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PubMed1999

Differential sensitivity of 5-HT1B auto and heteroreceptors.

The effect of the native and rodent-selective 5-HT1B receptor agonists (5-hydroxytryptamine (5-HT) and CP93,129) on the K+-evoked overflows of [3H]5-HT, [3H]dopamine (DA) and [3H]acetylcholine (ACh) was studied in synaptosome preparations obtained from rat brain striatum or hippocampus loaded with radiolabeled neurotransmitter. The aim of the study was to compare the different potencies of the specific 5-HT1B receptor agonists to stimulate the auto and heteroreceptors and to modulate the different neurotransmitter release. Results show that under the same experimental conditions, 5-HT and CP93,129 exhibited significantly higher potencies in inhibiting the K+-evoked overflow of [3H]5-HT from synaptosomes of rat striatum (IC50=2.0+/-1.8 nM and 20.5+/-3.1 nM, respectively) than in inhibiting the K+-evoked overflow of [3H]DA from synaptosomes of the same cerebral region (IC50= 0.8+/-0.2 microM and 1.8+/-0.4 microM, respectively), or [3H]ACh from synaptosomes of hippocampus (IC50=1.7+/-0.8 microM for CP93,129). The inhibitory effects of the 5-HT1B receptor agonists on [3H] K+-overflows were antagonized by the selective 5-HT1B receptor antagonist (SB224289), further indicating that the observed effects were 5-HT1B receptor specific. Sumatriptan, a selective r5-HT1D receptor agonist, did not show any significant effect on the K+-overflow of [3H]5-HT in the range of concentrations (10(-10) to 10(-6) M), and did not affect the K+ overflow of [3H]DA or [3H]ACh at concentrations (10(-9) to 10(-4) M), which exclude the involvement of 5-HT1D receptors. These inhibitory effects of the 5-HT1B receptor agonists were highly attenuated by pertussis toxin in the three systems studied, suggesting the involvement of Gi/Go-proteins in the transduction mechanism pathway of the receptor generated signal. In conclusion, these results suggest that 5-HT1B heteroreceptors located on dopaminergic and cholinergic terminals exhibit a lower sensitivity to 5-HT1B receptor agonist and antagonist than do 5-HT1B autoreceptors. The observed difference in functional sensitivities of 5-HT1B auto- and heteroreceptors may represent important consequences in the physiological control of the release of serotonin versus that of other neurotransmitters.

Acetylcholine↗
PubMed2003

Absolute contraindications in relation to potential drug interactions in outpatient prescriptions: analysis of the first five million prescriptions in 1999.

OBJECTIVES: Adverse drug interactions increase morbidity and mortality. To prevent these, situations leading to adverse prescriptions must be clarified. This study quantifies and analyses prescriptions with potential adverse drug interactions in primary health care in the north of France over a 3-month period. METHODS: All prescriptions administered between 1 January and 31 March 1999 were analysed to identify potential interactions amongst drugs appearing on the same prescription sheet. The regional French healthcare database was compiled to further classify contra-indications. RESULTS: There were 5,358,374 prescriptions administered to 44% of the overall population of the Nord-Pas de Calais area (1,754,372 patients/3,990,167 general population). There were 14,390 prescriptions classified as either absolute (26%) or relative contraindications (74%). Nine drug categories accounted for most of the absolute contraindications: dopaminergic antiparkinsonians, neuroleptic agents, migraine treatments (such as ergot alkaloids, sumatriptan and other triptan derivatives), prokinetic drugs (cisapride), antibacterial drugs (macrolides), antifungals (imidazoles), antiarrhythmics, betablockers and analgesics (opioids and floctafenine). In 54% of patients exposed, the incurred risk was either QT prolongation/Torsade de Pointes or antagonism of dopaminergic antiparkinson agents with dopamine receptor antagonists prescribed as antipsychotic agents. CONCLUSIONS: Among a non-selected population of ambulatory outpatients, the number of quarterly prescriptions with contra-indications with potentially harmful drug interaction was 27 in 10,000 prescriptions. This would extrapolate to nearly 200,000 contra-indications on the same-prescription sheets in France in the first quarter of 1999.

