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Results for “Methylergonovine”

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At least 19 recordsLinked to original sources
PubMedDate not supplied

The use of methylergonovine (Methergine) in the initial control of drug induced refractory headache.

This study investigated the efficacy of methylergonovine maleate (Methergine) in the treatment of drug induced refractory headache (DIRH). Sixty consecutive patients (51 female and 9 male) diagnosed with DIRH were treated with methylergonovine maleate for a maximum of six months, using a within subject design. All patients were withdrawn from the medications they were taking upon entering the study. Concurrently, they were given 0.2-0.4 mg of methylergonovine maleate three times a day. Patients were provided the means to control breakthrough episodes of headache. Treatment outcome was assessed using a patient self-report scale (much better, better, same, worse, and much worse), and also visual analogue pain intensity scales. The side effects of the drug were assessed with patient self-report. Methylergonovine was effective in 44 (73%) patients. Twelve (20%) patients reported unchanged pain and 4 (6%) patients got worse. Side effects were reported by 24 patients. These were predominantly abdominal cramping. It is concluded that methylergonovine maleate is effective in the initial control of drug induced refractory headache. However, because methylergonovine is a metabolic byproduct of methysergide, the possibility or fibrotic disorders needs to be considered if methylergonovine is to be used for long term therapy.

Adult↗
PubMed2000

Modulation of contractions to ergonovine and methylergonovine by nitric oxide and thromboxane A2 in the human coronary artery.

This study explored the modulatory effects of nitric oxide and thromboxane A2 on contractions to ergonovine and methylergonovine in human coronary arteries. To elucidate the different role of nitric oxide synthase in the response to the ergot alkaloids, the serotonin (5-HT) receptors involved in nitric oxide synthase in the response to the ergot alkaloids, the 5-HT receptors involved in nitric oxide release and the contraction of the vascular smooth muscle were characterized with more selective 5-HT-receptor agonists and antagonists. Rings of human coronary arteries from explanted hearts were suspended in organ chambers for isometric tension recording. After testing for contractile (potassium chloride, 60 mM) and endothelial function (substance P, 10(-8) M), respectively, they were exposed to ergot alkaloids or other agonists in the absence or presence of U 46619 (10(-9) M), or nitro-L-arginine (10(-4) M), or both. Ergonovine and methylergonovine were comparable, weak vasoconstrictors in untreated preparations. Contractions to ergonovine were augmented by U 46619, but not by nitro-L-arginine. Contractions to methylergonovine were augmented only by combining U 46619 and nitro-L-arginine. Serotonin and methylergonovine, but not ergonovine, elicited endothelium-dependent, nitric oxide-mediated relaxations. Nonselective 5-HT(1B/1D)-receptor stimulation caused both contractions and relaxations; selective 5-HT1B stimulation caused relaxations only. In the human coronary artery, contractions to ergonovine are not dependent on NO release but are synergistically augmented by thromboxane. Methylergonovine causes similar effects on the vascular smooth muscle, but contractions are inhibited by the release of NO from the endothelium. The 5-HT receptor on the endothelium appears to be different from the receptor on the vascular smooth muscle, which mediates the contractile response to the ergot alkaloids.

Adult↗
PubMed1991

Effect of direct intracoronary administration of methylergonovine in patients with and without variant angina.

The effects of intracoronary administration of methylergonovine were studied in 21 patients with variant angina and 22 patients with atypical chest pain and in others without angina pectoris (control group). Methylergonovine was administered continuously at a rate of 10 micrograms/min up to 50 micrograms. In all patients with variant angina, coronary spasm was provoked at a mean dose of 28 +/- 13 micrograms (mean +/- SD). In the control group neither ischemic ST change nor localized spasm occurred. The basal tone of the right coronary artery was significantly lower than that of the left coronary artery. The percentage of vasoconstriction of the right coronary artery was significantly higher than that of the left coronary artery. These results suggest that spasm provocation tests, which use an intracoronary injection of a relatively low dose of methylergonovine, have a high sensitivity in variant angina and the vasoreactivity of the right coronary artery may be greater than that of the other coronary arteries.

Adult↗
PubMedDate not supplied

Methylergonovine-induced diffuse coronary spasm in a patient with exercise-induced coronary spasm after heart transplantation.

