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The Use And Misuse Of Nonsteroidal Anti-inflammatory Drugs (nsaids)
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ANTIIMFLAMMATORY EFFECT OF ACETAMINOPHEN (PARACETAMOL)
Observational
studies suggest that acetaminophen, which is a very weak
antiinflammatory agent at the typical daily dose of 1000 mg, is
associated with a reduced incidence of gastrointestinal adverse effects
compared to tNSAIDs. At this dose, acetaminophen inhibits both
cyclooxygenases by about 50%. The ability of acetaminophen to inhibit
the enzyme is conditioned by the peroxide tone of the immediate
environment (Boutaud et al., 2002). This may partly explain the poor
antiinflammatory activity of acetaminophen, since sites of inflammation
usually contain increased concentrations of leukocyte-generated
peroxides.
NSAIDs find their chief clinical application as
antiinflammatory agents in the treatment of musculoskeletal disorders,
such as rheumatoid arthritis and osteoarthritis. In general, NSAIDs
provide only symptomatic relief from pain and inflammation associated
with the disease, do not arrest the progression of pathological injury
to tissue, and are not considered to be "disease-modifying"
anti-rheumatic drugs.
2. PAIN RELIEVE (ANALGESIC)
NSAIDs
usually are classified as mild analgesics. However, consideration of the
type of pain, as well as its intensity, is important in the assessment
of analgesic efficacy. NSAIDs are particularly effective when
inflammation has caused sensitization of pain receptors to normally
painless mechanical or chemical stimuli. Pain that accompanies
inflammation and tissue injury probably results from local stimulation
of pain fibers and enhanced pain sensitivity (hyperalgesia), in part a
consequence of increased excitability of central neurons in the spinal
cord.
Bradykinin, released from plasma kininogen, and cytokines,
such as TNF-a, IL-1, and IL-8, appear to be particularly important in
eliciting the pain of inflammation. These agents liberate prostaglandins
and probably other mediators that promote hyperalgesia. Neuropeptides,
such as substance P and calcitonin gene-related peptide (CGRP), also may
be involved in eliciting pain.
In general, NSAIDs do not affect either hyperalgesia or pain caused by the direct action of prostaglandins, consistent with the notion that the analgesic effects of these agents are due to inhibition of prostaglandin synthesis. However, relief of pain by these compounds may occur via mechanisms other than inhibition of prostaglandin synthesis, including antinociceptive effects at peripheral or central neurons (Burke et al, 2008)
When employed as analgesics, these drugs usually are effective only against pain of low-to-moderate intensity, such as dental pain. Although their maximal efficacy is generally much less than the opioids, NSAIDs lack the unwanted adverse effects of opiates in the CNS, including respiratory depression and the development of physical dependence. NSAIDs do not change the perception of sensory modalities other than pain. Chronic postoperative pain or pain arising from inflammation is controlled particularly well by NSAIDs, whereas pain arising from the hollow viscera usually is not relieved. An exception to this is menstrual pain. The release of prostaglandins by the endometrium during menstruation may cause severe cramps and other symptoms of primary dysmenorrhea; treatment of this condition with NSAIDs has met with considerable success (Marjoribanks et al., 2003).
3. FEVERISH CONDITION ( ANTIPYRETIC)
Regulation of body temperature requires a delicate balance between the production and loss of heat; the hypothalamus regulates the set point at which body temperature is maintained. This set point is elevated in fever, and NSAIDs promote its return to normal. These drugs do not influence body temperature when it is elevated by factors such as exercise or in response to ambient temperature.
Fever may reflect infection or result from tissue damage, inflammation, graft rejection, or malignancy. These conditions all enhance formation of cytokines such as IL-1b, IL-6, interferons, and TNF-a. The cytokines increase synthesis of PGE2 in circumventricular organs in and adjacent to the preoptic hypothalamic area; PGE2, in turn, increases cyclic AMP and triggers the hypothalamus to elevate body temperature by promoting an increase in heat generation and a decrease in heat loss. Aspirin and NSAIDs suppress this response by inhibiting PGE2 synthesis. Prostaglandins, especially PGE2, acting via its EP3 receptor, can produce fever when infused into the cerebral ventricles or when injected into the hypothalamus. As with pain, NSAIDs do not inhibit the fever caused by directly administered prostaglandins; rather they inhibit fever caused by agents that enhance the synthesis of IL-1 and other cytokines, which presumably cause fever, at least in part, by inducing the endogenous synthesis of prostaglandins.
