Ergonovine
Ergotamine
Angina Pectoris, Variant
Ergot Alkaloids
Oxytocics
Ergotism
Cyproheptadine
Lysergic Acid
Long lasting spasticity in controlled vasospastic angina. (1/111)
OBJECTIVE: To evaluate changes in coronary artery spasticity in patients with vasospastic angina who had been stable for years under continuous drug treatment. METHODS: Follow up coronary angiography was performed under intracoronary ergonovine provocation in 27 well controlled patients with vasospastic angina and no organic stenosis; the tests were done > 24 months after the initial coronary angiography, in which occlusive spasm had been induced by the same regimen of ergonovine provocation. RESULTS: The mean (SD) follow up period was 47.2 (21.6) months. All patients had been free from angina attack for more than 24 months under treatment with antianginal drugs. During this follow up period, organic stenosis developed in only one case. Occlusive spasm was observed during follow up coronary angiography in 23 patients. Spasm with 90% narrowing was observed in three other patients, and diffuse significant narrowing was seen in the final patient. No significant difference was found in spasticity (p = 0.75) between the initial and the follow up tests. CONCLUSIONS: Repeated ergonovine provocation during coronary angiography after a controlled period of several years showed that coronary spasm remains inducible in most patients. Discontinuance of drug treatment during the remission from anginal attacks achieved by medication may put the patient at high risk. (+info)Alkaloid binding and activation of D2 dopamine receptors in cell culture. (2/111)
Ergot and pyrrolizidine alkaloids, either extracted from endophyte-infected tall fescue, synthesized, or purchased commercially, were evaluated in cultured cells to estimate their binding to the D2 dopamine receptor and subsequent effects on cyclic AMP production in GH4ZR7 cells, transfected with a rat D2 dopamine receptor. Ergopeptide alkaloid (alpha-ergocryptine, bromocryptine, ergotamine tartrate, and ergovaline) inhibition of the binding of the D2-specific radioligand, [3H]YM-09151-2, exhibited inhibition constants (K(I)) in the nanomolar range, whereas dopamine was less potent (micromolar). The lysergic acid amides (ergine and ergonovine) were 1/100th as potent as the ergopeptide alkaloids. Ergovaline and ergotamine tartrate were equally effective in inhibiting vasoactive intestinal peptide (VIP)-stimulated cyclic AMP production, with consistent nanomolar effective concentration (EC50) values. The remaining ergopeptide alkaloids (alpha-ergocryptine and bromocryptine), lysergic acid amides (ergonovine and ergine), and dopamine were 1/100th as potent. Two representative pyrrolizidines, N-formylloline and N-acetylloline, exhibited no binding activity at the D2 dopamine receptor or effects on the cyclic AMP system within the concentration ranges of nanomolar to millimolar. Our results indicate that the commercially available ergot alkaloids ergotamine tartrate and ergonovine may be used interchangeably in the D2 dopamine receptor system to simulate the effects of extracted ergovaline and ergine and to examine responses in receptor binding and the inhibition of cyclic AMP. (+info)Influence of the endothelium, nitric oxide and serotonergic receptors on coronary vasomotor responses evoked by ergonovine in conscious dogs. (3/111)
1. The respective contributions of coronary vascular endothelium, nitric oxide (NO) and serotonergic receptors to the effects of ergonovine on large and small coronary arteries were investigated in conscious dogs. 2. In seven dogs with an endothelium intact, ergonovine (30 - 1000 microg, i.v.) induced a biphasic response on large coronary artery with an early and transient vasodilatation (up to +2.9+/-0.5% from 3310+/-160 microm, P<0.01) followed by a sustained vasoconstriction (down to -4.9+/-0.5%, P<0.001) which occurred simultaneously with a sustained increase in coronary blood flow (CBF) (up to +100+/-26% from 28+/-4 ml min(-1), P<0.001). After endothelium removal (balloon angioplasty), the ergonovine-induced vasodilatation was abolished and vasoconstriction potentiated (-6.4+/-0.9% after vs -4.9+/-0.5% before endothelium removal, P<0.01). 3. After blockade of NO synthesis by Nomega-nitro-L-arginine (30 mg kg(-1)) in four other dogs, the early vasodilatation induced by ergonovine was abolished but the delayed vasoconstriction as well as the increase in CBF remained unchanged. 4. Both ketanserin and methiothepin (0.3 mg kg(-1)) abolished the early vasodilatation and reduced the delayed vasoconstriction induced by ergonovine. Ketanserin decreased and methiothepin abolished the reduction in coronary resistance induced by ergonovine. 5. Thus, the complex interactions between vascular endothelium and serotonergic receptors to ergonovine-induced constriction of large coronary arteries might explain the induction of coronary spasms in patients with endothelial dysfunction. (+info)Ergocryptine and other ergot alkaloids stimulate the release of [3H]dopamine from rat striatal synaptosomes. (4/111)
