BRIEF REVIEW on NON-STEROIDAL ANTI-INFLAMMATORY DRUGS (Nsaids): a CLASS of ANTI-INFLAMMATORY and ANTIPYRETIC DRUGS Kiran S
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(ASIO-JPHMR) [ISSN: 2455-281X ISSN: 2455-281X Contents lists available at http://www.albertscience.com ASIO Journal of Pharmaceutical & Herbal Medicines Research (ASIO-JPHMR) Volume 5, Issue 1; 2019; 43-48 BRIEF REVIEW ON NON-STEROIDAL ANTI-INFLAMMATORY DRUGS (NSAIDs): A CLASS OF ANTI-INFLAMMATORY AND ANTIPYRETIC DRUGS Kiran S. Kadam†, S. S. Pekamwar Department of Pharmaceutical Chemistry, School Of Pharmacy, Swami Ramanand Teerth Marathwada University, Nanded- 431606, Maharashtra, India. ARTICLE INFO ABSTRACT Non-steroidal anti-inflammatory drugs are a well-known class of generic drugs, Review Article most of the times physicians suggest the Non-steroidal anti-inflammatory drugs Received: 30th May, 2019 acts as anti-inflammatory or antipyretic drugs. This study was performed to Accepted: 20th July, 2019 know all facts regarding these drugs and to provide a combined data for this Corresponding Author: class of drugs regarding its medicinal use, adverse drugs reactions, †Kiran S. Kadam contraindications, mode of action and structural activity relationship. This class M. Pharm. (Pharmaceutical chemistry) of drug is safe up to certain limit if the dose of the drug increase then the risk of School Of Pharmacy, SRTMU, side effects may also increase so this article is beneficial to know these all facts Nanded-431606, Maharashtra, India regarding this class of drugs for everyone. Contact number: 9960092374 E-mail: [email protected] Keywords: Non-steroidal Anti-inflammatory Drugs, Anti-inflammatory drugs, Generic drug, adverse drug reactions, Antipyretic. © www.albertscience.com, All Right Reserved. 1. INTRODUCTION these drugs as these drugs have no any effect on performance of the athletes it only work to relieve the A non-steroidal anti-inflammatory drug is a class of pain during continuous competitions. drugs that provide analgesic (pain-killing) The regular use of NSAIDs may provide some benefit to and antipyretic (fever reducing) effects and in higher athletes; however, athletes should be aware of the doses have anti-inflammatory effects. The name non- potential risks of Non-steroidal anti-inflammatory drugs steroidal itself indicates that these classes of drug is as mentioned in the adverse effects [3]. different than the steroids and have a broad range of other effects like eicosanoid-depressing, anti- MEDICAL USES [1- 4]: inflammatory action. The well-known examples of the NSAIDs are usually used for the treatment of acute or drugs from this class are ibuprofen, naproxen, all are chronic operative conditions where pain and mostly available on counter in every country. As inflammation are present. paracetamol has only little anti-inflammatory effect, it NSAIDs are generally used for the symptomatic relief of treats pain mainly by blocking COX-2 mostly in CNS but the conditions like; Osteoarthritis, Rheumatoid arthritis, not mostly in the rest of the body [1]. Mild-to-moderate pain due to inflammation and tissue Most of the NSAIDS are shows synthesis of injury, Lower back pain, Inflammatory arthropathies prostaglandins and thromboxane by blocking COX-1 and (e.g. spondylitis, psoriatic arthritis, reactive arthritis), COX-2. Tennis elbow, Headache, Migraine, Acute gout, Inhibition of COX-2 may produce the anti-inflammatory, Dysmenorrhea (menstrual pain) ,bone pain, analgesic and antipyretic effects and inhibition of COX-1 Postoperative pain, Muscle stiffness and pain due may results in gastrointestinal bleeding and ulcers [2]. to Parkinson's disease, pyrexia (fever), Ileus and renal The NSAID are very helpful for the athletes for colic etc. competing continuously in the competitions and anti- doping agencies also have no any objection on the use of DOI Link :: http://doi-ds.org/doilink/10.2016-19146535/ ; DOI Link :: http://doi-ds.org/doilink/07.2019-68375121/ 43 Kiran S. Kadama et al. / ASIO Journal of Pharmaceutical & Herbal Medicines Research (ASIO-JPHMR), 5(1), 43-48 Persons who have had past GI problems from Most of the NSAIDs are well absorbed in the GIT and NSAID have high bioavailability. Are having high lipophilicity so people with the conditions Peptic ulcer or stomach mostly are given by oral route. Some drugs may show bleeding hepatic first-pass metabolism like diclofenac which give Uncontrolled hypertension rise to decrease the bioavailability. Some NSAIDs are Kidney disease prodrugs such as sulindac and parecoxib which require People that suffer with inflammatory bowel hepatic metabolism to convert into its active metabolites disease (Crohn's disease or ulcerative colitis) (Sulindac sulphide and valdecoxib). Past transient ischemic NSAIDs are highly plasma protein bound drugs attack (excluding ibuprofen) particularly