Coronary artery spasm is a rarely reported condition after heart transplantation. We report a case of exercise-induced coronary artery spasm in a patient 1-year after orthotopic heart transplantation. Serial quantitative coronary angiography showed significant diffuse loss of luminal diameter. Provocative testing with intracoronary acetylcholine and intravenous methylergonovine maleate was performed in an effort to document efficacy of the antispasm regimen. Infusion of acetylcholine into the left anterior descending coronary artery resulted in transient closure of the vessel. Diffuse spasm resulting in hypotension and ventricular fibrillation occurred with intravenous methylergonovine maleate administration. Because of the risk of provoking diffuse spasm, intravenous administration of methylergonovine maleate should be avoided in the posttransplantation setting. Review of the literature suggests that coronary artery spasm after transplantation is often associated with severe transplant coronary artery disease and may be associated with a poor prognosis. Coronary artery spasm may be a more common cause of syncope and death after transplantation than it is currently thought to be.

Acetylcholine↗
PubMed1978

The role of methylergonovine maleate in augmenting extraamniotic saline for midtrimester abortion.

This study was conducted in Bombay, India, to evaluate the role of oral methylergonovine maleate (Methergine, Sandoz Pharmaceuticals, East Hanover, N.J., USA) in augmenting the effect of intermittent extraamniotic instillation of 20% saline for midtrimester abortion in 200 patients. Methylergonovine maleate (MEM) administration was randomly allocated to half the study subjects. All the study procedures were performed by a single operator, and to minimize evaluator bias, another physician evaluated all the study patients after abortion. This study showed that a statistically significant higher percentage of patients in the MEM treated group aborted within 24 hours. At 36 and 48 hours, the differences were not statistically significant, although the cumulative abortion rates were higher for subjects who received the drug than for those who did not. The incidence of incomplete abortions was lower for those treated with MEM than for those not treated with the drug, but the difference was not statistically significant. The rates of complications and side effects were similar for both study groups.

Abortion, Induced↗
PubMedDate not supplied

Methylergonovine maleate as a cluster headache prophylactic: a study and review.

Methylergonovine maleate (Methergine), an ergot derivative with vasoconstrictive properties, has been cited as an effective treatment for vascular headaches. Few studies are available to support its use in headache management. An uncontrolled pilot study of 20 episodic cluster headache patients confirmed its effectiveness and tolerability as an adjunct cluster headache prophylactic. Decreased headache frequency was reported by 19 of 20 patients (95%), and 15 of 20 patients (75%) reported decreased intensity of headaches within 1 week of initiating therapy. A review of methylergonovine's pharmacokinetic, molecular, and tolerability profile clarifies its mechanisms and clinical role in headache management.

Cluster Headache↗
PubMed1985

Methylergonovine-induced spasm of saphenous vein coronary bypass graft.

A case of repeated methylergonovine-induced spasm of a saphenous vein bypass graft in a 56-year-old man is presented. Prior to the operation, spasm was induced by methylergonovine in the stenosed right coronary artery. Six months after the operation, coronary angiographic studies showed induced spasm of the right coronary graft but no spasm in native vessels nor in the other graft to the left anterior descending coronary artery.

Angina Pectoris↗
PubMed1975

Effect of methylergonovine on puerperal prolactin secretion.

Serum prolactin concentration was measured by radioimmunoassay in 29 women, in the first 1 1/2 hours postpartum. Fourteen women received 0.2 mg methylergonovine maleate (Methergine) intramuscularly after the delivery of the placenta. Fifteen women who served as controls received only saline. The rise in serum prolactin concentration seen in the control women (266.4 ng/ml +/- 40.8 SE) was significantly greater than that seen in methylergonovine-treated patients (141.0 ng/ml +/- 29.0. SE).

Female↗
PubMed1989

Effect of intracoronary nicardipine on methylergonovine-induced coronary artery spasm in patients with variant angina.

In a double-blind, randomized placebo controlled study, the effect of intracoronary (IC) nicardipine (0.4 mg) on methylergonovine (0.4 mg) induced coronary artery spasm was assessed in 16 patients with a history of variant angina. Reversal of the methylergonovine-induced coronary artery spasm was observed in 100% of patients treated with IC nicardipine and 25% of patients treated with placebo (p less than 0.01). There were no significant differences between the nicardipine and placebo treatment groups with respect to heart rate, blood pressure, proportion of patients experiencing chest pain or ST segment changes. These findings demonstrate that IC nicardipine is safe and could be effective in the reversal of coronary artery spasm in patients with variant angina.

