• Title/Summary/Keyword: Acetaminophen

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Rectal Absorption of Acetaminophen from Polyethylene Glycol and Witepsol Suppositories (아세트아미노펜의 Polyethylene glycol 및 Witepsol 좌제의 직장흡수 - 병원제제를 목적으로 한 아세트아미노펜좌제의 조제 및 유용성 검토-)

  • Lee, Hye Suk;Jin, Sun Kyung;Choi, Jung Hwa;Ku, Young Soon
    • Korean Journal of Clinical Pharmacy
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    • v.8 no.2
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    • pp.143-146
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    • 1998
  • Acetaminophen (APAP) suppositories with active ingredients, i.e., polyethylene glycol (PEG), Witepsol H-15 (WH), were prepared for hospital use and investigated on their drug release characteristics and pharmacokinetics. WH was employed as oil-soluble base with an aim of reducing fragility and mucosa irritancy that are common drawbacks found in PEG suppositories. Also hollow type suppository was tried as compared with conventional type suppository. Drug release tests revealed that in most formulations, more than $80\%$ of loaded APAP were released within 20 minutes, except for APAP-WH hollow type suppositories. Significant differences in the plasma concentration profile were observed among four type suppositories. $T_{max}$ of APAP-PEG and APAP-WH suppositories were 90 and 60 minutes, respectively, in hollow types. APAP-WH hollow type suppositories demonstrated fast absorption rates of APAP as compared with those of APAP-PEG suppositories. No burst effect was observed from APAP-WH suppository in contrast to APAP conventional type suppository, whereas AUCs of all the suppositories were similar. APAP-WH hollow type suppository may be an useful dosage form for hospital use.

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Toxicity of a combination of florfrenicol and acetaminophen in pigs administered at overdose

  • Chae, Won-Seok;Yoo, Chang-Yeul;Tutkun, Lutfiye;Kim, Suk;Lee, Hu-Jang
    • Journal of Preventive Veterinary Medicine
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    • v.42 no.4
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    • pp.182-185
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    • 2018
  • This study examined the overdose toxicity of Super-Neophensan, containing florfenicol and acetaminophen, upon pigs. SNP-3.0 (n=10) was administered at the dosage level of 3 kg/ton feed for 7 consecutive days, which is 3 times the recommended dose based on the guidelines of the manufacturer, and the control group (CON) (n=10) was administered the normal diet without the drug. The body weight, weight gain and feed efficiency in SNP-3.0 treated with the drug for 14 days post-administration showed no significant differences compared with those in CON. In hematological and blood biochemical analyses, all parameters were not affected by over-dosage of the drug. In the same way, there were no significant differences between SNP-3.0 and CON on markers for liver and kidney functions. As no adverse effects were observed with the drug in an overdose oral toxicity test, this study suggests that the drug was identified as a safe agent in pigs administered with three times the recommended dose.

The Relationship between Prohibitin 1 Expression, Hepatotoxicity Induced by Acetaminophen, and Hepatoprotection by S-Adenosylmethionine in AML12 Cells

  • Eunhye Cho;Soohan Jung;Jina Kim;Kwang Suk Ko
    • Journal of Microbiology and Biotechnology
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    • v.32 no.11
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    • pp.1447-1453
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    • 2022
  • Prohibitin 1 (Phb1) is a pleiotropic protein, located mainly in the mitochondrial inner membrane and involved in the regulation of cell proliferation and the stabilization of mitochondrial protein. Acetaminophen (APAP) is one of the most commonly used over-the-counter analgesics worldwide. However, at high dose, the accumulation of N-acetyl-p-benzoquinone imine (NAPQI) can lead to APAP-induced hepatotoxicity. In this study, we sought to understand the regulation of mRNA expression in relation to APAP and GSH metabolism by Phb1 in normal mouse AML12 hepatocytes. We used two different Phb1 silencing levels: high-efficiency (HE, >90%) and low-efficiency (LE, 50-60%). In addition, the siRNA-transfected cells were further pretreated with 0.5 mM of Sadenosylmethionine (SAMe) for 24 h before treatment with APAP at different doses (1-2 mM) for 24 h. The expression of APAP metabolism-related and antioxidant genes such as Cyp2e1 and Ugt1a1 were increased during SAMe pretreatment. Moreover, SAMe increased intracellular GSH concentration and it was maintained after APAP treatment. To sum up, Phb1 silencing and APAP treatment impaired the metabolism of APAP in hepatocytes, and SAMe exerted a protective effect against hepatotoxicity by upregulating antioxidant genes.

Hepatoprotective Effect of Gagam-GongJin-dan extract against Acetaminophen-Induced Liver Injury in Mice (Acetaminophen 유도 마우스 간 손상에 대한 가감공진단(加減拱辰丹) 추출물의 간보호 효과)

