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PubMed1996

A model to assess the effectiveness of topical antipruritics.

A model has been developed to determine the effectiveness of topical antipruritics. It utilizes controlled, experimentally induced itch and has demonstrated the effectiveness of the direct action on cutaneous receptor sites of a topical anesthetic, benzocaine, in a topical antipruritic formulation, and has been used to differentiate between two effective topical antipruritics. Three studies are presented: The first study examined the reliability of the experimentally induced itch. Several indices of reliability were computed from the data of this first study. Cronbach's alpha was 0.92. Winer's theta also was 0.92. Simple test-retest reliability, computed at intervals of 29 min, 1 day, and 6-7 days, resulted in Pearson correlations of 0.84, 0.73, and 0.60, respectively. In the second study, the model differentiated statistically between the itch relief resulting from the topical application of a formulation with 6% benzocaine and the same formulation without benzocaine. The third study examined 2 known topical antipruritics: one containing 6% benzocaine and the other 1% hydrocortisone. Both topical antipruritics were found to relieve itch; however, the benzocaine antipruritic produced statistically significantly greater itch relief in more subjects than the hydrocortisone antipruritic at both 1 and 30 min after application. These results demonstrate that OTC antipruritics can be differentiated for effectiveness.

Administration, Topical↗
PubMed1988

Evaluation of a new method of assessing pruritus and antipruritic drugs.

A new method (Pain-Track) for recording subjective symptoms was evaluated for its capacity to quantify clinical itch. The Pain-Track system includes portable data loggers carried by the patients, a personal computer with a software package for storage and analysis of the data and a terminal unit to connect the loggers and computer. Every 60 min a signal from the logger commands the patient to mark his presence and rate the itch intensity. During night time the hourly buzz can be turned off but the intensity rate can be adjusted whenever wanted. The antipruritic effect of betamethasone dipropionate and its cream base was studied according to a double-blind, crossover protocol in 30 adult outpatients with atopic dermatitis, 26 of whom completed the study. Analysis with parametric and nonparametric methods showed that the itch intensity was significantly lower during active treatment than with placebo. Onset of the antipruritic action was rapid. Examination of the 'itch profile' revealed that atopics have more intense itch both in the mornings and evenings than during the day. It is concluded that by using a drug with known antipruritic effect we have shown that Pain-Track is a useful tool for assessing clinical pruritus and the antipruritic effects of drugs. The main advantages are possibilities for frequent recordings, surveillance of compliance improving authenticity, and storage and analysis of a large amount of data.

Adult↗
PubMed1995

The antipruritic effects of chlorpheniramine, cyproheptadine and sulphapyridine monitored with limb activity meters on chloroquine induced pruritus among patients with malaria.

Limb activity meters, otherwise modified self-winding watches that can record limb agitative movements such as in itch-provoked scratch, were introduced for an objective evaluation of the relative effectiveness of three antipruritic drugs: chlorpheniramine, cyproheptadine, and sulphapyridine for palliating pruritus associated with chloroquine chemosuppressive treatment of acute malarial febrile paroxysms in eighteen adult patients. Six fit and healthy subjects were also studied to obtain data for unmedicated controls. The meters were used to monitor the upper and lower limb activities of the patients during nocturnal sleep for 6 hours over 3 consecutive nights, after they had developed the chloroquine-induced pruritus and were then administered the antipruritic medications, six patients per drug, by a random selection. Sulphapyridine antipruritic treatment significantly reduced the activities of the upper limbs of itchy patients much greater than did cyproheptadine (P < 0.0001, right hand; P < 0.01 left hand). However sulphapyridine-treated patients still itched significantly more than controls from the greater activities in the dominant right hand of the patients (P < 0.05). Cyproheptadine had a marginally-better performance than chlorpheniramine, generally, in palliating the chloroquine-induced pruritus but only in one of 3 nights, for the right hand recordings, were the limb activities significantly different. There was no significant difference observed in the activities of the lower limbs for the unmedicated controls compared to itchy patients, irrespective of the antipruritic treatment mode. Five out of the 6 patients treated with sulphapyridine also complained of anorexia plus a feeling of fullness or indigestion.(ABSTRACT TRUNCATED AT 250 WORDS)

Adolescent↗
PubMedDate not supplied

Antipruritic action of thalidomide.

