The stable quality of hospital preparations is the basis for their clinical efficacy. Gynecological antipruritic prescription is widely used in gynecology clinics of Chinese medicine hospitals. Therefore,in this study,the production process of gynecological antipruritic lotion was optimized based on the concept of quality by design( QbD). The production process of the gynecological antipruritic lotion was developed to ensure its process stability and reliable quality,and enhance its clinical applicability. With total amount of matrine and oxymatrine used as the critical quality attribute( CQA) of the production process,parameter levels were designed based on production practice of hospital preparations,and Plackett-Burman and Box-Behnken experiments were used to optimize the water extraction and alcohol precipitation process of antipruritic lotion based on CQA of intermediates and final product. The soaking time,the first extraction time,and the second extraction time were determined as the critical process parameters( CPPs) of the production process. The optimal preparation process was as follows: water volume of 8 times,soaking for 0. 5 h,extraction for 2 times,the first extraction for 30 min,the second extraction for 56 min,alcohol concentration of 50%,and alcohol precipitation for 3 h. Furthermore,the design space was established based on the binomial regress model between CPPs and CQA,so as to set the optimization target and risk range; and the control space was displayed by overlay plot. The results of three repeated experiments in the control space showed that the relative standard deviation( RSD) of CQA was 4. 70%,and the similarity of chromatogram for gynecological antipruritic lotion was 0. 978,0. 974,and 0. 998,respectively. The above results indicated that the operation in the control space can guarantee the quality and stability of gynecological antipruritic lotion,suitable for practical application.
Antipruritics ; Drugs, Chinese Herbal ; Water

Pruritus or itching is an unpleasant sensation well know to all of us which provokes the desire to scratch, usually lasting for minutes in hours and related to cutaneous diseases. However, generalized idiopathic pruritus may affect large areas, last longer, from months to years. Generalized pruritus can often be the primary manifestation of systemic diseases. Pruritus shares many features and pathways with pain but is a separate sensation from pain with its own precipitants and blockers. For example, loss of touch sensitivity dose not stop itching(e.g.,tabes dorsalis), however, in an area insensitive to pain, itching does not occur(e.g.,syringomyelia, leprosy). Unlike pain, specific receptors for pruritus and clear pathways for its transmission have not yet been identified. Until now, it has not been possible to isolate a universal mediator to explain pruritus. There are a wide variety of chemical substances known to be the mediators of pruritus. Well known among these is histamine, but in most cases of generalized pruritus is is not the main cases of generalized pruritus it is not the main mediatro. Our lack of understanding of the mechanism of pruritus is reflected by the inefficiency of many of the available antipruritic agents. I herein present an update review of the pathophysiology of pruritus, possible causes of generalized pruritus, the differential diagnosis and the basic principles of treatment.
Antipruritics ; Diagnosis, Differential ; Histamine ; Pruritus* ; Sensation

BACKGROUND: Severe pruritus is a challenging condition, and it is more difficult to deal with in older patients due to their limitations in taking oral medication because of underlying diseases, possible interaction with concurrent medications, and poor general condition. OBJECTIVE: We evaluated the efficacy and safety of naltrexone (Revia®), an opioid antagonist, in elderly patients with severe pruritus that was not easily controlled with conventional antipruritics. METHODS: Eighteen patients were enrolled, with a mean age of 73 years. They additionally received 50 mg of naltrexone per day for an average of 2 months. RESULTS: Using the visual analogue scale, 13 (72.2%) of 18 patients showed a "much improved" condition, reporting more than a 50% decrease in pruritus intensity. Sixteen (88.9%) showed symptomatic improvement, and only 2 (11.1%) had persistent pruritus. Five patients reported side effects including insomnia, fatigue, constipation, and anorexia. However, reactions were either limited to the first 2 weeks or well managed. CONCLUSION: Naltrexone could be an effective and safe alternative treatment option to control severe pruritus in older patients.
Aged ; Anorexia ; Antipruritics ; Constipation ; Fatigue ; Humans ; Naltrexone* ; Pruritus* ; Sleep Initiation and Maintenance Disorders

BACKGROUND: Since the treatment guidelines for atopic dermatitis (AD) were released by the Korean Atopic Dermatitis Association (KADA) work group in 2006, there have been several advances in AD management. OBJECTIVE: We aimed to establish updated evidence- and experience-based treatment guidelines for Korean AD. METHODS: We collected a database of references from relevant systematic AD reviews and guidelines regarding general AD management such as bathing and skin care, avoidance of exacerbating factors, education and psychosocial support, and the use of moisturizers and topical anti-inflammatory and antipruritic drugs. Evidence for each statement was graded and the strength of the recommendation for each statement classified. Thirty-nine KADA council members participated in three rounds of voting to establish an expert consensus of recommendations. RESULTS: Basic AD treatment includes proper bathing and skin care, avoidance of exacerbating factors, proper education and psychosocial support, and use of moisturizers. The regular use of moisturizer has a steroid-sparing effect and reduces relapse episodes. The short- and long-term use of topical corticosteroids and calcineurin inhibitors improves AD symptoms and should be encouraged to use in an active and proactive treatment. Wet-wrap therapy can be used for rapid recovery of acute exacerbation. Topical antipruritic drugs cannot be recommended for the treatment of AD. CONCLUSION: This report provides up-to-date evidence- and experience-based treatment guidelines for AD regarding general management and topical treatment. In addition, the average agreement scores obtained by a panel of experts based on the Korean healthcare system and patient adherence are presented.
Adrenal Cortex Hormones ; Antipruritics ; Baths ; Calcineurin ; Consensus* ; Delivery of Health Care ; Dermatitis, Atopic* ; Education ; Korea* ; Patient Compliance ; Politics ; Recurrence ; Skin Care

