Practice Paper 4: Answers
Anthony B. Starr, Hiruni Jayasena, David Capewell, Saran Shantikumar in Get ahead! Medicine, 2016
Ibuprofen is an NSAID. Other drugs belonging to this class include aspirin, diclofenac, ketorolac and naproxen. They have multiple actions, but are mainly used for their analgesic, antipyretic and anti-inflammatory properties. NSAIDs work by inhibiting the enzyme cyclooxygenase, which is responsible for the synthesis of proinflammatory prostaglandins. Prostaglandins are also important in regulating mucosal protection by gastric acid secretion and renal blood flow. Because of this role of prostaglandins, if their synthesis is inhibited by NSAIDs, the loss of regulation promotes gastric acid mucosal damage (increasing the risk of gastritis and peptic ulcer disease) and reduced renal blood flow (increasing the risk of renal failure). Therefore, patients prone to gastritis, peptic ulcer disease and renal impairment should not be prescribed NSAIDs, and individuals who require long-term treatment should be prescribed gastroprotective agents such as omeprazole. NSAIDs are also contraindicated in asthmatic patients, along with β-blockers, as they can trigger bronchospasm in sensitive individuals.
Ayurveda Renaissance – Quo Vadis?
D. Suresh Kumar in Ayurveda in the New Millennium, 2020
Ibuprofen is a non-steroidal potent modulator of inflammation and analgesia. It is a non-selective inhibitor of the cyclooxygenase enzymes COX-1 and COX-2, but not of lipoxygenase, which catalyzes steps in the biochemical inflammation pathways derived from arachidonic acid (Vane and Botting 1995). Newly pressed extra virgin olive oil contains the aldehyde oleocanthal, whose pungency induces a strong stinging sensation in the throat, very similar to that caused by solutions of ibuprofen (Breslin et al. 2001) (Figure 11.3). Like ibuprofen, oleocanthal caused dose-dependent inhibition of COX-1 and COX-2 activities. But it had no effect on lipoxygenase in vitro (Beauchamp et al. 2005). This finding has striking similarity with the teachings of Ayurveda and is one of the rare scientific reports noting common pharmacological activity for compounds with similar taste. As such, it is consistent with the tenet of Ayurveda that the similarity of taste of substances indicates similar pharmacological activity. Though dissimilar in chemical structure, both (-) oleocanthal (left) and ibuprofen (right) are pungent and have anti-inflammatory activity.
Pharmacological interventions
Grahame Smith in Dementia Care, 2018
Nonopioid analgesics are normally aspirin, ibuprofen or paracetamol. Paracetamol is generally preferred as it does not have as many side effects as aspirin or ibruprofen. Aspirin (derived from willow bark) has a long history but it was not until the end of the nineteenth century that it was first patented. Aspirin has good analgesic, anti-inflammatory, antipyretic and antiplatelet properties. It is thought to act by blocking the cyclooxygenase pathway; however by doing so it may produce side effects involving the digestive tract and kidneys. Ibuprofen also works by blocking the cyclooxygenase pathway so it has similar effect for mild to moderate pain. Paracetamol (discovered over 100 years ago) is used to relieve pain and fever. It does not appear to have any anti-inflammatory or antiplatelet effect and therefore has much fewer side effects than aspirin or ibuprofen. It is thought that its mechanism of action is via cyclooxygenase 3 inhibition. It is important to be aware that paracetamol is dangerous when taken in excess.