Contraindications↗
PubMed2003

Absolute contraindications in relation to potential drug interactions in outpatient prescriptions: analysis of the first five million prescriptions in 1999.

OBJECTIVES: Adverse drug interactions increase morbidity and mortality. To prevent these, situations leading to adverse prescriptions must be clarified. This study quantifies and analyses prescriptions with potential adverse drug interactions in primary health care in the North of France over a 3-month period. METHODS: All prescriptions administered between 1 January 1999 and 31 March 1999 were analysed to identify potential interactions amongst drugs appearing on the same prescription sheet. The regional French healthcare database was compiled to further classify contraindications. RESULTS: There were 5,358,374 prescriptions administered to 44% of the overall population of the Nord-Pas de Calais area (1,754,372 patients per 3,990,167 general population). There were 14,390 prescriptions classified as either absolute (26%) or relative contraindications (74%). Nine drug categories accounted for most of the absolute contraindications: dopaminergic antiparkinsonians, neuroleptic agents, migraine treatments (such as ergot alkaloids, sumatriptan and other triptan derivatives), prokinetic drugs (cisapride), antibacterial drugs (macrolides), antifungals (imidazoles), antiarrhythmics, beta-blockers and analgesics (opioids and floctafenine). In 54% of patients exposed, the incurred risk was either QT prolongation/Torsade de Pointes or antagonism of dopaminergic antiparkinson agents with dopamine receptor antagonists prescribed as antipsychotic agents. CONCLUSIONS: Among a non-selected population of ambulatory outpatients, the number of quarterly prescriptions with contraindications with potentially harmful drug interactions is 27 in 10,000 prescriptions. This would extrapolate to nearly 200,000 contraindications on same-prescription sheets in France in the first quarter of 1999.

Adolescent↗
PubMed1999

Antimigraine drugs.

Migraine is a paroxysmal disorder characterized by attacks of headache, nausea, vomiting, photophobia, phonophobia, and malaise. This review summarizes new treatment options for therapy of the acute attack. Mild or moderate migraine attacks are treated with antiemetics followed by analgesics such as aspirin, paracetamol, nonsteroidal anti-inflammatory drugs, or antiemetics combined with ergotamine or dihydroergotamine. Sumatriptan, a specific serotonin (5-HT)1B/D agonist is used when attacks do not respond to ergotamine, or when intolerable side effects occur. The new migraine drugs zolmitriptan, naratriptan, rizatriptan, and eletriptan differ slightly in their pharmacological profiles, which translates into minor differences in efficacy, headache recurrence, and side effects. New drugs in migraine prophylaxis include cyclandelate, valproic acid and magnesium.

Analgesics↗
PubMed1999

A retrospective long-term analysis of the epidemiology and features of drug-induced headache.

Drug-induced headache is well known to result from the abuse of compounds taken for the treatment of primary headache. The features of drug-induced headache depend on various features including the availability of drugs, the regional health system, and psychogenic factors of the patients. We performed a retrospective study on a series of 257 consecutive German patients presenting with drug-induced headache during the period 1983-1996. Our aim study was to evaluate the demographic features, the frequency of various drugs used, in particular of ergotamine derivates, and changes in these features during the study period. The frequency of drug-induced headache among all headache patients was 8%, with a female preponderance of 81%. Drug-induced headache occurred in all age groups, predominantly in migraine patients (35%). The mean number of substances used was 2.7, mainly, acetaminophen (47.9%), ergotamine tartrate (45%), and combined analgesics (56%). We did not find a significant difference between the associations with ergotamine tartrate and dihydroergotamine, although the latter was taken less frequently. Comparing the early and late years of our study period, there were no changes in the frequency of drug-induced headache (8% versus 7%), although changes in the frequency of some drugs changed (barbiturates, ergotamine tartrate, and codeine intake decreased whereas nonsteroidal anti-inflationary drugs, combined analgesics, and sumatriptan intake increased). Our data suggest that changes in drug availability and the introduction of classification criteria and treatment recommendations did not have a major impact on the frequency of drug-induced headache.

