Eighty-nine patients receiving NSAIDs and 22 control subjects not taking NSAIDs were studied in a cross-sectional survey at Veterans Affairs and University hospitals. Measurements of serum thyroxine (T4), free T4 index, triiodothyronine (T3), and thyrotropin (thyroid-stimulating hormone [TSH]) were obtained for all subjects.
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Unmethylated CpG motifs found in bacterial DNA are potent activators of the innate and acquired immune systems, and rapidly induce the production of proinflammatory cytokines. We hypothesized that CpG DNA may also elicit the production of prostaglandins (PG), which are central lipid mediators of the immune and inflammatory response. To test our hypothesis, we stimulated murine spleen cells and RAW 264.7 murine macrophage cells with CpG DNA and assessed the effects on the PG synthesis pathway. Compared to control, DNA-containing CpG motifs induced >5-fold increase in PGE (2) production and rapidly up-regulated cyclooxygenase-2 (COX-2) at both the mRNA and protein level. CpG DNA was an extremely strong inducer of COX-2 as concentrations as low as 3 ng/ml induced COX-2 protein expression. The CpG DNA-induced PGE (2) down-regulated the immune response elicited by CpG. Blockade of PGE (2) production with selective COX-2 inhibitors or neutralizing anti-PGE (2) antibody markedly enhanced IFN-gamma secretion in vitro from CpG DNA-stimulated spleen cells. Moreover, selective COX-2 inhibition increased CpG DNA-induced IFN-gamma secretion in vivo. Inhibition of COX-2 also increased CpG DNA-induced lytic activity of NK cells. Taken together, these data indicate that DNA containing CpG motifs is a potent inducer of COX-2 and PGE (2) production. CpG-induced PG may subsequently down-regulate the immune and inflammatory responses elicited by the CpG DNA.
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In the late 20(th) century, the treatment of cancer began to include its prevention. Today, compounds exist that will lower the risk of developing certain types of cancer. This has been demonstrated in studies where chemically induced tumor growth has been slowed or reversed. Anti-inflammatory compounds having chemopreventive activity are piroxicam, sulindac, aspirin, celecoxib and curcumin. The selective estrogen receptor modulators, tamoxifen and raloxifene, are beneficial in the prevention of estrogen dependent tumors. Retinoids, vitamin A derivatives, such as targretin and fenretinide are useful in the prevention of tumors. Compounds containing sulfur, such as sulforaphane and oltipraz, are even useful as radioprotective agents. The steroid dehydroepiandosterone can inhibit experimental carcinogenesis. All of these chemical classes provide a start for the medicinal chemist to design more effective chemopreventive agents. The biomarkers used to determine the chemopreventive activity of new compounds are quite often activities of enzymes. The identification of those individuals at high risk is still in its infancy and presents a troubling dilemma.
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Cocrystals (CCs) used in the pharmaceutical industry are defined as complex crystals formed by reaction between an API and a cocrystal former (CCF); unlike salts, CCs do not show proton transfer. Recently, pharmaceutical CCs have been used to improve the drug-likeness of APIs, such as solubility and stability. Grinding is more effective for CC synthesis than crystallization from solution because in the former case, the API can predominantly interact with the CCF without being affected by solvents. However, this method is tedious because the API is ground with only one CCF at a time. We developed a cocktail cocrystal grinding (CCG) method, in which a mixture of CCFs having the same functional group was used. No false negatives/positives were observed in CCG when carbamazepine was used as the model compound. This method could be used to obtain CCs of piroxicam and spironolactone. False negatives were observed for only one compound from among three model compounds, indicating that CCG facilitates efficient CC detection and that it has higher throughput than does the conventional method. Further, CCG is fast and suitable for rational CC screening, and it helps identify the partial structure of CCFs that forms synthons with an API.
