Analgesic and anti-inflammatory activity

At equipotent doses, the analgesic and anti-inflammatory activity of all NSAIDs and aspirin are similar. The selection of a specific NSAID should be based on tolerability, previous response, and cost. Some patients respond to one NSAID better than to another. If an insufficient response is achieved with one NSAID, another agent from the same or a different chemical class should be tried. Pain relief occurs rapidly (within hours), but antiinflammatory benefits are not realized until after 2 to 3 weeks of continuous therapy. This period is the minimal duration that should be considered an adequate NSAID trial. 

Ficarra R, Ficarra P, Tommasini S, et al. Leaf extracts of some Cordia species analgesic and anti-inflammatory activities as well as their chromatographic analysis. Farmaco 1995 50 245-256. 

SSR240612 is a new, potent, and orally active selective antagonist of Bi receptors in humans and several animal species. It exhibits analgesic and anti-inflammatory activities in mice and rats and is currently in preclinical development for the treatment of inflammatory and neurogenic pain. 

A new series of heterocyclic ethers were synthesized. The analgesic and anti-inflammatory activities of these compounds were comparable with the... 

Iwli et al [97] have reports based on the evaluation of plant-extract of D. multiradiata for antileishmanial activity using a mechanism-based radiorespirometric micro-technique. Extracts were found to be active at concentrations of 50 pg/ml or less against a visceral leishmania isolate. A number of Dorstenia species used traditionally as anti-snake venom were subjected to a pharmacological screening process and were found to possess analgesic and anti-inflammatory activities [98]. Many of the flavonoids isolated from African Dorstenia show moderate to good antioxidant activities [Croft, unpublished results]. The cytotoxic properties of... 

Hydrochlorides of dibenzazonines 14b, 106,107, and 108 have been tested by Pecherer and Brossi (29) for analgesic and anti-inflammatory activity, antiappetite and blood pressure effects, and activity against a series of infections. The alkaloid protostephanine (3) exerts a moderately strong and persistent hypotensive effect. Most of the other compounds show some central nervous activity. Independent studies have also found CNS activity for compounds 107, 109, and 110, all of which behave as hypotensive agents (30). 

Since its introduction in I96S. it has been widely used as an anti-inflammatuiy analgesic in RA. spondylitis, and OA. and to a lcs.scr extent in gout. Although both its analgesic and anti-inflammatory activities arc well established, it appears to be no more effective than aspirin. 

B. Aniline Derivatives - A structure-activity study of a new series of alkoxyaniline derivatives has been reported along with a detailed workup of one of them . This compound (XII) appears to have good analgesic and anti-inflammatory activity, associated with some CNS depressant effects. An antidiuretic effect was described for acetaminophen 9 a d it was suggested that this drug might be a useful substitute for vasopressin in certain patients with diabetes insipidus. Evidence was also presented to show that acetophenetidin has antipyretic activity which is not dependent on metabolism to N-acetyl-p-aminophenol. 

Ochna squarrosa L. (root bark) Lophirone A (351) lophirone L (217) lophirone H (322) calodenone (350). Used in Indian traditional systems of medicine. Analgesic and anti-inflammatory activities. Anuradha et al., 2006(306]. 

Ferulic acid, a phenolic compound of dong quai, was found to exert analgesic and anti-inflammatory activity in both the early and late phases of the inflammatory process in laboratory animals (Ozaki, 1992). The analgesic action is said to be 1.7 times greater than that of aspirin (Walker et al., 1998). Histamine-mediated inflammation is not affected by dong quai (Sung et al., 1982). 

Efficacy Analgesic and anti-inflammatory activity better than gold standard ... 

The pharmacological activities of two more compounds were later described. 5-/S-Diethylaminoethyl-3-a-phenylpropyl-l,2,4-oxadiazole citrate (AF634) seems to have an activity similar to that of oxolamine , but 5-diethylaminoethyl-3-jf)-methoxyphenyl-l, 2,4-oxadiazole (AF594, mexola-mine) seems, in the main, to possess analgesic and anti-inflammatory activities . ... 