Adult↗
PubMed2000

Placebo effect in the acute treatment of migraine: subcutaneous placebos are better than oral placebos.

We carried out a meta-analysis of 22 trials to determine the comparative placebo effect of (a) subcutaneous vs. oral and (b) in-hospital vs. at-home administration in the treatment of migraine. The headache relief rates were combined from the placebo arms of these randomised clinical trials assessing the value of sumatriptan in acute treatment of migraine. The main outcome measure was the proportion of patients reclassified from severe or moderate headache severity to no or mild headache severity 2 h after the beginning of treatment. In the oral regimen 222 of 865 patients (25.7%) reported no or mild headache severity after 2 h, compared to 279 of 862 patients (32.4%) of those receiving subcutaneous placebo (6.7% difference; 95% CI 2.4-11.0%). Adjusting for treatment setting and severity of headache at baseline did not change the observed difference. After placebo treatment at home 285 of 1,054 patients (27.0%) reported no or mild headache severity after 2 h, compared to 216 of 673 patients (32.1%) among those receiving placebo in hospital (5.1 % difference; 95% CI 0.6-9.5%). When adjusted for route of administration and severity of headache at baseline, the difference in relief rates between home and hospital setting disappeared. These findings indicate that subcutaneous administration enhances the placebo effect of acute treatment of migraine. Future trials of antimigraine drugs assessing the relative efficacy of various routes of administration should use a double-dummy technique. The interpreting of placebo-controlled trial results must therefore consider that the effect in the drug arm of the trial depends in part on the route of administration.

Administration, Oral↗
PubMed2004

[Difficult decisions: headache treatment in pregnancy and childhood].

In pregnancy and in childhood, headache and migraine are challenging therapeutic problems.However, this review aims to give treatment recommendations for drug and non-drug therapy in both patient groups which are based on scientific evidence. Pregnant women often lose their migraine attacks which reappear during lactation. During pregnancy acute headache can be treated with paracetamol, in the middle trimenon also ASA and ibuprofen are allowed. Triptans for the acute treatment of migraine are contraindicated. As prophylactic agents, only metoprolol, fluoxetine, and magnesium are possible. In childhood, drug of first choice for acute headache treatment is ibuprofen. Migraine can also be treated by sumatriptan nasal spray. In migraine prophylaxis, flunarizine is drug of first choice, no prophylactic drugs are evaluated for tension-type headache in childhood. The problems of specific contraindications and of the off-label use of drugs in this particular life periods are discussed.

Child↗
PubMed2006

[Prophylactic measures and acute treatment of migraine].

The treatment of migraine consists of the acute treatment of the migraine attack and prophylactic measures for either pharmacological or non-pharmacological management. Since the retreat of the ergotamines one can only choose between one of the well-established analgesics and one of seven triptans for the treatment of the migraine attack. Although neither a new triptan nor an innovative new application form has been introduced, the year 2006 will be remembered as the year when the first triptan (naratriptan) was released as a prescription-free over-the-counter drug and when the first sumatriptan generics were marketed in Germany. In addition to the beta-blockers metoprolol and propranolol and the calcium antagonist flunarizine two antiepileptic drugs, topiramate and valproic acid, have been rated as first-line prophylactic drugs in Germany. Due to an extensive and successful study program topiramate has been officially approved in Germany.

Anticonvulsants↗
PubMed1996

[Animal models and their results in relation to the therapy of migraine].