Ergocryptine is an ergot alkaloid that affects dopaminergic activity principally by interacting with D2-type receptors. In this study the ability of ergocryptine and several other ergot alkaloids to release [3H]dopamine from isolated nerve endings was demonstrated using in vitro superfusion of rat striatal synaptosomes. Ergocryptine, ergocristine, and bromocryptine produced an elevation in baseline dopamine release of approximately 400% with effective concentrations (EC50) of approximately 30 microM. Ergotamine, ergonovine, ergovaline, and ergocornine were devoid of activity. The time-course of the ergocryptine-stimulated release was relatively slow compared with amphetamine, nicotine, or K+-stimulated [3H]dopamine release; the maximal increase in release required a 5-min treatment. A number of receptor antagonists were examined for their ability to block ergocryptine-stimulated release. Of the dopaminergic, adrenergic, serotonergic, GABA-ergic, and cholinergic antagonists examined, only phentolamine produced a moderate attenuation in evoked release. Omission of Ca++ from the medium did not affect ergocryptine-evoked release. Following ergocryptine treatment, the synaptosomes were fully responsive to other stimulant. The results indicate that, in addition to interacting with dopamine receptors, several ergot alkaloids may produce dopaminergic effects by increasing the release of dopamine from central nerve endings. Several mechanisms to account for the evoked neurotransmitter release are discussed. (+info)Safety and clinical impact of ergonovine stress echocardiography for diagnosis of coronary vasospasm. (5/111)
OBJECTIVES: We sought to address the issues of safety, feasibility and clinical impact of noninvasive diagnosis of coronary vasospasm (CVS). BACKGROUND: The safety of ergonovine provocation for CVS performed outside the catheterization laboratory has been questioned. METHODS: We performed a retrospective analysis of the results of bedside ergonovine provocation testing by monitoring left ventricular regional wall motion abnormalities (RWMAs) using two-dimensional echocardiography (Erg Echo). RESULTS: After confirming that there was no significant epicardial coronary stenosis, Erg Echo was performed on 1,372 patients from July 1991 to December 1997. Ergonovine echocardiography was terminated prematurely in 13 patients (0.9%) because of limitations caused by side effects unrelated to myocardial ischemia. Among 1,359 completed tests, 31% (n = 421) showed positive results, with development of RWMAs in 412 tests (98%) or ST displacement in electrocardiograms of nine tests (2%). Arrhythmias developed in 1.9% (26/1,372), including transient ventricular tachycardia (n = 2) and atrioventricular block (n = 4), which were promptly reversed with nitroglycerin. There was no mortality or development of myocardial infarction. Based on the angiographic criteria of 218 patients, the sensitivity and specificity of Erg Echo for the diagnosis of CVS were 93% and 91%, respectively. Since 1994, Erg Echo has become a more popular diagnostic method than invasive spasm provocation testing in the catheterization laboratory and has comprised more than 95% of all spasm provocation tests during the last three years. In the outpatient clinic, 453 patients underwent Erg Echo safely. CONCLUSIONS: Although this is a retrospective study in a single center, we believe that Erg Echo is highly feasible, accurate and safe for the diagnosis of CVS and can replace invasive angiographic spasm provocation testing in the catheterization laboratory. (+info)New combined spasm provocation test in patients with rest angina: intracoronary injection of acetylcholine after intracoronary administration of ergonovine. (6/111)
