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- Vaginal use of Ibuprofen isobutanolammonium (ginenorm): efficacy, tolerability, and pharmacokinetic data: a review of available data. [Journal Article]
- ISRN Obstet Gynecol 2012.:673131.
Vaginal infection and inflammation with or without vulvar involvement are very common gynecologicaly clinical conditions associated with morbidity and reduced quality of life. Vaginal infections are commonly treated with causal antimicrobial treatments. In addition to specific antimicrobial treatment, anti-inflammatory therapy, both systemic or topical (vaginal douche), could be useful in the integrated treatment approach of these conditions reducing symptoms and speeding up the recovery in vulvovaginitis. Ibuprofen is a well-known effective and well-tolerated anti-COX (anti-COX1 and COX2) compound. In addition, several in vitro studies suggest that Ibuprofen shares antimicrobial and antifungal activities. Ibuprofen isobutanolammonium (Ib-isb) (Ginenorm) is a soluble salt from formulation suitable for external and intravaginal use. This salt completely dissociates in aqueous solution. Ib-isob is available in sachet and vaginal douche pharmaceutical formulations. Clinical efficacy of Ib-isob has been documented in 10 clinical studies (6 controlled and 4 open trials) which have enrolled in total 399 women with vulvovaginitis. The six controlled clinical trials were performed both versus placebo (2 studies) or versus active comparators such as benzydamine. In these studied, Ib-Isb has been used in general for 7 consecutive days with a twice application daily regimen at the dose of 1 g per application. Topical application of Ib-isob induced a marked and rapid reduction in signs (erythema, oedema) and symptoms (itching and burning sensation) of vulvovaginitis. In head-to-head studies carried out in comparison with other topical products, Ib-isob induced a more rapid reduction in both subjective and objective symptoms. In particular a remarkable significant improvement of all the symptoms has been observed in the group of patients treated with Ib-isob in comparison with women receiving benzydamine. The clinical data available for Ib-isob confirm that this salt, specifically developed for gynecological use, is effective and well tolerated in vulvovaginal inflammation conditions. Efficacy of Ib-isob was greater in comparison with commonly used products. Ibuprofen-isob may be considered a useful and effective tool for the topical treatment of nonspecific vaginal diseases.
- Oral ingestion of a topical benzydamine hydrochloride-containing gynaecological preparation in association with television advertising in Italy: analysis of cases managed by a National Poison Control Centre. [Journal Article]
- BMJ Open 2012; 2(1):e000204.
Objective To evaluate the impact of a television advertising campaign on the risk of oral ingestion of a topical non-prescription gynaecological preparation containing benzydamine hydrochloride. Design An interrupted time series design with data routinely collected. Setting A National Poison Control Centre. Participants 215 cases of hazardous exposure to the preparation under study occurred in Italy from January 2005 to December 2010. Primary and secondary outcome measures Mean daily rate of cases of exposure by gender in three different periods, that is, pre-advertisement period, before the advertisement was broadcast (from 1 January 2005 to 19 December 2009), advertisement period, when the advertisement was repeatedly launched (from 20 December 2009 to 27 February 2010), post-advertisement period (from 28 February 2010 to 6 March 2010); observed/expected ratios of cases, with expected cases based on data from the pre-advertisement period, adjusted for estimated variations in the number of users. Comparison of the distribution of the main characteristics of cases in the three different periods by means of Pearson's χ(2) test or Fisher's exact test. Results The adjusted observed/expected ratio of cases in women was 7.48 (95% CI 5.76 to 9.56) in the advertisement period and 2.97 (95% CI 2.24 to 3.85) in the post-advertisement period. Regarding the characteristics of cases, there was an increased proportion of cases of exposure due to confusion about the correct administration route in the advertisement and post-advertisement periods (81% and 55%, respectively, compared to 16% for the pre-advertisement period.) and of individuals with clinical effects (55%, 52% and 27%, respectively). Conclusions In Italy, an advertisement for a non-prescription medicine seems to have confused consumers regarding the administration route. This effect was observed even after the advertisement had stopped being broadcast. These results highlight the need for the monitoring of medication errors and adverse effects before, during and after advertising.