Compound N—O N=C—R Antispasmodic activity in vitro) Local anaesthetic activity Analgesic and anti-inflammatory activity Anti-inflammatory activity Central anti-tussive activity ( ) Antitussive activity b)... 

Some of the most commonly and frequently used spices throughout the world are hot peppers of the Capsicum family, of which capsaicin 23 is the major pungent ingredient. Because of its analgesic and anti-inflammatory activities, topical application of capsaicin has been used for the treatment of a variety of neuropathic pain conditions. Autoradiographic visualization of a tritiated resiniferatoxin probe in tissues of various species identified the vanilloid receptor (VR) as a molecular target [73, 74]. Additionally, capsaicin was used as a molecular probe to isolate the first nociceptive receptor, VR1 [75], Characterization of VR1 revealed it to be a member of the Transient Receptor Potential (TRP) ion channel family and a nonselective cation channel activated by capsaicin or elevated temperatures. 

Vitamin K displays antibacterial and antimycotic properties, and it was demonstrated that it also has analgesic and anti-inflammatory activity. Studies of the influence of vitamin K on blood sugar levels are being continued because its presence in pancreas was observed it has been suggested that it may affect the insulin secretion. Other investigations have shown that vitamin K can be more powerful than vitamin E and coenzyme Qio in scavenging radicals (Malomi et al., 1993). 

Like lycorine (1), hemanthidine (55) has stronger analgesic and anti-inflammatory activity than aspirin (489,496), and vittatine has been found to potentiate the analgesic effect of morphine (60). Moreover, some alkaloids of this series, such as hemanthamine (53) or papiramine (48) have a hypotensive effect (41,498), and hemanthamine shows strong antiretroviral activity (483). 

The deepened understanding of the mode of action of Aspirin vfas an important prerequisite that in the following years a number of other natural products were discovered, which, like saUcyhc acid from willow bark (Cortex salix alba), exhibit analgesic and anti-inflammatory activity. 

For a complete description of the synthetic utility of the Houben-Hoesch reaction as it applies to other aromatic systems, as well as some mechanistic discussions, the reader is directed to two reviews on the subject. Due to the diminished electrophilic reactivity of nitriles compared to other carboxylic acid derivatives as well as the broad number of Friedel-Crafts substrates, most Houben-Hoesch pyrrole acylation reactions are conducted intramolecularly. However, an impressive intermolecular example was delineated by Chang and co-workers in efforts directed toward the synthesis of novel 2-[5-aroylpyrrolo]alkanoic acids, for evaluation of their potential analgesic and anti-inflammatory activities. Treatment of substituted pyrrole 4 and 3-cyanopyridine (5) with acid in dry chloroform resulted in the preparation of 6 in good yield. 

Six-membered heterocycles comprise an important class of bioactive heterocycles. They attract considerable interest by medicinal chanists because of their wide spectrum of therapeutic and pharmacological properties. They are recogiuzed for possessing antibacterial, antiviral, antitumor, antiplatelet aggregation, antihypertensive, analgesic, and anti-inflammatory activities (Matsuda and Hirao 1965 Hurst and Hull 1961 Bokaeva 1967 Kato 1984 Sadanandam et al. 1992 Kurono et al. 1987). 

Sayyah, M., G. Saroukhani, A. Peirovi, and M. KamaUnejad, 2003. Analgesic and anti-inflammatory activity of the leaf essential oil of Laurus nobilis Linn. Phytother. Res., 17(7) 733-736. 

Non-selective NSAIDs inhibit both COX isoforms. Celecoxib is an NSAID that exhibits antipyretic, analgesic, and anti-inflammatory activities. The mechanism of action of celecoxib is due to inhibition of prostaglandin synthesis via inhibition of COX-2. At therapeutic concentrations in humans, celecoxib does... 

Low molecular weight peptides (mol. wt. 1000-10,000) with analgesic and anti-inflammatory activities are descrihed in a Japanese patent. Two anti-inflammatory peptides (mol. wt. 257,000 and 19,(X)0) have also been isolated from Chinese almonds (peach kernels, Prunus persicd) ... 

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