Nabumetone is a nonsteroidal anti-inflammatory prodrug, which exerts its pharmacological effects via the metabolite 6-methoxy-2-naphthylacetic acid (6-MNA). Nabumetone itself is non-acidic and, following absorption, it undergoes extensive first-pass metabolism to form the main circulating active metabolite (6-MNA) which is a much more potent inhibitor of preferentially cyclo-oxygenase (COX)-2. The three major metabolic pathways of nabumetone are O-demethylation, reduction of the ketone to an alcohol, and an oxidative cleavage of the side-chain occurs to yield acetic acid derivatives. Essentially no unchanged nabumetone and < 1% of the major 6-MNA metabolite are excreted unchanged in the urine from which 80% of the dose can be recovered and another 10% in faeces. Nabumetone is clinically used mainly for the management of patients with osteoarthritis (OA) or rheumatoid arthritis (RA) to reduce pain and inflammation. The clinical efficacy of nabumetone has also been evaluated in patients with ankylosing spondylitis, soft tissue injuries and juvenile RA. The optimum oral dosage of nabumetone for OA patients is 1 g once daily, which is well tolerated. The therapeutic response is superior to placebo and similar to nonselective COX inhibitors. In RA patients, nabumetone 1 g at bedtime is optimal, but an additional 0.5-1 g can be administered in the morning for patients with persistent symptoms. In RA, nabumetone has shown a comparable clinical efficacy to aspirin (acetylsalicylic acid), diclofenac, piroxicam, ibuprofen and naproxen. Clinical trials and a decade of worldwide safety data and long-term postmarketing surveillance studies show that nabumetone is generally well tolerated. The most frequent adverse effects are those commonly seen with COX inhibitors, which include diarrhoea, dyspepsia, headache, abdominal pain and nausea. In common with other COX inhibitors, nabumetone may increase the risk of GI perforations, ulcerations and bleedings (PUBs). However, several studies show a low incidence of PUBs, and on a par with the numbers reported from studies with COX-2 selective inhibitors and considerably lower than for nonselective COX inhibitors. This has been attributed mainly to the non-acidic chemical properties of nabumetone but also to its COX-1/COX-2 inhibitor profile. Through its metabolite 6-MNA, nabumetone has a dose-related effect on platelet aggregation, but no effect on bleeding time in clinical studies. Furthermore, several short-term studies have shown little to no effect on renal function. Compared with COX-2 selective inhibitors, nabumetone exhibits similar anti-inflammatory and analgesic properties in patients with arthritis and there is no evidence of excess GI or other forms of complications to date.
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The overall quantitative consumption indicators of the entire therapeutic group, and the dose per inhabitant per day (DID) of the systemic active principles which were significantly most prescribed, were determined. 3967487 NSAID prescriptions were dispensed, at a pharmaceutical cost of 2369, 483, 257 pesetas. Naproxen and Piroxicam were the active principles most used in terms of their DIDs. Of the population groups analysed, it is essentially the pensioners group which consumes these drugs.
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Thirty women presenting for major gynaecological oncology surgery under a standardized, combined epidural/general anaesthetic technique received either placebo or tenoxicam 20 mg intravenously, in a randomized double-blinded manner prior to surgery. Plasma and urinary electrolytes, creatinine, prostaglandins PgE2 and PgF1 alpha, and thromboxane (TxB2) were collected 12 hours preoperatively and then for four days postoperatively. There were no significant differences in any of the measured parameters between the groups, at any of the measurement times. Mean (SD) creatinine clearance at baseline, 24 h and 48 h was 100.4 (29.7) and 86.9 (27.5), 128.1 (45.9) and 115.0 (40.3), 137.5 (50.7) and 121.6 (38.6) in the placebo and tenoxicam groups respectively (P = 0.28). Both groups required similar amounts of intraoperative ephedrine and intravenous fluids to maintain blood pressure. The minimal changes in plasma and renal parameters reflect predictable responses to major surgery and rehydration rather than any response to cyclooxygenase inhibition. This may underscore the importance of maintenance of blood pressure during the course of surgery and postoperative care, and perhaps the usefulness of a fluid loading regimen to preserve renal function during surgery. The predicted attenuation of renal prostaglandin-mediated protective mechanisms and enhancement of the catecholamine-mediated renal vasoconstriction by the use of a single 20 mg dose of tenoxicam in this study were not seen. Modulation of renal concentrating mechanisms or excretion of sodium and potassium by tenoxicam was not apparent and a large increase in study size would be required to detect a significant difference in these parameters as a consequence of the drug, over and above any changes in response to surgery and epidural anaesthesia.
