flunarizine

Summary

Summary: Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. It is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy.

Top Publications

  1. Leone M, Grazzi L, La Mantia L, Bussone G. Flunarizine in migraine: a minireview. Headache. 1991;31:388-91 pubmed
    b>Flunarizine is a non-selective calcium antagonist. It distributes preferentially in the adipose tissue and passes the blood brain barrier...
  2. Lin Z, Musiano D, Abbot A, Shum L. In vitro plasma protein binding determination of flunarizine using equilibrium dialysis and liquid chromatography-tandem mass spectrometry. J Pharm Biomed Anal. 2005;37:757-62 pubmed
    A highly sensitive method was developed and validated for determining the free fraction of flunarizine in human plasma...
  3. Sørensen P, Larsen B, Rasmussen M, Kinge E, Iversen H, Alslev T, et al. Flunarizine versus metoprolol in migraine prophylaxis: a double-blind, randomized parallel group study of efficacy and tolerability. Headache. 1991;31:650-7 pubmed
    The prophylactic effect of flunarizine and metoprolol was studied in a multi-center randomized, double-blind trial of 149 patients with migraine with or without aura...
  4. Campana G, Bucolo C, Murari G, Spampinato S. Ocular hypotensive action of topical flunarizine in the rabbit: role of sigma 1 recognition sites. J Pharmacol Exp Ther. 2002;303:1086-94 pubmed
    ..In the present study, flunarizine, a calcium channel blocker with a complex pharmacological profile, bound to sigma1 sites expressed in the iris-..
  5. Ayoub A, Aumann D, Hörschelmann A, Kouchekmanesch A, Paul P, Born J, et al. Differential effects on fast and slow spindle activity, and the sleep slow oscillation in humans with carbamazepine and flunarizine to antagonize voltage-dependent Na+ and Ca2+ channel activity. Sleep. 2013;36:905-11 pubmed publisher
    ..oscillation, with Ca2+ and Na+ conductances playing crucial roles, we employed the actions of carbamazepine and flunarizine to reduce the efficacy of Na+ and Ca2+ channels, respectively, for probing in healthy human subjects mechanisms ..
  6. Subramanyam K, David J, Joseph T. Interaction of flunarizine with sodium valproate or ethosuximide in gamahydroxybutyrate induced absence seizures in rats. Indian J Exp Biol. 2001;39:998-1001 pubmed
    Sodium valproate(VPA), ethosuximide(ESM), 200 mg/kg ip and flunarizine (FLU) 5 or 10 mg/kg ip were first administered independently to rats in order to study their effects on behavioural and EEG aspects of spike and wave discharges (SWDs)..
  7. Boccia G, Del Giudice E, Crisanti A, Strisciuglio C, Romano A, Staiano A. Functional gastrointestinal disorders in migrainous children: efficacy of flunarizine. Cephalalgia. 2006;26:1214-9 pubmed
    ..of functional gastrointestinal disorders (FGIDs) in children with migraine headache and the effects of flunarizine on gastrointestinal manifestations. We studied 50 migrainous children (mean age 8.63 years)...
  8. Jaishree J, Kumaresan S, Sudha S, David J, Kulkarni C. Individual and combined effects of N6-cyclopentyladenosine, flunarizine and diazepam on aminophylline-induced recurrent generalized seizures in mice. Pol J Pharmacol. 2003;55:559-64 pubmed
    Protective effects of anticovulsant agents, N6-cyclopentyladenosine (CPA) and flunarizine (FLN) against aminophylline (AMPH) (280 mg/kg)-induced convulsions were tested in different groups of mice...
  9. Allais G, De Lorenzo C, Quirico P, Airola G, Tolardo G, Mana O, et al. Acupuncture in the prophylactic treatment of migraine without aura: a comparison with flunarizine. Headache. 2002;42:855-61 pubmed
    In a randomized controlled trial extending over 6 months, we evaluated the effectiveness of acupuncture versus flunarizine in the prophylactic treatment of migraine without aura...