The effect of thalidomide on itch was studied in 11 patients with chronic pruritus from psoriasis, eczema, nodular prurigo, senile pruritus and primary biliary cirrhosis. Itch, assessed subjectively by the patients on a 10 cm line and measured objectively as nocturnal scratch movement, was decreased by thalidomide 200 mg on the 2 nights it was given. There was no improvement in the underlying disorders and it is concluded that thalidomide is a primary antipruritic agent. The patients all became drowsy and it seems likely that, as with most other antipruritic agents, the antipruritic action of thalidomide results from a central depressant effect. The primary antipruritic effect of thalidomide should now be assessed therapeutically.

Adult↗
PubMed1983

An animal model for preclinical screening of systemic antipruritic agents.

Reliable antipruritic agents that can be given systemically are not available at present. This may be due to the lack of animal models for screening such compounds. Bombesin, a tetradecapeptide originally isolated from frog skin, induces dose-related excessive scratching when administered intracerebroventricularly (i.c.v.) to rats. With the help of a microcomputer, we monitored the scratching elicited by a standard, submaximal dose of bombesin (0.10 microgram, i.c.v.). This system provides 1) a sensitive and novel way of assessing drug-induced behavioral depression, and 2) a means of quantifying interactions between bombesin and possible antagonists. Thus, bombesin-induced grooming is antagonized by behaviorally nondepressant doses of methdilazine, trimeprazine, and chlorpromazine but not by morphine, haloperidol, diphenhydramine, hydroxyzine, mepyramine, cimetidine, or cyproheptadine. Methdilazine and trimeprazine are used clinically as antipruritic agents. The model therefore offers a means of evaluating new, systemic antipruritic agents, particularly those which may be active in treating histamine-independent pruritus.

Animals↗
PubMed2005

Antipruritic effect of the single oral administration of German chamomile flower extract and its combined effect with antiallergic agents in ddY mice.

The single peroral administration of the ethyl acetate extract or essential oil of German chamomile (Matricaria recutita L.) showed remarkable antipruritic effects in the compound 48/80-induced itch-scratching test in ddY mice, if suitable vehicle was used. The ethyl acetate extract or essential oil of German chamomile dissolved in the vehicle of 10% ethanol, 10% Tween 80 and 80% physiological saline was orally administrated 2 h before pruritus provocation by compound 48/80 subcutaneous injection. The ethyl acetate extract or essential oil of German chamomile showed significant dose-dependent inhibition of the compound 48/80-induced scratching without affecting spontaneous motor activity. The antipruritic effects of antihistamine H1 antagonists, oxatomide (10 mg/kg) and fexofenadine (10 mg/kg), were only partial in this test. However, the antipruritic effects of these agents were remarkably enhanced by the combined administration of the ethyl acetate extract of German chamomile (300 mg/kg). Thus, the co-medication with the ethyl acetate extract, or essential oil of German chamomile and antihistamines might be effective for the pruritus which could not be perfectly resolved alone by conventional antihistamines.

Administration, Oral↗
PubMed2004

Over-the-counter topical antipruritic agents are commonly recommended by office-based physicians: an analysis of US practice patterns.

BACKGROUND: Pruritus is one of the most common complaints among patients who visit physicians. Over-the-counter topical antipruritic medications are widely recommended by physicians and are self-administered by patients for the treatment of pruritus. However, there are few scientific controlled studies evaluating the effect of these drugs on pruritus. OBJECTIVES: To assess the role of physician-recommended over-the-counter medications for the treatment of pruritus. METHODS: Records were analyzed for office-based physician visits in which over-the-counter antipruritic topical medications were recommended in the National Ambulatory Medical Care Survey between the years 1995 and 2000. RESULTS: The largest proportion of over-the-counter antipruritic agent recommendations were during visits to dermatologists, accounting for 41% of all such recommendations. Other physicians that recommended such agents included family physicians and pediatricians, accounting respectively for 26% and 21% of the recommendations. The most commonly recommended over-the-counter medications included hydrocortisone preparations (72%) and diphenhydramine (15%). Over-the-counter medications were more frequently recommended in the pediatric age group. CONCLUSION: This study demonstrates that over-the-counter medications are frequently recommended for the treatment of pruritus.

Adolescent↗
PubMed1983

Mechanism of action of antipruritic drugs.