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The aim of the study was to describe the long-term toxicity of antirheumatic and anti-inflammatory drugs in a paediatric rheumatology clinic population. One hundred and seventeen children were studied on first admission to a paediatric rheumatology clinic and after a mean of 8.6 +/- 0.4 years of follow-up. Medical records from the intermediate period were reviewed. The patients had 155 exposures to non-steroidal anti-inflammatory drugs (NSAIDs), 88 exposures to disease-modifying antirheumatic drugs (DMARDs) and 12 exposures of prednisolone during a total of 682 patient years. Drug toxicity was measured in terms of the number of toxic events, number of drug discontinuations due to toxicity, number of side-effects per patient year of drug exposure and as a toxicity index. Side-effects were seen in 69 (27%) of the drug exposures, corresponding to 0.10 toxic events per patient year of exposure. Abdominal pain was the most common side-effect, and was reported in 21 (14%) of the exposures to NSAIDs. Five severely toxic events, all leading to hospitalisation, occurred. The toxicity of NSAIDs was not significantly different from that of DMARDs with regard to the number of toxic events (21% and 31%, respectively, NS) and drug discontinuations due to toxicity (17% and 14%, respectively, NS). Piroxicam tended to be more toxic than ibuprofen (46% versus 18% toxic events, p <0.05; 36% versus 16% discontinuations due to toxicity, NS; 0.33 versus 0.05 side-effects per patient year and a toxicity index of 1.45 versus 0.20 units per patient year). Gold tended to be more toxic than antimalarials (41% versus 15% toxic events, p<0.05; 24% versus 12% discontinuations, NS; 0.37 versus 0.08 side-effects per patient year and a toxicity index of 1.56 versus 0.23 units per patient year). It was concluded that antirheumatic and anti-inflammatory drugs led to side-effects in 27% of the exposed children during 9 years of follow-up. There was an overlap of the toxicity of certain NSAIDs and the most commonly employed DMARDs.
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The gel was prepared by using carbopol 934 as gelling agent and methyl paraben as a preservative in an Aloe vera gel base. The formulated gel was also evaluated for physicochemical parameters like pH, viscosity, drug content, and in vitro diffusion assessment. Pharmacodynamic activity of the formulation was evaluated in Wistar albino rats. The formulated gel was compared with that of similar marketed gel (commercial piroxicam gel (CPG)) against the same parameters.
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The searches identified 10 trials; four are included (287 participants aged five to 39 years; maximum follow up of four years) and one is currently awaiting classification pending publication of the full trial report. Three trials compared ibuprofen to placebo (two from the same centre with some of the same participants); one trial assessed piroxicam versus placebo.The three ibuprofen trials were deemed to have good or adequate methodological quality, but used various outcomes and summary measures. Reviewers considered measures of lung function, nutritional status, radiological assessment of pulmonary involvement, intravenous antibiotic usage, hospital admissions, survival and adverse effects. Combined data from the two largest ibuprofen trials showed a significantly lower annual rate of decline for lung function, percent predicted forced expiratory volume in one second mean difference 1.32 (95% confidence interval 0.21 to 2.42); forced vital capacity mean difference 1.27 (95% confidence interval 0.26 to 2.28); forced expiratory flow (25-75%) mean difference 1.80 (95% confidence interval 0.15 to 3.45). The post-hoc analysis of data from two trials split by age showed a statistically significant slower rate of annual decline of percent predicted forced expiratory volume in one second and forced vital capacity in the ibuprofen group in younger children, mean difference 1.41% (95% confidence interval 0.03 to 2.80) and mean difference 1.32% (95% confidence interval 0.04 to 2.60) respectively. In one trial, long-term use of high-dose ibuprofen was associated with reduced intravenous antibiotic usage, improved nutritional and radiological pulmonary status. No major adverse effects were reported, but the power of the trials to identify clinically important differences in the incidence of adverse effects was low.We did not have any concerns with regards to risk of bias for the trial comparing piroxicam to placebo. However, the trial did not report many data in a form that we could analyse in this review. No data were available for the review's primary outcome of lung function; available data for hospital admissions showed no difference between the groups. No analysable data were available for any other review outcome.