Until now, our understanding of migraine pathophysiology has been fairly incomplete. So far no animal model has allowed an explanation of all facets of the clinically heterogeneous condition migraine. However, it is now generally accepted that the migraine headache is due to activation of the trigeminal system. The model of neurogenic inflammation after stimulation of the trigeminal ganglion or systemic administration of capsaicin allows study of the inhibitory interactions between antimigraine compounds and peripheral trigeminal fibre terminals that sustain a sterile meningeal inflammation through release of allogenic and vasoactive neuropeptides, such as substance P and calcitonin gene-related peptide. Studies with the model of superior sagittal sinus stimulation have revealed central actions of antimigraine agents such as ergotamine and sumatriptan, but also acetylsalicylic acid on neurotransmission of trigeminal nociceptive input in the brainstem. A likely explanation for the slowly progressing neurological deficits is cortical spreading depression (CSD), which can easily be elicited in many species. However, CSD has not been observed in vivo in humans. The described models strongly influenced the development of new medications for migraine treatment and have improved our understanding of migraine pathophysiology.

English Abstract↗
PubMed1996

[Medical therapy for menstrual migraine].

A menstrual migraine occurs in approximately 7-10 % of women suffering from migraine. The migraine occurs from 2 days before until 3 days after the end of the menstrual period. The choice of treatment depends on the duration of the attack, which ranges from 3 to 7 days. An attack of up to 3 days duration should be treated with acetylsalicylic acid, ergotamine tartrate or naproxen, each in combination with an antiemetic (domperidone, metoclopramide). If there is no response, sumatriptan can be administered orally (25-100 mg) or subcutaneously (6 mg). In the attacks continue for more than 3 days, short-term prophylaxis with naproxen or the application of an estrogen-containing patch is indicated. Neither ovulation inhibitors nor traditional migraine prophylaxis has an influence on menstrual migraine. Patients should keep a headache diary. Short-term prophylaxis with ergotamine tartrate or tamoxifen is obsolete.

English Abstract↗
PubMed2006

Early satiety in cancer patients: a common and important but underrecognized symptom.

INTRODUCTION: The severity of anorexia correlates with the presence of early satiety. The sense of fullness limits nutritional intake. The symptom is poorly understood because most assessment questionnaires do not include early satiety. METHODS: Patients rarely volunteer early satiety. Central and peripheral mechanisms may be involved in the genesis of early satiety. These would include central sensory specific satiety, food aversions, diurnal changes in intake, gastric motility and accommodation and as gastrointestinal hormones. CONCLUSIONS: Prokinetic medications, such as metoclopramide are used to treat early satiety. However, other medications which influence gastric accommodation such as clonidine, sumatriptan, or sildenafil, or diminish enteric afferent output such as kappa opioid receptor agonists, may favorably influence early satiety and should be subject to future research. Translational research is needed to understand the relationship of early satiety to gastric motility and accommodation.

Anorexia↗
PubMed2005

Patients' preference for triptans and other medications as a tool for assessing the efficacy of acute treatments for migraine.

Oral triptans are effective and well tolerated acute treatments for migraine, but clinical differences between them are small and difficult to measure in conventional clinical trials. Patient preference assesses a global measure of efficacy and tolerability, and may be a more sensitive means of distinguishing between these drugs. In a series of studies, patients consistently expressed a clear preference for triptans over their usual non-triptan acute medications, e.g., analgesics and ergotamine. Direct comparator studies of patient preference with oral triptans showed that patients could distinguish between different triptans, and between different formulations of the same triptan. Patients could even distinguish between the three oral doses of sumatriptan. The most frequently provided reasons for preference were speed of response and overall effectiveness. Patient preference is a sensitive clinical trial endpoint and physicians should consider using it when reviewing the efficacy of acute migraine medications.

Administration, Oral↗
PubMed2001

Pathophysiology of primary headaches.