More Information

Publications62

  1. Krymchantowski A, Jevoux C, Moreira P. An open pilot study assessing the benefits of quetiapine for the prevention of migraine refractory to the combination of atenolol, nortriptyline, and flunarizine. Pain Med. 2010;11:48-52 pubmed publisher
    ..Accordingly, the aim of this study was to evaluate the use of Quetiapine (QTP) in the preventive treatment of refractory migraine, defined as previous unresponsiveness to the combination of atenolol, nortriptyline, and flunarizine.
  2. So H, Kim H, Lee J, Park S, Park C, Kim Y, et al. Flunarizine induces Nrf2-mediated transcriptional activation of heme oxygenase-1 in protection of auditory cells from cisplatin. Cell Death Differ. 2006;13:1763-75 pubmed
    We investigated the cytoprotective mechanisms of flunarizine in cisplatin-induced death of auditory cells...
  3. Domitrz I. [Hypnic headache as a primary short-lasting night headache: a report of two cases]. Neurol Neurochir Pol. 2005;39:77-9 pubmed
    ..The headache is boring, unilateral or with diffuse location. Lithium carbonate and flunarizine show the best efficacy, caffeine and melatonin may also be useful...
  4. Reveiz Herault L, Cardona A, Ospina E, Carrillo P. [Effectiveness of flunarizine in the prophylaxis of migraine: a meta-analytical review of the literature]. Rev Neurol. 2003;36:907-12 pubmed
    Migraine is a common and disabling health problem among young and middle aged adults. Flunarizine have been used as a prophylactic medication in its management for more than two decades...
  5. Fabiani G, Pastro P, Froehner C. Parkinsonism and other movement disorders in outpatients in chronic use of cinnarizine and flunarizine. Arq Neuropsiquiatr. 2004;62:784-8 pubmed
    ..and the patterns of movement disorders (MD) in outpatients submitted to the chronic use of cinnarizine (cz) or flunarizine (fz), and to establish the main risk factors for MD development...
  6. Bussone G, Cerbo R, Martucci N, Micieli G, Zanferrari C, Grazzi L, et al. Alpha-dihydroergocryptine in the prophylaxis of migraine: a multicenter double-blind study versus flunarizine. Headache. 1999;39:426-31 pubmed
    ..double-blind, clinical study was designed to compare the efficacy and safety of alpha-dihydroergocryptine and flunarizine in the prophylaxis of migraine without aura...
  7. Berilgen M, Bulut S, Gonen M, Tekatas A, Dag E, Mungen B. Comparison of the effects of amitriptyline and flunarizine on weight gain and serum leptin, C peptide and insulin levels when used as migraine preventive treatment. Cephalalgia. 2005;25:1048-53 pubmed
    The tricyclic antidepressant amitriptyline (AMT) and the calcium channel blocker flunarizine are frequently used in the preventive treatment of migraine, but the side-effect of prominent weight gain that frequently emerges during ..
  8. Teive H, Troiano A, Germiniani F, Werneck L. Flunarizine and cinnarizine-induced parkinsonism: a historical and clinical analysis. Parkinsonism Relat Disord. 2004;10:243-5 pubmed
    Drug-Induced Parkinsonism (DIP) represents the second leading cause of Parkinsonism (PK) in several countries. Flunarizine and cinnarizine are some of the most common drugs that cause DIP...
  9. Wood P, Hirst D. Cinnarizine and flunarizine as radiation sensitisers in two murine tumours. Br J Cancer. 1988;58:742-5 pubmed
    The effect of the calcium antagonists, cinnarizine and flunarizine on the radiation sensitivity of two murine tumours, RIF-1 and SCCVII/St was investigated. Initial experiments giving the compounds at 50 mg kg-1 i.p...
  10. Muthuraman A, Sood S, Singla S, Rana A, Singh A, Singh A, et al. Ameliorative effect of flunarizine in cisplatin-induced acute renal failure via mitochondrial permeability transition pore inactivation in rats. Naunyn Schmiedebergs Arch Pharmacol. 2011;383:57-64 pubmed publisher
    This study was aimed to evaluate the protective effect of flunarizine on cisplatin-induced acute renal failure. Administration of cisplatin (6 mg/kg, i.p...
