Cox 2 inhibition cyclooxygenase 2 inhibitors. Medical search. Frequent questions

Decreases inflammation, pain, and fever, probably through inhibition of cyclooxygenase (COX-2 inhibitor) activity and prostaglandin synthesis. (wikipedia.org)
5-9 Data also indicate that Carprofen inhibits the production of osteoclast-activating factor (OAF), PGE 1 , and PGE 2 by its inhibitory effects on prostaglandin biosynthesis. (drugs.com)
Cyclo-oxygenase (COX)-2 inhibitors reduce OAC prostaglandin production but also have potentially detrimental effects on vascular endothelial function by reducing prostacyclin production and increasing the risk of cardiovascular events. (uea.ac.uk)
We have examined the effects of inhibiting microsomal prostaglandin synthase-1 (mPGES-1), the enzyme downstream of COX-2 in the prostaglandin synthetic cascade. (uea.ac.uk)
T he immune-inflammatory dysregulation theory in schizophrenia 1 , 2 posits an imbalance of pro- and anti-inflammatory cytokines and elevated levels of inflammatory proteins (eg, C-reactive protein, S100 calcium-binding protein B [S100B], and prostaglandin E2) in subgroups of patients with schizophrenia experiencing an exacerbation of symptoms. (psychiatrist.com)
11 , 12 A case has been made for adjunctive treatment of symptoms of schizophrenia using anti-inflammatory drugs, such as cyclooxygenase (COX) inhibitors, since these medications shift the immune responsivity from predominantly type-2 to type-1 and inhibit prostaglandin E2 synthesis. (psychiatrist.com)
Both the gastric and renal toxicities induced by traditional NSAIDs and selective COX-2 inhibitors seem to be related to inhibition of prostaglandin, but not leukotriene, synthesis. (unipv.it)
METHODOLOGY/PRINCIPAL FINDINGS: Here we report that cyclooxygenase (COX) activity and prostaglandin E(2) (PGE(2)) are crucially involved in induction of UCP1 expression in inguinal white adipocytes, but not in classic interscapular brown adipocytes. (ku.dk)

The mechanism of action of Carprofen, like that of other NSAIDs, is believed to be associated with the inhibition of cyclooxygenase activity. (drugs.com)
NSAIDS with preferential cyclo-oxygenase 2 inhibitions have been developed. (gpnotebook.com)
Selective COX-2 (cyclooxygenase-2) inhibitors (coxibs) cause less GI irritation and platelet inhibition than other NSAIDs. (msdmanuals.com)
As a class, cyclooxygenase inhibitory NSAIDs may be associated with gastrointestinal, renal and hepatic toxicity. (petsupplies4less.com)
2 Follow up usually means NSAIDs in combination with weight management. (caninearthritisandjoint.com)
Angiotensin converting enzyme (ACE) inhibitors, angiotensin-II receptor blockers (ARBs), diuretics and nonsteroidal anti-inflammatory drugs (NSAIDs) all have the potential to decrease renal function. (bpac.org.nz)
NSAIDs are associated with an increased risk of AKI, due to blockade of the COX-2 enzyme preventing prostacyclin synthesis, which causes afferent arteriolar vasoconstriction. (bpac.org.nz)
This means that selective COX-2 inhibitors, while undoubtedly safer than NSAIDs in terms of gastric toxicity, are not devoid of renal toxicity (in addition to their now clearly established adverse effects on coronary heart disease risk). (unipv.it)
Clinical trials of up to 3 years' duration have supported these findings, linking several cyclooxgenase 2 (COX-2) selective and nonselective NSAIDs to an increased risk for serious and potentially fatal CV thrombotic events, MI, and stroke. (medscape.com)

Notably, COX-2 inhibition with the specific inhibitor celecoxib represses PGE 2 secretion, presenting a feasible pharmacological option for treatment of infectious exacerbation in asthma in the future. (monash.edu)
The anti-proliferative effects were equivalent to those produced by COX-2 inhibitory concentrations of celecoxib and NS-398. (uea.ac.uk)
In contrast to the effects of the COX-2 inhibitor celecoxib, mPGES-1 inhibition had no effects on Akt kinase activity in OAC cells. (uea.ac.uk)
We have also confirmed that celecoxib has anticancer actions separate from the inhibition of COX-2. (uea.ac.uk)

