Analgesic characteristics

This particular series of drugs represents a situation where the analysis suggests a possible mechanism of action. The chemicals to be discussed are a group of imidazolines, VIII, which were synthesized for their analgesic characteristics (13). 

Like the arylacetic acids the arylpropionic acid analogues also exhibit potent anti-inflammatory properties besides usual antipyretic and analgesic characteristics. A few examples of this category of compounds are discussed here, flurbiprofen ketoprofen indoprofen fenoprofen calcium. 

The drug is observed to minimise voluntary muscle spasm by a central effect. However, the indications for the citrate are considered usually as an adjunct for the relief of discomfort amalgamated with severe painful musculoskeletal conditions, which is not yet vividly understood, but that may be associated with the analgesic characteristics of the drug substance. It has been duly observed that it does not exert its action by relaxing directly the tense skeletal muscles in man. However, the observed peripheral atropine-like actions are relatively mild in nature. Importantly, it helps to minimise voluntary muscle spasm by virtue of its central inhibitory activity specifically on the cerebral motor areas of eourse, an apparent central effect very much identical to that of atropine. 

Some of these indazoles showed analgesic activity greater than that of aspirin and several possessed significant antiinflammatory action. Both properties were the most striking and characteristic ones of the series. In a few cases the authors isolated the corresponding indazolones (705) which were less active than (704) in terms of analgesic and antiinflammatory properties. 

The majority of analgesics can be classified as either central or peripheral on the basis of their mode of action. Structural characteristics usually follow the same divisions the former show some relation to the opioids while the latter can be recognized as NSAlD s. The triamino pyridine 17 is an analgesic which does not seem to belong stmcturally to either class. Reaction of substituted pyridine 13 (obtainable from 12 by nitration ) with benzylamine 14 leads to the product from replacement of the methoxyl group (15). The reaction probably proceeds by the addition elimination sequence characteristic of heterocyclic nucleophilic displacements. Reduction of the nitro group with Raney nickel gives triamine 16. Acylation of the product with ethyl chlorofor-mate produces flupirtine (17) [4]. 

Neuropathic pain is initiated or caused by a primary lesion in the peripheral or central nervous system. The causative agent may be trauma, nerve-invading cancer, herpes zoster, HIV, stroke, diabetes, alcohol or other toxic substances. Neuropathic pain is refractory to most analgesic drugs. Altered sodium channel activity is characteristics of neuropathic pain states. 

The analgesic alkaloid epibatidine (57) continues to receive much synthetic interest <96JOC4600, 96T11053, 96TL7845> and Tmdell has devised a novel approach to the synthesis of this alkaloid, the key step of which utilizes a [4 + 2] cycloaddition of methyl 3-bromopropiolate with A -Boc-pyrrole (55) to afford the 7-azabicyclo[2.2.1]heptane skeleton 56 characteristic of this alkaloid <96JOC7189>. 

AIA runs a characteristic clinical course [9]. It is more frequent in women than men, and is unusual in children, beginning in adulthood, on average at the age of 30 years. Rhinorrhea and nasal congestion are usually the first symptoms, subsequently complicated by polyposis. Asthma and aspirin hypersensitivity develop 2-15 years later. Once developed, aspirin intolerance remains through life, although sporadic disappearance of intolerance has been reported. Asthma, characterized by blood and nasal eosinophilia, rims a protracted course despite avoidance of analgesics. In about half the patients, the course of asthma is severe, necessitating use of systemic corticosteroids. 

Pain episodes usually can be managed at home. Hospitalized patients usually require parenteral analgesics. Analgesic options include opioids, nonsteroidal anti-inflammatory agents, and acetaminophen. The patient characteristics and severity of the crisis should determine the choice of agent and regimen. 

Dextromethorphan, contained in many nonprescription cough medicines, will produce a heavy psychedelic trip, but the nausea characteristic of the opiates may constitute a problem. Kosterlitz and Villareal (Eds.) AGONIST AND ANTAGONIST ACTIONS OF NARCOTIC ANALGESIC DRUGS (1972) and Braude et al. (Eds.) NARCOTIC ANTAGONISES (1973) are useful. 

The analgesic response to THC may be variable and appears to depend on personality characteristics of the subject (Raft et al. 1977). 

Every componnd of this series differs to a certain degree from the other in their qualitative, yet primarily quantitative characteristics. They all act on the CNS by causing moderate sedative and antiemetic effects, affecting thermoregulatory processes, skeletal muscle, endocrine system, and by potentiating action of analgesics. 

An alkaloid is a complex organic chemical substance found in plants, which characteristically combines nitrogen with other elements, has a bitter taste, and typically has some toxic, stimulant, analgesic effects. There are many different alkaloids, 30 of which are found in the opium plant. While morphine is the most important alkaloid in opium—for its natural narcotic qualities as well as providing the chemical structure for heroin—another alkaloid, codeine, is also sought after for its medicinal attributes. Other alkaloids include papaverine, narcotine, nicotine, atropine, cocaine, and mescaline. While the concentration of morphine in opium varies depending on where and how the plant is cultivated, it typically ranges from 3 percent to 20 percent. 

It is a clear, colourless liquid with a characteristic odour but a blue dye is added for distinction from chloroform. It is a potent analgesic with a rapid onset of action but muscular relaxation with this agent is inadequate. Induction and recovery are slow. 

Water-soluble Stable in solution Pain on IV injection Non-irritant on subcutaneous injection Painful on arterial injection No sequelae from arterial injection Low incidence of venous thrombosis Pharmacodynamic characteristics Rapid onset Cumulation Excitatory effects Respiratory complications Hypotension Tachycardia Analgesic... 

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