The incidence of provoked coronary spasm with the standard single spasm provocation test has been relatively low in patients with rest angina. The present study examined the clinical usefulness of a newly designed spasm provocation test, an intracoronary injection of acetylcholine (ACh) following an ergonovine (ER) test, in patients with rest angina who demonstrated low disease activity and atypical chest pain. Triple sequential spasm provocation tests were performed in 24 patients with atypical chest pain who had no ischemia and in 40 patients with rest angina who had distinct ischemia. Initially, an ACh test (20-100 microg) and then an ER test (40-64 microg) were performed and then, if no spasm was provoked, an intracoronary injection of ACh was given after the ER test to evaluate coronary spasm. Coronary spasm was defined as total or subtotal occlusion. In the 24 patients with atypical chest pain, no spasm was provoked by intracoronary injection of either ACh or ER, but coronary spasms were induced in 2 patients using the new method, with the remaining 22 not experiencing spasm (specificity of new method, 92%). In the 40 patients with rest angina, intracoronary injection of ACh induced coronary spasm in 22 patients (group I) and 6 (group II) demonstrated spasm with intracoronary injection of ER. Coronary spasm was not induced by either the ACh test or the ER test in 12 patients (group III). The intracoronary administration of ACh after the ER test provoked spasm in 11 of 12 patients. Diffuse spasms were provoked in 10 of 11 patients. In patients with rest angina, the frequency of chest pain attacks in 1 month experienced by patients in group III (0.8+/-0.8) was significantly lower than that of patients in group I (7.0+/-5.3, p<0.01) or II (3.5+/-2.3, p<0.05). No serious or irreversible complications related to this new combined method were observed. In conclusion, this method was safe and reliable for the induction of coronary spasm in patients with rest angina who may have low disease activity. (+info)Differences between coronary hyperresponsiveness to ergonovine and vasospastic angina. (7/111)
The objective of the present study was to investigate the differences between coronary hyperresponsiveness without ischemia and vasospastic angina in an ergonovine provocation test using multivariate analysis. We have sometimes experienced a more than 50% narrowing response of vascular diameter without ischemia in a coronary response to ergonovine. We studied 107 patients with less than 50% stenosis in a coronary arteriogram. Their vascular responses to ergonovine were measured and the patients were divided into three groups, as follows: Group 1 had 50% or less vascular narrowing response without ischemia; Group 2 had a vascular hyperresponsiveness of more than 50% narrowing response without ischemia; and Group 3 experienced a hyperresponsiveness with ischemia. The degree of coronary response was found to be related to smoking, inpaired glucose tolerance (IGT) and the Gensini score by multiple regression analysis. A multiple logistic analysis revealed that the Gensini score and smoking were significant predictive factors for Group 3 (odds ratio: 1.20 and 8.97). The only factor different between Group 2 and Group 1 was gender. The coronary hyperresponsiveness to ergonovine without ischemia differs from vasospastic angina in the degree of coronary atherosclerosis and smoking habits. The patients with hyperresponsiveness had similar characteristics to those with atypical chest pain rather than vasospastic angina, except for a gender difference. (+info)Activity of 6-methyl-8-substituted ergolines against the 7,12-dimethylbenz(a)anthracene-induced mammary carcinoma. (8/111)
The ability of a series of 8-beta-carboxamido ergolines, 8-formamido ergolines, and 8-methyl ergolines to cause regressions of established dimethylbenz[a]anthracene-induced mammary carcinomas was compared to some ergot alkaloids. Although most of the ergoline derivatives depressed serum prolactin concentrations in rats, only a few had pronounced effects against the dimethylbenz[a]anthracene-induced mammary carcinoma in rats. Some derivatives from each of the three groups of substituted ergolines gave comparable activities against the dimethylbenz[a]anthracene-induced mammary carcinoma. (+info)Ergonovine is a medication that belongs to a class of drugs called ergot alkaloids. It is derived from the ergot fungus and is used in medical settings as a uterotonic agent, which means it causes the uterus to contract. Ergonovine is often used after childbirth to help the uterus return to its normal size and reduce bleeding.
Ergonovine works by binding to specific receptors in the smooth muscle of the uterus, causing it to contract. It has a potent effect on the uterus and can also cause vasoconstriction (narrowing of blood vessels) in other parts of the body. This is why ergonovine is sometimes used to treat severe bleeding caused by conditions such as uterine fibroids or ectopic pregnancy.
