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

The serotonin receptor agonist m-chlorophenylpiperazine (m-CPP) stimulates the release of cortisol and prolactin, and induces migraine-like headaches. We have studied the neuroendocrine and headache responses to m-CPP in 8 subjects with migraine and 10 normal subjects. Each subject underwent two challenge tests, one with 0.25 mg/kg PO of m-CPP and the other with placebo, administered in a double-blind crossover format. Serial measurements of serum cortisol, prolactin, and m-CPP levels were made at 30-min intervals for 210 min following ingestion of the medication. The incidence and severity of headache was assessed by a structured telephone interview after each test. We confirmed that m-CPP stimulates the release of cortisol and prolactin, and may induce headache, in both migraine subjects and normal controls. The cortisol response as well as ratings of headache severity and duration directly correlated with plasma levels of m-CPP. There were highly significant associations between the cortisol response and both headache severity and duration, independent of m-CPP plasma levels. We did not find statistically significant differences between the migraine and normal subjects in terms of their neuroendocrine or headache responses to m-CPP.
Cephalalgia 1993 Dec
PMID:Headache and cortisol responses to m-chlorophenylpiperazine are highly correlated. 831 48

Sumatriptan is a new serotonin receptor agonist that is useful in the treatment of migraine headache. More than 70 percent of patients with migraine headaches respond to subcutaneous sumatriptan within two hours, although headaches recur in up to two-thirds of initial responders. Side effects include lightheadness, a sensation of tingling or warmth, and breathlessness. Compared with the combination of ergotamine and caffeine, sumatriptan appears to work earlier and more completely but is associated with a higher rate of recurrent headache. Sumatriptan may be a useful additional therapy for migraine headache.
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PMID:Sumatriptan: a new serotonin agonist for the treatment of migraine headache. 838 4

Ondansetron hydrochloride is a new serotonin receptor antagonist that is effective in preventing emesis associated with cancer chemotherapy. The antiemetic effect appears to be exerted through a peripheral vagal blocking within the gastrointestinal tract, as well as an inhibitory effect within the chemoreceptor trigger zone (CTZ). Plasma concentrations of ondansetron peak 1 hour after an oral dose, and the tablet has an absolute bioavailability of 59%. Ondansetron undergoes extensive hepatic oxidative metabolism in the liver. The half-life of ondansetron is 3.5 hours in healthy volunteers; elderly patients have a slightly reduced clearance, and pediatric patients have increased clearance. Although less than 10% of ondansetron is recovered unchanged in the urine, most metabolites are eliminated by this route. The recommended dose of ondansetron is 0.15 mg/kg for three doses on the day of chemotherapy (30 minutes before chemotherapy and 4 and 8 hours afterward). An alternative regimen includes a single-day dose of 32 mg IV in adult patients before chemotherapy. The efficacy of ondansetron therapy for delayed emesis has not been determined. Ondansetron has proven to be appropriate as a single agent or as an addition to standard antiemetic therapy (ie, corticosteroids, benzodiazepines, neurotransmitter blockers) in preventing and treating acute chemotherapy-induced emesis (CIE). Initial results of clinical trials in prevention of radiotherapy-induced emesis and anesthesia-induced emesis appear positive. Ondansetron is well tolerated, with few adverse events (eg, headache, sedation).
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PMID:Ondansetron: a novel antiemetic agent. 848 93

Women with migraine often experience a worsening of symptoms at menopause. Use of exogenous estrogens is not helpful and may even exacerbate the condition. Although initial pharmacologic management generally is focused on control of individual headaches, attempts to stabilize the underlying migraine mechanism through serotonin receptor downregulation are likely to provide a better outcome.
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PMID:Approach to the patient with migraine. 859 22

Postoperative nausea and vomiting (PONV) are common side effects after surgery and have numerous patient factors and etiologies. Although self-limiting, PONV is not without risks and complications. In the past numerous antiemetics have been used successfully in the management of PONV; however, these drugs are associated with adverse effects. Ondansetron is a serotonin receptor antagonist that is effective in preventing and treating PONV. It is believed that ondansetron binds at the serotonin receptor both in the vagal afferents of the gastrointestinal tract and in the chemoreceptor trigger zone. The reported side effects from ondansetron are minor compared with those of the more commonly used antiemetics such as droperidol and metoclopramide and include headache, dizziness, musculoskeletal pain, drowsiness and sedation, and shivers.
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PMID:Ondansetron: perioperative use of a serotonin receptor antagonist for the prevention and treatment of nausea and vomiting. 863 70

Most current randomised controlled trials concern the acute treatment of migraine. Sumatriptan, a serotonin receptor agonist, was evaluated in 8 randomised controlled trials. Using a novel cartridge self-injector system subcutaneous sumatriptan was found superior to placebo, and oral sumatriptan in doses from 25 mg to 100 mg was found superior to placebo with no difference among doses. An oral dose of 100 mg sumatriptan was not superior to a combination of lysine acetylsalicylate plus metoclopramide, and 100 mg sumatriptan given 4 hrs after subcutaneous sumatriptan could not prevent recurrence of headache. Nasal dihydroergotamine was found to have some efficacy in acute migraine treatment, whereas nasal butorphanol, although effective in repeated doses, was hampered by many side effects. The prophylactic effect of valproate was confirmed in one randomised controlled trial.
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PMID:Drug treatment of migraine: acute treatment and migraine prophylaxis. 883 13

