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- Pharmaceuticals and personal care products in a mesoscale subtropical watershed and their application as sewage markers. [JOURNAL ARTICLE]
- J Hazard Mater 2014 Sep 3.:696-705.
This study comprehensively analyzed 23 classes of 51 pharmaceuticals and personal care products (PPCPs) in the two major prongs of Jiulong River and its estuary in southeast China, where the levels of the targeted PPCPs were mostly unknown. For both Jiulong River and its estuary, nine PPCPs were detected with 100% detection frequencies including two anti-inflammatory and analgesic drugs (ketoprofen and diclofenac acid), a stimulant (caffeine), a plasticizer (bisphenol A), two preservatives (methyl paraben and propyl paraben), two antimicrobials (triclosan and triclocarban) and a β-blocks (metoprolol), among which bisphenol A and caffeine accounted for more than 60% in concentrations. PPCPs generally had higher concentrations in dry season than normal season and wet season, while certain PPCPs, such as UV filters, showed higher concentrations in wet season, which were presumed to be related to their usage patterns. The concentrations of PPCPs were significantly correlated to several quality parameters of the surface water. The selected sewage markers were also used to track sewage in the studied river and the ratios of easily removed markers and conservative markers were used to identify the contribution of raw or treated sewage input. From our result, Jiulong River and its estuary were likely polluted by potential discharge of raw sewage.
- Propyphenazone-based analogues as prodrugs and selective cyclooxygenase-2 inhibitors. [Journal Article]
- ACS Med Chem Lett 2014 Sep 11; 5(9):983-8.
Improving the gastrointestinal safety profile of nonsteroidal anti-inflammatory drugs (NSAIDs) is an important goal. Herein, we report two strategies, using the nonacidic propyphenazone structure, with potential to overcome the side effects of NSAIDs. Propyphenazone was employed to temporarily mask the free acid group of the widely used NSAIDs ibuprofen, diclofenac, and ketoprofen to develop three mutual prodrugs hypothesized to have minimal GI irritation. The three prodrugs exhibit in vivo anti-inflammatory and analgesic activities with improved potency over each parent drug when compared to a nonhydrolyzable control betahistine-propyphenazone (BET-MP). Additionally, ANT-MP formed by the irreversible coupling of propyphenazone and 4-aminoantipyrine, displayed exceptional COXII selectivity (COXII IC50 of 0.97 ± 0.04 μM, compared to no observed inhibition of COXI at 160 μM). Inhibition of COXII suppresses inflammatory diseases without affecting COXI-mediated GI tract events. ANT-MP exhibited maximal analgesic effect when tested in vivo in an abdominal writhing assay (100% protection) and its anti-inflammatory activity showed a peak at 2 h in a carrageenan-induced paw edema model. Its unique selectivity toward the COXII enzyme was investigated using molecular modeling techniques.
- Extracorporeal Life Support and Plasmapheresis in a Case of Severe Polyintoxication. [JOURNAL ARTICLE]
- J Emerg Med 2014 Sep 11.
Resuscitation without return to spontaneous circulation in patients with suicidal ingestion of cardiotoxic drugs necessitates alternative bridging therapies for drug removal.To show the effectiveness of emergency extracorporeal membrane oxygenation (ECMO) and plasmaspheresis in severe polyintoxication.A 21-year-old woman developed asystole after suicidal polyintoxication with 1.75 g carvedilol, 300 mg amlodipine, 6 g amitriptyline, 500 mg torsemide, 1.5 g ketoprofen, 28 g nicotinic acid, and 16 g gabapentin. After 3 h of cardiopulmonary resuscitation without return to spontaneous circulation, ECMO was used as a bridging therapy and a temporary pacemaker was inserted. Plasma peak levels were measured for amlodipine (29.3 μg/L), amitriptyline (1456 μg/L), carvedilol (585 μg/L), and gabapentin (126.8 mg/L). To facilitate drug removal, therapeutic plasma exchange was performed. The patient could be weaned from ECMO at day 4 and extubated on day 8 after admission without neurologic sequelae.ECMO and plasma exchange should be considered as a therapeutic option in selected patients under resuscitation without return to spontaneous circulation after severe intoxication.
- Breastfeeding and migraine drugs. [JOURNAL ARTICLE]
- Eur J Clin Pharmacol 2014 Sep 13.