Like other ergot alkaloids, ergonovine can have serious side effects if not used carefully. It should be administered under the close supervision of a healthcare provider and should not be used in women with certain medical conditions, such as high blood pressure or heart disease. Ergonovine can also interact with other medications, so it's important to inform your healthcare provider of all medications you are taking before receiving this drug.
Coronary vasospasm refers to a sudden constriction (narrowing) of the coronary arteries, which supply oxygenated blood to the heart muscle. This constriction can reduce or block blood flow, leading to symptoms such as chest pain (angina) or, in severe cases, a heart attack (myocardial infarction). Coronary vasospasm can occur spontaneously or be triggered by various factors, including stress, smoking, and certain medications. It is also associated with conditions such as coronary artery disease and variant angina. Prolonged or recurrent vasospasms can cause damage to the heart muscle and increase the risk of cardiovascular events.
Ergotamine is a type of ergopeptine alkaloid, derived from the ergot fungus (Claviceps purpurea) that parasitizes certain grains, particularly rye. It is a potent vasoconstrictor and has been used medically to prevent migraines and treat cluster headaches, as well as for other uses such as controlling postpartum hemorrhage and reducing symptoms of orthostatic hypotension.
Ergotamine works by binding to serotonin receptors in the brain and causing vasoconstriction of cranial blood vessels, which can help to relieve migraine headaches. However, it can also cause serious side effects such as nausea, vomiting, muscle pain, numbness or tingling in the extremities, and in rare cases, more severe reactions such as ergotism, a condition characterized by vasoconstriction of peripheral blood vessels leading to gangrene.
Ergotamine is usually taken orally, but can also be administered rectally or by inhalation. It is important to follow the dosage instructions carefully and avoid taking excessive amounts, as this can increase the risk of serious side effects. Ergotamine should not be taken during pregnancy or while breastfeeding, and it may interact with other medications, so it is important to inform your healthcare provider of all medications you are taking before starting ergotamine therapy.
Angina pectoris, variant (also known as Prinzmetal's angina or vasospastic angina) is a type of chest pain that results from reduced blood flow to the heart muscle due to spasms in the coronary arteries. These spasms cause the arteries to narrow, temporarily reducing the supply of oxygen-rich blood to the heart. This can lead to symptoms such as chest pain, shortness of breath, and fatigue.
Variant angina is typically more severe than other forms of angina and can occur at rest or with minimal physical exertion. It is often treated with medications that help relax the coronary arteries and prevent spasms, such as calcium channel blockers and nitrates. In some cases, additional treatments such as angioplasty or bypass surgery may be necessary to improve blood flow to the heart.
It's important to note that chest pain can have many different causes, so it is essential to seek medical attention if you experience any symptoms of angina or other types of chest pain. A healthcare professional can help determine the cause of your symptoms and develop an appropriate treatment plan.
Ergot alkaloids are a type of chemical compound that is produced naturally by certain fungi belonging to the genus Claviceps. These alkaloids are most famously known for being produced by the ergot fungus (Claviceps purpurea), which infects cereal grains such as rye and causes a condition known as ergotism in humans and animals that consume the contaminated grain.
Ergot alkaloids have a complex chemical structure and can have various effects on the human body. They are known to act as powerful vasoconstrictors, which means that they cause blood vessels to narrow and can increase blood pressure. Some ergot alkaloids also have psychoactive effects and have been used in the past for their hallucinogenic properties.
In modern medicine, certain ergot alkaloids are used in the treatment of various conditions, including migraines and Parkinson's disease. However, these compounds can be highly toxic if not used properly, and their use must be carefully monitored to avoid serious side effects.
Oxytocics are a class of medications that stimulate the contraction of uterine smooth muscle. They are primarily used in obstetrics to induce or augment labor, and to control bleeding after childbirth. Oxytocin is the most commonly used oxytocic and is naturally produced by the posterior pituitary gland. Synthetic forms of oxytocin, such as Pitocin, are often used in medical settings to induce labor or reduce postpartum bleeding. Other medications with oxytocic properties include ergometrine and methylergometrine. It's important to note that the use of oxytocics should be monitored carefully as overuse can lead to excessive uterine contractions, which may compromise fetal oxygenation and increase the risk of uterine rupture.