2 The constitutive cyclooxygenase, COX-1, synthesizes prostaglandins necessary for normal gastrointestinal and renal function. (drugs.com)
The inducible cyclooxygenase, COX-2, generates prostaglandins involved in inflammation. (drugs.com)
Carprofen has also been shown to inhibit the release of several prostaglandins in two inflammatory cell systems: rat polymorphonuclear leukocytes (PMN) and human rheumatoid synovial cells, indicating inhibition of acute (PMN system) and chronic (synovial cell system) inflammatory reactions. (drugs.com)
Prostaglandins derived from the cyclooxygenase (COX) pathway and epoxyeicosatrienoic acids (EETs) from the cytochrome P450/soluble epoxide hydrolase (sEH) pathway are important eicosanoids that regulate angiogenesis and tumorigenesis. (cdc.gov)
COX-2 inhibitors, which block the formation of prostaglandins, suppress tumor growth, whereas sEH inhibitors, which increase endogenous EETs, stimulate primary tumor growth and metastasis. (cdc.gov)
They inhibit cyclooxygenase (COX) enzymes and thus decrease production of prostaglandins. (merckmanuals.com)
Clooxygenase (COX) is an enzyme responsible for the formation of prostaglandins from arachidonic acid, including thromboxanes and prostaglandins. (cancer-research-network.com)
COX-2 is an inducible enzyme that catalyzes the conversion of arachidonic acid to downstream prostaglandins involved in inflammation and vascular homeostasis. (cancer-research-network.com)
Moreover, COX-2 induces increased expression of prostaglandins, which play a key role in regulating inflammation, controlling pulmonary vascular tension, and barrier function. (cancer-research-network.com)
Maintaining the correct balance between prostaglandins and leukotrienes is essential for continuing good health, but both classes of mediators also play an important role in the pathogenesis of several diseases.Recently, a new class of anti-inflammatory drugs, the lipoxygenase (LOX)/COX inhibitors, has been developed as a means of simultaneously inhibiting the synthesis of prostaglandins, thromboxanes and leukotrienes. (unipv.it)

Additionally, these drugs, both non-selective inhibitors and selective cyclooxygenase-2 inhibitors, are frequently associated with side effects, impairing patients' compliance to their use 6 . (bvsalud.org)

Since AEA levels are regulated by COX-2 and FAAH, inhibition of both enzymes along with low-dose glucocorticoids may provide a therapeutic option to maximally boost the endocannabinoid system in RA, with possible beneficial effects. (uni-regensburg.de)

The term "triple whammy" refers to the concurrent use of an angiotensin converting enzyme (ACE) inhibitor or an angiotensin-II receptor blocker (ARB), with a diuretic and a non-steroidal anti-inflammatory drug (NSAID), including cyclo-oxygenase-2 (COX-2) inhibitors. (bpac.org.nz)
Recent studies have shown that cyclo-oxygenase (COX)-2 is important in renal physiology. (unipv.it)

Meloxicam and etodolac inhibit COX-2 up to 50 times more than COX-1. (gpnotebook.com)
However they may still inhibit COX-1 at therapeutic doses (1). (gpnotebook.com)
As we previously described, proadifen, a P450 monooxygenase inhibitor, might also be able to inhibit some ABC transporters, including breast cancer resistance protein (BCRP). (spandidos-publications.com)
It was previously reported that proadifen (SKF-525A), a well-known cytochrome P450 monooxygenase inhibitor, not only has anti-proliferative potential in some cancer cell lines, but it is also able to inhibit BCRP and MRP1 transporter proteins ( 8 ). (spandidos-publications.com)
They also inhibit renal function and reduce the efficacy of diuretics and ACE inhibitors, drugs that are commonly used by elderly patients. (unipv.it)