- In vitro drug metabolism by C-terminally truncated human flavin-containing monooxygenase 3. [Journal Article]
- Biochem Pharmacol 2012 Feb 15; 83(4):551-8.
Human flavin-containing monooxygenase 3 (hFMO3) is a microsomal drug-metabolizing monooxygenase that catalyzes the NADPH-dependent oxygenation of a wide range of drugs and xenobiotics which contain a soft-nucleophiles, usually sulfur or nitrogen. As the release from the microsomal membranes can facilitate the in vitro experimental determination of drug metabolism by hFMO3, in this work we identified and eliminated the membrane anchoring sequence without affecting the activity of the enzyme and producing a soluble active enzyme. The truncated hFMO3 carrying a C-terminal deletion of 17 amino acids (tr-hFMO3) was expressed and purified from the cytosolic fraction. The tr-hFMO3 proves to be detached from the membrane, properly folded and fully active towards well-known marker substrates such as benzydamine and sulindac sulfide with measured apparent K(m) values of 45 ± 8 μM and 25 ± 4 μM, respectively. Its activity was further tested with newly discovered Aurora kinase inhibitors, Tozasertib and Danusertib, and compared to those of the wild type enzyme. The use of this soluble form of the hFMO3 enzyme as opposed to the usual microsomal preparations is advantageous for in vitro drug metabolism studies that are a requirement in the early phases of drug development by pharmaceutical industry.
- Efficacy of benzydamine hydrochloride, chlorhexidine, and povidone iodine in the treatment of oral mucositis among patients undergoing radiotherapy in head and neck malignancies: A drug trail. [Journal Article]
- Contemp Clin Dent 2011 Jan; 2(1):8-12.
Oral mucositis is a common and debilitating complication of radiotherapy, which is associated with significant morbidity. It is therefore extremely important that mucositis be prevented, or at least treated to reduce its severity and sequelae. The objective of the study was to manage oral mucositis induced by radiotherapy and to reduce pain by using Benzydamine hydrochloride (0.15%), Chlorhexidine (0.2%), and Povidone iodine (5%).Benzydamine hydrochloride was observed to be effective and delayed the development of severe form of mucositis and appears more efficient in the management of radiation-induced mucositis.Benzydamine hydrochloride (0.15%) is safe, well tolerated, helps not just in delaying the progression of mucositis but also reduces the intensity of pain.
- The effect of polyvinylpyrrolidone-sodium hyaluronate gel (Gelclair) on oral microbial colonization and pain control compared with other rinsing solutions in patients with oral mucositis after allogeneic stem cells transplantation. [Clinical Trial, Comparative Study, Journal Article]
- Med Sci Monit 2011 Oct; 17(10):CR572-6.
Gelclair is an oral lubricating gel used in the management of oral mucositis (OM). We evaluated its efficacy, tolerance and impact on oral cavity microbial colonization in patients with OM after allogeneic hematopoietic stem cells transplantation.Gelclair was administered in a group of 22 patients with active OM. A control group of 15 patients used other rinsing solutions (chlorhexidine, benzydamine, salvia). Tests with oral cavity swabs for microbiology analysis were performed once a week.The characteristics of OM in both groups were comparable, and rinsing solutions had satisfactory tolerability. There was no difference in the median improvement of oral intake and OM-related pain relief, which was assessed mostly as "slight effect". In the Gelclair group, the effect duration was longer (median 3 [0-5] vs. 1 [0-3] hours, p = 0.001). There was significant increase of Enterococcus faecalis and Candida sp. colonization of the oral cavity over the course of the hospitalization and significantly reduced incidence of such colonization in patients with OM in the Gelclair group: 1/22 (5%) vs. 6/15 (40%), p = 0.01. In vitro tests showed inhibited growth of Enterococcus faecalis and Candida sp. colonies within the area of the Gelclair application.Gelclair may be individually helpful in the management of OM and pain in patients after allogeneic stem cells transplantation. Its use did not lead to worsened oral bacterial and yeast colonization and probably even helped to protect mucosa from Enterococcus and Candida sp. Further studies based on larger cohorts are needed.
