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At least 127 records · Page 7Linked to original sources
PubMed1980

The effect of single dose ergotamine tartrate on peripheral arteries in migraine patients: methodological aspects and time effect curve.

Ergotamine tartrate (0.5 mg/70 kg) was given intravenously to 17 migraine patients. Arm, finger, ankle and big toe systolic blood pressures were measured with strain gauge technique for up to 4 hours and again after 22 hours. Systolic arm blood pressure increased transiently (duration less than 3 hours). Peripheral systolic blood pressures decreased in all patients (for toes a few to 55 mmHg) and at 22 hours well sustained decreases were still found. Further 10 migraine patients received 2-4 mg ergotamine tartrate as suppositories and peripheral systolic blood pressures were measured for 3 days. A decrease in peripheral systolic blood pressure was found after 24 hours but had disappeared after 48 hours. Contrary to common belief the present study investigating the effect of ergotamine directly on arteries has shown a long duration of its vasoconstrictory effect. Thus the effect of a single dose of ergotamine on the arteries should be followed for days.

Adult↗
PubMed1974

Buccal absorption of ergotamine.

The rate of disappearance of ergotamine from the mouth after buccal administration has been studied in seven subjects. Allowance has been made for non-absorptive losses of the drug due to experimental technique. The absorption of ergotamine across the buccal mucosa appears to be a passive process, pH-dependent but independent of ergotamine concentration or the simultaneous presence of caffeine. Because of the low solubility of ergotamine at the pH of saliva, it is unlikely that therapeutically useful amounts of the drug would have absorbed across the buccal mucosa even after the drug had been in the mouth for five minutes.

Absorption↗
PubMed1975

Enhanced prostaglandin synthesis contributes to the venoconstrictor activity of ergotamine.

Spiral strips from dog saphenous veins were contracted by 2.5 X 10(-9) M ergotamine, a concentration giving about 50% of maximal response. Phentolamine (3.6 X 10(-6) M) reduced these effects by 60% and indomethacin (2.8 X 10(-7) M) by 30%. Indomethacin was more effective in reducing ergotamine-induced increase of prostaglandin E-like activity in the bathing fluid than those induced by noradrenaline or potassium chloride. Arachidonic acid was more effective in increasing tension in ergotamine-stimulated than in noradrenaline- or potassium-stimulated veins. These findings suggest that the long-lasting venoconstrictor activity of ergotamine is mediated mainly by alpha-adrenoceptors but that enhanced formation of prostaglandin E-like substance(s) may also contribute.

Animals↗
PubMed1986

Ergotamine-induced peripheral ischaemia reversed by oral thymoxamine hydrochloride.

Although there is no generally accepted therapy for ergotamine-induced vasoconstriction, infusion of directly acting vasodilators is regarded presently as the treatment of choice. We present a case of peripheral arterial ischaemia secondary to excessive use of ergotamine suppositories, which was reversed with oral thymoxamine hydrochloride (an alpha 1-adrenoceptor antagonist) and ergotamine withdrawal. We suggest that in patients with ergotamine-induced peripheral arterial vasoconstriction with no evidence of gangrene, oral thymoxamine may be considered as a useful adjunct or possible alternative to infused vasodilator treatment.

Adult↗
PubMed1980

Effect of bromocriptine, ergotamine and other ergot alkaloids on the hormone secretion and growth of a rat pituitary tumour.

The effect of bromocriptine on hormone secretion and the growth of the prolactin- and growth hormone (GH)-secreting rat pituitary tumour of the GH3 cell line has been compared with that of ergotamine and other ergot alkaloids. Bromocriptine in doses ranging from 1 to 20 mg/kg had no effect on tumour growth or on the excessive secretion of GH by the tumour; prolactin concentrations were reduced only by the highest dosage of the drug. Similarly the tumour was resistant to the administration of ergocryptine, ergocornine and the synthetic ergolines, lergotrile and CH 29-717. In contrast, ergotamine reduced secretion of both GH and prolactin and considerably inhibited the growth of the tumour. Experiments in vitro showed that ergotamine inhibited DNA synthesis of the tumour cells and decreased hormone secretion. It was concluded that ergotamine had a direct inhibitory action on the GH3 cell tumour which was not mediated through the dopaminergic mechanisms.