Breastfeeding women may suffer from migraine. While we have many drugs for its treatment and prophylaxis, the majority are poorly studied in breastfeeding women. We conducted a review of the most common anti-migraine drugs (AMDs) and we determined their lactation risk.For each AMD, we collected all retrievable data from Hale's Medications and Mother Milk (2012), from the LactMed database (2014) of the National Library of Medicine, and from a MedLine Search of relevant studies published in the last 10 years.According to our review, AMDs safe during breastfeeding are as follows: low-dose acetylsalicylic acid (ASA), ibuprofen, sumatriptan, metoprolol, propranolol, verapamil, amitriptyline, escitalopram, paroxetine, sertraline, acetaminophen, caffeine, and metoclopramide. AMDs compatible with breastfeeding but warranting caution are as follows: diclofenac, ketoprofen, naproxen, most new triptans, topiramate, valproate, venlafaxine, and cyproheptadine. Finally, high-dose ASA, atenolol, nadolol, cinnarizine, flunarizine, ergotamine, methysergide, and pizotifen are contraindicated.According to our review, the majority of the revised AMDs were assessed to be compatible with breastfeeding.
- In Vivo Predictive Dissolution: Transport Analysis of the CO2 , Bicarbonate In Vivo Buffer System. [JOURNAL ARTICLE]
- J Pharm Sci 2014 Sep 11.
Development of an oral in vivo predictive dissolution medium for acid drugs with a pKa in the physiological range (e.g., Biopharmaceutics Classification System Class IIa) requires transport analysis of the complex in vivo CO2 /bicarbonate buffering system. In this report, we analyze this buffer system using hydrodynamically defined rotating disk dissolution. Transport analysis of drug flux was predicted using the film model approach of Mooney et al based on equilibrium assumptions as well as accounting for the slow hydration reaction, CO2 + H2 O → H2 CO3 . The accuracy of the models was compared with experimentally determined results using the rotating disk dissolution of ibuprofen, indomethacin, and ketoprofen. The equilibrium and slow hydration reaction rate models predict significantly different dissolution rates. The experimental results are more accurately predicted by accounting for the slow hydration reaction under a variety of pH and hydrodynamic conditions. Although the complex bicarbonate buffering system requires further consideration given its dynamic nature in vivo, a simplifying irreversible reaction (IRR) transport analysis accurately predicts in vitro rotating disk dissolution rates of several carboxylic acid drugs. This IRR transport model provides further insight into bicarbonate buffer and can be useful in developing more physiologically relevant buffer systems for dissolution testing. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci.
- Reducing Transcranial Direct Current Stimulation-Induced Erythema With Skin Pretreatment: Considerations for Sham-Controlled Clinical Trials. [JOURNAL ARTICLE]
- Neuromodulation 2014 Sep 11.
Transcranial direct current stimulation (tDCS)-induced erythema (skin reddening) has been described as an adverse effect that can harm blinding integrity in sham-controlled designs. To tackle this issue, we investigated whether the use of topical pretreatments could decrease erythema and other adverse effects associated with tDCS.Thirty healthy volunteers were recruited, and four interventions were applied 30 min prior to tDCS in a Latin square design: placebo, ketoprofen 2%, hydroxyzine 1%, and lidocaine 5%. TDCS was applied for 30 min (2 mA, anode and cathode over F3 and F4, respectively) in two active sessions with a minimum 1-week interval. The Draize erythema scoring system scale was used to assess erythema intensity; a tDCS questionnaire was used to assess other adverse effects (e.g., tingling, itching, burning sensation, and pain).We found that ketoprofen (but not hydroxyzine or lidocaine) significantly attenuated tDCS-induced erythema regarding intensity and duration, with a medium effect compared with placebo. Erythema was overall mild, short-lived (lasting 18-24 min after tDCS ending), and more intense under the anode. Subjects with darker skin color also tended to present less intense tDCS-induced erythema. The prevalence of other adverse effects was low and did not differ between dermatological groups.Ketoprofen 2% topical pretreatment might be an interesting strategy to reduce tDCS-induced erythema and might be useful for blinding improvement in further sham-controlled tDCS trials.
- Effects of High-Frequency Bio-Oxidative Ozone Therapy in Temporomandibular Disorder-Related Pain. [JOURNAL ARTICLE]
- Med Princ Pract 2014 Sep 3.
Objective: It was the aim of this study to compare the efficacy of ozone therapy and drug treatment in patients with painful temporomandibular joint (TMJ) disorder (TMD). Subjects and Methods: A total of 63 patients with TMD were enrolled; 33 were treated with bio-oxidative therapy and 30 with a ketoprofen tablet thiocolchicoside capsule 2 × 1 for 7 days. Maximum voluntary interincisal mouth opening (MMO) was measured in millimeters using a scale and recorded during the pre- and posttreatment periods. The patients evaluated their subjective pain using a visual analogue scale (VAS). Data were analyzed using the Mann-Whitney U test, the Kolmogorov-Smirnov test, and the independent t test. Results: The mean MMO of the group that received ozone therapy during the pretreatment period was 46.51 ± 8.2 mm, and it immediately increased to 48.78 ± 7.5 mm after 1 week of ozone therapy, which was statistically significant (p = 0.04). For those who received medication, the mean MMO during the pretreatment period was 46.30 mm, and at the end of 1 week it was 46.9 mm. In the ozone group, 29% of patients showed a gradual decrease in their VAS pain scores compared to pretreatment values (6.3 ± 2.1 to 3.0 ± 2.2). In the medication group, 24% of patients showed a significant decrease in VAS pain scores during the follow-up period (6.9 ± 1.4 to 5.0 ± 1.5). Conclusion: This study showed that bio-oxidative therapy was a more effective treatment than medication therapy for relieving TMJ pain. © 2014 S. Karger AG, Basel.
