets in various coated and uncoated formulations
- It is indicated for the prevention and control of excessive bleeding following vaginal childbirth
- The product is approved and marketed in the US with regulatory clearance
Clinical Overview
Clinically, methylergometrine is indicated for the prevention and control of excessive bleeding following vaginal childbirth, specifically targeting postpartum and post-abortion hemorrhage. It is employed to reduce uterine atony and related hemorrhagic complications by promoting uterine muscle contraction.
Pharmacodynamically, methylergometrine exerts its effects primarily through partial agonist and antagonist activity at multiple receptor systems, including adrenergic, dopaminergic, and tryptaminergic receptors. Its principal mechanism involves direct action on uterine smooth muscle, increasing tone, frequency, and amplitude of rhythmic contractions. This action is mediated through antagonism of dopamine D1 receptors, resulting in a rapid and sustained tetanic uterotonic effect. These contractions shorten the third stage of labor, thereby decreasing blood loss.
In terms of absorption, distribution, metabolism, and excretion (ADME), methylergometrine is a substrate and inhibitor of cytochrome P450 CYP3A4 enzymes, indicating potential for metabolic interactions and altered plasma levels when co-administered with other CYP3A4 substrates or inhibitors. Such interactions necessitate careful consideration during clinical use. Data on absolute bioavailability, protein binding, and elimination half-life are not specified here.
Safety considerations include its vasoconstrictive properties, which can produce hypertension and related cardiovascular effects. Use is contraindicated in patients with hypertensive disorders or vascular disease due to risk of adverse events. As a dopamine antagonist and ergot derivative, it may also present risks of off-target neurological or systemic effects if misused or overdosed.
Methylergometrine is approved internationally and appears in various formulations used in obstetric practice. It is categorized under uterotonic agents, ergolines, and dopamine antagonists.
For API sourcing and quality control, it is important to ensure compliance with pharmacopeial standards regarding purity, isomeric composition, and residual solvents. Given its activity on CYP enzymes and narrow therapeutic index, stringent control of impurities and consistency in synthesis is critical to mitigate variability and safety risks during pharmaceutical manufacturing.
Identification & chemistry
| Generic name | Methylergometrine |
|---|---|
| Molecule type | Small molecule |
| CAS | 113-42-8 |
| UNII | W53L6FE61V |
| DrugBank ID | DB00353 |
Pharmacology
| Summary | Methylergometrine is a semisynthetic ergot alkaloid that targets dopamine D1 and 5-hydroxytryptamine 2B receptors to increase uterine smooth muscle tone and contractility. It induces sustained uterotonic contractions, facilitating the prevention and control of postpartum hemorrhage. Its pharmacodynamic effects result from partial agonism and antagonism at multiple receptor types, enhancing uterine motor activity in a dose-dependent manner. |
|---|---|
| Mechanism of action | Methylergometrine acts directly on the smooth muscle of the uterus and increases the tone, rate, and amplitude of rhythmic contractions through binding and the resultant antagonism of the dopamine D1 receptor. Thus, it induces a rapid and sustained tetanic uterotonic effect which shortens the third stage of labor and reduces blood loss. |
| Pharmacodynamics | Methylergometrine is a semisynthetic ergot alkaloid and a derivative of ergonovine and is used for the prevention and control of postpartum and post-abortion hemorrhage. In general, the effects of all the ergot alkaloids appear to results from their actions as partial agonists or antagonists at adrenergic, dopaminergic, and tryptaminergic receptors. The spectrum of effects depends on the agent, dosage, species, tissue, and experimental or physiological conditions. All of the alkaloids of ergot significantly increase the motor activity of the uterus. After small doses contractions are increased in force or frequency, or both, but are followed by a normal degree of relaxation. As the dose is increased, contractions become more forceful and prolonged, resting tonus is markedly increased, and sustained contracture can result. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Dopamine D1 receptor | Humans | antagonist |
| 5-hydroxytryptamine receptor 2B | Humans |
ADME / PK
| Absorption | Absorption is rapid after oral (60% bioavailability) and intramuscular (78% bioavailability) administration. |
|---|---|
| Half-life | 3.39 hours |
| Metabolism | Hepatic, with extensive first-pass metabolism. |
| Route of elimination | Ergot alkaloids are mostly eliminated by hepatic metabolism and excretion, and the decrease in bioavailability following oral administration is probably a result of first-pass metabolism in the liver. |
| Volume of distribution | * 56.1 ± 0 L |
Formulation & handling
- Methylergometrine is available for both oral and parenteral administration, including intramuscular and intravenous injections.