The cerebral circulation is innervated by sympathetic, parasympathetic, and sensory nerves, which store a considerable number of neurotransmitters. The role of these has been evaluated in primary headaches. A clear association between head pain and the release of calcitonin gene-related peptide was demonstrated. In cluster headache and in a case of chronic paroxysmal headache there was in addition the release of vasoactive intestinal peptide, which was associated with the facial symptoms (nasal congestion, rhinorrhea). In parallel with sumatriptan treatment, head pain subsided and neuropeptide release normalized. These data show the involvement of sensory and parasympathetic mechanisms in the pathophysiology of primary headaches.

Blood Vessels↗
PubMed2001

Treatment and management of cluster headache.

Cluster headache is an uncommon yet well-defined neurovascular syndrome occurring in both episodic and chronic varieties. The most striking feature of cluster headache is the unmistakable circadian and circannual periodicity. Inheritance may play a role in some families. The attacks are of extreme intensity, of short duration, occur unilaterally, and are accompanied by signs and symptoms of autonomic dysfunction. In contrast to migraine, during an attack the cluster patient prefers to pace about. Attacks frequently occur at night. Although the pathophysiology of cluster headache remains to be fully elucidated, several seminal observations have recently been made. The medical treatment of cluster headache includes both acute therapy aimed at aborting individual attacks and prophylactic therapy aimed at preventing recurrent attacks during the cluster period. Agents used for acute therapy include inhalation of oxygen, sumatriptan, and dihydroergotamine. Transitional prophylaxis involves the short-term use of either corticosteroids or ergotamine derivatives. The cornerstone of maintenance prophylaxis is verapamil, yet methysergide, lithium, and divalproex sodium may also be employed. In some patients, melatonin or topiramate may be useful adjunctive therapies.

Cluster Headache↗
PubMed2002

Cluster headache: the challenge of clinical trials.

The design and execution of clinical trials poses special problems for cluster headache. Although there is less inter-individual and intra-individual variability of attacks than seen with migraine, the brevity of attacks, spontaneous remissions unrelated to treatment, and the relative rarity of cluster headaches challenge investigators. The International Headache Society has developed guidelines that represent a compromise between scientific rigor and practicality. Only injectable sumatriptan for acute attacks and verapamil for prophylaxis have demonstrated a robust therapeutic effect in controlled clinical trials.

Clinical Protocols↗
PubMed2002

Antiepileptic Drug Therapy in Migraine Headache.

Severe migraine affects more than 28 million Americans. It is associated with episodic as well as long-term disability and suffering, yet it is underdiagnosed and undertreated. Acute treatments have advanced considerably, ignited by sumatriptan and the subsequent triptans; unfortunately migraine prevention has lagged far behind. There are no great migraine preventives! No migraine preventive agent studied in good randomized, double blind, placebo-controlled trials proved to be 50% better than placebo. Migraine trials typically focus on episodic migraine, a milder, gentler type of migraine that is selected for low frequency, lack of daily headaches, no preventive need, and previous failure to no more than a few preventive agents. These features are not typical of the usual migraine patient seen in most neurologic practices, thus the results of clinical trials may not carryover to real world situations. Treatment of frequent, chronic, or pervasive migraine is inadequate, and never has been studied in randomized controlled trials. Traditional migraine preventives, eg, beta-blockers, calcium channel blockers, and tricyclic antidepressants, are often ineffective in difficult or complicated populations. The antiepileptic drugs represent a category of pharmaceutics that target the neuronal instability and central hyperexcitability of migraine, and, through these actions, may be more effective than traditional preventives. Episodic migraine attacks are associated with peripheral and central sensitization; however, if attacks are frequent, severe, or long lasting, this sensitization may increase the risk of developing daily headaches. If antiepileptic drugs have an effect on central sensitization, perhaps mediated via glutamate inhibition or gamma-aminobutyric acid potentiation, it is appropriate to use these agents early in migraine treatment, particularly in the highly comorbid patient, possibly in conjunction with agents that antagonize the 5HT2 receptor. This report reviews the best currently available evidence on antiepileptic drugs in the prevention of episodic migraine, and tabulates potential drug-drug and cytochrome P450 interactions. All antiepileptic drugs presented are effective in migraine prevention. However, deciding on the best agent for each individual patient will require recognizing comorbidity and assessing antiepileptic drug pharmacodynamics, tolerability, and safety.