The specificity of a particular NSAID for COX-2 versus COX-1 may vary from species to species. (drugs.com)
Prescribing a NSAID concurrently with an ACE inhibitor/ARB and a diuretic increases the risk of AKI considerably. (bpac.org.nz)
2 The risk of AKI is highest in the first month of NSAID treatment. (bpac.org.nz)
The estimated degree of risk that patients are exposed to when taking combinations of an ACE inhibitor/ARB, diuretic and NSAID varies according to study design. (bpac.org.nz)
3 Another study found that the concurrent use of either an ACE inhibitor/ARB or a diuretic with a NSAID was not associated with a significantly increased risk of AKI. (bpac.org.nz)
It has not been conclusively established whether occasional, short-term use (e.g. one or two days) of a NSAID in a patient taking an ACE inhibitor or ARB with a diuretic poses an increased risk. (bpac.org.nz)

ACE inhibitors or ARBs generally preserve renal function. (bpac.org.nz)

Concomitant inhibition of FAAH and COX-2 reversed these effects. (uni-regensburg.de)
Because statins are substrates for the cytochrome P450 isoenzyme 3A4 (CYP3A4), concomitant use of CYP3A4 inhibitors (eg, indinavir and other protease inhibitors) can increase plasma concentrations and the attendant risk for myopathy. (medscape.com)

Recent research has revealed that β 2 - Adrenergic receptor (β 2 -AR) agonists lose bronchodilatory efficacy because the receptor-mediated molecular pathways responsible for their beneficial actions are desensitized by infection. (monash.edu)
These results demonstrate a critical interaction of these two lipid metabolism pathways on tumorigenesis and suggest dual inhibition of COX-2 and sEH as a potential therapeutic strategy for cancer therapy. (cdc.gov)
Meanwhile, CAY10404 is a potent inhibitor of PKB/Akt and MAPK signaling pathways and induces apoptosis in NSCLC cells. (cancer-research-network.com)
These compounds are synthesized in vivo through what can now be regarded as the "orthodox" cyclooxygenase pathways, which came to light largely through the work of Sune Bergström, who led a team then based at the Karolinska Institutet in Stockholm. (jci.org)
Here, we focus on newly uncovered pathways, involving either the cyclooxygenases (COXs) or nonenzymatic chemical transformations, that lead to the formation of bioactive prostanoids and of previously unknown lipid mediators produced by COX-2. (jci.org)

Previous studies suggest that the cyclooxygenase-2 (COX-2) inhibitor nimesulide has a remarkable protective effect against different types of brain injury including ischemia. (biomedcentral.com)
Nimesulide (12 mg/kg) not only reduced infarct volume but also enhanced functional recovery when the first treatment was given up to 2 h after stroke. (biomedcentral.com)
These data show that nimesulide protects against permanent focal cerebral ischemia, even with a 2 h post-treatment delay. (biomedcentral.com)
Nimesulide (N-(4-nitro-2-phenoxyphenyl)-methanesulfonamide) is a non-steroidal anti-inflammatory drug with potent effects. (biomedcentral.com)

These findings have important implications for the therapeutic potential of using COX-2 inhibitors in the treatment of stroke. (biomedcentral.com)

Three different methods of inhibiting mPGES-1 (RNA interference, a novel small molecule inhibitor and the endogenous inhibitor 15-deoxy-Delta(12,14)-PGJ(2)) also blocked leptin induced mPGES-1 expression and PGE2 production and abolished the leptin-induced proliferative and anti-apoptotic effects in OE33 cells, without affecting COX-2 expression. (uea.ac.uk)

We conclude that inhibition of mPGES-1 has potentially beneficial effects in OAC without the potentially detrimental effects on vascular endothelial prostacyclin synthesis. (uea.ac.uk)
Inhibition of leukotriene synthesis increases anti-inflammatory efficacy, particularly in rheumatic diseases, while reducing the risk of gastric damage. (unipv.it)