Astemizole and terfenadine, two potent non-sedative H1 antihistamines, had no effect on itch measured objectively as nocturnal scratching and subjectively on a 10 cm line. Trimeprazine, however, a more sedative but less potent H1 antihistamine, was antipruritic, as was nitrazepam, a sedative benzodiazepine. We concluded (a) that antipruritic drugs act centrally by a property related to sedation; (b) H1 receptor antagonists have a peripheral antipruritic action only when itch is due to histamine release, as in the wealing disorders. Thus the new nonsedative H1 antihistamines have no place in the treatment of itch from other causes.

Adolescent↗
PubMedDate not supplied

Screening topical antipruritics: a histamine-induced itch human model.

Itch is a subjective symptom; its magnitude (intensity) may be only estimated by the reports of patients or volunteers. We utilized a comparative screening method to identify and quantify the efficacy of topical antipruritics with a histamine-induced itch human model. Ten individuals responsive to histamine-induced itch sensation were enrolled. Both forearms served as test sites. Each test site was treated randomly either by histamine injection only or pretreated with a coded candidate formula for 30 min and then a histamine injection. Itch was experimentally induced in each test site by the intracutaneous injection of 100 microg histamine dihydrochloride dissolved in 1 ml normal saline. Itch magnitude was measured each minute after histamine injection for 20 min with a magnitude visual analogue scale. Itch duration was also recorded. Formulation D significantly (p < 0.05) decreased itch magnitude (within a 20-min test period), from 2.6 +/- 2.1 cm (mean +/- SD) to 2.2 +/- 2.1 cm (mean +/- SD) when compared to its vehicle control; it also significantly (p < 0.05) shortened itch duration (15.0 +/- 7.4 min; mean +/- SD) in comparison with its vehicle control (20.3 +/- 7.0 min; mean +/- SD). Of all the formulations tested, formulation D was the most effective antipruritic in decreasing histamine-induced itch. This method may act as a simple and robust screening procedure when evaluating potential antipruritics and allow a comparison among products. Until validated with disease-induced itch, e.g., atopic dermatitis, the model should be considered screening in nature.

Administration, Cutaneous↗
PubMed1998

Studies on Kochiae Fructus. V. Antipruritic effects of oleanolic acid glycosides and the structure-requirement.

We examined the antipruritic effects of various oleanolic acid glycosides from natural medicines such as Kochiae Fructus (the fruit of Kochia scoparia SCHRAD.) and Momordicae Radix (the roots of Momordica cochinchinensis SPRENG.) using a compound 48/80-induced pruritic model in mice. Oleanolic acid 3-O-monodesmosides showed an antipruritic effect, while oleanolic acid 3,28-O-bisdesmosides and their common sapogenol oleanolic acid lacked the activity. This evidence indicated that the 3-O-glycoside moiety and the 28-carboxyl group in oleanolic acid glycosides were essential for exhibiting the antipruritic effect. Furthermore, it was found that the 3-O-glucuronides showed more potent activity than the corresponding 3-O-glucosides.

Animals↗
PubMed2000

Systemic drugs with antipruritic potency.

Despite the predominance of itch as a leading and distressing symptom in most of the dermatological and several systemic diseases, there is relatively little progress in understanding its pathophysiology. This is most likely the main reason for the limited number of satisfactory anti-itch treatments and the fact that even today various therapies have empirical but not evidence-based character. There are no specific antipruritic drugs on the market, but there are a high number of case reports and experimental investigations describing medications with antipruritic potency. It is therefore the aim of this article to briefly review the major systemic antipruritic drugs and give a short overview on the different types of pruritus and their possible systemic therapy.

Antipruritics↗
PubMed1996

[An animal model for screening of antiallergic and antipruritic drugs].

4-Aminopyridine(4-AP) 1 mg.kg-1 sc at the scruff induced a licking response in mice. Antiallergic and antipruritic drugs, such as diphenhydramine HCl(20 mg.kg-1 ip), doxepin(12.5 mg.kg-1 ig), prednisone(10 mg.kg-1 ig), dexamethasone(10 mg.kg-1 ip), fluocinolone (applied to the surface of skin), Pi Yan Ping(applied to the surface of skin), disodium cromoglicate(400 mg.kg-1 ip), ketotifen(1 mg.kg-1 ip), etc. markedly inhibited the licking response elicited by 4-AP. The calcium antagonist nifedipine(500 mg.kg-1 lg) and the potassium channel opener minoxidil(400 mg.kg-1 ig) produced the same inhibitory effect. H2-receptor antagonist cimetidine(200 mg.kg-1 ip) and ranitidine(150 mg.kg-1 ip) showed no effect. Morphine HCl(10 mg.kg-1 ip) and diazepam(0.02 mg.kg-1 ip) exhibited antagonistic effect on the licking response induced by 4-AP, but phenobarbital(25 mg.kg-1 ip), pentobarbital(15 mg.kg-1 ip) and aspirin(300 mg.kg-1 ig) did not. These results indicate that many antiallergic or antipruritic drugs inhibited the licking response induced by 4-AP. The method of licking response elicited by 4-AP has the merit of simplicity and convenience and may be used for screening antiallergic and antipruritic drugs.