NSAIDs reduce fever in most situations, but not the circadian variation in temperature or the rise in response to exercise or increased ambient temperature. Comparative analysis of the impact of NSAIDs and selective COX-2 inhibitors suggests that COX-2 is the dominant source of prostaglandins that mediate the rise in temperature evoked by bacterial LPS administration (McAdam et al., 1999). Debilitating disease may not respond adequately to full therapeutic doses of NSAIDs and may require aggressive therapy with second-line agents.
3. DUCTUS ARTERIOSUS
Prostaglandins also have been implicated in the maintenance of patency of the ductus arteriosus, and indomethacin and other tNSAIDs have been used in neonates to close the inappropriately patent ductus. Both COX-1 and COX-2 appear to participate in maintaining patency of the ductus arteriosus in fetal lambs (Clyman et al., 1999), while in mice COX-2 appears to play the dominant role (Loftin et al., 2002). It is not known which isoform(s) is involved in maintaining patency of the fetal ductus in utero in humans.
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ABSRACT - [ Total Page(s): 1 ]ABSTRACT COMING SOON ... Continue reading---
CHAPTER TWO - [ Total Page(s): 3 ]EXCLUSION CRITERIAAll pharmacists not practicing as community pharmacistsAll patent medicine vendors and outlets2.4 SAMPLE SIZE DETERMINATIONa. Retrospective review of prescriptions: All prescriptions from November 2013 and April 2014 were obtained from the Outpatient Pharmacy Department prescription bank. The prescriptions containing NSAIDs were separated from those without NSAIDs.b. Ilorin metropolis is made up of three local government areas: Ilorin West, Ilori ... Continue reading---
CHAPTER THREE - [ Total Page(s): 8 ]CHAPTER THREE RESULTS3.1 RESULTS OF ANALYSIS OF PRESCRIPTIONS/TREATMENT SHEETSOut of 1497 prescription sheets 1297 prescriptions contained NSAIDs with total of 1392 NSAIDs. The prescribing rate was hence found to be 86.6%. 7.3% of prescriptions contained more than one NSAIDs. ... Continue reading---
CHAPTER FOUR - [ Total Page(s): 2 ]CHAPTER FOURDISCUSSIONStudy of the Prescribing pattern of Nonsteroidal Antiinflammatory Drugs indicated more number of females assess health care for pain and related conditions than their male counterpart (Table 3.1), although there is widespread assumption that women will consult more readily for all symptoms or conditions and that men will be more reluctant or will delay consulting may result in health care providers assuming that women have a lower level of symptom severity before deciding ... Continue reading---
CHAPTER FIVE - [ Total Page(s): 1 ]CHAPTER FIVE CONCLUSIONThe prescribing rate of NSAIDs was high. The prevalence of NSAIDs misuse by residents was high Ibuprofen was the most highly misused among the residents. Dispensing pattern of NSAIDs by Pharmacists appeared to agree with the choice of medication use among residents. Educational status, occupation, prior knowledge of medication use and dispensing pattern of Pharmacists are factors that can influence public choice of NSAIDs use. ... Continue reading---
REFRENCES - [ Total Page(s): 5 ]Slater DM, Zervou S, Thornton S. (2002). Prostaglandins and prostanoid receptors in human pregnancy and parturition. J. Soc. Gynecol. Investig. 9:118-124.Soleymani F, Ahmadizar A and Abdollahi MA(2013). Survey on the factors influencing the pattern of medicine's use: Concerns on irrational use of drugs. J Res Pharm Pract. 2(2), 59–63.Solomon SD, McMurray JJ, Pfeffer MA, Wittes J, Fowler R, Finn P, Anderson WF, Zauber A, Hawk E, Bertagnolli M (2005). Cardiovascular risk associated with c ... Continue reading---