Effects of Single-Dose Preemptive Pregabalin and Intravenous Ibuprofen on Postoperative Opioid Consumption and Acute Pain after Laparoscopic Cholecystectomy
Published in Journal of Investigative Surgery, 2019
Omer Karaca, Huseyin U. Pınar, Emin Turk, Rafi Dogan, Ali Ahiskalioglu, Sezen K. Solak
Ibuprofen is an analgesic, anti-inflammatory, and antipyretic NSAID. The analgesic efficacy of ibuprofen is related to cyclooxygenase enzyme inhibition. A rapid reverse and competitive inhibition of the isoenzymes COX-1 and COX-2 are caused by ibuprofen administration. The analgesic, antipyretic, and anti-inflammatory effects of ibuprofen depend on COX-2 inhibition, while COX-1 causes unwanted side effects.23 Studies in the literature reported that combined use of pregabalin and NSAID decreased both pain and opioid consumption. Jokela et al. showed that a preemptive, single, oral dose of 150 mg of pregabaline and an 800 mg dose of ibuprofen taken postoperatively twice a day decreased pain during the early postoperative period, but did not reduce the amount of postoperative analgesic required in patients undergoing gynecologic laparoscopic surgery.24 Another study indicated that pregabalin and celecoxib, which is a COX-2 enzyme inhibitory as preemptive analgesia, reduced postoperative pain and morphine consumption after maxillomandibular advancement surgery.25 We indicated that it was decreased pain, total opioid and rescue analgesic required; Likewise PACU stay in the preemptive single dose of 150 mg pregabalin and IV 800 mg ibuprofen group compared to the preemptive 150 mg pregabalin group.
Ibuprofen-based advanced therapeutics: breaking the inflammatory link in cancer, neurodegeneration, and diseases
Published in Drug Metabolism Reviews, 2021
Arun Upadhyay, Ayeman Amanullah, Vibhuti Joshi, Rohan Dhiman, Vijay Kumar Prajapati, Krishna Mohan Poluri, Amit Mishra
Ibuprofen is one of the most consistently prescribed OTC drugs for rheumatoid pain worldwide with an effective dose of 600–1200 mg/day, which may also be increased up to 2400 mg/day in extreme cases (Godfrey and Cruz 1975; Rainsford 1999). The rapid onset of the effects of Ibuprofen after its oral intake makes it a suitable choice for the treatment of acute pain and fever (Rainsford 2009). The drug is removed quickly from the plasma with a half-life of 2 h; also, it does not participate in the generation of toxic metabolites as happens in the case of many other NSAIDs, hence present lower toxicity as compared to other similar drugs (Graham and Williams 2004; Rainsford 2009). The Phase I metabolism of Ibuprofen involves several cytochrome P450 enzymes that subsequently hydroxylate the isobutyl chain of both the enantiomers, converting them into hydroxy-derivatives followed by the oxidation reaction that leads to the formation of 3-carboxy-Ibuprofen and p-carboxy-2-propionate (Evans 2001; Sanoh et al. 2012). In the phase II metabolism, the drugs containing carboxylic acid, like Ibuprofen, are converted into their acyl glucuronides before getting eliminated via urinary excretion (Brocks and Jamali 1999; Monrad et al. 2014).
Localized, on-demand, sustained drug delivery from biopolymer-based materials
Published in Expert Opinion on Drug Delivery, 2022
Junqi Wu, Sawnaz Shaidani, Sophia K. Theodossiou, Emily J. Hartzell, David L. Kaplan
Over 80% of the patients who undergo surgery report acute postoperative pain. The current standard of care is oral pain medication that patients take as needed, requiring patients to determine dosing [28]. Non-steroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen and aspirin are widely used to relieve pain, fever, and other inflammatory processes [9]. The main mechanism behind NSAIDS is the inhibition of the enzyme cyclooxygenase (COX). There are two types of COX isoenzymes: COX1 and COX2. Most NSAIDs do not distinguish between the two; COX1 is important for maintaining gastrointestinal mucosa, kidney function, and platelet aggregation, while COX2 is expressed during inflammatory responses. As a result, when patients take NSAIDs, adverse gastric and renal events are common [9]. Additionally, the use of prescription opioids for pain management doubled between 2001 and 2013, significantly contributing to ongoing opioid misuse [7]. To address these issues and decrease adverse events related to systemic delivery of APIs for pain management, implantable, biodegradable, and biocompatible local drug delivery systems at or near the target site can be useful.
Related Knowledge Centers
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