- Outcomes and safety of drug provocation tests. [Evaluation Studies, Journal Article]
- Allergy Asthma Proc 2011 Jul-Aug; 32(4):301-6.
Drug provocation tests (DPTs) are considered the gold standard for identifying adverse drug reactions (ADRs). The aim of this study was to analyze DPT results and discuss severe systemic reactions associated with them. This was a retrospective analysis of 500 patients with ADRs who sought treatment and were submitted to DPTs when indicated between 2006 and 2010. We performed DPTs according to the European Network for Drug Allergy recommendations. Single-blind, placebo-controlled DPTs were performed with antibiotics, local anesthetics, and nonsteroidal anti-inflammatory drugs, as well as with other drugs. Patient characteristics, DPT results, and reactions were analyzed. The sample comprised 198 patients (80.8% of whom were female patients) submitted to 243 DPTs. Ages ranged from 9 to 84 years (mean, 39.9 years). The 243 DPTs were performed with local anesthetics (n = 93), antibiotics (n = 19), acetaminophen (n = 44), benzydamine (n = 33), COX-2 inhibitors (n = 26), dipyrone (n = 7), aspirin (n = 4), or other drugs (n = 17). The results of 4 tests (1.6%) were inconclusive, whereas those of 10 (4.1%) revealed positive reactions to antibiotics (2/19), COX-2 inhibitors (2/26), acetaminophen (3/44), and local anesthetics (3/93). Two severe reactions were observed: cephalexin-induced anaphylactic shock and bupivacaine-induced anaphylaxis without shock. Four patients (2.0%) reacted to the placebo before administration of the drug. Drug provocation tests are safe for use in clinical practice but they should be placebo-controlled and should be performed under the supervision of an allergist. To confirm a presumptive diagnosis and to manage allergies appropriately, it is crucial to perform DPTs.
- Oral rinses, mouthwashes and sprays for improving recovery following tonsillectomy. [Journal Article, Meta-Analysis, Review]
- Cochrane Database Syst Rev 2011; (7):CD007806.
This is an update of a Cochrane Review first published in The Cochrane Library in Issue 1, 2010.Tonsillectomy is the surgical removal of lymphoid tissue, the palatine tonsil, which is located at the back of the throat. It is still commonly performed for patients who have recurrent bouts of acute tonsillitis. Although tonsillectomy is considered a fairly minor procedure, pain and bleeding are two of the most common complications; either may delay recovery and can on occasion lead to hospital readmission. Postoperative tonsillectomy medication should provide an adequate reduction in morbidity while minimising side effects, therefore topical agents would seem to be an ideal, safe option. A number of mouthwashes and topical sprays are available which offer pain relief or can help to reduce bleeding in the immediate postoperative period.To assess the effects of oral rinses, mouthwashes and sprays in improving recovery following tonsillectomy.We searched the Cochrane Ear, Nose and Throat Disorders Group Trials Register; the Cochrane Central Register of Controlled Trials (CENTRAL); PubMed; EMBASE; CINAHL; Web of Science; BIOSIS Previews; Cambridge Scientific Abstracts; ICTRP and additional sources for published and unpublished trials. The date of the most recent search was 22 April 2011.We included randomised controlled trials in which mouthwashes, used pre- and postoperatively, have been compared with placebo.Two review authors selected trials for inclusion, assessed the risk of bias and extracted data independently.We included six trials (528 participants; 397 children and 131 adults). The period of follow up ranged from 24 hours to two weeks. Few of the trials provided reliable data for the pre-specified primary outcomes and none for the secondary outcomes. Lidocaine spray appeared to be more effective than saline spray at reducing the severity of pain but only until the third postoperative day. A small number of participants experienced a burning or stinging sensation with benzydamine spray but not sufficient to discontinue usage.The risk of bias was high in most of the included trials and poor reporting quality and inadequate data did not permit comprehensive and reliable conclusions to be made. Future trials should be well-constructed and pay more attention to the methods used to assess outcomes, the timing of the assessments, and the quality of reporting and subsequent analysis of the data.