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Tenoxicam, a new non-steroidal anti-inflammatory drug has been compared with piroxicam and indomethacin in a range of pharmacological and biochemical inflammation test systems. In a chronic (17-day) adjuvant arthritis in the rat, tenoxicam and piroxicam were equally effective in reducing several indices of inflammation and were less ulcerogenic and better tolerated than indomethacin. The oxicams reduced the oedematous and cellular components of a carrageenan pleurisy at 4 hours while at 24 hours they increased exudate volume and selectively inhibited the accumulation of mononuclear cells. These agents also reduced the inflammatory component of a delayed hypersensitivity response to methylated bovine serum albumin in the mouse. The oxicams were about 100-fold less active than indomethacin as inhibitors of prostaglandin synthetase but all three compounds reduced about equally the release of prostaglandin E2 from phagocytosing rat PMN and interleukin 1-stimulated human rheumatoid synovial cells. The compounds had no effect on the release of superoxide anion, lysosomal enzymes or collagenase from cultured cells, neither did they inhibit isolated collagenase. Only indomethacin stabilized albumin against heat denaturation.
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Some NSAIDs are available over the counter and women are under-represented in the VA population.
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A randomized double-blind trial with tenoxicam 10 mg/d and 20 mg/d and placebo was carried out for 2 weeks in 90 patients suffering from various extra-articular inflammatory conditions. Statistical analysis revealed significant differences in favour of tenoxicam as regards improvement of all parameters with an intensity which was moderate or severe at baseline, e.g. tenderness, mobility pain, functional limitation. The efficacy of tenoxicam at both dosages was similar (no statistically significant difference). Tenoxicam was well tolerated but some mild adverse reactions were observed in all three treatment groups.
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Therapeutic administration of recombinant Rspo1 protein reduced the loss of body weight, diarrhea, and rectal bleeding in a mouse model of acute or chronic DSS-induced colitis. Histologic evaluation revealed that Rspo1 improved mucosal integrity in both villus and/or crypt compartments in the small intestine and colon by stimulating crypt cell growth and mucosal regeneration in DSS-treated mice. Moreover, Rspo1 significantly reduced DSS-induced myeloperoxidase activity and inhibited the overproduction of proinflammatory cytokines, including tumor necrosis factor-alpha, IL-1alpha, IL-6, interferon-gamma, and granulocyte-macrophage colony-stimulating factor, in mouse intestinal tissue, indicating that Rspo1 may reduce DSS-induced inflammation by preserving the mucosal barrier function. Likewise, Rspo1 therapy also alleviated TNBS-induced interstitial inflammation and mucosal erosion in the mouse colon. Furthermore, Rspo1 substantially decreased the histopathologic severity of chronic enterocolitis by repairing crypt epithelium and simultaneously suppressing inflammatory infiltration in piroxicam-exposed IL-10(-/-) mice. Endogenous Rspo1 protein was localized to villus epithelium and crypt Paneth cells in mouse small intestine.
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Idebenone, a compound with protective efficacy against neurotoxicity both in in vitro and in in vivo models, exists in two different oxidative states: the ubiquinol-derivative (reduced idebenone) and the ubiquinone-derivative (oxidised idebenone). In the present study, we have observed that both the redox forms of idebenone have a dose-dependent inhibitory effect on the enzymatic metabolism of arachidonic acid in astroglial homogenates (IC50 reduced idebenone: 1.76 +/- 0.86 microM; IC50 oxidised idebenone: 16.65 +/- 3.48 microM), while in platelets, they are apparently less effective (IC50 reduced idebenone: 18.28 +/- 4.70 microM; IC50 oxidised idebenone: > 1 mM). We have also observed that the oxidised form preferentially inhibited cyclooxygenase vs. lipoxygenase metabolism (IC50 ratio lipoxygenase/cyclooxygenase: 3.22), while the reduced form did not discriminate between the two pathways (IC50 ratio lipoxygenase/cyclooxygenase: 1.38). In this respect, the inhibitory action of reduced idebenone resembled that of the antioxidant nordihydroguaiaretic acid, while oxidised idebenone behaved similarly as indomethacin and piroxicam--two typical anti-inflammatory agents. Our results suggest the existence of two distinct mechanisms of action for the two redox forms of idebenone and a preferential action of the drug on arachidonic acid metabolism in the central nervous system.
