Non-steroidal anti-inflammatory drugs diclofenac

Schwaiger J, Ferling H, Mallow U, Wintermayr H, Negele R (2004) Toxic effects of non-steroideal anti-inflammatory drug diclofenac. Part I. Histopathological alterations and bioaccumulation in rainbow trout. Aquat Toxicol 68 141-150... 

Arthrotec tablets contain the non-steroidal anti-inflammatory drug diclofenac and the prostaglandin misoprostol. The combination of the two active ingredients makes Arthrotec suitable in patients predisposed to gastrointestinal ulceration. Dulco-lax (bisacodyl) tablets act as a stimulant laxative. Voltarol Retard tablets contain the non-steroidal anti-inflammatory drug diclofenac. All... 

M.A., Meharg, A.A., Pattee, O.H. and Pain, D.J. (2008) Apparent tolerance of turkey vultures (Cathartes aura) to the non-steroidal anti-inflammatory drug diclofenac. Environ Toxicol Chem, 27, 2341-2345. 

The phosphonic acid analog of NSAID (Non-Steroidal Anti-Inflammatory Drug) diclofenac was successfully synthesized in the laboratory of B. Mugrage using a novel acid catalyzed Arbuzov reaction as the key step followed by a TMSBr promoted dealkylation. It needs to be pointed out that the nucleophilic attack takes place on the ortho-quinonoid intermediate in a non-SN2 process. 

Topical non-steroidal anti-inflammatory drugs (NSAIDs) decrease pain from corneal abrasion. Available ocular NSAIDs are diclofenac 0.1%, ketorolac 0.5%, nepafenac... 

Celecoxib, a non-steroidal anti-inflammatory drug, is a cyclo-oxygenase-2 selective inhibitor that is as effective as diclofenac and naproxen. It should be used for the shortest period required to control symptoms. Use is associated v/ith an increased risk of thrombotic events and the cyclo-oxygenase-2 selective inhibitors are contraindicated in cerebrovascular disease. Mobic is the proprietary preparation of meloxicam. 

Concomitant administration of methotrexate and Voltarol, a proprietary preparation of diclofenac, a non-steroidal anti-inflammatory drug, may result in accumulation of methotrexate as its excretion is reduced. The use of diclofenac and diuretics such as bendroflumethiazide may increase the risk of nephrotoxicity. Concomitant use of alcohol and an angiotensin-converting enzyme inhibitor such as lisinopril (Zestril) may result in an enhanced hypotensive effect. Alcohol and the benzodiazepine diazepam (Valium) may result in enhanced sedation. 

Diclofenac is a non-steroidal anti-inflammatory drug. NSAIDs interact with both angiotensin-converting enzyme inhibitors, such as enalapril, and beta-adrenoceptor blockers, such as atenolol, resulting in antagonism to the hypotensive reaction, leading to a hypertensive reaction. NSAIDs interact with... 

Juvenile chronic arthritis is defined as a group of systemic inflammatory disorders affecting children below the age of 16 years. Pharmacotherapy is aimed to reduce pain and non-steroidal anti-inflammatory drugs are used. Ibuprofen is used at a dose of 30-40 mg/kg daily up to a maximum of 2.4 g. Other agents used include diclofenac at a dose of 1-3 mg/kg daily. 

The opioid analgesics, such os codeine, tramadol and fentanyl may cause drowsiness. Sumatriptan, which is a serotonin agonist, also tends to cause drowsiness. Modern non-steroidal anti-inflammatory drugs, such as diclofenac, do not cause drowsiness. 

Diclofenac (a non-steroidal anti-inflammatory drug) is marketed as Voltarol oral slow-release formulations. 

The first-line agents in the treatment of rheumatoid arthritis are non-steroidal anti-inflammatory drugs such as diclofenac. Diclofenac and indometacin, another NSAID, tend to have similar activity hov/ever, indometacin has a higher incidence of side-effects and therefore diclofenac is more appropriate for initial treatment. Sodium aurothiomalate is classified as a disease-modifying antirheumatic drug and is used as a second-line treatment in rheumatoid arthritis, but has been superseded by methotrexate, administered v/eekly. Paracetamol is often indicated in the management of osteoarthritis. Local intra-articular injections of dexamethasone may be administered for the relief of soft-tissue inflammatory conditions. 

Diclofenac is a phenylacetic acid derivative, non-steroidal anti-inflammatory drug. It is available as the potassium and sodium salts. Potassium salts are slightly more soluble than the sodium salts. Diclofenac can be used in breastfeeding mothers since the amount that passes through breast milk is too small to be harmful to the baby. However, diclofenac is contraindicated in pregnancy, especially during the last trimester. 

Diclofenac is available as dispersible tablets, tablets, gel, suppositories and for intravenous or intramuscular injection. The maximum dose of diclofenac administered via any route is 150 mg. As v/ith other non-steroidal anti-inflammatory drugs, concomitant use in patients receiving venlafaxine increases the risk of bleeding. 

Alternative products to diclofenac include naproxen and mefenamic acid, both of which are non-steroidal anti-inflammatory drugs. Co-codamol is a mixture of the opioid analgesic codeine and paracetamol and it does not possess the anti-inflammatory component. It may be used in pain management either where NSAIDs are contraindicated or in patients who are intolerant to the effects of NSAIDs. 

Some non-steroidal anti-inflammatory drugs (NSAIDs) were found to have the following capacity factors in a particular mobile on a reverse-phase column aspirin 0.4, naproxen 3.6, ibuprofen 14.5, diclofenac 10.4, paracetamol 0.2. Given that the column had a t of 2 min determine the retention times of the NSAIDs. 