4-Aminopyridine↗
PubMed1999

Antipruritic effect of DA-5018, a capsaicin derivative, in mice.

The antipruritic effect of DA-5018, a capsaicin derivative, was examined in mice. Male ICR mice were topically pretreated with Zostrix-HP (0.075% capsaicin cream), 0.1%, 0.3% DA-5018 cream or cream base (control) twice daily for 4 days. One hour after the last application, itch was induced either by compound 48/80 (50 microg, s.c.) or leukotriene B4 (0.03 nmol, i.d.) injection into the rostral back of the animals, and the number of scratches made by the animals at the injection site was counted for 60 min post-injection. DA-5018 cream (both 0.1 and 0.3%) significantly inhibited compound 48/80-induced scratching when compared with the cream base control (p<0.01), while Zostrix-HP showed minimal inhibition of the scratching behavior. In leukotriene B4-induced itch model, Zostrix-HP and 0.3% DA-5018 cream significantly inhibited the scratching during the first 10-min period (p<0.01). The results suggest that DA-5018 cream can be used as an antipruritic agent and warrant clinical evaluation.

Administration, Topical↗
PubMed2003

[Antipruritic effects of pimecrolimus and tacrolimus].

The development of topical calcineurin inhibitors resulted in a significant improvement in the treatment of inflammatory skin diseases such as atopic dermatitis. In addition, an excellent amelioration of pruritus could be observed. Other itchy dermatoses such as chronic irritative hand dermatitis, rosacea, graft-versus-host-disease, renal pruritus, lichen sclerosus, prurigo simplex, prurigo nodularis, scrotal eczema, and inverse psoriasis also have been treated successfully with pimecrolimus and tacrolimus. The antipruritic effect currently is believed to be related to the inhibition of inflammatory cytokines. Furthermore, recent investigations indicate a release of neuropeptides from sensory nerve fibers and degranulation of mast cells mediated by pimecrolimus and tacrolimus. Similar effects have been observed during capsaicin treatment. These findings may provide a possible explanation for initially observed calcineurin inhibitors related side-effects such as burning and pruritus. Moreover, the antipruritic potency may be related to a direct effect on nerve fibers leading to suppression of itch mediated by unknown mechanisms.

Administration, Topical↗
PubMed2005

Spontaneous scratching behavior in MRL/lpr mice, a possible model for pruritus in autoimmune diseases, and antipruritic activity of a novel kappa-opioid receptor agonist nalfurafine hydrochloride.

Pruritus is a common, distressing and difficult to manage complication of many autoimmune diseases. A suitable animal model of autoimmune disease associated pruritus would contribute to a better understanding of the pathophysiology of this symptom and lead to the development of safe and effective antipruritic agents. We noticed spontaneous scratching behavior in aged MRL/lpr mice, a model of autoimmune disease. This scratching behavior was observed in a specific pathogen-free environment and was more frequent in female mice. In contrast to animal models of dermatitis; NC/Nga mice, the serum IgE and IgG1 levels in MRL/lpr mice were not elevated. These features indicate that this scratching behavior is similar to human autoimmune disease associated pruritus. The antipruritic effects of an antihistamine (chlorpheniramine), an opioid receptor antagonist (naltrexone), and a novel kappa-opioid receptor agonist (nalfurafine hydrochloride [TRK-820]) were evaluated. The frequency of scratching was not reduced by oral administration of chlorpheniramine, suggesting that the behavior is antihistamine-resistant. The oral administration of nalfurafine and subcutaneously administered naltrexone inhibited the scratching behavior without causing gross behavioral changes. In conclusion, MRL/lpr mice scratching behavior is a suitable model of pruritus that occurs in autoimmune diseases, and nalfurafine was shown to be efficacious against this behavior suggesting that it may be beneficial in patients with autoimmune disease associated pruritus.