  11. Civelek E, Solmaz I, Onal M, Kircelli A, Temiz C, Secer H, et al. Comparison of intrathecal flunarizine and nimodipine treatments in cerebral vasospasm after experimental subarachnoid hemorrhage in rabbits. Acta Neurochir Suppl. 2011;110:69-73 pubmed publisher
    the aim of this study was to assess and to compare the ability of intrathecal flunarizine and nimodipine to prevent vasospasm in a rabbit model of subarachnoid hemorrhage (SAH)...
  12. Rescifina A, Floresta G, Marrazzo A, Parenti C, Prezzavento O, Nastasi G, et al. Development of a Sigma-2 Receptor affinity filter through a Monte Carlo based QSAR analysis. Eur J Pharm Sci. 2017;106:94-101 pubmed publisher
    ..that six of these compounds have already been tested for affinity at ?2 receptor and, of these, two (Flunarizine and Terbinafine) have shown an experimental ?2 receptor pKi>7...
  13. Golumbek P, Rho J, Spain W, van Brederode J. Effects of flunarizine on spontaneous synaptic currents in rat neocortex. Naunyn Schmiedebergs Arch Pharmacol. 2004;370:176-82 pubmed
    b>Flunarizine, a non-selective blocker of voltage-dependent Ca(2+) and Na(+) channels, is clinically effective against several neurological disorders, including epilepsy, migraine, and alternating hemiplegia of childhood...
  14. Castellino S, Friedman H, Elion G, Ong E, Marcelli S, Page R, et al. Flunarizine enhancement of melphalan activity against drug-sensitive/resistant rhabdomyosarcoma. Br J Cancer. 1995;71:1181-7 pubmed
    b>Flunarizine, a diphenylpiperazine calcium channel blocker, is known to increase tumor blood flow. It also interferes with calmodulin function, repair of DNA damage and drug resistance associated with P-glycoprotein...
  15. Dissanayake K, Wanniarachchi D, Ranawaka U. Case report of hypnic headache: a rare headache disorder with nocturnal symptoms. BMC Res Notes. 2017;10:318 pubmed publisher
    ..There was no satisfactory response to paracetamol, diclofenac sodium, mefenamic acid, tramadol, flunarizine and sodium valproate. Indomethacin was started with the provisional diagnosis of hypnic headache...
  16. Shin M, Kim C, Min B, Ogawa S, Tanaka E, Akaike N. A selective T-type Ca2+ channel blocker R(-) efonidipine. Naunyn Schmiedebergs Arch Pharmacol. 2008;377:411-21 pubmed publisher
    ..Furthermore, we compared the effects of R(-) efonidipine with those of flunarizine and mibefradil on both T-type and HVA Ca2+ channels in rat hippocampal CA1 neurons by using the nystatin ..
  17. Zhang Y, Zhang L, Li B, Wang L. [Effects of acupuncture preventive treatment on the quality of life in patients of no-aura migraine]. Zhongguo Zhen Jiu. 2009;29:431-5 pubmed
    ..The observation group was treated with acupuncture combined with oral administration of Flunarizine Hydrochloride vacuity capsules, and Baihui (GV 20), Shenting (GV 24) and Benshen (GB 13) were selected as main ..
  18. Upadhyay S, Ali S. Molecular recognition of flunarizine dihydrochloride and β-cyclodextrin inclusion complex by NMR and computational approaches. Chem Cent J. 2018;12:33 pubmed publisher
    b>Flunarizine dihydrochloride (FLN) is used in the prophylactic treatment of migraine, vertigo, occlusive peripheral vascular disease and epilepsy...
  19. Suzuki T, Mizoguchi H, Noguchi H, Yoshii T, Misawa M. Effects of flunarizine and diltiazem on physical dependence on barbital in rats. Pharmacol Biochem Behav. 1993;45:703-12 pubmed
    The effects of flunarizine and diltiazem both on development of physical dependence on barbital and on barbital withdrawal signs in rats were examined using the drug-admixed food (DAF) method...
  20. Granados Loarca E. [Calcium antagonists in the urethral syndrome of women with urinary incontinence and urgency]. Actas Urol Esp. 2006;30:406-8 pubmed
    ..The antagonists of the calcium can be useful in those patients with urethral syndrome especially the biggest women. ..
