Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0033774 (pruritus)
14,546 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Cutaneous fungal infections are frequently associated with an inflammatory component including irritated skin, itching and stinging/burning. Therapeutic anti-fungal agents that have anti-inflammatory activity have the potential to provide clinical benefit beyond fungus eradication. Recently, certain anti-fungal agents have been shown to have intrinsic anti-inflammatory activity, therefore we sought to determine the extent of the anti-inflammatory activity of these compounds. The anti-inflammatory activities of eight anti-fungal agents (butoconazole, ciclopirox olamine, fluconazole, miconazole nitrate, sertaconazole nitrate, terconazole, tioconazole and ketoconazole) were compared in a number of preclinical models of dermal inflammation and pruritus. While butoconazole, ciclopirox olamine, fluconazole, and miconazole nitrate were all found to have anti-inflammatory activity, only sertaconazole nitrate reduced the release of cytokines from activated lymphocytes and mitigated inflammation in animal models of irritant contact dermatitis and neurogenic inflammation. In addition, sertaconazole nitrate inhibited contact hypersensitivity and scratching responses in a murine model of pruritus. Furthermore, the in vitro and in vivo anti-inflammatory activity of sertaconazole nitrate was found to be greater than other topical anti-fungal agents examined. These studies demonstrate that topical administration of clinically relevant concentrations of sertaconazole nitrate resulted in an efficacious anti-inflammatory activity against a broad spectrum of dermal inflammation models and itch. The anti-inflammatory properties of sertaconazole may contribute to the efficacy of the drug in the treatment of cutaneous fungal conditions and provide greater anti-inflammatory activity compared with other anti-fungal agents.
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PMID:Anti-inflammatory and anti-itch activity of sertaconazole nitrate. 1686 38

Numerous cases of Gongylonema spp. infection with associated pathological lesions and clinical signs were identified in a collection of Goeldi's monkeys (Callimico goeldii) (GMs) at a zoological park during a 3-yr period. An increase in the incidence of clinical signs in the GMs and other callitrichid species prompted an investigation to determine the prevalence of infection within the collection and evaluate treatment protocols. Twenty-one callitrichids [nine GMs, four golden lion tamarins (Leontopithecus rosalia), six cotton-top tamarins (Saguinus oedipus), and two golden-headed lion tamarins (Leontopithecus chrysomelas)] were included in this study. Many of the animals had been positively diagnosed on past examinations. Repeated cytological evaluations of scrapings taken from the mucosa of the tongue were performed to diagnose infection. The animals were randomly divided into two groups and treated with either ivermectin (290 microg/kg p.o., q7 days for four doses) or mebendazole (70 mg/kg p.o. q24 hr for three doses). Follow-up scrapings were performed on all animals at days 35, 64, and 156. Numerous animals displayed clinical signs (facial pruritus, inflammation, and ptyalism) before and throughout the investigation; however, Gongylonema spp. infections were only confirmed by tongue scrapings in two animals. Fecal floatation by using a sodium nitrate solution for recovery of spirurid eggs also was performed, but it yielded no positive results. The low number of confirmed cases precluded comparative evaluation of the efficacy of the anthelmintic treatment protocols. However, both regimes seemed subjectively similar in decreasing clinical signs and were safe with no adverse effects. Diagnosis of Gongylonema spp. infection is challenging, even when severe clinical signs are present. This investigation further demonstrates the lack of a reliable ante-mortem test for the parasite and underscores the importance of treatment based on clinical signs. Until a more sensitive test is available, further comparison studies on treatment regimes will be difficult and likely unrewarding.
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PMID:Evaluation of control and treatment of Gongylonema spp. infections in callitrichids. 1746 72

Arterial vasodilation with concomitant hyperdynamic circulation is a common finding in cirrhotic subjects. Elevated levels of plasma endogenous opioid peptides have been reported in cholestasis and cirrhosis. Increased opioid peptides contribute to different manifestations of chronic liver disease such as pruritus, ascitis, and hepatic encephalopathy. In this study the potential role of opioid system in cirrhosis-induced vascular hyporesponsiveness was investigated. Bile duct ligated and sham operated animals received daily subcutaneous administration of naltrexone, an opioid receptor antagonist (20 mg/kg/day), or saline for 28 days. After 4 weeks the superior mesenteric artery was cannulated and was perfused according to McGregor method and then phenylephrine vasoconstrictor response of mesenteric vessels (10(-10) to 10(-6 )mol) was examined. In order to evaluate the effects of acute opioid receptor blockade, additional groups of animals were treated by acute single intraperitoneal naltrexone injection (20 mg/kg). Plasma level of nitrite/nitrate as an indicator for nitric oxide production was measured. Biliary cirrhosis was accompanied with a decrease in baseline perfusion pressure in mesenteric vascular bed (P < 0.01). Chronic opioid receptor blockade significantly increased this parameter (P < 0.01). The maximum pressure response to phenylephrine was decreased significantly in cirrhosis while chronic naltrexone treatment completely improved it (P < 0.01). Acute single injection of naltrexone could not influence the understudied homodynamic parameters. Chronic opioid receptor blockade did not modulate the increased nitrite/nitrate levels following cholestasis. This study provided evidence on the contribution of endogenous opioid system to vascular hyporesponsiveness in cirrhosis which is not directly correlated to high plasma NO levels.
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PMID:Opioid receptor blockade improves mesenteric responsiveness in biliary cirrhosis. 1846 46