- It is a small molecule lysergamide with moderate water solubility (0.204 g/L) and a LogP of 1.59, indicating balanced lipophilicity for formulation considerations.
- Avoid co-administration with grapefruit products due to CYP3A4 inhibition, which can increase systemic exposure and affect safety.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) is approaching patent expiry in the US, marking a transition toward increased generic competition and market maturity. Post-patent, the API is expected to enter a mature phase characterized by multiple generic entries and stabilized pricing. |
|---|
| Markets | US |
|---|
Supply Chain
| Supply chain summary | Methylergometrine is produced by a limited number of originator companies, primarily Novartis Pharmaceuticals Corp and Pharmaforce Inc. The branded product, Methergine, is mainly marketed in the US, with multiple packagers involved in its distribution. Patent expiry status suggests that generic competition is either existing or likely, given the presence of various repackagers and suppliers active in the market. |
|---|
Safety
| Toxicity | Signs and symptoms of overexposure: hypertension, seizures, headache, hypotension, nausea, and vomiting. |
|---|
- Exposure may cause central nervous system effects including seizures and headache
- Overexposure symptoms include hypertension, hypotension, nausea, and vomiting
- Handle with appropriate protective equipment to minimize inhalation and dermal contact
Methylergometrine is a type of Uterotonics
Uterotonics are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that are widely used in the field of obstetrics and gynecology. These drugs are primarily employed to induce or enhance uterine contractions, thereby promoting labor and preventing postpartum hemorrhage.
Uterotonics exert their pharmacological effects by targeting specific receptors in the smooth muscle of the uterus. One of the most commonly used uterotonics is oxytocin, a hormone naturally produced by the body during childbirth. Synthetic forms of oxytocin, known as oxytocin analogs, are also utilized in medical settings to initiate or augment labor.
In addition to oxytocin, other uterotonics include ergot alkaloids, such as methylergonovine, and prostaglandin analogs, such as misoprostol. These drugs act through different mechanisms to stimulate uterine contractions.
The administration of uterotonics requires careful monitoring and precise dosing to avoid complications. While they are generally safe and effective, uterotonics can cause side effects, including nausea, vomiting, and uterine hyperstimulation. Therefore, medical professionals closely monitor patients receiving uterotonics to ensure optimal outcomes.
Overall, uterotonics play a vital role in obstetric care, facilitating safe and efficient labor and preventing excessive bleeding after childbirth. These pharmaceutical APIs have significantly contributed to improving maternal and neonatal health worldwide, making them indispensable tools in the field of obstetrics and gynecology.
Methylergometrine (Uterotonics), classified under Genitourinary Agents
Genitourinary agents are a category of pharmaceutical active ingredients (APIs) that are specifically designed to target and treat disorders related to the genitourinary system. The genitourinary system encompasses the organs and structures involved in the production, storage, and elimination of urine, as well as the reproductive organs.
These APIs play a crucial role in the treatment of various genitourinary conditions, including urinary tract infections (UTIs), erectile dysfunction, urinary incontinence, benign prostatic hyperplasia (BPH), and other related disorders. They exert their therapeutic effects by interacting with specific receptors or enzymes in the genitourinary system, regulating physiological processes, and restoring normal function.
Some commonly used genitourinary agents include alpha-blockers, which relax the smooth muscles in the prostate and bladder neck, improving urine flow in patients with BPH. Additionally, phosphodiesterase type 5 inhibitors (PDE5 inhibitors) are widely prescribed for erectile dysfunction, as they enhance blood flow to the penile tissues, facilitating erection.
These APIs are typically formulated into various dosage forms, such as tablets, capsules, creams, gels, or injections, allowing for convenient administration to patients. The development and production of genitourinary agents involve stringent quality control measures and compliance with regulatory guidelines to ensure safety, efficacy, and consistent product performance.
In summary, genitourinary agents form a crucial category of pharmaceutical APIs used to treat a range of disorders affecting the genitourinary system. Their targeted mechanisms of action and diverse dosage forms make them valuable tools in improving genitourinary health and enhancing patients' quality of life.
Methylergometrine API manufacturers & distributors
Compare qualified Methylergometrine API suppliers worldwide. We currently have 1 companies offering Methylergometrine API, with manufacturing taking place in 1 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Emeishan Hongsen Biopharm... | Producer | China | China | CoA, MSDS | 107 products |
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