  21. Dora B, Balkan S, Tercan E. Normalization of high interictal cerebrovascular reactivity in migraine without aura by treatment with flunarizine. Headache. 2003;43:464-9 pubmed
    ..Patients were started on prophylactic treatment with flunarizine 10 mg per day, and measurements were repeated at the end of every month for 3 months...
  22. Kwon Y, Falk M, Bennett M. Flunarizine rescues reduced lifespan in CLN3 triple knock-out Caenorhabditis elegans model of batten disease. J Inherit Metab Dis. 2017;40:291-296 pubmed publisher
    ..Remarkably, maximal therapeutic efficacy in this model animal was observed with 1 ?M flunarizine, the identical concentration previously identified in cell-based neuronal models of CLN3 disease...
  23. Popoli P, Pezzola A, Scotti de Carolis A. Possible involvement of the adenosinergic system in flunarizine anticonvulsant activity in rats. Arch Int Pharmacodyn Ther. 1990;306:45-56 pubmed
    The present work deals with an EEG and behavioral study on the effects of the calcium antagonist flunarizine against the convulsions due to pentylenetetrazole in rats. Flunarizine (1.5-18 mg/kg, i.p...
  24. Munhoz R, Werneck L, Teive H. The differential diagnoses of parkinsonism: findings from a cohort of 1528 patients and a 10 years comparison in tertiary movement disorders clinics. Clin Neurol Neurosurg. 2010;112:431-5 pubmed publisher
    ..This decrease probably reflects higher awareness regarding the risk of this motor complication and the more widely used newer antipsychotics. ..
  25. Udagatti V, Dinesh Kumar R. Migraine Related Vertigo. Indian J Otolaryngol Head Neck Surg. 2017;69:563-567 pubmed publisher
    ..The patient and caretakers were thoroughly counseled and educated, started on Flunarizine 10 mg and Dimenhydrinate 50 mg; advice healthy life style, necessary precautions, compliance to treatment...
  26. Dimpfel W, Wedekind W, Spüler M. Field potential analysis in the freely moving rat during the action of cyclandelate or flunarizine. Pharmacol Res. 1992;25:287-97 pubmed
    Cyclandelate and flunarizine, two vasoactive Ca2+ channel or Ca2+ overload blockers have been compared with respect to their in vivo action on field potentials recorded from the depths of the brain in freely moving rats...
  27. Zagvazdin Y, Bodo M, Sarkadi A, Szporny L. Cerebroprotective drugs shorten the hypoxia-induced onset of electrical silence in unanesthetized rats. Pharmacol Res. 2000;42:261-8 pubmed
    ..Pentobarbital (30 and 60 mgkg(-1)i.p.), chloralhydrate (400 mgkg(-1)i.p.) flunarizine (50-100 mgkg(-1)p.o.), hydergine (3-50 mgkg(-1)p.o.), nicergoline (50 mgkg(-1)and 85 mgkg(-1)p.o...
  28. Pudukulatham Z, Zhang F, Gadotti V, M Dahoma S, Swami P, Tamboli Y, et al. Synthesis and characterization of a disubstituted piperazine derivative with T-type channel blocking action and analgesic properties. Mol Pain. 2016;12: pubmed publisher
    ..It has been previously reported that certain piperazine-based compounds such as flunarizine are able to inhibit T-type calcium channels...
  29. Dalla Volta G, Magoni M, Cappa S, Di Monda V. Insomnia and perceptual disturbances during flunarizine treatment. Headache. 1990;30:62-3 pubmed
    ..cases of sleep disturbances and perceptual disorder appearing in close temporal relationship with initiation of flunarizine therapy for migraine prophylaxis: these side effects disappeared after therapy interruption; resumption of the ..
  30. Chang I, Adam M, Jayadev S, Bird T, Natarajan N, Glass I. Novel pregnancy-triggered episodes of CAPOS syndrome. Am J Med Genet A. 2017;: pubmed publisher
    ..Prophylactic administration of acetazolamide or flunarizine may prevent acute episodes of ataxia or mitigate neurologic symptoms, although their efficacies have not been ..
  31. El Sabban F, Reid K, Edmonds H. Comparative effect of flunarizine in two animal models of stroke. Clin Exp Pharmacol Physiol. 2000;27:107-9 pubmed
    ..differed in the extent of their vascular leakage areas and in their response to the cerebroprotective agent flunarizine. 4...