The incidence of mycotic infections is on the rise in the United States. The failure of patients and clinicians to recognize a fungal infection early may lead to extensive, severe, and difficult-to-treat disease. Treatment decisions must include an awareness of the etiologic organism involved, the potential for long-term recurrence, symptoms such as inflammation and itching, and the importance of patient adherence to treatment. Sertaconazole nitrate, a broad-spectrum imidazole agent with antifungal, antibacterial, antiinflammatory, and antipruritic properties, is the topical antifungal agent most recently approved by the US Food and Drug Administration. A review of its mechanisms of action, pharmacokinetic profile, fungistatic and fungicidal activities, and clinical properties examines a substantial body of research findings that establish its efficacy, safety, and tolerability. Its use in the treatment of tinea pedis and other superficial mycotic infections is reviewed here.
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PMID:Comprehensive management of patients with superficial fungal infections: the role of sertaconazole nitrate. 1869 45

Dermatomycoses are contagious superficial fungal infections, which are highly prevalent in developed and developing countries. Caused by a range of Epidermophyton, Microsporum and Trichophyton species, dermatomycoses manifest on glabrous skin as 'ringworm', an annular scaly lesion with a variable inflammatory component. Itch is the chief subjective symptom, particularly in tinea cruris. Unless lesions are extensive or resistant to local therapy, dermatomycoses of glabrous skin are treated with topical antifungal agents, such as imidazoles and allylamines. Studies show, however, that the addition of a topical corticosteroid to imidazole therapy increases the bioavailability and prolongs the activity of the antimycotic, while rapidly reducing inflammatory symptoms. Travocort is a combination of 1% isoconazole nitrate (ISN), a broad-spectrum imidazole with established antimicrobial activity and antimycotic efficacy, and 0.1% diflucortolone valerate (DFV), a potent topical corticosteroid with low systemic absorption and therefore a low risk of systemic glucocorticoid side-effects. In randomised, double-blind controlled clinical trials, Travocort therapy showed a more rapid onset of action, faster relief of itch and other inflammatory symptoms, improved overall therapeutic benefits and better mycological cure rate during the first 2 weeks of treatment compared with ISN monotherapy. Travocort is well tolerated and, because of prolonged ISN retention in the skin, provides antifungal protection against reinfection for some weeks after therapy.
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PMID:The advantages of topical combination therapy in the treatment of inflammatory dermatomycoses. 1878 60

The efficacy of 2% creams of miconazole nitrate and sertaconazole were compared in a double-blind clinical trial carried out on 100 patients with an established diagnosis of cutaneous dermatophytosis. Assessments were performed on days 0, 15, 29 and 43 in our dermatology clinic. Cure was defined according to clinical assessment confirmed by microscopical examination and culture. The groups were similar in age, gender, weight and clinical presentation. The reported side-effects, most commonly pruritus, occurred in 22 (40.0%) and 15 (33.3%) patients in the sertaconazole and miconazole groups, respectively (P = 0.28), but were not serious enough to stop the treatment. The only significant difference between the groups was in per-protocol cure rate by day 15, when patients in the sertaconazole group had a higher cure rate than the miconazole group (P < 0.01). In conclusion, sertaconazole was superior to miconazole in producing an early response in our patients. Given the higher price of sertaconazole and the ability of the considerably less expensive miconazole to produce equally good response after a month, the usefulness of sertaconazole as an alternative to miconazole in Iran requires further study.
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PMID:Sertaconazole 2% cream vs. miconazole 2% cream for cutaneous mycoses: a double-blind clinical trial. 1979 95

Tinea pedis typically presents as a pruritic, erythematous, and scaly eruption on the foot, with symptoms correlated with the severity of infection. Although many clinical studies have assessed the antifungal action of various agents, relatively little attention has been devoted to evaluating if antifungal agents are capable of improving subjective symptoms while treating the infection. A single-center, open-label, observational, proof of concept study was conducted in 21 participants (age range, 16-74 years) to evaluate if sertaconazole nitrate cream 2% used twice daily for 7 days was able to reduce participants' perceived itching while treating the infection. Findings included participants' overall assessment of quality of life (QOL) with the Dermatology Life Quality Index (DLQI) and participants' overall satisfaction with treatment. The pruritus visual analog scale (VAS) was used to assess the subjective symptom of itching. Results indicated the mean total score of changes in perception of QOL was 8.95 at baseline and 3.38 at day 7, a within-group change of -5.57 (P < .0001), and the mean reduction in reported itching from baseline to day 7 was -63.10% (P < .0001). Fifteen of 21 participants (71.4%) were somewhat or very satisfied with the results of their treatment. The implication of these findings is that successful elimination of the inflammatory symptoms of tinea. pedis, such as pruritus, may promote adherence to therapy by directly affecting participants' perception of QOL. Furthermore, early and rapid relief of symptoms, as seen in this study, may encourage patients to continue therapy for the full recommended period of 4 to 6 weeks, thereby reducing the risk for relapse that leads to chronic disease.
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PMID:Observational evaluation of sertaconazole nitrate cream 2% in the treatment of pruritus related to tinea pedis. 2009 22

