Ketoprofen Versus Paracetamol in the Treatment of Acute Migraine

The efficacy and safety of ketoprofen and paracetamol were compared for the treatment of acute migraine in a randomized, double-blind study of 64 patients. Thirty-four patients received ketoprofen 100 mg intramuscularly, and 30 patients received paracetamol 500 mg intramuscularly. Partial or complete relief of pain and other symptoms was achieved 15 to 20 minutes after administration in the ketoprofen group and within 35 minutes in the paracetamol group. Complete relief of pain was achieved within 30 to 40 minutes after ketoprofen in 28 patients (82.5%) compared to 5 patients (17.5%) in the paracetamol group. Six of the patients treated with ketoprofen needed a second dose for complete relief of pain during the 4-hour follow-up period. Side effects were rare and minimal. Our findings suggest that ketoprofen produced statistically significant benefit in the treatment of acute migraine.     

Nodular hyperplasia surrounding fibrolamellar carcinoma

We report a case of acetaminophen-induced liver necrosis in a 14-year-old girl. At autopsy, a 9 cm subcapsular nodule was present in the right lobe of the liver which showed distinct zonation: a central greyish white area of fibrolamellar carcinoma with a peripheral fleshy, tan-coloured rim ranging from 1 to 2 cm in thickness. This peripheral zone consisted of nodular, hyperplastic parenchyma resembling the changes seen in focal nodular hyperplasia, and stood out from the adjacent necrotic parenchyma. The sparing of this zone from the deleterious effects of acetaminophen provides indirect evidence of a predominantly arterial rather than portal blood supply to this region. The arterial supply was most probably derived from the tumour vasculature and may explain the parenchymal hyperplasia sometimes reported adjacent to a fibrolamellar carcinoma. Awareness of this phenomenon is essential when evaluating a needle biopsy, as sampling of this region may lead to a false negative diagnosis.     

Pollen extracts reduce the hepatotoxicity of paracetamol in mice

Cernitins are preparations obtained from plant pollen which contain numerous compounds of potential biological significance. This work deals with the influence of cernitins upon acute paracetamol toxicity in mice. The survival rate and indices of hepatic injury: aminotransferase and alkaline phosphatase activities, bilirubin level in serum, glutathione and cytochrome P-450 content in liver, liver weight, histopathologic picture of the liver and presence of glycogen and lipids in stained liver sections, under different experimental protocols, were determined. It was found that cernitins are able to increase the survival rate of mice and reduce liver injury in acute paracetamol poisoning. Cernitins are more effective when administered after, rather than before, a dose of paracetamol. The possible mechanism through which cernitins may act is discussed.     

Simultaneous multiwavelength spectrophotometric quantitation of active components in analgesic formulations. Comparative study of three calculation methods

This work deals with the UV spectrophotometric quantitation of a mixture of compounds with overlapped spectra. The mixture spectrum is resolved by use of three computational programs based on different algorithms, namely Multicomponent Analysis (commercial software available from Hewlett-Packard), MULTIC (relying on multiple regression analysis) and SIMPLEX. The results obtained for mixtures of acetylsalicylic acid, acetaminophen and caffeine in commercial analgesic formulations, are compared.     

Comparison of a traditional paracetamol medication and a new paracetamol/paracetamol-methionine ester combination

Summary The SUR 2647 combination is a sachet formulation containing free paracetamol and its N-acetyl-methionate ester (SUR 2647). In a randomized, single-blind, between-patient study the onset of analgesia, duration and efficacy of the SUR 2647 combination vs paracetamol was investigated in outpatients after oral surgery. One group (n=27) received sachets of SUR 2647 combination 2 b.i.d. (equivalent to 2 g paracetamol ×2) on the day of operation, and one sachet b.i.d. (equivalent to 1 g paracetamol ×2) for the following two days. The other group (n=26) received paracetamol tablets 2 q.i.d. on the day of operation (1 g×4) and one tablet q.i.d. (0.5 g×4) for the following two days. Several objective and subjective assessments, including pain score on a visual analogue scale, were recorded for comparison of the postoperative courses. Median onset of analgesia for both groups was 0.5 h. The duration after SUR 2647 combination was 5.5 h as compared to 2.5 h for paracetamol. Mean pain scores showed that the SUR 2647 combination regime reduced pain significantly more than the paracetamol regime from 0.5 to 3.0 h after initiation of medication. The mean pain scores did not show a significant difference during the remaining observation period. Mild to moderate drowsiness was reported in both treatment groups, but it was more common in subjects given SUR 2647 combination.     