Furthermore, COX-2 plays an important role in the treatment of pulmonary inflammation. (cancer-research-network.com)

The efficacy of vascular endothelial growth factor (VEGF), COX-2, calcium and aromatase inhibitors in an ovarian hyperstimulation syndrome (OHSS) rat model was tested. (nih.gov)
COX-2/sEH dual pharmacological inhibitors also potently suppress primary tumor growth and metastasis by inhibiting tumor angiogenesis via selective inhibition of endothelial cell proliferation. (cdc.gov)
However, unlike the two COX-2 inhibitors, mPGES-1 inhibition did not reduce endothelial prostacyclin production. (uea.ac.uk)

Inhibition of MMPs has provided a significant increase in the survival rate in clinical trials, according to the frequent overexpression of MMPs in malignant tumors and the correlation with a highly aggressive phenotype and poor prognosis [ 8 - 10 ]. (biomedcentral.com)

Conclusions Taken together, our results show that, like viruses, bacteria induce prostanoid-dependent β 2 -AR desensitization on ASM cells. (monash.edu)
Antitumor activity of NVP-BKM120- a selective pan class 1 PI3 Kinase inhibitor showed differential forms of cell death based on P53 status of glioma cells. (mdanderson.org)
We show for the first time that proadifen is able to enhance the cytotoxic properties of MTX in cBCRP cells, particularly through the inhibition of BCRP expression and activity. (spandidos-publications.com)
In OAC cells, reduction of mPGES-1 with RNA interference blocked PGE2 production, inhibited serum-induced proliferation and enhanced apoptosis in the COX-2 expressing cell lines (OE33 and FLO) but had no effect in COX-2 deficient BIC-1 cells. (uea.ac.uk)
But, how does CAY10404 protect against cancer cells via COX-2? (cancer-research-network.com)
Tumor cells utilize a complex set of molecular mechanisms in order to metastasize [ 2 ]. (biomedcentral.com)

Using pharmacological inhibitors as probes, we show here that dual inhibition of COX-2 and sEH synergistically inhibits primary tumor growth and metastasis by suppressing tumor angiogenesis. (cdc.gov)

The role of COX-2 in tumorigenesis involves regulating apoptosis, increasing angiogenesis, regulating immune response, and increasing invasiveness. (cancer-research-network.com)

The Verapamil group showed the lowest corpus luteum formation, while the Parecoxib (COX-2 inhibition), the Parecoxib + Verapamil (COX-2 + Calcium inhibition), the Bevacizumab + Parecoxib (VEGF + COX-2 inhibition) and the Bevacizumab + Verapamil (VEGF + Calcium inhibition) groups were also characterized by lower corpus luteum numbers compared to the OHSS group. (nih.gov)

ACE inhibitors or ARBs and diuretics are commonly prescribed together, either as individual medicines or combination formulations, however, prescribers should remember that using these medicines together (the "double whammy") can increase the risk of AKI. (bpac.org.nz)

Our findings indicate that glucocorticoid-induced adhesion is dependent on CB(1) /CB(2) /TRPV-1 activation. (uni-regensburg.de)
Our findings suggest that brain uptake of some antiepileptic drugs can be enhanced through COX-2 inhibition. (uky.edu)
A goal of this Perspective is to provide a succinct view of salient findings and historical background in this area necessary for the reader to evaluate the potential importance of the newly uncovered "unorthodox" routes ( 2 - 4 ) initiated via cyclooxygenase (for detailed reviews see refs. (jci.org)
CONCLUSIONS/SIGNIFICANCE: Our findings provide evidence that induction of UCP1 expression in white adipose tissue, but not in classic interscapular brown adipose tissue is dependent on cyclooxygenase activity. (ku.dk)

Studies suggest that inhibition of COX-2, which occurs with both nonselective COX inhibitors and coxibs, has a prothrombotic effect that can increase risk of myocardial infarction, stroke, and claudication. (merckmanuals.com)

