Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0018681 (headache)
56,091 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Twenty-five migraine patients (9 males and 16 females) aged 22-71 who had used between 7 and 60 mg ergotamine tartrate per week for 1.5-30 y volunteered to participate in the study. Side-effects attributable to ergotamine were wide ranging and included daily headache and pain in the limbs. Wide variation in sensitivity to the drug was observed and side-effects were not always proportional to the dose of ergotamine. Random serum ergotamine concentrations were estimated in all patients and 10 of them volunteered to take a 2 mg oral challenge of ergotamine tartrate. Ergotamine was not detected in 44% of the random estimations even though all patients exhibited clinical signs of ergotamine tartrate overdose. The remaining 56% estimations all showed low drug concentrations. After the 2 mg oral challenge of ergotamine in the 10 patients, significantly higher concentrations, but still within therapeutic range, were detected in the sera when compared with mean concentrations achieved after the same oral dose of the drug in healthy, non-migrainous subjects.
...
PMID:Ergotamine toxicity and serum concentrations of ergotamine in migraine patients. 643 Jul 84

An attempt was made to determine the plasma ergotamine concentrations in nine male patients with cluster headache 15-600 min after oral therapeutic doses of ergotamine tartrate (Cafergot). Some of the patients were studied twice. Five patients received a constant dose of 2-4 mg daily for at least seven days. Four patients were given 1 mg five times on one day and three patients a single oral dose of 2 mg. Ergotamine was determined by means of high performance liquid chromatography with fluorescence detection--a new highly sensitive, specific method, the detection limit of which is less than 100 pg/ml for ergotamine. Ergotamine tartrate was not discovered in any of the plasma samples. In one patient ergotamine could not be detected in the cerebrospinal fluid one hour after a single oral dose of 2 mg. The oral biological availability is less than 1%, which is the maximal available fraction of unchanged ergotamine after oral administration. A clinical benefit was observed in several of our patients. These effects of the drug may be because of active metabolites being formed and/or to high affinity of ergotamine to cranial vessels.
Cephalalgia 1981 Dec
PMID:Low biological availability of ergotamine tartrate after oral dosing in cluster headache. 681 61

The vasoconstrictor activity of sumatriptan and ergotamine were compared by injecting these drugs in the hand vein of migraine subjects. We used the "venotest method", which permits the evaluation of the venoconstrictor effect of small doses of drugs, acting locally in the hand vein. Sumatriptan injected at increasing doses in the hand vein provoked contraction only at high doses (500 micrograms): venoconstriction lasted 5-15 minutes and was similar in intensity and duration to that induced by 0.5-1 micrograms of 5-hydroxytryptamine (5-HT). Likewise, ergotamine induced contraction only at a dose of 50 micrograms: this venoconstrictor effect was long lasting (at least 1 hour). Ergotamine-induced hand vein contraction, almost completely inhibited by ketanserin, seems mediated at least in part by 5-HT2 receptors, like the one induced by 5-HT and sumatriptan, already observed in a previous study. Clinical doses of ergotamine (0.25 mg intramuscular) and of sumatriptan (6 mg subcutaneous) do not provoke hand vein contraction for at least 1 hour: this could be due to a low activity of these drugs on the 5-HT2 vein receptors or a technique that is unsuitable to detect the vasoconstrictor effect of drugs given by the systemic route. The long lasting venoconstrictor effect of ergotamine may be due to a slow dissociation from receptor sites. The short vasoconstriction induced by sumatriptan could account for the recurrence of headache in many sumatriptan-treated migraine subjects.
Headache 1994 Apr
PMID:Comparison between venoconstrictor effects of sumatriptan and ergotamine in migraine patients. 801 33

Drug therapy is only one possibility to treat headache or migraine. In a migraine attack aspirin, acetaminophen, non-steroidal antiinflammatory drugs like ibuprofen, naproxen and mefenamic acid are used. Further more weak opiates, caffeine, metoclopramide and the new 5-HT1-receptor agonist sumatriptan are effective in the attack. Ergotamine and dihydroergotamine are probably the most effective though their side effects are troublesome. For prophylactic treatment, the beta-adrenergic receptor blockers propranolol, metoprolol and atenolol are the drugs of first choice. Also calcium channel antagonists like flunaricine and antidepressant drugs like amitryptiline and doxepine are used.
...
PMID:[Pharmacotherapy of headache with special reference to migraine]. 805 12

The responses in cervicogenic headache to four different agents have been studied. Nitroglycerin was given sublingually to 27 patients. Eighteen patients got more than 20% increase of their headache. Of those with any headache increase at all, 12 got bilateral and 12 unilateral pain. The typical late cluster headache response to nitroglycerin was not seen in cervicogenic headache. The provocative effect of nitroglycerin seemed less marked in cervicogenic than in cluster headache. Oxygen inhalation, a frequently used treatment for cluster headache, was given to 14 patients with cervicogenic headache. In general, the effect seemed uncertain and probably clearly inferior to the effect in cluster headache. Ergotamine treatment (given to 13 patients) also seemed to be of little avail in cervicogenic headache. Morphine injections given to 11 cervicogenic headache patients resulted in "marked" improvement in 4, but complete pain freedom was only seen in 2 cases. In our opinion, the present results add further evidence to the view that different etiologic and pathogenetic factors underlie cervicogenic headache and cluster headache.
Headache 1993 May
PMID:Cervicogenic headache: responses to nitroglycerin, oxygen, ergotamine and morphine. 832 Jan