- Fluorescence quenching of biologically active carboxamide by aniline and carbon tetrachloride in different solvents using Stern-Volmer plots. [Journal Article]
- Spectrochim Acta A Mol Biomol Spectrosc 2011 Sep; 79(5):1985-91.
Fluorescence quenching of biologically active carboxamide namely (E)-2-(4-chlorobenzylideneamino)-N-(2-chlorophenyl)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide [ECNCTTC] by aniline and carbon tetrachloride (CCl4) quenchers in different solvents using steady state method and time resolved method using only one solvent has been carried out at room temperature to understand the role of quenching mechanisms. The Stern-Volmer plot has been found to be linear for all the solvents studied. The probability of quenching per encounter p (p') was determined in all the solvents and was found to be less than unity. Further, from the studies of rate parameters and life time measurements in n-heptane and cyclohexane with aniline and carbon tetrachloride as quenchers have been shown that, the phenomenon of quenching is generally governed by the well-known Stern-Volmer (S-V) plot. The activation energy Ea (or E'a) of quenching was determined using the literature values of activation energy of diffusion Ed and the experimentally determined values of p (or p'). It has been found that, the activation energy Ea (E'a) is greater than the activation energy for diffusion Ed in all solvents. Hence, from the magnitudes of Ea (or E'a) as well as p (or p') infer that, the quenching mechanism is not solely due to the material diffusion, but there is also contribution from the activation energy.
- Efficacy of topical benzydamine hydrochloride gel on oral mucosal ulcers: an in vivo animal study. [Comparative Study, Journal Article]
- Int J Oral Maxillofac Surg 2011 Sep; 40(9):973-8.
The aim of this study was to investigate the effect of benzydamine hydrochloride bioadhesive gel on healing of oral mucosal ulceration in an animal model. For in vivo determination of the effects of the bioadhesive gel, 36 rabbits were separated into three groups: the first group was treated with the gel formulation without active agent, the second group with the gel formulation containing benzydamine, and the third group received no treatment. Clinical healing was established by measuring the area of the ulcer in each test group on days 3, 6, 9 and 12. Histological healing was determined on the same days. Benzydamine containing gel applications resulted in a decrease in the ulcer area in 12 days (p=0.000). Histological evaluation showed that the benzydamine group had a higher mean histological score than the base and the control groups during the whole test period, and the difference between the benzydamine group and the control group was significant (p=0.04). The bioadhesive gel formulation of benzydamine hydrochloride showed a statistically significant increased rate of mucosal repair in this experimental standard mucosal wound animal study. It is a candidate for the topical treatment of oral mucosal ulcerative lesions.
- Characterization of enzyme activities of Cytochrome P450 enzymes, Flavin-dependent monooxygenases, N-acetyltransferases and UDP-glucuronyltransferases in human reconstructed epidermis and full-thickness skin models. [Journal Article, Research Support, Non-U.S. Gov't]
- Toxicol In Vitro 2011 Sep; 25(6):1209-14.
With the perspective to use human reconstructed skin models for genotoxicity testing which require metabolic activation of xenobiotics, this study aimed to characterize activities of biotransforming enzymes within two human reconstructed skin models, the epidermis model EpiDerm™ (MatTek) and the Phenion® Full-Thickness skin model Phenion®FT (Henkel). According to existing gene expression profiles, Cytochrome P450 (CYP) enzymes, Flavin-dependent monooxygenases (FMO), N-acetyltransferases (NAT) and UDP-glucuronyltransferases (UDP-GT) were investigated in S9 or microsomal fractions. CYP-catalyzed monooxygenation was assayed using 7-ethoxyresorufin, pentoxyresorufin and benzyloxyresorufin as substrates. FMO activity was tested using benzydamine. Conjugating activities of NAT and UDP-GT were determined by acetylation of p-aminobenzoic acid or glucuronation of 4-methylumbelliferone, respectively. Although CYPs were detected by expression profiling, no CYP activity was detected in either the epidermal nor the full-thickness reconstructed skin model while expression and activity of FMO, UDP-GT and NAT were demonstrated in both.