Angina Pectoris, Variant↗
PubMed1978

Fluoremetric determination of methylergonovine maleate and ergonovine maleate in tablets and injections.

A column cleanup, followed by a shakeout and fluorometric determination, has been developed to determine methylergonovine maleate and ergonovine maleate in tablets and injections. The ether eluate is extracted with tartaric acid solution. An aliquot is diluted with sodium tartrate solution, and this solution is excited at 325 nm. The resulting fluorescence is measured at 432 nm. Results obtained using this method compare favorably with those from the official NF XIV procedure and a semiautomated procedure. Recoveries of 100 and 99% were obtained from one sample each of spiked excipient tablets of methylergonovine maleate and ergonovine maleate, respectively.

Ergonovine↗
PubMed1980

Plasma and tissue concentrations of methylergometrine (methylergonovine) in the rabbit.

The concentrations of methylergometrine (M) (methylergonovine) in the plasma, uterus, liver, and kidneys of the rabbit were determined by a radioimmunoassay after a single 0.2 mg/kg intravenous injection and the drug response was studied in the uterus in situ. M disappeared quickly from the plasma with a mean distribution phase half-life of 0.91 min. According to the fast uterine tissue uptake of M the drug response in this effector organ began quickly. The stimulated concentrations in the peripheral compartment of the two-compartment open model can be useful in the understanding of the rapid drug effect, but they do not describe the real situation in any particular tissue.

Animals↗
PubMed1988

Methylergonovine-induced hypertonus in term pregnancy. A case report.

The administration of methylergonovine maleate to a patient at term is rare. A patient received the drug at 36 weeks' gestation, with subsequent development of fetal distress secondary to uterine tetany. Treatment with terbutaline and magnesium sulfate was unsuccessful in alleviating the uterine hypertonus, necessitating cesarean section.

Adolescent↗
PubMed1981

Clinical pharmacokinetics of methylergometrine (methylergonovine).

Pharmacokinetic studies carried out on methylergometrine (methylergonovine) by a radioimmunoassay are reviewed. After intravenous injection the half-life of the distribution phase was only 1-3 min, explaining the fast and strong oxytocic response in puerperal mothers. The fast tissue uptake was also obtained in the rabbit uterus in situ with a steep dose-response curve. The rate of gastrointestinal absorption appeared to be slower in patients during puerperium (Tmax 3 h) in comparison with healthy male volunteers (Tmax 0.5 h). The bioavailability after administration was about 60%. After intramuscular injection the rate of absorption was rapid (Tmax 0.5 h). The short half-life of the elimination phase (about 0.5-2 h), low apparent volume of distribution (about that of extracellular water of the body), and the relatively high total plasma clearance value (about 120-240 ml/min) were direct evidence of the rapid elimination of the drug from the body. After repeated oral administrations no accumulation was found. Only about 3% of the single oral dose was excreted into urine, indicating hepatic metabolism and elimination. Although methylergometrine had a good penetration into breast milk in dogs, in postpartum women the mild concentrations were hardly measurable and clinically nonsignificant. Apparently there is no correlation between the plasma level and clinical effect of methylergometrine.

Animals↗
PubMed1975

Semiautomated analysis of ergonovine maleate or methylergonovine maleate tablets and injections by colorimetric or fluorometric systems.

Two semiautomated analytical systems have been developed to determine ergonovine and methylergonovine maleate in single tablets and injections. The active ingredient is dissolved in a tartrate buffer. In the fluorometric method the stream is automatically diluted with tartrate buffer and excited with ultraviolet light; the resulting fluorescence is measured and recorded. In the colorimetric method, the stream is automatically made basic with sodium hydroxide and extracted with n-butanol. The extract is mixed with p-dimethylaminobenzaldehyde reagent. After reaction, the solution is mixed with sodium nitrite solution, and the developed color is measured at 550 nm. Recoveries of 100% were obtained from spiked placebos. Standard deviations for powdered tablet and injection samples ranged from 0.63 to 1.24%. Comparisons with the USP XVIII methods are presented.

Autoanalysis↗