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Gastrointestinal effects of Syzigium aromaticum (L) Merr. & Perry (Myrtaceae) in animal models.

BACKGROUND: Gastrointestinal disorders constitute one of the most common diseases world-wide and the treatment of some of them has since con … eously with distilled water (10 ml kg(-1)) and standard antiulcer drugs (omeprazole 20.0 mg kg(-1), cimetidine 100.0 mg kg(-1) and misoprostol 0.2 mg kg(-1)), respectively. Lastly, the effect of SYZ was investigated on a segment of isolated rabbit ileum and subsequently compared with acetylcholine 5.5 x 10(-5) M. The effects of atropine (3.4 x 10(-6) M and 3 …

Phase II study of paclitaxel, ifosfamide, and carboplatin in patients with recurrent or metastatic head and neck squamous cell carcinoma.

BACKGROUND: In the current study the authors assessed the antitumor activity (including response rate, duration of response, and survival) a … s repeated every 3-4 weeks. All patients were premedicated with dexamethasone, diphenhydramine, and cimetidine before paclitaxel infusion. Prophylactic hematopoietic growth factors were not given. RESULTS: Among 56 patients entered onto the study, 55 patients were analyzed for survival rates (locoregional recurrence alone in 56% of patients and distant meta …

Drug repurposing in oncology: Compounds, pathways, phenotypes and computational approaches for colorectal cancer.

The strategy of using existing drugs originally developed for one disease to treat other indications has found success across medical fields. Such drug repurposing promises faster access of drugs to patients while reducing costs in the long and difficult process of drug development. However, the number of existing drugs and diseases, together with the heterogeneity of patients and diseases, notably including cancers, can make repurposing time consuming and inefficient. The key question we address is how to efficiently repurpose an existing drug to treat a given indication. As drug efficacy rem

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… TM ) | Angiotensin receptor blocker | Hypertension | | + | | | | | + | [ 73 , 74 ] TCV116 (Candesartan TM ) | Angiotensin receptor blocker | Hypertension | | + | | | | | + | [ 75 ] Mesalamine (Mesalazine TM ) | Aminosalicylate | Inflammatory bowel diseases | | + | + | | | + | | [ 76 ] Cimetidine … potrace 1.16, written by Peter Selinger 2001-2019 </metadata><g transform="translate(1.000000,15.000000) scale(0.019444,-0.019444)" fill="currentColor" stroke="none"><path d="M0 440 l0 -40 480 0 480 0 0 40 0 40 -480 0 -480 0 0 -40z M0 280 l0 -40 480 0 480 0 0 40 0 40 -480 0 -480 0 0 -40z"/></g></svg> O Cimetidine …

Neuroendocrine mechanisms during reversible hypovolaemic shock in humans with emphasis on the histaminergic and serotonergic system.

In humans, the head-up tilted position results in central hypovolaemia which mimicks haemorrhage and is associated with cardiovascular chang … ympathoadrenal response was affected by histaminergic receptor blockade. The H2-receptor antagonist cimetidine inhibited plasma A, while the H1-receptor antagonist mepyramine attenuated plasma NA and reduced cardiovascular tolerance, and also induced some sedation. A possible effect of sedation and anxiolysis was investigated by administration of the GABAerg …

A new isoquinolinone derivative with noble vasorelaxation activity.

The pharmacological effects of BDPBI (7-bromo-1,4-dihydro-2-phenyl-4,4-bis(4-pyridinylmethyl)2H-isoquinolin-3-one dihydrochloride) were tested on isolated endothelium-containing or denuded aorta of the guinea pig. BDPBI with the formula C(27)H(24)BrCl(2)N(3)O was synthesized starting with 3-isochromanone. In the endothelium-containing preparations of the aortic rings, phenylephrine (PHE; 10 micromol/l) elicited contracture and acetylcholine (ACh; 10 micromol/l) or BDPBI (0.01-10 micromol/l) elicited relaxation effects on the PHE-precontracted preparations. The BDPBI-elicited effect on the PHE-

Toxicity profile of supratherapeutic loperamide: a systematic review and dose-response analysis.