It shows a high affinity and selectivity for COX-2 with a COX-2/COX-1 IC 50 selectivity ratio of 0.06 (whole blood assay) [ 13 ]. (biomedcentral.com)

Cold-induced expression of UCP1 in inguinal white adipocytes was repressed in COX2 knockout (KO) mice and by administration of the COX inhibitor indomethacin in wild-type mice. (ku.dk)

Inhibition of COX-1 is thought to be associated with gastrointestinal and renal toxicity while inhibition of COX-2 provides anti-inflammatory activity. (drugs.com)

HMG-CoA inhibitors, also known as statins, are linked to an exposure-related risk for myopathy that presents as muscle pain, tenderness, or weakness, with elevated creatine kinase levels greater than 10 times the upper limit of normal. (medscape.com)

Obviously, CAY10404 Attenuates cyclooxygenase activity, significantly decreasing BAL PGE2 and 6-keto PGF1α. (cancer-research-network.com)

Launaeaspinosa and Pulicaria undulata were the powerful AChE inhibitor (IC 50 values were 16.69 and 29.06 µg/mL, respectively) followed with L. coronopifolia and S. libanotica extracts (IC 50 values were 61.89 and 49.83 µg/mL, respectively) and they were efficient in scavenging superoxide radicals and metal ions, nitric oxide formation inhibition, as well as, lipid peroxide production suppression. (niscair.res.in)

Angiotensin-converting enzyme (ACE) inhibitors: Antihypertensive effect of ACE inhibitors may be diminished. (wikipedia.org)

1 Inhibition is maximal when steady state plasma concentrations are reached, usually after three to seven days of treatment. (bpac.org.nz)

This proadifen-MTX synergism was also mediated by the inhibition of various cellular proteins engaged in apoptosis, including Mc-1, Bcl-xL, survivin and activation of procaspase-3. (spandidos-publications.com)

In this regard, we tested the hypothesis that seizures increase brain extracellular glutamate, which signals through an N-methyl-D-aspartate (NMDA) receptor and cyclooxygenase-2 (COX-2) in brain capillaries to increase blood-brain barrier P-glycoprotein expression. (uky.edu)
The use of PGE(2) receptor antagonists implicated EP(4) as a main PGE(2) receptor, and injection of the stable PGE(2) analog (EP(3/4) agonist) 16,16 dm PGE(2) induced UCP1 expression in inguinal white adipose tissue. (ku.dk)

The recommended dosage for oral administration to dogs is 2 mg/lb of body weight daily. (petsupplies4less.com)

no such glutamate-induced increases were seen in brain capillaries from COX-2-null mice. (uky.edu)

Selective serotonin reuptake inhibitors (SSRIs) are commonly considered suitable first-line therapy for premenstrual disorders. (medscape.com)

Equally exciting are opportunities for effective chemoprevention with nonsteroidal anti-inflammatory agents, both synthetic and naturally occurring, or selective cyclooxygenase-2 inhibitors. (aacrjournals.org)

This occurs via TLR2-dependent upregulation of cyclooxygenase 2 (COX-2) mRNA expression and increased secretion of PGE 2 . (monash.edu)
Thus, bacterial infectious stimuli act in a PGE 2 -dependent manner to severely curtail the beneficial actions of β 2 -Agonists. (monash.edu)
CAY10404 induces a concentration-dependent decrease in the level of the anti-apoptotic proteins (Bcl-2 and Bcl-X L ) and pAkt and pGSK-3β. (cancer-research-network.com)
Our results indicate that cyclooxygenase-dependent induction of UCP1 expression in white adipose tissues is important for diet-induced thermogenesis providing support for a surprising role of COX activity in the control of energy balance and obesity development. (ku.dk)
The extent of this effect is dependent on the variability of CYP3A4 inhibition. (medscape.com)

And the reduced COX-2 activity is associated with the pathogenesis of pulmonary fibrosis in human and animal models. (cancer-research-network.com)
Inhibition of COX activity attenuated diet-induced UCP1 expression and increased energy efficiency and adipose tissue mass in obesity-resistant mice kept at thermoneutrality. (ku.dk)

