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Analgesics during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Phenacetin is one of the major metabolites of acetaminophen. It has analgesic and antipyretic actions with poor anti-inflammatory effects. Phenacetin is often used in combination with other analgesics, and. The frequency of malformations was not increased among more than 18,000 offspring of mothers who used this analgesic either alone or in combination with other agents (Heinonen et al., 1977; Jick et al., 1981). In addition, findings for acetaminophen also are relevant to this drug because a large proportion of acetaminophen is metabolized to phenacetin. No association between birth defects and phenacetin was found in experimental animals according to manufacturer’s package insert.
Nonopioid and Adjuvant Analgesic Agents
Published in Pamela E. Macintyre, Stephan A. Schug, Acute Pain Management, 2021
Pamela E. Macintyre, Stephan A. Schug
Renal toxicity, historically linked to phenacetin, rarely occurs with paracetamol despite its apparent COX-2 inhibitory effect (Graham et al, 2013). It is specifically recommended for use in patients with renal impairment. Paracetamol hypersensitivity and allergies are unlikely, and it can be used in patients with aspirin-exacerbated respiratory disease (AERD). Compared with NSAIDs, paracetamol causes little or no gastrointestinal (GI) toxicity, and it does not have a significant effect on platelet function, although it can enhance the effect of warfarin (Graham et al, 2013). It can lead to hemolysis if given to patients with the extremely rare glucose-6-phosphate dehydrogenase (G6PD) deficiency.
The Treatment of the Special Forms of Mental Disease
Published in Francis X. Dercum, Rest, Suggestion, 2019
It not infrequently happens that patients become the victims of narcotic habits other than those already discussed—e.g., veronalism or sulphonalism. Sometimes, also, one of the less commonly used narcotics, such as paraldehyd, somnal, or chloralamid, is the intoxicant to which the patient becomes addicted. One of the worst and most horrible cases of drug inebriety that I have been called upon to treat, was a case of paraldehyd habit in which a woman took enormous doses of this disgusting narcotic daily. She constantly reeked with the unpleasant odor of the drug, while her mucous membranes were ulcerated and her form much emaciated. Occasionally ether and chloroform are used by inebriates. Among the rarer forms of drug addiction met with at the present day are the phenacetin habit and the antipyrin habit. These habits, however, are less harmful than those alteady mentioned, and can, as a rule, be treated more readily.
Evaluation of the effect of Bovis Calculus Artifactus on eight rat liver cytochrome P450 isozymes using LC-MS/MS and cocktail approach
Published in Xenobiotica, 2021
Yun-Jing Zhang, Wen-Li Zhou, Fei Yu, Qian Wang, Can Peng, Jia-Yi Kan
The simultaneous incubation of substrates may lead to substrate interactions and inhibition of CYP activity by the solvent. So we used the concentrations of the substrates below their respective Michaelis constants to minimize the interactions and used organic solvents at low concentration (<1% (volume/volume)). Phenacetin had no effect on the metabolism of other probe drugs when it was lower than 152 μM. In this experiment, the concentration of phenacetin was 150 μM. Bupropion is the preferred probe drug for CYP2B6 and has been used in many cocktail methods and has no effect on the activities of other isozymes when less than 100 μM. According to the Km value of bupropion (67–168 μM), the concentration of bupropion is selected to be 95 μM, and 2.4 μM for amodiaquine (Km values: 2.6 μM). For tolbutamide, the concentration was set at 109 μM (Km values: 67–838 μM). The concentration of S-mephenytoin was set at 50 μM according to the Km value of (78 μM). As probe drug of CYP2D6, dextromethorphan has no effect on other probe drugs when the concentration is lower than 25 μM. In this study, the concentration of dextromethorphan is 10 μM. Midazolam was selected as a CYP3A4 probe drug with a concentration of 32 μM. When the concentration of chlorzoxazone is less than 50 μM, it has no effect on other subtypes of enzymes. In this experiment, the concentration of chlorzoxazone is 15 μM (Xia et al. 2021; Yang et al. 2014).
The development and hepatotoxicity of acetaminophen: reviewing over a century of progress
Published in Drug Metabolism Reviews, 2020
Mitchell R. McGill, Jack A. Hinson
The development of APAP as a drug began with a happy accident. In the 1880s, two medical interns working under German physician Adolf Kussmaul at the University of Strassburg were given the wrong compound by a pharmacist who thought he was dispensing naphthalene to treat a patient’s intestinal worms. While the compound was ineffective against the parasite, it did reduce the patient’s fever (Cahn and Hepp 1886). Chemists soon identified the new antipyretic as acetanilide and it was marketed by the German company Kalle under the brand name Antifebrin (Cahn and Hepp 1886). The analgesic effects of acetanilide were initially attributed to the acetyl moiety that distinguished it from its precursor aniline, resulting in an acetylation craze that likely led to the development of phenacetin (N-acetyl-p-ethoxyacetanilide), the immediate precursor of APAP. Bayer chemists seeking a use for the unwanted by-product of dye synthesis, p-aminophenol, decided to acetylate it. Like acetanilide, the product phenacetin exhibited strong analgesic and antipyretic effects and quickly became the drug of choice. However, acetanilide and phenacetin both produced serious adverse effects, leading to the search for a safer alternative. In 1893, clinical pharmacologist Joseph Baron von Mering was the first to administer the recently synthesized drug APAP to humans (von Mering 1893). However, von Mering claimed that APAP produced side effects similar to acetanilide and phenacetin, most notably methemoglobinemia. APAP was subsequently discarded in favor of phenacetin, which was taken either alone or in combination with aspirin and caffeine. Phenacetin remained the preferred mild analgesic until approximately 1970.
Smoking-adjusted risk of renal pelvis cancer by occupation: a population-based cohort study of Nordic men
Published in Acta Oncologica, 2020
Irmina Maria Michalek, Kristina Kjærheim, Jan Ivar Martinsen, Pär Sparén, Laufey Tryggvadóttir, Elisabete Weiderpass, Eero Pukkala, Elsebeth Lynge
A possible cause of the elevated risk of renal pelvis cancer among physicians that should be considered is exposure to phenacetin. Phenacetin is an analgesic and antipyretic drug that was extensively used in the past. According to IARC, phenacetin is carcinogenic to the renal pelvis [1]. However, there is no study on healthcare providers being at elevated exposure to phenacetin. Also, the literature is too sparse to suggest that addiction to analgesic drugs is prevalent in this group [8]. Nevertheless, the observation of excess risk of renal pelvis cancer among physicians, a professional group with easy access to this drug, is noteworthy.