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A study was carried out in order to investigate the chronotherapy (dosing time dependency) of an NSAID, the tenoxicam administered in ankylosing spondylitis, rheumatoid arthritis and osteoarthritis of the hip. These variations in efficacy exist as much for pain as for stiffness and maximum efficacy is obtained with administration at 8 am or 12 pm. Since the tolerance was good, we recommend midday as an optimal once-a-day dosing time.
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Since glutathione (GSH) depletion (about 20% of total GSH content) can impair the cell's defence against the toxic actions of drugs and may lead to cell injury and death, we examined the effect of piroxicam, naproxen and ketoprofen on GSH levels in various organs of the rat (brain, eye, liver, stomach, heart, leg adductor muscle). Ketoprofen in brain and leg adductor muscle dramatically decreases the GSH levels, giving rise to potential cellular toxicity.
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A mononuclear Ru(II) complex containing two piroxicam (Pir(-)) ligands was synthesized and fully characterized. Interaction studies of the Pir(-) anion and the Ru(II) complex with DNA and BSA were carried out using spectroscopic techniques. The results suggested that the Pir(-) anion binds to DNA in a moderately strong fashion via intercalation between the base stacks of double-stranded DNA, while the Ru(II) complex is a groove binder and interacts with DNA with more affinity. Moreover, the results demonstrated that the microenvironment and the secondary structure of BSA were changed in the presence of Pir(‾) and Ru(II) complex. The free Pir(‾) ligand and the Ru(II) complex can lead to the photocleavage of DNA supercoiled pUC57. Finally, the binding of the Ru(II) complex to BSA and DNA was modeled by molecular docking and molecular dynamic simulation methods.
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Analgesics are commonly used to provide pain relief after surgery. These drugs produce some extended depression of immunity. A prospective randomized controlled trial was designed to observe expressions of T-lymphocyte subsets (CD3(+), CD3(+)CD4(+) and CD3(+)CD8(+)), natural-killer cells (CD3(-)CD16(+)CD56(+)), and activated T-lymphocytes (CD3(+)CD25(+)) of patients undergoing gastric cancer surgeries and receiving patient-controlled intravenous analgesia (PCIA).
piroxicam, sport interruption for a week, proper warming-up and wearing suggestions during out-of-water exercises in the symptomatic group. Absence of intervention in the asymptomatic one.
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Non-steroidal anti-inflammatory drugs (NSAIDs) are the most commonly used analgesics and antipyretics, which form an interesting drug group because of their new and alternate functions. The ability of the NSAIDs belonging to the oxicam chemical group to induce membrane fusion at low physiologically relevant concentrations is a new function that has drawn considerable attention. Membrane fusion is dependent on the interplay of physicochemical properties of both drugs and membranes. Here, we have elucidated the effects of different oxicam drugs, Meloxicam, Piroxicam, Tenoxicam, Lornoxicam, and Isoxicam, on an identical membrane-mimetic system. This highlights only the differential effects of the drugs on drug-membrane interactions, which in turn modulate their role as membrane fusogens. The partitioning behavior and the location of the drugs in dimyristoylphosphatidylcholine vesicles have been studied using second-derivative absorption spectroscopy, fluorescence quenching, steady-state fluorescence anisotropy, and time-resolved fluorescence lifetime measurements. Fusion kinetics has been monitored by fluorescence assays and dynamic light scattering was used to provide a snapshot of the vesicle diameter distribution at different time points. The differential perturbing effect of the drugs on the membrane is dependent both on their partitioning and location. Although partitioning governs the extent of fusion, the location modulates the rates of each step.