Journal Article↗
PubMed2003

Cluster Headache and Cluster Variants.

Patients must be cognizant of the time course of the cluster headache periods to optimally tailor their therapy. Steroids provide the fastest onset of prophylactic effect. Once steroids are initiated, it remains difficult to wean patients off of them, and that is why it is always recommended to associate another prophylactic agent from the onset with the steroids. All triptans can be considered; however, only injectable sumatriptan and zolmitriptan have been the subject of controlled studies, and the former remains the gold standard because of its speed of action. Lithium, although not a first-line therapy, remains mainly efficacious for the chronic form of cluster headache. There does not seem a significant tendency for analgesic rebound-withdrawal headache with cluster headache compared with migraine. Scientific studies of the treatment of cluster headache are inherently difficult because of the rarity of the syndrome, the short duration of attacks, and the relatively short duration of the cluster period, along with the presence of spontaneous remissions. Moreover, still a significant proportion of the available evidence on this subject is uncontrolled. Active, rather than placebo, control individuals are recommended. As far as surgical procedures are concerned, although only recently introduced and less documented, gamma-knife radiosurgery should be preferred to the procedures associated with craniotomy, which are inherently associated with a higher complication potential risk.

Journal Article↗
PubMed1993

Activity of serotonin (5-HT) receptor agonists, partial agonists and antagonists at cloned human 5-HT1A receptors that are negatively coupled to adenylate cyclase in permanently transfected HeLa cells.

The activity of serotonin (5-HT) receptor agonists, partial agonists and antagonists, and various other neurotransmitter receptor antagonists at human 5-HT1A receptors that are negatively coupled to adenylate cyclase in permanently transfected HeLa cells was investigated. 5-HT1A receptor-mediated inhibition of adenylate cyclase was studied by measuring inhibition of cAMP accumulation, induced by forskolin. At 100 microM forskolin produced a 100-fold increase in cAMP formation: 5-HT concentration dependently inhibited the cAMP formation; maximal inhibition was attained at 1 microM 5-HT and represented 90% of the stimulated cAMP formation. Full inhibition was observed with 5-HT1A receptor agonists: N,N-dipropyl-8-hydroxy-2-aminotetralin (8-OH-DPAT) and flesinoxan, and non-selective 5-HT receptor agonists: d-lysergic acid diethylamide (d-LSD), RU 24,969, bufotenine, methysergide and tryptamine. The rank order of potency of the compounds for inhibiting the cAMP formation corresponded to the rank order of the binding affinities of the drugs for the 5-HT1A receptor. Partial inhibition was obtained with submicromolar concentrations of buspirone, spiroxatrine and ipsapirone. A slight inhibition was observed with 1 microM 5-HT receptor agonist CP 93129 and 1 microM 5-HT receptor antagonists mesulergine and BW-501. No inhibition was found with: the 5-HT receptor agonists quipazine, sumatriptan and 1-(2,5-dimethoxy-4-methylphenyl)-2- aminopropane (DOM); the 5-HT receptor antagonist ICS-205,930; and other neurotransmitter receptor antagonists such as pindolol, CGP 20712-A, prazosin, sulpiride and pyrilamine. Spiperone and pindolol fully antagonized the agonist-mediated inhibition of forskolin-stimulated cAMP formation. Partial inhibition of the agonist-mediated inhibition of forskolin-stimulated cAMP formation was apparent with 1 microM ocaperidone and 1 microM ipsapirone. It can be concluded that HeLa cells, permanently expressing human 5-HT1A receptors, are a valid cellular system for studying the negative coupling of 5-HT1A receptors to adenylate cyclase and the action of compounds thereupon.

8-Hydroxy-2-(di-n-propylamino)tetralin↗