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Famotidine brain

Mariusz J Świąder, Stanisław J Czuczwar
H2 histamine receptors are localized postsynaptically in the CNS. The aim of this study was to evaluate the effects of acute (1 day) and prolonged (7 day) administration of the H2 histamine receptor antagonist, famotidine, on the anticonvulsant activity of conventional antiepileptic drugs (AEDs; valproate, carbamazepine, diphenylhydantoin and phenobarbital) against maximal electroshock (MES)-induced seizures in mice. In addition, the effects of these drugs alone or in combination with famotidine were studied on motor performance and long-term memory...
June 2014: Pharmacological Reports: PR
Ali Mojtahedin, Esmaeal Tamaddonfard, Ali Zanboori
In the present study, effects of intracerebroventricular (icv) administration of histamine, mepyramine (H1-receptor antagonist) and famotidine (H2-receptor antagonist) have been investigated on the formalin test in rats. Subcutaneous injection of formalin (50 microl, 1%) into the ventral surface of the left hind paw produced a marked biphasic pain response (first phase: 0-5 min and second phase: 15-45 min). All the performed treatments did not significantly influence the first phase of pain. Histamine at the doses of 10 and 40 microg and mepyramine and famotidine at the same doses of 20 and 80 microg, significantly (P < 0...
July 2008: Indian Journal of Physiology and Pharmacology
R Zamfirova, A Bocheva, Y Dobrinova, S Todorov
1. Tyr-K-MIF-1 is a melanocyte inhibiting factor (MIF) neuropeptide, isolated from the brain. Opposite to other MIFs (Tyr-MIF-1, Tyr-W-MIF-1), it has a very low affinity for opiate mu-receptors, but interacts with Tyr-MIF-1 specific binding sites. Tyr-MIF-1 and Tyr-W-MIF-1 evoke antinociception mainly by activating opioid receptors. We investigated the possible antinociceptive effect of Tyr-K-MIF-1 and the involvement of histaminergic system in its mechanism of action. 2. Tested on rats by paw-pressure test, Tyr-K-MIF-1 (0...
April 2007: Autonomic & Autacoid Pharmacology
Mila Kesiova, Albena Alexandrova, Neli Yordanova, Margarita Kirkova, Simeon Todorov
The potential antioxidant activity of diphenhydramine (histamine H1-receptor antagonist) and famotidine (histamine H2 receptor antagonist) was studied. Diphenhydramine inhibited the spontaneous, Fe(II)-induced and Fe(II)/ascorbate-induced lipid peroxidation, while famotidine showed a biphasic concentration-dependent effect on spontaneous lipid peroxidation (a stimulation by 1 mM and an inhibition by 5 mM) and increased Fe(II)-induced- and inhibited Fe(II)/ascorbate-induced lipid peroxidation in the rat liver and brain...
March 2006: Pharmacological Reports: PR
Mariusz J Swiader, Jarogniew J Łuszczki, Marian Wielosz, Stanisław J Czuczwar
The aim of this study was to evaluate the effects of H(1) (antazoline and astemizole) or H(2) (cimetidine and famotidine) histamine receptor antagonists on the clonic phase, tonic seizures and morality of mice challenged with aminophylline to induce convulsions in mice. Moreover, the total plasma and brain concentrations of theophylline were evaluated. Astemizole (1 mg/kg) did not affect the threshold for aminophylline-induced seizures, but when administered at a dose of 2 mg/kg, it significantly reduced the CD(50) value of aminophylline from 249 mg/kg to 211 mg/kg (p < 0...
July 2005: Pharmacological Reports: PR
Keri E Cannon, Mark W Fleck, Lindsay B Hough
Even though conventional systemic doses of cimetidine and other histamine H(2) antagonists display minimal brain penetration, central nervous system (CNS) effects (including seizures and analgesia) have been reported after administration of these drugs in animals and man. To test the hypothesis that cimetidine-like drugs produce these CNS effects via inhibition of GABA(A) receptors, the actions of these drugs were studied on seven different, precisely-defined rat recombinant GABA(A) receptors using whole-cell patch clamp recordings...
October 8, 2004: Life Sciences
Yoshinori Nagata, Hiroyuki Kusuhara, Shuichi Hirono, Hitoshi Endou, Yuichi Sugiyama
The choroid plexus (CP) acts as a site for the elimination of xenobiotic organic compounds from the cerebrospinal fluid (CSF). The purpose of the present study is to investigate the role of rat organic anion transporter 3 (rOat3; Slc22a8) in the uptake of H(2)-receptor antagonists (cimetidine, ranitidine, and famotidine) by the isolated rat CP. Saturable uptake of cimetidine and ranitidine was observed in rOat3-LLC with K(m) values of 80 and 120 microM, respectively, whereas famotidine was found to be a poor substrate...