INTRODUCTION: Life-threatening cardiotoxicity resulting from supratherapeutic loperamide exposure (i.e., >16 mg per day) has been increasing … gestion of substances in order to increase loperamide exposure was reported in 5% cases (n = 6, all cimetidine). Syncope was frequently reported (45%, n = 58). Severe cases (64%, n = 83) were mainly characterized by polymorphic (55%, n = 46) or sustained monomorphic (40%, n = 33) ventricular tachycardias. Typical signs of opioid toxicity were reported in 12% …

Gastric acid secretion is augmented by the replacement of extracellular Na+ with K+ or other ions.

We examined the validity of the high K+ condition, widely used as a model to investigate the mechanism of acid secretion, employing isolated rabbit gastric glands. When Na+ in the nutrient solution was replaced with K+, the acid secretion monitored by the accumulation of 14C-aminopyrine increased K+-concentration-dependently. Stimulation of carbachol or dbcAMP was also greatly enhanced by K+. The responses to forskolin, phorbol ester, gastrin and submaximal dose of histamine were potentiated in the high K+ condition, but the responses to isobutylmethylxanthine, calyculin A and the maximal dose

Critical role of histamine H4 receptor in leukotriene B4 production and mast cell-dependent neutrophil recruitment induced by zymosan in vivo.

The recently identified histamine receptor, H4, was shown to be primarily expressed on leukocytes and has been implicated in the activation of lymphocytes, eosinophils, and mast cells in vitro. Its function in vivo, however, has not yet been characterized. We present evidence for a critical role of H4 receptor in the mast cell-dependent recruitment of neutrophils. Mice injected with zymosan into the pleural cavity developed massive neutrophilia within hours after challenge. Neutrophilia was dose-dependently reduced when mice were pretreated with thioperamide, a known H(3/4) receptor antagonist

NH(4)Cl inhibition of acid secretion: possible involvement of an apical K(+) channel in bullfrog oxyntic cells.

This study was undertaken to determine the mechanism by which ammonium chloride (NH(4)Cl) inhibits stimulated acid secretion in the bullfrog gastric mucosa. To this end, four possible pathways of inhibition were studied: 1) blockade of basolateral K(+) channel, 2) blockade of ion transport activity, 3) neutralization of secreted H(+) in the luminal solution, or 4) ATP depletion. Addition of nutrient 10 mM NH(4)Cl (calculated NH(3) concentration = 92.5 microM and NH(4)(+) concentration = 9.91 mM) inhibited acid secretion within 30 min. Inhibition of acid secretion did not occur by blockade of b

Common variable immunodeficiency. Old questions are getting clearer.

Common variable immunodeficiency (CVID) is a heterogeneous entity characterized by an impaired ability to produce antibodies. The failure is localized in partially mature B lymphocytes, though T lymphocyte abnormalities are occasionally present. This deficiency affects antibody synthesis and class switch from IgD and IgM, to IgG and IgA. CVID is related to selective IgA deficiency, and both abnormalities may coincide in one same family, and evolve from one to another in the same patient. The symptoms generally manifest in adults, but can occur at any age, even in infancy. Recurrent bacterial i

Randomized trial of single agent paclitaxel given weekly versus every three weeks and with peroral versus intravenous steroid premedication to patients with ovarian cancer previously treated with platinum.

The aim of this study was to evaluate the efficacy and toxicity of paclitaxel given at the same dose intensity and administered weekly (arm A) or every 3 weeks (arm B). and to assess the safety of intravenous steroids versus standard peroral premedication. Two hundred and eight patients with advanced ovarian cancer previously treated with no more than one platinum-containing regimen were randomized to receive either a weekly infusion of paclitaxel or an infusion every 3 weeks. The median delivered dose intensity was 77.6 mg/m2/week in the weekly arm, and 72.7 mg/m2/week in the every 3 weeks ar

Mediation by bradykinin of rat paw oedema induced by collagenase from Clostridium histolyticum.

