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Methylergonovine
drug data and news
Methylergonovine drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Methylergonovine | ||
| Brand Names/Synonyms | Basofortina; CHEMBANK991; Ergometrine, Methyl-; ME 277; Metenarin; Methergen; Methergin; Methergine; Methylergobasin; Methylergobasine; Methylergobrevin; Methylergometrin; Methylergometrine; Methylergonovin; Methylergonovine; Norforms; Partergin; Ryegonovin; Spametrin-M | ||
| Indication | For the prevention and control of excessive bleeding following vaginal childbirth | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Methylergonovine 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. | ||
| Mechanism Of Action | Methylergonovine 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. | ||
| Methylergonovine News (When available) |
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| Dosage Forms | INJECTION (intramuscular or intravenous), TABLETS | ||
| Drug_Category | Oxytocics | ||
| Absorption | Absorption is rapid after oral (60% bioavailability) and intramuscular (78% bioavailability) administration. | ||
| Interactions |
Interactions for Methylergonovine: CYP 3A4 Inhibitors (e.g. Macrolide Antibiotics and Protease Inhibitors) There have been rare reports of serious adverse events in connection with the coadministration of certain ergot alkaloid drugs (e.g. dihydroergotamine and ergotamine) and potent CYP 3A4 inhibitors, resulting in vasospasm leading to cerebral ischemia and/or ischemia of the extremities. Although there have been no reports of such interactions with methylergonovine alone, potent CYP 3A4 inhibitors should not be coadministered with methylergonovine. Examples of some of the more potent CYP 3A4 inhibitors include macrolide antibiotics (e.g., erythromycin, troleandomycin, clarithromycin), HIV protease or reverse transcriptase inhibitors (e.g., ritonavir, indinavir, nelfinavir, delavirdine) or azole antifungals (e.g., ketoconazole, itraconazole, voriconazole). Less potent CYP 3A4 inhibitors should be administered with caution. Less potent inhibitors include saquinavir, nefazodone, fluconazole, grapefruit juice, fluoxetine, fluvoxamine, zileuton, and clotrimazole. These lists are not exhaustive, and the prescriber should consider the effects on CYP 3A4 of other agents being considered for concomitant use with methylergonovine. No pharmacokinetic interactions involving other cytochrome P450 isoenzymes are known. Caution should be exercised when Methergine® (methylergonovine maleate) is used concurrently with other vasoconstrictors or ergot alkaloids. | ||
| Toxicity | Signs and symptoms of overexposure: hypertension, seizures, headache, hypotension, nausea, and vomiting. | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | Not Available | ||
| Chemical Formula | C20H25N3O2 | ||
| Molecular Weight | 339.432 g/mol | ||
| Smiles String | CCC(CO)NC(=O)C1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C | ||
| Melting Point | 172 °C | ||
| Water Solubility | 25 mg/mL | ||
| State | Solid | ||
| LogP/Hphobicity | 1.01 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Hepatic, with extensive first-pass metabolism. | ||
| Half Life | 3.39 hours | ||
| Protein Binding [%] | Not Available | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Methylergonovine.html http://www.rxlist.com/cgi/generic2/methylerg.htm http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/met1256.shtml | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00739 | ||
| CAS Registry Number | 113-42-8 | ||
| KEGG Compound ID | C07800 | ||
| PubChem ID | SID:366829 | ||
| PharmGKB ID | PA450460 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | Not Available |
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