September 2004: Drug Metabolism and Disposition: the Biological Fate of Chemicals
F Burdan, Barbara Madej, Elzbieta Radzikowska, J Dudka, Agnieszka Korobowicz, M Pasternak, R Maciejewski
Cathepsins are lysosomal enzymes that are used a sensitive markers in various toxicological investigations. The purpose of this study was to evaluate and compare the influence of cimetidine and famotidine on the cerebral cortex, particularly on the activity of cortical cathepsin B, D and L in the frontal lobe of rat brain. The drugs were administered intraperitoneally, twice a day, for six weeks to male Wistar rats in two doses. The initial dose was 2.85 mg/kg for cimetidine and 0.285 mg/kg for famotidine. The second dose was 10 times higher...
2003: Acta Physiologica Hungarica
R Y Yuan, C R Kao, J J Sheu, C H Chen, C S Ho
OBJECTIVE: To describe a patient who developed delirium when switched from cimetidine to famotidine. CASE SUMMARY: An 84-year-old Taiwanese woman was hospitalized for tarry stools. Her past medical history revealed only a decrease in renal function. She tolerated both oral and intravenous cimetidine therapy with a daily dose of 400-900 mg intermittently for 20 years. On hospital days 1-3, cimetidine 300 mg was injected intravenously every eight hours without difficulty...
September 2001: Annals of Pharmacotherapy
L A Linday, J A Tsiouris, I L Cohen, R Shindledecker, R DeCresce
Using single subject research design, we performed pilot research to evaluate the safety and efficacy of famotidine for the treatment of children with autistic spectrum disorders. We studied 9 Caucasian boys, 3.8-8.1 years old, with a DSM-IV diagnosis of a pervasive developmental disorder, living with their families, receiving no chronic medications, and without significant gastrointestinal symptoms. The dose of oral famotidine was 2 mg/kg/day (given in two divided doses); the maximum total daily dose was 100 mg...
2001: Journal of Neural Transmission
M Odeh, A Oliven
H2-receptor antagonists may cause various types of central nervous system reactions, particularly in patients with advanced age and/or impaired renal or liver function. These reactions have rarely been reported in association with famotidine. In five elderly patients, four of them with renal failure, central nervous system reactions developed shortly after initiation with famotidine therapy. These adverse reactions completely resolved after famotidine withdrawal. The authors' five cases and the other seven previously reported emphasize the need for dosage adjustment of famotidine in elderly patients and in those with renal failure, and that these patients should be carefully monitored for development of central nervous system reactions, which sometimes could be very serious...
October 1998: Journal of Clinical Gastroenterology
J Kawakami, K Yamamoto, M Shimokawa, Y Sawada, A Asanuma, K Yanagisawa, T Iga
To clarify the dominant mechanism for the convulsant activity of H2 antagonists, the effects of an H2 antagonist, cimetidine, on membrane currents induced by various agonists were investigated. In Xenopus oocytes injected with mouse-brain mRNA, acetylcholine (ACh), serotonin (5-HT), gamma-aminobutyric acid (GABA), glycine (Gly), glutamic acid (Glu), kainic acid (KA), quisqualic acid (QA) and N-methyl-D-aspartic acid (NMDA)-induced current responses were recorded under a voltage-clamp condition. Cimetidine inhibited GABA-induced currents in a concentration-dependent manner; however, the current responses induced by the other agonists were not modified...
September 1997: Biological & Pharmaceutical Bulletin
M Chang, H Saito, K Abe
We investigated the effect of cimetidine, a clinically used H2-receptor antagonist, on the induction of long-term potentiation (LTP) in the dentate gyrus of anesthetized rats. Intracerebroventricular injection of cimetidine (50-100 nmol) inhibited the induction of LTP in a dose-dependent manner. The inhibitory effect of cimetidine was not mimicked by other H2-receptor antagonists (ranitidine, famotidine) or the H1-receptor antagonist diphenhydramine or the H3-receptor antagonist thioperamide. These results suggest that cimetidine inhibits hippocampal synaptic plasticity by a novel brain mechanism unrelated to H1, H2 or H3 receptors...
July 1997: Japanese Journal of Pharmacology
L A Linday
Famotidine (Pepcid, a histamine-2 receptor blocker, is marketed for the treatment of peptic ulcer disease, gastroesophageal reflux, and the treatment of pathological hypersecretory conditions, including the Zollinger-Ellison syndrome. Recent reports indicate that it is also effective in relieving the deficit (or withdrawal) symptoms of adults with schizophrenia. Autism, a neuropsychiatric disorder which presents within the first few years of life, is defined by deficient social interaction, communication, language, play, and a markedly restricted repertoire of activities and interests...
