Pharmacodynamic of cyclooxygenase inhibitors in humans

Capone, Marta L.; Tacconelli, Stefania; Francesco, Luigia Di; Sacchetti, Andrea; Sciulli, Maria G.; Patrignani, Paola

doi:10.1016/j.prostaglandins.2006.05.019

Cited by 168 publications

(122 citation statements)

References 54 publications

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“…Similarly to other NSAIDs, naproxen is used as a treatment of arthritis, febrile syndrome, and pain because of its analgesic, antipyretic, and anti-inflammatory activity. Naproxen is a nonselective COX inhibitor with a balanced inhibitory effect on both COX-isozymes (COX-1 and COX-2) [28][29][30]. This drug possesses also a chiral centre, and it was observed in in vitro tests concerning inhibition of prostaglandin synthesis that the activity resides mostly in the (S)-enantiomer.…”

Section: (S)-naproxenmentioning

confidence: 99%

Metabolic chiral inversion of 2-arylpropionic acid derivatives (profens)

Morris

2017

Medical Research Journal

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2-arylpropionic acid derivatives (profens) are one of the most popular anti-inflammatory, analgesic, and antipyretic drugs. They belong to a group of nonsteroidal anti-inflammatory drugs (NSAID) and exhibit metabolic chiral inversion. Enantiomers of these chiral drugs are often characterised by different pharmacological activity. It is estimated that the values of metabolic chiral inversion of (R)-ibuprofen in humans are between 35 and 70%, depending on the condition of the liver and the intake of other medicines, while (R)-flurbiprofen undergoes chiral metabolic inversion to its opposed (S) form only in small range.The described phenomenon in the case of (R)-ketoprofen is limited to a maximum of around 10%. The metabolic chiral inversion is associated with potentially important pharmacotherapeutic and toxicological consequences, and so an attempt was made to analyse this phenomenon for the most commonly used drugs from the profens group.

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Section: (S)-naproxenmentioning

confidence: 99%

Metabolic chiral inversion of 2-arylpropionic acid derivatives (profens)

Morris

2017

Medical Research Journal

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“…NSAIDs are characterized in two distinct classes according to their ability to selectively block COX-2 and this is given by the ratio of the IC50 for COX-1 and COX-2 with in vitro studies [22][23][24]: a) Non-selective COX inhibitors: block both COX-1 and COX-2 in a non-selective manner. They traditionally possess a carboxylic acid (-COOH) as a functional group and represent the most prescribed NSAIDs for fever, pain and inflammation treatment; b) Cox-2 selective inhibitors: selectively block COX-2.…”

Section: Interplay Between Mechanism Of Action and Therapeutic Effectsmentioning

confidence: 99%

Oxaprozin-Loaded Lipid Nanoparticles towards Overcoming NSAIDs Side-Effects

et al. 2015

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“…14 We identified prescriptions for low-dose aspirin (75 mg, 100 mg, or 150 mg) and high-dose aspirin (500 mg), other nonselective NSAIDs (phenylbutazon, indomethacin, sulindac, aceclofenac, piroxicam, tenoxicam, lornoxicam, ibuprofen, naproxen, ketoprofen, fenoprofen, flurbiprofen, dexibuprofen, tiaprofenic acid, tolfenamic acid, and nabumeton), older selective COX-2 inhibitors (diclofenac, etodolac, and meloxicam), and newer selective COX-2 inhibitors (celecoxib, rofecoxib, and etoricoxib). 21 We examined older and newer COX-2 inhibitors separately as well as together because of overlapping COX-2 selectivity.…”

Section: Nonsteroidal Anti-inflammatory Drug Usementioning

confidence: 99%

Nonsteroidal anti‐inflammatory drugs and the risk of skin cancer

Johannesdottir

Chang

Mehnert

et al. 2012

Cancer

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BACKGROUND: Nonsteroidal anti-inflammatory drugs (NSAIDs) may prevent the development of cancer by inhibiting cyclooxygenase (COX) enzymes, which are involved in carcinogenesis. Therefore, the authors of this report examined the association between NSAID use and the risk of squamous cell carcinoma (SCC), basal cell carcinoma (BCC), and malignant melanoma (MM). METHODS: From 1991 through 2009, all incident cases of SCC (n ¼ 1974), BCC (n ¼ 13,316), and MM (n ¼ 3242) in northern Denmark were identified. Approximately 10 population controls (n ¼ 178,655) were matched to each case by age, gender, and county of residence. The use of aspirin, other nonselective NSAIDs, or selective COX-2 inhibitors was ascertained through a prescription database. Conditional logistic regression analyses adjusted for potential confounders were used to compute odds ratios as estimates of incidence rate ratios (IRRs). RESULTS: For NSAIDs overall, ever use (>2 prescriptions) compared with nonuse ( 2 prescriptions) was associated with a decreased risk of SCC (IRR, 0.85; 95% confidence interval [CI], 0.76-0.94) and MM (IRR, 0.87; 95% CI, 0.80-0.95), especially for long-term use (!7 years) and high-intensity use (>25% prescription coverage during the total duration of use). NSAID use was not associated with a reduced risk of BCC overall (IRR, 0.97; 95% CI, 0.93-1.01), but the risk of BCC at sites other than the head and neck was reduced in association with long-term use (IRR, 0.85; 95% CI,) and high-intensity use (IRR, 0.79; 95% CI, 0.69-0.91). All estimates of reduced risk were driven primarily by the use of nonselective NSAIDs and older COX-2 inhibitors (diclofenac, etodolac, and meloxicam). CONCLUSIONS: The current results indicated that NSAID use may decrease the risk of SCC and MM.

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Pharmacodynamic of cyclooxygenase inhibitors in humans

Cited by 168 publications

References 54 publications

Metabolic chiral inversion of 2-arylpropionic acid derivatives (profens)

Metabolic chiral inversion of 2-arylpropionic acid derivatives (profens)

Oxaprozin-Loaded Lipid Nanoparticles towards Overcoming NSAIDs Side-Effects

Nonsteroidal anti‐inflammatory drugs and the risk of skin cancer

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