Age Factors↗
PubMed2002

Antipruritic and antihyperalgesic actions of loperamide and analogs.

Loperamide and three of its analogs were evaluated for their ability to inhibit binding to cloned human opioid receptor subtypes and to produce antipruritus and antinociception following local s.c. administration to rodents. All four compounds were fully efficacious agonists with affinities of 2 to 4 nM for the cloned human mu opioid receptor. Local s.c. injection of loperamide, ADL 01-0001 or ADL 01-0002 at the same site as the introduction of the pruritogenic compound 48/80 resulted in antipruritic activity in a mouse model of itch. Similarly, i.paw or i.pl. administration of compounds ADL 01-0001, ADL 01-0002 and ADL 01-0003 to inflamed paws caused potent antinociception, inhibiting late phase formalin-induced flinching, Freund's adjuvant-induced mechanical hyperalgesia and tape stripping-induced mechanical hyperalgesia. Loperamide and its analogs were efficacious in animal models of itch and inflammatory pain, and may have potential therapeutic utility as antipruritic and antihyperalgesic agents.

Analgesics↗
PubMed2004

Antipruritic effects of two different 5-HT3 receptor antagonists and an antihistamine in haemodialysis patients.

Pruritus is the most distressing symptom in haemodialysis (HD) patients. Its aetiology has not yet been delineated, and thus there are no good therapeutical options. Case reports and series attribute antipruritic potency to the serotonin receptor antagonists of the 5-HT3 type in renal pruritus. It was the aim of this study to investigate the antipruritic effect of two different 5-HT3 receptor antagonists and an antihistamine in 11 patients undergoing HD. Pruritus was induced by iontophoresis with serotonin and histamine and recorded before and after HD. These data were compared to those obtained after oral pretreatment with the 5-HT3 receptor antagonists tropisetron 5 mg and ondansetron 8 mg and the antihistamine cetirizine 10 mg. Ten healthy volunteers served as a control group. Vasocutaneous parameters (wheal and flare), skin temperature and alloknesis were also determined. Itching in HD patients and controls was not significantly diminished by oral pretreatment with the serotonin receptor antagonists. In controls, but not in HD patients, cetirizine significantly reduced itching, skin temperature and vasocutaneous parameters. Our data additionally demonstrate that there are no significant differences in vasocutaneous parameters, itching and alloknesis in HD patients before and after dialysis. We conclude that 5-HT3 receptor blockers such as tropisetron and ondansetron and the antihistamine cetirizine do not sufficiently reduce serotonin- and histamine-induced itching in haemodialyis patients.

Adult↗
PubMed1999

The antipruritic effect of a 5-HT3 receptor antagonist (tropisetron) is dependent on mast cell depletion--an experimental study.

The background of this study is that 5-HT3 receptor antagonists are reported to have an antipruritic effect in uremic and cholestatic pruritus. Recently, we could not confirm such an effect in healthy subjects under experimental conditions. Therefore, it was the aim of the present study to further evaluate a possible antipruritic effect of a 5-HT3 receptor antagonist (tropisetron) on serotonin- and histamine-induced itch before and after skin mast cell depletion in 10 healthy subjects. The results were compared to serotonin and histamine iontophoresis in non-pretreated and pretreated skin with an orally applied antihistamine (cetirizine). Skin mast cell depletion was performed by iontophoretical application of compound 48/80. Wheals and flares were planimetrically evaluated. Itching and burning sensations were rated on an analog scale over a 24-min period. The test protocol also comprised alloknesis, defined as induction of perifocal itch sensations by a mechanical stimulus. When serotonin was iontophoretically applied after mast cells had been depleted before, oral tropisetron resulted not only in significantly lower whealing, itching and alloknesis but also reduced flares. In contrast, after oral pretreatment with tropisetron histamine-induced reactions before and after mast cell depletion did not significantly change. Our study demonstrates that in this model, tropisetron as a 5-HT3 receptor antagonist does not effect histamine-induced itch but has a measurable effect in serotonin-induced reactions when mast cells were depleted before. From these data evidence now exists why tropisetron is to some extent effective in certain types of pruritus such as uremic pruritus, known for increased histamine liberation and increased serotonin levels as well as degranulated and diffusely spread mast cells in the skin.

Adult↗