Ergotism is a condition that results from the consumption of ergot alkaloids, which are found in ergot fungus that infects grains such as rye. There are two types of ergotism: convulsive and gangrenous. Convulsive ergotism can cause seizures, muscle spasms, vomiting, and mental disturbances. Gangrenous ergotism, on the other hand, can lead to constriction of blood vessels, resulting in dry gangrene of the extremities, which can ultimately require amputation. Ergotism has been known since ancient times and was once a significant public health problem before modern agricultural practices were implemented.
Cyproheptadine is an antihistamine and anticholinergic medication that is primarily used to treat symptoms of allergies, such as runny nose, sneezing, and itching. It works by blocking the action of histamine, a substance in the body that causes allergic reactions.
Cyproheptadine also has other uses, including the treatment of migraines and cluster headaches, appetite stimulation in people with certain medical conditions, and as a sedative in some cases. It is available in various forms, such as tablets, capsules, and syrup.
Like all medications, cyproheptadine can have side effects, including drowsiness, dry mouth, dizziness, and blurred vision. It is important to follow the dosage instructions carefully and talk to a healthcare provider if you experience any bothersome or persistent side effects.
Ergotamines are a type of medication that is derived from the ergot fungus (Claviceps purpurea). They are primarily used to treat migraines and cluster headaches. Ergotamines work by narrowing blood vessels around the brain, which helps to alleviate the symptoms of migraines and headaches.
Ergotamines are available in various forms, including tablets, suppositories, and injectable solutions. They can be taken orally, rectally, or intravenously, depending on the severity of the symptoms and the patient's medical history. Ergotamines should be used with caution, as they can cause serious side effects such as nausea, vomiting, muscle pain, and weakness.
Ergotamines are also used in the treatment of other conditions, including postpartum hemorrhage, heart failure, and high blood pressure during pregnancy. However, their use in these conditions is typically reserved for cases where other treatments have been ineffective or contraindicated.
It's important to note that ergotamines can interact with a variety of medications, including certain antidepressants, antibiotics, and HIV medications. Therefore, it's essential to inform your healthcare provider about all the medications you are taking before starting treatment with ergotamines.
Lysergic acid is not a medical term per se, but it is a key component in the chemical structure of several psychedelic drugs, including LSD (lysergic acid diethylamide). Medically, lysergic acid itself does not have any approved uses. However, I can provide you with a definition of LSD:
LSD (Lysergic Acid Diethylamide) is a potent synthetic hallucinogenic drug, derived from lysergic acid, a compound found in the ergot fungus that grows on grains. LSD is typically consumed orally, often by placing it on absorbent paper, which is then dried and cut into small squares known as "blotters."
LSD is classified as a Schedule I controlled substance in the United States and in many other countries, indicating that it has a high potential for abuse, no currently accepted medical use, and a lack of safety under medical supervision. Its effects on perception, mood, and thought are highly unpredictable and can vary greatly among users and even between experiences had by the same user.
Coronary vessels refer to the network of blood vessels that supply oxygenated blood and nutrients to the heart muscle, also known as the myocardium. The two main coronary arteries are the left main coronary artery and the right coronary artery.
The left main coronary artery branches off into the left anterior descending artery (LAD) and the left circumflex artery (LCx). The LAD supplies blood to the front of the heart, while the LCx supplies blood to the side and back of the heart.
The right coronary artery supplies blood to the right lower part of the heart, including the right atrium and ventricle, as well as the back of the heart.
Coronary vessel disease (CVD) occurs when these vessels become narrowed or blocked due to the buildup of plaque, leading to reduced blood flow to the heart muscle. This can result in chest pain, shortness of breath, or a heart attack.
Isosorbide dinitrate is a medication that belongs to a class of drugs called nitrates. It is primarily used in the prevention and treatment of angina pectoris, which is chest pain caused by reduced blood flow to the heart muscle.
The medical definition of Isosorbide dinitrate is:
A soluble nitrate ester used in the prevention and treatment of anginal attacks. It acts by dilating coronary and peripheral arteries and veins, thereby reducing cardiac workload and increasing oxygen delivery to the heart muscle. Its therapeutic effects are attributed to its conversion to nitric oxide, a potent vasodilator, in the body. Isosorbide dinitrate is available in various forms, including tablets, capsules, and oral solutions, and is typically taken 2-3 times daily for optimal effect.
Ergometrine
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