- Skin permeation enhancement effects of the gel and whole-leaf materials of Aloe vera, Aloe marlothii and Aloe ferox. [JOURNAL ARTICLE]
- J Pharm Pharmacol 2014 Sep 5.
The aim of this study was to investigate the in-vitro permeation enhancement effects of the gel and whole-leaf materials of Aloe vera, Aloe marlothii and Aloe ferox using ketoprofen as a marker compound.The permeation studies were conducted across excised female abdominal skin in Franz diffusion cells, and the delivery of ketoprofen into the stratum corneum-epidermis and epidermis-dermis layers of the skin was investigated using a tape-stripping technique.A. vera gel showed the highest permeation-enhancing effect on ketoprofen (enhancement ratio or ER = 2.551) when compared with the control group, followed by A. marlothii gel (ER = 1.590) and A. ferox whole-leaf material (ER = 1.520). Non-linear curve fitting calculations indicated that the drug permeation-enhancing effect of A. vera gel can be attributed to an increased partitioning of the drug into the skin, while A. ferox whole leaf modified the diffusion characteristics of the skin for ketoprofen. The tape stripping results indicated that A. marlothii whole leaf delivered the highest concentration of the ketoprofen into the different skin layers.Of the selected aloe species investigated, A. vera gel material showed the highest potential as transdermal drug penetration enhancer across human skin.
- Drug-induced adverse reactions via breastfeeding: a descriptive study in the French Pharmacovigilance Database. [JOURNAL ARTICLE]
- Eur J Clin Pharmacol 2014 Sep 4.
Most drugs are excreted in maternal milk and may therefore be ingested by children during breastfeeding. Data concerning the safety of the use of drugs by breastfeeding women are patchy, and almost nothing is known about this issue for many drugs.The aim of this study was to describe the adverse drug reactions of drugs transmitted in breast milk on the basis of the data collected in the French Pharmacovigilance Database. All spontaneous reports of adverse drug reactions (ADRs) in breastfed infants recorded in the National Pharmacovigilance Database by the 31 French regional pharmacovigilance centres between 1984 and June 2011 were investigated.Between January 1985 and June 2011, 276 adverse drug reactions in 174 breastfed children were notified to the French Pharmacovigilance Network. The most frequently reported adverse drug reactions were neurological (28.6 %) and gastrointestinal (20.3 %). Sixty-five of the adverse drug reactions recorded were considered to be serious (37.4 %). The results of our study confirm that certain drugs were frequently implicated in serious adverse drug reactions. Two cases of ADRs (1.1 %) had a 'certain' causality score (I4) and 13 (7.5 %) a 'likely' score (I3). The suspected drugs include antiepileptic drugs, opiate analgesics and benzodiazepines. These results also demonstrate that some drugs that were thought to be anodyne or for which no data were available, such as ketoprofen and hydroxyzine, may be implicated in adverse effects. Finally, these data show that certain drugs, like pseudoephedrine, which should not be used during breastfeeding, were nevertheless implicated in several of the adverse drug reactions recorded.This study shows that ADR via breastfeeding are rarely reported due to low awareness or low occurrence of ADR via breast milk. These results highlight the need for additional pharmacokinetic, clinical and epidemiological studies, given the paucity of published data. They also demonstrate the need to improve information for the general public about drugs and self-medication during breastfeeding.
- Chronic treatment with zinc hydroaspartate induces anti-inflammatory and anti-ulcerogenic activity in rats. [Journal Article]
- Pharmacol Rep 2014 Oct; 66(5):862-6.
The previous study indicated the enhancement of the anti-inflammatory effect of ketoprofen by acute and sub chronic administration of zinc hydroaspartate.The present study examined anti-inflammatory, anti-ulcerogenic and analgesic activity induced by chronic (14 days) administration of ZHA (30mg/kg, po), with a combination of a single administration of ketoprofen, in rats. Moreover, the zinc concentration in serum and stomach mucosa was also determined.Chronic ZHA po administration exhibits anti-inflammatory activity and enhanced the effect induced by ketoprofen. Likewise, ZHA administration demonstrated anti-ulcerogenic activity. While ZHA alone did not exhibit analgesic action, it enhanced the effect of ketoprofen.The present study demonstrated for the first time that chronic treatment with zinc salt exhibits anti-inflammatory activity. Besides, anti-ulcerogenic activity and the enhancing properties of zinc to ketoprofen induced anti-inflammatory and analgesic activity were also shown.