  32. Wood P, Hirst D. Cinnarizine and flunarizine improve the tumour radiosensitisation induced by erythrocyte transfusion in anaemic mice. Br J Cancer. 1989;60:36-40 pubmed
    The ability of the calcium antagonists, cinnarizine and flunarizine, to enhance the radiosensitisation produced by the administration of an erythrocyte transfusion to anaemic, RIF-1 or SCCVII/St tumour bearing mice was determined...
  33. Visudtibhan A, Lusawat A, Chiemchanya S, Visudhiphan P. Flunarizine for prophylactic treatment of childhood migraine. J Med Assoc Thai. 2004;87:1466-70 pubmed
    To determine the effectiveness of flunarizine for migraine prophylaxis in children...
  34. Corvera J, Corvera Behar G, Lapilover V, Ysunza A. Objective evaluation of the effect of flunarizine on vestibular neuritis. Otol Neurotol. 2002;23:933-7 pubmed
    To determine whether vestibular autorotation tests (VAT) would show significant differences in vestibular oculomotor reflex (VOR) parameters in vertiginous patients before and after treatment with flunarizine.
  35. Bisol L, Brunstein M, Ottoni G, Ramos F, Borba D, Daltio C, et al. Is flunarizine a long-acting oral atypical antipsychotic? A randomized clinical trial versus haloperidol for the treatment of schizophrenia. J Clin Psychiatry. 2008;69:1572-9 pubmed
    b>Flunarizine is known as a nonspecific calcium channel blocker that has been used for decades for the treatment of migraine, vertigo, and cognitive deficits related to cerebrovascular disorders...
  36. Tort A, Dall Igna O, de Oliveira R, Mantese C, Fett P, Gomes M, et al. Atypical antipsychotic profile of flunarizine in animal models. Psychopharmacology (Berl). 2005;177:344-8 pubmed
    b>Flunarizine is known as a calcium channel blocker commonly used in many countries to treat migraine and vertigo...
  37. D Ancona S, Mazzo M, Pea F. Increased spontaneous cell detachment of F10 cells induced in vitro by some calcium-channel blockers. J Chemother. 1992;4:235-8 pubmed
    We investigated the action of some Ca(++)-channel blockers such as flunarizine, nifedipine and verapamil on F10 cells in vitro...
  38. Zhang Y, Wang L, Liu H, Li N, Li J, Yi J. The design and protocol of acupuncture for migraine prophylaxis: a multicenter randomized controlled trial. Trials. 2009;10:25 pubmed publisher
    ..design and perform a randomized controlled clinical trial to evaluate the efficacy of acupuncture compared with flunarizine in the prophylactic therapy of patients with migraine without aura in China...
  39. Capanna R, Marcovecchio M, Verrotti A, Trotta D, Chiarelli F, Mohn A. Episodic spontaneous hypothermia potentially triggered by hyperinsulinemia. Horm Res. 2009;72:124-8 pubmed publisher
    ..the episodes, episodic spontaneous hypothermia triggered by hyperinsulinemia was suspected, and treatment with flunarizine, a drug considered the first line in the treatment of migraine-related disorders, was started with a resulting ..
  40. Schurks M, Kastrup O, Diener H. Triptan responsive hypnic headache?. Eur J Neurol. 2006;13:666-7 pubmed
  41. Amery W. Onset of action of various migraine prophylactics. Cephalalgia. 1988;8 Suppl 8:11-3 pubmed
    ..studies were pooled to study the onset of action of three pharmacologically different migraine prophylactics: flunarizine, pizotifen and propranolol...
  42. Trepakova E, Dech S, Salata J. Flunarizine is a highly potent inhibitor of cardiac hERG potassium current. J Cardiovasc Pharmacol. 2006;47:211-20 pubmed
    b>Flunarizine has been widely used for the management of a variety of disorders such as peripheral vascular diseases, migraine, and epilepsy...
  43. Belforte J, Magariños Azcone C, Armando I, Buño W, Pazo J. Pharmacological involvement of the calcium channel blocker flunarizine in dopamine transmission at the striatum. Parkinsonism Relat Disord. 2001;8:33-40 pubmed
    Single intrastriatal microinjections of 25, 50 and 100nmol/microl of flunarizine in normal rats produced a dose-dependent turning behavior toward the injected side when they were challenged with apomorphine (1mg/kg, s.c)...