Animals↗
PubMed2000

Physiological responses of Brahman and Hereford steers to an acute ergotamine challenge.

Research was conducted to evaluate the sensitivity of Bos indicus and Bos taurus cattle to a tall fescue ergopeptine alkaloid by assessing vital sign responses. Eight Polled Hereford and seven Red Brahman steers received bolus i.v. injections of ergotamine tartrate and saline vehicle in a simple cross-over design. Physiological traits measured 30 min and immediately before and 30, 60, and 90 min after treatment were respiration rate, rectal temperature, skin temperature at the tailhead and tail tip, systolic and diastolic blood pressure, and heart rate. Blood samples were collected immediately before and 105 min after treatments to determine plasma prolactin and cortisol concentrations. Steers were fed a fescue-free diet in drylot. Ambient temperature and relative humidity averaged 31 degrees C and 55%, respectively, during data collection. No breed x treatment x time interactions were apparent for vital signs. The treatment x time interaction was significant (P < .05) for blood pressure and skin temperature. Ergotamine increased (P < .01) blood pressure and decreased (P < .01) skin temperature. The breed x treatment x time interactions were significant for prolactin (P < .1) and cortisol (P < .01). Ergotamine decreased plasma (P < .01) prolactin and increased (P < .01) cortisol concentrations in both breeds, despite some breed variation. Across all traits, Brahman and Hereford steers responded similarly to acute ergotamine exposure, indicating that the breeds are alike in acute sensitivity to a systemically administered ergopeptine alkaloid associated with fescue toxicosis.

Animals↗
PubMedDate not supplied

[Risks related to the use of ergotamine in the therapy of hemicrania. Description of a case].

The ergotamine tartrate used for the migraine headache therapy can induce to a condition of chronic intoxication (ergotism) similar to what occurs after the ingestion of Claviceps purpurea contaminated rye. The case of an Italian woman affected by chronic migraine rectally treated with ergotamine showed cerebral and legs ischaemic indications--angiographically documented--vasospasm in the carotid and femoral arterial area. The withdrawal of the drug produced complete remission. It is therefore important to consider ergotism as a cause of the non-atherosclerotic vascular ischaemic disease; the authors also underline the serious risks linked to the ergotamine self prescription should the maximum dose of the 10 mg be exceeded via rectum over the period of one week (see the above illustrated case). No other evidence of intoxication due to ergotamine with angiography documentation with femoral and carotid involvement is described in literature.

Ergotamine↗
PubMed1995

[Ergotamine-induced anorectal lesions].

During the past 10 years several reports on perianal ulcerations secondary to chronic use of ergotamine suppositories were published. The present case reports deal with 2 female patients who used ergotamine suppositories for treatment of sick head aches for several years. In both cases the suppositories were used chronically. The first patient, a 60 year old woman has been treated repeatedly because of recurrent perianal ulcerations. An infection and a carcinoma could be excluded. The diagnosis of ergotamine induced ulcerations could be suspected only after a detailed work up of the patients past medical history and interview of family members. The ulcerations healed within a few months after broad excision and withdrawal of the medication. The second patient, a 51 year old woman complained of severe obstipation which occurred within a few months. The investigations showed a circular stenosis in the lower third of the rectum. The patient was treated successfully by bougienage under general anaesthesia. These case reports demonstrate the difficulties in diagnosis such lesions and emphasize the importance of a close medical follow-up when ergotamine suppositories are used for treatment of migraine. Whenever possible, a continuous treatment should be avoided.

Anal Canal↗
PubMed1994

[Ergotamine-induced rectal lesions in asymptomatic patients].

Suppositories containing ergotamine can cause anorectal lesions and even fistulae. We therefore carried out prospective investigations on 20 patients (17 female, 3 male) who had been prescribed ergotamine suppositories for migraine therapy. No serious ulceration was found. There was one case of reduced local blood circulation and three patients showed signs of increased blood circulation in the anterior rectal wall. In two further cases we found local hyperemia with minor bleeding. In our opinion anorectal ergotism is a possible, although rare consequence of ergotamine suppository abuse. For longterm treatment alternative routes of ergotamine administration or other groups of substances should therefore be used.