BACKGROUND: Since the treatment guidelines for atopic dermatitis (AD) were released by the Korean Atopic Dermatitis Association (KADA) work group in 2006, there have been several advances in AD management. OBJECTIVE: We aimed to establish updated evidence- and experience-based treatment guidelines for Korean AD. METHODS: We collected a database of references from relevant systematic AD reviews and guidelines regarding general AD management such as bathing and skin care, avoidance of exacerbating factors, education and psychosocial support, and the use of moisturizers and topical anti-inflammatory and antipruritic drugs. Evidence for each statement was graded and the strength of the recommendation for each statement classified. Thirty-nine KADA council members participated in three rounds of voting to establish an expert consensus of recommendations. RESULTS: Basic AD treatment includes proper bathing and skin care, avoidance of exacerbating factors, proper education and psychosocial support, and use of moisturizers. The regular use of moisturizer has a steroid-sparing effect and reduces relapse episodes. The short- and long-term use of topical corticosteroids and calcineurin inhibitors improves AD symptoms and should be encouraged to use in an active and proactive treatment. Wet-wrap therapy can be used for rapid recovery of acute exacerbation. Topical antipruritic drugs cannot be recommended for the treatment of AD. CONCLUSION: This report provides up-to-date evidence- and experience-based treatment guidelines for AD regarding general management and topical treatment. In addition, the average agreement scores obtained by a panel of experts based on the Korean healthcare system and patient adherence are presented.
Adrenal Cortex Hormones ; Antipruritics ; Baths ; Calcineurin ; Consensus* ; Delivery of Health Care ; Dermatitis, Atopic* ; Education ; Korea* ; Patient Compliance ; Politics ; Recurrence ; Skin Care

The neurophysiology of itch, the dominant symptom of skin disease, has previously received scant attention. Recent advances in the neurophysiology and molecular basis of itch include the use of microneurography to demonstrate the existence of a subset of itch-dedicated afferent C neurons distinct from neurons which transmit pain; use of functional positron emission tomography (PET) and magnetic resonance imaging (MRI) of the brain to reveal an itch-specific activation matrix, and new evidence of a functional "dialogue" between C neuron terminals and dermal mast cells in which recently described proteinase-activated receptor type 2 (PAR2) and transient receptor potential vanilloid 1 (TRPV1) receptors, proteases and endovanilloids play a major role. As a necessary prerequisite to diagnosis and management, a pathophysiologically based classification of itch is proposed. Recent advances in understanding of the pathomechanisms of itch of cholestasis include the role of opioids and opioid antagonists. Focusing on neurogenic itch (itch without visible rash), common causes are reviewed and guidelines for laboratory and radiological investigation are proposed. A stepwise approach to management of generalised itch is recommended, including broadband or narrow band ultraviolet (UV), tricyclics such as doxepin, opioid antagonists including naltrexone and selective serotonin reuptake inhibitors (SSRIs) such as paroxetine. For troublesome localised itches such as insect bite reactions, physical urticaria, lichen simplex chronicus or, less commonly, notalgia paraesthetica, brachioradial pruritus, local cooling devices which rely on the cooling action of dimethyl ethers on thermosensitive TRP voltage-sensitive ion channels are now commercially available for shortterm relief.
Antipruritics ; therapeutic use ; Diagnosis, Differential ; Diagnostic Imaging ; methods ; Humans ; Neurons, Afferent ; physiology ; Pruritus ; diagnosis ; physiopathology ; therapy ; Treatment Outcome ; Ultraviolet Therapy ; methods

OBJECTIVETo investigate the antipruritic mechanisms of pimecrolimus cream for women facial dermatitis.

METHODSTopical pimecrolimus cream 1% was applied in 52 women patients with facial dermatitis. The Investigators Global Assessment (IGA) score, severity of pruritus (SP) scores, and a basic syntax and molecular substrate (molecular psychophysics) of nociception and pruriception established by temperature-sensitive transient receptor potential (TRP) channels were used to evaluate the clinical signs, severity of pruritus, and skin sensory phenomenon.