Dual inhibition of cyclooxygenase-2 and soluble epoxide hydrolase synergistically suppresses primary tumor growth and metastasis. (cdc.gov)
In turn, de novo formed vessels enhance tumor invasion and metastasis through the production of MMP 2 and 9 and uPA, which further degrade ECM. (biomedcentral.com)

Many medications must be continued through the perioperative period, with the last dose taken with a sip of clear liquid up to 2 hours prior to the procedure, and resumed during recovery. (medscape.com)
Therefore, patients can be given their routine medications with sips of water up to 2 hours before anesthesia. (medscape.com)

3 In an in vitro study using canine cell cultures, Carprofen demonstrated selective inhibition of COX-2 versus COX-1. (drugs.com)
Ten plant extracts were prepared and tested in in vitro assays against COX-2, COX-1 and acetylcholinesterase with evaluation of their antioxidant properties. (niscair.res.in)

The impact of β 2 -AR desensitization is demonstrated by reduced gene expression of the critical anti-inflammatory molecule MKP-1 in response to β 2 -Agonists, as well as impaired bronchodilation in a mouse lung slices. (monash.edu)

2 Overall risk of colon cancer is approximately 5% in the general population without family history, with 92% of colorectal cancers diagnosed after age 50. (naturalmedicinejournal.com)
These genetic disorders account for 1-2% and 3-5% of all colorectal cancers, respectively. (naturalmedicinejournal.com)
While IBD-related colorectal cancers account for only 1-2% of all CRC cases, CRC accounts for 10-15% of deaths in patients with IBD. (naturalmedicinejournal.com)

OBJECTIVE: In rheumatoid arthritis (RA) synovial fluid, levels of the endocannabinoids anandamide (AEA) and 2-arachidonylglycerol are elevated. (uni-regensburg.de)

However, liquids are cleared from the stomach within 2 hours of ingestion, and no differences in the volume or pH of gastric contents is noted in those patients taking clear fluids 2 hours before surgery compared to those taking clear fluids 9 hours before surgery. (medscape.com)

Those at greatest risk for colon cancer are carriers of 1 of 2 familial genetic disorders, familial adenomatous polyposis (FAP) or hereditary non-polyposis colon cancer (HNPCC), also known as Lynch syndrome. (naturalmedicinejournal.com)
thus, large bowel cancer is a major public health problem (2) . (aacrjournals.org)
The male-to-female ratio in head and neck cancer is 2:1. (medscape.com)

for all patients the balance of GI and cardiovascular risk should be considered before prescribing a COX-2 inhibitor, particularly for those with risk factors for heart disease (such as hypertension, hyperlipidaemia, diabetes and smoking, as well as for patients with peripheral arterial disease) and those taking low dose aspirin, for whom GI benefit has not been clearly demonstrated. (gpnotebook.com)
given the association between cardiovascular risk and exposure to COX-II inhibitors, doctors are advised to use the lowest effective dose for the shortest possible duration of treatment. (gpnotebook.com)

evidence suggests that selective COX-2 inhibitors, as a class, may cause an increased risk of thrombotic events (e.g. (gpnotebook.com)
Prostanoids, as they are known today, are a specific class of bioactive mediators generated via initial actions of cyclooxygenase. (jci.org)
The LOX/COX inhibitor licofelone, which is currently in phase III trials, is the first of this new class and in the most advanced stage of development. (unipv.it)

COX-II inhibitors must not be used in patients with established ischaemic heart disease and/or cerebrovascular disease, and also in patients with peripheral arterial disease. (gpnotebook.com)
caution should be exercised when prescribing COX-II inhibitors to patients with risk factors for heart disease, such as hypertension, hyperlipidaemia, diabetes and smoking. (gpnotebook.com)
Patients with an initial valgus and posterior tilt of greater than 15° (B1.1.2 fracture) were found to have a 17-fold higher risk of treatment failure than did patients with a tilt in both planes of less than 15° (B1.2.1 fracture). (medscape.com)

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