Adult↗
PubMedDate not supplied

Successful limb salvage with prostaglandin infusion: a review of ergotamine toxicity.

OBJECTIVE: A case of severe acute peripheral arterial insufficiency secondary to ergotamine toxicity treated successfully with intravenously administered prostaglandin is presented to highlight the features of this condition and to demonstrate the efficacy of treatment with prostaglandin infusion. CLINICAL FEATURES: A 35-year-old unemployed Caucasian woman with a background of polypharmacy abuse and recurrent migraines presented to St Vincent's Hospital Emergency Department with limb-threatening ischaemia of both legs secondary to chronic ergotamine overuse. INTERVENTION AND OUTCOME: A prostaglandin infusion was started and a dramatic and rapid improvement of her peripheral circulation occurred within six hours. CONCLUSION: Ergotamine toxicity is an uncommon but well documented cause of peripheral vascular insufficiency that should be recognised and treated aggressively because its sequelae can be disastrous. Intravenously administered prostaglandin proved to be successful in this case and is a logical choice as first-line therapy for ergotamine toxicity.

Adult↗
PubMed1981

Ocular ergotamine tartrate toxicity during treatment of Vacor-induced orthostatic hypotension.

A 20-year-old woman developed severe orthostatic hypotension after attempting suicide by ingesting the rodenticide, Vacor. Oral ergotamine tartrate, 6 mg a day, was useful in treating the orthostatic hypotension. However, a bilateral toxic retinal vasculopathy, consisting of a severe generalized vasoconstriction and mild macular edema, occurred within three weeks. Additional findings were an extinguished electroretinogram and a reduced dark-adaptation retinal sensitivity; because we performed these two tests after instituting ergotamine therapy we do not know whether to attribute their abnormal results to Vacor toxicity, ergotamine toxicity, or a combination of the two.

Adult↗
PubMed1985

Intramuscular ergotamine: plasma levels and dynamic activity.

Ergotamine tartrate (0.5 mg) was injected intramuscularly into 10 subjects with migraine. The effect on peripheral arteries, measured as a decrease in toe-arm systolic gradients, developed slowly and was well sustained after 29 hr. In contrast, ergotamine was quickly absorbed (t1/2 = 3 min) and plasma levels (measured by HPLC) declined, with a biologic t1/2 of 2.5 hr. A hypothetic effect compartment model was adopted and kinetic and dynamic data were simultaneously fitted on a computer. Calculated from mean data, the rate constant for equilibration of the drug between plasma and effector site was 0.07 hr-1, with a t1/2 of 9.9 hr, and the steady-state plasma concentration resulting in 50% of maximal effect (Cpss50) was 0.24 ng/ml. The largest variability for the estimated kinetic and dynamic parameters among subjects was found for Cpss50 (coefficient of variation = 110%), indicating that, in addition to some kinetic variability, dynamic variability (difference in sensitivity) should be anticipated in the therapeutic use of ergotamine.

Adult↗
PubMed1988

Placebo-controlled double-blind trial of pirprofen and an ergotamine tartrate compound in migraine attacks.

Sixty-one patients, 16 with classic and 45 with common migraine, were treated during three subsequent attacks with pirprofen, a new inhibitor of prostaglandin synthesis; an ergotamine tartrate compound; or placebo, in a randomized, double-blind multicentre study. Pain relief after a single dose and reduction of the attack intensity occurred most often with pirprofen in patients who needed more than one dose. Among them, however, the duration of attack was shortest with ergotamine. Working ability was well preserved with pirprofen, especially among patients with common migraine, and this treatment was ranked highest by the patients. However, no statistically significant differences were found between pirprofen and ergotamine. No serious side effects were observed with pirprofen. This study establishes the usefulness of pirprofen in the treatment of acute migraine.

Adolescent↗
PubMed1983

[Doppler ultrasound studies of the extracranial cerebral vessels in migraine patients after ergotamine tartrate administration].