Ergotamine and analgesic misuse are now recognized as causes of chronic daily headache and the condition responds well to drug withdrawal with reduced headache frequency. In this study, we have investigated whether medication misuse is associated with an alteration in membrane transduction which is sensitive to drug withdrawal. This was carried out by assay of the thrombin-stimulated generation of inositol phosphates in platelets from 12 migraine patients with chronic daily headache and analgesic misuse, 7 migraine patients with chronic daily headache and ergotamine misuse and 7 control subjects. After drug withdrawal, a significant decrease in headache frequency was seen at one month in both patient groups. Withdrawal of analgesics produced a significant decrease in thrombin-stimulated inositol phosphate production at one month; this was further decreased a month later with a reduction in Bmax of 60% and no significant change in KD. A similar pattern was obtained in ergot misuse patients, with the KD value decreasing by 56% one month after drug withdrawal. These results provide evidence of an adaptation in transduction with misuse of analgesics and ergotamine which correlates with headache frequency.
Cephalalgia 1993 Aug
PMID:Cellular adaptation in migraineurs with chronic daily headache. 839 71

Ergotamine has been used for many years in the treatment of migraine, although there is little formal clinical evidence that it is significantly more efficacious than placebo. A number of side effects associated with ergotamine have been reported in the literature, including myocardial infarction, ischaemia of limb extremities, and fibrotic changes. Long-term use has led to reported cases of ergotamine-induced headache, vascular reactivity, and subclinical ergotism. When the safety profile of this drug is considered, coupled with its debatable efficacy from a clinical review previously published, the resulting poor risk:benefit ratio brings into question the continued use of ergotamine as a migraine treatment and calls for better controlled trials of its efficacy, or lack of, in the acute treatment of migraine.
Cephalalgia 1996 Feb
PMID:Side effects of ergotamine. 882 93

Members of the new class of antimigraine compounds, 5HT1B/1D agonists, as well as ergotamine, may cause vasoconstriction through stimulation of 5HT receptors on peripheral vessels. The cardiovascular effects of 20 mg oral zolmitriptan (Zomig, formerly 311C90), 2 mg oral ergotamine and the combination were assessed in a randomized double-blind, placebo-controlled crossover study in 12 healthy subjects. Pharmacodynamic measures included oscillometric blood pressure, systolic blood pressure at the toe and arm using a strain gauge technique, stroke volume and cardiac output using bioimpedance cardiography, high-resolution ultrasound to measure brachial arterial diameter and a novel Doppler method to measure blood flow velocity. Both drugs produced small degrees of peripheral vasoconstriction, including increases in diastolic blood pressure and blood flow velocity and decreases in arterial diameter and toe-arm systolic pressure gradient. These effects were generally additive with the combination but of no clinical importance. There were no significant changes in cardiac output, stroke volume heart rate or ECG. Zolmitriptan, at eight times the likely therapeutic dose, was generally well tolerated both alone and in combination with ergotamine. Ergotamine had no clinically important effects on zolmitriptan pharmacokinetics.
Cephalalgia 1997 Oct
PMID:Peripheral vascular effects and pharmacokinetics of the antimigraine compound, zolmitriptan, in combination with oral ergotamine in healthy volunteers. 935 Mar 83

The effect of the migraine drugs ergotamine and sumatriptan on the cerebral blood flow (CBF) autoregulation was studied in halothane/nitrous oxide-anesthetized normotensive Wistar Kyoto rats. Ergotamine, an ergot alkaloid affecting 5HT, norepinephrine, and dopamine receptors, was administered intravenously as a single dose of 25 microg/kg. Sumatriptan, a selective 5HT1-like receptor agonist, was administered by intravenous infusion of 300 microg/kg/h. CBF was measured with the intracarotid 133Xe-injection method. The blood pressure limits of CBF autoregulation were determined by computerized least sum of square analysis. CBF autoregulation was preserved after both ergotamine and sumatriptan. Ergotamine shifted the lower blood pressure limit of CBF autoregulation towards higher blood pressures from 60 +/- 3 mmHg to 82 +/- 4 mmHg (p<0.01), but did not significantly affect the upper blood pressure limit of CBF autoregulation. Sumatriptan had no significant effects on the blood pressure limits of CBF autoregulation.
Cephalalgia
PMID:Differential effects of migraine drugs on cerebral blood flow autoregulation. 973 33

Vasoconstrictive agents have been widely used in the treatment of migraine. These types of drugs have various side effects and are not suitable for many patients. Due to nausea or vomiting, nonoral treatment is often required, but only a few nonvasoconstrictive drugs exist in a parenteral form and are suitable for the treatment of acute migraine in the emergency setting. In a randomized, double-blind, crossover trial we evaluated the efficacy of 1,000 mg lysine-acetylsalicylic acid i.v. (LAS) compared to 0.5 mg ergotamine s.c. in 56 patients (112 attacks) with acute migraine. To gain further insight into the possible role of vasoconstriction, blood flow velocities (BFV) were measured in intra- and extracranial arteries using duplex sonography and transcranial Doppler sonography. Both agents were equally potent in relieving headache. Intravenous LAS resulted in a significantly faster relief and had fewer side effects. LAS had no effect on BFV. Ergotamine increased BFV in the middle cerebral artery only. No correlation was found between changes in BFV and the relief of headache. This is the first trial to compare the intravenous formulation of LAS in the treatment of migraine with another antimigraine medication and suggests that it is an effective and safe drug for the parenteral treatment of acute migraine attacks.
...
PMID:Lysine-acetylsalicylic acid in acute migraine attacks. 1002 11


<< Previous 1 2 3 4 Next >>