Sertaconazole nitrate is a broad-spectrum antifungal agent indicated in the United States for the treatment of tinea pedis interdigitalis. The objective of this subgroup analysis was to evaluate the safety and efficacy of sertaconazole nitrate cream 2%, specifically in participants with tinea pedis interdigitalis (ie, fungal skin disease of the toe web) of dermatophyte origin. A total of 92 participants were included in this analysis. The primary end points were eradication of the pathogen (confirmed by fungal culture results) and reduction in total clinical score (TCS) of at least 2 points. Secondary end points included reducing signs and symptoms and reporting adverse events (AEs). After 4 weeks of treatment, 88.8% (79/89) of evaluable participants achieved success on the primary end points. Most participants also demonstrated substantial improvement in signs and symptoms after 4 weeks of treatment: 63.7% (58/91) were free of erythema, 33.0% (30/91) were free of desquamation, and 91.2% (83/91) were free of itch. The rate of reported AEs was low (8.7% [8/92]), and none were considered serious. These findings indicate that sertaconazole nitrate cream 2% is highly safe and effective in the treatment of tinea pedis interdigitalis.
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PMID:Safety and efficacy of sertaconazole nitrate cream 2% in the treatment of tinea pedis interdigitalis: a subgroup analysis. 2034 85

Antiallergic activity of Aristolochia bracteolata was evaluated by using compound 48/80 induced anaphylaxis, dermatitis rhinitis and pruritus, as a preclinical model for acute phase of hypersensitivity reactions. The late phase hypersensitivity was evidenced by considering toluidine diisocyanate induced volume of bronchoalveolar fluid secretion and its inhibition. The possible antiallergic mechanism was evaluated by using compound 48/80 induced mast cell activation and estimated serum nitric oxide (NO), rat peritoneal fluid NO, bronchoalveolar fluid NO and blood histamine levels. The present study implied that the chloroform extract of Aristolochia bracteolata had potent and significant inhibitory effect on compound 48/80 induced pruritus and dermatitis activity in Swiss albino mice. It showed significant effect in toluidine diisocyanate induced rhinitis in swiss albino mice. Mast cell membrane stabilization activity was also observed in compound 48/80 induced mast cell activation. A significant reduction was observed in serum nitrate levels, rat peritoneal fluid nitrate levels and BAL nitrate levels. The extract was also found to possess significant inhibitory effect on blood histamine levels. It could be concluded that chloroform extract of A. bracteata possess potent antiallergic activity, possibly through mast cell membrane stabilization, inhibiting NO and histamine pathway.
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PMID:Antiallergic activity of Aristolochia bracteolata Lank in animal model. 2035 66

Prostaglandin D(2) (PGD(2)) is known to have antipruritic activity by suppressing histamine release. However, agents that can topically induce PGD(2) for itch relief are not well established. The antimycotic sertaconazole nitrate (STZ) has been shown to exhibit anti-itch properties; however, the mechanism for this activity has not been elucidated. STZ mitigated degranulation of RBL-2H3 (rat basophilic leukemia) mast cells induced by compound 48/80, a pruritogenic agent known to promote the release of histamine, and augmented PGD(2) production in mast cells and macrophages. Addition of exogenous PGD(2) abrogated compound 48/80-induced degranulation by acting through the prostanoid D receptor 1 (DP1). STZ induced p38 mitogen-activated protein kinase (MAPK) phosphorylation in mast cells and a pharmacological inhibitor of p38 MAPK, SB203580, resulted in the attenuation of PGD(2) levels. Finally, in a murine model of pruritus, the scratching behavior induced by compound 48/80 was mitigated by topical application of STZ. This effect was reversed by the addition of the cyclooxygenase inhibitor, ibuprofen, or a DP1 receptor antagonist (MK0524). Collectively, these results suggest that STZ mediates its anti-itch effects by boosting the antipruritic agent, PGD(2), by the activation of the p38-MAPK pathway. This is the first report to demonstrate a promising approach to topically induce PGD(2) for improving pruritus.
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PMID:Induction of prostaglandin D2 through the p38 MAPK pathway is responsible for the antipruritic activity of sertaconazole nitrate. 2050 47


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