May 1997: Medical Hypotheses
R B Rosse, K Kendrick, M Fay-McCarthy, G D Prell, P Rosenberg, L C Tsui, R J Wyatt, S I Deutsch
Histaminergic projections innervate brain areas implicated in the pathophysiology of schizophrenia. In a previous open-label study, there was the suggestion that famotidine, and H2 histamine-receptor antagonist, possessed adjuvant therapeutic properties when added to the stable neuroleptic medications regimens of 10 treatment-refractory patients. In that study, the maximal dosage of famotidine was limited to 40 mg/day, the recommended maximal dosage for the treatment of peptic ulcer disease. In this study, we examined 18 patients fulfilling DSM-III-R criteria for schizophrenia and schizoaffective disorder who had famotidine (100 mg/day) added to their stable neuroleptic medication regimen...
August 1996: Clinical Neuropharmacology
M Shimokawa, K Yamamoto, J Kawakami, Y Sawada, T Iga
Convulsive potency was evaluated to investigate the mechanism of neurotoxic convulsion induced by histamine H2 receptor antagonists (H2 blockers). Four H2 blockers, cimetidine (721-1236 nmol), ranitidine (477-954 nmol), famotidine (7.4-44 nmol), and nizatidine (226-603 nmol) were administered intracerebrally (i.c.) to mice. Dose dependency of clonic and/or tonic convulsion was observed, and the ED50 values of convulsive occurrence for cimetidine, ranitidine, famotidine, and nizatidine were 997, 662, 23.4, and 404 nmol, respectively...
February 1996: Toxicology and Applied Pharmacology
W S Tung, M A Helfaer, J R Kirsch, R J Traystman
OBJECTIVE: To determine whether histamine-2 (H2) receptor antagonists can blunt the increase in cerebral blood flow after cerebral ischemia. DESIGN: Prospective, randomized trial. SETTING: Animal laboratory. SUBJECTS: Piglets aged 1 to 2 wks. INTERVENTIONS: Three groups of piglets were anesthetized with pentobarbital, mechanically ventilated, and hemodynamically monitored. Each animal was randomized to receive one of three treatments 20 mins before ischemia: famotidine (0...
February 1993: Critical Care Medicine
L K Oyewumi, D Vollick, H Merskey, C Plumb
Some patients suffering from schizophrenia fail to respond to or tolerate adequate doses of available antipsychotic medications. Thus, innovative pharmacotherapeutic approaches, such as augmentation strategies, play an important role in the management of these treatment-resistant patients. A recent case report suggested that the administration of famotidine to a patient suffering from schizophrenia with peptic ulcer disease was associated with improvement in the deficit symptoms of schizophrenia. Famotidine is a potent highly selective H2 receptor antagonist which crosses the blood-brain barrier...
March 1994: Journal of Psychiatry & Neuroscience: JPN
T Naruse, R Ishii
We investigated whether histaminergic neurons in the brain are involved in diazepam-induced hyperphagia in rats. Pretreatment with intracerebroventricular (ICV) injection of either histamine H1-receptor antagonist, pyrilamine (10 and 30 micrograms) or histamine H2-receptor antagonist, famotidine (3 and 10 micrograms) did not affect only diazepam (1 mg/kg, subcutaneous, SC)-induced hyperphagia in nondeprived rats, but also spontaneous feeding in food-deprived rats. In addition, pretreatment with ICV injection of histamine H3-receptor antagonist, thioperamide, and histamine H3-receptor agonist, (R) alpha methylhistamine, enhanced and inhibited diazepam-induced hyperphagia (1 mg/kg, SC) in nondeprived rats, respectively...
August 1995: Pharmacology, Biochemistry, and Behavior
G Le Gros, X M Zhang, P G Parsons
Nontoxic doses of the histamine H2 antagonists ranitidine, cimetidine, lamtidine and mifentidine rapidly and reversibly increased tyrosinase activity in an amelanotic human melanoma cell line (MM96L) with low constitutive activity. The H2 antagonists, famotidine and MGTI, and the imidazol(in)e receptor ligand clonidine had no effect either alone or in competition with ranitidine, whilst metiamide decreased tyrosinase activity. Lysosomotropic amines had a similar effect to ranitidine, except that induction reached a plateau at 6 h and was insensitive to amiloride...
December 1994: Melanoma Research
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