1. Collagenases are thought to play a major role in the pathology of gas gangrene caused by Clostridium histolyticum, because they can destr … okinin A, which augment the oedema-inducing effect of bradykinin.5. Indomethacin or mepyramine plus cimetidine failed to inhibit collagenase-induced paw oedema.Thus, prostaglandins and histamine do not seem to be involved in collagenase-induced paw oedema.6. After subplantar injection of collagenase, the sensitivity scores in a modified formalin-test rapidly …

Unlocking hidden potential: advancements, approaches, and obstacles in repurposing drugs for cancer therapy.

High rates of failure, exorbitant costs, and the sluggish pace of new drug discovery and development have led to a growing interest in repurposing "old" drugs to treat both common and rare diseases, particularly cancer. Cancer, a complex and heterogeneous disease, often necessitates a combination of different treatment modalities to achieve optimal outcomes. The intrinsic polygenicity of cancer, intricate biological signalling networks, and feedback loops make the inhibition of a single target frequently insufficient for achieving the desired therapeutic impact. As a result, addressing these c

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… This in silico screening method has been demonstrated in the identification of cimetidine, an anti-peptic ulcer drug, as a potential treatment for lung adenocarcinoma [ 41 ]. … Brimblecombe R Duncan W Durant G Ganellin C Parsons M Black J The pharmacology of cimetidine, a new histamine H2-receptor antagonist Br J Pharm 2010 160 S52 3 10.1111/j.1476-5381.2010.00854.x PMC2947417 20590655 128. …

Prospects for repurposing CNS drugs for cancer treatment.

Drug repurposing is the idea of using an already approved drug for another disease or disorder away from its initial use. This new approach ensures the reduction in high cost required for developing a new drug in addition to the time consumed, especially in the tumor disorders that show an unceasing rising rate with an unmet success rate of new anticancer drugs. In our review, we will review the anti-cancer effect of some CNS drugs, including both therapeutic and preventive, by searching the literature for preclinical or clinical evidence for anticancer potential of central nervous system drug

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… candidates with good toxicity profile and experimental evidence, to be subjected to clinical trials to validate their off-label usage. 4 The project has provided a list of candidate drugs, including Losartan, Omeprazole, Statins, Nitroglycerin, Chloroquine/ Hydroxychloroquine, Propranolol, Mebendazole, Cimetidine … candidates with good toxicity profile and experimental evidence, to be subjected to clinical trials to validate their off-label usage. 4 The project has provided a list of candidate drugs, including Losartan, Omeprazole, Statins, Nitroglycerin, Chloroquine/ Hydroxychloroquine, Propranolol, Mebendazole, Cimetidine …

Chemotherapy-induced acute kidney injury: epidemiology, pathophysiology, and therapeutic approaches.

Despite significant advancements in oncology, conventional chemotherapy remains the primary treatment for diverse malignancies. Acute kidney injury (AKI) stands out as one of the most prevalent and severe adverse effects associated with these cytotoxic agents. While platinum compounds are well-known for their nephrotoxic potential, other drugs including antimetabolites, alkylating agents, and antitumor antibiotics are also associated. The onset of AKI poses substantial risks, including heightened morbidity and mortality rates, prolonged hospital stays, treatment interruptions, and the need for

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… Additionally, by the same mechanism, Cimetidine has shown protective effects in both animal and human studies, whether used alone or in combination with verapamil, and without interfering with the antitumor effects of cisplatin ( 54 – 58 ). … Nephrotoxic effects of platinum cytostatics–preventative effects of nifedipine and cimetidine. Sb Lek. (1994) 95:173–83. 57. Sprowl JA, van Doorn L, Hu S, van Gerven L, de Bruijn P, Li L, et al. …

Topical Imiquimod is an Effective and Safe Drug for Molluscum Contagiosum in Children.

Dear Editor, Molluscum contagiosum (MC) is a very common skin infection caused by a molluscipox virus gene of the poxvirus family. It usuall … etinoin, cantharidin, trichloroacetic and salicylic acid, potassium hydroxide, interferon-alfa, and cimetidine). Imiquimod is a topically applicable Toll-like receptor (TLR)-7/8 agonist, which is capable of stimulating the innate cutaneous immunity and the cellular arm of the adaptive immune response and of exerting potent anti-viral, anti-tumor and immunore …

Acetaminophen poisoning: an evidence-based consensus guideline for out-of-hospital management.