Serotonin syndrome, a condition with numerous clinical neurological manifestations, is the result of central serotonergic hyperstimulation. Features of the syndrome include mental status and behavioral changes (agitation, excitement, hypomania, obtundation), motor system involvement (myoclonus, hemiballismus, tremor, hyperreflexia, motor weakness, dysarthria, ataxia) and autonomic symptoms (fever, chills, diarrhea). Serotonin syndrome has been reported exclusively in patients on medications for psychiatric illness and Parkinsonism, despite the fact that the putative action of many antimigraine agents also involves the serotonin system. We herein report six patients with migraine who developed symptoms suggestive of the serotonin syndrome. Five were taking one or more serotomimetic agents for migraine prophylaxis (sertraline, paroxetine, lithium, imipramine, amitriptyline). In each case the symptoms and signs developed in close temporal proximity with use of a migraine abortive agent known to interact with serotonin receptors. In three instances the agent was subcutaneous sumatriptan and, in three, intravenous dihydroergotamine. In each instance the symptoms were transient and there was full recovery. With the ever increasing use of migraine medications active at serotonin receptor sites, cases of serotonin syndrome will likely occur more frequently. It is important that physicians treating migraine are aware of the serotonin syndrome and are able to recognize its varying presentations.
Cephalalgia 1996 Aug
PMID:Serotonin syndrome complicating migraine pharmacotherapy. 886 67

Analgesic abuse has recently been recognized as a cause of deterioration in primary headache patients. Although the pathogenesis of this headache transformation is still obscure, alteration of serotonin receptor function is one possible mechanism. To assess the plasticity of 5HT2 serotonin receptors in this condition, we investigated receptor binding by the platelet membrane in patients with analgesic-induced headache (AIH), migraine and non-headache controls. The technique involved radioligand binding with (phenyl-4-3H)spiperone and ketanserin. A greater density of receptor numbers (Bmax) was found in patients with AIH and in non-headache controls (96.47 +/- 10.21 and 92.01 +/- 13.15 fmol/mg protein), as compared to migraine patients (49.52 +/- 5.14 fmol/mg protein). The value of dissociation equilibrium constant (KD) remained unchanged (3.07 +/- 0.49, 2.24 +/- 0.24 and 2.91 +/- 0.42 nM for patients with AIH, migraine and non-headache controls, respectively). Based on these findings, we suggest that up-regulation of 5HT2 serotonin receptors may be a possible mechanism of headache transformation in patients with AIH.
Cephalalgia 1996 Oct
PMID:Serotonin receptor adaptation in patients with analgesic-induced headache. 906 19

The potent serotonin receptor (5-HT3) antagonists are new highly selective agents for the prevention and control of chemotherapy-induced nausea and vomiting that have been shown to be comparable to or more effective than traditional metoclopramide regimens. This study was designed to compare the antiemetic efficacy of dolasetron and metoclopramide in chemotherapy-naive and non-naive cancer patients receiving high-dose cisplatin-containing chemotherapy. This multicentre, double-blind, randomized trial compared the efficacy and safety of single i.v. doses of dolasetron mesilate salt (1.2 or 1.8 mg/kg) and metoclopramide (7 mg/kg) in 226 patients for the prevention of acute emesis and nausea associated with the administration of high-dose (> or = 80 mg/m2) cisplatin. Efficacy and safety were evaluated for 24 h. Complete responses were achieved by 57%, 48%, and 35% of patients given dolasetron mesilate 1.8 mg/kg (P = 0.0009 vs metoclopramide), dolasetron mesilate 1.2 mg/kg (P = 0.0058 vs metoclopramide), and metoclopramide, respectively. Overall, dolasetron was significantly more effective than metoclopramide for time to first emetic episode, nausea, patient satisfaction, and investigator global assessment of efficacy. Males, chemotherapy-naive patients, and alcoholics had higher response rates. Dolasetron was well tolerated, with mild-to-moderate headache most commonly reported. Twelve percent of patients receiving metoclopramide reported extrapyramidal symptoms compared with 0% of patients receiving dolasetron. In conclusion, dolasetron mesilate was effective for the prevention of CINV with high-dose cisplatin. Single i.v. doses of dolasetron mesilate were more effective than 7 mg/kg metoclopramide in preventing nausea and vomiting induced by highly emetogenic cisplatin-containing chemotherapy. In addition, 1.8 mg/kg dolasetron mesilate consistently produced the highest response rates and appears to be the most effective dose for further clinical development.
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PMID:A double-blind, multicentre comparison of intravenous dolasetron mesilate and metoclopramide in the prevention of nausea and vomiting in cancer patients receiving high-dose cisplatin chemotherapy. 901 Sep 86

Migraine is a paroxysmal disorder with attacks of headache, nausea, vomiting, photo- and phonophobia and malaise. Mild migraine attacks are treated with antiemetics followed by analgesics such as aspirin (acetylsalicylic acid), paracetamol (acetaminophen) or nonsteroidal anti-inflammatory drugs (NSAIDs). Moderate to severe attacks are treated by antiemetics combined with ergotamine or dihydroergotamine. Sumatriptan, a specific serotonin 5-HT1B/D receptor agonist, is used if attacks do not respond to ergotamine or if intolerable adverse effects occur. The new migraine drugs zolmitriptan, naratriptan, rizatriptan and eletriptan differ in their pharmacological profile from sumatriptan, but this translates into only minor differences in efficacy, headache recurrence and adverse effects. Migraine prophylaxis should be implemented when more than 3 attacks occur per month, if attacks do not respond to acute treatment or if the adverse effects of acute treatment are severe. Substances with proven efficacy include the beta-blockers metoprolol and propranolol and the calcium antagonist flunarizine. Drugs less effective or those with unpleasant adverse effects are the serotonin receptor antagonists (pizotifen, methysergide and lisuride), dihydroergotamine, cyclandelate, NSAIDs, valproic acid (sodium valproate) and amitriptyline. The efficacy of aspirin or magnesium is still under evaluation.
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PMID:A practical guide to the management and prevention of migraine. 982 55


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