  44. Aishworiya R, Low P, Tay S. Alternating hemiplegia of childhood: successful treatment with topiramate and flunarizine, a case report. Ann Trop Paediatr. 2011;31:149-52 pubmed publisher
    ..A single effective treatment for this condition is yet to be established; flunarizine is currently the most widely used but with varying degrees of success...
  45. Bitton J, Sauerwein H, Weiss S, Donner E, Whiting S, Dooley J, et al. A randomized controlled trial of flunarizine as add-on therapy and effect on cognitive outcome in children with infantile spasms. Epilepsia. 2012;53:1570-6 pubmed publisher
    ..In a randomized controlled trial, patients received a standardized therapy plus flunarizine or placebo. The standardized treatment consisted of vigabatrin as first-line therapy...
  46. Gracia Naya M, Rios C, García Gómara M, Sanchez Valiente S, Mauri Llerda J, Santos Lasaosa S, et al. [A comparative study of the effectiveness of topiramate and flunarizine in independent series of chronic migraine patients without medication abuse]. Rev Neurol. 2013;57:347-53 pubmed
    ..To show that flunarizine is as effective as topiramate in cases of chronic migraine without medication abuse...
  47. Salvinelli F, Trivelli M, Casale M, Firrisi L, Di Peco V, D Ascanio L, et al. Treatment of benign positional vertigo in the elderly: a randomized trial. Laryngoscope. 2004;114:827-31 pubmed
    The objective of the study was to evaluate the efficacy of three therapeutic strategies (Semont maneuver, flunarizine, and no treatment) in patients with benign paroxysmal positional vertigo. Randomized prospective trial...
  48. Mangabeira Albernaz P. Calcium antagonists as a peripherally acting labyrinthine suppressant in humans. Acta Otolaryngol Suppl. 1988;460:99-103 pubmed
    ..The cumulative analysis of the results indicates that cinnarizine, flunarizine and bencyclan have produced good clinical results, particularly in patients with vascular problems...
  49. Clark J, Milakovic M, Cull A, Klose M, Mercier A. Evidence for postsynaptic modulation of muscle contraction by a Drosophila neuropeptide. Peptides. 2008;29:1140-9 pubmed publisher
    ..with L-type calcium channel blockers, nifedipine and nicardipine, but not by T-type blockers, amiloride and flunarizine. The present results provide evidence that this Drosophila peptide can act postsynaptically in addition to its ..
  50. Zhang Y, Sun W, Qin J, Jiang Y, Wu X. [Clinical characteristics of alternating hemiplegia of childhood in 13 patients]. Zhonghua Er Ke Za Zhi. 2003;41:680-3 pubmed
    ..Twelve patients received flunarizine therapy. Flunarizine reduced the severity, duration, or frequency of hemiplegic attacks in 8 patients...
  51. Keith I, Will J, Huxtable R, Weir K. Anti-platelet agents reduce morphological changes of chronic hypoxic pulmonary hypertension. Histol Histopathol. 1987;2:203-6 pubmed
    ..In Study 2, hypoxic rats treated with the calcium blocker, flunarizine, were found to have less medial hypertrophy than a control group of hypoxic rats...
  52. Keers R, Farmer A, Aitchison K. Extracting a needle from a haystack: reanalysis of whole genome data reveals a readily translatable finding. Psychol Med. 2009;39:1231-5 pubmed publisher
    ..One such agent, flunarizine, is structurally related to other first-generation derivatives of antihistamines such as antipsychotics...
  53. Sakurai Yamashita Y, Sakaguchi S, Yoshikawa D, Okimura N, Masuda Y, Katamine S, et al. Female-specific neuroprotection against transient brain ischemia observed in mice devoid of prion protein is abolished by ectopic expression of prion protein-like protein. Neuroscience. 2005;136:281-7 pubmed
    ..However, female Zrch I Prnp(0/0) mice showed mild neuronal loss similar to wild-type mice. Flunarizine, a T- and L-type Ca(2+)-channel antagonist, significantly reduced the neuronal loss in female but not in male ..