  • Kim, Hong-Hun;Mok, Ji-Ye;Park, Kwang-Hyun;Jeong, Seung-Il;Hwang, Byung-Soon;Hwang, Sung-Yeoun;Cho, Jung-Keun;Jang, Seon-Il
    • The Korea Journal of Herbology
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    • v.25 no.3
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    • pp.149-157
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    • 2010
  • Objective:Gagam-Gongjin-dan (GGD) is an oriental medicinal prescription composited with Cervi parvum Cornu, Corni Fructus, Angelica Gigantis Radix, Lycii Fructus, Dioscoreae Rhizoma, Citri Pericarpium, Gastrodiae Rihzoma, Agastachis Herba, Cassiae cortex, Scutellariae Radix and Schisandrae Fructus. The purpose of this study was to investigate the effects of GGD extract against acetaminophen (APAP)-induced liver injury in mice. Methods:GGD extract was prepared by extracting with methanol for 7 days. The extract was freeze-dried following filtration through vacuum distillation system. The first, we investigated the antioxidant effects of GGD extract on electronic donating ability (DPPH), nitrite (NO) scavenging and superoxide dismutase (SOD)-like activity. The next, we investigated the possible hepatoprotective effect of GGD extract administration against acetaminophen-induced liver injury in mice. Mice were orally administrated with or without GGD extract of different doses (25-100 mg/kg/day) one times per day for 6 days. After 3 days, APAP was orally applied with a single dose (400 mg/kg). Results:GGD extract increased DPPH, NO and SOD-like activities in dose dependant. APAP treatment significantly increased aspartate aminotransferase (AST) and alanine aminotransferase (ALT) activities in plasma. Also, APAP treatment significantly evaluated lipid peroxidation product thiobarbituric reacting substances (TBARS) and depleted some antioxidant enzymes (superoxide dismutase, catalase, d-aminolevulinate dehydratase and gluthathione peroxidase activities) in liver homogenates compared to the control group. However, the orally administration of GGD extract was able to counteract these effects. Histological studies provided supportive evidence for biochemical analysis Conclusions:These results suggest that GGD extract has a potential antioxidant and hepatoprotective effect against APAP-induced liver injury, these properties may contribute to liver disease care.

Elevation of Procalcitonin in an Adolescent Acetaminophen Intoxication (아세트아미노펜 중독 청소년에서의 프로칼시토닌 상승)

  • Kim, So Eun;Lee, Jae Baek;Jin, Young Ho;Yoon, Jae Chol;Jo, Si On;Jeong, Tae Oh
    • Journal of The Korean Society of Clinical Toxicology
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    • v.17 no.1
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    • pp.38-41
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    • 2019
  • Procalcitonin (PCT) is commonly employed in medical practice as a diagnostic biomarker of bacterial infection and also as a monitoring biomarker for antimicrobial therapy. There have been a few published reports concerning elevated PCT levels in people with acute liver injury caused by an overdose of acetaminophen. We report here on a case of PCT elevation in an adolescent with acute acetaminophen poisoning without any bacterial infection or liver injury. A 15-year-old girl had deliberately ingested 20 tablets of 650 mg acetaminophen (13 g) and she presented to our emergency department. The PCT level on admission was elevated to 65.64 ng/mL (reference range: 0-0.5 ng/mL). Her PCT level on the second day peaked up to 100 ng/mL and then it gradually decreased. There was no evidence of liver injury or infection on the computed tomography examination and other lab tests. The patient regained her good health and was discharged on the sixth day of hospitalization.

Laboratory analysis of acute acetaminophen overdose patients in Emergency Medical Centers: including analysis of one toxicological laboratory data (응급의료센터에서 아세트아미노펜 과다복용 환자의 검사실 분석 현황: 일개 중독분석실 농도 분석자료 포함)

  • Kim, In Chan;Won, Sinae;Lee, Arum;Jung, Haeun;Lee, Jeongsun;Oh, Bum Jin
    • Journal of The Korean Society of Clinical Toxicology
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    • v.19 no.1
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    • pp.31-37
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    • 2021
  • Purpose: Acetaminophen (APAP) is a widely available drug responsible for a large part of drug-induced hepatotoxicity in developed countries. Although acetaminophen overdose cases in Korea are being continuously reported, there are no reports related to the level of this drug in the patient's blood or of laboratory analysis at emergency departments (ED). This study sought to analyze the acetaminophen overdose cases at a toxicological laboratory and to survey APAP analysis services offered at select EDs. Methods: We analyzed the demographic and analytic data at a toxicological laboratory run by the National Emergency Medical Center (NMC) in 2019-2020. We surveyed the APAP laboratory service in the 38 regional emergency medical centers (EMCs) and 68 local EMCs near the toxicological laboratory. Results: We studied 175 acute poisoning cases (112 women) with positive blood APAP results (mean age 47.0±24.1 years). Suicide attempts comprised 40.0% of the cases and 30.3% APAP overdose events. In the univariate analysis, we observed that patients were significantly younger, with fewer underlying medical diseases. There were a higher number of APAP overdose events, more favorable initial mental status, more toxic quantity intake in the above treatment line group (p<0.05), In multivariate analysis, the toxic amount intake was significantly more frequent in the above treatment line group (p<0.01). Hospital APAP analysis services were available in six EMCs (3/38 regional and 3/68 local). The hospital blood APAP level reporting intervals were shorter than outside-hospital laboratory services (p<0.01, regional 7.0±3.0 vs. 40.6±27.5, local 5.3±3.1 vs. 57.9±45.1 hours). The NMC toxicological laboratory reporting interval was shorter than the other outside-hospital laboratories (p<0.01, regional 5.7±0.6 vs. 50.2±22.7 local 7.5±3.0 vs. 70.5±41.5 hours). Conclusion: Over the treatment line group, toxic amount intake was significantly more frequent. Only six of 106 EMCs have their own APAP analysis service in their hospitals.