Doppler ultrasound investigations were done in 20 patients with migraine during the symptom-free interval after oral administration of 2 mg and 6 mg ergotamine tartrate. The observed changes of end-diastolic flow velocity as a measure of peripheral total resistance permit simultaneous assessment of the vasoconstrictor effect of ergotamine in the perfusion area of the internal and external carotid arteries. A dosage of 2 mg led to an exclusive increase of resistance in the external carotid artery area without significant changes in the internal carotid area. A maximal therapeutic dosage of 6 mg ergotamine tartrate did not lead to a significant increase of the vasoconstrictor effect in the external carotid circulation. In addition, a barely registrable increase of resistance in the internal carotid area could now be observed.

Adult↗
PubMed1982

Local regulation of subcutaneous blood flow in normal subjects and in migraine patients before and after single-dose ergotamine tartrate.

Local blood flow regulation of the foot was studied in 15 normal subjects and in nine migraine patients. Changes in arterial and venous pressures were induced by lowering and elevation of the limb. Changes in blood flow were estimated from the changes in the wash-out rate of a subcutaneous 133-Xenon depot. The local vasoconstrictor response to increased venous pressure elicited during lowering was identical in the normal subjects and in the migraine patients. During elevation, however, an abnormality in the autoregulation of blood flow could be demonstrated, as a decrease in blood flow during elevation to +40 cm was more pronounced in the patients than in the normal subjects (P = 0.04). About 3 h after 0.5 mg ergotamine tartrate/70 kg body weight i.v. the local regulation of blood flow had markedly changed in normal subjects as well as in migraine patients. During elevation to +20 and to +40 cm, blood flow increased significantly (P = 0.01 and P = 0.02). In two subjects the isotope depot was infiltrated with lidocaine and the ergotamine-induced increase in blood flow during elevation was blocked. The results may indicate that the veno-receptor of the veno-arteriolar reflex underlying the local vasoconstrictor response is a tension receptor, which due to the veno-constrictor effect of ergotamine is triggered even at heart level.

Adult↗
PubMed1995

Teratogen update: ergot and ergotamine.

Ergotamine is a purified ergot alkaloid that has been suspected of being teratogenic. Animal data have shown effects mainly at doses toxic to the mother. Clinical reports in humans have been anecdotal, but in many the malformations are consistent with vascular injury. However, epidemiologic studies have not shown any clear increase in malformations among exposed infants. This may reflect the limited exposure and toxicity when used episodically. Ergot toxicity which can result in severe vasospasm does not spare the fetus or mother and ergotamine should not be considered without risk. Ergotamine should be avoided in pregnancy, and the counselling of the woman with an exposed fetus should focus on possible toxic exposure.

Abnormalities, Drug-Induced↗
PubMed1989

Ergotamine enhances acetylcholine-induced relaxation in various vascular segments of rabbits.

The vasodilator response to acetylcholine and-betanechol in segments of rabbit carotid, superior mesenteric and femoral arteries preconstricted with phenylephrine and with intact endothelium was enhanced when the vessels were preincubated with ergotamine but not with ergometrine for 60 min or longer. The vasodilator response to acetylcholine and its enhancement by ergotamine were completely prevented after methylene blue pretreatment or endothelium removal. These results were taken as evidence that the potentiation by ergotamine of the vasodilator response to acetylcholine is probably due to an increased production of EDRF from the vascular endothelium.

Acetylcholine↗
PubMed1976

Determination of the content and purity of ergotamine preparations by means of high-pressure liquid chromatography.

A reversed-phase system of high-pressure liquid chromatography with solvent gradient is described for testing the purity of ergotamine as an active substance and for checking its concentration in pharmaceutical preparations. Because of its good resolution, this system can be used not only for the selective assay of ergotamine but also for the identification and quantitative determination, in the same chromatogram, of seven known isomerization and hydrolysis breakdown products. Simultaneous detection at two different UV wavelengths also makes it possible to measure further breakdown products formed by addition at the 9,10 double bond (lumi-compounds). The advantages of the system lie in the determination of all of the products within ca. 20 min, direct injection of low-dosage injection solutions and sensitive detection of polar breakdown products. The system is reproducible with regard to retention times and quantitative determination. It is suitable as a quality-control method for the routine determination of the content and purity of ergotamine preparations.

Chromatography, High Pressure Liquid↗