RESULTSThe IGA scores at day 1 and 4 of treatment and the SP score at day 1, 4, and 11 of treatment were significantly lower than the baseline scores before treatment (P < 0.05). Among these 52 patients, 28 (53.8%) showed positive capsaicin-like response (i.e., burning with consequent rapid amelioration of pruritus) at the application sites, 12 (23.1%) showed camphor-like response (i.e., warming with consequent rapid amelioration of pruritus), and 12 (23.1%) showed negative capsaicin-like response or negative camphor-like response.

CONCLUSIONSTreatment with pimecrolimus cream 1% can rapidly and effectively improve the signs and symptoms of facial dermatitis in adult women patients. Pimecrolimus cream 1% may act on the transient potential vanilloid 1 (TRPV1) receptor in the skin sensory afferents to induce capsaicin-like response or camphor-like response and then desensitizes TRPV1 and rapidly inhibits or alleviate itching.

Administration, Topical ; Adolescent ; Adult ; Antipruritics ; administration & dosage ; Dermatitis ; complications ; drug therapy ; Face ; Female ; Humans ; Middle Aged ; Pruritus ; drug therapy ; etiology ; Tacrolimus ; administration & dosage ; analogs & derivatives ; Young Adult

The mainstay therapy against leishmaniasis is still pentavalent antimonial drugs; however, the rate of antimony resistance is increasing in endemic regions such as Iran. Understanding the molecular basis of resistance to antimonials could be helpful to improve treatment strategies. This study aimed to recognize genes involved in antimony resistance of Leishmania tropica field isolates. Sensitive and resistant L. tropica parasites were isolated from anthroponotic cutaneous leishmaniasis patients and drug susceptibility of parasites to meglumine antimoniate (Glucantime(R)) was confirmed using in vitro assay. Then, complementary DNA-amplified fragment length polymorphism (cDNA-AFLP) and real-time reverse transcriptase-PCR (RT-PCR) approaches were utilized on mRNAs from resistant and sensitive L. tropica isolates. We identified 2 known genes, ubiquitin implicated in protein degradation and amino acid permease (AAP3) involved in arginine uptake. Also, we identified 1 gene encoding hypothetical protein. Real-time RT-PCR revealed a significant upregulation of ubiquitin (2.54-fold), and AAP3 (2.86-fold) (P<0.05) in a resistant isolate compared to a sensitive one. Our results suggest that overexpression of ubiquitin and AAP3 could potentially implicated in natural antimony resistance.
Amino Acid Transport Systems/*genetics/metabolism ; Antimony/*pharmacology ; Antipruritics/*pharmacology ; *Drug Resistance ; Humans ; Leishmania tropica/drug effects/enzymology/*genetics/isolation & purification ; Leishmaniasis, Cutaneous/*parasitology ; Protozoan Proteins/*genetics/metabolism ; Ubiquitin/*genetics/metabolism

Airway remodeling is an important pathological feature of asthma and the basis of severe asthma. Proliferation of airway smooth muscle cells (ASMCs) is a major contributor to airway remodeling. As an important Ca(2+) channel, transient receptor potential vanilloid 1 (TRPV1) plays the key role in the cell pathological and physiological processes. This study investigated the expression and activity of TRPV1 channel, and further clarified the effect of TRPV1 channel on the ASMCs proliferation and apoptosis in order to provide the scientific basis to treat asthmatic airway remodeling in clinical practice. Immunofluorescence staining and reverse transcription polymerase chain reaction (RT-PCR) were used to detect the expression of TRPV1 in rat ASMCs. Intracellular Ca(2+) was detected using the single cell confocal fluorescence microscopy measurement loaded with Fluo-4/AM. The cell cycles were observed by flow cytometry. MTT assay and Hoechst 33258 staining were used to detect the proliferation and apoptosis of ASMCs in rats respectively. The data showed that: (1) TRPV1 channel was present in rat ASMCs. (2) TRPV1 channel agonist, capsaicin, increased the Ca(2+) influx in a concentration-dependent manner (EC50=284.3±58 nmol/L). TRPV1 channel antagonist, capsazepine, inhibited Ca(2+) influx in rat ASMCs. (3) Capsaicin significantly increased the percentage of S+G2M ASMCs and the absorbance of MTT assay. Capsazepine had the opposite effect. (4) Capsaicin significantly inhibited the apoptosis, whereas capsazepine had the opposite effect. These results suggest that TRPV1 is present and mediates Ca(2+) influx in rat ASMCs. TRPV1 activity stimulates proliferation of ASMCs in rats.
Animals ; Antipruritics ; pharmacology ; Apoptosis ; physiology ; Bronchi ; cytology ; metabolism ; Calcium Signaling ; drug effects ; physiology ; Capsaicin ; analogs & derivatives ; pharmacology ; Cell Proliferation ; Myocytes, Smooth Muscle ; cytology ; metabolism ; Rats ; Rats, Sprague-Dawley ; TRPV Cation Channels ; antagonists & inhibitors ; metabolism