The well known, beneficial influence of non-steroidal anti-inflammatory drugs (NSAID) on the progress of Alzheimer s disease has been confirmed for some NSAID subtypes. The work by Weggen et al. indicates the potential of COX 1 inhibitors (e.g. Diclofenac, Sulindac, Indomethacin, Ibuprofen, but not the most prominent, Aspirin) in PS inhibition [17]. 

ASA = aspirin NSAIDs = non-steroidal anti-inflammatory drugs, such as ibuprofen, naproxen, and diclofenac CNS stimulants include drugs such as pseudoephedrine, dextroamphetamine, theophylline, and caffeine MAO = monoamine oxidase CNS depressants include drugs such as benzodiazepines, barbiturates, and ethanol SSRIs = selective serotonin reuptake inhibitors, such as fluoxetine, sertraline, and paroxetine. Antidiabetic agents include drugs such as insulin, glipizide, glyburide, and metformin. 

The OAT proteins play a critical role in the excretion and detoxification of a wide variety of drugs, toxins, hormones and neurotransmitter metabolites. A number of common non-steroid anti-inflammatory drugs (NSAID), including acetyl salicylate and salicylate, acetaminophen, diclofenac, ibuprofen, ketoprofen, indomethacin, and naproxen, are substrates of one or more OAT isoforms, so that there can be significant interactions between NSAlDs and other drugs. The 3-lactam antibiotics (penicillins, cephalosporins and penems) and the antiviral nucleosides adefovir, cidofovir,... 

Some non-steroidal anti-inflammatory drugs (NSAIDs) are licensed for the prevention and treatment of post-operative pain. They may be inadequate for relief of very severe pain. Examples in use are diclofenac and ibuprofen. 

Diazepam - anxiolytic and hypnotic benzodiazepine premedication sedative Diclofenac - non-steroidal anti-inflammatory drug Diethylcarbamazine - anthelmintic... 

Takeuchi K, Abe K, Yasujima M, Sato M, Tanno M, Sato K, YoidtinagaK. No adverse effect of non-steroidal anti-inflammatory drugs, sulindac and diclofenac sodium, on blood pressure control with a calcium antagonist, nifedipine, in elderly hypertensive patients. TchokuJExp Med (1991) 165, 201-Z... 

The NIICRs to benzoic acid, cinnamic acid, cinnamic aldehyde, methyl nicotinate and diethyl fuma-rate can be inhibited by peroral acetylsalicylic acid and indomethacin (Lahti et al. 1983, 1987) and by a topical application of diclofenac or naproxen gels (Johansson and Lahti 1988). The duration of inhibition by a single dose of acetylsalicylic acid can be as long as 4 days (Kujala and Lahti 1989). The mechanism by which non-steroidal anti-inflammatory drugs inhibit NIICRs in human skin has not been defined, but it is probably ascribable to the inhibition of prostaglandin metabolism. 

Substituted propionic acid derivatives and related compounds form an important class of non-steroidal anti-inflammatory drugs, but most do not contain readily oxidisable groups. However, pirprofen and diclofenac (Figure 6.53) have been assayed by HPLC-ED. Diclofenac has been measured in plasma using an amino-propyl-modified silica column with acetonitrile-aq. perchloric acid (2.5 mmol L ) (35 + 65) as eluent after LLE into benzene. ED was at a GCE (+0.9 V vs Ag/AgCl). 4-(2,6-Dichloro-4-methoxyphenyl)aminophenylacetic acid was the internal standard. The LoD was 5 pgL (2mL sample). An alternative method for diclofenac in plasma and synovial fluid has been described. LLE into dichloro-methane was followed by analysis using an ODS-modified silica column with acetonitrile-aq. sodium acetate (50mmolL pH 3) (40 + 60) as eluent and ED... 

A number of anti-inflammatory drugs have now been tested for their therapeutic efficacy in AD. For example, the steroid prednisolone, which is lipophilic, has been administered to patients with AD for up to a year but the results were disappointing. The potent non-steroidal anti-inflammatories diclofenac and indomethacin have also been tested but shown to have minimal benefit with a high frequency of side effects. Perhaps these results are not surprising as it seems likely that the inhibition of COX will have little beneficial effect on the symptoms of AD once neuronal death has occurred, as seems likely in the clinical studies in which the patients were in the advanced... 

This chapter concentrates on some drug choices in acute rather than chronic pain, but the same principles can be used to determine the appropriateness of other types of analgesic. The drugs considered in this section are paracetamol, non-steroidal anti-inflammatories (NSAIDs specifically diclofenac, ibuprofen, indometacin, naproxen, sulindac and tenoxicam) and opioids (codeine, dihydrocodeine, morphine, pethidine and tramadol). Unless otherwise stated, all pharmacokinetic data originate from standard reference sources [1-5] and apply to adults only. 

A controlled release preparation of diclofenac sodium, a non-steroidal anti-inflammatory agent, was developed for transdennal administration. PVAl and PVAl/polyacrylic acid(PAA) alloy membranes were prepared from a solvent-casting technique using different PVAl/PAA v/v ratios. The release of the drug from the membrane was evaluated under in viti o conditions at pH 7.4. The delivery system provided linear release without time lag, burst effect and boundary layer resistance. The effects of such variables as film thickness and PVAl/PAA ratio on the permeation behaviour of the polymeric membranes are discussed. The optimal PVAl/PAA was found to be 50/ 50. 48 refs. 

Agata, M.,Abe, T and Kon, M.,19. Effect of topical diclofenac sodium, a non steroidal anti-inflamatory drug onvarious ocular inflammatory models in animals. Acta. Soc. Ophthalmol. Jap. 87 19. 

---