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The efficacy and safety of tenoxicam was compared to that of piroxicam in 48 Nigerian patients with Osteoarthritis of the knee or hips. Of these 31 females and 11 males, with a mean age of 52.5 +/- 11.0 years, were evaluated for comparable efficacy and tolerability. On fulfilling the selection criteria each patient was treated with either tenoxicam 20 mg or piroxicam 20 mg daily for six weeks. Efficacy was evaluated in terms of presence of pain (at rest, with mobility and after one day of normal activity), functional status and physicians global assessment of therapeutic efficacy. Tolerability was evaluated by incidence of adverse events whilst safety was evaluated by measurement of haematological and biochemical profile pre and post therapy. Thirty seven patients had been on previous medication before being switched over to trial drug. There was a dose change in three patients in the piroxicam group due to inefficacy. Also there was loss of efficacy during maintenance in one patient in the piroxicam group. Clinical efficacy was judged excellent or good in 82.3% of patients with tenoxicam and 76.0% with piroxicam. Tolerability was excellent or good in 88.2% of patients with tenoxicam and 60.0% with piroxicam. The incidence of adverse event was 15.8% with tenoxicam and 21.7% with piroxicam. Overall, when judged on various evaluation parameters, tenoxicam 20 mg/day appears to be more effective and better tolerated than piroxicam 20 mg/day, though these differences were not statistically significant.
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In short-term use, NSAIDs vary considerably in their effect on blood pressure. Of the drugs studied, indomethacin and naproxen were associated with the largest increases in blood pressure. The average effects of piroxicam, aspirin, ibuprofen, and sulindac were negligible.
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In human liver microsomes (n = 7), desmethylnaproxen formation was observed with a mean kM of 92 (21) mumol.l-1, Vmax of 538 pmol.min-1.mg-1 protein and Cint2 (reflective of a second binding site) of 0.36 microliter.min-1.mg-1 protein. This Cint2 term was added since Eadie-Scatchard analysis suggested the involvement of more than one enzyme. Studies using putative specific P450 inhibitors demonstrated inhibition of this reaction by sulfaphenazole, (apparent Ki = 1.6 mumol.l-1), warfarin (apparent Ki = 27 mumol.l-1), piroxicam (apparent Ki = 23 mumol.l-1) and tolbutamide (apparent Ki = 128 mumol.l-1). No effect was observed when alpha-naphthoflavone and troleandomycin were employed as inhibitors, but reaction with furafylline produced, on average, a maximum inhibition of 23%. At a naproxen concentration of 150 mumol.l-1, formation of desmethylnaproxen was observed in cells expressing P450 1A2, 2C8, 2C9 and its allelic variant 2C9R144C. To further characterize these reactions, saturation kinetics experiments were conducted for the P450s 1A2, 2C8 and 2C9. The kM and Vmax for P450 1A2 were 189.5 mumol.l-1 and 7.3 pmol.min-1.pmol-1 P450, respectively. Likewise, estimates of kM and Vmax for P450 2C9 were 340.5 mumol.l-1 and 41.4 pmol. min-1.pmol-1 P450, respectively. Reliable estimates of kM and Vmax could not be made for P450 2C8 due to the nonsaturable nature of the process over the concentration range studied.
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This work describes the single adsorption of seven pharmaceuticals (carbamazepine, oxazepam, sulfamethoxazole, piroxicam, cetirizine, venlafaxine and paroxetine) from water onto a commercially available activated carbon and a non-activated carbon produced by pyrolysis of primary paper mill sludge. Kinetics and equilibrium adsorption studies were performed using a batch experimental approach. For all pharmaceuticals, both carbons presented fast kinetics (equilibrium times varying from less than 5 min to 120 min), mainly described by a pseudo-second order model. Equilibrium data were appropriately described by the Langmuir and Freundlich isotherm models, the last one giving slightly higher correlation coefficients. The fitted parameters obtained for both models were quite different for the seven pharmaceuticals under study. In order to evaluate the influence of water solubility, log Kow, pKa, polar surface area and number of hydrogen bond acceptors of pharmaceuticals on the adsorption parameters, multiple linear regression analysis was performed. The variability is mainly due to log Kow followed by water solubility, in the case of the waste-based carbon, and due to water solubility in the case of the commercial activated carbon.