bound with albumin. When given with other Past stroke (excluding ibuprofen) drugs the plasma protein displacement may observe Past myocardial infarction (excluding ibuprofen) such as with oral antidiabetic, anticancer drugs and Coronary artery disease (excluding ibuprofen) some anticoagulants. In this case the protein displacement may leads to the toxicity of the drug. The Undergoing coronary artery bypass surgery acidic functionality and the lipophilic residue of the Taking ibuprofen for heart NSAID tend it to bind with the plasma protein albumin. Congestive heart failure (excluding low-dose Metabolism of NSAIDs takes place in liver and excreted ibuprofen) out in urine. The half-life of various NSAID derivatives In third trimester of pregnancy are varies such as aspirin (0.25-0.3 hours) and Persons who have undergone gastric bypass piroxicam (45-50 hours). All these pharmacokinetics surgery parameters can be altered with aging. Persons who have a history of allergic or allergic- type NSAID hypersensitivity reactions, e.g. aspirin- USE OF NSAID IN POST-OPERATIVE PAIN [4, 5]: induced asthma. Recent studies have showed that the NSAID are used to relieve pain in post-operative conditions. In past studies ADVERSE EFFECTS OF NSAID [4-6]: it was observed that the arachidonic acid cascade Increase risk of GI-problems like bleeding in metabolites have role to mediate pain and inflammation intestine at the site of operation and surgery. NSAID are used to When used for pain management after surgery it treat the minor pain in the minor surgeries like dental may cause kidney damage surgeries and it was also used as adjuvant with analgesic Dyspepsia after major surgeries. Also described the role of Shows synergistic effect with many drugs which prostaglandins in the pain and inflammation and discuss may be fatal ex. NSAID with quinolone may results the effects of NSAID on post-operative pain and major into seizure surgical procedures and also their potential side effects. NSAID show their action by inhibiting COX enzyme Usually the general mechanism of pain as how exactly but this is nonselective and as COX and the pain sensation or inflammation occurs was shown in Prostaglandins are responsible for synthesis of this review. extracellular matrix that is collagen that gives Tissue injury may directly have mechanical and thermal strength to the muco-skeletal system, so indirectly damage to the nerve endings, to inflammation by the are responsible for increased injury risk resulting release of chemicals and hyper-algesia generated by due to reduces tissue adaptation or healing. algogenic, to inflammation and sprouting of damaged Also shows cardiac disorder and post-operative nerves into the injured tissues. After noxious stimuli to cardiovascular disorder. the peripheral nerves, androgenic impulses in axons Gastrointestinal toxicity: Dyspepsia Gastro promote the release of substance p from the nerve duodenal ulcers GI bleeding and perforation endings, resulting in vasodilation and increase in Cardiovascular adverse effects: Edema, vascular permeability and sensitization of nociceptors. Hypertension, Congestive heart failure, Myocardial infarction, Stroke and other Thrombotic events Due to this the local oedema and release of Nephrotoxicity: Electrolyte imbalance, Sodium prostaglandins, leukotriene, bradykinin, serotonin and retention, Edema, Reduce glomerular filtration histamine like androgenic substances leas o rate, Nephritic syndrome , Acute interstitial inflammation and hyperalgesia. Arachidonic acid can be nephritis, Renal papillary necrosis, Chronic kidney metabolized to the prostaglandin endoperoxides (PgE) disease by the enzyme COX or to hydroperoxy derivatives PHARMACOKINETICS [6, 7]: (HPETE) and leukotriene by thelipo-oxygenase pathway. Major action of NSAID is shown due to blocking of In this way NSAID inhibit the synthesis of Prostaglandins cyclooxygenase enzymes (COX-1 and COX-2) ultimately and inactivate the Cox enzyme to show its action. All inhibiting the prostaglandins synthesis. Their these events are shown in the figure below. pharmacokinetic activity ADME is given below- DOI Link :: http://doi-ds.org/doilink/10.2016-19146535/ ; DOI Link :: http://doi-ds.org/doilink/07.2019-68375121/ 44 Kiran S. Kadama et al. / ASIO Journal of Pharmaceutical & Herbal Medicines Research (ASIO-JPHMR), 5(1), 43-48 Fig. 1: General Mechanism of Pain Some other characteristics of NSAIDS are increasing in activity is it inhibit the COX (cyclooxygenase) enzyme. dose it only increases the side effects but not the On same side it is also used as anti-pyretic, analgesic and analgesic effect. uricosuric agents. Do not bring respiratory depression and any type of One of the powerful signalling agents from the body that physical or physiological dependence as opioids. is prostaglandins are biosynthesized