黄芪总黄酮抗肝损伤作用初探

目的研究黄芪总黄酮(total navonoids 0f Astragalus,TFA)对扑热息痛所致小鼠肝损伤的预防功效。方法观察不同剂量(0、100、300、400、500 ms/kg)扑热息痛对c57BL/6J小鼠肝脏的损伤作用,比较经1天或5天(每天2次)的TFA预处理后对扑热息痛(400 mg/kg)所致肝损伤的防护作用。结果扑热息痛对小鼠肝损伤作用具有明显的量效关系。不同剂量的TFA对扑热息痛诱导小鼠肝损伤有不同程度的防护作用,其作用强度与药物浓度成正比；TFA可增加血清中SOD活性(P＜0．05)；高剂量的TFA(100mg/kg)具有降低肝组织中脂质过氧化物质的作用；此外,在相同TFA剂量下,5天组对扑热息痛诱导小鼠肝损伤的预防作用优于1天组。结论提示TFA可预防扑热息痛诱导的肝损伤,其预防作用与其使用时间有密切关系。     

Synergistic antinociceptive interaction between acetaminophen or metamizol and B vitamins in the formalin test

There is evidence that B vitamins produce antinociception in animals. However, potentiation of NSAID‐induced antinociception by B vitamins is unclear. The current study was designed to investigate the antinociceptive interaction between a mixture of B vitamins and either acetaminophen or metamizol. Acetaminophen (56–316 mg/kg), metamizol (32–178 mg/kg), and the mixture of B vitamins (32–178 mg/kg of thiamine, pyridoxine, and cyanocobalamin in a 100:100:1 proportion, respectively) or a combination of each drug with the B vitamins mixture was administered orally to female Wistar rats, and the antinociceptive effect determined in the formalin test. Isobolographic analyses were used to define the nature of the interaction between NSAIDs and B vitamins. Oral administration of either drug produced a dose‐related antinociceptive effect. Isobolographic analyses revealed that both acetaminophen or metamizol and the B vitamins mixture interacted synergistically in the formalin test, suggesting that these two combinations could be useful in treating inflammatory pain states. Drug Dev. Res. 66:286–294, 2006. © 2006 Wiley‐Liss, Inc.     

Protective Effects of Polydatin from Grapes and Reynoutria japonica Houtt. on Damaged Macrophages Treated with Acetaminophen

The unregulated use of acetaminophen (APAP), an antipyretic and analgesic drug, harms hepatocytes and kidney cells, leading to liver failure and acute kidney injury. Herein, we investigate whether APAP damages macrophages in the immune system by observing its effects on macrophage proliferation and apoptosis. Using proteomics, we analyzed the effects of APAP on macrophage protein expression profiles and evaluated whether polydatin, the active ingredient in grapes and wine, can repair the damaged cells. The results showed that APAP alters the morphology and physiological processes of macrophages, inhibits macrophage proliferation, and promotes apoptosis. We observed 528 differentially expressed proteins when 500 µg/mL APAP was administered to the cells. These proteins are involved in biological processes including cell division, apoptosis, and acute phase response. Overall, our findings demonstrate that APAP harms the immune system by damaging macrophages and that polydatin can repair this damage.     

Quantification of active ingredients in suppositories by FT‐Raman spectroscopy

An efficient method for the quantitative determination of acetaminophen (AAP) and diclofenac sodium (DS) in commercial suppositories based on partial least squares (PLS) treatment of FT‐Raman spectra is described. The relative standard errors of prediction (RSEP) were calculated for calibration and validation data sets to evaluate the quality of the constructed models. In the case of DS determination, RSEP error values of 1.9 % and 2.3 % for the calibration and validation data sets, respectively, were found. For AAP these errors amounted to 1.6–2.3 % and 1.8–2.8 %, respectively, for the different calibration models. Four commercial preparations containing 5, 12.5, 16.7 and 33.3 % (w/w) AAP and one containing 5 % (w/w) DS were successfully quantified using the developed models. Concentrations derived from the developed models correlated strongly with the declared values and yielded recoveries of 99.4–100.2 % and 99.6 % for AAP and DS, respectively. The proposed procedure can be used as a fast, economic and reliable method for quantification of the active pharmaceutical ingredients in suppositories. Copyright © 2012 John Wiley & Sons, Ltd.