The objective of this guideline is to assist poison center personnel in the appropriate out-of-hospital triage and initial management of pat … n emergency department in accordance with the poison center's normal triage criteria. 2) The use of cimetidine as an antidote is not recommended (Grade A).

Radioprotectors & mitigators in radiation therapy: Harnessing diverse pathways for optimizing clinical outcomes.

Radioprotectors are agents that protect normal tissues from the harmful effects of radiation during cancer treatment. Combining these protective agents with advanced radiotherapy techniques such as stereotactic body radiotherapy (SBRT) and proton therapy offers a promising strategy to enhance therapeutic efficacy while minimizing normal tissue toxicity. However, despite extensive research and the identification of numerous potential radioprotectors, only a few have made it into clinical practice. It is primarily because the transition from laboratory research to clinical application faces sign

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… , Famotidine) | Mice (liver, oxidative stress model) | Cimetidine: 50 mg/kg i.p.; Famotidine: 20 mg/kg i.p., 30 min before irradiation | Gamma, 2 and 4 Gy | Reducing clastogenic effects of radiation | DMF: Not known | 36 Flagellin ( e.g. , CBLB502, TLR5 agonist) | Mice, Rhesus monkeys | Single systemic … Radioprotective effects of vitamin C, cimetidine, and famotidine on lipid peroxidase and hepatic glutathione levels in mouse liver. Int J Cell Biol. 2025;2025:1106920. doi: 10.1155/ijcb/1106920. 37. Burdelya LG, Brackett CM, Kojouharov B, Gitlin II, Leonova KI, Gleiberman AS, et al. …

Repurposing drugs in oncology (ReDO)-selective PDE5 inhibitors as anti-cancer agents.

Selective phosphodiesterase 5 inhibitors, including sildenafil, tadalafil and vardenafil, are widely-used in the treatment of erectile dysfunction and pulmonary arterial hypertension. They are also well-known as examples of successful drug repurposing in that they were initially developed for angina and only later developed for erectile dysfunction. However, these drugs may also be effective cancer treatments. A range of evidentiary sources are assessed in this paper and the case made that there is pre-clinical and clinical evidence that these drugs may offer clinical benefit in a range of can

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… Interventions that have been explored include pre-operative ketorolac [ 107 ] or aspirin [ 108 ], depot progesterone [ 109 ], cimetidine [ 110 ] and immunonutrition with l-arginine [ 111 ]. … Repurposing drugs in oncology (ReDO)-cimetidine as an anti-cancer agent. Ecancermedicalscience. 2014;8:485. doi: 10.3332/ecancer.2014.485. 101. Vila-Leahey A, Oldford SA, Marignani PA, et al. Ranitidine modifies myeloid cell populations and inhibits breast tumor development and spread in mice. …

Targeting Tumor Glycans for Cancer Therapy: Successes, Limitations, and Perspectives.

Aberrant glycosylation is a hallmark of cancer and can lead to changes that influence tumor behavior. Glycans can serve as a source of novel clinical biomarker developments, providing a set of specific targets for therapeutic intervention. Different mechanisms of aberrant glycosylation lead to the formation of tumor-associated carbohydrate antigens (TACAs) suitable for selective cancer-targeting therapy. The best characterized TACAs are truncated O-glycans (Tn, TF, and sialyl-Tn antigens), gangliosides (GD2, GD3, GM2, GM3, fucosyl-GM1), globo-serie glycans (Globo-H, SSEA-3, SSEA-4), Lewis anti

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… Finally, an interesting observation is that cimetidine, a histamine H2 receptor antagonist inhibiting stomach acid production, dramatically improves survival in patients with colorectal cancer exhibiting high concentrations of SLeX and SLeA in tumor cells [ 284 ]. … Cimetidine is able to block E-selectin expression on vascular endothelium, and this inhibits adhesion of cancer cells to endothelial cells [ 285 ], suggesting that cimetidine can prevent metastasis development by suppression of E-selectin/SLeX and SLeA interaction. …